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Synthesis and biological evaluation of amino-conjugated bile acid derivatives against non-alcoholic steatohepatitis

文献类型：期刊论文

作者Wu, Zhitao2,3; Zhang, Mingge1,2; Yan, Meng Kun1,2; Li, Chenyue2,4; Pan, Guoyu1,2,3; Xuan, Lijiang1,2,3
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2025-07-01
卷号122页码:6
关键词Non-alcoholic steatohepatitis (NASH) Bile acid derivatives Anti-lipid accumulation activities Anti-inflammatory activities Anti-fibrosis activities
ISSN号0960-894X
DOI10.1016/j.bmcl.2025.130210
英文摘要Non-alcoholic steatohepatitis (NASH) is emerging as a rapidly growing health concern. Bile acids (BAs) function as endocrine signaling molecules and exhibit therapeutic potential for NASH. To develop safer and more effective BA derivatives for NASH treatment, 25 amino acid-conjugated bile acid derivatives were designed and synthesized based on the pharmacological properties of the leading compound A17. The anti-lipid accumulation, antiinflammatory and anti-fibrosis activities of these compounds were evaluated, and their structure-activity relationships were elucidated. Notably, compound C04 exhibited superior in vitro activity compared to obeticholic acid and demonstrated enhanced efficacy in improving both NASH and fibrosis in preclinical murine models via oral administration. These findings suggest that C04 is a promising candidate for NASH treatment and warrants further investigation.
资助项目State Key Laboratory of Drug Research[SIMM1601ZZ-03] ; National Natural Science Foun-dation of China[82373746] ; National Natural Science Foun-dation of China[82173878] ; Shanghai Municipal Science and Technology Major Project[TM202301L001]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:001461841000001
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/316953]  
专题新药研究国家重点实验室
通讯作者Pan, Guoyu; Xuan, Lijiang
作者单位1.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
2.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, 501 Haike Rd, Shanghai 201203, Peoples R China
3.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210029, Peoples R China
4.Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Wu, Zhitao,Zhang, Mingge,Yan, Meng Kun,et al. Synthesis and biological evaluation of amino-conjugated bile acid derivatives against non-alcoholic steatohepatitis[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2025,122:6.
APA Wu, Zhitao,Zhang, Mingge,Yan, Meng Kun,Li, Chenyue,Pan, Guoyu,&Xuan, Lijiang.(2025).Synthesis and biological evaluation of amino-conjugated bile acid derivatives against non-alcoholic steatohepatitis.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,122,6.
MLA Wu, Zhitao,et al."Synthesis and biological evaluation of amino-conjugated bile acid derivatives against non-alcoholic steatohepatitis".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 122(2025):6.

入库方式： OAI收割

来源：上海药物研究所

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