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Natural Bioactive Compounds and Human Health

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

Deadline for manuscript submissions: closed (31 March 2024) | Viewed by 66370

Special Issue Editors


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Guest Editor
Division of Cell and Molecular Biology, PG and Research Department of Zoology, St. Joseph's College (Autonomous), Devagiri, Kozhikode 673008, Kerala, India
Interests: cancer; nutraceuticals; functional foods; inflammation; anticancer activity; nutrition
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department of Medical Biochemistry, Faculty of Basic Medical Sciences, College of Medicine, Alex Ekwueme Federal University, Ndufu-Alike lkwo, P.M.B. 1010, Abakaliki 482131, Nigeria
Interests: functional foods; virgin coconut oil; anticancer activity; hepatotoxicity; heavy metal toxicity

E-Mail Website
Guest Editor
Department of Botany and Microbiology, Faculty of Biology, University of Bucharest, 1-3 Portocalelor Street, 060101 Bucharest, Romania
Interests: functional foods; essential oils; pest control; nutrition; phytochemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Over the past few decades, the incidence rate of both infectious and degenerative diseases has significantly increased. These diseases account for high mortality among developing and underdeveloped countries. This has led to the quest for new drug compounds for the management of various diseases. Natural products are important sources of drug candidates which are presently in the various stages of drug development, including preclinical and clinical trials. Traditional herbal medicines and their bioactive compounds are a major source of pharmacologically active molecules. The application of these herbal medicines has been useful in the management of microbial infections and chronic diseases such as cancers, cardiovascular diseases and obesity. Apart from plant products, animal-derived bioactive compounds such as honey polyphenols, venom-derived compounds and nutritious molecules are also important in the management of human health. Further, microbial products including antioxidants, pigments and antimicrobial bioactives are also considered as drug candidates.

Thus, the present Special Issue aims to consolidate the contributions of natural bioactive compounds in the management of human health based on in silico, in vitro and in vivo studies, including results from clinical trials.

Potential topics include, but are not limited to:

  • Chemical composition and bioavailability of bioactive compounds;
  • Antioxidant and anti-inflammatory properties;
  • Antimicrobial plant and animal products;
  • Pharmacological effects of natural products of plant/ animal/ microbial origin;
  • Novel drug-delivery strategies for bioactive natural products;
  • Combination of natural products and pharmacological drugs in medicine;
  • Molecular mechanism of action of natural products;
  • Essential oils and biological effects;
  • Green synthesized nanoparticles and their biological effects;
  • Functional foods and nutraceuticals.

Dr. Arunaksharan Narayanankutty
Dr. Ademola C. Famurewa
Dr. Eliza Oprea
Guest Editors

Manuscript Submission Information

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Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • bioactive natural products
  • secondary metabolites
  • animal products
  • microbial products
  • antidiabetic activity
  • anticancer effects
  • hypolipidemic activity
  • antimicrobial potentials
  • essential oils
  • anti-inflammatory effects

Published Papers (33 papers)

