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Anti-inflammatory and Antioxidant Properties of Natural Products and Their Derivatives

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

Deadline for manuscript submissions: closed (30 April 2022) | Viewed by 29023

Special Issue Editor


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Guest Editor
Department of Experimental Biology, Faculty of Science, Palacký University, Šlechtitelů 27, CZ-78371 Olomouc, Czech Republic
Interests: anti-inflammatory; medicinal plants; plant extracts; natural products; brassinosteroids
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Special Issue Information

Dear Colleagues,

Inflammation together with oxidation stress is associated with many diseases, and is currently a serious problem. The treatment of acute- or chronic-inflammation-related disorders by natural products is still in high demand by pharmaceutical companies due to the lack of effective anti-inflammatory drugs. The relative dearth of currently available anti-inflammatory drugs without side effects stimulates a search for new active substances. Natural products provide new potential anti-inflammatory and antioxidant compounds. Products coming from nature with anti-inflammatory and antioxidant activities could serve as a template for new derivatives based on this natural wealth.

New active anti-inflammatory and antioxidant natural compounds or extracts could be found in plants, plant products, mushrooms, marine organisms, and insects, and their products. Newly isolated, identified, or derivatized compounds are studied for their biological activity. Anti-inflammatory and antioxidant compounds are deeply investigated for their mechanisms of action and pharmacological activities.

This Special Issue “Anti-Inflammatory and Antioxidant Properties of Natural Products and Their Derivatives” invites researchers to contribute original research or review articles related to the anti-inflammatory activity or antioxidant properties (including mechanisms and pharmacological characterization) of extracts from plants, marine organisms, mushrooms, and insects, and their products, as well as their fractions or purified substances (extraction procedures, isolation, and identification).

Dr. Lucie Rárová
Guest Editor

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Keywords

  • Anti-inflammatory activity
  • Antioxidant properties
  • Natural products
  • Derivatives

Published Papers (6 papers)

