Cladosporamide A, a new protein tyrosine phosphatase 1B inhibitor, produced by an Indonesian marine sponge-derived Cladosporium sp

枝孢酰胺 A 是一种新型蛋白酪氨酸磷酸酶 1B 抑制剂,由印度尼西亚海洋海绵衍生的枝孢菌属产生

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作者:Henki Rotinsulu, Hiroyuki Yamazaki, Shino Sugai, Natsuki Iwakura, Defny S Wewengkang, Deiske A Sumilat, Michio Namikoshi

Abstract

Cladosporamide A (1), a new protein tyrosine phosphatase (PTP) 1B inhibitor, was isolated together with a known prenylated flavanone derivative (2) from the culture broth of an Indonesian marine sponge-derived Cladosporium sp. TPU1507 by solvent extraction, ODS column chromatography, and preparative HPLC (ODS). The structure of 1 was elucidated based on 1D and 2D NMR data. Compound 1 modestly inhibited PTP1B and T-cell PTP (TCPTP) activities with IC50 values of 48 and 54 μM, respectively. The inhibitory activity of 2 against PTP1B (IC50 = 11 μM) was approximately 2-fold stronger than that against TCPTP (IC50 = 27 μM).

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