Two new protein tyrosine phosphatase 1B inhibitors, hyattellactones A and B, from the Indonesian marine sponge Hyattella sp.

被引:31
作者
Abdjul, Delfly B. [1 ]
Yamazaki, Hiroyuki [1 ]
Takahashi, Ohgi [1 ]
Kirikoshi, Ryota [1 ]
Mangindaan, Remy E. P. [2 ]
Namikoshi, Michio [1 ]
机构
[1] Tohoku Pharmaceut Univ, Fac Pharmaceut Sci, Sendai, Miyagi 9818558, Japan
[2] Sam Ratulangi Univ, Fac Fisheries & Marine Sci, Manado 95115, Indonesia
关键词
Hyattellactone; Scalarane sesterterpene; Marine sponge; Hyattella sp; PTP1B inhibitor; Phyllofolactone; TARGET; PTP1B;
D O I
10.1016/j.bmcl.2014.12.058
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Two unique sesterterpenes, hyattellactones A (1) and B (2), together with two known sesterterpenes, phyllofolactones F (3) and G (4), were isolated from the Indonesian marine sponge Hyattella sp. The structures of the two new compounds, 1 and 2 were assigned based on their spectroscopic data. Hyattellactone A (1) was a scalarane sesterterpene with an alpha, beta-unsaturated-gamma-lactone ring and C-ethyl group, while B (2) was an epimer of 1 at the C-24 position. Compounds 1 and 3 inhibited PTP1B activity with IC50 values of 7.45 and 7.47 mu M, respectively. On the other hand, compounds 2 and 4 (24S-isomers of 1 and 3, respectively) showed much reduced activity than the 24R-isomers. (C) 2014 Elsevier Ltd. All rights reserved.
引用
收藏
页码:904 / 907
页数:4
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