title: Inhibitory effects of Polygonum cuspidatum water extract (PCWE) and its component resveratrol [correction of rasveratrol] on acyl-coenzyme A-cholesterol acyltransferase activity for cholesteryl ester synthesis in HepG2 cells.
abstract: The pharmacological effects of Polygonum cuspidatum water extract (PCWE) on lipid biosynthesis were investigated in cultured human hepatocyte HepG2 cells. The addition of PCWE (5 and 20 microg/ml), which had no effect on cell proliferation and cellular protein content, caused a marked decrease in the cellular cholesterol content, particularly, the cholesteryl ester content following 24 h of incubation. The incorporation of (14)C-oleate into the cellular cholesteryl ester fraction was also reduced remarkably during incubation for 6 and 24 h. The effect of PCWE on acyl-coenzyme A-cholesterol acyltransferase (ACAT) activity were studied in vitro to explore the mechanism by which PCWE inhibits cholesterol ester formation. The data confirmed that PCWE, in a dose dependent manner, remarkably inhibits ACAT activity. Among the main active chemicals of P. cuspidatum, resveratrol, a kind of flavonoid, decreased ACAT activity in a dose-dependent manner from the level of 10(-3) M. Theses results strongly suggest that PCWE reduces the cholesteryl ester formation in human hepatocytes by inhibiting ACAT.
authors.affiliation: Faculty of Biotechnology, Dong-A University, Saha-Gu, Pusan 604-712, Republic of Korea.
authors.forename: Cheol-Soo
authors.initials: CS
authors.lastname: Park
authors.forename: Young-Choon
authors.initials: YC
authors.lastname: Lee
authors.forename: Jong-Dae
authors.initials: JD
authors.lastname: Kim
authors.forename: Hyung-Min
authors.initials: HM
authors.lastname: Kim
authors.forename: Cheorl-Ho
authors.initials: CH
authors.lastname: Kim
mesh_terms: D000818:Animals; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D002788:Cholesterol Esters / Q000096:biosynthesis*; D004305:Dose-Response Relationship, Drug; D045468:Fallopia japonica; D022781:Hepatocytes / Q000166:cytology / Q000201:enzymology / Q000378:metabolism; D006801:Humans; D008862:Microsomes, Liver / Q000201:enzymology / Q000378:metabolism; D010936:Plant Extracts / Q000494:pharmacology; D018517:Plant Roots; D051381:Rats; D000077185:Resveratrol; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013267:Stilbenes / Q000494:pharmacology*; D014867:Water
chemical_list: D002788:Cholesterol Esters; D010936:Plant Extracts; D013267:Stilbenes; D014867:Water; D002785:Sterol O-Acyltransferase; D000077185:Resveratrol