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Modern Natural Drug Discovery

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

Deadline for manuscript submissions: closed (31 December 2023) | Viewed by 1642

Special Issue Editor

School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China
Interests: organic synthesis; medicinal chemistry; drug synthesis; biological evaluation; anticancer agents
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Due to their diverse range of multidimensional chemical structures, natural products (NPs) and their derivatives have played and will continue to play a key role in drug discovery and structural diversity. Approximately 35 percent of chemical medicines originate directly or indirectly from natural products. NPs offer special features in comparison with conventional synthetic molecules, lending both advantages and challenges in the drug discovery process. NPs are a promising source for the discovery of scaffolds with high structural diversity and various bioactivities that can be directly developed or used as lead compounds for optimization into modern drugs. We believe that contemporary scientific and technological advances will provide a strong basis for NP-based drug discovery, further contributing to enhancing human health.

Dr. Wen-Wei Qiu
Guest Editor

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

  • natural products
  • drug discovery
  • bioactive
  • lead compound
  • structure–activity relationship optimization

Published Papers (2 papers)

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Research

16 pages, 3266 KiB  
Article
Synthesis and Anti-Inflammatory Activity of Ferulic Acid-Sesquiterpene Lactone Hybrids
by Xiyan Duan, Ning Liu, Ke Lv, Junqi Wang, Mingyue Li, Yanwei Zhang, Xiaoguang Huo, Shiqi Bao, Zhuo Shen and Xuemei Zhang
Molecules 2024, 29(5), 936; https://doi.org/10.3390/molecules29050936 - 21 Feb 2024
Viewed by 463
Abstract
Acute lung injury (ALI) is a respiratory failure disease associated with high mortality rates in patients. The primary pathological damage is attributed to the excessive release of pro-inflammatory mediators in pulmonary tissue. However, specific therapy for ALI has not been developed. In this [...] Read more.
Acute lung injury (ALI) is a respiratory failure disease associated with high mortality rates in patients. The primary pathological damage is attributed to the excessive release of pro-inflammatory mediators in pulmonary tissue. However, specific therapy for ALI has not been developed. In this study, a series of novel ferulic acid-parthenolide (FA-PTL) and ferulic acid-micheliolide (FA-MCL) hybrid derivatives were designed, synthesized, and evaluated for their anti-inflammatory activities in vitro. Compounds 2, 4, and 6 showed pronounced anti-inflammatory activity against LPS-induced expression of pro-inflammatory cytokines in vitro. Importantly, compound 6 displayed good water solubility, and treatment of mice with compound 6 (10 mg/kg) significantly prevented weight loss and ameliorated inflammatory cell infiltration and edema in lung tissue, as well as improving the alveolar structure. These results suggest that compound 6 (((1aR,7aS,8R,10aS,10bS,E)-8-((dimethylamino)methyl)-1a-methyl-9-oxo-1a,2,3,6,7,7a,8,9,10a,10b-decahydrooxireno[2′,3′:9,10]cyclodeca[1,2-b]furan-5-yl)methyl (E)-3-(4-hydroxy-3-methoxyphenyl)acrylate 2-hydroxypropane-1,2,3-tricarboxylate) might be considered as a lead compound for further evaluation as a potential anti-ALI agent. Full article
(This article belongs to the Special Issue Modern Natural Drug Discovery)
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13 pages, 3318 KiB  
Article
Gypenosides Synergistically Reduce the Extracellular Matrix of Hepatic Stellate Cells and Ameliorate Hepatic Fibrosis in Mice
by Han Li, Hanghang Wang, Aiping Yang, Mingzhen Xue, Junyang Wang, Qi Lv, Jian Liu, Lihong Hu, Yinan Zhang and Xiachang Wang
Molecules 2023, 28(14), 5448; https://doi.org/10.3390/molecules28145448 - 17 Jul 2023
Viewed by 931
Abstract
Liver fibrosis resulting from chronic liver damage is becoming one of the major threats to health worldwide. Active saponin constituents isolated from Gynostemma pentaphyllum were found to possess a protective effect in liver diseases. Here, we obtained a naturally abundant gypenoside, XLVI, and [...] Read more.
Liver fibrosis resulting from chronic liver damage is becoming one of the major threats to health worldwide. Active saponin constituents isolated from Gynostemma pentaphyllum were found to possess a protective effect in liver diseases. Here, we obtained a naturally abundant gypenoside, XLVI, and evaluated its liver protection activity in both animal and cellular models. The results showed that it ameliorated acute and chronic liver injuries and lightened the process of fibrogenesis in vivo. XLVI can inhibit TGF-β-induced activation of hepatic stellate cells and ECM deposition in vitro. The underlying mechanism study verified that it upregulated the protein expression of protein phosphatase 2C alpha and strengthened the vitality of the phosphatase together with a PP2Cα agonist gypenoside NPLC0393. These results shed new light on the molecular mechanisms and the potential therapeutic function of the traditional herb Gynostemma pentaphyllum in the treatment of liver fibrosis. Full article
(This article belongs to the Special Issue Modern Natural Drug Discovery)
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