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Discovery of novel capsaicin analogs as TRPV1 inhibitors for the treatment of idiopathic pulmonary fibrosis

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资源类型：
Pubmed体系：
作者：
Cao Yu[1,2,5] * ; Wen Yongju[1,3,5] ; Zhou Zongyuan[1,5] ; Xi Ruiying[1,5] ; Shuai Wen[2] ; Zhang Jichao[1,5] ; Suksamrarn Apichart[4] ; Zhang Guolin[1] ; Lu Xiao-Xia[1] ; Wang Fei[1] ;
机构： [1]Center for Natural Products Research, Chengdu Instiute of Biology, Chinese Academy of Sciences, Chengdu, 610041, PR China [2]State Key Laboratory of Biotherapy and Cancer Center, Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, National Clinical Research Center for Geriatrics, West China Hospital, and Collaborative Innovation Center of Biotherapy, Sichuan University, 610041, PR China [3]College of Chemistry and Biongineering Yichun University, Yichun, 336000, PR China [4]Department of Chemistry and Center of Exellence for Irnovation in Chemistry, Faculty of Science, Ramkhamhaeng University, Bangkok, 10240, Thailand [5]University of Chinese Acaderry of Sciences, Beljung, 100049, PR China
出处：
DOI： 10.1016/j.ejmech.2024.117229
ISSN：

关键词： Capsaicin analogs Idiopathic pulmonary fibrosls TGFp/Smads pathway MAPK pathway TRPV1 inhibilors

摘要：
Idiopathic pulmonary fibrosis (IPF) is a progressive and fatal interstitial lung disease for which few drugs are available in clinical practice. Here, we identified novel capsaicin analogs by combining in-house chemical library screening and further structural optimization. (E)-1-(3,4-dihydroxyphenyl)-7-phenylhept-1-en-3-one (Compound 14) was found to be the most potent in inhibiting TGF-β-induced collagen accumulation, proliferation and migration in fibroblast cells. Furthermore, compound 14 (IC50 = 0.51 ± 0.06 μM) showed over 100-fold increasing antifibrotic activity compared to capsaicin (IC50 = 53.71 ± 4.78 μM). Notably, compound 14 could target TRPV1, thereby affecting the expression of the fibrosis markers Collagen Ⅰ and α-SMA by inhibiting the TGF-β/Smads and MAPK pathways to exert antifibrotic activity in vitro. Compound 14 significantly inhibited collagen deposition in lung tissues, ameliorated alveolar structures, and increased survival rates in mice with bleomycin-induced pulmonary fibrosis. In addition, compound 14 possessed lower cytotoxicity (compared to nitedanib) and no toxicity in mice. Overall, compound 14 promise as a potential drug candidate for the treatment of IPF.Copyright © 2024 Elsevier Masson SAS. All rights reserved.

基金：
National Natural Science Foundation of China (no. 22177110 and 21977092), Biological Resources Pro- gramme, Chinese Academy of Sciences (KFJ-BRP-008), and the Sichuan Science and Technology Program (2023ZYD0042). Support from the Thailand Research Fund (no DBG6180030) is gratefully acknowledged.
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2025]版：
无
最新[2023]版：
大类 | 2 区 医学
小类 | 1 区 药物化学
第一作者：
第一作者机构： [1]Center for Natural Products Research, Chengdu Instiute of Biology, Chinese Academy of Sciences, Chengdu, 610041, PR China [2]State Key Laboratory of Biotherapy and Cancer Center, Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, National Clinical Research Center for Geriatrics, West China Hospital, and Collaborative Innovation Center of Biotherapy, Sichuan University, 610041, PR China [5]University of Chinese Acaderry of Sciences, Beljung, 100049, PR China
通讯作者：
推荐引用方式(GB/T 7714)：
Cao Yu,Wen Yongju,Zhou Zongyuan,et al.Discovery of novel capsaicin analogs as TRPV1 inhibitors for the treatment of idiopathic pulmonary fibrosis[J].European Journal Of Medicinal Chemistry.2025,284:117229.doi:10.1016/j.ejmech.2024.117229.
APA：
Cao Yu,Wen Yongju,Zhou Zongyuan,Xi Ruiying,Shuai Wen...&Wang Fei.(2025).Discovery of novel capsaicin analogs as TRPV1 inhibitors for the treatment of idiopathic pulmonary fibrosis.European Journal Of Medicinal Chemistry,284,
MLA：
Cao Yu,et al."Discovery of novel capsaicin analogs as TRPV1 inhibitors for the treatment of idiopathic pulmonary fibrosis".European Journal Of Medicinal Chemistry 284.(2025):117229

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