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Plant Extracts: Biological and Pharmacological Activity—the Second Edition

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (30 October 2023) | Viewed by 129454

Special Issue Editors

Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Italy
Interests: pharmacology; natural products; neurotransmission; behavioral pharmacology; experimental pharmacology; preclinical pharmacology; CB1 receptor; PPARs; cannabinoids; endocannabinoids; CB2 receptor
Special Issues, Collections and Topics in MDPI journals
Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Pharmacology and Toxicology Section, University of Florence, 50139 Florence, Italy
Interests: pharmacology; medicinal plants; chronic pain; nervous system pathologies and treatment; glia; cholinergic receptors; opioid receptors
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Due to the success of the first edition of the Special Issue “Plant Extracts: Biological and Pharmacological Activity”, we have launched a second edition.

The use of plant extracts in therapy dates back many years. Plant extracts have been commonly used over the years to treat and prevent chronic and acute diseases and promote health. Although many plant extracts have been studied, many others have not. Therefore, a Special Issue on the pharmacology of plant extracts is timely.

This Special Issue aims to provide a comprehensive overview of the latest discoveries in plant extract products with an emphasis on pharmacological activity. We cordially invite authors to contribute original research articles, as well as reviews, that help to unravel the biological activities of naturally occurring products and create opportunities for their future use.

Prof. Dr. Raffaele Capasso
Dr. Lorenzo Di Cesare Mannelli
Guest Editors

Manuscript Submission Information

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Keywords

  • plant extracts
  • medicinal plants
  • biological activity
  • medical use
  • plant side effects
  • pharmacological interactions

Published Papers (49 papers)

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Research

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16 pages, 8743 KiB  
Article
Hexane Fraction of Adenophora triphylla var. japonica Root Extract Inhibits Angiogenesis and Endothelial Cell-Induced Erlotinib Resistance in Lung Cancer Cells
by Hyun-Ji Park, Jae-Hoon Jeong, Yung-Hyun Choi and Shin-Hyung Park
Molecules 2024, 29(3), 597; https://doi.org/10.3390/molecules29030597 - 25 Jan 2024
Viewed by 591
Abstract
The aim of this study was to investigate the anti-angiogenic effects of the hexane fraction of Adenophora triphylla var. japonica root extract (HAT) and its influence on the development of erlotinib resistance in human lung cancer cells. HAT significantly reduced the migration, invasion, [...] Read more.
The aim of this study was to investigate the anti-angiogenic effects of the hexane fraction of Adenophora triphylla var. japonica root extract (HAT) and its influence on the development of erlotinib resistance in human lung cancer cells. HAT significantly reduced the migration, invasion, and tube formation of human umbilical vein endothelial cells (HUVECs). The phosphorylation levels of vascular endothelial growth factor receptor 2 (VEGFR2) and its downstream molecules were decreased via HAT, indicating its anti-angiogenic potential in endothelial cells (ECs). A docking analysis demonstrated that β-sitosterol and lupeol, representative components of HAT, exhibit a high affinity for binding to VEGFR2. In addition, conditioned media from HAT-pretreated H1299 human lung cancer cells attenuated cancer-cell-induced chemotaxis of HUVECs, which was attributed to the decreased expression of angiogenic and chemotactic factors in H1299 cells. Interestingly, co-culture of erlotinib-sensitive PC9 human lung cancer cells with HUVECs induced erlotinib resistance in PC9 cells. However, co-culture with HAT-pretreated HUVECs partially restored the sensitivity of PC9 cells to erlotinib. HAT inhibited the development of erlotinib resistance by attenuating hepatocyte growth factor (HGF) production by ECs. Taken together, our results demonstrate that HAT exerts its anticancer effects by regulating the crosstalk between ECs and lung cancer cells. Full article
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18 pages, 3410 KiB  
Article
Discovery of Transfer Factors in Plant-Derived Proteins and an In Vitro Assessment of Their Immunological Activities
by Mesfin Yimam, Teresa Horm, Shengxin Cai, Alexandria O’Neal, Ping Jiao, Mei Hong, Thida Tea and Qi Jia
Molecules 2023, 28(24), 7961; https://doi.org/10.3390/molecules28247961 - 05 Dec 2023
Viewed by 903
Abstract
Repeated exposure to pathogens leads to evolutionary selection of adaptive traits. Many species transfer immunological memory to their offspring to counteract future immune challenges. Transfer factors such as those found in the colostrum are among the many mechanisms where transfer of immunologic memory [...] Read more.
Repeated exposure to pathogens leads to evolutionary selection of adaptive traits. Many species transfer immunological memory to their offspring to counteract future immune challenges. Transfer factors such as those found in the colostrum are among the many mechanisms where transfer of immunologic memory from one generation to the next can be achieved for an enhanced immune response. Here, a library of 100 plants with high protein contents was screened to find plant-based proteins that behave like a transfer factor moiety to boost human immunity. Aqueous extracts from candidate plants were tested in a human peripheral blood mononuclear cell (PBMC) cytotoxicity assay using human cancerous lymphoblast cells—with K562 cells as a target and natural killer cells as an effector. Plant extracts that caused PBMCs to exhibit enhanced killing beyond the capability of the colostrum-based transfer factor were considered hits. Primary screening yielded an 11% hit rate. The protein contents of these hits were tested via a Bradford assay and Coomassie-stained SDS-PAGE, where three extracts were confirmed to have high protein contents. Plants with high protein contents underwent C18 column fractionation using methanol gradients followed by membrane ultrafiltration to isolate protein fractions with molecular weights of <3 kDa, 3–30 kDa, and >30 kDa. It was found that the 3–30 kDa and >30 kDa fractions had high activity in the PBMC cytotoxicity assay. The 3–30 kDa ultrafiltrates from the top two hits, seeds from Raphanus sativus and Brassica juncea, were then selected for protein identification by mass spectrometry. The majority of the proteins in the fractions were found to be seed storage proteins, with a low abundance of proteins involved in plant defense and stress response. These findings suggest that Raphanus sativus or Brassica juncea extracts could be considered for further characterization and immune functional exploration with a possibility of supplemental use to bolster recipients’ immune response. Full article
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19 pages, 6184 KiB  
Article
The Hypotensive and Vasodilatory Effects Observed in Rats Exposed to Chiranthodendron pentadactylon Larreat Flowers Can Be Attributed to Cyanidin 3-O-Glucoside
by Juan Luis Escobar-Ramírez, Jacinto Santiago-Mejía, Maribel Soto-Núñez, Oscar Salvador Barrera-Vázquez, Roberto Vargas-Querea and Gil Alfonso Magos-Guerrero
Molecules 2023, 28(23), 7698; https://doi.org/10.3390/molecules28237698 - 22 Nov 2023
Viewed by 793
Abstract
Chiranthodendron pentadactylon Larreat is a tree native to southeastern Mexico and Guatemala. Its flower is used in Mexican folk medicine to treat a variety of diseases, including conditions of blood pressure. However, scientific information on its usefulness in this pathology is lacking. The [...] Read more.
Chiranthodendron pentadactylon Larreat is a tree native to southeastern Mexico and Guatemala. Its flower is used in Mexican folk medicine to treat a variety of diseases, including conditions of blood pressure. However, scientific information on its usefulness in this pathology is lacking. The present study evaluates the effect of a methanolic extract (ME) from the flower and its active constituents on heart rate (HR) and mean arterial pressure (MAP) in anesthetized rats (MAPHR). The study also analyzed the effects on rat-isolated aortic rings (RIAR) and the rat mesenteric arterial bed (MABR). Active fractions were chromatographed, which led to the isolation of cyanidin 3-O-glucoside (C3G) identified through HPLC. The Chiranthodendron pentadactylon flowers produced hypotensive and vasorelaxant effects associated with C3G. The vasorelaxant effect is a mechanism underlying the synthesis and release of nitric oxide (NO). Neither cholinergic receptors nor prostaglandins are involved. ME and C3G cause cardiovascular depression in anesthetized rats via cholinergic and prostanoid mechanisms. Our research expands the scientific understanding of the flowers on the rat cardiovascular system. This amplifies the appreciation of the flower’s ethnomedicine employed to control blood pressure. However, researchers need to conduct toxicity studies to determine the safety of this plant. Full article
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21 pages, 6357 KiB  
Article
A Study of Gentianae Radix et Rhizoma Class Differences Based on Chemical Composition and Core Efficacy
by Baixin Kou, Yuxin Jiang, Yanan Chen, Jingrong Yang, Jin Sun, Yan Yan, Lili Weng and Chunping Xiao
Molecules 2023, 28(20), 7132; https://doi.org/10.3390/molecules28207132 - 17 Oct 2023
Viewed by 863
Abstract
(1) Background: Establishment of a method for evaluating Gentianae Radix et Rhizoma (GRR) classes based on chemical composition and core efficacy; (2) Methods: Liquid chromatography–mass spectrometry (LC–MS) was used to determine the chemical constituents of GRR-first class (GF) and GRR-second class (GS). The [...] Read more.
(1) Background: Establishment of a method for evaluating Gentianae Radix et Rhizoma (GRR) classes based on chemical composition and core efficacy; (2) Methods: Liquid chromatography–mass spectrometry (LC–MS) was used to determine the chemical constituents of GRR-first class (GF) and GRR-second class (GS). The cell viability, liver function, oxidative stress enzyme activity, and inflammatory factor levels of GF and GS on H2O2-induced HepG2 cells were determined with CCK-8, ELISA, and biochemical methods, and the antioxidant activity of the two was evaluated using bioefficacy; ELISA, biochemical methods, real-time fluorescence quantitative polymerase chain reaction (RT-qPCR) method, and Western blot (WB) were used to determine the liver function, oxidative stress enzyme activity, inflammatory factor levels, and expression of related genes and proteins in mice with acute liver injury (ALI) model induced with 0.3% CCl4 olive oil solution after gavage administration; (3) Results: GF and GS had the same types of components, but the cyclic enol ether terpenes such as morinlon goside c, loganin, gentiopicroside, and swertiamarin differed significantly between the two; the effect of GF on CCl4-induced acute hepatic injury in C57BL/6 mice was stronger compared to GS. It helped alleviate weight loss, increase hepatic and splenic indices, improve hepatic lobular structure and hepatocyte status, inhibit collagen deposition, enhance oxidative stress and anti-inflammatory-related genes and protein expression, and decrease apoptotic genes and proteins more significantly than GS; (4) Conclusions: In this study, we established a GRR class evaluation method combining chemical composition and core medicinal effects, which can rapidly determine the differential composition of GF and GS, detect the quality of GRR through antioxidant bioefficacy, and validate it with in vivo experiments, which provides references for the evaluation of the class of GRR and the rational use of medication in the clinic. Full article
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23 pages, 8528 KiB  
Article
Artemisinin Confers Neuroprotection against 6-OHDA-Induced Neuronal Injury In Vitro and In Vivo through Activation of the ERK1/2 Pathway
by Qin Li, Shuai Li, Jiankang Fang, Chao Yang, Xia Zhao, Qing Wang, Wenshu Zhou and Wenhua Zheng
Molecules 2023, 28(14), 5527; https://doi.org/10.3390/molecules28145527 - 20 Jul 2023
Viewed by 1418
Abstract
Parkinson’s disease (PD) is an age-related, progressive neurodegenerative disease characterized by the gradual and massive loss of dopaminergic neurons in the substantia nigra pars compacta (SNc). We have recently reported that artemisinin, an FDA-approved first-line antimalarial drug, possesses a neuroprotective effect. However, the [...] Read more.
Parkinson’s disease (PD) is an age-related, progressive neurodegenerative disease characterized by the gradual and massive loss of dopaminergic neurons in the substantia nigra pars compacta (SNc). We have recently reported that artemisinin, an FDA-approved first-line antimalarial drug, possesses a neuroprotective effect. However, the effects and underlying mechanisms of artemisinin on Parkinson’s disease remain to be elucidated. In this study, we investigated the neuroprotective effects of artemisinin on 6-OHDA and MPP+ in neuronal cells and animal models, as well as the underlying mechanisms. Our results showed that artemisinin significantly attenuated the loss of cell viability, LDH release, elevated levels of reactive oxygen species (ROS), the collapse of the mitochondria trans-membrane potential and cell apoptosis in PC12 cells. Western blot results showed that artemisinin stimulated the phosphorylation of ERK1/2, its upstream signaling proteins c-Raf and MEK and its downstream target CREB in PC12 cells in a time- and concentration-dependent manner. In addition, the protective effect of artemisinin was significantly reduced when the ERK pathway was blocked using the ERK pathway inhibitor PD98059 or when the expression of ERK was knocked down using sgRNA. These results indicate the essential role of ERK in the protective effect of artemisinin. Similar results were obtained in SH-SY5Y cells and primary cultured neurons treated with 6-OHDA, as well as in cellular models of MPP+ injury. More interestingly, artemisinin attenuated PD-like behavior deficit in mice injected with 6-OHDA evaluated by behavioral tests including swimming test, pole-test, open field exploration and rotarod tests. Moreover, artemisinin also stimulated the phosphorylation of ERK1/2, inhibited apoptosis, and rescued dopaminergic neurons in SNc of these animals. Application of ERK pathway inhibitor PD98059 blocked the protective effect of artemisinin in mice during testing. Taking these results together, it was indicated that artemisinin preserves neuroprotective effects against 6-OHDA and MPP+ induced injury both in vitro and in vivo by the stimulation of the ERK1/2 signaling pathway. Our findings support the potential therapeutic effect of artemisinin in the prevention and treatment of Parkinson’s disease. Full article
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12 pages, 826 KiB  
Article
Biomolecular Screening of Pimpinella anisum L. for Antioxidant and Anticholinesterase Activity in Mice Brain
by Aamir Mushtaq, Fatima Habib, Rosana Manea, Rukhsana Anwar, Umar Farooq Gohar, Muhammad Zia-Ul-Haq, Mobasher Ahmad, Claudia Mihaela Gavris and Liana Chicea
Molecules 2023, 28(5), 2217; https://doi.org/10.3390/molecules28052217 - 27 Feb 2023
Viewed by 1076
Abstract
Hundreds of the plants have been explored and evaluated for antioxidant and anti-amnesic activities, so far. This study was designed to report the biomolecules of Pimpinella anisum L. for the said activities. The aqueous extract of dried P. anisum seeds was fractionated via [...] Read more.
