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A Novel Sarsolenane Diterpene as a PTP1B Inhibitor from Hainan Soft Coral Sarcophyton trocheliophorum Marenzeller
Author(s) -
Liang Linfu,
Wang Jinan,
Shi Xiaoxuan,
Zhu Yinghua,
Li Jia,
Zhu Weiliang,
Wang Heyao,
Guo Yuewei
Publication year - 2017
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.201600819
Subject(s) - chemistry , diterpene , coral , stereochemistry , metabolite , inhibitory postsynaptic potential , enzyme , biochemistry , protein tyrosine phosphatase , neuroscience , ecology , biology
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 ( IC 50 =13.7 µmol•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.