A novel sesquiterpene quinone from Hainan sponge Dysidea villosa

被引:47
|
作者
Li, Yan [1 ]
Zhang, Yu [1 ]
Shen, Xu [1 ]
Guo, Yue-Wei [1 ]
机构
[1] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
关键词
Dysidea villosa; Sesquiterpene quinone; PTP1B inhibitory activity; TYPE-1; REVERSE-TRANSCRIPTASE; HUMAN PHOSPHOLIPASE A(2); CORAL SARCOPHYTON-LATUM; SELECTIVE INHIBITOR; VIRUS; HYDROQUINONES; DERIVATIVES; AVARONE;
D O I
10.1016/j.bmcl.2008.11.068
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new sesquiterpene quinone, 21-dehydroxybolinaquinone (5), together with two known related analogues, bolinaquinone (6) and dysidine (7), had been isolated from the Hainan sponge Dysidea villosa. The structure of the new compound 5 was elucidated on the basis of detailed analysis of spectroscopic data and by comparison with related model compounds. Compounds 5-7 were evaluated for the inhibitory activity against hPTP1B, a potential drug target for treatment of type-II diabetes and obesity, and cytotoxic activity against Hela cell line. The results showed that dysidine (7) had the strongest hPTP1B inhibitory activity with an IC50 value of 6.70 mu M and 6 had significant cytotoxic activity against Hela cell line with an IC50 value of 5.45 mu M. New compound 5 showed moderate PTP1B inhibitory activity and cytotoxicity with IC50 values of 39.50 and 19.45 mu M, respectively. (C) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码:390 / 392
页数:3
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