Two selective novel triterpene glycosides from sea cucumber, Telenata ananas:: Inhibitors of chemokine receptor-5

被引:35
作者
Hegde, VR
Chan, TM
Pu, HY
Gullo, VP
Patel, MG
Das, P
Wagner, N
Parameswaran, PS
Naik, CG
机构
[1] Schering Plough Corp, Res Inst, Kenilworth, NJ 07033 USA
[2] Natl Inst Oceanog, Panaji, Goa, India
关键词
D O I
10.1016/S0960-894X(02)00599-1
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
The aqueous methanolic extract of a sea cucumber was found to contain two triterpene glycosides 1 and 2. The structures of 1 and 2 were established based on high-resolution NMR studies. Compounds 1 and 2 exhibited inhibitory activity (K-i) of 30 and 5 muM, respectively, in a chemokine receptor subtype 5 (CCR5) assay. Both compounds did not show any significant inhibition in a CXCR2 assay at 50 muM, suggesting their selectivity for the CCR5 receptor. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:3203 / 3205
页数:3
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