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Research

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15 pages, 1298 KiB  
Article
Vitamin D3 Bioaccessibility from Supplements and Foods—Gastric pH Effect Using a Static In Vitro Gastrointestinal Model
by Evangelia Pasidi and Patroklos Vareltzis
Molecules 2024, 29(5), 1153; https://doi.org/10.3390/molecules29051153 - 05 Mar 2024
Viewed by 806
Abstract
Vitamin D3 deficiency is a global phenomenon, which can be managed with supplementation and food fortification. However, vitamin D3 bioaccessibility may depend on factors such as matrix composition and interactions throughout the gastrointestinal (GI) tract. This research focused on the effect [...] Read more.
Vitamin D3 deficiency is a global phenomenon, which can be managed with supplementation and food fortification. However, vitamin D3 bioaccessibility may depend on factors such as matrix composition and interactions throughout the gastrointestinal (GI) tract. This research focused on the effect of different matrices on vitamin D3 content during digestion, as well as the effect of pH on its bioaccessibility. The INFOGEST protocol was employed to simulate digestion. Three different types of commercial supplements, two foods naturally rich in vitamin D3, and three fortified foods were investigated. High-Performance Liquid Chromatography was used to determine the initial vitamin D3 content in the supplements and foods, as well as after each digestion stage. The results indicate that the foods exhibited higher bioaccessibility indices compared to the supplements and a higher percentage retention at the end of the gastric phase. The pH study revealed a positive correlation between an increased gastric pH and the corresponding content of vitamin D3. Interestingly, exposing the matrix to a low pH during the gastric phase resulted in an increased intestinal content of D3. Vitamin D3 is more bioaccessible from foods than supplements, and its bioaccessibility is susceptible to changes in gastric pH. Fasting conditions (i.e., gastric pH = 1) enhance the vitamin’s bioaccessibility. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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17 pages, 5086 KiB  
Article
Phytochemical Composition and Antioxidant and Anti-Inflammatory Activities of Humboldtia sanjappae Sasidh. & Sujanapal, an Endemic Medicinal Plant to the Western Ghats
by Jameema Sidhic, Satheesh George, Ahmed Alfarhan, Rajakrishnan Rajagopal, Opeyemi Joshua Olatunji and Arunaksharan Narayanankutty
Molecules 2023, 28(19), 6875; https://doi.org/10.3390/molecules28196875 - 29 Sep 2023
Viewed by 956
Abstract
Ethnomedicinal plants are important sources of drug candidates, and many of these plants, especially in the Western Ghats, are underexplored. Humboldtia, a genus within the Fabaceae family, thrives in the biodiversity of the Western Ghats, Kerala, India, and holds significant ethnobotanical importance. [...] Read more.
Ethnomedicinal plants are important sources of drug candidates, and many of these plants, especially in the Western Ghats, are underexplored. Humboldtia, a genus within the Fabaceae family, thrives in the biodiversity of the Western Ghats, Kerala, India, and holds significant ethnobotanical importance. However, many Humboldtia species remain understudied in terms of their biological efficacy, while some lack scientific validation for their traditional uses. However, Humboldtia sanjappae, an underexplored plant, was investigated for the phytochemical composition of the plant, and its antioxidant, enzyme-inhibitory, anti-inflammatory, and antibacterial activities were assessed. The LC-MS analysis indicated the presence of several bioactive substances, such as Naringenin, Luteolin, and Pomiferin. The results revealed that the ethanol extract of H. sanjappae exhibited significant in vitro DPPH scavenging activity (6.53 ± 1.49 µg/mL). Additionally, it demonstrated noteworthy FRAP (Ferric Reducing Antioxidant Power) activity (8.46 ± 1.38 µg/mL). Moreover, the ethanol extract of H. sanjappae exhibited notable efficacy in inhibiting the activities of α-amylase (47.60 ± 0.19µg/mL) and β-glucosidase (32.09 ± 0.54 µg/mL). The pre-treatment with the extract decreased the LPS-stimulated release of cytokines in the Raw 264.7 macrophages, demonstrating the anti-inflammatory potential. Further, the antibacterial properties were also evident in both Gram-positive and Gram-negative bacteria. The observed high zone of inhibition in the disc diffusion assay and MIC values were also promising. H. sanjappae displays significant anti-inflammatory, antioxidant, antidiabetic, and antibacterial properties, likely attributable to its rich composition of various biological compounds such as Naringenin, Luteolin, Epicatechin, Maritemin, and Pomiferin. Serving as a promising reservoir of these beneficial molecules, the potential of H. sanjappae as a valuable source for bioactive ingredients within the realms of nutraceutical and pharmaceutical industries is underscored, showcasing its potential for diverse applications. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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13 pages, 846 KiB  
Article
Synthesis of Bis-Chalcones and Evaluation of Its Effect on Peroxide-Induced Cell Death and Lipopolysaccharide-Induced Cytokine Production
by Alby Tom, Jisha Jacob, Manoj Mathews, Rajakrishnan Rajagopal, Ahmed Alfarhan, Damia Barcelo and Arunaksharan Narayanankutty
Molecules 2023, 28(17), 6354; https://doi.org/10.3390/molecules28176354 - 30 Aug 2023
Viewed by 884
Abstract
Plant secondary metabolites are important sources of biologically active compounds with wide pharmacological potentials. Among the different classes, the chalcones form integral pharmacologically active agents. Natural chalcones and bis-chalcones exhibit high antioxidant and anti-inflammatory properties in various experiments. Studies are also underway to [...] Read more.
Plant secondary metabolites are important sources of biologically active compounds with wide pharmacological potentials. Among the different classes, the chalcones form integral pharmacologically active agents. Natural chalcones and bis-chalcones exhibit high antioxidant and anti-inflammatory properties in various experiments. Studies are also underway to explore more biologically active bis-chalcones by chemical synthesis of these compounds. In this study, the effects of six synthetic bis-chalcones were evaluated in intestinal epithelial cells (IEC-6); further, the anti-inflammatory potentials were studied in lipopolysaccharide-induced cytokine production in macrophages. The synthesized bis-chalcones differ from each other first of all by the nature of the aromatic cores (functional group substitution, and their position) and by the size of a central alicycle. The exposure of IEC-6 cells to peroxide radicals reduced the cell viability; however, pre-treatment with the bis-chalcones improved the cell viability in these cells. The mechanism of action was observed to be the increased levels of glutathione and antioxidant enzyme activities. Further, these bis-chalcones also inhibited the LPS-stimulation-induced inflammatory cytokine production in RAW 264.7 macrophages. Overall, the present study indicated the cytoprotective and anti-inflammatory abilities of synthetic bis-chalcones. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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21 pages, 5172 KiB  
Article
Ethanolic Extract Propolis-Loaded Niosomes Diminish Phospholipase B1, Biofilm Formation, and Intracellular Replication of Cryptococcus neoformans in Macrophages
by Kritapat Kietrungruang, Sanonthinee Sookkree, Sirikwan Sangboonruang, Natthawat Semakul, Worrapan Poomanee, Kuntida Kitidee, Yingmanee Tragoolpua and Khajornsak Tragoolpua
Molecules 2023, 28(17), 6224; https://doi.org/10.3390/molecules28176224 - 24 Aug 2023
Viewed by 1177
Abstract
Secretory phospholipase B1 (PLB1) and biofilms act as microbial virulence factors and play an important role in pulmonary cryptococcosis. This study aims to formulate the ethanolic extract of propolis-loaded niosomes (Nio-EEP) and evaluate the biological activities occurring during PLB1 production and biofilm formation [...] Read more.
Secretory phospholipase B1 (PLB1) and biofilms act as microbial virulence factors and play an important role in pulmonary cryptococcosis. This study aims to formulate the ethanolic extract of propolis-loaded niosomes (Nio-EEP) and evaluate the biological activities occurring during PLB1 production and biofilm formation of Cryptococcus neoformans. Some physicochemical characterizations of niosomes include a mean diameter of 270 nm in a spherical shape, a zeta-potential of −10.54 ± 1.37 mV, and 88.13 ± 0.01% entrapment efficiency. Nio-EEP can release EEP in a sustained manner and retains consistent physicochemical properties for a month. Nio-EEP has the capability to permeate the cellular membranes of C. neoformans, causing a significant decrease in the mRNA expression level of PLB1. Interestingly, biofilm formation, biofilm thickness, and the expression level of biofilm-related genes (UGD1 and UXS1) were also significantly reduced. Pre-treating with Nio-EEP prior to yeast infection reduced the intracellular replication of C. neoformans in alveolar macrophages by 47%. In conclusion, Nio-EEP mediates as an anti-virulence agent to inhibit PLB1 and biofilm production for preventing fungal colonization on lung epithelial cells and also decreases the intracellular replication of phagocytosed cryptococci. This nano-based EEP delivery might be a potential therapeutic strategy in the prophylaxis and treatment of pulmonary cryptococcosis in the future. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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18 pages, 3187 KiB  
