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

doi:10.1002/cjoc.201600819

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 天然药物化学研究室

	A Novel Sarsolenane Diterpene as a PTP1B Inhibitor from Hainan Soft Coral Sarcophyton trocheliophorum Marenzeller
	Liang, Linfu 1,3; Wang, Jinan 2; Shi, Xiaoxuan 3; Zhu, Yinghua 3; Li, Jia1 ; Zhu, Weiliang2 ; Wang, Heyao1 ; Guo, Yuewei1
刊名	CHINESE JOURNAL OF CHEMISTRY
	2017-08
卷号	35 期号:8 页码:1246-1250
关键词	Sarcophyton trocheliophrum sarsolenane structure elucidation PTP1B inhibitory activity binding mode
ISSN号	1001-604X
DOI	10.1002/cjoc.201600819
文献子类	Article
英文摘要	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.
资助项目	National Natural Science Foundation of China[41506187] ; National Natural Science Foundation of China[81520108028] ; National Natural Science Foundation of China[21672230] ; National Natural Science Foundation of China[41676073] ; National Natural Science Foundation of China[81603022] ; SCTSM Project[15431901000] ; SCTSM Project[14431901100] ; Hunan Provincial Natural Science Foundation of China[2015JJ3176] ; SKLDR/SIMM Projects[SIMM1501ZZ-03] ; China Postdoctoral Science Foundation[2016M601677]
WOS关键词	TYROSINE-PHOSPHATASE 1B ; NATURAL-PRODUCTS ; CEMBRANOIDS ; DISCOVERY
WOS研究方向	Chemistry
语种	英语
CSCD记录号	CSCD:6061193
出版者	WILEY-V C H VERLAG GMBH
WOS记录号	WOS:000407852800006
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/272542]
专题	天然药物化学研究室中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Guo, Yuewei
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China 3.Cent South Univ Forestry & Technol, Coll Mat Sci & Engn, Changsha 410004, Hunan, Peoples R China;
推荐引用方式 GB/T 7714	Liang, Linfu,Wang, Jinan,Shi, Xiaoxuan,et al. A Novel Sarsolenane Diterpene as a PTP1B Inhibitor from Hainan Soft Coral Sarcophyton trocheliophorum Marenzeller[J]. CHINESE JOURNAL OF CHEMISTRY,2017,35(8):1246-1250.
APA	Liang, Linfu.,Wang, Jinan.,Shi, Xiaoxuan.,Zhu, Yinghua.,Li, Jia.,...&Guo, Yuewei.(2017).A Novel Sarsolenane Diterpene as a PTP1B Inhibitor from Hainan Soft Coral Sarcophyton trocheliophorum Marenzeller.CHINESE JOURNAL OF CHEMISTRY,35(8),1246-1250.
MLA	Liang, Linfu,et al."A Novel Sarsolenane Diterpene as a PTP1B Inhibitor from Hainan Soft Coral Sarcophyton trocheliophorum Marenzeller".CHINESE JOURNAL OF CHEMISTRY 35.8(2017):1246-1250.