共 32 条
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.
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页码:999 / 1002
页数:4
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