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Research

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14 pages, 3216 KiB  
Article
Pinosylvin Shifts Macrophage Polarization to Support Resolution of Inflammation
by Konsta Kivimäki, Tiina Leppänen, Mari Hämäläinen, Katriina Vuolteenaho and Eeva Moilanen
Molecules 2021, 26(9), 2772; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26092772 - 08 May 2021
Cited by 15 | Viewed by 2878
Abstract
Pinosylvin is a natural stilbenoid found particularly in Scots pine. Stilbenoids are a group of phenolic compounds identified as protective agents against pathogens for many plants. Stilbenoids also possess health-promoting properties in humans; for instance, they are anti-inflammatory through their suppressing action on [...] Read more.
Pinosylvin is a natural stilbenoid found particularly in Scots pine. Stilbenoids are a group of phenolic compounds identified as protective agents against pathogens for many plants. Stilbenoids also possess health-promoting properties in humans; for instance, they are anti-inflammatory through their suppressing action on proinflammatory M1-type macrophage activation. Macrophages respond to environmental changes by polarizing towards proinflammatory M1 phenotype in infection and inflammatory diseases, or towards anti-inflammatory M2 phenotype, mediating resolution of inflammation and repair. In the present study, we investigated the effects of pinosylvin on M2-type macrophage activation, aiming to test the hypothesis that pinosylvin could polarize macrophages from M1 to M2 phenotype to support resolution of inflammation. We used lipopolysaccharide (LPS) to induce M1 phenotype and interleukin-4 (IL-4) to induce M2 phenotype in J774 murine and U937 human macrophages, and we measured expression of M1 and M2-markers. Interestingly, along with inhibiting the expression of M1-type markers, pinosylvin had an enhancing effect on the M2-type activation, shown as an increased expression of arginase-1 (Arg-1) and mannose receptor C type 1 (MRC1) in murine macrophages, and C-C motif chemokine ligands 17 and 26 (CCL17 and CCL26) in human macrophages. In IL-4-treated macrophages, pinosylvin enhanced PPAR-γ expression but had no effect on STAT6 phosphorylation. The results show, for the first time, that pinosylvin shifts macrophage polarization from the pro-inflammatory M1 phenotype towards M2 phenotype, supporting resolution of inflammation and repair. Full article
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13 pages, 3262 KiB  
Article
Oxyresveratrol Ameliorates Dextran Sulfate Sodium-Induced Colitis in Rats by Suppressing Inflammation
by Jiah Yeom, Seongho Ma, Jeong-Keun Kim and Young-Hee Lim
Molecules 2021, 26(9), 2630; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26092630 - 30 Apr 2021
Cited by 8 | Viewed by 1972
Abstract
Colitis causes destruction of the intestinal mucus layer and increases intestinal inflammation. The use of antioxidants and anti-inflammatory agents derived from natural sources has been recently highlighted as a new approach for the treatment of colitis. Oxyresveratrol (OXY) is an antioxidant known to [...] Read more.
Colitis causes destruction of the intestinal mucus layer and increases intestinal inflammation. The use of antioxidants and anti-inflammatory agents derived from natural sources has been recently highlighted as a new approach for the treatment of colitis. Oxyresveratrol (OXY) is an antioxidant known to have various beneficial effects on human health, such as anti-inflammatory, antibacterial activity, and antiviral activity. The aim of this study was to investigate the therapeutic effect of OXY in rats with dextran sulfate sodium (DSS)-induced acute colitis. OXY ameliorated DSS-induced colitis and repaired damaged intestinal mucosa. OXY downregulated the expression of pro-inflammatory cytokine genes (TNF-α, IL-6, and IL-1β) and chemokine gene MCP-1, while promoting the production of anti-inflammatory cytokine IL-10. OXY treatment also suppressed inflammation via inhibiting cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) expression in the colon, as well as the activity of myeloperoxidase (MPO). OXY exhibited anti-apoptotic effects, shifting the Bax/Bcl-2 balance. In conclusion, OXY might improve DSS-induced colitis by restoring the intestinal mucus layer and reducing inflammation within the intestine. Full article
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16 pages, 5117 KiB  
Article
Exploring Effects of Chitosan Oligosaccharides on the DSS-Induced Intestinal Barrier Impairment In Vitro and In Vivo
by Yujie Wang, Rong Wen, Dongdong Liu, Chen Zhang, Zhuo A. Wang and Yuguang Du
Molecules 2021, 26(8), 2199; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26082199 - 11 Apr 2021
Cited by 25 | Viewed by 3009
Abstract
Intestinal barrier dysfunction is an essential pathological change in inflammatory bowel disease (IBD). The mucus layer and the intestinal epithelial tight junction act together to maintain barrier integrity. Studies showed that chitosan oligosaccharide (COS) had a positive effect on gut health, effectively protecting [...] Read more.
Intestinal barrier dysfunction is an essential pathological change in inflammatory bowel disease (IBD). The mucus layer and the intestinal epithelial tight junction act together to maintain barrier integrity. Studies showed that chitosan oligosaccharide (COS) had a positive effect on gut health, effectively protecting the intestinal barrier in IBD. However, these studies usually focused on its impact on the intestinal epithelial tight junction. The influence of COS on the intestinal mucus layer is still poorly understood. In this study, we explored the effect of COS on intestinal mucus in vitro using human colonic mucus-secreted HT-29 cells. COS relieved DSS (dextran sulfate sodium)-induced mucus defects. Additionally, the structural characteristics of COS greatly influenced this activity. Finally, we evaluated the protective effect of COS on intestinal barrier function in mice with DSS-induced colitis. The results indicated that COS could manipulate intestinal mucus production, which likely contributed to its intestinal protective effects. Full article
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21 pages, 9787 KiB  
Article
Periplaneta americana Oligosaccharides Exert Anti-Inflammatory Activity through Immunoregulation and Modulation of Gut Microbiota in Acute Colitis Mice Model
by Kaimin Lu, Jing Zhou, Jie Deng, Yangjun Li, Chuanfang Wu and Jinku Bao
Molecules 2021, 26(6), 1718; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26061718 - 19 Mar 2021
Cited by 11 | Viewed by 2586
Abstract
The incidence and prevalence of inflammatory bowel disorders (IBD) are increasing around the world due to bacterial infection, abnormal immune response, etc. The conventional medicines for IBD treatment possess serious side effects. Periplaneta americana (P. americana), a traditional Chinese medicine, has [...] Read more.
The incidence and prevalence of inflammatory bowel disorders (IBD) are increasing around the world due to bacterial infection, abnormal immune response, etc. The conventional medicines for IBD treatment possess serious side effects. Periplaneta americana (P. americana), a traditional Chinese medicine, has been used to treat arthritis, fever, aches, inflammation, and other diseases. This study aimed to evaluate the anti-inflammatory effects of oligosaccharides from P. Americana (OPA) and its possible mechanisms in vivo. OPA were purified and biochemical characterization was analyzed by HPGPC, HPLC, FT-IR, and GC–MS. Acute colitis mice model was established, the acute toxicity and anti-inflammatory activity were tested in vivo. The results showed OPA with molecular mass of 1.0 kDa were composed of 83% glucose, 6% galactose, 11% xylose, and the backbone was (1→4)-Glcp. OPA had potent antioxidant activities in vitro and significantly alleviated the clinical symptoms of colitis, relieved colon damage without toxic side effects in vivo. OPA exhibited anti-inflammatory activity by regulating Th1/Th2, reducing oxidative stress, preserving intestinal barrier integrity, and inhibiting TLR4/MAPK/NF-κB pathway. Moreover, OPA protected gut by increasing microbial diversity and beneficial bacteria, and reducing pathogenic bacteria in feces. OPA might be the candidate of complementary and alternative medicines of IBD with low-cost and high safety. Full article
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18 pages, 5851 KiB  
Article
Stevioside Activates AMPK to Suppress Inflammation in Macrophages and Protects Mice from LPS-Induced Lethal Shock
by Fuyao Wei, Hong Zhu, Na Li, Chunlei Yu, Zhenbo Song, Shuyue Wang, Ying Sun, Lihua Zheng, Guannan Wang, Yanxin Huang, Yongli Bao and Luguo Sun
Molecules 2021, 26(4), 858; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26040858 - 06 Feb 2021
Cited by 13 | Viewed by 2817
Abstract
Stevioside, a diterpenoid glycoside, is widely used as a natural sweetener; meanwhile, it has been proven to possess various pharmacological properties as well. However, until now there were no comprehensive evaluations focused on the anti-inflammatory activity of stevioside. Thus, the anti-inflammatory activities of [...] Read more.
Stevioside, a diterpenoid glycoside, is widely used as a natural sweetener; meanwhile, it has been proven to possess various pharmacological properties as well. However, until now there were no comprehensive evaluations focused on the anti-inflammatory activity of stevioside. Thus, the anti-inflammatory activities of stevioside, both in macrophages (RAW 264.7 cells, THP-1 cells, and mouse peritoneal macrophages) and in mice, were extensively investigated for the potential application of stevioside as a novel anti-inflammatory agent. The results showed that stevioside was capable of down-regulating lipopolysaccharide (LPS)-induced expression and production of pro-inflammatory cytokines and mediators in macrophages from different sources, such as IL-6, TNF-α, IL-1β, iNOS/NO, COX2, and HMGB1, whereas it up-regulated the anti-inflammatory cytokines IL-10 and TGF-β1. Further investigation showed that stevioside could activate the AMPK -mediated inhibition of IRF5 and NF-κB pathways. Similarly, in mice with LPS-induced lethal shock, stevioside inhibited release of pro-inflammatory factors, enhanced production of IL-10, and increased the survival rate of mice. More importantly, stevioside was also shown to activate AMPK in the periphery blood mononuclear cells of mice. Together, these results indicated that stevioside could significantly attenuate LPS-induced inflammatory responses both in vitro and in vivo through regulating several signaling pathways. These findings further strengthened the evidence that stevioside may be developed into a therapeutic agent against inflammatory diseases. Full article
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Review

