Journal
BIOLOGICAL & PHARMACEUTICAL BULLETIN
Volume 29, Issue 2, Pages 382-384Publisher
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/bpb.29.382
Keywords
Lycopus lucidus; acyl-CoA; cholesterol acytransferase (ACAT); pentacyclic triterpene; atherosclerosis
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Acyl-CoA: cholesterol acyltransferase (ACAT) catalyzes the acylation of cholesterol to cholesteryl ester with long chain fatty acids and ACAT inhibition is a useful strategy for treating hypercholesterolemia or atherosclerosis. Pentacyclic triterpenes, ursolic acid (1), oleanolic acid (2), and betulinic acid (3) were isolated from the methanol extracts of the leaves of Lycopus lucidus TURCZ. by bioassay-guided fractionation. The structures of compounds 1-3 were elucidated by their spectroscopic data analysis. Among them, betulinic acid (3) exhibited more potent human ACAT-1 and ACAT-2 inhibitory activities with IC50 values of 16.2 +/- 0.6 and 28.8 +/- 1.3 mu M, respectively.
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