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Bioactive Compounds: From Extraction to Biological Evaluations

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

Deadline for manuscript submissions: closed (28 February 2023) | Viewed by 44820

Special Issue Editors


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Guest Editor
College of Veterinary Medicine, Jilin University, Changchun 130021, China
Interests: natural compound; virulence factor; resistance enzyme; anti-infection; gut microbiota
Special Issues, Collections and Topics in MDPI journals
Department of Pharmacy, Colleage of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, China
Interests: TCM; bioactive compounds; antibacterial compounds; host-directed therapy

Special Issue Information

Dear Colleagues,

Bioactive compounds, such as flavonoids, alkaloid, polysaccharose and essential oil, are secondary metabolites found in small quantities in various plants, especially in medicinal plants used in the traditional medicine. Bioactive compounds are capable of modulating metabolic processes and demonstrate positive properties such as antioxidant effect, inhibition of receptor activities, inhibition or induction of enzymes, and induction and inhibition of gene expression in host and pathogenic microorganisms. Bioactive compounds are the substance basis of pharmacology in medicinal plant (e.g., ginkgetin, artemisinin, berberine, paclitaxel, etc.), and the leading compounds for developing new drugs (salicylic acid, atropine, ephedrine, penicillin, etc.).

In this context, we are proposing a new Special Issue titled "Bioactive Compounds: From Extraction to Biological Evaluations". This Special Issue welcomes the submission of original research and review manuscripts focusing on bioactive compounds as substances for regulating the immunity, metabolism, oxidative stress, etc., of host, and for inhibition of the pathogenic microorganisms infection, as well as the study on extraction technology and chemical structure analysis of bioactive compounds.

Prof. Dr. Jianfeng Wang
Dr. Lizi Yin
Guest Editors

Manuscript Submission Information

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

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 compounds
  • extraction technology
  • chemical structure analysis
  • modulation of host
  • treatment of metabolic related diseases
  • antimicrobial activity
  • antiinfection

Published Papers (24 papers)

