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KMID : 0545120130230091206
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Journal of Microbiology and Biotechnology
2013 Volume.23 No. 9 p.1206 ~ p.1211
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PTP1B Inhibitory Secondary Metabolites from Marine-Derived Fungal Strains Penicillium spp. and Eurotium sp.
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Sohn Jae-Hak
Lee Yu-Ri
Lee Dong-Sung
Kim Youn-Chul
Oh Hyun-Cheol
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Abstract
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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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KEYWORD
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Penicillium, Eurotium, Fungal metabolites, protein tyrosine phosphatase 1B (PTP1B) inhibition, Enzyme kinetics analysis
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