Hundreds of the plants have been explored and evaluated for antioxidant and anti-amnesic activities, so far. This study was designed to report the biomolecules of Pimpinella anisum L. for the said activities. The aqueous extract of dried P. anisum seeds was fractionated via column chromatography and the fractions so obtained were assessed for the inhibition of acetylcholinesterase (AChE) via in vitro analysis. The fraction which best inhibited AChE was so named as the P. anisum active fraction (P.aAF). The P.aAF was then chemically analyzed via GCMS, which indicated that oxadiazole compounds were present in it. The P.aAF was then administered to albino mice to conduct the in vivo (behavioral and biochemical) studies. The results of the behavioral studies indicated the significant (p < 0.001) increase in inflexion ratio, by the number of hole-pokings through holes and time spent in a dark area by P.aAF treated mice. Biochemical studies demonstrated that the oxadiazole present in P.aAF on one hand presented a noteworthy reduction in MDA and the AChE level and on the other hand promoted the levels of CAT, SOD and GSH in mice brain. The LD50 for P.aAF was calculated as 95 mg/Kg/p.o. The findings thus supported that the antioxidant and anticholinesterase activities of P. anisum are due to its oxadiazole compounds. Full article
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13 pages, 2370 KiB  
Article
Extraction and Quantification of Azelaic Acid from Different Wheat Samples (Triticum durum Desf.) and Evaluation of Their Antimicrobial and Antioxidant Activities
by Chiara Spaggiari, Giannamaria Annunziato, Costanza Spadini, Sabrina Lucia Montanaro, Mattia Iannarelli, Clotilde Silvia Cabassi and Gabriele Costantino
Molecules 2023, 28(5), 2134; https://doi.org/10.3390/molecules28052134 - 24 Feb 2023
Cited by 3 | Viewed by 2158
Abstract
Azelaic Acid (AzA) is a 9-carbon atom dicarboxylic acid, with numerous pharmacological uses in dermatology. Its effectiveness in papulopustular rosacea and acne vulgaris, among other dermatological disorders such as keratinization and hyper-pigmentation, is thought to be related to its anti-inflammatory and antimicrobial properties. [...] Read more.
Azelaic Acid (AzA) is a 9-carbon atom dicarboxylic acid, with numerous pharmacological uses in dermatology. Its effectiveness in papulopustular rosacea and acne vulgaris, among other dermatological disorders such as keratinization and hyper-pigmentation, is thought to be related to its anti-inflammatory and antimicrobial properties. It is a by-product of Pityrosporum fungal mycelia metabolism but also it is found in different cereals such as barley, wheat, and rye. Diverse topical formulations of AzA exist in commerce, and it is mainly produced via chemical synthesis. In this study we describe the extraction of AzA from whole grains and whole-grain flour (Triticum durum Desf.) through green methods. Seventeen different extracts were prepared and analyzed for their AzA content by HPLC-MS methods and then screened for their antioxidant activity using spectrophotometric assays (ABTS, DPPH, and Folin–Ciocalteu). Minimum-inhibitory-concentration (MIC) assays against several bacterial and fungal pathogens were performed, to validate their antimicrobial activity. The obtained results indicate that whole grain extracts provide a wider spectrum of activity than the flour matrix; in particular, the Naviglio® extract showed higher AzA content, while the hydroalcoholic ultrasound-assisted extract provided better antimicrobial and antioxidant activity. The data analysis was performed using principal component analysis (PCA), as an unsupervised-pattern-recognition technique, to extract useful analytical and biological information. Full article
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19 pages, 26307 KiB  
Article
Examining the Effect of Notocactus ottonis Cold Vacuum Isolated Plant Cell Extract on Hair Growth in C57BL/6 Mice Using a Combination of Physiological and OMICS Analyses
by Junko Shibato, Fumiko Takenoya, Ai Kimura, Cheol Woo Min, Michio Yamashita, Ravi Gupta, Sun Tae Kim, Randeep Rakwal and Seiji Shioda
Molecules 2023, 28(4), 1565; https://doi.org/10.3390/molecules28041565 - 06 Feb 2023
Viewed by 1748
Abstract
The biological and psychological importance of hair is recognized worldwide. Molecules that can promote the activation of hair follicle stem cells and the initiation of the growth phase have been subjects of research. Clarifying how hair regeneration is regulated may help to provide [...] Read more.
The biological and psychological importance of hair is recognized worldwide. Molecules that can promote the activation of hair follicle stem cells and the initiation of the growth phase have been subjects of research. Clarifying how hair regeneration is regulated may help to provide hair loss treatments, including cosmetic and even psychological interventions. We examined the hair-growing effects of a cell extract (CE) obtained from cactus Notocactus ottonis by the cold vacuum extraction protocol, by investigating its hair-growing effects, relevant mechanisms, and potential factors therein. Using male C57BL/6 mice, vehicle control (VC: propylene glycol: ethanol: water), MXD (minoxidil, positive control), and N. ottonis CE (N-CE, experimental) were applied topically to the backs of mice. The results showed that MXD and N-CE were more effective in promoting hair growth than VC. An increase in number of hair follicles was observed with N-CE in hematoxylin-eosin-stained skin tissue. The metabolite composition of N-CE revealed the presence of growth-promoting factors. Using mouse back whole-skin tissue samples, whole-genome DNA microarray (4 × 44 K, Agilent) and proteomics (TMT-based liquid chromatography-tandem mass spectrometry) analyses were carried out, suggesting the molecular factors underlying hair-promoting effects of N-CE. This study raises the possibility of using the newly described N. ottonis CE as a hair-growth-promoting agent. Full article
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15 pages, 3773 KiB  
Article
Protective Effects of Sophorae tonkinensis Gagnep. (Fabaceae) Radix et Rhizoma Water Extract on Carbon Tetrachloride-Induced Acute Liver Injury
by Congcong Zhou, Aijing Liu, Gengsong Liu, Cheng Yang, Qiaoyan Zhou, Haizhu Li, Hongchun Yang, Mengmeng Yang, Gonghe Li, Hongbin Si and Changbo Ou
Molecules 2022, 27(24), 8650; https://doi.org/10.3390/molecules27248650 - 07 Dec 2022
Cited by 2 | Viewed by 1453
Abstract
Sophorae tonkinensis Radix et Rhizoma (STR) is a traditional Chinese herbal medicine. STR can reduce aminotransferase activity; however, the specific mechanism remains unclear. Here, we explored the potential therapeutic effects and hepatoprotective mechanism of STR on liver damage in mice. The chemical characteristics [...] Read more.
Sophorae tonkinensis Radix et Rhizoma (STR) is a traditional Chinese herbal medicine. STR can reduce aminotransferase activity; however, the specific mechanism remains unclear. Here, we explored the potential therapeutic effects and hepatoprotective mechanism of STR on liver damage in mice. The chemical characteristics of the extract were characterized using ultra-high-performance liquid chromatography-tandem mass spectrometry fingerprinting, and its antioxidant capacity was verified using free radical scavenging tests. Forty-eight Kunming mice were randomly assigned into six groups. The model was made after the corresponding drug was given. The results showed that the STR water extract pretreatment significantly reduced serum aminotransferase and related liver function indicators compared with that in the model group. Furthermore, the STR water extract pretreatment significantly inhibited the apoptosis of liver cells, the level of liver high-mobility group box 1 (HMGB1), and inflammatory factors in hepatic tissue compared with that in the model group, and significantly downregulated the levels of toll-like receptor 4 (TLR4), Myeloid differentiation factor 88 (MyD88), and nuclear factor kappa B (NF-κB) compared with those in the model group. Overall, the STR water extract exerted a significant protective effect on CCL4-induced acute liver injury in this study, and the accurate active ingredients of the STR water extract will be explored in the near future. Full article
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16 pages, 3066 KiB  
Article
Lactobacillus paracasei HY7015 and Lycopus lucidus Turcz. Extract Promotes Human Dermal Papilla Cell Cytoprotective Effect and Hair Regrowth Rate in C57BL/6 Mice
by Hayera Lee, Hyeonji Kim, Ji-Hyun Kim, Soo-Dong Park, Jae-Jung Shim and Jeong-Lyoul Lee
Molecules 2022, 27(23), 8235; https://doi.org/10.3390/molecules27238235 - 25 Nov 2022
Cited by 2 | Viewed by 2008
Abstract
Hair loss is a disease that requires accurate diagnosis and type-specific medical treatment. Many hair loss treatments have some side effects, such as hormone-related effects, so there is a need for safe and effective hair loss treatment. In this study, we investigated the [...] Read more.
Hair loss is a disease that requires accurate diagnosis and type-specific medical treatment. Many hair loss treatments have some side effects, such as hormone-related effects, so there is a need for safe and effective hair loss treatment. In this study, we investigated the effects of Lactobacillus paracasei HY7015 (HY7015) and Lycopus lucidus Turcz. (LT) extract on hair regrowth and protection. In vitro experiments were conducted to assess the effects of HY7015 and/or LT extract on human follicle dermal papilla cells (HFDPC) of cytoprotective functions such as proliferations, antioxidants, anti-inflammatory, and growth factor expressions. In animal experiments, we investigated hair regrowth rate, hair follicle formation and secretion of growth factors in telogenic C57BL/6 mice. We confirmed the cytoprotective effects of HY7015 and LT through regulations of proliferation, SOD and IL-1β in HFDPC. In mouse experiments, oral administration of HY7015 and LT promoted hair regrowth as well as hair follicle maturation in the dermal skin of C57BL/6 mice, and upregulated VEGF and IGF-1 growth factor levels in mouse serum. In summary, our data demonstrate that ingestions of HY7015 and LT can promote hair regrowth by enhancing cytoprotective effects and expressions of growth factors. Full article
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13 pages, 2627 KiB  
Article
Inhibitory Effects of Selected Medicinal Plants on Bacterial Growth of Methicillin-Resistant Staphylococcus aureus
by In-Geun Jung, Jae-Young Jeong, Seung-Hoon Yum and You-Jin Hwang
Molecules 2022, 27(22), 7780; https://doi.org/10.3390/molecules27227780 - 11 Nov 2022
Cited by 9 | Viewed by 2077
Abstract
Methicillin-resistant Staphylococcus aureus (MRSA) is a serious threat to global public health due to its capacity of tolerate conventional antibiotics. Medicinal plants are traditionally used to treat infectious diseases caused by bacterial pathogens. In the present study, 16 medicinal plants were screened for [...] Read more.
Methicillin-resistant Staphylococcus aureus (MRSA) is a serious threat to global public health due to its capacity of tolerate conventional antibiotics. Medicinal plants are traditionally used to treat infectious diseases caused by bacterial pathogens. In the present study, 16 medicinal plants were screened for antibacterial activities to preselect more effective species. Ethanol extracts of selected medicinal plants (Caesalpinia sappan L., Glycyrrhiza uralensis Fisch., Sanguisorba officinalis L., and Uncaria gambir Roxb) were partitioned successively with different solvents (n-hexane, chloroform, ethyl acetate, 1-butanol, and water). Disc diffusion assay and broth microdilution were performed to evaluate the antibacterial activities of plant extracts and fractions against Staphylococcus aureus strains. Furthermore, the cytotoxicity of the extracts and fractions was determined against the human hepatoma (HepG2) and human lung carcinoma (A549) cell lines using a trypan blue exclusion method. A few extracts and fractions showed significant inhibitory effects on the bacterial growth of all tested strains, including multidrug-resistance (MDR) clinical isolates. The ethyl acetate fraction of C. sappan had the most potent effects with minimum inhibitory/bactericidal concentrations (MIC/MBC) of 31.2/62.5 μg/mL and showed low cytotoxicity with over 90% cell viability in both cells. Our results suggest that medicinal plants have considerable potential as alternatives to conventional antibiotics. Full article
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17 pages, 2644 KiB  
Article
Pharmacological Validation for the Folklore Use of Ipomoea nil against Asthma: In Vivo and In Vitro Evaluation
by Taha Alqahtani, Sajida Parveen, Yahia Alghazwani, Hanan M. Alharbi, Reem M. Gahtani, Nadia Hussain, Kashif ur Rehman and Musaddique Hussain
Molecules 2022, 27(14), 4653; https://doi.org/10.3390/molecules27144653 - 21 Jul 2022
Cited by 3 | Viewed by 1648
Abstract
Oxidative stress is the key factor that strengthens free radical generation which stimulates lung inflammation. The aim was to explore antioxidant, bronchodilatory along with anti-asthmatic potential of folkloric plants and the aqueous methanolic crude extract of Ipomoea nil (In.Cr) seeds which [...] Read more.