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Research

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20 pages, 8029 KiB  
Article
Tetramethylpyrazine Antagonizes the Subchronic Cadmium Exposure-Induced Oxidative Damage in Mouse Livers via the Nrf2/HO-1 Pathway
by Xue Hu, Siqi Zhao, Ziming Guo, Yiling Zhu, Shuai Zhang, Danqin Li and Gang Shu
Molecules 2024, 29(7), 1434; https://doi.org/10.3390/molecules29071434 - 22 Mar 2024
Viewed by 551
Abstract
Hepatic oxidative stress is an important mechanism of Cd-induced hepatotoxicity, and it is ameliorated by TMP. However, this underlying mechanism remains to be elucidated. To investigate the mechanism of the protective effect of TMP on liver injuries in mice induced by subchronic cadmium [...] Read more.
Hepatic oxidative stress is an important mechanism of Cd-induced hepatotoxicity, and it is ameliorated by TMP. However, this underlying mechanism remains to be elucidated. To investigate the mechanism of the protective effect of TMP on liver injuries in mice induced by subchronic cadmium exposure, 60 healthy male ICR mice were randomly divided into five groups of 12 mice each, namely, control (CON), Cd (2 mg/kg of CdCl2), Cd + 100 mg/kg of TMP, Cd + 150 mg/kg of TMP, and Cd + 200 mg/kg of TMP, and were acclimatized and fed for 7 d. The five groups of mice were gavaged for 28 consecutive days with a maximum dose of 0.2 mL/10 g/day. Except for the control group, all groups were given fluoride (35 mg/kg) by an intraperitoneal injection on the last day of the experiment. The results of this study show that compared with the Cd group, TMP attenuated CdCl2-induced pathological changes in the liver and improved the ultrastructure of liver cells, and TMP significantly decreased the MDA level (p < 0.05) and increased the levels of T-AOC, T-SOD, and GSH (p < 0.05). The results of mRNA detection show that TMP significantly increased the levels of Nrf2 in the liver compared with the Cd group as well as the HO-1 and mRNA expression levels in the liver (p < 0.05). In conclusion, TMP could inhibit oxidative stress and attenuate Cd group-induced liver injuries by activating the Nrf2 pathway. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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17 pages, 7216 KiB  
Article
Apigenin Inhibits the Progression of Osteoarthritis by Mediating Macrophage Polarization
by Xueyan Ji, Wei Du, Wenqing Che, Liping Wang and Lu Zhao
Molecules 2023, 28(7), 2915; https://doi.org/10.3390/molecules28072915 - 24 Mar 2023
Cited by 7 | Viewed by 1984
Abstract
Objective: The overall purpose of this study was to investigate the mechanism of macrophage polarization on chondrocyte injury in osteoarthritis and the protective effect of apigenin on chondrocytes in osteoarthritis. Method: Primary chondrocytes were isolated from the knee cartilage of three-day-old mice, and [...] Read more.
Objective: The overall purpose of this study was to investigate the mechanism of macrophage polarization on chondrocyte injury in osteoarthritis and the protective effect of apigenin on chondrocytes in osteoarthritis. Method: Primary chondrocytes were isolated from the knee cartilage of three-day-old mice, and cells positive for Alsine blue staining and type II collagen immunocytochemical staining were identified and used in followup experiments. Transwell coculture was performed. Chondrocytes were inoculated in the inferior compartment, and macrophages were inoculated in the upper compartment. The experimental groups were the N group, LPS group, and LPS+ apigenin group. The effect of macrophage polarization on chondrocyte inflammation and the protective effect of apigenin on chondrocytes were verified by the drug administration. Real-time quantitative PCR (qPCR) and Western blot were used to detect the expression of RNA and protein. Experimental OA was induced by modified Hulth surgery in mice. Modified Hulth surgery was performed on the mouse’s right knee to induce experimental osteoarthritis in mice, with the nonoperative right knee serving as an ipsilateral control. The mice were randomly assigned to three groups (six mice per group): the sham group, the modified Hulth group, and the modified Hulth + apigenin group. Animals were given gavage for four weeks. The protective effect of apigenin on articular cartilage was verified by histological staining and immunohistochemical analysis. Results: Histological staining showed that apigenin had a protective effect on cartilage degeneration induced by modified Hulth surgery. The PCR results showed that apigenin significantly reduced the expression levels of IL-1, IL-6, MMP3, and MMP13 in the articular cartilage of OA mice, and it had a protective effect on articular cartilage. Apigenin reduced the levels of IL-1, IL-6, TNF-α, and IL-12 in macrophages and increased the levels of MG-L1, MG-L2, ARG-1, and IL-10, which can inhibit the M1 polarization of macrophages and promote M2 polarization. In the coculture system, apigenin decreased the protein levels of TRPM7, P-mTOR, BAX, and c-caspase3 in macrophages, while significantly increasing the protein levels of Bcl2. The levels of IL-1, IL-6, MMP13, TNF-α, P38, JNK, and ERK phosphorylation were reduced in chondrocytes. Conclusion: Apigenin alleviates cartilage injury in OA mice induced by modified Hulth. Apigenin inhibits chondrocyte inflammation through the MAPK pathway. Apigenin alleviates macrophage-polarization-induced inflammatory response and chondrocyte apoptosis in the macrophage–chondrocyte coculture system through the TRPM7-mTOR pathway. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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33 pages, 9806 KiB  
Article
Chemical Constituents and Hypoglycemic Mechanisms of Dendrobium nobile in Treatment of Type 2 Diabetic Rats by UPLC-ESI-Q-Orbitrap, Network Pharmacology and In Vivo Experimental Verification
by Zhaoyang Li, Meiling Zeng, Keyong Geng, Donna Lai, Zhi Xu and Wei Zhou
Molecules 2023, 28(6), 2683; https://doi.org/10.3390/molecules28062683 - 16 Mar 2023
Cited by 4 | Viewed by 1767
Abstract
This study aimed to systematically explore the chemical constituents of D. nobile and its hypoglycemic effect by UPLC-ESI-Q-Orbitrap, network pharmacology and in vivo experiment. The chemical constituents of D. nobile were qualitatively analyzed, and the hypoglycemic compounds were quickly identified. Network pharmacological analysis [...] Read more.
This study aimed to systematically explore the chemical constituents of D. nobile and its hypoglycemic effect by UPLC-ESI-Q-Orbitrap, network pharmacology and in vivo experiment. The chemical constituents of D. nobile were qualitatively analyzed, and the hypoglycemic compounds were quickly identified. Network pharmacological analysis and molecular docking technique were applied to assist in the elucidation of the hypoglycemic mechanisms of D. nobile. A type 2 diabetic mellitus (T2DM) rat model was established using the HFD and STZ method for in vivo experimental verification, and these T2DM rats were treated with D. nobile extract and D. nobile polysaccharide for two months by gavage. The results showed that a total of 39 chemical constituents of D. nobile, including alkaloids, bibenzyls, phenanthrenes and other types of compounds, were identified. D. nobile extract and D. nobile polysaccharide could significantly ameliorate the body weight, hyperglycemia, insulin resistance, dyslipidemia and morphological impairment of the liver and pancreas in the T2DM rats. α-Linolenic acid, dihydroconiferyl dihydro-p-coumarate, naringenin, trans-N-feruloyltyramine, gigantol, moscatilin, 4-O-methylpinosylvic acid, venlafaxine, nordendrobin and tristin were regarded as the key hypoglycemic compounds of D. nobile, along with the hypoglycemic effect on the PI3K-AKT signaling pathway, the insulin signaling pathway, the FOXO signaling pathway, the improvement of insulin resistance and the AGE-RAGE signaling pathway. The Western blotting experiment results confirmed that D. nobile activated the PI3K/AKT pathway and insulin signaling pathway, promoted glycogen synthesis via regulating the expression of glycogen synthase kinase 3 beta (GSK-3β) and glucose transporter 4 (GLUT4), and inhibited liver gluconeogenesis by regulating the expression of phosphoenolpyruvate carboxykinase (PEPCK) and glucose 6 phosphatase (G6pase) in the liver. The results suggested that the hypoglycemic mechanism of D. nobile might be associated with liver glycogen synthesis and gluconeogenesis, contributing to improving insulin resistance and abnormal glucose metabolism in the T2DM rats. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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15 pages, 2736 KiB  
