title: Inhibition of carbonyl reductase activity in pig heart by alkyl phenyl ketones.
abstract: The inhibitory effects of alkyl phenyl ketones on carbonyl reductase activity were examined in pig heart. In this study, carbonyl reductase activity was estimated as the ability to reduce 4-benzoylpyridine to S(-)-alpha-phenyl-4-pyridylmethanol in the cytosolic fraction from pig heart (pig heart cytosol). The order of their inhibitory potencies was hexanophenone > valerophenone > heptanophenone > butyrophenone > propiophenone. The inhibitory potencies of acetophenone and nonanophenone were much lower. A significant relationship was observed between Vmax/Km values for the reduction of alkyl phenyl ketones and their inhibitory potencies for carbonyl reductase activity in pig heart cytosol. Furthermore, hexanophenone was a competitive inhibitor for the enzyme activity. These results indicate that several alkyl phenyl ketones including hexanophenone inhibit carbonyl reductase activity in pig heart cytosol, by acting as substrate inhibitors.
authors: Graduate School of Pharmaceutical Sciences, Kumamoto University, 5-1, Oe-honmachi, Kumamoto 862-0973, Japan. yorishig@gpo.kumamoto-u.ac.jp
authors: Yorishige
authors: Y
authors: Imamura
authors: Rika
authors: R
authors: Narumi
authors: Hideaki
authors: H
authors: Shimada
mesh_terms: D000429:Alcohol Oxidoreductases / Q000037:antagonists & inhibitors*; D000818:Animals; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D007659:Ketones / Q000494:pharmacology*; D009206:Myocardium / Q000201:enzymology*; D013552:Swine
chemical_list: D004791:Enzyme Inhibitors; D007659:Ketones; D000429:Alcohol Oxidoreductases; C019642:alcohol dehydrogenase (NADP+)