Oxidative stress is the key factor that strengthens free radical generation which stimulates lung inflammation. The aim was to explore antioxidant, bronchodilatory along with anti-asthmatic potential of folkloric plants and the aqueous methanolic crude extract of Ipomoea nil (In.Cr) seeds which may demonstrate as more potent, economically affordable, having an improved antioxidant profile and providing evidence as exclusive therapeutic agents in respiratory pharmacology. In vitro antioxidant temperament was executed by DPPH, TFC, TPC and HPLC in addition to enzyme inhibition (cholinesterase) analysis; a bronchodilator assay on rabbit’s trachea as well as in vivo OVA-induced allergic asthmatic activity was performed on mice. In vitro analysis of 1,1-Diphenyl-2-picrylhydrazyl radical (DPPH) expressed as % inhibition 86.28 ± 0.25 with IC50 17.22 ± 0.56 mol/L, TPC 115.5 ± 1.02 mg GAE/g of dry sample, TFC 50.44 ± 1.06 mg QE/g dry weight of sample, inhibition in cholinesterase levels for acetyl and butyryl with IC50 (0.60 ± 0.67 and 1.5 ± 0.04 mol/L) in comparison with standard 0.06 ± 0.002 and 0.30 ± 0.003, respectively, while HPLC characterization of In.Cr confirmed the existence with identification as well as quantification of various polyphenolics and flavonoids i.e., gallic acid, vanillic acid, chlorogenic acid, quercetin, kaempferol and others. However, oral gavage of In.Cr at different doses in rabbits showed a better brochodilation profile as compared to carbachol and K+-induced bronchospasm. More significant (p < 0.01) reduction in OVA-induced allergic hyper-responses i.e., inflammatory cells grade, antibody IgE as well as altered IFN-α in airways were observed at three different doses of In.Cr. It can be concluded that sound mechanistic basis i.e., the existence of antioxidants: various phenolic and flavonoids, calcium antagonist(s) as well as enzymes’ inhibition profile, validates folkloric consumptions of this traditionally used plant to treat ailments of respiration. Full article
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14 pages, 23867 KiB  
Article
Antioxidant and Gastroprotective Activity of Suaeda fruticosa Forssk. Ex J.F.Gmel
by Afsheen Ayaz, QurratUlAin Jamil, Musaddique Hussain, Fayyaz Anjum, Adeel Sarfraz, Taha Alqahtani, Nadia Hussain, Reem M. Gahtani, Ayed A. Dera, Hanan M. Alharbi and Shahid M. Iqbal
Molecules 2022, 27(14), 4368; https://doi.org/10.3390/molecules27144368 - 07 Jul 2022
Cited by 6 | Viewed by 1681
Abstract
Suaeda fruticosa Forssk. Ex J.F.Gmel is traditionally used for inflammatory and digestive disorders, as a carminative, and for diarrhea. This plant is widely distributed in Asia, Africa, and the Mediterranean region. Aqueous methanolic extract of S. fruticosa (Sf.Cr) was prepared and screened for [...] Read more.
Suaeda fruticosa Forssk. Ex J.F.Gmel is traditionally used for inflammatory and digestive disorders, as a carminative, and for diarrhea. This plant is widely distributed in Asia, Africa, and the Mediterranean region. Aqueous methanolic extract of S. fruticosa (Sf.Cr) was prepared and screened for phytoconstituents through qualitative and GC-MS analysis. Quantification of total phenolic and flavonoid contents was performed, while antioxidant capacity was determined by DPPH, CUPRAC, FRAP, and ABTS assays. The gastroprotective activity was assessed in an ethanol-induced ulcer model. Gastric secretory parameters and macroscopic ulcerated lesions were analyzed and scored for ulcer severity. After scoring, histopathology was performed, and gastric mucus contents were determined. Oral pre-treatment of Sf.Cr demonstrated significant gastroprotection. The gastric ulcer severity score and ulcer index were reduced while the %-inhibition of ulcer was increased dose-dependently. The Sf.Cr significantly elevated the pH of gastric juice, while a decrease in total acidity and gastric juice volume was observed. Histopathology demonstrated less oedema and neutrophil infiltration in gastric mucosa of rats pre-treated with the Sf.Cr in comparison to ethanol-intoxicated animals. Furthermore, the gastric mucus contents were increased as determined by alcian blue binding. Sf.Cr showed marked gastroprotective activity, which can be attributed to antioxidant, antisecretory, and cytoprotective effects. Full article
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13 pages, 1362 KiB  
Article
Biochemical, Kinetic and Biological Properties of Group V Phospholipase A2 from Dromedary
by Mona Alonazi, Aida Karray, Raida Jallouli and Abir Ben Bacha
Molecules 2022, 27(11), 3437; https://doi.org/10.3390/molecules27113437 - 26 May 2022
Viewed by 1241
Abstract
Secretory group V phospholipase A2 (PLA2-V) is known to be involved in inflammatory processes in cellular studies, nevertheless, the biochemical and the enzymatic characteristics of this important enzyme have been unclear yet. We reported, as a first step towards understanding the [...] Read more.
Secretory group V phospholipase A2 (PLA2-V) is known to be involved in inflammatory processes in cellular studies, nevertheless, the biochemical and the enzymatic characteristics of this important enzyme have been unclear yet. We reported, as a first step towards understanding the biochemical properties, catalytic characteristics, antimicrobial and cytotoxic effects of this PLA2, the production of PLA2-V from dromedary. The obtained DrPLA2-V has an absolute requirement for Ca2+ and NaTDC for enzymatic activity with an optimum pH of 9 and temperature of 45 °C with phosphatidylethanolamine as a substrate. Kinetic parameters showed that Kcat/Kmapp is 2.6 ± 0.02 mM−1 s−1. The enzyme was found to display potent Gram-positive bactericidal activity (with IC50 values of about 5 µg/mL) and antifungal activity (with IC50 values of about 25 µg/mL)in vitro. However, the purified enzyme did not display a cytotoxic effect against cancer cells. Full article
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19 pages, 3908 KiB  
Article
Cardioprotective Effect of Rumex vesicarius Linn. Leaf Extract against Catecholamine-Induced Cardiotoxicity
by Imran Ahmad Khan, Musaddique Hussain, Nadia Hussain, Ali M. Alqahtani and Taha Alqahtani
Molecules 2022, 27(11), 3383; https://doi.org/10.3390/molecules27113383 - 24 May 2022
Cited by 8 | Viewed by 2042
Abstract
Rumex vesicarius (L.) is a folklore medicinal herb that has been used for centuries to cure cardiovascular diseases. The present work was carefully designed to ascertain the pharmacological basis for R. vesicarius’s therapeutic efficacy in cardiovascular diseases, as well as the underlying [...] Read more.
Rumex vesicarius (L.) is a folklore medicinal herb that has been used for centuries to cure cardiovascular diseases. The present work was carefully designed to ascertain the pharmacological basis for R. vesicarius’s therapeutic efficacy in cardiovascular diseases, as well as the underlying mechanism. In the ex vivo investigation, the aqueous-methanolic leaf extract of R. vesicarius was shown to have endothelium-dependent vasorelaxant effects in rabbit aorta tissue preparations, and its hypotensive responses were quantified by pressure and force transducers coupled to the Power Lab Data Acquisition System. Furthermore, when rabbits were subjected to adrenaline-induced myocardial infarction, R. vesicarius demonstrated cardioprotective characteristics. In contrast to the intoxicated group, the myocardial infarction model showed lower ALP, CK-MB, CRP, LDH, ALT, troponin, and AST levels (p > 0.005–0.000), as well as edema, necrosis, apoptosis, inflammatory cell enrolment, and necrosis. R. vesicarius exhibited significant antioxidant activity and delayed noradrenaline-induced platelet aggregation. Its cardioprotective, anticoagulant, and vasorelaxant properties in both investigations (in vivo and ex vivo) are mediated through partial endothelium-dependent, NO and calcium channel blockade mediated vasorelaxation. The minimizing of adrenaline, oxidative stress, and tissue damage demonstrate its therapeutic efficacy in cardiovascular diseases. Full article
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13 pages, 2298 KiB  
Article
Antimicrobial Activity of Green Silver Nanoparticles Synthesized by Different Extracts from the Leaves of Saudi Palm Tree (Phoenix Dactylifera L.)
by Jihan F. Al Mutairi, Fatimah Al-Otibi, Hassna M. Alhajri, Raedah I. Alharbi, Saud Alarifi and Seham S. Alterary
Molecules 2022, 27(10), 3113; https://doi.org/10.3390/molecules27103113 - 12 May 2022
Cited by 3 | Viewed by 1598
Abstract
The Arabian desert is rich in different species of medicinal plants, which approved variable antimicrobial activities. Phoenix dactylifera L. is one of the medical trees rich in phenolic acids and flavonoids. The current study aimed to assess the antibacterial and antifungal properties of [...] Read more.
The Arabian desert is rich in different species of medicinal plants, which approved variable antimicrobial activities. Phoenix dactylifera L. is one of the medical trees rich in phenolic acids and flavonoids. The current study aimed to assess the antibacterial and antifungal properties of the silver nanoparticles (AgNPs) green-synthesized by two preparations (ethanolic and water extracts) from palm leaves. The characteristics of the produced AgNPs were tested by UV-visible spectroscopy and Transmitted Electron Microscopy (TEM). The antifungal activity of Phoenix dactylifera L. was tested against different species of Candida. Moreover, its antibacterial activity was evaluated against two Gram-positive and two Gram-negative strains. The results showed that AgNPs had a spherical larger shape than the crude extracts. AgNPs, from both preparations, had significant antimicrobial effects. The water extract had slightly higher antimicrobial activity than the ethanolic extract, as it induced more inhibitory effects against all species. That suggests the possible use of palm leaf extracts against different pathogenic bacteria and fungi instead of chemical compounds, which had economic and health benefits. Full article
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18 pages, 20732 KiB  
Article
Lycopodium Mitigates Oxidative Stress and Inflammation in the Colonic Mucosa of Acetic Acid-Induced Colitis in Rats
by Salim M. A. Bastaki, Naheed Amir, Ernest Adeghate and Shreesh Ojha
Molecules 2022, 27(9), 2774; https://doi.org/10.3390/molecules27092774 - 26 Apr 2022
Cited by 7 | Viewed by 2626
Abstract
Inflammatory bowel diseases (IBDs) such as ulcerative colitis (UC) and Crohn’s disease (CD) are diseases of the gastrointestinal system involving genetic and environmental factors attributed to oxidative stress and inflammation. Targeting oxidative stress and inflammation by novel dietary compounds of natural origin convincingly [...] Read more.
Inflammatory bowel diseases (IBDs) such as ulcerative colitis (UC) and Crohn’s disease (CD) are diseases of the gastrointestinal system involving genetic and environmental factors attributed to oxidative stress and inflammation. Targeting oxidative stress and inflammation by novel dietary compounds of natural origin convincingly appears to be one of the important therapeutic strategies to keep the disease in remission. As there is no permanent cure for IBD except for chronic long-term treatment or surgery, it is therefore imperative to investigate plant-based agents that are receiving attention for their therapeutic benefits to overcome the debilitating clinical conditions of IBD. Lycopodium (LYCO), a plant of tropical and subtropical origin and known by numerous names such as ground pine, club moss, or devil’s claw, has been popularly used for centuries in traditional medicine including Chinese and Indian medicines. In the present study, the effect of LYCO has been investigated in an acetic acid (AA)-induced colitis model in Wistar rats. LYCO was orally administered at the dose of 50 mg/kg/day either 3 days before or 30 min after the induction of IBD and continued for 7 days by intrarectal administration of AA. The changes in body weight and macroscopic and microscopic analysis of the colon of rats of different experimental groups were observed on days 0, 2, 4, and 7. The levels of myeloperoxidase (MPO), reduced glutathione (GSH), and malondialdehyde (MDA) were measured. AA caused a significant reduction in body weight and increased macroscopic and microscopic ulcer scores along with a significant decline in antioxidant enzymes, superoxide dismutase (SOD), and catalase and antioxidant substrate, glutathione (GSH). There was a concomitant increased formation of malondialdehyde (MDA), a marker of lipid peroxidation, and raised myeloperoxidase (MPO) activity, a marker of neutrophil activation. Treatment with LYCO significantly improved IBD-induced reduction in body weight, improved histology, inhibited MDA formation, and restored antioxidants along with reduced MPO activity. AA also caused the release of proinflammatory cytokines such as interleukin-1β (IL-1β) and interleukin-23 (IL-23). Furthermore, AA also increased the levels of calprotectin, a protein released by neutrophils under inflammatory conditions of the gastrointestinal tract. LYCO treatment significantly reduced the release of calprotectin and proinflammatory cytokines. The results demonstrate that LYCO treatment has the potential to improve disease activity by inhibiting oxidative stress, lipid peroxidation, and inflammation along with histological preservation of colonic tissues. Full article
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14 pages, 4559 KiB  
Article
Korean Red Ginseng and Ginsenoside Rg3 Suppress Asian Sand Dust-Induced Epithelial–Mesenchymal Transition in Nasal Epithelial Cells
by Seung-Heon Shin, Mi-Kyung Ye, Dong-Won Lee, Mi-Hyun Chae and You-Jin Hwang
Molecules 2022, 27(9), 2642; https://doi.org/10.3390/molecules27092642 - 20 Apr 2022
Cited by 4 | Viewed by 1608
Abstract
Chronic rhinosinusitis (CRS) is characterized by chronic inflammation of the sinonasal mucosa with epithelial dedifferentiation toward the mesenchymal phenotype, known as the epithelial–mesenchymal transition (EMT). Asian sand dust (ASD) can induce nasal mucosal inflammation and cause the development of EMT. Korean red ginseng [...] Read more.
Chronic rhinosinusitis (CRS) is characterized by chronic inflammation of the sinonasal mucosa with epithelial dedifferentiation toward the mesenchymal phenotype, known as the epithelial–mesenchymal transition (EMT). Asian sand dust (ASD) can induce nasal mucosal inflammation and cause the development of EMT. Korean red ginseng (KRG) and ginsenoside Rg3 have been used as traditional herbal medicines to treat various diseases. The aim of this study was to investigate their effect on ASD-induced EMT in nasal epithelial cells. Primary nasal epithelial cells were incubated with ASD with or without KRG or Rg3, and the production of transforming growth factor-β1 (TGF-β1) and interleukin (IL)-8 was measured. EMT markers were determined by RT-PCR, Western blot analysis, and confocal microscopy, and transcription factor expression by Western blot analysis. The effect on cell migration was evaluated using the wound scratch assay. Results showed ASD-induced TGF-β1 production, downregulation of E-cadherin, and upregulation of fibronectin in nasal epithelial cells. KRG and Rg3 suppressed TGF-β1 production (31.7% to 43.1%), upregulated the expression of E-cadherin (26.4% to 88.3% in mRNA), and downregulated that of fibronectin (14.2% to 46.2% in mRNA and 52.3% to 70.2% in protein). In addition, they suppressed the ASD-induced phosphorylation of ERK, p38, and mTOR, as well as inhibiting the ASD-induced migration of nasal epithelial cells (25.2% to 41.5%). The results of this study demonstrate that KRG and Rg3 inhibit ASD-induced EMT by suppressing the activation of ERK, p38, and mTOR signaling pathways in nasal epithelial cells. Full article
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15 pages, 3886 KiB  
Article
The Root Extract of Peucedanum praeruptorum Dunn Exerts Anticancer Effects in Human Non-Small-Cell Lung Cancer Cells with Different EGFR Mutation Statuses by Suppressing MET Activity
by Hyun-Ji Park, Jae-Hoon Jeong and Shin-Hyung Park
Molecules 2022, 27(7), 2360; https://doi.org/10.3390/molecules27072360 - 06 Apr 2022
Cited by 6 | Viewed by 1997
Abstract
The aim of this study was to investigate the anticancer effects of the root extract of Peucedanum praeruptorum Dunn (EPP) in human non-small-cell lung cancer (NSCLC) cells and explore the mechanisms of action. We used four types of human lung cancer cell lines, [...] Read more.
