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

被引:13
|
作者
Maarisit, Wilmar [1 ,2 ]
Yamazaki, Hiroyuki [1 ]
Kanno, Syu-ichi [1 ]
Tomizawa, Ayako [1 ]
Rotinsulu, Henki [3 ]
Wewengkang, Defny S. [3 ]
Sumilat, Deiske A. [2 ]
Ukai, Kazuyo [1 ]
Kapojos, Magie M. [4 ]
Namikoshi, Michio [1 ]
机构
[1] Tohoku Med & Pharmaceut Univ, Fac Pharmaceut Sci, Sendai, Miyagi 9818558, Japan
[2] Sam Ratulangi Univ, Fac Fisheries & Marine Sci, Kampus Bahu, Manado 95115, Indonesia
[3] Sam Ratulangi Univ, Fac Math & Nat Sci, Kampus Bahu, Manado 95115, Indonesia
[4] Univ Pembangunan Indonesia, Fac Nursing, Bahu 95115, Manado, Indonesia
关键词
Tetramic acid; Melophlin; Sarasinoside; Marine sponge; Petrosia sp; Protein tyrosine phosphatase 1B; NATURAL-PRODUCTS; MELOPHLUS-SARASSINORUM; ASTEROPUS-SARASINOSUM; DIABETES TREATMENT; OLIGOGLYCOSIDES; SAPONINS; TARGETS; CELLS; A1; C1;
D O I
10.1016/j.bmcl.2016.12.077
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:999 / 1002
页数:4
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