Article
Therapeutic Applications of Essential Oils from Native and Cultivated Ecuadorian Plants: Cutaneous Candidiasis and Dermal Anti-Inflammatory Activity
by Lilian Sosa, Lupe Carolina Espinoza, Eduardo Valarezo, Núria Bozal, Ana Calpena, María-José Fábrega, Laura Baldomà, María Rincón and Mireia Mallandrich
Molecules 2023, 28(15), 5903; https://doi.org/10.3390/molecules28155903 - 05 Aug 2023
Viewed by 1583
Abstract
Essential oils are a complex mixture of aromatic substances whose pharmacological actions, including antimicrobial, antioxidant, anticancer, and anti-inflammatory activities, have been widely reported. This study aimed to evaluate the anti-Candida and dermal anti-inflammatory activity of essential oils from native and cultivated Ecuadorian [...] Read more.
Essential oils are a complex mixture of aromatic substances whose pharmacological actions, including antimicrobial, antioxidant, anticancer, and anti-inflammatory activities, have been widely reported. This study aimed to evaluate the anti-Candida and dermal anti-inflammatory activity of essential oils from native and cultivated Ecuadorian plants. Essential oils from Bursera graveolens, Dacryodes peruviana, Mespilodaphne quixos, and Melaleuca armillaris were isolated by hydrodistillation and were characterized physically and chemically. Its tolerance was analyzed by in vitro and in vivo studies. The antifungal activity was studied against Candida albicans, Candida glabrata, and Candida parapsilosis, whereas the anti-inflammatory effect was evaluated by a mouse ear edema model. The main compounds were limonene, α-phellandrene, (E)-methyl cinnamate, and 1,8-cineole, respectively. All essential oils showed high tolerability for skin application, antifungal activity against the three Candida strains, and anti-inflammatory efficacy by decreasing edema and overexpression of pro-inflammatory cytokines. Dacryodes peruviana essential oil showed the highest antifungal activity. On the other hand, Dacryodes peruviana and Melaleuca armillaris showed the greatest anti-inflammatory potential, decreasing edema by 53.3% and 65.25%, respectively, and inhibiting the overexpression of TNF-α, IL-8, IL-17A, and IL-23. The results suggest that these essential oils could be used as alternative therapies in the treatment of both cutaneous candidiasis and dermal inflammation. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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19 pages, 1878 KiB  
Article
Comprehensive Quality Evaluation of Polygonatum cyrtonema and Its Processed Product: Chemical Fingerprinting, Determination and Bioactivity
by Jianguang Zhang, Junjun Wang, Li Yang, Yue Wang, Wenfang Jin, Jing Li and Zhifeng Zhang
Molecules 2023, 28(11), 4341; https://doi.org/10.3390/molecules28114341 - 25 May 2023
Cited by 6 | Viewed by 1152
Abstract
Processing of Chinese herbal medicines (CHMs) is a traditional pharmaceutical technology in Chinese medicine. Traditionally, proper processing of CHMs is necessary to meet the specific clinical requirements of different syndromes. Processing with black bean juice is considered one of the most important techniques [...] Read more.
Processing of Chinese herbal medicines (CHMs) is a traditional pharmaceutical technology in Chinese medicine. Traditionally, proper processing of CHMs is necessary to meet the specific clinical requirements of different syndromes. Processing with black bean juice is considered one of the most important techniques in traditional Chinese pharmaceutical technology. Despite the long-standing practice of processing Polygonatum cyrtonema Hua (PCH), there is little research on the changes in chemical constituents and bioactivity before and after processing. This study investigated the influence of black bean juice processing on the chemical composition and bioactivity of PCH. The results revealed significant changes in both composition and contents during processing. Saccharide and saponin content significantly increased after processing. Moreover, the processed samples exhibited considerably stronger DPPH and ABTS radical scavenging capacity, as well as FRAP-reducing capacity, compared to the raw samples. The IC50 values for DPPH were 1.0 ± 0.12 mg/mL and 0.65 ± 0.10 mg/mL for the raw and processed samples, respectively. For ABTS, the IC50 values were 0.65 ± 0.07 mg/mL and 0.25 ± 0.04 mg/mL, respectively. Additionally, the processed sample demonstrated significantly higher inhibitory activity against α-glucosidase and α-amylase (IC50 = 1.29 ± 0.12 mg/mL and 0.48 ± 0.04 mg/mL) compared to the raw sample (IC50 = 5.58 ± 0.22 mg/mL and 0.80 ± 0.09 mg/mL). These findings underscore the significance of black bean processing in enhancing the properties of PCH and lay the foundation for its further development as a functional food. The study elucidates the role of black bean processing in PCH and offers valuable insights for its application. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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15 pages, 3148 KiB  
Article
Evaluation of the Biological Properties of an Optimized Extract of Polygonum cuspidatum Using Ultrasonic-Assisted Extraction
by Gabriela Fletes-Vargas, Rogelio Rodríguez-Rodríguez, Neith Pacheco, Alejandro Pérez-Larios and Hugo Espinosa-Andrews
Molecules 2023, 28(10), 4079; https://doi.org/10.3390/molecules28104079 - 13 May 2023
Viewed by 1291
Abstract
Phytochemicals are natural compounds found in plants that have potential health benefits such as antioxidants, anti-inflammatory and anti-cancer properties, and immune reinforcement. Polygonum cuspidatum Sieb. et Zucc. is a source rich in resveratrol, traditionally consumed as an infusion. In this study, P. cuspidatum root [...] Read more.
Phytochemicals are natural compounds found in plants that have potential health benefits such as antioxidants, anti-inflammatory and anti-cancer properties, and immune reinforcement. Polygonum cuspidatum Sieb. et Zucc. is a source rich in resveratrol, traditionally consumed as an infusion. In this study, P. cuspidatum root extraction conditions were optimized to increase antioxidant capacity (DPPH, ABTS+), extraction yield, resveratrol concentration, and total polyphenolic compounds (TPC) via ultrasonic-assisted extraction using a Box–Behnken design (BBD). The biological activities of the optimized extract and the infusion were compared. The optimized extract was obtained using a solvent/root powder ratio of 4, 60% ethanol concentration, and 60% ultrasonic power. The optimized extract showed higher biological activities than the infusion. The optimized extract contained 16.6 mg mL−1 resveratrol, high antioxidant activities (135.1 µg TE mL−1 for DPPH, and 230.4 µg TE mL−1 for ABTS+), TPC (33.2 mg GAE mL−1), and extraction yield of 12.4%. The EC50 value (effective concentration 50) of the optimized extract was 0.194 µg mL−1, which revealed high cytotoxic activity against the Caco-2 cell line. The optimized extract could be used to develop functional beverages with high antioxidant capacity, antioxidants for edible oils, functional foods, and cosmetics. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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12 pages, 5124 KiB  
Article
In Vivo Neuropharmacological Effects of Neophytadiene
by Maria L. Gonzalez-Rivera, Juan Carlos Barragan-Galvez, Deisy Gasca-Martínez, Sergio Hidalgo-Figueroa, Mario Isiordia-Espinoza and Angel Josabad Alonso-Castro
Molecules 2023, 28(8), 3457; https://doi.org/10.3390/molecules28083457 - 14 Apr 2023
Cited by 9 | Viewed by 1976
Abstract
Neophytadiene (NPT) is a diterpene found in the methanolic extracts of Crataeva nurvala and Blumea lacera, plants reported with anxiolytic-like activity, sedative properties, and antidepressant-like actions; however, the contribution of neophytadiene to these effects is unknown. This study determined the neuropharmacological (anxiolytic-like, [...] Read more.
Neophytadiene (NPT) is a diterpene found in the methanolic extracts of Crataeva nurvala and Blumea lacera, plants reported with anxiolytic-like activity, sedative properties, and antidepressant-like actions; however, the contribution of neophytadiene to these effects is unknown. This study determined the neuropharmacological (anxiolytic-like, antidepressant-like, anticonvulsant, and sedative) effects of neophytadiene (0.1–10 mg/kg p.o.) and determined the mechanisms of action involved in the neuropharmacological actions using inhibitors such as flumazenil and analyzing the possible interaction of neophytadiene with GABA receptors using a molecular docking study. The behavioral tests were evaluated using the light–dark box, elevated plus-maze, open field, hole-board, convulsion, tail suspension, pentobarbital-induced sleeping, and rotarod. The results showed that neophytadiene exhibited anxiolytic-like activity only to the high dose (10 mg/kg) in the elevated plus-maze and hole-board tests, and anticonvulsant actions in the 4-aminopyridine and pentylenetetrazole-induced seizures test. The anxiolytic-like and anticonvulsant effects of neophytadiene were abolished with the pre-treatment with 2 mg/kg flumazenil. In addition, neophytadiene showed low antidepressant effects (about 3-fold lower) compared to fluoxetine. On other hand, neophytadiene had no sedative or locomotor effects. In conclusion, neophytadiene exerts anxiolytic-like and anticonvulsant activities with the probable participation of the GABAergic system. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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14 pages, 876 KiB  
Article
Evaluation of the Antihypertensive Activity of Eggplant Acetylcholine and γ-Aminobutyric Acid in Spontaneously Hypertensive Rats
by Wenhao Wang, Shohei Yamaguchi, Masahiro Koyama and Kozo Nakamura