The aim of this study was to investigate the anticancer effects of the root extract of Peucedanum praeruptorum Dunn (EPP) in human non-small-cell lung cancer (NSCLC) cells and explore the mechanisms of action. We used four types of human lung cancer cell lines, including H1299 (epidermal growth factor receptor (EGFR) wild-type), PC9 (EGFR Glu746-Ala750 deletion mutation in exon 19; EGFR tyrosine kinase inhibitor (TKI)-sensitive), H1975 (EGFR L858R/T790M double-mutant; EGFR TKI-resistant), and PC9/ER (erlotinib-resistant) cells. EPP suppressed cell growth and the colony formation of NSCLC cells in a concentration-dependent manner. EPP stimulated chromatin condensation, increased the percentage of sub-G1 phase cells, and enhanced the proportion of annexin V-positive cells, demonstrating that EPP triggered apoptosis in NSCLC cells regardless of the EGFR mutation and EGFR TKI resistance status. The phosphorylation level of the signal transducer and activator of transcription 3 (STAT3) and AKT was decreased by EPP. The expression of STAT3 target genes was also downregulated by EPP. EPP reversed hepatocyte growth factor (HGF)-induced MET phosphorylation and gefitinib resistance. Taken together, our results demonstrate that EPP exerted anticancer effects not only in EGFR TKI-sensitive NSCLC cells, but also in EGFR TKI-resistant NSCLC cells, by suppressing MET activity. Full article
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15 pages, 2391 KiB  
Article
Prokinetic and Laxative Effects of Chrozophora tinctoria Whole Plant Extract
by Ayaz Ali Sher, Arshad Iqbal, Naveed Muhammad, Syed Lal Badshah, Abdul-Hamid Emwas and Mariusz Jaremko
Molecules 2022, 27(7), 2143; https://doi.org/10.3390/molecules27072143 - 26 Mar 2022
Cited by 3 | Viewed by 2248
Abstract
Chrozophora tinctoria (Euphorbiaceae) has been used as an emetic, anthelminthic, and cathartic agent in traditional medicine. We used gas chromatography-mass spectrometry (GC-MS) to characterize the composition of ethyl acetate (EAC) and dichloromethane (DCMC) fractions from the whole Chrozophora tinctoria plant. EAC and DCMC [...] Read more.
Chrozophora tinctoria (Euphorbiaceae) has been used as an emetic, anthelminthic, and cathartic agent in traditional medicine. We used gas chromatography-mass spectrometry (GC-MS) to characterize the composition of ethyl acetate (EAC) and dichloromethane (DCMC) fractions from the whole Chrozophora tinctoria plant. EAC and DCMC fractions were evaluated for acetylcholinesterase (AChE) inhibitory activity and acute toxicity. Their effects on intestinal propulsive movement and spasmogenic activity of the gastrointestinal tract (GIT) muscle were also assessed. The compounds detected in both fractions were mostly fatty acids, with about seven compounds in EAC and 10 in DCMC. These included pharmacologically active compounds such as imipramine, used to treat depression, or hexadecanoic acid methyl ester, an antioxidant. Both EAC and DCMC fractions inhibited acetylcholinesterase (AChE) activity with IC50 values of 10 µg and 130 µg, respectively. Both the fractions were found to be toxic in a dose-dependent manner, inducing emesis at 0.5 g or higher and lethargy and mortality from 3–5 g upwards. Similarly, both of the fractions showed laxative activity in metronidazole- and loperamide-induced constipation models. EAC relaxed the intestinal muscle at a lower dose (1 mg/mL) than DCMC. Similarly, the EAC extract showed a significant relaxation effect (EC50 = 0.67 ± 0.15 mg/mL) on KCL-induced contraction in rabbit jejunum as compared to DCMC (EC50 = 5.04 ± 0.05 mg/kg). The present study strongly supports the folklore that this valuable plant is a cathartic agent. Further work is required to isolate and validate the bioactive compounds that act as diarrheal agents in Chrozophora tinctoria. Full article
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13 pages, 1009 KiB  
Article
Laser Light Treatment Improves the Mineral Composition, Essential Oil Production and Antimicrobial Activity of Mycorrhizal Treated Pelargoniumgraveolens
by Mohammad K. Okla, Samina Rubnawaz, Turki M. Dawoud, Saud Al-Amri, Mohamed A. El-Tayeb, Mostafa A. Abdel-Maksoud, Nosheen Akhtar, Ahlem Zrig, Gehad AbdElgayed and Hamada AbdElgawad
Molecules 2022, 27(6), 1752; https://doi.org/10.3390/molecules27061752 - 08 Mar 2022
Cited by 9 | Viewed by 1787
Abstract
Pelargonium graveolens, rose-scented geranium, is commonly used in the perfume industry. P. graveolens is enriched with essential oils, phenolics, flavonoids, which account for its tremendous biological activities. Laser light treatment and arbuscular mycorrhizal fungi (AMF) inoculation can further enhance the phytochemical content [...] Read more.
Pelargonium graveolens, rose-scented geranium, is commonly used in the perfume industry. P. graveolens is enriched with essential oils, phenolics, flavonoids, which account for its tremendous biological activities. Laser light treatment and arbuscular mycorrhizal fungi (AMF) inoculation can further enhance the phytochemical content in a significant manner. In this study, we aimed to explore the synergistic impact of these two factors on P. graveolens. For this, we used four groups of surface-sterilized seeds: (1) control group1 (non-irradiated; non-colonized group); (2) control group2 (mycorrhizal colonized group); (3) helium-neon (He-Ne) laser-irradiated group; (4) mycorrhizal colonization coupled with He-Ne laser-irradiation group. Treated seeds were growing in artificial soil inculcated with Rhizophagus irregularis MUCL 41833, in a climate-controlled chamber. After 6 weeks, P. graveolens plants were checked for their phytochemical content and antibacterial potential. Laser light application improved the mycorrhizal colonization in P. graveolens plants which subsequently increased biomass accumulation, minerals uptake, and biological value of P. graveolens. The increase in the biological value was evident by the increase in the essential oils production. The concomitant application of laser light and mycorrhizal colonization also boosted the antimicrobial activity of P. graveolens. These results suggest that AMF co-treatment with laser light could be used as a promising approach to enhance the metabolic content and yield of P. graveolens for industrial and pharmaceutical use. Full article
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23 pages, 4790 KiB  
Article
Polarity Directed Appraisal of Pharmacological Potential and HPLC-DAD Based Phytochemical Profiling of Polygonum glabrum Willd
by Tahira Sultana, Madiha Ahmed, Nosheen Akhtar, Mohammad K. Okla, Abdulrahman Al-Hashimi, Wahidah H. Al-Qahtani, Hamada Abdelgawad and Ihsan-ul-Haq
Molecules 2022, 27(2), 474; https://doi.org/10.3390/molecules27020474 - 12 Jan 2022
Cited by 2 | Viewed by 1398
Abstract
The present study was designed to evaluate polarity-dependent extraction efficiency and pharmacological profiling of Polygonum glabrum Willd. Crude extracts of leaves, roots, stems, and seeds, prepared from solvents of varying polarities, were subjected to phytochemical, antioxidant, antibacterial, antifungal, antidiabetic, and cytotoxicity assays. Maximum [...] Read more.
The present study was designed to evaluate polarity-dependent extraction efficiency and pharmacological profiling of Polygonum glabrum Willd. Crude extracts of leaves, roots, stems, and seeds, prepared from solvents of varying polarities, were subjected to phytochemical, antioxidant, antibacterial, antifungal, antidiabetic, and cytotoxicity assays. Maximum extraction yield (20.0% w/w) was observed in the case of an acetone:methanol (AC:M) root extract. Distilled water:methanol (W:M) leaves extract showed maximum phenolic contents. Maximum flavonoid content and free radical scavenging potential were found in methanolic (M) seed extract. HPLC-DAD quantification displayed the manifestation of substantial quantities of quercetin, rutin, gallic acid, quercetin, catechin, and kaempferol in various extracts. The highest ascorbic acid equivalent total antioxidant capacity and reducing power potential was found in distilled water roots and W:M leaf extracts, respectively. Chloroform (C) seeds extract produced a maximum zone of inhibition against Salmonella typhimurium. Promising protein kinase inhibition and antifungal activity against Mucor sp. were demonstrated by C leaf extract. AC:M leaves extract exhibited significant cytotoxic capability against brine shrimp larvae and α-amylase inhibition. Present results suggest that the nature of pharmacological responses depends upon the polarity of extraction solvents and parts of the plant used. P. glabrum can be considered as a potential candidate for the isolation of bioactive compounds with profound therapeutic importance. Full article
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16 pages, 2992 KiB  
Article
Pharmacological Justification for the Medicinal Use of Plumeria rubra Linn. in Cardiovascular Disorders
by Imran Ahmad Khan, Musaddique Hussain, Shahzada Khurram Syed, Malik Saadullah, Ali M. Alqahtani, Taha Alqahtani, Afaf A. Aldahish, Saeed Asiri and Ling-Hui Zeng
Molecules 2022, 27(1), 251; https://doi.org/10.3390/molecules27010251 - 31 Dec 2021
Cited by 9 | Viewed by 2235
Abstract
Plumeria rubra (L.) is a traditional folkloric medicinal herb used to treat cardiovascular disorders. The present investigation was methodically planned to investigate the pharmacological foundations for the therapeutic effectiveness of P. rubra in cardiovascular illnesses and its underlying mechanisms. Ex vivo vaso-relaxant effects [...] Read more.
Plumeria rubra (L.) is a traditional folkloric medicinal herb used to treat cardiovascular disorders. The present investigation was methodically planned to investigate the pharmacological foundations for the therapeutic effectiveness of P. rubra in cardiovascular illnesses and its underlying mechanisms. Ex vivo vaso-relaxant effects of crude leaf extract of P. rubra were observed in rabbit aorta ring preparations. Hypotensive effects were measured using pressure and force transducers connected to the Power Lab data acquisition system. Furthermore, P. rubra displayed cardioprotective properties in rabbits when they were exposed to adrenaline-induced myocardial infarction. In comparison to the intoxicated group, the myocardial infarction model showed decreased troponin levels, CK-MB, LDH, ALT, ALP, AST, and CRP, as well as necrosis, apoptosis, oedema, and inflammatory cell enrollment. P. rubra has revealed good antioxidant properties and prolonged the noradrenaline intoxicated platelet adhesion. Its anticoagulant, vasorelaxant, and cardioprotective effects in both in vivo and ex vivo investigations are enabled by blocking L-type calcium channels, lowering adrenaline, induced oxidative stress, and tissue tear, justifying its therapeutic utility in cardiovascular disorders. Full article
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14 pages, 2727 KiB  
Article
Assessment of Anti-Inflammatory and Antimicrobial Potential of Ethanolic Extract of Woodfordia fruticosa Flowers: GC-MS Analysis
by Agnieszka Najda, Aarti Bains, Prince Chawla, Anil Kumar, Sebastian Balant, Magdalena Walasek-Janusz, Dariusz Wach and Ravinder Kaushik
Molecules 2021, 26(23), 7193; https://doi.org/10.3390/molecules26237193 - 27 Nov 2021
Cited by 14 | Viewed by 2729
Abstract
Currently, the potential utilization of natural plant-derived extracts for medicinal and therapeutic purposes has increased remarkably. The current study, therefore, aimed to assess the antimicrobial and anti-inflammatory activity of modified solvent evaporation-assisted ethanolic extract of Woodfordia fruticosa flowers. For viable use of the [...] Read more.
Currently, the potential utilization of natural plant-derived extracts for medicinal and therapeutic purposes has increased remarkably. The current study, therefore, aimed to assess the antimicrobial and anti-inflammatory activity of modified solvent evaporation-assisted ethanolic extract of Woodfordia fruticosa flowers. For viable use of the extract, qualitative analysis of phytochemicals and their identification was carried out by gas chromatography–mass spectroscopy. Analysis revealed that phenolic (65.62 ± 0.05 mg/g), flavonoid (62.82 ± 0.07 mg/g), and ascorbic acid (52.46 ± 0.1 mg/g) components were present in high amounts, while β-carotene (62.92 ± 0.02 µg/mg) and lycopene (60.42 ± 0.8 µg/mg) were present in lower amounts. The antimicrobial proficiency of modified solvent-assisted extract was evaluated against four pathogenic bacterial and one fungal strain, namely Staphylococcusaureus (MTCC 3160), Klebsiellapneumoniae (MTCC 3384), Pseudomonasaeruginosa (MTCC 2295), and Salmonellatyphimurium (MTCC 1254), and Candidaalbicans (MTCC 183), respectively. The zone of inhibition was comparable to antibiotics streptomycin and amphotericin were used as a positive control for pathogenic bacterial and fungal strains. The extract showed significantly higher (p < 0.05) anti-inflammatory activity during the albumin denaturation assay (43.56–86.59%) and HRBC membrane stabilization assay (43.62–87.69%). The extract showed significantly (p < 0.05) higher DPPH (2,2-diphenyl-1-picrylhydrazyl) scavenging assay and the obtained results are comparable with BHA (butylated hydroxyanisole) and BHT (butylated hydroxytoluene) with percentage inhibitions of 82.46%, 83.34%, and 84.23%, respectively. Therefore, the obtained results concluded that ethanolic extract of Woodfordia fruticosa flowers could be utilized as a magnificent source of phenols used for the manufacturing of value-added food products. Full article
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13 pages, 3046 KiB  
Article
Ginsenoside Rb1 Mitigates Escherichia coli Lipopolysaccharide-Induced Endometritis through TLR4-Mediated NF-κB Pathway
by Aftab Shaukat, Irfan Shaukat, Shahid Ali Rajput, Rizwan Shukat, Sana Hanif, Imran Shaukat, Xinxin Zhang, Chao Chen, Xuyang Sun, Tingzhu Ye, Kaifeng Niu, Zhiqiu Yao, Shadab Shaukat, Muhammad Safdar, Mohamed Abdelrahman, Umair Riaz, Junwei Zhao, Xiaoying Gu and Liguo Yang
Molecules 2021, 26(23), 7089; https://doi.org/10.3390/molecules26237089 - 23 Nov 2021
Cited by 8 | Viewed by 2058
Abstract
Endometritis is the inflammatory response of the endometrial lining of the uterus and is associated with low conception rates, early embryonic mortality, and prolonged inter-calving intervals, and thus poses huge economic losses to the dairy industry worldwide. Ginsenoside Rb1 (GnRb1) is a natural [...] Read more.
