Inhibition of diacylglycerol acyltransferase by phenylpyropenes produced by Penicillium griseofulvum F1959.
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.
Lee
Seung Woong
SW
Natural Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejon 305-333, Korea.
Rho
Mun-Chual
MC
Choi
Jung-Ho
JH
Kim
Koanhoi
K
Choi
Yong Seok
YS
Lee
Hyun Sun
HS
Kim
Young Kook
YK
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
D006576:Heterocyclic Compounds, 4 or More Rings; D014280:Triglycerides; C471250:phenylpyropene A; C471251:phenylpyropene B; C455267:phenylpyropene C; D051048:Diacylglycerol O-Acyltransferase