Molecules 2023, 28(6), 2835; https://doi.org/10.3390/molecules28062835 - 21 Mar 2023
Cited by 1 | Viewed by 1467
Abstract
Daily consumption of eggplant powder containing 2.3 mg acetylcholine (ACh) is known to alleviate hypertension and improve mental status. However, eggplant powder used in clinical trials also contains the antihypertensive compound γ-aminobutyric acid (GABA). Although our previous study indicated that the main antihypertensive [...] Read more.
Daily consumption of eggplant powder containing 2.3 mg acetylcholine (ACh) is known to alleviate hypertension and improve mental status. However, eggplant powder used in clinical trials also contains the antihypertensive compound γ-aminobutyric acid (GABA). Although our previous study indicated that the main antihypertensive compound in eggplant is ACh, given that GABA amounts in eggplant do not reach the effective dosage, the effects of GABA on the antihypertensive effect of eggplant remain unclear. It is necessary to establish whether there is a synergistic effect between GABA and ACh and whether GABA in eggplant exerts antihypertensive effects. Consequently, here we sought to evaluate the effects of GABA on the antihypertensive effects of eggplant. We used a probability sum (q) test to investigate the combined effects of ACh and GABA and prepared eggplant powder with very low ACh content for oral administration in animals. ACh and GABA exhibited additive effects but the GABA content in eggplants was not sufficient to promote a hypotensive effect. In conclusion, ACh is the main component associated with the antihypertensive effects of eggplant but GABA within eggplants has a minimal effect in this regard. Thus, compared with GABA, ACh could be a more effective functional food constituent for lowering blood pressure. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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12 pages, 559 KiB  
Article
Evaluation of the Chemical Composition of Selected Varieties of L. caerulea var. kamtschatica and L. caerulea var. emphyllocalyx
by Józef Gorzelany, Oskar Basara, Ireneusz Kapusta, Korfanty Paweł and Justyna Belcar
Molecules 2023, 28(6), 2525; https://doi.org/10.3390/molecules28062525 - 09 Mar 2023
Cited by 6 | Viewed by 1365
Abstract
Lonicera caerulea fruits are a rich source of vitamins, organic acids, and phenolic compounds, which are characterised by their health-promoting properties. The content of bioactive compounds in this fruit may vary depending on the cultivar and the harvest date. The fruits of the [...] Read more.
Lonicera caerulea fruits are a rich source of vitamins, organic acids, and phenolic compounds, which are characterised by their health-promoting properties. The content of bioactive compounds in this fruit may vary depending on the cultivar and the harvest date. The fruits of the L. caerulea var. kamtschatica cultivars ‘Duet’ and ‘Aurora’ and the L. caerulea var. emphyllocalyx cultivars ‘Lori’, ‘Colin’ and ‘Willa’ were used in this study. L. emphyllocalyx fruit, especially the cultivar ‘Willa’, was characterised as having a higher acidity by an average of 29.96% compared to L. kamtschatica. The average ascorbic acid content of the L. kamtschatica fruit was 53.5 mg·100 g−1 f.w., while L. emphyllocalyx fruit had an average content that was 14.14% lower. The antioxidant activity (determined by DPPH, FRAP, and ABTS) varied according to the cultivar and the species of fruit analysed. The total polyphenol content differed significantly depending on the cultivar analysed; fruits of the L. emphyllocalyx cultivar ‘Willa’ were characterised by the lowest content of total polyphenols—416.94 mg GAE·100 g−1 f.w.—while the highest content of total polyphenols—747.85 GAE·100 g−1 f.w.—was found in the fruits of the L. emphyllocalyx cultivar ‘Lori’. Lonicera caerulea fruits contained 26 different phenolic compounds in their compositions, of which the highest content was characterised by cyanidin 3-O-glucoside (average: 347.37 mg·100 g−1). On the basis of this study, it appears that both L. kamtschatica fruits and L. emphyllocalyx fruits, especially of the cultivars ‘Lori’ and ‘Willa’, can be used in food processing. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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18 pages, 4933 KiB  
Article
Ganoderic Acid A and Its Amide Derivatives as Potential Anti-Cancer Agents by Regulating the p53-MDM2 Pathway: Synthesis and Biological Evaluation
by Yi Jia, Yan Li, Hai Shang, Yun Luo and Yu Tian
Molecules 2023, 28(5), 2374; https://doi.org/10.3390/molecules28052374 - 04 Mar 2023
Cited by 5 | Viewed by 1699
Abstract
The mechanisms of action of natural products and the identification of their targets have long been a research hotspot. Ganoderic acid A (GAA) is the earliest and most abundant triterpenoids discovered in Ganoderma lucidum. The multi-therapeutic potential of GAA, in particular its [...] Read more.
The mechanisms of action of natural products and the identification of their targets have long been a research hotspot. Ganoderic acid A (GAA) is the earliest and most abundant triterpenoids discovered in Ganoderma lucidum. The multi-therapeutic potential of GAA, in particular its anti-tumor activity, has been extensively studied. However, the unknown targets and associated pathways of GAA, together with its low activity, limit in-depth research compared to other small molecule anti-cancer drugs. In this study, GAA was modified at the carboxyl group to synthesize a series of amide compounds, and the in vitro anti-tumor activities of the derivatives were investigated. Finally, compound A2 was selected to study its mechanism of action because of its high activity in three different types of tumor cell lines and low toxicity to normal cells. The results showed that A2 could induce apoptosis by regulating the p53 signaling pathway and may be involved in inhibiting the interaction of MDM2 and p53 by binding to MDM2 (KD = 1.68 µM). This study provides some inspiration for the research into the anti-tumor targets and mechanisms of GAA and its derivatives, as well as for the discovery of active candidates based on this series. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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14 pages, 2399 KiB  
Article
Extraction of Antioxidant Compounds from Brazilian Green Propolis Using Ultrasound-Assisted Associated with Low- and High-Pressure Extraction Methods
by Thiago Dantas Teixeira, Bruna Aparecida Souza Machado, Gabriele de Abreu Barreto, Jeancarlo Pereira dos Anjos, Ingrid Lessa Leal, Renata Quartieri Nascimento, Katharine Valéria Saraiva Hodel and Marcelo Andrés Umsza-Guez
Molecules 2023, 28(5), 2338; https://doi.org/10.3390/molecules28052338 - 03 Mar 2023
Cited by 5 | Viewed by 1598
Abstract
The demand for bee products has been growing, especially regarding their application in complementary medicine. Apis mellifera bees using Baccharis dracunculifolia D.C. (Asteraceae) as substrate produce green propolis. Among the examples of bioactivity of this matrix are antioxidant, antimicrobial, and antiviral [...] Read more.
The demand for bee products has been growing, especially regarding their application in complementary medicine. Apis mellifera bees using Baccharis dracunculifolia D.C. (Asteraceae) as substrate produce green propolis. Among the examples of bioactivity of this matrix are antioxidant, antimicrobial, and antiviral actions. This work aimed to verify the impact of the experimental conditions applied in low- and high-pressure extractions of green propolis, using sonication (60 kHz) as pretreatment to determine the antioxidant profile in the extracts. Total flavonoid content (18.82 ± 1.15–50.47 ± 0.77 mgQE·g−1), total phenolic compounds (194.12 ± 3.40–439.05 ± 0.90 mgGAE·g−1) and antioxidant capacity by DPPH (33.86 ± 1.99–201.29 ± 0.31 µg·mL−1) of the twelve green propolis extracts were determined. By means of HPLC-DAD, it was possible to quantify nine of the fifteen compounds analyzed. The results highlighted formononetin (4.76 ± 0.16–14.80 ± 0.02 mg·g−1) and p-coumaric acid (<LQ—14.33 ± 0.01 mg·g−1) as majority compounds in the extracts. Based on the principal component analysis, it was possible to conclude that higher temperatures favored the release of antioxidant compounds; in contrast, they decreased the flavonoid content. Thus, the obtained results showed that samples pretreated with 50 °C associated with ultrasound displayed a better performance, which may support the elucidation of the use of these conditions. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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31 pages, 7062 KiB  
Article
Study on the Comprehensive Phytochemicals and the Anti-Ulcerative Colitis Effect of Saussurea pulchella
by Yunhe Liu, Caixia Wang, Junzhe Wu, Luying Tan, Peng Gao, Sinuo Wu, Daohao Tang, Qianyun Wang, Cuizhu Wang, Pingya Li and Jinping Liu
Molecules 2023, 28(4), 1526; https://doi.org/10.3390/molecules28041526 - 04 Feb 2023
Cited by 2 | Viewed by 1712
Abstract
Background: Saussurea pulchella (SP) is a traditional medicinal plant that is widely used in folk medicine because of its diverse biological activities, particularly its anti-inflammatory effects. However, the alleviation effect of SP on ulcerative colitis (UC) has not yet been realized. Purpose: To [...] Read more.
