Human ACAT-1 and ACAT-2 inhibitory activities of pentacyclic triterpenes from the leaves of Lycopus lucidus TURCZ.
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 IC(50) values of 16.2+/-0.6 and 28.8+/-1.3 microM, respectively.
Lee
Woo Song
WS
National Research Laboratory of Lipid Metabolism & Atherosclerosis, Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-333, Republic of Korea.
Im
Kyung-Ran
KR
Park
Yong-Dae
YD
Sung
Nack-Do
ND
Jeong
Tae-Sook
TS
D000818:Animals; D002460:Cell Line; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D031333:Lycopus / Q000737:chemistry*; D015394:Molecular Structure; D009828:Oleanolic Acid / Q000302:isolation & purification / Q000494:pharmacology; D053978:Pentacyclic Triterpenes; D018515:Plant Leaves / Q000737:chemistry; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*; D014315:Triterpenes / Q000302:isolation & purification / Q000494:pharmacology*; D000094062:Betulinic Acid; D000097245:Ursolic Acid; D000097587:Sterol O-Acyltransferase 2
D004791:Enzyme Inhibitors; D009828:Oleanolic Acid; D053978:Pentacyclic Triterpenes; D002785:Sterol O-Acyltransferase; D014315:Triterpenes; D000094062:Betulinic Acid; D000097245:Ursolic Acid; D000097587:Sterol O-Acyltransferase 2; C493492:sterol O-acyltransferase 1