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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anticholesteremic Agents / chemistry
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Anticholesteremic Agents / isolation & purification
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Anticholesteremic Agents / pharmacology
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / isolation & purification*
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Enzyme Inhibitors / pharmacology*
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Humans
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Ilex / chemistry*
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Molecular Structure
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Pentacyclic Triterpenes
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Plant Extracts / chemistry
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Sterol O-Acyltransferase / antagonists & inhibitors*
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Sterol O-Acyltransferase / metabolism
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Sterol O-Acyltransferase 2
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Triterpenes / chemistry
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Triterpenes / isolation & purification*
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Triterpenes / pharmacology*
Substances
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Anticholesteremic Agents
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Enzyme Inhibitors
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Pentacyclic Triterpenes
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Plant Extracts
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Triterpenes
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betulin
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Sterol O-Acyltransferase
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sterol O-acyltransferase 1
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lupeol