Endometritis is the inflammatory response of the endometrial lining of the uterus and is associated with low conception rates, early embryonic mortality, and prolonged inter-calving intervals, and thus poses huge economic losses to the dairy industry worldwide. Ginsenoside Rb1 (GnRb1) is a natural compound obtained from the roots of Panax ginseng, having several pharmacological and biological properties. However, the anti-inflammatory properties of GnRb1 in lipopolysaccharide (LPS)-challenged endometritis through the TLR4-mediated NF-κB signaling pathway has not yet been researched. This study was planned to evaluate the mechanisms of how GnRb1 rescues LPS-induced endometritis. In the present research, histopathological findings revealed that GnRb1 ameliorated LPS-triggered uterine injury. The ELISA and RT-qPCR assay findings indicated that GnRb1 suppressed the expression level of pro-inflammatory molecules (TNF-α, IL-1β and IL-6) and boosted the level of anti-inflammatory (IL-10) cytokine. Furthermore, the molecular study suggested that GnRb1 attenuated TLR4-mediated NF-κB signaling. The results demonstrated the therapeutic efficacy of GnRb1 in the mouse model of LPS-triggered endometritis via the inhibition of the TLR4-associated NF-κB pathway. Taken together, this study provides a baseline for the protective effect of GnRb1 to treat endometritis in both humans and animals. Full article
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23 pages, 4400 KiB  
Article
Caragana rosea Turcz Methanol Extract Inhibits Lipopolysaccharide-Induced Inflammatory Responses by Suppressing the TLR4/NF-κB/IRF3 Signaling Pathways
by Ankita Mitra, Akash Ahuja, Laily Rahmawati, Han Gyung Kim, Byoung Young Woo, Yong Deog Hong, Mohammad Amjad Hossain, Zhiyun Zhang, Soo-Yong Kim, Jongsung Lee, Jong-Hoon Kim and Jae Youl Cho
Molecules 2021, 26(21), 6660; https://doi.org/10.3390/molecules26216660 - 03 Nov 2021
Cited by 4 | Viewed by 2394
Abstract
Caragana rosea Turcz, which belongs to the Leguminosae family, is a small shrub found in Northern and Eastern China that is known to possess anti-inflammatory properties and is used to treat fever, asthma, and cough. However, the underlying molecular mechanisms of its anti-inflammatory [...] Read more.
Caragana rosea Turcz, which belongs to the Leguminosae family, is a small shrub found in Northern and Eastern China that is known to possess anti-inflammatory properties and is used to treat fever, asthma, and cough. However, the underlying molecular mechanisms of its anti-inflammatory effects are unknown. Therefore, we used lipopolysaccharide (LPS) in RAW264.7 macrophages to investigate the molecular mechanisms that underlie the anti-inflammatory activities of a methanol extract of Caragana rosea (Cr-ME). We showed that Cr-ME reduced the production of nitric oxide (NO) and mRNA levels of iNOS, TNF-α, and IL-6 in a concentration-dependent manner. We also found that Cr-ME blocked MyD88- and TBK1-induced NF-κB and IRF3 promoter activity, suggesting that it affects multiple targets. Moreover, Cr-ME reduced the phosphorylation levels of IκBα, IKKα/β and IRF3 in a time-dependent manner and regulated the upstream NF-κB proteins Syk and Src, and the IRF3 protein TBK1. Upon overexpression of Src and TBK1, Cr-ME stimulation attenuated the phosphorylation of the NF-κB subunits p50 and p65 and IRF3 signaling. Together, our results suggest that the anti-inflammatory activity of Cr-ME occurs by inhibiting the NF-κB and IRF3 signaling pathways. Full article
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12 pages, 2530 KiB  
Article
Anti-Cancer Properties of Ginkgolic Acids in Human Nasopharyngeal Carcinoma CNE-2Z Cells via Inhibition of Heat Shock Protein 90
by Hong-Mei Li, Hui Ma, Xiaolong Sun, Bohan Li, Chengjiang Cao, Yiqun Dai, Meilin Zhu and Cheng-Zhu Wu
Molecules 2021, 26(21), 6575; https://doi.org/10.3390/molecules26216575 - 30 Oct 2021
Cited by 2 | Viewed by 1711
Abstract
Ginkgo biloba L. has been used in traditional Chinese medicine (TCM) for thousands of years. However, the anti-cancer properties of ginkgolic acids (GAS) isolated from G. biloba have not been investigated in human nasopharyngeal carcinoma cells. In this study, GAS exhibited an inhibitory [...] Read more.
Ginkgo biloba L. has been used in traditional Chinese medicine (TCM) for thousands of years. However, the anti-cancer properties of ginkgolic acids (GAS) isolated from G. biloba have not been investigated in human nasopharyngeal carcinoma cells. In this study, GAS exhibited an inhibitory effect on the ATPase activity of heat shock protein 90 (Hsp90) and anti-proliferative activities against four human cancer cell lines, with IC50 values ranging from 14.91 to 23.81 μg·mL−1. In vivo experiments confirmed that GAS inhibited tumor growth in CNE-2Z cell-xenografted nude mice with low hepatotoxicity. We further demonstrated that GAS suppressed migration and invasion and induced the apoptosis of CNE-2Z cells by inducing the degradation of Hsp90 client proteins (MMP-2, MMP-9, Her-2, c-Raf, Akt, and Bcl-2). Together, GAS are new Hsp90 inhibitors by binding to Hsp90 (hydrogen bond and hydrophobic interaction). Thus, GAS from G. biloba might represent promising Hsp90 inhibitors for the development of anti-nasopharyngeal carcinoma agents. Full article
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15 pages, 2735 KiB  
Article
Standardized Extract of Asparagus officinalis Stem Attenuates SARS-CoV-2 Spike Protein-Induced IL-6 and IL-1β Production by Suppressing p44/42 MAPK and Akt Phosphorylation in Murine Primary Macrophages
by Ken Shirato, Jun Takanari and Takako Kizaki
Molecules 2021, 26(20), 6189; https://doi.org/10.3390/molecules26206189 - 14 Oct 2021
Cited by 13 | Viewed by 3224
Abstract
Excessive host inflammation following infection with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is associated with severity and mortality in coronavirus disease 2019 (COVID-19). We recently reported that the SARS-CoV-2 spike protein S1 subunit (S1) induces pro-inflammatory responses by activating toll-like receptor 4 [...] Read more.
Excessive host inflammation following infection with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is associated with severity and mortality in coronavirus disease 2019 (COVID-19). We recently reported that the SARS-CoV-2 spike protein S1 subunit (S1) induces pro-inflammatory responses by activating toll-like receptor 4 (TLR4) signaling in macrophages. A standardized extract of Asparagus officinalis stem (EAS) is a unique functional food that elicits anti-photoaging effects by suppressing pro-inflammatory signaling in hydrogen peroxide and ultraviolet B-exposed skin fibroblasts. To elucidate its potential in preventing excessive inflammation in COVID-19, we examined the effects of EAS on pro-inflammatory responses in S1-stimulated macrophages. Murine peritoneal exudate macrophages were co-treated with EAS and S1. Concentrations and mRNA levels of pro-inflammatory cytokines were assessed using enzyme-linked immunosorbent assay and reverse transcription and real-time polymerase chain reaction, respectively. Expression and phosphorylation levels of signaling proteins were analyzed using western blotting and fluorescence immunomicroscopy. EAS significantly attenuated S1-induced secretion of interleukin (IL)-6 in a concentration-dependent manner without reducing cell viability. EAS also markedly suppressed the S1-induced transcription of IL-6 and IL-1β. However, among the TLR4 signaling proteins, EAS did not affect the degradation of inhibitor κBα, nuclear translocation of nuclear factor-κB p65 subunit, and phosphorylation of c-Jun N-terminal kinase p54 subunit after S1 exposure. In contrast, EAS significantly suppressed S1-induced phosphorylation of p44/42 mitogen-activated protein kinase (MAPK) and Akt. Attenuation of S1-induced transcription of IL-6 and IL-1β by the MAPK kinase inhibitor U0126 was greater than that by the Akt inhibitor perifosine, and the effects were potentiated by simultaneous treatment with both inhibitors. These results suggest that EAS attenuates S1-induced IL-6 and IL-1β production by suppressing p44/42 MAPK and Akt signaling in macrophages. Therefore, EAS may be beneficial in regulating excessive inflammation in patients with COVID-19. Full article
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13 pages, 5567 KiB  
Article
Anti-Herpes Simplex 1 Activity of Simmondsia chinensis (Jojoba) Wax
by Zipora Tietel, Sarit Melamed, Noy Eretz-Kdosha, Ami Guetta, Raanan Gvirtz, Navit Ogen-Shtern, Arnon Dag and Guy Cohen
Molecules 2021, 26(19), 6059; https://doi.org/10.3390/molecules26196059 - 07 Oct 2021
Cited by 6 | Viewed by 2391
Abstract
Jojoba (Simmondsia chinensis (Link) Schneider) wax is used for various dermatological and pharmaceutical applications. Several reports have previously shown beneficial properties of Jojoba wax and extracts, including antimicrobial activity. The current research aimed to elucidate the impact of Jojoba wax on skin [...] Read more.
Jojoba (Simmondsia chinensis (Link) Schneider) wax is used for various dermatological and pharmaceutical applications. Several reports have previously shown beneficial properties of Jojoba wax and extracts, including antimicrobial activity. The current research aimed to elucidate the impact of Jojoba wax on skin residential bacterial (Staphylococcus aureus and Staphylococcus epidermidis), fungal (Malassezia furfur), and virus infection (herpes simplex 1; HSV-1). First, the capacity of four commercial wax preparations to attenuate their growth was evaluated. The results suggest that the growth of Staphylococcus aureus, Staphylococcus epidermidis, and Malassezia furfur was unaffected by Jojoba in pharmacologically relevant concentrations. However, the wax significantly attenuated HSV-1 plaque formation. Next, a complete dose–response analysis of four different Jojoba varieties (Benzioni, Shiloah, Hatzerim, and Sheva) revealed a similar anti-viral effect with high potency (EC50 of 0.96 ± 0.4 µg/mL) that blocked HSV-1 plaque formation. The antiviral activity of the wax was also confirmed by real-time PCR, as well as viral protein expression by immunohistochemical staining. Chemical characterization of the fatty acid and fatty alcohol composition was performed, showing high similarity between the wax of the investigated varieties. Lastly, our results demonstrate that the observed effects are independent of simmondsin, repeatedly associated with the medicinal impact of Jojoba wax, and that Jojoba wax presence is required to gain protection against HSV-1 infection. Collectively, our results support the use of Jojoba wax against HSV-1 skin infections. Full article
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8 pages, 4655 KiB  
Article
Inhibitory Effect of Osthole from Cnidium monnieri (L.) Cusson on Fusarium oxysporum, a Common Fungal Pathogen of Potato
by Hongli Zheng, Yahan Chen, Qiuli Guo, Hong Wei, Jianying Yue, Hongyou Zhou and Mingmin Zhao
Molecules 2021, 26(13), 3818; https://doi.org/10.3390/molecules26133818 - 23 Jun 2021
Cited by 9 | Viewed by 2085
Abstract
Fusarium wilt of potato is one of the most common diseases of potato in China, and is becoming a serious threat in potato production. It has been reported that osthole from Cnidium monnieri (L.) Cusson can inhibit plant pathogens. Here, we [...] Read more.
Fusarium wilt of potato is one of the most common diseases of potato in China, and is becoming a serious threat in potato production. It has been reported that osthole from Cnidium monnieri (L.) Cusson can inhibit plant pathogens. Here, we test the anti-fungal activity of C. monnieri osthole against Fusarium oxysporum in potatoes. The results showed that at a concentration of 5 mg/mL, osthole was able to obviously inhibit mycelial growth of F. oxysporum. We found that osthole caused changes of mycelial morphology, notably hyphal swelling and darkening. Osthole significantly reduced the spore germination of Fusarium by 57.40%. In addition, osthole also inhibited the growth of other pathogens such as Fusarium moniliforme J. Sheld, Thanatephorus cucumeris Donk, and Alternaria alternata (Fr.) Keissl, but not Alternaria solani Jonesetgrout and Valsa mali Miyabe and G. Yamada. Our results suggest that osthole has considerable potential as an agent for the prevention and treatment of potato Fusarium wilt. Full article
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12 pages, 713 KiB  
Article
The Chemical Compositions, and Antibacterial and Antioxidant Activities of Four Types of Citrus Essential Oils
by Xiaocai Lin, Shan Cao, Jingyu Sun, Dongliang Lu, Balian Zhong and Jiong Chun
Molecules 2021, 26(11), 3412; https://doi.org/10.3390/molecules26113412 - 04 Jun 2021
Cited by 44 | Viewed by 4197
Abstract
Nanfeng mandarins (Citrus reticulata Blanco cv. Kinokuni), Xunwu mandarins (Citrus reticulata Blanco), Yangshuo kumquats (Citrus japonica Thunb) and physiologically dropped navel oranges (Citrus sinensis Osbeck cv. Newhall) were used as materials to extract peel essential oils (EOs) via hydrodistillation. [...] Read more.