Article
Baicalin Relieves LPS-Induced Lung Inflammation via the NF-κB and MAPK Pathways
by Bingyu Shen, Haoqing Zhang, Zhengjin Zhu, Zixi Ling, Fangyuan Zeng, Yazhou Wang and Jianguo Wang
Molecules 2023, 28(4), 1873; https://doi.org/10.3390/molecules28041873 - 16 Feb 2023
Cited by 7 | Viewed by 1863
Abstract
Baicalin is an active ingredient extracted from the Chinese medicine Scutellaria and has many beneficial effects. Pulmonary interstitial and alveolar edema are common symptoms of an acute lung injury (ALI). We investigated the effects of baicalin on LPS-induced inflammation and the underlying mechanisms [...] Read more.
Baicalin is an active ingredient extracted from the Chinese medicine Scutellaria and has many beneficial effects. Pulmonary interstitial and alveolar edema are common symptoms of an acute lung injury (ALI). We investigated the effects of baicalin on LPS-induced inflammation and the underlying mechanisms in mice and cells. The protein contents and mRNA expression of TNF-α, IL-1β, and IL-6 in RAW264.7 cells and mice were detected using ELISA and qRT-PCR. Baicalin significantly suppressed TNF-α, IL-1β, and IL-6 levels and expression, both in vitro and in vivo, compared with the LPS group. Baicalin inhibits the expression of TLR4 and MyD88, resulting in significant decreases in p-p65, p-p38, p-ERK, and p-JNK, as measured by the Western blotting of RAW264.7 cells. A baicalin treatment for 12 h resulted in a rapid increasing of the white blood cell number and significantly improved the pathological changes in the lung. We also found that the baicalin pretreatment for 12 h could decrease the MPO content and wet/dry (W/D) weight ratio, which indicates that baicalin can significantly reduce pulmonary edema. Furthermore, the baicalin pretreatment also resulted in the recovery of TGF-β protein levels and decreased iNOS. Baicalin inhibits ALI inflammation in mice and cells and is a potential candidate for the treatment of ALI. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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15 pages, 4480 KiB  
Article
Effects of Dietary Ferulic Acid on Intestinal Health and Ileal Microbiota of Tianfu Broilers Challenged with Lipopolysaccharide
by Ziting Tang, Gang Shu, Hong Du, Yilei Zheng, Hualin Fu, Wei Zhang, Cheng Lv, Funeng Xu, Haohuan Li, Ping Ouyang, Juchun Lin, Li-Jen Chang, Felix Kwame Amevor and Xiaoling Zhao
Molecules 2023, 28(4), 1720; https://doi.org/10.3390/molecules28041720 - 10 Feb 2023
Cited by 5 | Viewed by 1721
Abstract
Lipopolysaccharide (LPS) has been considered the primary agent to establish animal models of inflammation, immunological stress, and organ injury. Previous studies have demonstrated that LPS impaired gastrointestinal development and disrupted intestinal microbial composition and metabolism. Ferulic acid (FA) isolated from multiple plants exhibits [...] Read more.
Lipopolysaccharide (LPS) has been considered the primary agent to establish animal models of inflammation, immunological stress, and organ injury. Previous studies have demonstrated that LPS impaired gastrointestinal development and disrupted intestinal microbial composition and metabolism. Ferulic acid (FA) isolated from multiple plants exhibits multiple biological activities. This study investigated whether FA ameliorated intestinal function and microflora in LPS-challenged Tianfu broilers. The results showed that LPS challenge impaired intestinal function, as evidenced by decreased antioxidant functions (p < 0.05), disrupted morphological structure (p < 0.05), and increased intestinal permeability (p < 0.05); however, these adverse effects were improved by FA supplementation. Additionally, FA supplementation preserved sIgA levels (p < 0.05), increased mRNA expression levels of CLDN and ZO-1 (p < 0.05), and enhanced epithelial proliferation (p < 0.05) in the ileal mucosa in LPS-challenged chickens. Moreover, FA supplementation rectified the ileal microflora disturbances in the LPS-challenged broilers. The results demonstrate that dietary FA supplementation decreased LPS-induced intestinal damage by enhancing antioxidant capacity and maintaining intestinal integrity. Furthermore, FA supplementation protects intestinal tight junctions (TJs), elevates secretory immunoglobulin A (sIgA) levels, and modulates ileal microflora composition in LPS-challenged broilers. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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14 pages, 5336 KiB  
Article
Analyses of Transcriptomics upon IL-1β-Stimulated Mouse Chondrocytes and the Protective Effect of Catalpol through the NOD2/NF-κB/MAPK Signaling Pathway
by Yong Pang, Lu Zhao, Xueyan Ji, Kaijin Guo and Xiaoxing Yin
Molecules 2023, 28(4), 1606; https://doi.org/10.3390/molecules28041606 - 07 Feb 2023
Cited by 3 | Viewed by 1494
Abstract
The overall objective of this study was to investigate the mechanism of inflammation on chondrocyte injury and the protective effect of catalpol on chondrocytes in an inflammatory environment. Chondrocytes were isolated and cultured from the knee joints of three-day-old newborn mice. Alcian Blue [...] Read more.
The overall objective of this study was to investigate the mechanism of inflammation on chondrocyte injury and the protective effect of catalpol on chondrocytes in an inflammatory environment. Chondrocytes were isolated and cultured from the knee joints of three-day-old newborn mice. Alcian Blue staining and the immunocytochemistry staining of type II collagen were used to identify the purity of chondrocytes. Primary chondrocytes were stimulated by IL-1β (10 ng/mL) and subjected to transcriptome analysis. Differentially expressed genes (DEGs) were further analyzed based on Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses. In this experimental study, we performed the viability assay to determine the effects of different concentrations of catalpol on the cell viability of chondrocytes. Chondrocytes were seeded in six-well plates and exposed to 10 μM catalpol 2 h prior to treatment with IL-1β (10 ng/mL). Quantitative real-time (qPCR) and Western blotting were performed to evaluate the RNA and protein expression, respectively. Based on the results of transcriptomics analysis, we found the NOD2 signaling pathway, the NF-kappa B signaling pathway, and the MAPK signaling pathway showed significant changes in chondrocyte damage caused by inflammation. Catalpol (10 μM and 100 μM) could significantly reduce NO, IL-6, IL-1β, and TNF-α in supernatant of chondrocytes. Catalpol significantly inhibited the mRNA expression of IL-1, IL-6, and IL-12 in chondrocytes induced by IL-1β. Catalpol markedly inhibited MMP3, MMP13 mRNA, and protein levels. Catalpol could significantly reduce TNF-α mRNA levels in inflammatory chondrocytes. Inflammation causes significant increases in mRNA levels and protein levels of NOD2, mRNA levels, and protein levels were markedly suppressed by catalpol. In addition, catalpol could significantly increase IKBα protein levels and significantly lower intranuclear P65 levels. Catalpol significantly lowered the phosphorylation protein levels of ERK, p38, and JNK. Our transcriptomic analysis demonstrated that the activation of NOD2 and its downstream pathways, NF-κB and MAPK, is an important cause of the inflammatory injury to chondrocytes induced by IL-1β. Catalpol inhibited the activation of the NOD2 signaling pathway, which reduced the phosphorylation of ERK, p38, and JNK, inhibited the degradation of IκBα, inhibited p65 translocation into the nucleus, reduced the release of inflammatory cytokines, and attenuated the inflammatory damage to chondrocytes. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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18 pages, 1898 KiB  