Background: Saussurea pulchella (SP) is a traditional medicinal plant that is widely used in folk medicine because of its diverse biological activities, particularly its anti-inflammatory effects. However, the alleviation effect of SP on ulcerative colitis (UC) has not yet been realized. Purpose: To investigate the chemical composition and therapeutic effect of SP extract against UC. Methods: First, qualitative and quantitative analysis of SP 75% ethanol extract was performed by UPLC-Q/TOF-MS. Second, a dextran sodium sulfate (DSS) model of UC mice was developed to study the effects of SP on the symptoms, inflammatory factors, oxidative stress indexes and colon histopathology. Third, an integration of network pharmacology with metabolomics was performed to investigate the key metabolites, biological targets and metabolisms closely related to the effect of SP. Results: From the SP ethanol extract, 149 compounds were identified qualitatively and 20 were determined quantitatively. The SP could dose-dependently decrease the DAI score, spleen coefficient and the levels of TNF-α, IL-6, iNOS, MPO and MDA; increase the colon length, GSH level and SOD activity; and protect the intestinal barrier in the UC mice. Moreover, 10 metabolite biomarkers,18 targets and 5 metabolisms were found to play crucial roles in the treatment of UC with SP. Conclusions: SP 75% ethanol extract could effectively alleviate the progression of UC and, therefore, could be classified as a novel natural treatment for UC. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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15 pages, 1704 KiB  
Article
Proximate Composition and Nutritional Values of Selected Wild Plants of the United Arab Emirates
by Mohammad Shahid, Rakesh Kumar Singh and Sumitha Thushar
Molecules 2023, 28(3), 1504; https://doi.org/10.3390/molecules28031504 - 03 Feb 2023
Cited by 4 | Viewed by 2531
Abstract
Wild plants supply food and shelter to several organisms; they also act as important sources of many nutrients and pharmaceutical agents for mankind. These plants are widely used in traditional medicinal systems and folk medicines. The present study analyzed the nutritional and proximate [...] Read more.
Wild plants supply food and shelter to several organisms; they also act as important sources of many nutrients and pharmaceutical agents for mankind. These plants are widely used in traditional medicinal systems and folk medicines. The present study analyzed the nutritional and proximate composition of various compounds in selected wild plants available in the UAE, viz., Chenopodium murale L., Dipterygium glaucum Decne., Heliotropium digynum Asch. ex C.Chr., Heliotropium kotschyi Gürke., Salsola imbricata Forssk., Tribulus pentandrus Forssk., Zygophyllum qatarense Hadidi. The predominant amino acids detected in the plants were glycine, threonine, histidine, cysteine, proline, serine, and tyrosine; the highest quantities were observed in H. digynum and T. pentandrus. The major fatty acids present were long-chain saturated fatty acids; however, lauric acid was only present in S. imbricata. The presence of essential fatty acids such as oleic acid, α-Linoleic acid, and linolenic acid was observed in H. digynum, S. imbricata, and H. kotschyi. These plants also exhibited higher content of nutrients such as carbohydrates, proteins, fats, ash, and fiber. The predominant vitamins in the plants were vitamin B complex and vitamin C. C. murale had higher vitamin A, whereas vitamin B complex was seen in T. pentandrus and D. glaucum. The phosphorus and zinc content were high in T. pentandrus; the nitrogen, calcium, and potassium contents were high in H. digynum, and D. glaucum. Overall, these plants, especially H. digynum and T. pentandrus contain high amounts of nutritionally active compounds and important antioxidants including trace elements and vitamins. The results from the experiment provide an understanding of the nutritional composition of these desert plant species and can be better utilized as important agents for pharmacological drug discovery, food, and sustainable livestock production in the desert ecosystem. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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16 pages, 1700 KiB  
Article
Screening of Active Ingredients from Wendan Decoction in Alleviating Palmitic Acid-Induced Endothelial Cell Injury
by Nan Xu, Muhammad Ijaz, Haiyan Shi, Muhammad Shahbaz, Meichao Cai, Ping Wang, Xiuli Guo and Lei Ma
Molecules 2023, 28(3), 1328; https://doi.org/10.3390/molecules28031328 - 30 Jan 2023
Cited by 3 | Viewed by 1579
Abstract
(1) Objective: Traditional Chinese medicine (TCM) plays an important role in the treatment of numerous illnesses. As a classic Chinese medicine, Wendan Decoction (WDD) encompasses a marvelous impact on the remedy of hyperlipidemia. It is known that hyperlipidemia leads to cardiovascular injury, therefore [...] Read more.
(1) Objective: Traditional Chinese medicine (TCM) plays an important role in the treatment of numerous illnesses. As a classic Chinese medicine, Wendan Decoction (WDD) encompasses a marvelous impact on the remedy of hyperlipidemia. It is known that hyperlipidemia leads to cardiovascular injury, therefore anti-vascular endothelial cell injury (AVECI) may be an underlying molecular mechanism of WDD in the cure of hyperlipidemia. However, there is no relevant research on the effect of WDD on vascular endothelial cells and its pharmacodynamic substances. Therefore, the purpose of this study was to investigate the protective effect of WDD on vascular endothelial cells. (2) Methods: The chemical constituents of WDD were determined by LC-MS/MS technology. The protective effects of 16 batches of WDD on samples from human umbilical vein endothelial cells (HUVECs) were evaluated. Finally, gray relation analysis (GRA) and partial least squares regression (PLSR) were used to analyze the potential correlation between chemical ingredients and AVECI. (3) Results: The results indicated that WDD had apparent protective effect on endothelial cells, and pharmacological properties in 16 batches of WDD tests were apparently discrepant. The GRA and PLSR showed that trigonelline, liquiritin, hesperidin, hesperetin, scopoletin, morin, quercetin, isoliquiritigenin, liquiritigenin and formononetin may be the active ingredients of AVECI in WDD. (4) Conclusions: WDD has a protective effect on endothelial cell injury induced by palmitic acid, which may be related to its component content. This method was suitable for the search of active components in classical TCM. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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13 pages, 1784 KiB  
Article
Root Bark Extract of Oroxylum indicum Vent. Inhibits Solid and Ascites Tumors and Prevents the Development of DMBA-Induced Skin Papilloma Formation
by Seema Menon, Jawaher J. Albaqami, Hamida Hamdi, Lincy Lawrence, Menon Kunnathully Divya, Liya Antony, Jose Padikkala, Shaji E. Mathew and Arunaksharan Narayanankutty
Molecules 2022, 27(23), 8459; https://doi.org/10.3390/molecules27238459 - 02 Dec 2022
Cited by 2 | Viewed by 1448
Abstract
Oroxylum indicum is a traditionally used plant in Ayurvedic and folk medicines. The plant is useful for the management of gastrointestinal diseases as well as skin diseases. In the present study, we analyzed the antitumor potential of O. indicum in Dalton’s lymphoma ascites [...] Read more.
Oroxylum indicum is a traditionally used plant in Ayurvedic and folk medicines. The plant is useful for the management of gastrointestinal diseases as well as skin diseases. In the present study, we analyzed the antitumor potential of O. indicum in Dalton’s lymphoma ascites tumor cells (DLA) and Ehrlich ascites carcinoma (EAC)-induced solid and ascites tumors. Further, the potential of O. indicum extract (OIM) on skin papilloma induction by dimethyl benz(a) anthracene (DMBA) and croton oil was evaluated. The chemical composition of the extract was analyzed using UPLC-Q-TOF-MS. The predominant compounds present in the extract were demethoxycentaureidin 7-O-rutinoside, isorhamnetin-3-O-rutinoside, baicalein-7-O-glucuronide, 5,6,7-trihydroxyflavone, 3-Hydroxy-3′,4′,5′-trimethoxyflavone, 5,7-dihydroxy-3-(4-methoxyphenyl) chromen-4-one, and 4′-Hydroxy-5,7-dimethoxyflavanone. Treatment with high-dose OIM enhanced the percentage of survival in ascites tumor-bearing mice by 34.97%. Likewise, high and low doses of OIM reduced the tumor volume in mice by 61.84% and 54.21%, respectively. Further, the skin papilloma formation was brought down by the administration of low- and high-dose groups of OIM (by 67.51% and 75.63%). Overall, the study concludes that the Oroxylum indicum root bark extract is a potentially active antitumor and anticancer agent. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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11 pages, 917 KiB  
Article
Chemical Composition, Antioxidant, Anti-Bacterial, and Anti-Cancer Activities of Essential Oils Extracted from Citrus limetta Risso Peel Waste Remains after Commercial Use
by Arunaksharan Narayanankutty, Naduvilthara U. Visakh, Anju Sasidharan, Berin Pathrose, Opeyemi Joshua Olatunji, Abdullah Al-Ansari, Ahmed Alfarhan and Varsha Ramesh
Molecules 2022, 27(23), 8329; https://doi.org/10.3390/molecules27238329 - 29 Nov 2022
Cited by 10 | Viewed by 2192
Abstract
Citrus plants are widely utilized for edible purposes and medicinal utility throughout the world. However, because of the higher abundance of the antimicrobial compound D-Limonene, the peel waste cannot be disposed of by biogas production. Therefore, after the extraction of D-Limonene from the [...] Read more.
