PTP1B Inhibitory Secondary Metabolites from Marine-Derived Fungal Strains Penicillium spp. and Eurotium sp.

被引：23
作者：
Sohn, Jae Hak [1 ]
Lee, Yu-Ri [1 ]
Lee, Dong-Sung [2 ,3 ]
Kim, Youn-Chul [2 ,3 ]
Oh, Hyuncheol [2 ,3 ]
机构：
[1] Silla Univ, Coll Med & Life Sci, Pusan 617736, South Korea
[2] Wonkwang Univ, Hanbang Body Fluid Res Ctr, Iksan 570749, South Korea
[3] Wonkwang Univ, Coll Pharm, Inst Pharmaceut Res & Dev, Iksan 570749, South Korea
来源：
JOURNAL OF MICROBIOLOGY AND BIOTECHNOLOGY | 2013年 / 23卷 / 09期
关键词：
Penicillium; Eurotium; fungal metabolites; protein tyrosine phosphatase 1B (PTP1B) inhibition; enzyme kinetic analysis; TYROSINE-PHOSPHATASE; 1B; INSULIN SENSITIVITY; DERIVATIVES; RESISTANCE; OBESITY;
D O I：
10.4014/jmb.1303.03078
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：
The selective inhibition of PTP1B has been widely recognized as a potential drug target for the treatment of type 2 diabetes and obesity. In the course of screening for PTP1B inhibitory fungal metabolites, the organic extracts of several fungal species isolated from marine environments were found to exhibit significant inhibitory effects, and the bioassay-guided investigation of these extracts resulted in the isolation of fructigenine A (1), cyclopenol (2), echinulin (3), flavoglaucin (4), and viridicatol (5). The structures of these compounds were determined mainly by analysis of NMR and MS data. These compounds inhibited PTP1B activity with 50% inhibitory concentration values of 10.7, 30.0, 29.4, 13.4, and 64.0 mu M, respectively. Furthermore, the kinetic analysis of PTP1B inhibition by compounds 1 and 5 suggested that compound 1 inhibited PTP1B activity in a noncompetitive manner, whereas compound 5 inhibited PTP1B activity in a competitive manner.
引用
收藏
页码：1206 / 1211
页数：6
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