Article
Exploring the Relationship between Biosynthetic Gene Clusters and Constitutive Production of Mycosporine-like Amino Acids in Brazilian Cyanobacteria
by Rafael B. Dextro, Endrews Delbaje, Vanessa Geraldes, Ernani Pinto, Paul F. Long and Marli F. Fiore
Molecules 2023, 28(3), 1420; https://doi.org/10.3390/molecules28031420 - 02 Feb 2023
Cited by 6 | Viewed by 2014
Abstract
Cyanobacteria are oxygenic phototrophic prokaryotes that have evolved to produce ultraviolet-screening mycosporine-like amino acids (MAAs) to lessen harmful effects from obligatory exposure to solar UV radiation. The cyanobacterial MAA biosynthetic cluster is formed by a gene encoding 2-epi-5-epi-valiolone synthase [...] Read more.
Cyanobacteria are oxygenic phototrophic prokaryotes that have evolved to produce ultraviolet-screening mycosporine-like amino acids (MAAs) to lessen harmful effects from obligatory exposure to solar UV radiation. The cyanobacterial MAA biosynthetic cluster is formed by a gene encoding 2-epi-5-epi-valiolone synthase (EVS) located immediately upstream from an O-methyltransferase (OMT) encoding gene, which together biosynthesize the expected MAA precursor 4-deoxygadusol. Accordingly, these genes are typically absent in non-producers. In this study, the relationship between gene cluster architecture and constitutive production of MAAs was evaluated in cyanobacteria isolated from various Brazilian biomes. Constitutive production of MAAs was only detected in strains where genes formed a co-linear cluster. Expectedly, this production was enhanced upon exposure of the strains to UV irradiance and by using distinct culture media. Constitutive production of MAAs was not detected in all other strains and, unexpectedly, production could not be induced by exposure to UV irradiation or changing growth media. Other photoprotection strategies which might be employed by these MAA non-producing strains are discussed. The evolutionary and ecological significance of gene order conservation warrants closer experimentation, which may provide a first insight into regulatory interactions of genes encoding enzymes for MAA biosynthesis. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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14 pages, 6585 KiB  
Article
ACT001 Relieves NMOSD Symptoms by Reducing Astrocyte Damage with an Autoimmune Antibody
by Hongen Li, Mo Yang, Honglu Song, Mingming Sun, Huanfen Zhou, Junxia Fu, Di Zhou, Wenhao Bai, Biyue Chen, Mengying Lai, Hao Kang and Shihui Wei
Molecules 2023, 28(3), 1412; https://doi.org/10.3390/molecules28031412 - 02 Feb 2023
Viewed by 1824
Abstract
Neuromyelitis optica spectrum disorder (NMOSD) is a central nervous system inflammatory demyelinating disease, the pathogenesis of which involves autoantibodies targeting the extracellular epitopes of aquaporin-4 on astrocytes. We neutralized the AQP4-IgG from NMOSD patient sera using synthesized AQP4 extracellular epitope peptides and found [...] Read more.
Neuromyelitis optica spectrum disorder (NMOSD) is a central nervous system inflammatory demyelinating disease, the pathogenesis of which involves autoantibodies targeting the extracellular epitopes of aquaporin-4 on astrocytes. We neutralized the AQP4-IgG from NMOSD patient sera using synthesized AQP4 extracellular epitope peptides and found that the severe cytotoxicity produced by aquaporin-4 immunoglobin (AQP4-IgG) could be blocked by AQP4 extracellular mimotope peptides of Loop A and Loop C in astrocyte protection and animal models. ACT001, a natural compound derivative, has shown anti-tumor activity in various cancers. In our study, the central nervous system anti-inflammatory effect of ACT001 was investigated. The results demonstrated the superior astrocyte protection activity of ACT001 at 10 µM. Furthermore, ACT001 decreases the behavioral score in the mouse NMOSD model, which was not inferior to Methylprednisolone Sodium Succinate, the first-line therapy of NMOSD in clinical practice. In summary, our study showed that astrocytes are protected by specific peptides, or small molecular drugs, which is a new strategy for the treatment of NMOSD. It is possible for ACT001 to be a promising therapy for NMOSD. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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21 pages, 2896 KiB  
Article
Chemical Composition, Antioxidant Activity and Cytocompatibility of Polyphenolic Compounds Extracted from Food Industry Apple Waste: Potential in Biomedical Application
by Parinaz Hobbi, Oseweuba Valentine Okoro, Maryam Hajiabbas, Masoud Hamidi, Lei Nie, Véronique Megalizzi, Paul Musonge, Gianina Dodi and Amin Shavandi
Molecules 2023, 28(2), 675; https://doi.org/10.3390/molecules28020675 - 09 Jan 2023
Cited by 8 | Viewed by 1844
Abstract
Apple pomace (AP) from the food industry is a mixture of different fractions containing bioactive polyphenolic compounds. This study provides a systematic approach toward the recovery and evaluation of the physiochemical and biological properties of polyphenolic compounds from AP. We studied subcritical water [...] Read more.
Apple pomace (AP) from the food industry is a mixture of different fractions containing bioactive polyphenolic compounds. This study provides a systematic approach toward the recovery and evaluation of the physiochemical and biological properties of polyphenolic compounds from AP. We studied subcritical water extraction (SCW) and solvent extraction with ethanol from four different AP fractions of pulp, peel, seed, core, and stem (A), peel (B), seed and core (C), and pulp and peel (D). The subcritical water method at the optimum condition resulted in total polyphenolic compounds (TPC) of 39.08 ± 1.10 mg GAE per g of AP on a dry basis compared to the ethanol extraction with TPC content of 10.78 ± 0.94 mg GAE/g db. Phloridzin, chlorogenic acid, and quercetin were the main identified polyphenolics in the AP fractions using HPLC. DPPH radical scavenging activity of fraction B and subcritical water (SW) extracts showed comparable activity to ascorbic acid while all ethanolic extracts were cytocompatible toward human fibroblast (3T3-L1) and salivary gland acinar cells (NS-SV-AC). Our results indicated that AP is a rich source of polyphenolics with the potential for biomedical applications. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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19 pages, 1098 KiB  
Article
Wound Healing Potential of an Oleoresin Essential Oil Chemotype from Canarium schweinfurthii Engl.
by Michel Bonnard, Enzo Martin and Isabelle Parrot
Molecules 2022, 27(22), 7966; https://doi.org/10.3390/molecules27227966 - 17 Nov 2022
Cited by 3 | Viewed by 1553
Abstract
This study was conducted to investigate the chemical composition of essential oil (EO) extracted from an oleoresin of Canarium schweinfurthii widespread in the Gabonese tropical forest. A great variability in the chemical composition of EO was observed, among which a chemical profile rich [...] Read more.
