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

자연과학 > 생물
( Jae Hak Sohn ) , ( Yu Ri Lee ) , ( Dong Sung Lee ) , ( Youn Chul Kim ) , ( Hyun Cheol Oh )
한국미생물생명공학회(구 한국산업미생물학회)
Journal of Microbiology and Biotechnology 2013년, 제23권 제9호, 1206~1211페이지(총6페이지)
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    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 μM, 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.
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