Intestinal Expression and Metabolic Activity of the CYP3A Subfamily in Female Rats

The intestinal expression of the CYP3A subfamily was investigated in female rats, and the intestinal metabolism of two CYP3A substrates, testosterone and rifabutin, was examined and compared between males and females. CYP3A1/23 and CYP3A2 intestinal expression was barely detected in male and female...

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Veröffentlicht in:Biological & pharmaceutical bulletin 2005, Vol.28(2), pp.311-315
Hauptverfasser: Aiba, Tetsuya, Yoshinaga, Mariko, Ishida, Kazuya, Takehara, Yutaka, Hashimoto, Yukiya
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container_title Biological & pharmaceutical bulletin
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creator Aiba, Tetsuya
Yoshinaga, Mariko
Ishida, Kazuya
Takehara, Yutaka
Hashimoto, Yukiya
description The intestinal expression of the CYP3A subfamily was investigated in female rats, and the intestinal metabolism of two CYP3A substrates, testosterone and rifabutin, was examined and compared between males and females. CYP3A1/23 and CYP3A2 intestinal expression was barely detected in male and female rats. Although CYP3A9 was predominantly expressed in the female rat liver, its expression in the intestine was not different between the two sexes. The rate of testosterone 6β-hydroxylation in the female intestine was similar to that for males. Rifabutin was also metabolized at similar rates in both intestines, although the metabolic rate was greater in the female liver. These results indicate that the intestinal drug metabolizing activity of the CYP3A subfamily is similar between males and females, and that CYP3A9 is involved in the intestinal metabolism of CYP3A substrates in both sexes.
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subjects Animals
Aryl Hydrocarbon Hydroxylases - biosynthesis
Aryl Hydrocarbon Hydroxylases - genetics
Aryl Hydrocarbon Hydroxylases - metabolism
CYP3A9
Cytochrome P-450 CYP3A
Female
Gene Expression Regulation, Enzymologic - physiology
intestinal metabolism
Intestinal Mucosa - metabolism
Intestines - enzymology
Male
Microsomes, Liver - enzymology
Microsomes, Liver - metabolism
Oxidoreductases, N-Demethylating - biosynthesis
Oxidoreductases, N-Demethylating - genetics
Oxidoreductases, N-Demethylating - metabolism
Rats
Rats, Wistar
rifabutin
RNA, Messenger - biosynthesis
RNA, Messenger - genetics
Substrate Specificity
testosterone
title Intestinal Expression and Metabolic Activity of the CYP3A Subfamily in Female Rats
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