This study was conducted to investigate the chemical composition of essential oil (EO) extracted from an oleoresin of Canarium schweinfurthii widespread in the Gabonese tropical forest. A great variability in the chemical composition of EO was observed, among which a chemical profile rich in terpinolene and α-phellandrene (31.2 and 21.8%, respectively), was found and tested as a natural active ingredient for topical applications. After the evaluation of eye and skin irritancy and sensitization potentials of EO on in vitro and in chemico models, the in vitro modulating potential on a model of wound re-epithelialization was assessed. The terpinolene and α-phellandrene-rich chemotype have been proven to accelerate wound healing in a dose-dependent manner (concentration range from 1.8 to 9.0 μg/mL). In addition, the ability of this EO to modulate the pro-inflammatory response in human keratinocytes stimulated by UVB was observed in vitro by the reduction in levels of interleukin 6 (IL-6) and tumour necrosis factor-alpha (TNF-α), suggesting a possible implication during the inflammation phase of wound healing. Despite the high variability in EO composition, a method of solid-phase microextraction (SPME) of the oleoresin headspace is proposed for the in situ identification of the terpinolene and α-phellandrene-rich chemotype instead of conducting hydrodistillation. These results offer interesting perspectives for the development of innovative natural ingredients for the topical route, ingredients obtained in an eco-responsible and non-destructive way. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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17 pages, 3180 KiB  
Article
Cinnamaldehyde Resist Salmonella Typhimurium Adhesion by Inhibiting Type I Fimbriae
by Lizi Yin, Yuyun Dai, Han Chen, Xuewen He, Ping Ouyang, Xiaoli Huang, Xiangang Sun, Yanru Ai, Siyuan Lai, Ling Zhu and Zhiwen Xu
Molecules 2022, 27(22), 7753; https://doi.org/10.3390/molecules27227753 - 10 Nov 2022
Cited by 5 | Viewed by 2463
Abstract
Salmonella Typhimurium (S. Typhimurium), a common foodborne pathogen, severely harms the public and food security. Type I fimbriae (T1F) of S. Typhimurium, plays a crucial role in the pathogenic processes; it mediates the adhesion of bacteria to the mannose receptor [...] Read more.
Salmonella Typhimurium (S. Typhimurium), a common foodborne pathogen, severely harms the public and food security. Type I fimbriae (T1F) of S. Typhimurium, plays a crucial role in the pathogenic processes; it mediates the adhesion of bacteria to the mannose receptor on the host cell, assists the bacteria to invade the host cell, and triggers an inflammatory response. Cinnamaldehyde is the main ingredient in cinnamon essential oil. In this study, cinnamaldehyde was demonstrated to inhibit the expression of T1F by hemagglutination inhibition test, transmission electron microscopy, and biofilms. The mechanism of cinnamaldehyde action was studied by proteomics technology, PCR and Western blotting. The results showed that cinnamaldehyde can inhibit T1F in S. typhimurium without the growth of bacteria, by regulating the level of expression and transcription of fimA, fimZ, fimY, fimH and fimW. Proteomics results showed that cinnamaldehyde downregulated the subunits and regulators of T1F. In addition, the invasion assays proved that cinnamaldehyde can indeed reduce the ability of S. typhimurium to adhere to cells. The results of animal experiments showed that the colonization in the intestinal tract and the expression levels of inflammatory cytokine were significantly decreased, and the intestinal mucosal immune factors MUC1 and MUC2 were increased under cinnamaldehyde treatment. Therefore, cinnamaldehyde may be a potential drug to target T1F to treat Salmonella infections. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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13 pages, 3317 KiB  
Article
The Antiviral Activity of Caprylic Monoglyceride against Porcine Reproductive and Respiratory Syndrome Virus In Vitro and In Vivo
by Luyu Yang, Jianhua Wen, Yang Zhang, Zheyan Liu, Zhipeng Luo, Lei Xu, Siyuan Lai, Huaqiao Tang, Xiangang Sun, Youjun Hu, Ling Zhu and Zhiwen Xu
Molecules 2022, 27(21), 7263; https://doi.org/10.3390/molecules27217263 - 26 Oct 2022
Cited by 2 | Viewed by 1544
Abstract
Porcine reproductive and respiratory syndrome (PRRS) is a disease with a major economic impact in the global pig industry, and this study aims to identify potential anti-PRRSV drugs. We examined the cytotoxicity of four medium-chain fatty acids (MCFAs) (caprylic, caprylic monoglyceride, decanoic monoglyceride, [...] Read more.
Porcine reproductive and respiratory syndrome (PRRS) is a disease with a major economic impact in the global pig industry, and this study aims to identify potential anti-PRRSV drugs. We examined the cytotoxicity of four medium-chain fatty acids (MCFAs) (caprylic, caprylic monoglyceride, decanoic monoglyceride, and monolaurin) and their inhibition rate against PRRSV. Then the MCFAs with the best anti-PRRSV effect in in vitro assays were selected for subsequent in vivo experiments. Potential anti-PRRSV drugs were evaluated by viral load assay, pathological assay, and cytokine level determination. The results showed that caprylic monoglyceride (CMG) was the least toxic to cells of the four MCFAs, while it had the highest PRRSV inhibition rate. Then the animals were divided into a low-CMG group, a medium-CMG group, and a high-CMG group to conduct the in vivo evaluation. The results indicated that piglets treated with higher concentrations of caprylic monoglyceride were associated with lower mortality and lower viral load after PRRSV infection (p < 0.05). The pulmonary pathology of the piglets also improved after CMG treatment. The levels of pro-inflammatory cytokines (IL-6, IL-8, IL-1β, IFN-γ, TNF-α) were significantly downregulated, and the levels of anti-inflammatory cytokine (IL-10) were significantly upregulated in the CMG-treated piglets compared to the positive control group (p < 0.05). Taken together, the present study revealed for the first time that caprylic monoglyceride has strong antiviral activity against PRRSV in vitro and in vivo, suggesting that caprylic monoglyceride could potentially be used as a drug to treat PRRS infection. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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18 pages, 3074 KiB  
Article
Effects of Extracts and Flavonoids from Drosera rotundifolia L. on Ciliary Beat Frequency and Murine Airway Smooth Muscle
by Alexander Hake, Frank Begrow, Verena Spiegler, Nico Symma, Andreas Hensel and Martina Düfer
Molecules 2022, 27(19), 6622; https://doi.org/10.3390/molecules27196622 - 05 Oct 2022
Cited by 4 | Viewed by 2071
Abstract
Extracts from Drosera rotundifolia are traditionally used to treat cough symptoms during a common cold. The present study aimed to investigate the impact of extracts from D. rotundifolia and active compounds on the respiratory tract. Tracheal slices of C57BL/6N mice were used ex [...] Read more.
Extracts from Drosera rotundifolia are traditionally used to treat cough symptoms during a common cold. The present study aimed to investigate the impact of extracts from D. rotundifolia and active compounds on the respiratory tract. Tracheal slices of C57BL/6N mice were used ex vivo to examine effects on airway smooth muscle (ASM) and ciliary beat frequency (CBF). Phosphodiesterase (PDE) inhibition assays were carried out to test whether PDE1 or PDE4 are targeted by the active compounds. An ethanol–water extract, as well as an aqueous fraction of this extract, exerted antispasmodic properties against acetylcholine-induced contractions. In addition, contractions induced by 60 mM K+ were abrogated by the aqueous fraction. Effects on ASM could be attributed to the flavonoids quercetin, 2″-O-galloylhyperoside and hyperoside. Moreover, the Drosera extract and the aqueous fraction increased the CBF of murine tracheal slices. Quercetin and 2″-O-galloylhyperoside were identified as active compounds involved in the elevation of CBF. Both compounds inhibited PDE1A and PDE4D. The elevation of CBF was mimicked by the subtype-selective PDE inhibitor rolipram (PDE4) and by 8-methoxymethyl-IBMX. In summary, our study shows, for the first time, that a Drosera extract and its flavonoid compounds increase the CBF of murine airways while antispasmodic effects were transferred to ASM. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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10 pages, 2527 KiB  
