期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 4, 页码 999-1002出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.12.077
关键词
Tetramic acid; Melophlin; Sarasinoside; Marine sponge; Petrosia sp.; Protein tyrosine phosphatase 1B
资金
- Kanae Foundation for the Promotion of Medical Science
- Basic Science Research Projects from The Sumitomo Foundation
During the search for protein tyrosine phosphatase 1B (PTP1B) inhibitors from marine organisms, the known tetramic acid derivative, melophlin C (1), was isolated as an active component together with the new nortriterpenoid saponin, sarasinoside S (2), and three homologues: sarasinosides A1 (3), I-1 (4), and J (5), from the Indonesian marine sponge Petrosia sp. The structure of 2 was elucidated on the basis of its spectroscopic data. Compound 1 inhibited PTP1B activity with an IC50 value of 14.6 mu M, while compounds 2-5 were not active at 15.2-16.0 mu M. This is the first study to report the inhibitory effects of a tetramic acid derivative on PTP1B activity. (C) 2017 Elsevier Ltd. All rights reserved.
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