Nanfeng mandarins (Citrus reticulata Blanco cv. Kinokuni), Xunwu mandarins (Citrus reticulata Blanco), Yangshuo kumquats (Citrus japonica Thunb) and physiologically dropped navel oranges (Citrus sinensis Osbeck cv. Newhall) were used as materials to extract peel essential oils (EOs) via hydrodistillation. The chemical composition, and antibacterial and antioxidant activities of the EOs were investigated. GC-MS analysis showed that monoterpene hydrocarbons were the major components and limonene was the predominate compound for all citrus EOs. The antibacterial testing of EOs against five different bacteria (Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Salmonella typhimurium) was carried out using the filter paper method and the broth microdilution method. Kumquat EO had the best inhibitory effect on B. subtilis, E. coli and S. typhimurium with MIC (minimum inhibitory concentration) values of 1.56, 1.56 and 6.25 µL/mL, respectively. All citrus EOs showed the antioxidant activity of scavenging DPPH and ABTS free radicals in a dose-dependent manner. Nanfeng mandarin EO presented the best antioxidant activity, with IC50 values of 15.20 mg/mL for the DPPH assay and 0.80 mg/mL for the ABTS assay. The results also showed that the antibacterial activities of EOs might not be related to their antioxidant activities. Full article
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16 pages, 5752 KiB  
Article
Quorum Sensing and NF-κB Inhibition of Synthetic Coumaperine Derivatives from Piper nigrum
by Yael Kadosh, Subramani Muthuraman, Karin Yaniv, Yifat Baruch, Jacob Gopas, Ariel Kushmaro and Rajendran Saravana Kumar
Molecules 2021, 26(8), 2293; https://doi.org/10.3390/molecules26082293 - 15 Apr 2021
Cited by 3 | Viewed by 2303
Abstract
Bacterial communication, termed Quorum Sensing (QS), is a promising target for virulence attenuation and the treatment of bacterial infections. Infections cause inflammation, a process regulated by a number of cellular factors, including the transcription Nuclear Factor kappa B (NF-κB); this factor is found [...] Read more.
Bacterial communication, termed Quorum Sensing (QS), is a promising target for virulence attenuation and the treatment of bacterial infections. Infections cause inflammation, a process regulated by a number of cellular factors, including the transcription Nuclear Factor kappa B (NF-κB); this factor is found to be upregulated in many inflammatory diseases, including those induced by bacterial infection. In this study, we tested 32 synthetic derivatives of coumaperine (CP), a known natural compound found in pepper (Piper nigrum), for Quorum Sensing Inhibition (QSI) and NF-κB inhibitory activities. Of the compounds tested, seven were found to have high QSI activity, three inhibited bacterial growth and five inhibited NF-κB. In addition, some of the CP compounds were active in more than one test. For example, compounds CP-286, CP-215 and CP-158 were not cytotoxic, inhibited NF-κB activation and QS but did not show antibacterial activity. CP-154 inhibited QS, decreased NF-κB activation and inhibited bacterial growth. Our results indicate that these synthetic molecules may provide a basis for further development of novel therapeutic agents against bacterial infections. Full article
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13 pages, 589 KiB  
Article
Phenolic Compounds and Bioactive Properties of Ruscus aculeatus L. (Asparagaceae): The Pharmacological Potential of an Underexploited Subshrub
by Joana P. B. Rodrigues, Ângela Fernandes, Maria Inês Dias, Carla Pereira, Tânia C. S. P. Pires, Ricardo C. Calhelha, Ana Maria Carvalho, Isabel C. F. R. Ferreira and Lillian Barros
Molecules 2021, 26(7), 1882; https://doi.org/10.3390/molecules26071882 - 26 Mar 2021
Cited by 6 | Viewed by 2706
Abstract
Ruscus aculeatus L. is a subshrub used in traditional medicine in different parts of the world, namely in Europe and the Iberian Peninsula. According to reported folk knowledge, the aerial parts are mainly used as diuretics and the underground organs are used for [...] Read more.
Ruscus aculeatus L. is a subshrub used in traditional medicine in different parts of the world, namely in Europe and the Iberian Peninsula. According to reported folk knowledge, the aerial parts are mainly used as diuretics and the underground organs are used for the treatment of disorders of the urinary system and as a laxative. In this work, the aerial part and the roots and rhizomes of R. aculeatus were chemically characterized with regard to the content of phenolic compounds and bioactive properties. Aqueous (infusions and decoctions) preparations and hydroethanolic extracts from the two mentioned parts of the plant were prepared. Nine phenolic compounds were detected in all the extracts. Apigenin-C-hexoside-C-pentoside isomer II was the major compound in aqueous extracts and, in the hydroethanolic extract was quercetin-O-deoxyhexoside-hexoside followed by apigenin-C-hexoside-C-pentoside isomer II. All extracts revealed antioxidant activity and potential to inhibit some of the assayed bacteria; aqueous extracts of the aerial part and infusions of roots and rhizomes did not show cytotoxic effects on a non-tumor primary cell culture. This preliminary study provides suggestions of the biological potential associated with the empirical uses and knowledge of this species, in particular its bioactivities. Full article
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17 pages, 1751 KiB  
Article
Extract from the Marine Seaweed Padina pavonica Protects Mitochondrial Biomembranes from Damage by Amyloidogenic Peptides
by Mario Caruana, Angelique Camilleri, Maria Ylenia Farrugia, Stephanie Ghio, Michaela Jakubíčková, Ruben J. Cauchi and Neville Vassallo
Molecules 2021, 26(5), 1444; https://doi.org/10.3390/molecules26051444 - 07 Mar 2021
Cited by 7 | Viewed by 2957
Abstract
The identification of compounds which protect the double-membrane of mitochondrial organelles from disruption by toxic confomers of amyloid proteins may offer a therapeutic strategy to combat human neurodegenerative diseases. Here, we exploited an extract from the marine brown seaweed Padina pavonica (PPE) as [...] Read more.
The identification of compounds which protect the double-membrane of mitochondrial organelles from disruption by toxic confomers of amyloid proteins may offer a therapeutic strategy to combat human neurodegenerative diseases. Here, we exploited an extract from the marine brown seaweed Padina pavonica (PPE) as a vital source of natural bioactive compounds to protect mitochondrial membranes against insult by oligomeric aggregates of the amyloidogenic proteins amyloid-β (Aβ), α-synuclein (α-syn) and tau, which are currently considered to be major targets for drug discovery in Alzheimer’s disease (AD) and Parkinson’s disease (PD). We show that PPE manifested a significant inhibitory effect against swelling of isolated mitochondria exposed to the amyloid oligomers, and attenuated the release of cytochrome c from the mitochondria. Using cardiolipin-enriched synthetic lipid membranes, we also show that dye leakage from fluorophore-loaded vesicles and formation of channel-like pores in planar bilayer membranes are largely prevented by incubating the oligomeric aggregates with PPE. Lastly, we demonstrate that PPE curtails the ability of Aβ42 and α-syn monomers to self-assemble into larger β-aggregate structures, as well as potently disrupts their respective amyloid fibrils. In conclusion, the mito-protective and anti-aggregator biological activities of Padina pavonica extract may be of therapeutic value in neurodegenerative proteinopathies, such as AD and PD. Full article
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15 pages, 327 KiB  
Article
In Vitro Phytotherapeutic Properties of Aqueous Extracted Adenia viridiflora Craib. towards Civilization Diseases
by Werawat Wannasaksri, Nattira On-Nom, Chaowanee Chupeerach, Piya Temviriyanukul, Somsri Charoenkiatkul and Uthaiwan Suttisansanee
Molecules 2021, 26(4), 1082; https://doi.org/10.3390/molecules26041082 - 18 Feb 2021
Cited by 8 | Viewed by 2609
Abstract
Adenia viridiflora Craib. is an indigenous edible plant that became an endangered species due to limited consumption of the local population with unknown reproduction and growth conditions. The plant is used as a traditional herb; however, its health applications lack scientific-based evidence. A. [...] Read more.
Adenia viridiflora Craib. is an indigenous edible plant that became an endangered species due to limited consumption of the local population with unknown reproduction and growth conditions. The plant is used as a traditional herb; however, its health applications lack scientific-based evidence. A. viridiflora Craib. plant parts (old leaves and young shoots) from four areas as Kamphaeng Phet (KP), Muang Nakhon Ratchasima (MN), Pakchong Nakhon Ratchasima (PN), and Uthai Thani (UT) origins were investigated for phenolic compositions and in vitro health properties through the inhibition of key enzymes relevant to obesity (lipase), diabetes (α-glucosidase and dipeptidyl peptidase-IV), Alzheimer’s disease (cholinesterases and β-secretase), and hypertension (angiotensin-converting enzyme). Phenolics including p-coumaric acid, sinapic acid, naringenin, and apigenin were detected in old leaves and young shoots in all plant origins. Old leaves exhibited higher total phenolic contents (TPCs) and total flavonoid contents (TFCs), leading to higher enzyme inhibitory activities than young shoots. Besides, PN and MN with higher TPCs and TFCs tended to exhibit greater enzyme inhibitory activities than others. These results will be useful to promote this plant as a healthy food with valuable medicinal capacities to support its consumption and agricultural stimulation, leading to sustainable conservation of this endangered species. Full article
13 pages, 2693 KiB  
Article
Caralluma europaea (Guss.) N.E.Br.: Anti-Inflammatory, Antifungal, and Antibacterial Activities against Nosocomial Antibiotic-Resistant Microbes of Chemically Characterized Fractions
by Fatima Ez-Zahra Amrati, Mohammed Bourhia, Hamza Saghrouchni, Meryem Slighoua, Andriy Grafov, Riaz Ullah, Essam Ezzeldin, Gamal A. Mostafa, Ahmed Bari, Samir Ibenmoussa and Dalila Bousta
Molecules 2021, 26(3), 636; https://doi.org/10.3390/molecules26030636 - 26 Jan 2021
Cited by 31 | Viewed by 3259
Abstract
Caralluma europaea (Guss.) N.E.Br.: (C. europaea) is a wild medicinal plant belonging to the family Apocynaceae. It is commonly used in traditional medicines for treating several diseases. The present work aims to evaluate the anti-inflammatory, antibacterial, and antifungal potentials of C. [...] Read more.
Caralluma europaea (Guss.) N.E.Br.: (C. europaea) is a wild medicinal plant belonging to the family Apocynaceae. It is commonly used in traditional medicines for treating several diseases. The present work aims to evaluate the anti-inflammatory, antibacterial, and antifungal potentials of C. europaea fractions including hydro ethanol (ET CE), n-butanol (But CE), and polyphenol (Poly CE). The chemical composition of hydroethanol, n-butanol, and polyphenol-rich fractions from C. europaea were determined using GC-MS after silylation. The anti-inflammatory effect of hydroethanol, n-butanol, and polyphenol-rich fractions was studied by carrageenan-induced paw edema. Antibacterial and antifungal activities of hydroethanol, n-butanol, and polyphenol-rich fractions against Gram-positive bacteria, Gram-negative bacteria, and yeasts were assessed using the disc diffusion and micro-dilution assays. The findings of the chemical characterization affirmed the presence of interesting bioactive compounds in C. europaea fractions. The polyphenol-rich fraction was the best inhibitor of edema by75.68% after 6 h of treatment. The hydroethanol fraction was the most active against both bacteria and yeasts. This study contributes to society as it provides potential bioactive compounds in C. europaea extract, which may help in fighting nosocomial antibiotic-resistant microbes. Full article
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9 pages, 911 KiB  
Article
Subacute Assessment of the Toxicity and Antidepressant-Like Effects of Origanum Majorana L. Polyphenols in Swiss Albino Mice
by Amal Amaghnouje, Hamza Mechchate, Imane Es-safi, Smahane Boukhira, Ali S. Aliqahtani, Omar M. Noman, Fahd A. Nasr, Raffaele Conte, Anna Calarco and Dalila Bousta
Molecules 2020, 25(23), 5653; https://doi.org/10.3390/molecules25235653 - 30 Nov 2020
Cited by 25 | Viewed by 2402
Abstract
Origanum majorana L. is a plant commonly used in folk medicine to treat depression and several neurological disorders. This study aims to evaluate the antidepressant-like effect of the Origanum majorana L. polyphenols (OMP) obtained from the aerial parts using two different depression model [...] Read more.
Origanum majorana L. is a plant commonly used in folk medicine to treat depression and several neurological disorders. This study aims to evaluate the antidepressant-like effect of the Origanum majorana L. polyphenols (OMP) obtained from the aerial parts using two different depression model tests: The forced swimming test (FST) and the tail suspension test (TST) in Swiss albino mice. The experiments were performed on days 1, 7, 14, and 21 with daily administration of different treatments. Two different doses were chosen for this study (50 and 100 mg/kg), and paroxetine was used as a positive control. Immobility as a consequence of the depression state was significantly reduced following the treatment with OMP, indicating an antidepressant effect. A subacute toxicity study was also performed following the Organization for Economic Co-operation and Development (OECD) Guidelines (407), showing no sign of toxicity for the studied doses. The phytochemical screening revealed the presence of 12 components, all belonging to polyphenols: Arbutin, rosmarinic acid, ursolic acid, quercetin-3-O-glucoside, quercetin-7-O-glucuronic acid, luteolin-7-O-glucoside, kaempferol-3-0-glucuronic acid, Kaempferol-3-0-pentose, caffeic acid, catechin, quercetin, and rutin. These findings suggest that O. majorana has interesting antidepressant-like properties, which deserve further investigation. Full article
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14 pages, 712 KiB  
Article
Anacyclus pyrethrum (L): Chemical Composition, Analgesic, Anti-Inflammatory, and Wound Healing Properties
by Fatima Zahra Jawhari, Abdelfattah El Moussaoui, Mohammed Bourhia, Hamada Imtara, Hamza Mechchate, Imane Es-Safi, Riaz Ullah, Essam Ezzeldin, Gamal A. Mostafa, Andriy Grafov, Samir Ibenmoussa, Dalila Bousta and Amina Bari
Molecules 2020, 25(22), 5469; https://doi.org/10.3390/molecules25225469 - 23 Nov 2020
Cited by 34 | Viewed by 4423
Abstract
Background: Anacyclus pyrethrum (A. pyrethrum) is a wild species belonging to the family Asteraceae, which is used in traditional medicines. Aim of the study: This work was undertaken to study the chemical composition, analgesic, anti-inflammatory, and wound healing properties of hydroalcoholic [...] Read more.