Article
Shionone-Targeted Pneumolysin to Ameliorate Acute Lung Injury Induced by Streptococcus pneumoniae In Vivo and In Vitro
by Runbao Du, Tian Wang, Hongfa Lv, Yinuo Zou, Xiaoning Hou, Nana Hou, Peng Zhang, Hongen Li and Gefu Chi
Molecules 2022, 27(19), 6258; https://doi.org/10.3390/molecules27196258 - 23 Sep 2022
Cited by 2 | Viewed by 1602
Abstract
Streptococcus pneumoniae (S. pneumoniae), as a Gram-positive bacterium, can cause severe bacterial pneumonia, and result in high morbidity and mortality in infected people. Meanwhile, isolated drug-resistant S. pneumoniae is growing, which raises concerns about strategies for combatting S. pneumoniae infection. To [...] Read more.
Streptococcus pneumoniae (S. pneumoniae), as a Gram-positive bacterium, can cause severe bacterial pneumonia, and result in high morbidity and mortality in infected people. Meanwhile, isolated drug-resistant S. pneumoniae is growing, which raises concerns about strategies for combatting S. pneumoniae infection. To disturb S. pneumoniae pathogenicity and its drug-resistance, developing novel anti-infective strategies or compounds is urgent. In this study, the anti-infective effect of shionone was explored. A minimum inhibitory concentration (MIC) assay and growth curve determination were performed to evaluate the effect of the tetracyclic triterpenoid compound shionone against S. pneumoniae. Hemolysis tests, western blotting, oligomerization inhibition assays, and molecular docking were carried out to explore the anti-infective mechanism of shionone. Moreover, the protective effect of shionone was also confirmed in a mousepneumonia model. The results showed that the excellent hemolytic inhibitory activity of shionone was observed at less than 8 μg/mL. Meanwhile, shionone could disturb the oligomerization of pneumolysin (PLY) but did not interfere with PLY expression at less than 4 μg/mL. Molecular docking suggested that shionone targeted the ASP-59, ILE-60, THR-57, PHE-344, and ASN-346 amino acid sites to reduce S. pneumoniae pathogenicity. Furthermore, shionone alleviated lung histopathologic injury and decreased lung bacterial colonization in vivo. The above results showed that shionone could bind to the PLY active pocket under the concentrations of 8 μg/mL and neutralize PLY hemolysis activity to reduce S. pneumoniae pathogenicity in vitro and in vivo. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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18 pages, 2836 KiB  
Article
Protection of Erythrocytes and Microvascular Endothelial Cells against Oxidative Damage by Fragaria vesca L. and Rubus idaeus L. Leaves Extracts—The Mechanism of Action
by Sylwia Cyboran-Mikołajczyk, Katarzyna Męczarska, Katarzyna Solarska-Ściuk, Katarzyna Ratajczak-Wielgomas, Jan Oszmiański, Vera Jencova and Dorota Bonarska-Kujawa
Molecules 2022, 27(18), 5865; https://doi.org/10.3390/molecules27185865 - 10 Sep 2022
Cited by 2 | Viewed by 1450
Abstract
The aim of this work is to determine the biological activity of ellagitannins rich extracts from leaves of raspberry (Rubus idaeus L.) and wild strawberry (Fragaria vesca L.) in relation to cells and cell membranes. Detailed qualitative and quantitative analysis of [...] Read more.
The aim of this work is to determine the biological activity of ellagitannins rich extracts from leaves of raspberry (Rubus idaeus L.) and wild strawberry (Fragaria vesca L.) in relation to cells and cell membranes. Detailed qualitative and quantitative analysis of phenolic compounds of the extract was made using chromatographic methods. Cytotoxic and antioxidant activities of tested extracts in relation to erythrocytes and human vascular endothelial cells (HMEC-1) were determined by using fluorimetric and spectrophotometric methods. In order to establish the influence of the extracts on the physical properties of the membrane, such as osmotic resistance and erythrocytes shapes, mobility and/or hydration of polar heads and fluidity of hydrocarbon chains of membrane lipids, microscopic and spectroscopic methods were used. The results showed that the extracts are non-toxic for erythrocytes and HMEC-1 cells (up to concentration of 50 µg/mL), but they effectively protect cells and their membranes against oxidative damage. The increase in osmotic resistance of erythrocytes, formation of echinocytes and changes only in the polar part of the membrane caused by the extracts demonstrate their location mainly in the hydrophilic part of the membrane. The results indicate that tested extracts have high biological activities and may be potentially used in delaying the ageing process of organisms and prevention of many diseases, especially those associated with oxidative stress. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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10 pages, 2122 KiB  
Article
Antioxidant and Anti-Melanogenesis Effects of Colloidal Gold Camellia sinensis L. Extracts
by Seoyeon Shin, Minjeong Kim, Nuri Song, Sangouk Sun, Joonyong Choi and Kyungmok Park
Molecules 2022, 27(17), 5593; https://doi.org/10.3390/molecules27175593 - 30 Aug 2022
Cited by 3 | Viewed by 1889
Abstract
Green tea extract derived from the leaves of Camellia sinensis L. (CS), is a representative beverage with antioxidant, anti-cancer, and anti-viral properties. CS extract is also used in cosmetics. Colloidal gold is generally a sol or colloidal suspension of gold nanoparticles in water. [...] Read more.
Green tea extract derived from the leaves of Camellia sinensis L. (CS), is a representative beverage with antioxidant, anti-cancer, and anti-viral properties. CS extract is also used in cosmetics. Colloidal gold is generally a sol or colloidal suspension of gold nanoparticles in water. Colloidal gold green tea (CGCS), cultivated as a fertilizer using this colloidal gold solution, contains gold minerals and possesses anti-inflammatory, analgesic, and anti-tumor properties. However, the skin bioactivity of CGCS has not yet been investigated. In this study, we investigated the effect of the CGCS extract on skin whitening. CGCS extract contained high levels of phenols and flavonoids and displayed 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity in a concentration-dependent manner. CGCS extract inhibited melanin synthesis and tyrosinase activity in B16F10 cells more effectively than the CS extract. Moreover, the CGCS extract decreased the expression levels of the melanogenesis-related proteins, tyrosinase, tyrosinase-related proteins (TRPs), and microphthalmia-associated transcription factor (MITF). In conclusion, our study showed that the CGCS extract inhibits the expression of tyrosinase, TRP-1, and TRP-2 via the downregulation of MITF, thereby inhibiting melanin synthesis. Therefore, CGCS can potentially be used as a skin-whitening ingredient in the cosmetic industry. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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12 pages, 1302 KiB  
Article
The Antioxidant Activity of a Commercial and a Fractionated Phycocyanin on Human Skin Cells In Vitro
by Roberto Puglisi, Elisa Biazzi, Daniela Gesmundo, Roberta Vanni, Aldo Tava and Silvia Cenadelli
Molecules 2022, 27(16), 5276; https://doi.org/10.3390/molecules27165276 - 18 Aug 2022
Cited by 5 | Viewed by 1768
Abstract
The protective effects for cells against chemical and UVA stress of a commercial phycocyanin (PC) for food use and a PC extracted from Arthrospira platensis (Spirulina) in phosphate buffer were assessed. The purity of the commercial PC, spectrophotometrically estimated as A620/A [...] Read more.
