A tetramic acid derivative with protein tyrosine phosphatase 1B inhibitory activity and a new nortriterpene glycoside from the Indonesian marine sponge Petrosia sp.

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• 作者：Wilmar Maarisit^a ; ^b ; Hiroyuki Yamazaki^a ; ^{yamazaki@tohoku-mpu.ac.jp} ; Syu-ichi Kanno^a ; Ayako Tomizawa^a ; Henki Rotinsulu^c ; Defny S. Wewengkang^c ; Deiske A. Sumilat^b ; Kazuyo Ukai^a ; Magie M. Kapojos^d ; Michio Namikoshi^a
• 关键词：Tetramic acid ; Melophlin ; Sarasinoside ; Marine sponge ; Petrosia sp. ; Protein tyrosine phosphatase 1B
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：27
• 期：4
• 页码：999-1002
• 全文大小：468 K
• 卷排序：27

文摘

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), I1 (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 μM, while compounds 2–5 were not active at 15.2–16.0 μM. This is the first study to report the inhibitory effects of a tetramic acid derivative on PTP1B activity.