title: Saucerneol B derivatives as human acyl-CoA: cholesterol acyltransferase inhibitors.
abstract: 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.
authors.affiliation: Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-333, Korea.
authors.forename: Tae-Sook
authors.initials: TS
authors.lastname: Jeong
authors.forename: Kyung Soon
authors.initials: KS
authors.lastname: Kim
authors.forename: Hana
authors.initials: H
authors.lastname: Yu
authors.forename: Mi Jeong
authors.initials: MJ
authors.lastname: Kim
authors.forename: Kyung-Hyun
authors.initials: KH
authors.lastname: Cho
authors.forename: Yang-Kyu
authors.initials: YK
authors.lastname: Choi
authors.forename: Hyoung-Chin
authors.initials: HC
authors.lastname: Kim
authors.forename: Ho-Yong
authors.initials: HY
authors.lastname: Park
authors.forename: Woo Song
authors.initials: WS
authors.lastname: Lee
mesh_terms: 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
chemical_list: D000214:Acyl Coenzyme A; D000924:Anticholesteremic Agents; D005663:Furans; D017705:Lignans; C446969:saucerneol B; D002785:Sterol O-Acyltransferase