New preaustinoids from a marine-derived fungal strain Penicillium sp. SF-5497 and their inhibitory effects against PTP1B activity

被引：16
|
作者：
Park, Jin-Soo [1 ]
Tran Hong Quang [2 ]
Nguyen Thi Thanh Ngan [3 ]
Sohn, Jae Hak [4 ]
Oh, Hyuncheol [1 ]
机构：
[1] Wonkwang Univ, Coll Pharm, Iksan 54538, South Korea
[2] VAST, Inst Marine Biochem, 18 Hoang Quoc Viet, Hanoi, Vietnam
[3] VAST, Inst Genome Res, 18 Hoang Quoc Viet, Hanoi, Vietnam
[4] Silla Univ, Coll Med & Life Sci, Busan 46958, South Korea
来源：
JOURNAL OF ANTIBIOTICS | 2019年 / 72卷 / 08期
关键词：
INSULIN SENSITIVITY; MEROTERPENES; PROTEIN; ASSOCIATION; DERIVATIVES; OBESITY;
D O I：
10.1038/s41429-019-0187-7
中图分类号：
Q81 [生物工程学（生物技术）]; Q93 [微生物学];
学科分类号：
071005 ; 0836 ; 090102 ; 100705 ;
摘要：
Chemical investigation of the marine-derived fungal isolate Penicillium sp. SF-5497 resulted in the isolation of two new preaustinoid-related meroterpenoids, named preaustinoid A6 (1) and preaustinoid A7 (2), along with three known metabolites (3-5). Their structures were elucidated by extensive spectroscopic analyses, such as 1D and 2D NMR and MS data. Among these, compounds 1 and 3 inhibited PTP1B activity in a dose-dependent manner, with IC50 values of 17.6 and 58.4 mu M, respectively. Furthermore, kinetic analyses indicated that compound 1 inhibited PTP1B in a noncompetitive manner, with the K-i value of 17.0 mu M.
引用
收藏
页码：629 / 633
页数：5
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