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KMID : 0613820170270030325
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Journal of Life Science
2017 Volume.27 No. 3 p.325 ~ p.333
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Screening of Phenolic Compounds with Inhibitory Activities against HMG-CoA Reductase
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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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High level of plasma cholesterol is strongly associated with the development of atherosclerosis and coronary heart disease. Clinical trials designed to reduce plasma cholesterol level by diet or pharmacological intervention have resulted in marked reduction of disease incidence. The enzyme 3-hydroxy- 3-methylglutaryl coenzyme A (HMG-CoA) reductase which reduces cholesterol biosynthesis in the liver is the key enzyme of the mevalonate pathway that produces cholesterol. In this study, 71 naturally occurring phenolic compounds were tested for inhibitory activities against HMG-CoA reductase. Eleven compounds out of 71 showed inhibitory activities: three hydrolyzable tannin (geraniin, acetonyl geraniin and pentagalloyl β-D-glucose), four benzoic acid derivatives (benzoic acid, trans-cinnamic acid, 2,4-dihydroxybenzoic acid and 2,5-dihydroxybenzoic acid), and four naphthoquinone derivatives (1,2-naphthoquinone, 1,4-naphthoquinone, plumbagin and shikonin). At the concentration of 10 μg/ml, 1,4-naphthoquinone inhibited HMG-CoA reductase by 99.4%, and then plumbagin 91.4%, pentagalloyl β-D-glucose 46.6%, 2,4-dihydroxybenzoic acid 40.9%, shikonin 37.7%, 1,2-naphthoquinone 36.6%, trans-cinnamic acid 32.0%, acetonyl geraniin 30.2%, benzoic acid 28.5%, geraniin 28.3% and 2,5-dihydroxybenzoic acid 22.3%, respectively. IC50 values of 1,4-naphthoquinone and plumbagin was 2.1 μg/ml and 5.8 μg/ml, respectively.
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KEYWORD
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HMG CoA reductase, 1, 4-naphthoquinone, plumbagin, pentagalloyl β-D-glucose
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