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KMID : 0613820180280020247
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Journal of Life Science
2018 Volume.28 No. 2 p.247 ~ p.256
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Screening of Flavonoid Compounds with HMG-CoA Reductase Inhibitory Activities
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Son Kun-Ho
Lee Ju-Yeon
Lee Jeong-Soon
Kang Sam-Sik
Sohn Ho-Yong
Kwon Chong-Suk
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Abstract
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3-Hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors (statins) are widely used drugs for lowering blood lipid levels and preventing cardiovascular diseases. HMG-CoA reductase is a key enzyme to control the biosynthesis of cholesterol. We have tested HMG-CoA reductase-inhibitory activity on the flavonoids of 98 species in vitro. The anti-hypercholesterolemic activities of flavonoids were studied using an HMG-CoA reductase assay equipped with a 96-well UV plate. This assay was based on the spectrophotometric measurement of the decrease in absorbance, which represents the oxidation of NADPH by the catalytic subunit of HMG-CoA reductase in the presence of the substrate HMG-CoA. Among the clinically available statins, pravastatin was used as a positive control. Among the tested compounds, kuraridin, morin and sophoraflavanone G showed strong inhibition activities. In particular, morin and sophoraflavanone G inhibited HMG-CoA reductase by 45.0% and 54.6% at a concentration of 10 μg/ml, and the IC50 values were calculated to 13.31 μg/ml and 7.26 μg/ml respectively.
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KEYWORD
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HMG-CoA reductase, kuraridin, morin, sophoraflavanone G
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