Citrus plants are widely utilized for edible purposes and medicinal utility throughout the world. However, because of the higher abundance of the antimicrobial compound D-Limonene, the peel waste cannot be disposed of by biogas production. Therefore, after the extraction of D-Limonene from the peel wastes, it can be easily disposed of. The D-Limonene rich essential oil from the Citrus limetta risso (CLEO) was extracted and evaluated its radical quenching, bactericidal, and cytotoxic properties. The radical quenching properties were DPPH radical scavenging (11.35 ± 0.51 µg/mL) and ABTS scavenging (10.36 ± 0.55 µg/mL). There, we observed a dose-dependent antibacterial potential for the essential oil against pathogenic bacteria. Apart from that, the essential oil also inhibited the biofilm-forming properties of E. coli, P. aeruginosa, S. enterica, and S. aureus. Further, cytotoxicity was also exhibited against estrogen receptor-positive (MCF7) cells (IC50: 47.31 ± 3.11 µg/mL) and a triple-negative (MDA-MB-237) cell (IC50: 55.11 ± 4.62 µg/mL). Upon evaluation of the mechanism of action, the toxicity was mediated through an increased level of reactive radicals of oxygen and the subsequent release of cytochrome C, indicative of mitotoxicity. Hence, the D-Limonene rich essential oil of C. limetta is useful as a strong antibacterial and cytotoxic agent; the antioxidant properties exhibited also increase its utility value. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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11 pages, 820 KiB  
Article
Antioxidant, Antimicrobial, Cytotoxicity, and Larvicidal Activities of Selected Synthetic Bis-Chalcones
by Aswathi Moothakoottil Kuttithodi, Divakaran Nikhitha, Jisha Jacob, Arunaksharan Narayanankutty, Manoj Mathews, Opeyemi Joshua Olatunji, Rajakrishnan Rajagopal, Ahmed Alfarhan and Damia Barcelo
Molecules 2022, 27(23), 8209; https://doi.org/10.3390/molecules27238209 - 25 Nov 2022
Cited by 4 | Viewed by 1623
Abstract
Plants are known to have numerous phytochemicals and other secondary metabolites with numerous pharmacological and biological properties. Among the various compounds, polyphenols, flavonoids, anthocyanins, alkaloids, and terpenoids are the predominant ones that have been explored for their biological potential. Among these, chalcones and [...] Read more.
Plants are known to have numerous phytochemicals and other secondary metabolites with numerous pharmacological and biological properties. Among the various compounds, polyphenols, flavonoids, anthocyanins, alkaloids, and terpenoids are the predominant ones that have been explored for their biological potential. Among these, chalcones and bis-chalcones are less explored for their biological potential under in vitro experiments, cell culture models, and animal studies. In the present study, we evaluated six synthetic bis-chalcones that were different in terms of their aromatic cores, functional group substitution, and position of substitutions. The results indicated a strong antioxidant property in terms of DPPH and ABTS radical-scavenging potentials and ferric-reducing properties. In addition, compounds 1, 2, and 4 exhibited strong antibacterial activities against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Salmonella enteritidis. The disc diffusion assay values were indicative of the antibacterial properties of these compounds. Overall, the study indicated the antioxidant and antimicrobial properties of the compounds. Our preliminary studies point to the potential of this class of compounds for further in vivo investigation. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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11 pages, 2107 KiB  
Article
The Chemical Composition and Antimitotic, Antioxidant, Antibacterial and Cytotoxic Properties of the Defensive Gland Extract of the Beetle, Luprops tristis Fabricius
by Ovungal Sabira, Attuvalappil Ramdas Vignesh, Anthyalam Parambil Ajaykumar, Sudhir Rama Varma, Kodangattil Narayanan Jayaraj, Merin Sebastin, Kalleringal Nikhila, Annet Babu, Vazhanthodi Abdul Rasheed, Valiyaparambil Sivadasan Binitha, Zeena koldath Vasu and Madathilpadi Subrahmanian Sujith
Molecules 2022, 27(21), 7476; https://doi.org/10.3390/molecules27217476 - 02 Nov 2022
Cited by 5 | Viewed by 2428
Abstract
The unpredictable invasion of the Mupli beetle, Luprops tristis Fabricius (Coleoptera: Tenebrionidae), makes areas uninhabitable to humans. These beetles produce a strong-smelling, irritating secretion as a defence mechanism, which causes blisters on contact with human skin. In the current study, gas chromatography high-resolution [...] Read more.
The unpredictable invasion of the Mupli beetle, Luprops tristis Fabricius (Coleoptera: Tenebrionidae), makes areas uninhabitable to humans. These beetles produce a strong-smelling, irritating secretion as a defence mechanism, which causes blisters on contact with human skin. In the current study, gas chromatography high-resolution mass spectrometry (GC-HRMS) analysis of the defensive gland extract of the Mupli beetle revealed the presence of compounds such as 2,3,dimethyl-1,4-benzoquinone, 1,3-dihydroxy-2-methylbenzene, 2,5-dimethyl hydroquinone, tetracosane, oleic acid, hexacosane, pentacosane, 7-hexadecenal and tert-hexadecanethiol. The defensive gland extracts showed considerable antibacterial activity on Gram-negative and Gram-positive bacteria in an agar diffusion assay. The chromosomal aberration analysis using root tips of Allium cepa L. exposed to the defensive secretion showed chromosomal aberrations such as disturbed metaphase, sticky chromosomes and chromosomal breakage. The antioxidant activity of the extract was determined using a radical scavenging (DPPH) assay. A cytotoxic assay of the defensive gland extract against Dalton’s lymphoma ascites (DLA) cell line showed anticancer properties. In the present study, the defensive gland extract of the Mupli beetle, L. tristis, which is generally perceived as a nuisance insect to humans, was found to have beneficial biological activities. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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14 pages, 634 KiB  
Article
Fatty-Acid-Rich Agave angustifolia Fraction Shows Antiarthritic and Immunomodulatory Effect
by Enrique Jiménez-Ferrer, Gabriela Vargas-Villa, Gabriela Belen Martínez-Hernández, Manases González-Cortazar, Alejandro Zamilpa, Maribel Patricia García-Aguilar, Martha Lucía Arenas-Ocampo and Maribel Herrera-Ruiz
Molecules 2022, 27(21), 7204; https://doi.org/10.3390/molecules27217204 - 24 Oct 2022
Cited by 3 | Viewed by 1294
Abstract
Agave angustifolia is a xerophytic species widely used in Mexico as an ingredient in sweet food and fermented beverages; it is also used in traditional medicine to treat wound pain and rheumatic damage, and as a remedy for psoriasis. Among the various A. [...] Read more.
Agave angustifolia is a xerophytic species widely used in Mexico as an ingredient in sweet food and fermented beverages; it is also used in traditional medicine to treat wound pain and rheumatic damage, and as a remedy for psoriasis. Among the various A. angustifolia extracts and extract fractions that have been evaluated for their anti-inflammatory effects, the acetonic extract (AaAc) and its acetonic (F-Ac) and methanolic (F-MeOH) fractions were the most active in a xylene-induced ear edema model in mice, when orally administered. Four fractions resulting from chemically resolving F-Ac (F1–F4) were locally applied to mice with phorbol 12-myristate 13-acetate (TPA)-induced ear inflammation; F1 inhibited inflammation by 70% and was further evaluated in a carrageenan-induced mono-arthritis model. When administered at doses of 12.5, 25, and 50 mg/kg, F1 reduced articular edema and the spleen index. In addition, it modulated spleen and joint cytokine levels and decreased pain. According to a GC–MS analysis, the main components of F1 are fatty-acid derivatives: palmitic acid methyl ester, palmitic acid ethyl ester, octadecenoic acid methyl ester, linoleic acid ethyl ester, and oleic acid ethyl ester. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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12 pages, 692 KiB  
Article
Phytochemical Composition and In Vitro Antioxidant, Anti-Inflammatory, Anticancer, and Enzyme-Inhibitory Activities of Artemisia nilagirica (C.B. Clarke) Pamp
by Jawaher J. Albaqami, Tancia P. Benny, Hamida Hamdi, Ammar B. Altemimi, Aswathi Moothakoottil Kuttithodi, Joice Tom Job, Anju Sasidharan and Arunaksharan Narayanankutty
Molecules 2022, 27(20), 7119; https://doi.org/10.3390/molecules27207119 - 21 Oct 2022
Cited by 2 | Viewed by 1732
Abstract
Plants have been employed in therapeutic applications against various infectious and chronic diseases from ancient times. Various traditional medicines and folk systems have utilized numerous plants and plant products, which act as sources of drug candidates for modern medicine. Artemisia is a genus [...] Read more.
Plants have been employed in therapeutic applications against various infectious and chronic diseases from ancient times. Various traditional medicines and folk systems have utilized numerous plants and plant products, which act as sources of drug candidates for modern medicine. Artemisia is a genus of the Asteraceae family with more than 500 species; however, many of these species are less explored for their biological efficacy, and several others are lacking scientific explanations for their uses. Artemisia nilagirica is a plant that is widely found in the Western Ghats, Kerala, India and is a prominent member of the genus. In the current study, the phytochemical composition and the antioxidant, enzyme-inhibitory, anti-inflammatory, and anticancer activities were examined. The results indicated that the ethanol extract of A. nilagirica indicated in vitro DPPH scavenging (23.12 ± 1.28 µg/mL), ABTS scavenging (27.44 ± 1.88 µg/mL), H2O2 scavenging (12.92 ± 1.05 µg/mL), and FRAP (5.42 ± 0.19 µg/mL). The anti-inflammatory effect was also noticed in the Raw 264.7 macrophages, where pretreatment with the extract reduced the LPS-stimulated production of cytokines (p < 0.05). A. nilagirica was also efficient in inhibiting the activities of α-amylase (38.42 ± 2.71 µg/mL), α-glucosidase (55.31 ± 2.16 µg/mL), aldose reductase (17.42 ± 0.87 µg/mL), and sorbitol dehydrogenase (29.57 ± 1.46 µg/mL). It also induced significant inhibition of proliferation in breast (MCF7 IC50 = 41.79 ± 1.07, MDAMB231 IC50 = 55.37 ± 2.11µg/mL) and colon (49.57 ± 1.46 µg/mL) cancer cells. The results of the phytochemical screening indicated a higher level of polyphenols and flavonoids in the extract and the LCMS analysis revealed the presence of various bioactive constituents including artemisinin. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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13 pages, 3458 KiB  