The protective effects for cells against chemical and UVA stress of a commercial phycocyanin (PC) for food use and a PC extracted from Arthrospira platensis (Spirulina) in phosphate buffer were assessed. The purity of the commercial PC, spectrophotometrically estimated as A620/A280 and confirmed by HPLC, was higher than that of the fractionated PC (2.0 vs. 1.5) but was twofold less concentrated. The oxygen radical antioxidant capacities (ORACs) of the commercial and fractionated PCs were 12,141 ± 1928 and 32,680 ± 3295 TE/100 g, respectively. The degradation of PCs upon exposure to UVA was spectrophotometrically estimated, and cytotoxicity was evaluated with the MTS [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) test on human fibroblasts and keratinocytes. A lower level of reactive oxygen species (ROS) was recorded in the two cell lines incubated with the commercial PC after menadione treatment (p < 0.01) and UVA exposure (p < 0.001) on fibroblasts after 5 min and keratinocytes up to 25 min, compared with controls. Differently, the fractionated PC was not protective and showed significant (p < 0.01) paradoxical prooxidant effects. Overall, the PC for food consumption demonstrated a high safety threshold and antioxidant ability to cells that, along with its coloring power, make it an excellent candidate for cosmetic formulations. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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13 pages, 3067 KiB  
Article
Piceatannol Alleviates Clostridium perfringens Virulence by Inhibiting Perfringolysin O
by Guizhen Wang, Hongtao Liu, Yawen Gao, Xiaodi Niu, Xuming Deng, Jianfeng Wang, Haihua Feng, Zhimin Guo and Jiazhang Qiu
Molecules 2022, 27(16), 5145; https://doi.org/10.3390/molecules27165145 - 12 Aug 2022
Cited by 4 | Viewed by 1470
Abstract
Clostridium perfringens (C. perfringens) is an important foodborne pathogen that can cause diseases such as gas gangrene and necrotizing enteritis in a variety of economic animals, seriously affecting public health and the economic benefits and healthy development of the livestock and [...] Read more.
Clostridium perfringens (C. perfringens) is an important foodborne pathogen that can cause diseases such as gas gangrene and necrotizing enteritis in a variety of economic animals, seriously affecting public health and the economic benefits and healthy development of the livestock and poultry breeding industry. Perfringolysin O (PFO) is an important virulence factor of C. perfringens and plays critical roles in necrotic enteritis and gas gangrene, rendering it an ideal target for developing new drugs against infections caused by this pathogen. In this study, based on biological activity inhibition assays, oligomerization tests and computational biology assays, we found that the foodborne natural component piceatannol reduced pore-forming activity with an inhibitory ratio of 83.84% in the concentration of 16 µg/mL (IC50 = 7.83 µg/mL) by binding with PFO directly and changing some of its secondary structures, including 3-Helix, A-helix, bend, and in turn, ultimately affecting oligomer formation. Furthermore, we confirmed that piceatannol protected human intestinal epithelial cells from the damage induced by PFO with LDH release reduced by 38.44% at 16 µg/mL, based on a cytotoxicity test. By performing an animal experiment, we found the C. perfringens clones showed an approximate 10-fold reduction in infected mice. These results suggest that piceatannol may be a candidate for anti-C. perfringens drug development. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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12 pages, 3479 KiB  
Article
Corilagin: A Novel Antivirulence Strategy to Alleviate Streptococcus pneumoniae Infection by Diminishing Pneumolysin Oligomers
by Qiushuang Sheng, Xiaoning Hou, Nan Wang, Minda Liu, Haoyu Zhu, Xuming Deng, Xiaoying Liang and Gefu Chi
Molecules 2022, 27(16), 5063; https://doi.org/10.3390/molecules27165063 - 09 Aug 2022
Cited by 2 | Viewed by 1516
Abstract
Pneumolysin (PLY) is a significant virulence factor of Streptococcus pneumoniae (S. pneumoniae), able to break through the defense system of a host and mediate the occurrence of a series of infections. Therefore, PLY as the most ideal target to prevent S. [...] Read more.
Pneumolysin (PLY) is a significant virulence factor of Streptococcus pneumoniae (S. pneumoniae), able to break through the defense system of a host and mediate the occurrence of a series of infections. Therefore, PLY as the most ideal target to prevent S. pneumoniae infection has received more and more attention and research. Corilagin is a tannic acid that exhibits excellent inhibition of PLY oligomers without bacteriostatic activity to S. pneumoniae. Herein, hemolytic activity assays, cell viability tests and western blot experiments are executed to evaluate the antivirulence efficacy of corilagin against PLY in vitro. Colony observation, hematoxylin and eosin (H&E) staining and cytokines of bronchoalveolar lavage fluid (BALF) are applied to assess the therapeutic effect of corilagin in mice infected by S. pneumoniae. The results indicate the related genes of corilagin act mainly via enrichment in pathways associated with pneumonia disease. Furthermore, molecular docking and molecular dynamics simulations show that corilagin might bind with domains 3 and 4 of PLY and interfere with its hemolytic activity, which is further confirmed by the site-directed mutagenesis of PLY. Additionally, corilagin limits PLY oligomer production without impacting PLY expression in S. pneumoniae cultures. Moreover, corilagin effectively relieves PLY-mediated cell injury without any cytotoxicity, even then reducing the colony count in the lung and the levels of pro-inflammatory factors in BALF and remarkably improving lung lesions. All the results demonstrate that corilagin may be a novel strategy to cope with S. pneumoniae infection by inhibiting PLY oligomerization. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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17 pages, 4733 KiB  
Article
Antioxidant Activity of Acanthopanax senticosus Flavonoids in H2O2-Induced RAW 264.7 Cells and DSS-Induced Colitis in Mice
by Jianqing Su, Xinyu Zhang, Qibin Kan and Xiuling Chu
Molecules 2022, 27(9), 2872; https://doi.org/10.3390/molecules27092872 - 30 Apr 2022
Cited by 2 | Viewed by 1879
Abstract
The redox reaction is a normal process of biological metabolism in the body that leads to the production of free radicals. Under conditions such as pathogenic infection, stress, and drug exposure, free radicals can exceed normal levels, causing protein denaturation, DNA damage, and [...] Read more.
The redox reaction is a normal process of biological metabolism in the body that leads to the production of free radicals. Under conditions such as pathogenic infection, stress, and drug exposure, free radicals can exceed normal levels, causing protein denaturation, DNA damage, and the oxidation of the cell membrane, which, in turn, causes inflammation. Acanthopanax senticosus (A. senticosus) flavonoids are the main bioactive ingredients with antioxidant function. H2O2-treated RAW 264.7 cells and DSS-induced colitis in mice were used to evaluate the antioxidant properties of A. senticosus flavonoids. The results show that A. senticosus flavonoids can significantly downregulate the levels of ROS and MDA in H2O2-treated RAW 264.7 cells and increase the levels of CAT, SOD, and GPx. A. senticosus flavonoids can also increase the body weights of DSS-induced colitis mice, increase the DAI index, and ameliorate the shortening of the colon. ELISA experiments confirmed that A. senticosus flavonoids could reduce the level of MDA in the mouse serum and increase the levels of SOD, CAT, and GPx. Histopathology showed that the tissue pathological changes in the A. senticosus flavonoid group were significantly lower than those in the DSS group. The Western blot experiments showed that the antioxidant capacity of A. senticosus flavonoids was accomplished through the Nrf2 pathway. In conclusion, A. senticosus flavonoids can relieve oxidative stress in vivo and in vitro and protect cells or tissues from oxidative damage. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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Review

