title: Inhibition of diacylglycerol acyltransferase by phenylpyropenes produced by Penicillium griseofulvum F1959.
abstract: Phenylpyropenes A, B, and C, isolated from Penicillium griseofulvum F1959, inhibited DGAT in rat liver microsomes with IC50 values of 78.7+/-1.6, 21.7+/-0.2, and 11.04+/-0.2 mM, respectively. In addition, a kinetic analysis using a Lineweaver-Burk plot revealed that phenylpyropene C was a noncompetitive inhibitor of DGAT. The apparent Michaelis constant (Km) value and inhibition constant (Ki) value were calculated to be 8 mM and 10.4 mM, respectively. Moreover, phenylpyropene C inhibited triglyceride formation in HepG2 cells.
authors.affiliation: Natural Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejon 305-333, Korea.
authors.forename: Seung Woong
authors.initials: SW
authors.lastname: Lee
authors.forename: Mun-Chual
authors.initials: MC
authors.lastname: Rho
authors.forename: Jung-Ho
authors.initials: JH
authors.lastname: Choi
authors.forename: Koanhoi
authors.initials: K
authors.lastname: Kim
authors.forename: Yong Seok
authors.initials: YS
authors.lastname: Choi
authors.forename: Hyun Sun
authors.initials: HS
authors.lastname: Lee
authors.forename: Young Kook
authors.initials: YK
authors.lastname: Kim
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D051048:Diacylglycerol O-Acyltransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006576:Heterocyclic Compounds, 4 or More Rings / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D008099:Liver / Q000648:ultrastructure; D008297:Male; D008861:Microsomes / Q000201:enzymology; D010407:Penicillium / Q000254:growth & development / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley; D014280:Triglycerides / Q000378:metabolism
chemical_list: D006576:Heterocyclic Compounds, 4 or More Rings; D014280:Triglycerides; C471250:phenylpyropene A; C471251:phenylpyropene B; C455267:phenylpyropene C; D051048:Diacylglycerol O-Acyltransferase