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24 pages, 12215 KiB  
Review
Flavonoids as Potential Anti-Inflammatory Molecules: A Review
by Jameel M. Al-Khayri, Gandasi Ravikumar Sahana, Praveen Nagella, Biljo V. Joseph, Fatima M. Alessa and Muneera Q. Al-Mssallem
Molecules 2022, 27(9), 2901; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27092901 - 02 May 2022
Cited by 186 | Viewed by 14688
Abstract
Hydroxylated polyphenols, also called flavonoids, are richly present in vegetables, fruits, cereals, nuts, herbs, seeds, stems, and flowers of numerous plants. They possess numerous medicinal properties such as antioxidant, anti-cancer, anti-microbial, neuroprotective, and anti-inflammation. Studies show that flavonoids activate antioxidant pathways that render [...] Read more.
Hydroxylated polyphenols, also called flavonoids, are richly present in vegetables, fruits, cereals, nuts, herbs, seeds, stems, and flowers of numerous plants. They possess numerous medicinal properties such as antioxidant, anti-cancer, anti-microbial, neuroprotective, and anti-inflammation. Studies show that flavonoids activate antioxidant pathways that render an anti-inflammatory effect. They inhibit the secretions of enzymes such as lysozymes and β-glucuronidase and inhibit the secretion of arachidonic acid, which reduces inflammatory reactions. Flavonoids such as quercetin, genistein, apigenin, kaempferol, and epigallocatechin 3-gallate modulate the expression and activation of a cytokine such as interleukin-1beta (IL-1β), Tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), and interleukin-8 (IL-8); regulate the gene expression of many pro-inflammatory molecules such s nuclear factor kappa-light chain enhancer of activated B cells (NF-κB), activator protein-1 (AP-1), intercellular adhesion molecule-1 (ICAM), vascular cell adhesion molecule-1 (VCAM), and E-selectins; and also inhibits inducible nitric oxide (NO) synthase, cyclooxygenase-2, and lipoxygenase, which are pro-inflammatory enzymes. Understanding the anti-inflammatory action of flavonoids provides better treatment options, including coronavirus disease 2019 (COVID-19)-induced inflammation, inflammatory bowel disease, obstructive pulmonary disorder, arthritis, Alzheimer’s disease, cardiovascular disease, atherosclerosis, and cancer. This review highlights the sources, biochemical activities, and role of flavonoids in enhancing human health. Full article
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