A Novel Sarsolenane Diterpene as a PTP1B Inhibitor from Hainan Soft Coral Sarcophyton trocheliophorum Marenzeller

被引：6

作者：

Liang, Linfu ^{[1
,2
]}

Wang, Jinan ^{[3
]}

Shi, Xiaoxuan ^{[1
]}

Zhu, Yinghua ^{[1
]}

Li, Jia ^{[2
]}

Zhu, Weiliang ^{[3
]}

Wang, Heyao ^{[2
]}

Guo, Yuewei ^{[2
]}

机构：

[1] Cent South Univ Forestry & Technol, Coll Mat Sci & Engn, Changsha 410004, Hunan, Peoples R China

[2] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China

[3] Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China

来源：

CHINESE JOURNAL OF CHEMISTRY | 2017年 / 35卷 / 08期

基金：

中国博士后科学基金; 中国国家自然科学基金;

关键词：

Sarcophyton trocheliophrum; sarsolenane; structure elucidation; PTP1B inhibitory activity; binding mode; TYROSINE-PHOSPHATASE; 1B; NATURAL-PRODUCTS; CEMBRANOIDS; DISCOVERY;

D O I：

10.1002/cjoc.201600819

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A novel sarsolenane diterpene, named secodihydrosarsolenone (1), as a minor component was obtained from the South China Sea soft coral Sarcophyton trocheliophorum Marenzeller. Its structure was elucidated by detailed spectroscopic analysis. Compound 1 exhibited moderate inhibitory activity (IC50=13.7 mu mol center dot L-1) against protein tyrosine phosphatase 1B (PTP1B), a key target for the treatment of type 2 diabetes, representing the first report of PTP1B inhibitory activity for sarsolenane diterpenes. This discovery promotes computational prediction of binding mode between the enzyme and the metabolite, suggesting a crucial role of the residues Tyr46, Ser216 and Arg221 in the binding action.

引用

页码：1246 / 1250

页数：5

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