Saucerneol B derivatives as human acyl-CoA: cholesterol acyltransferase inhibitors.
A series of 2a-i were prepared from a lead compound, saucerneol B (1) for evaluating their acyl-CoA: cholesterol acyltransferase inhibitory activities. Compounds 2a-g exhibited the high specificity of hACAT-1 than hACAT-2, whereas 2h and 2i showed very weak inhibitory activities in both hACAT-1 and hACAT-2. Saucerneol B (1) exhibited strong cholesterol-lowering effect in high cholesterol-fed mice.
Jeong
Tae-Sook
TS
Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-333, Korea.
Kim
Kyung Soon
KS
Yu
Hana
H
Kim
Mi Jeong
MJ
Cho
Kyung-Hyun
KH
Choi
Yang-Kyu
YK
Kim
Hyoung-Chin
HC
Park
Ho-Yong
HY
Lee
Woo Song
WS
D000214:Acyl Coenzyme A / Q000378:metabolism*; D000818:Animals; D000924:Anticholesteremic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D005663:Furans / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D015603:Keratinocytes / Q000187:drug effects* / Q000378:metabolism; D017705:Lignans / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
D000214:Acyl Coenzyme A; D000924:Anticholesteremic Agents; D005663:Furans; D017705:Lignans; C446969:saucerneol B; D002785:Sterol O-Acyltransferase