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

作者信息

Abdjul Delfly B, Yamazaki Hiroyuki, Takahashi Ohgi, Kirikoshi Ryota, Mangindaan Remy E P, Namikoshi Michio

机构信息

Faculty of Pharmaceutical Sciences, Tohoku Pharmaceutical University, Sendai 981-8558, Japan.

Faculty of Pharmaceutical Sciences, Tohoku Pharmaceutical University, Sendai 981-8558, Japan.

出版信息

Bioorg Med Chem Lett. 2015 Feb 15;25(4):904-7. doi: 10.1016/j.bmcl.2014.12.058. Epub 2014 Dec 30.

DOI:10.1016/j.bmcl.2014.12.058
PMID:25595683
Abstract

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 α,β-unsaturated-γ-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 7.47μM, respectively. On the other hand, compounds 2 and 4 (24S-isomers of 1 and 3, respectively) showed much reduced activity than the 24R-isomers.

摘要

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