Jump to: Research, Other

13 pages, 1160 KiB  
Review
Preliminary Microbiological Tests of S-Carvone and Geraniol and Selected Derivatives of These Compounds That May Be Formed in the Processes of Isomerization and Oxidation
by Agnieszka Wróblewska, Anna Fajdek-Bieda, Agata Markowska-Szczupak and Monika Radkowska
Molecules 2022, 27(20), 7012; https://doi.org/10.3390/molecules27207012 - 18 Oct 2022
Cited by 2 | Viewed by 1602
Abstract
This work presents a literature review on the biological activity of S-carvone, geraniol and derivatives of these compounds, which are formed in the process of isomerization (during the process of geraniol isomerization, oxidation products of this compound are also obtained). Moreover, this work [...] Read more.
This work presents a literature review on the biological activity of S-carvone, geraniol and derivatives of these compounds, which are formed in the process of isomerization (during the process of geraniol isomerization, oxidation products of this compound are also obtained). Moreover, this work presents preliminary microbiological tests of creams with the addition of these biologically active compounds: S-carvone, geraniol, carvacrol (an S-carvone isomerization product), nerol (a geraniol isomerization product), linalool (a geraniol isomerization product) and citral (a geraniol oxidation product). Because the post-reaction mixture obtained after the S-carvone isomerization has a relatively simple composition, it was also added to creams and tested without isolating pure compounds. This may be a cheaper alternative to creams prepared with the addition of pure compounds. The mixture obtained after the geraniol isomerization process has a very complex composition; therefore, only compounds with the lowest molecular weight and are easily commercially available were selected for studies. The content of the tested compounds in the creams ranged from 0.5 to 3 wet%. The following microorganisms were selected for microbiological tests: the Gram-negative bacterium Escherichia coli K12, the Gram-positive bacterium Staphylococcus epidermidis, and the fungi Candida albicans, Trichophyton rubrum, Aspergillus niger, and Penicillium chrysogenum. A content of 3% carvacrol, nerol, geraniol and citral inhibited the growth of E. coli, and attenuated the growth of C. albicans and T. rubrum. On the other hand, 3% carvacrol and citral only poorly attenuated the growth of the mould fungi P. chrysogenum and A. niger. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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15 pages, 2999 KiB  
Review
Progress of Microencapsulated Phycocyanin in Food and Pharma Industries: A Review
by Yang Li, Xu Li, Zi-Peng Liang, Xin-Ying Chang, Fu-Tong Li, Xue-Qing Wang and Xi-Jun Lian
Molecules 2022, 27(18), 5854; https://doi.org/10.3390/molecules27185854 - 09 Sep 2022
Cited by 10 | Viewed by 3027
Abstract
Phycocyanin is a blue fluorescent protein with multi-bioactive functions. However, the multi-bioactivities and spectral stability of phycocyanin are susceptible to external environmental conditions, which limit its wide application. Here, the structure, properties, and biological activity of phycocyanin were discussed. This review highlights the [...] Read more.
Phycocyanin is a blue fluorescent protein with multi-bioactive functions. However, the multi-bioactivities and spectral stability of phycocyanin are susceptible to external environmental conditions, which limit its wide application. Here, the structure, properties, and biological activity of phycocyanin were discussed. This review highlights the significance of the microcapsules’ wall materials which commonly protect phycocyanin from environmental interference and summarizes the current preparation principles and characteristics of microcapsules in food and pharma industries, including spray drying, electrospinning, electrospraying, liposome delivery, sharp-hole coagulation baths, and ion gelation. Moreover, the major technical challenge and corresponding countermeasures of phycocyanin microencapsulation are also appraised, providing insights for the broader application of phycocyanin. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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26 pages, 5099 KiB  
Review
Radix Asteris: Traditional Usage, Phytochemistry and Pharmacology of An Important Traditional Chinese Medicine
by Ke-Jie Li, Yang-Yang Liu, Dong Wang, Pei-Zheng Yan, De-Chao Lu and Dong-Sheng Zhao
Molecules 2022, 27(17), 5388; https://doi.org/10.3390/molecules27175388 - 24 Aug 2022
Cited by 4 | Viewed by 2170
Abstract
Radix Asteris (RA), also known as ‘Zi Wan’, is the dried root and rhizome of Aster tataricus L. f., which has been used to treat cough and asthma in many countries such as China, Japan, Korea and Vietnam. This article summarizes the available [...] Read more.
Radix Asteris (RA), also known as ‘Zi Wan’, is the dried root and rhizome of Aster tataricus L. f., which has been used to treat cough and asthma in many countries such as China, Japan, Korea and Vietnam. This article summarizes the available information on RA in ancient Chinese medicine books and modern research literature: its botanical properties, traditional uses, chemical composition, pharmacological activity, toxicity and quality control. Studies have shown that RA extracts contain terpenes, triterpenoid saponins, organic acids, peptides and flavonoids, and have various pharmacological activities such as anti-inflammatory, anti-tumor, anti-oxidation, and anti-depression. RA is considered to be a promising medicinal plant based on its traditional use, chemical constituents and pharmacological activities. However, there are few studies on its toxicity and the consistency of its components, which indicates the need for further in-depth studies on the toxicity and quality control of RA and its extracts. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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Other

Jump to: Research, Review

5 pages, 896 KiB  
Brief Report
Antiviral Activity of Porcine IFN-λ3 and IFN-α against Porcine Rotavirus In Vitro
by Lishuang Deng, Yue Yin, Zhiwen Xu, Fengqin Li, Jun Zhao, Huidan Deng, Zhijie Jian, Siyuan Lai, Xiangang Sun and Ling Zhu
Molecules 2022, 27(14), 4575; https://doi.org/10.3390/molecules27144575 - 18 Jul 2022
Cited by 2 | Viewed by 1454
Abstract
Interferons (IFNs) play a major role in the host’s antiviral innate immunity. In response to viral infection, IFNs bind their receptors and initiate a signaling cascade, leading to the accurate transcriptional regulation of hundreds of IFN-stimulated genes (ISGs). Porcine rotavirus (PoRV) belongs to [...] Read more.
Interferons (IFNs) play a major role in the host’s antiviral innate immunity. In response to viral infection, IFNs bind their receptors and initiate a signaling cascade, leading to the accurate transcriptional regulation of hundreds of IFN-stimulated genes (ISGs). Porcine rotavirus (PoRV) belongs to genus Rotavirus of the Reoviridae family; the infection is a global epidemic disease and a major threat to the pig industry. In this study, we found that IFN-λ3 inhibited the replication of PoRV in both MA104 cells and IPEC-J2 cells, and this inhibition was dose-dependent. Furthermore, the antiviral activity of IFN-λ3 was more potent in IPEC-J2 cells than in MA104 cells. Further research showed that IFN-λ3 and IFN-α might inhibit PoRV infection by activating ISGs, i.e., MxA, OASL and ISG15, in IPEC-J2 cells. However, the co-treatment of IFN-λ3 and IFN-α did not enhance the antiviral activity. Our data demonstrated that IFN-λ3 had antiviral activity against PoRV and may serve as a useful antiviral candidate against PoRV, as well as other viruses in swine. Full article
(This article belongs to the Special Issue Bioactive Compounds: From Extraction to Biological Evaluations)
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