Article ID Journal Published Year Pages File Type
2474892 Acta Pharmaceutica Sinica B 2012 6 Pages PDF
Abstract

Microbial transformation of lovastatin (1) by resting cells of a filamentous fungus, Beauveria bassiana AS 3.4270, yielded five metabolites (2–6), which were unambiguously characterized by various spectroscopic data analyses. The occurred reactions included hydroxylation, lactone hydrolysis and methylation. The inhibitory effects of all metabolites on the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase were evaluated. Of the five compounds, 4 exhibited comparable inhibitory effect to lovastatin on the HMG-CoA reductase with IC50 value of 2.2 μM, and inhibitory rate of 81.4%.

Graphical abstractMicrobial transformation of lovastatin (1) by resting cells of a filamentous fungus, Beauveria bassiana AS 3.4270, yielded five metabolites (2–6), whose inhibitory effects on the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase were evaluated.Figure optionsDownload full-size imageDownload as PowerPoint slide

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Health Sciences Pharmacology, Toxicology and Pharmaceutical Science Drug Discovery
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