Effect of malotilate (diisopropyl 1,3-dithiol-2-ylidenemalonate) on drug metabolizing activity in rat liver microsomes.
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概要
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The effect of malotilate (diisopropyl 1, 3-dithiol-2-ylidenemalonate) on drug metabolizing activity in rat liver microsomes was examined. Malotilte (500 mg/kg/day) was administered orally to rats for 3 days. The contents of cytochrome P-450 (P-450) and cytochrome <I>b</I><SUB>5</SUB> (<I>b</I><SUB>5</SUB>), the activity of NADPH-cytochrome <I>c</I> reductase, and the metabolization of aniline, aminopyrine, benzo(a)pyrene (B(a)P) and 7-ethoxycoumarin (7-EC) in the microsomal fraction were examined 24 hr after the final administration of malotilate. The content of <I>b</I><SUB>5</SUB> and the activity of NADPH-cytochrome <I>c</I> reductase were increased by the malotilate treatment, but the content of P-450 was not significantly affected. 7-EC O-deethylation was markedly and aminopyrine N-demethylation was moderately enhanced; in contrast, aniline hydroxylation was significantly and B(a)P hydroxylation was slightly reduced. Such different effects of malotilate among the four substrate-metabolizing activities may be due mainly to the increase in the content of <I>b</I><SUB>5</SUB>, which participates in the transport of the second electron required for P-450 function to various extents. It is also possible that malotilate affects the population of P-450 subtypes, each having a different substrate specificity and a different affinity for <I>b</I><SUB>5</SUB>.
- 公益社団法人 日本薬理学会の論文
著者
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OKUNO Hiroyasu
Third Department of Internal Medicine, Kansai Medical University
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SHIOZAKI Yasuko
Third Department of Internal Medicine, Kansai Medical University
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Okuno Hiroyasu
Third Department Of Internal Medicine Kansai Medical University
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Shiozaki Yasuko
Third Department Of Internal Medicine Kansai Medical University
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MURASE Toshihiko
Third Department of Internal Medicine, Kansai Medical University
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SAMESHIMA Yoshiko
Third Department of Internal Medicine, Kansai Medical University
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NAKANISHI Sadao
Third Department of Internal Medicine, Kansai Medical University
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