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 analyse...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 hydroxyla-tion,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 ex hibited comparable inhibitory effect to lovastatin on the HMG-CoA reductase with ICso value of 2.2μM,and inhibitory rate of 81.4%.展开更多
基金This work was financially supported by the Science&Technology Project of Guangdong Province(No.2011A080403020)the National Science&Technology Major Project“Key New Drug Creation and Manufacturing”,China(No.2009ZX09301-003-4-1)the Program for New Century Excellent Talents in University(NCET-06-0155).
文摘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 hydroxyla-tion,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 ex hibited comparable inhibitory effect to lovastatin on the HMG-CoA reductase with ICso value of 2.2μM,and inhibitory rate of 81.4%.
