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标题：Effects of 19-Oxygenated Lanosterol Derivatives on 3-Hydroxy-3-methylglutaryl Coenzyme A Reductase Activity and Lanosterol Demethylase Activity
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作者：Yoshiko SONODA ; Sachie SUZUKI ; Kinuyo UDAGAWA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1996
卷号：19
期号：1
页码：57-61
DOI：10.1248/bpb.19.57
出版社：The Pharmaceutical Society of Japan
摘要：The effects of 19-oxygenated lanosterol derivatives on lanosterol 14α-demethylase (P-450_14DM) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase activity were studied. 3β-Hydroxylanost-9 (11)-en-19-oic acid (6) was found to be an effective inhibitor (IC₅₀ : 0.5 μM) of P-450_14DM in the reconstituted system using purified pig liver P-450_14DM and was most active in inhibiting HMG-CoA reductase activity (IC₅₀ : 1.0μM) in mouse L cells. In [2-¹⁴C] acetate incorporation studies using mouse L cells, 6 was found to reduce the incorporation of acetate into C₂₇-sterol (desmosterol) with a concomitant increase in radiolabeled C₃₀-sterols. These results demonstrate that 6 is a dual-action inhibitor of cholesterol biosynthesis.
关键词：HMG-CoA reductase;cholesterol biosynthesis inhibitor;lanosterol demethylase;19-oxygenated lanosterol derivative;P-45014DM