Acyl-CoA: cholesterol acyltransferase inhibitors from Ilex macropoda.
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.
Im
Kyung-Ran
KR
College of Pharmacy, Woosuk University, Samrye, Korea.
Jeong
Tae-Sook
TS
Kwon
Byoung-Mog
BM
Baek
Nam-In
NI
Kim
Sung-Hoon
SH
Kim
Dae Keun
DK
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
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