Background: Anacyclus pyrethrum (A. pyrethrum) is a wild species belonging to the family Asteraceae, which is used in traditional medicines. Aim of the study: This work was undertaken to study the chemical composition, analgesic, anti-inflammatory, and wound healing properties of hydroalcoholic extracts of different parts (roots, seeds, leaves, and capitula) of A. pyrethrum. Material and Methods: The phytochemical analysis of the studied extracts was conducted by GC-MS. The analgesic activity was evaluated in mice using acetic acid and formaldehyde methods. The anti-inflammatory activity was tested using the inhibitory method of edema induced in rats. The healing activity of the hydroethanolic extracts was explored by excision and incision wound healing models in rats. Results: The phytochemical analysis of the studied plant extracts affirmed the presence of interesting compounds, including some newly detected elements, such as sarcosine, N-(trifluoroacetyl)-butyl ester, levulinic acid, malonic acid, palmitic acid, morphinan-6-One, 4,5.alpha.-epoxy-3-hydroxy-17-methyl, 2,4-undecadiene-8,10-diyne-N-tyramide, and isovaleric acid. The extracts of different parts (roots, seeds, leaves, and capitula) exhibited promising anti-inflammatory, analgesic, and wound healing effects, with percentages of inhibition up to 98%, 94%, and 100%, respectively. Conclusion: This study might contribute towards the well-being of society as it provides evidence on the potential analgesic, anti-inflammatory, and wound healing properties of A. pyrethrum. Full article
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13 pages, 296 KiB  
Article
Anti-Microbial, Anti-Oxidant, and α-Amylase Inhibitory Activity of Traditionally-Used Medicinal Herbs: A Comparative Analyses of Pharmacology, and Phytoconstituents of Regional Halophytic Plants’ Diaspora
by Mohsen S. Al-Omar, Hamdoon A. Mohammed, Salman A. A. Mohammed, Essam Abd-Elmoniem, Yasser I. Kandil, Hussein M. Eldeeb, Sridevi Chigurupati, Ghassan M. Sulaiman, Hadeel K. Al-Khurayyif, Basma S. Almansour, Prarthana M. Suryavamshi and Riaz A. Khan
Molecules 2020, 25(22), 5457; https://doi.org/10.3390/molecules25225457 - 20 Nov 2020
Cited by 22 | Viewed by 3449
Abstract
Halophytes are the category of plants growing under harsh conditions of super-salinity, and are wide-spread in the coastal Mediterranean climatic conditions and desert oasis. They are adept at surviving through maintaining excessive production of enzymatic, and non-enzymatic secondary metabolites, especially phenolics and flavonoids [...] Read more.
Halophytes are the category of plants growing under harsh conditions of super-salinity, and are wide-spread in the coastal Mediterranean climatic conditions and desert oasis. They are adept at surviving through maintaining excessive production of enzymatic, and non-enzymatic secondary metabolites, especially phenolics and flavonoids that primarily work as anti-oxidants and phytoalexins. Five major halophyte species growing in the kingdom’s Qassim’s high-salted desert regions were investigated for confirming their traditionally used biological activity of sugar-control and anti-infectious properties. In this context, the comparative presence of phenolics, and flavonoids together with anti-microbial, anti-oxidants, and the anti-diabetic potentials of the plants’ extracts were investigated through the α-amylase inhibition method. The highest concentrations of phenolics and flavonoids were detected in Salsola imbricata (360 mg/g of the extract as Gallic-Acid-Equivalents/GAE, and 70.5 mg/g of the extract as Rutin-Equivalents/RE). In contrast, the lowest concentrations of phenolics and flavonoids were detected in Salsola cyclophylla (126.6 mg/g GAE, and 20.5 mg/g RE). The halophytes were found rich in trace elements, a factor for water-retention in high-salinity plants, wherein iron and zinc elements were found comparatively in higher concentrations in Aeluropus lagopoides (4113 µg/kg, and 40.1 µg/kg, respectively), while the copper was detected in higher concentration (11.1 µg/kg) in S. imbricata, analyzed through Inductively Coupled Plasma Optical Emission Spectrometric (ICP-OES) analysis. The anti-oxidant potentials and α-amylase enzyme inhibition-based anti-diabetic activity of S. imbricata was significantly higher than the other halophytes under study, wherein S. cyclophylla exhibited the lowest level of α-amylase inhibition. The maximum DPPH radicals’ (52.47 mg/mL), and α-amylase inhibitions (IC50 22.98 µg/mL) were detected in A.lagopoides. The anti-microbial activity against the Methicillin-Resistant Staphylococcus aureus was strongly exhibited by Zygophyllum simplex (33 mm Inhibition Zone-Diameter, 50 µg/mL Minimum-Inhibitory-Concentration), while Escherichia coli, Enterococcus faecalis, and Candida albicans growths were moderately inhibited by Tamarix aphylla. The current findings exhibited significant differences among the locally distributed halophytic plants species with regards to their bioactivity levels, anti-oxidant potentials, and the presence of trace elements. The ongoing data corroborated the plants’ traditional uses in infections and diabetic conditions. The enhanced local distribution of the plants’ diaspora and higher density of occurrence of these plants species in this region, in comparison to their normal climatic condition’s counterparts, seemed to be affected by humans’ use of the species as part of the traditional and alternative medicine over a period of long time. Full article
13 pages, 2087 KiB  
Article
Anti-Melanogenic Effects of Ethanol Extracts of the Leaves and Roots of Patrinia villosa (Thunb.) Juss through Their Inhibition of CREB and Induction of ERK and Autophagy
by Deok Jeong, Sang Hee Park, Min-Ha Kim, Sarah Lee, Yoon Kyung Cho, You Ah Kim, Byoung Jun Park, Jongsung Lee, Hakhee Kang and Jae Youl Cho
Molecules 2020, 25(22), 5375; https://doi.org/10.3390/molecules25225375 - 17 Nov 2020
Cited by 7 | Viewed by 2811
Abstract
Patrinia villosa (Thunb.) Juss is a traditional herb commonly used in East Asia including Korea, Japan, and China. It has been administered to reduce and treat inflammation in Donguibogam, Korea. The mechanism for its anti-inflammatory effects has already been reported. In this study, [...] Read more.
Patrinia villosa (Thunb.) Juss is a traditional herb commonly used in East Asia including Korea, Japan, and China. It has been administered to reduce and treat inflammation in Donguibogam, Korea. The mechanism for its anti-inflammatory effects has already been reported. In this study, we confirmed the efficacy of Patrinia villosa (Thunb.) Juss ethanol extract (Pv-EE) for inducing autophagy and investigate its anti-melanogenic properties. Melanin secretion and content were investigated using cells from the melanoma cell line B16F10. Pv-EE inhibited melanin in melanogenesis induced by α-melanocyte-stimulating hormone (α-MSH). The mechanism of inhibition of Pv-EE was confirmed by suppressing the mRNA of microphthalmia-associated transcription factor (MITF), decreasing the phosphorylation level of CREB, and increasing the phosphorylation of ERK. Finally, it was confirmed that Pv-EE induces autophagy through the autophagy markers LC3B and p62, and that the anti-melanogenic effect of Pv-EE is inhibited by the autophagy inhibitor 3-methyl adenine (3-MA). These results suggest that Pv-EE may be used as a skin protectant due to its anti-melanin properties including autophagy. Full article
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19 pages, 2496 KiB  
Article
Metabolomic Profiling of Mango (Mangifera indica Linn) Leaf Extract and Its Intestinal Protective Effect and Antioxidant Activity in Different Biological Models
by Roberto O. Ybañez-Julca, Daniel Asunción-Alvarez, Ivan M. Quispe-Díaz, Javier Palacios, Jorge Bórquez, Mario J. Simirgiotis, Shagufta Perveen, Chukwuemeka R. Nwokocha, Fredi Cifuentes and Adrián Paredes
Molecules 2020, 25(21), 5149; https://doi.org/10.3390/molecules25215149 - 05 Nov 2020
Cited by 13 | Viewed by 3575
Abstract
Mangifera indica Linn popularly known as mango is used in folk medicine to treat gastrointestinal disorders. The aim of this study was to identify the metabolomic composition of lyophilized extract of mango leaf (MIE), to evaluate the antioxidant activity on several oxidative stress [...] Read more.
Mangifera indica Linn popularly known as mango is used in folk medicine to treat gastrointestinal disorders. The aim of this study was to identify the metabolomic composition of lyophilized extract of mango leaf (MIE), to evaluate the antioxidant activity on several oxidative stress systems (DPPH, FRAP, TBARS, and ABTS), the spasmolytic and antispasmodic activity, and intestinal protective effect on oxidative stress induced by H2O2 in rat ileum. Twenty-nine metabolites were identified and characterized based on their ultra-high-performance liquid chromatography (UHPLC) high-resolution orbitrap mass spectrometry, these include: benzophenone derivatives, xanthones, phenolic acids, fatty acids, flavonoids and procyanidins. Extract demonstrated a high antioxidant activity in in-vitro assays. MIE relaxed (p < 0.001) intestinal segments of rat pre-contracted with acetylcholine (ACh) (10−5 M). Pre-incubation of intestinal segments with 100 µg/mL MIE significantly reduced (p < 0.001) the contraction to H2O2. Similar effects were observed with mangiferin and quercetin (10−5 M; p < 0.05) but not for gallic acid. Chronic treatment of rats with MIE (50 mg/kg) for 28 days significantly reduced (p < 0.001) the H2O2-induced contractions. MIE exhibited a strong antioxidant activity, spasmolytic and antispasmodic activity, which could contribute to its use as an alternative for the management of several intestinal diseases related to oxidative stress. Full article
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13 pages, 893 KiB  
Article
In-Vivo Antidiabetic Activity and In-Silico Mode of Action of LC/MS-MS Identified Flavonoids in Oleaster Leaves
by Hamza Mechchate, Imane Es-Safi, Mohammed Bourhia, Andrii Kyrylchuk, Abdelfattah El Moussaoui, Raffaele Conte, Riaz Ullah, Essam Ezzeldin, Gamal A. Mostafa, Andriy Grafov, Hicham Bekkari and Dalila Bousta
Molecules 2020, 25(21), 5073; https://doi.org/10.3390/molecules25215073 - 01 Nov 2020
Cited by 12 | Viewed by 3818
Abstract
Background: Olea europea L. subsp. europaea var. sylvestris (Mill) Lehr (Oleaster) is a wild endemic olive tree indigenous to the Mediterranean region. Olea europea leaves represent a natural reservoir of bioactive molecules that can be used for therapeutic purposes. Aim of the study: [...] Read more.
Background: Olea europea L. subsp. europaea var. sylvestris (Mill) Lehr (Oleaster) is a wild endemic olive tree indigenous to the Mediterranean region. Olea europea leaves represent a natural reservoir of bioactive molecules that can be used for therapeutic purposes. Aim of the study: This work was conducted to study antidiabetic and antihyperglycemic activities of flavonoids from oleaster leaves using alloxan-induced diabetic mice. The mode of action of flavonoids against eight receptors that have a high impact on diabetes management and complication was also investigated using molecular docking. Results: During 28 days of mice treatment with doses 25 and 50 mg/kg b.w, the studied flavonoids managed a severe diabetic state (<450 mg/dL), exhibiting a spectacular antidiabetic and antihyperglycemic activity, and improved mice health status compared to diabetic control. The in-silico mode of action of oleaster flavonoids revealed the inhibition of protein tyrosine phosphatase 1B (PTP1B), Dipeptidyl-peptidase 4 (DPP4), α-Amylase (AAM), α-Glucosidase inhibition, Aldose reductase (AldR), Glycogen phosphorylase (GP), and the activation of free fatty acid receptor 1 (FFAR1). Conclusion: The findings obtained in the present work indicate that the flavonoids from the oleaster may constitute a safe multi-target remedy to treat diabetes. Full article
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17 pages, 4182 KiB  
Article
Water Extract of Lotus Leaf Alleviates Dexamethasone-Induced Muscle Atrophy via Regulating Protein Metabolism-Related Pathways in Mice
by Sang Hee Park, Jieun Oh, Minkyeong Jo, Jin Kyeong Kim, Dong Seon Kim, Han Gyung Kim, Keejung Yoon, Yoonyong Yang, Jeong-ho Geum, Jung-Eun Kim, Su-Young Choi, Ji Hye Kim and Jae Youl Cho
Molecules 2020, 25(20), 4592; https://doi.org/10.3390/molecules25204592 - 09 Oct 2020
Cited by 15 | Viewed by 4852
Abstract
Muscle atrophy is an abnormal condition characterized by loss of skeletal muscle mass and function and is primarily caused by injury, malnutrition, various diseases, and aging. Leaf of lotus (Nelumbo nucifera Gaertn), which has been used for medicinal purposes, contains various active [...] Read more.