Article
Evaluation of the Anti-Cancer Potential of Rosa damascena Mill. Callus Extracts against the Human Colorectal Adenocarcinoma Cell Line
by Hadeer Darwish, Sarah Alharthi, Radwa A. Mehanna, Samar S. Ibrahim, Mustafa A. Fawzy, Saqer S. Alotaibi, Sarah M. Albogami, Bander Albogami, Sedky H. A. Hassan and Ahmed Noureldeen
Molecules 2022, 27(19), 6241; https://doi.org/10.3390/molecules27196241 - 22 Sep 2022
Cited by 3 | Viewed by 1690
Abstract
Chemotherapy is an aggressive form of chemical drug therapy aiming to destroy cancer cells. Adjuvant therapy may reduce hazards of chemotherapy and help in destroying these cells when obtained from natural products, such as medical plants. In this study, the potential therapeutic effect [...] Read more.
Chemotherapy is an aggressive form of chemical drug therapy aiming to destroy cancer cells. Adjuvant therapy may reduce hazards of chemotherapy and help in destroying these cells when obtained from natural products, such as medical plants. In this study, the potential therapeutic effect of Rosa damascena callus crude extract produced in vitamin-enhanced media is investigated on colorectal cancer cell line Caco-2. Two elicitors, i.e., L-ascorbic acid and citric acid at a concentration of 0.5 g/L were added to the callus induction medium. Callus extraction and the GC–MS analysis of methanolic crude extracts were also determined. Cytotoxicity, clonogenicity, proliferation and migration of Caco-2 colorectal cancer cells were investigated using MTT cytotoxicity, colony-forming, Ki-67 flow cytometry proliferation and Migration Scratch assays, respectively. Our results indicated that L-ascorbic acid treatment enhanced callus growth parameters and improved secondary metabolite contents. It showed the least IC50 value of 137 ug/mL compared to 237 ug/mL and 180 ug/mL in the citric acid-treated and control group. We can conclude that R. damascena callus elicited by L-ascorbic acid improved growth and secondary metabolite contents as well as having an efficient antiproliferative, anti-clonogenic and anti-migratory effect on Caco-2 cancer cells, thus, can be used as an adjuvant anti-cancer therapy. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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14 pages, 1594 KiB  
Article
Chemical Composition and Antioxidant, Antiviral, Antifungal, Antibacterial and Anticancer Potentials of Opuntia ficus-indica Seed Oil
by Abeer S. Alqurashi, Luluah M. Al Masoudi, Hamida Hamdi and Abeer Abu Zaid
Molecules 2022, 27(17), 5453; https://doi.org/10.3390/molecules27175453 - 25 Aug 2022
Cited by 6 | Viewed by 1982
Abstract
Opuntia ficus-indica (OFI) is a cactus that is widely cultivated in the Kingdom of Saudi Arabia especially in the Taif region due to its favorable weather for growing, and it has benefits as a food and traditional medicine. The aim of the current [...] Read more.
Opuntia ficus-indica (OFI) is a cactus that is widely cultivated in the Kingdom of Saudi Arabia especially in the Taif region due to its favorable weather for growing, and it has benefits as a food and traditional medicine. The aim of the current study was to chemically characterize Opuntia ficus-indica seed oil from Taif, Kingdom of Saudi Arabia, using GC-MS and HPLC analysis and evaluate its antioxidant, antiviral, antifungal, antibacterial and anticancer activities. Linolenic acid was the dominating fatty acid in OFI oil, followed by oleic acid, linoleic acid, palmitic acid and stearic acid. Total tocopherol (α-, β-, Ɣ-tocopherol) was found to be 24.02 μg/mL. Campesterol was the main phytosterol, followed by γ- & β -sitosterol, and Stigmasterol. The phenolic components scored 30.5 mg gallic acid equivalent per ml of oil with 89.2% antioxidant activity (% DPPH radical inhibition) at 200 µL/mL of OFI oil. OFI oil showed an inhibition efficacy against microbial strains especially Saccharomyces cervisiae with a diameter (28.3 ± 0.4), MBC (15 µg/mL) and MIC bacteriostatic (10 µg/mL). While OFI oil had no effect against Aspergillus niger, OFI oil showed weak inhibitory activity against A-2780 (Ovarian carcinoma) cell line, although it showed significant inhibitory activity against PC-3 (Prostate carcinoma) cell line. OFI oil exhibited an antiviral effect (22.67 ± 2.79%) at 300 µg/mL of Oil against herpes simplex type 2 (HSV-2) virus. The bioactive compounds of OFI oil, as well as its main biological activities, make it a promising candidate for the non-communicable disease management. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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24 pages, 3997 KiB  
Article
Assessment of Cosmetic Properties and Safety of Use of Model Washing Gels with Reishi, Maitake and Lion’s Mane Extracts
by Aleksandra Ziemlewska, Magdalena Wójciak, Kamila Mroziak-Lal, Martyna Zagórska-Dziok, Tomasz Bujak, Zofia Nizioł-Łukaszewska, Dariusz Szczepanek and Ireneusz Sowa
Molecules 2022, 27(16), 5090; https://doi.org/10.3390/molecules27165090 - 10 Aug 2022
Cited by 1 | Viewed by 2552
Abstract
Natural cosmetics are becoming more and more popular every day. For this reason, this work investigates the properties of mushroom extracts, which are not as widely used in the cosmetics industry as plant ingredients. Water extracts of Grifolafrondosa (Maitake), Hericiumerinaceus (Lion’s Mane) and [...] Read more.
Natural cosmetics are becoming more and more popular every day. For this reason, this work investigates the properties of mushroom extracts, which are not as widely used in the cosmetics industry as plant ingredients. Water extracts of Grifolafrondosa (Maitake), Hericiumerinaceus (Lion’s Mane) and Ganoderma lucidum (Reishi) were tested for their antioxidant properties, bioactive substances content, skin cell toxicity, ability to limit TEWL, effect on skin hydration and pH, and skin irritation. Our research showed that Maitake extract contained the highest amount of flavonoids and phenols, and also showed the most effective scavenging of DPPH and ABTS radicals as well as Chelation of Fe2+ and FRAP radicals, which were 39.84% and 82.12% in a concentration of 1000 µg/mL, respectively. All tested extracts did not increase the amount of ROS in fibroblasts and keratinocytes. The addition of mushroom extracts to washing gels reduced the irritating effect on skin, and reduced the intracellular production of free radicals, compared with the cosmetic base. Moreover, it was shown that the analyzedcosmetics had a positive effect on the pH and hydration of the skin, and reduced TEWL. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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20 pages, 4084 KiB  
Article
Improvement in Solubility–Permeability Interplay of Psoralens from Brosimum gaudichaudii Plant Extract upon Complexation with Hydroxypropyl-β-cyclodextrin
by Rúbia Darc Machado, Júlio C. G. Silva, Luís A. D. Silva, Gerlon de A. R. Oliveira, Luciano M. Lião, Eliana M. Lima, Mariana C. de Morais, Edemilson C. da Conceição and Kênnia R. Rezende
Molecules 2022, 27(14), 4580; https://doi.org/10.3390/molecules27144580 - 19 Jul 2022
Viewed by 1625
Abstract
Psoralen (PSO) and 5-methoxypsoralen (5-MOP) are widely used drugs in oral photochemotherapy against vitiligo and major bioactive components of root bark extract of Brosimum gaudichaudii Trécul (EBGT), previously standardized by LC-MS. However, the exceptionally low water solubility of these psoralens can cause incomplete [...] Read more.
Psoralen (PSO) and 5-methoxypsoralen (5-MOP) are widely used drugs in oral photochemotherapy against vitiligo and major bioactive components of root bark extract of Brosimum gaudichaudii Trécul (EBGT), previously standardized by LC-MS. However, the exceptionally low water solubility of these psoralens can cause incomplete and variable bioavailability limiting their applications and patient adherence to treatment. Therefore, the purpose of this work was to investigate the effects of 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex on the solubility and jejunal permeability of PSO and 5-MOP from EBGT. Characterization of inclusion complexes were evaluated by current methods in nuclear magnetic resonance studies on aqueous solution, Fourier transform infrared spectroscopy, thermal analysis, and scanning electron microscopy in solid state. Ex vivo rat jejunal permeability was also investigated and compared for both pure psoralens and plant extract formulation over a wide HP-β-CD concentration range (2.5 to 70 mM). Phase solubility studies of the PSO- and 5-MOP-HP-β-CD inclusion complex showed 1:1 inclusion complex formation with small stability constants (Kc < 500 M−1). PSO and 5-MOP permeability rate decreased after adding HP-β-CD by 6- and 4-fold for pure standards and EBGT markers, respectively. Nevertheless, the complexation with HP-β-CD significantly improved solubility of PSO (until 10-fold) and 5-MOP (until 31-fold). As a result, the permeability drop could be overcome by solubility augmentation, implying that the HP-β-CD inclusion complexes with PSO, 5-MOP, or EBGT can be a valuable tool for designing and developing novel oral drug product formulation containing these psoralens for the treatment of vitiligo. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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Review

