title: Acyl-CoA: cholesterol acyltransferase inhibitors from Ilex macropoda.
abstract: Twigs from Ilex macropoda were extracted with MeOH, and the concentrated extracts were partitioned with CH2Cl2, EtOAc, n-BuOH, and H2O. Repeated column chromatography of the CH2Cl2 fraction ultimately resulted in the isolation of two compounds, via activity-guided fractionation, using ACAT inhibitory activity measurements. According to the physico-chemical data, the chemical structures of these isolated compounds were identified as lupeol (1) and betulin (2). Compounds 1 and 2 were shown to inhibit the activity of hACAT-1 and hACAT-2 in a dose-dependent manner, and compounds 1 and 2 inhibited hACAT-1 with IC50 values of 48 and 83 microM, respectively.
authors.affiliation: College of Pharmacy, Woosuk University, Samrye, Korea.
authors.forename: Kyung-Ran
authors.initials: KR
authors.lastname: Im
authors.forename: Tae-Sook
authors.initials: TS
authors.lastname: Jeong
authors.forename: Byoung-Mog
authors.initials: BM
authors.lastname: Kwon
authors.forename: Nam-In
authors.initials: NI
authors.lastname: Baek
authors.forename: Sung-Hoon
authors.initials: SH
authors.lastname: Kim
authors.forename: Dae Keun
authors.initials: DK
authors.lastname: Kim
mesh_terms: D000818:Animals; D000924:Anticholesteremic Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D006801:Humans; D030017:Ilex / Q000737:chemistry*; D015394:Molecular Structure; D053978:Pentacyclic Triterpenes; D010936:Plant Extracts / Q000737:chemistry; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D014315:Triterpenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D000097587:Sterol O-Acyltransferase 2; D000094062:Betulinic Acid; D000094042:Lupanes
chemical_list: D000924:Anticholesteremic Agents; D004791:Enzyme Inhibitors; D053978:Pentacyclic Triterpenes; D010936:Plant Extracts; D002785:Sterol O-Acyltransferase; D014315:Triterpenes; D000097587:Sterol O-Acyltransferase 2; C002503:betulin; D000094062:Betulinic Acid; C493492:sterol O-acyltransferase 1; C010480:lupeol; D000094042:Lupanes