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

作者：Maarisit Wilmar; Yamazaki Hiroyuki^*; Kanno Syu ichi; Tomizawa Ayako; Rotinsulu Henki; Wewengkang Defny S; Sumilat Deiske A; Ukai Kazuyo; Kapojos Magie M; Namikoshi Michio

来源：Bioorganic & Medicinal Chemistry Letters, 2017, 27(4): 999-1002.

DOI：10.1016/j.bmc1.2016.12.077

• Tetramic acid
• Melophlin
• Sarasinoside
• Marine sponge
• Petrosia sp.
• Protein tyrosine phosphatase 1B

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.

• 出版日期2017-2-15