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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Cell Line, Tumor
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Diacylglycerol O-Acyltransferase / antagonists & inhibitors*
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Diacylglycerol O-Acyltransferase / metabolism
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Heterocyclic Compounds, 4 or More Rings / chemistry
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Heterocyclic Compounds, 4 or More Rings / metabolism*
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Heterocyclic Compounds, 4 or More Rings / pharmacology*
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Humans
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Kinetics
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Liver / ultrastructure
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Male
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Microsomes / enzymology
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Penicillium / growth & development
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Penicillium / metabolism*
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Rats
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Rats, Sprague-Dawley
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Triglycerides / metabolism
Substances
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Heterocyclic Compounds, 4 or More Rings
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Triglycerides
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phenylpyropene A
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phenylpyropene B
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phenylpyropene C
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Diacylglycerol O-Acyltransferase