Jump to: Research

32 pages, 2719 KiB  
Review
Flavonoids with Anti-Angiogenesis Function in Cancer
by Qiang Wei and Yi-han Zhang
Molecules 2024, 29(7), 1570; https://doi.org/10.3390/molecules29071570 - 31 Mar 2024
Viewed by 662
Abstract
The formation of new blood vessels, known as angiogenesis, significantly impacts the development of multiple types of cancer. Consequently, researchers have focused on targeting this process to prevent and treat numerous disorders. However, most existing anti-angiogenic treatments rely on synthetic compounds and humanized [...] Read more.
The formation of new blood vessels, known as angiogenesis, significantly impacts the development of multiple types of cancer. Consequently, researchers have focused on targeting this process to prevent and treat numerous disorders. However, most existing anti-angiogenic treatments rely on synthetic compounds and humanized monoclonal antibodies, often expensive or toxic, restricting patient access to these therapies. Hence, the pursuit of discovering new, affordable, less toxic, and efficient anti-angiogenic compounds is imperative. Numerous studies propose that natural plant-derived products exhibit these sought-after characteristics. The objective of this review is to delve into the anti-angiogenic properties exhibited by naturally derived flavonoids from plants, along with their underlying molecular mechanisms of action. Additionally, we summarize the structure, classification, and the relationship between flavonoids with their signaling pathways in plants as anti-angiogenic agents, including main HIF-1α/VEGF/VEGFR2/PI3K/AKT, Wnt/β-catenin, JNK1/STAT3, and MAPK/AP-1 pathways. Nonetheless, further research and innovative approaches are required to enhance their bioavailability for clinical application. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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24 pages, 9266 KiB  
Review
Phytocompounds from Amazonian Plant Species against Acute Kidney Injury: Potential Nephroprotective Effects
by Alberto Souza Paes, Rosemary de Carvalho Rocha Koga, Priscila Faimann Sales, Hellen Karine Santos Almeida, Thiago Afonso Carvalho Celestino Teixeira and José Carlos Tavares Carvalho
Molecules 2023, 28(17), 6411; https://doi.org/10.3390/molecules28176411 - 02 Sep 2023
Cited by 1 | Viewed by 1569
Abstract
There are several Amazonian plant species with potential pharmacological validation for the treatment of acute kidney injury, a condition in which the kidneys are unable to adequately filter the blood, resulting in the accumulation of toxins and waste in the body. Scientific production [...] Read more.
There are several Amazonian plant species with potential pharmacological validation for the treatment of acute kidney injury, a condition in which the kidneys are unable to adequately filter the blood, resulting in the accumulation of toxins and waste in the body. Scientific production on plant compounds capable of preventing or attenuating acute kidney injury—caused by several factors, including ischemia, toxins, and inflammation—has shown promising results in animal models of acute kidney injury and some preliminary studies in humans. Despite the popular use of Amazonian plant species for kidney disorders, further pharmacological studies are needed to identify active compounds and subsequently conduct more complex preclinical trials. This article is a brief review of phytocompounds with potential nephroprotective effects against acute kidney injury (AKI). The classes of Amazonian plant compounds with significant biological activity most evident in the consulted literature were alkaloids, flavonoids, tannins, steroids, and terpenoids. An expressive phytochemical and pharmacological relevance of the studied species was identified, although with insufficiently explored potential, mainly in the face of AKI, a clinical condition with high morbidity and mortality. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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22 pages, 2402 KiB  
Review
A Comprehensive Review on Bioactive Compounds Found in Caesalpinia sappan
by Twinkle Vij, Pawase Prashant Anil, Rafeeya Shams, Kshirod Kumar Dash, Rhythm Kalsi, Vinay Kumar Pandey, Endre Harsányi, Béla Kovács and Ayaz Mukarram Shaikh
Molecules 2023, 28(17), 6247; https://doi.org/10.3390/molecules28176247 - 25 Aug 2023
Cited by 5 | Viewed by 2617
Abstract
Sappan wood (Caesalpinia sappan) is a tropical hardwood tree found in Southeast Asia. Sappan wood contains a water-soluble compound, which imparts a red color named brazilin. Sappan wood is utilized to produce dye for fabric and coloring agents for food and [...] Read more.
Sappan wood (Caesalpinia sappan) is a tropical hardwood tree found in Southeast Asia. Sappan wood contains a water-soluble compound, which imparts a red color named brazilin. Sappan wood is utilized to produce dye for fabric and coloring agents for food and beverages, such as wine and meat. As a valuable medicinal plant, the tree is also known for its antioxidant, anti-inflammatory, and anticancer properties. It has been observed that sappan wood contains various bioactive compounds, including brazilin, brazilein, sappan chalcone, and protosappanin A. It has also been discovered that these substances have various health advantages; they lower inflammation, enhance blood circulation, and are anti-oxidative in nature. Sappan wood has been used as a medicine to address a range of illnesses, such as gastrointestinal problems, respiratory infections, and skin conditions. Studies have also suggested that sappan wood may have anticarcinogenic potential as it possesses cytotoxic activity against cancer cells. Based on this, the present review emphasized the different medicinal properties, the role of phytochemicals, their health benefits, and several food and nonfood applications of sappan wood. Overall, sappan wood has demonstrated promising medicinal properties and is an important resource in traditional medicine. The present review has explored the potential role of sappan wood as an essential source of bioactive compounds for drug development. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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15 pages, 334 KiB  
Review
Medicinal Mushrooms: Their Bioactive Components, Nutritional Value and Application in Functional Food Production—A Review
by Paulina Łysakowska, Aldona Sobota and Anna Wirkijowska
Molecules 2023, 28(14), 5393; https://doi.org/10.3390/molecules28145393 - 14 Jul 2023
Cited by 15 | Viewed by 8561
Abstract
Medicinal mushrooms, e.g., Lion’s Mane (Hericium erinaceus (Bull.) Pers.), Reishi (Ganoderma lucidum (Curtis) P. Karst.), Chaga (Inonotus obliquus (Ach. ex Pers.) Pilát), Cordyceps (Ophiocordyceps sinensis (Berk.) G.H. Sung, J.M. Sung, Hywel-Jones and Spatafora), Shiitake (Lentinula edodes (Berk.) Pegler), [...] Read more.
Medicinal mushrooms, e.g., Lion’s Mane (Hericium erinaceus (Bull.) Pers.), Reishi (Ganoderma lucidum (Curtis) P. Karst.), Chaga (Inonotus obliquus (Ach. ex Pers.) Pilát), Cordyceps (Ophiocordyceps sinensis (Berk.) G.H. Sung, J.M. Sung, Hywel-Jones and Spatafora), Shiitake (Lentinula edodes (Berk.) Pegler), and Turkey Tail (Trametes versicolor (L.) Lloyd), are considered new-generation foods and are of growing interest to consumers. They are characterised by a high content of biologically active compounds, including (1,3)(1,6)-β-d-glucans, which are classified as dietary fibre, triterpenes, phenolic compounds, and sterols. Thanks to their low-fat content, they are a low-calorie product and are classified as a functional food. They have a beneficial effect on the organism through the improvement of its overall health and nutritional level. The biologically active constituents contained in medicinal mushrooms exhibit anticancer, antioxidant, antidiabetic, and immunomodulatory effects. In addition, these mushrooms accelerate metabolism, help fight obesity, and slow down the ageing processes thanks to their high antioxidant activity. The vast therapeutic properties of mushrooms are still not fully understood. Detailed mechanisms of the effects of medicinal mushrooms on the human organism still require long-term clinical studies to confirm their nutraceutical effects, their safety of use, and their dosage. Medicinal mushrooms have great potential to be used in the design of innovative functional foods. There is a need for further research on the possibility of incorporating mushrooms into food products to assess the interactions of their bioactive substances with ingredients in the food matrix. This review focuses on the properties of selected medicinal mushrooms and their effects on the human organism and presents current knowledge on the possibilities of their use in the production of functional foods. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
25 pages, 1980 KiB  
Review
Long Non-Coding RNAs as Novel Targets for Phytochemicals to Cease Cancer Metastasis
by Sadegh Rajabi, Huda Fatima Rajani, Niloufar Mohammadkhani, Andrés Alexis Ramírez-Coronel, Mahsa Maleki, Marc Maresca and Homa Hajimehdipoor
Molecules 2023, 28(3), 987; https://doi.org/10.3390/molecules28030987 - 18 Jan 2023
Cited by 3 | Viewed by 1896
Abstract
Metastasis is a multi-step phenomenon during cancer development leading to the propagation of cancer cells to distant organ(s). According to estimations, metastasis results in over 90% of cancer-associated death around the globe. Long non-coding RNAs (LncRNAs) are a group of regulatory RNA molecules [...] Read more.
Metastasis is a multi-step phenomenon during cancer development leading to the propagation of cancer cells to distant organ(s). According to estimations, metastasis results in over 90% of cancer-associated death around the globe. Long non-coding RNAs (LncRNAs) are a group of regulatory RNA molecules more than 200 base pairs in length. The main regulatory activity of these molecules is the modulation of gene expression. They have been reported to affect different stages of cancer development including proliferation, apoptosis, migration, invasion, and metastasis. An increasing number of medical data reports indicate the probable function of LncRNAs in the metastatic spread of different cancers. Phytochemical compounds, as the bioactive agents of plants, show several health benefits with a variety of biological activities. Several phytochemicals have been demonstrated to target LncRNAs to defeat cancer. This review article briefly describes the metastasis steps, summarizes data on some well-established LncRNAs with a role in metastasis, and identifies the phytochemicals with an ability to suppress cancer metastasis by targeting LncRNAs. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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23 pages, 1470 KiB  
Review
Maslinic Acid: A New Compound for the Treatment of Multiple Organ Diseases
by Yan He, Yi Wang, Kun Yang, Jia Jiao, Hong Zhan, Youjun Yang, De Lv, Weihong Li and Weijun Ding
Molecules 2022, 27(24), 8732; https://doi.org/10.3390/molecules27248732 - 09 Dec 2022
Cited by 8 | Viewed by 2551
Abstract
Maslinic acid (MA) is a pentacyclic triterpene acid, which exists in many plants, including olive, and is highly safe for human beings. In recent years, it has been reported that MA has anti-inflammatory, antioxidant, anti-tumor, hypoglycemic, neuroprotective and other biological activities. More and [...] Read more.
Maslinic acid (MA) is a pentacyclic triterpene acid, which exists in many plants, including olive, and is highly safe for human beings. In recent years, it has been reported that MA has anti-inflammatory, antioxidant, anti-tumor, hypoglycemic, neuroprotective and other biological activities. More and more experimental data has shown that MA has a good therapeutic effect on multiple organ diseases, indicating that it has great clinical application potential. In this paper, the extraction, purification, identification and analysis, biological activity, pharmacokinetics in vivo and molecular mechanism of MA in treating various organ diseases are reviewed. It is hoped to provide a new idea for MA to treat various organ diseases. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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23 pages, 2851 KiB  
Review
Collection of Hairy Roots as a Basis for Fundamental and Applied Research
by Anna Yurievna Stepanova, Maria Viktorovna Malunova, Evgeny Aleksandrovich Gladkov, Sergey Viktorovich Evsyukov, Dmitry Viktorovich Tereshonok and Aleksandra Ivanovna Solov’eva
Molecules 2022, 27(22), 8040; https://doi.org/10.3390/molecules27228040 - 19 Nov 2022
Cited by 11 | Viewed by 1976
Abstract
Due to population growth, instability of climatic conditions, and reduction of the areas of natural ecosystems, it becomes necessary to involve modern biotechnological approaches to obtain highly productive plant material. This statement applies both to the creation of plant varieties and the production [...] Read more.
Due to population growth, instability of climatic conditions, and reduction of the areas of natural ecosystems, it becomes necessary to involve modern biotechnological approaches to obtain highly productive plant material. This statement applies both to the creation of plant varieties and the production of new pharmaceutical raw materials. Genetic transformation of valuable medicinal plants using Agrobacterium rhizogenes ensures the production of stable and rapidly growing hairy roots cultures that have a number of advantages compared with cell culture and, above all, can synthesize root-specific substances at the level of the roots of the intact plant. In this regard, special attention should be paid to the collection of hairy roots of the Institute of Plant Physiology RAS, Russian Academy of Sciences, the founder of which was Dr. Kuzovkina I.N. Currently, the collection contains 38 hairy roots lines of valuable medicinal and forage plants. The review discusses the prospects of creating a hairy roots collection as a basis for fundamental research and commercial purposes. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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25 pages, 4684 KiB  
Review
Application of Metabolomics in Fungal Research
by Guangyao Li, Tongtong Jian, Xiaojin Liu, Qingtao Lv, Guoying Zhang and Jianya Ling
Molecules 2022, 27(21), 7365; https://doi.org/10.3390/molecules27217365 - 29 Oct 2022
Cited by 13 | Viewed by 3975
Abstract
Metabolomics is an essential method to study the dynamic changes of metabolic networks and products using modern analytical techniques, as well as reveal the life phenomena and their inherent laws. Currently, more and more attention has been paid to the development of metabolic [...] Read more.
Metabolomics is an essential method to study the dynamic changes of metabolic networks and products using modern analytical techniques, as well as reveal the life phenomena and their inherent laws. Currently, more and more attention has been paid to the development of metabolic histochemistry in the fungus field. This paper reviews the application of metabolomics in fungal research from five aspects: identification, response to stress, metabolite discovery, metabolism engineering, and fungal interactions with plants. Full article
(This article belongs to the Special Issue Natural Bioactive Compounds and Human Health)
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