Muscle atrophy is an abnormal condition characterized by loss of skeletal muscle mass and function and is primarily caused by injury, malnutrition, various diseases, and aging. Leaf of lotus (Nelumbo nucifera Gaertn), which has been used for medicinal purposes, contains various active ingredients, including polyphenols, and is reported to exert an antioxidant effect. In this study, we investigated the effect of water extract of lotus leaf (LL) on muscle atrophy and the underlying molecular mechanisms of action. Amounts of 100, 200, or 300 mg/kg/day LL were administered to dexamethasone (DEX)-induced muscle atrophy mice for 4 weeks. Micro-computed tomography (CT) analysis revealed that the intake of LL significantly increased calf muscle volume, surface area, and density in DEX-induced muscle atrophy mice. Administration of LL recovered moving distance, grip strength, ATP production, and body weight, which were decreased by DEX. In addition, muscle damage caused by DEX was also improved by LL. LL reduced the protein catabolic pathway by suppressing gene expression of muscle atrophy F-Box (MAFbx; atrogin-1), muscle RING finger 1 (MuRF1), and forkhead box O (FoxO)3a, as well as phosphorylation of AMP-activated kinase (AMPK). The AKT-mammalian target of the rapamycin (mTOR) signal pathway, which is important for muscle protein synthesis, was increased in LL-administered groups. The HPLC analysis and pharmacological test revealed that quercetin 3-O-beta-glucuronide (Q3G) is a major active component in LL. Thus, Q3G decreased the gene expression of atrogin-1 and MuRF1 and phosphorylation of AMPK. This compound also increased phosphorylation levels of mTOR and its upstream enzyme AKT in DEX-treated C2C12 cells. We identified that LL improves muscle wasting through regulation of muscle protein metabolism in DEX-induced muscle atrophy mice. Q3G is predicted to be one of the major active phenolic components in LL. Therefore, we propose LL as a supplement or therapeutic agent to prevent or treat muscle wasting, such as sarcopenia. Full article
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21 pages, 3857 KiB  
Article
Inhibition of Staphylococcus aureus LC 554891 by Moringa oleifera Seed Extract either Singly or in Combination with Antibiotics
by Gamal Enan, Abdul-Raouf Al-Mohammadi, Samir Mahgoub, Seham Abdel-Shafi, Eman Askar, Mohamed F. Ghaly, Mohamed A. Taha and Nashwa El-Gazzar
Molecules 2020, 25(19), 4583; https://doi.org/10.3390/molecules25194583 - 07 Oct 2020
Cited by 22 | Viewed by 4307
Abstract
Bacterial outbreaks caused by Staphylococcus aureus (S. aureus) are interesting due to the existence of multidrug resistant (MDR) isolates. Therefore, there is a need to develop novel ways to control such MDR S. aureus. In this study, some natural agents [...] Read more.
Bacterial outbreaks caused by Staphylococcus aureus (S. aureus) are interesting due to the existence of multidrug resistant (MDR) isolates. Therefore, there is a need to develop novel ways to control such MDR S. aureus. In this study, some natural agents such as honey bee (HB), extracts of either Moringa oleifera seeds (MSE), or leaves (MLE) and essential oils of garlic, clove, and moringa were studied for their inhibitory activity against this S. aureus pathogen. About 100 food samples including beef luncheon (n = 25), potato chips (n = 50), and corn flakes (n = 25) were investigated for possible pollution with the S. aureus bacteria. The isolated bacteria suspected to belong S. aureus that grew well onto Baird–Parker agar (Oxoid) and shiny halo zones and positive coagulase reaction were selected and identified by API-Kits; all of them that were approved belong to S. aureus (18 strains). The sensitivity of the obtained 18 S. aureus bacterial strains to 12 antibiotics were evaluated; all of them were resistant to ofloxacin; however, other antibiotics tested showed variable results. Interestingly, the S. aureus No. B3 isolated from beef luncheon was resistant to 10 antibiotics out of 12 ones tested. Multiple antibiotic resistance index (MAR) of this S. aureus strain was about 83.3%. Therefore, its identification was confirmed by sequencing of a 16S rRNA gene which approved a successful biochemical identification carried out by API Kits and such strain was designated S. aureus LC 554891. The genome of such strain appeared to contain mecA gene encoding methicillin resistance; it was found to contain hla, hlb, tsst-1, and finbA that encode α-blood hemolysis, β-blood hemolysis, toxic shock syndrome gene, and fibrinogen-binding protein gene, respectively. In addition, the virulence factors viz. sea; seb; sec encoding enterotoxins were detected in the DNA extracted from S. aureus B3 strain. Aqueous extract of Moringa oleifera seeds (MSE) showed inhibitory activity against S. aureus LC 554891 better than that obtained by tetracycline, essential oils or HB. Minimum inhibitory concentration (MIC) of MSE was 20µg/mL. Instrumental analysis of MSE showed 14 bioactive chemical compounds. Combinations of both MSE and tetracycline showed distinctive inhibitory activity against S. aureus LC 554891 than that obtained by either tetracycline or MSE singly. Full article
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10 pages, 2904 KiB  
Article
Phytochemical Identification, Acute, and Sub-Acute Oral Toxicity Studies of the Foliar Extract of Withania frutescens
by Abdelfattah EL Moussaoui, Mohammed Bourhia, Fatima Zahra Jawhari, Hamza Mechchate, Meryem Slighoua, Ahmed Bari, Riaz Ullah, Hafiz Majid Mahmood, Syed Saeed Ali, Samir Ibenmoussa, Dalila Bousta and Amina Bari
Molecules 2020, 25(19), 4528; https://doi.org/10.3390/molecules25194528 - 02 Oct 2020
Cited by 18 | Viewed by 3105
Abstract
Withania frutescens (W. frutescens) is a medicinal plant widely used to treat several diseases. This work aims to study phytochemical composition as well as acute and subacute toxicity of W. frutescens hydroethanolic extract in mice. The phytochemical composition of W. frutescens [...] Read more.
Withania frutescens (W. frutescens) is a medicinal plant widely used to treat several diseases. This work aims to study phytochemical composition as well as acute and subacute toxicity of W. frutescens hydroethanolic extract in mice. The phytochemical composition of W. frutescens extract was performed using gas chromatographic analysis. Acute toxicity was studied in vivo with oral administration of single doses 400 mg/kg, 1000 mg/kg, and 2000 mg/kg for 14 days. Subacute toxicity was studied with the administration of repeated doses of 400 mg/kg/day and 2000 mg/kg/day for 28 days. Phytochemical analysis of W. frutescens hydro-ethanolic extract confirmed the presence of interesting chemical compounds. Acute toxicity results showed no toxic symptoms in mice treated with an increasing dose up to a maximum of 2000 mg/kg. Alongside acute toxicity, subacute data showed no clinical symptoms nor biochemical or histological alteration in mice treated with an increasing dose up to a maximum of 2000 mg/kg compared to the control group (p < 0.05). This study shows no toxic effects in animals treated with W. frutescens extract, and, therefore, this plant can be considered safe in animals up to 2000 mg/kg under both acute and subacute toxicity conditions. Full article
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Review

Jump to: Research

14 pages, 875 KiB  
Review
Propolis and Diet Rich in Polyphenols as Cariostatic Agents Reducing Accumulation of Dental Plaque
by Anna Kurek-Górecka, Karolina Walczyńska-Dragon, Rafael Felitti, Stefan Baron and Paweł Olczyk
Molecules 2022, 27(1), 271; https://doi.org/10.3390/molecules27010271 - 02 Jan 2022
Cited by 10 | Viewed by 2674
Abstract
Conducted studies indicate the relationship between oral health and systemic diseases. Moreover, the latest research indicated that cariogenic bacteria may severely influence the course of SARS-CoV-2 infection and increase risk of COVID-19 complications. This article aims to review various applications of propolis and [...] Read more.
Conducted studies indicate the relationship between oral health and systemic diseases. Moreover, the latest research indicated that cariogenic bacteria may severely influence the course of SARS-CoV-2 infection and increase risk of COVID-19 complications. This article aims to review various applications of propolis and pay attention to a healthy diet rich in polyphenols, which may allow the reduction of dental plaque accumulation. A literature review has been conducted from June until November 2021. It showed that propolis could be a useful agent in decreasing the accumulation of dental plaque. Moreover, a diet rich in polyphenols prevents cariogenic bacteria and reduces the accumulation of dental plaque. A reduction of a dental plaque may influence the risk of a severe course of COVID-19. Therefore, propolis and a diet rich in polyphenols may play an important role in prophylaxis of systemic diseases. Recently, it has been proven that oral infection may affect cardiovascular system, musculoskeletal system, respiratory system, nervous system, as well as may be a risk factor for diabetes mellitus. These aspects should stimulate clinicians to further research about polyphenols. Full article
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14 pages, 321 KiB  
Review
The Common Cichory (Cichorium intybus L.) as a Source of Extracts with Health-Promoting Properties—A Review
by Katarzyna Janda, Izabela Gutowska, Małgorzata Geszke-Moritz and Karolina Jakubczyk
Molecules 2021, 26(6), 1814; https://doi.org/10.3390/molecules26061814 - 23 Mar 2021
Cited by 51 | Viewed by 8036
Abstract
Natural products are gaining more interest recently, much of which focuses on those derived from medicinal plants. The common chicory (Cichorium intybus L.), of the Astraceae family, is a prime example of this trend. It has been proven to be a feasible [...] Read more.
Natural products are gaining more interest recently, much of which focuses on those derived from medicinal plants. The common chicory (Cichorium intybus L.), of the Astraceae family, is a prime example of this trend. It has been proven to be a feasible source of biologically relevant elements (K, Fe, Ca), vitamins (A, B1, B2, C) as well as bioactive compounds (inulin, sesquiterpene lactones, coumarin derivatives, cichoric acid, phenolic acids), which exert potent pro-health effects on the human organism. It displays choleretic and digestion-promoting, as well as appetite-increasing, anti-inflammatory and antibacterial action, all owing to its varied phytochemical composition. Hence, chicory is used most often to treat gastrointestinal disorders. Chicory was among the plants with potential against SARS-CoV-2, too. To this and other ends, roots, herb, flowers and leaves are used. Apart from its phytochemical applications, chicory is also used in gastronomy as a coffee substitute, food or drink additive. The aim of this paper is to present, in the light of the recent literature, the chemical composition and properties of chicory. Full article
13 pages, 257 KiB  
Review
Bee Venom in Wound Healing
by Anna Kurek-Górecka, Katarzyna Komosinska-Vassev, Anna Rzepecka-Stojko and Paweł Olczyk
Molecules 2021, 26(1), 148; https://doi.org/10.3390/molecules26010148 - 31 Dec 2020
Cited by 35 | Viewed by 5100
Abstract
Bee venom (BV), also known as api-toxin, is widely used in the treatment of different inflammatory diseases such as rheumatoid arthritis or multiple sclerosis. It is also known that BV can improve the wound healing process. BV plays a crucial role in the [...] Read more.
Bee venom (BV), also known as api-toxin, is widely used in the treatment of different inflammatory diseases such as rheumatoid arthritis or multiple sclerosis. It is also known that BV can improve the wound healing process. BV plays a crucial role in the modulation of the different phases of wound repair. It possesses anti-inflammatory, antioxidant, antifungal, antiviral, antimicrobial and analgesic properties, all of which have a positive impact on the wound healing process. The mentioned process consists of four phases, i.e., hemostasis, inflammation, proliferation and remodeling. The impaired wound healing process constitutes a significant problem especially in diabetic patients, due to hypoxia state. It had been found that BV accelerated the wound healing in diabetic patients as well as in laboratory animals by impairing the caspase-3, caspase-8 and caspase-9 activity. Moreover, the activity of BV in wound healing is associated with regulating the expression of transforming growth factor (TGF-β1), vascular endothelial growth factor and increased collagen type I. BV stimulates the proliferation and migration of human epidermal keratinocytes and fibroblasts. In combination with polyvinyl alcohol and chitosan, BV significantly accelerates the wound healing process, increasing the hydroxyproline and glutathione and lowering the IL-6 level in wound tissues. The effect of BV on the wounds has been proved by numerous studies, which revealed that BV in the wound healing process brings about a curative effect and could be applied as a new potential treatment for wound repair. However, therapy with bee venom may induce allergic reactions, so it is necessary to assess the existence of the patient’s hypersensitivity to apitoxin before treatment. Full article
35 pages, 618 KiB  
Review
Caesalpinia ferrea C. Mart. (Fabaceae) Phytochemistry, Ethnobotany, and Bioactivities: A Review
by Nair Silva Macêdo, Zildene de Sousa Silveira, Antonio Henrique Bezerra, José Galberto Martins da Costa, Henrique Douglas Melo Coutinho, Barbara Romano, Raffaele Capasso, Francisco Assis Bezerra da Cunha and Márcia Vanusa da Silva
Molecules 2020, 25(17), 3831; https://doi.org/10.3390/molecules25173831 - 23 Aug 2020
Cited by 25 | Viewed by 4797
Abstract
Caesalpinia ferrea C. Mart., popularly known as “Jucá” or “Pau-ferro”, belongs to the Fabaceae family, and is classified as a native and endemic species in Brazil. Numerous studies that portray its ethnobotany, chemical composition, and biological activities exist in the literature. The [...] Read more.
Caesalpinia ferrea C. Mart., popularly known as “Jucá” or “Pau-ferro”, belongs to the Fabaceae family, and is classified as a native and endemic species in Brazil. Numerous studies that portray its ethnobotany, chemical composition, and biological activities exist in the literature. The present study aimed to systematically review publications addressing the botanical aspects, uses in popular medicine, phytochemical composition, and bioactivities of C. ferrea. The searches focused on publications from 2015 to March 2020 using the Scopus, Periódicos Capes, PubMed, Google Scholar, and ScienceDirect databases. The leaves, fruits, seeds, and bark from C. ferrea are used in popular medicine to treat disorders affecting several systems, including the circulatory, immune, cardiovascular, digestive, respiratory, genitourinary, musculoskeletal, and conjunctive systems. The most commonly found chemical classes in phytochemical studies are flavonoids, polyphenols, terpenoids, tannins, saponins, steroids, and other phenolic compounds. The biological properties of the extracts and isolated compounds of C. ferrea most cited in the literature were antibacterial, antifungal, antioxidant, antiproliferative, anti-inflammatory, and healing potential. However, further studies are still needed to clarify a link between its traditional uses, the active compounds, and the reported pharmacological activities, as well as detailed research to determine the toxicological profile of C. ferrea. Full article
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