title: ACAT inhibitory activity of exudates from Calocedrus macrolepis var. formosana.
abstract: Cholesterol acyltransferase (ACAT) is an enzyme controlling cholesterol esterification in cells. Large amounts of cholesterol esters accumulate in macrophages and smooth muscle cells of blood vessel walls resulting in the initial stages of atherosclerosis. Thus, atherosclerosis might be inhibited through inhibition of the activity of ACAT. In the present study, we identified by spectral analysis and chromatographic quantification that ferruginol was the most abundant component of exudates secreted from the wounding site of Calocedrus macrolepis Kurz var. formosana. Results obtained from the cholesterol absorption assay revealed that ferruginol exhibited a significant inhibitory activity on cholesterol absorption in mice macrophages (RAW 264.7 cell). Based on the results from analyzing the ratio of cholesterol esterification, ferruginol dose-dependently suppressed cholesterol esterification and the IC50 value was 2.0 microg/mL. In conclusion, ferruginol revealed strong inhibitory activities that retarded the absorption and esterification of cholesterol in cells. Our finding indicates that ferruginol might possess a potential for development as a pharmaceutical product for preventing arteriosclerosis.
authors: Molecular and Biological Agricultural Sciences Program, Taiwan International Graduate Program, National Chung-Hsing University and Academia Sinica, Taiwan.
authors: Yu-Hsin
authors: YH
authors: Hsieh
authors: Kuan-Jung
authors: KJ
authors: Chen
authors: Shih-Chang
authors: SC
authors: Chien
authors: Wen-Ling
authors: WL
authors: Cheng
authors: Jun-Hong
authors: JH
authors: Xiao
authors: Sheng-Yang
authors: SY
authors: Wang
mesh_terms: D045784:Abietanes / Q000737:chemistry / Q000494:pharmacology*; D000042:Absorption; D000818:Animals; D002784:Cholesterol / Q000737:chemistry; D002788:Cholesterol Esters / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D029779:Cupressaceae / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D010936:Plant Extracts / Q000494:pharmacology; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*
chemical_list: D045784:Abietanes; D002788:Cholesterol Esters; D010936:Plant Extracts; C431074:ferruginol; D002784:Cholesterol; D002785:Sterol O-Acyltransferase