Use of everted sacs of mouse small intestine as enzyme sources for the study of drug oxidation activities in vitro

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
C EmotoT Yokoi

Abstract

1. The use of everted sacs of the small intestine as an enzyme source for the study of the first-pass metabolism of xenobiotics by cytochrome P450s (P450, CYP) is described. Several drug oxidation activities for testosterone, chlorzoxazone, tolbutamide, bufuralol and warfarin were observed when everted sacs (1-cm segment) from different parts of mouse small intestine were incubated with an NADPH-generating system and each substrate. 2. Most of the drug hydroxylase activities resided in the upper part of mouse small intestine and these activities were much higher than those of intestinal microsomes. Drug oxidation activities decreased along the distance from the upper part of the small intestine except for warfarin hydroxylation. 3. Testosterone 6beta-hydroxylation in the everted sacs exhibited the highest catalytic activities among the drug oxidations tested here. In the upper part of the small intestine, the testosterone 6beta-hydroxylase activities of everted sacs subjected once to freezing and thawing were substantially decreased compared with the untreated everted sacs. 4. Testosterone 6beta-hydroxylase activities in the everted sacs of the small intestine were significantly inhibited by ketoconazole. Immunoreactive protein...Continue Reading

References

Nov 1, 1990·Chemical Research in Toxicology·R PeterC S Yang
Nov 15, 1989·Cancer·D J Stralka, H W Strobel
Oct 1, 1987·The Journal of Clinical Investigation·P B WatkinsP S Guzelian
Feb 1, 1994·Clinical Pharmacokinetics·D R Krishna, U Klotz
Jan 1, 1994·Carcinogenesis·D W Rosenberg, D C Mankowski
Dec 1, 1995·Clinical Pharmacology and Therapeutics·K KashfiA J Dannenberg
Jul 1, 1996·Clinical Pharmacology and Therapeutics·M F PaineK E Thummel
Jul 1, 1996·Biological & Pharmaceutical Bulletin·S KitagawaM Sasaki
Apr 15, 1997·Archives of Biochemistry and Biophysics·T YanagimotoT Kamataki
Nov 5, 1997·Archives of Biochemistry and Biophysics·H Yamazaki, T Shimada
May 20, 1999·Annual Review of Pharmacology and Toxicology·F P Guengerich
Feb 5, 2000·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·T HansenA Bader
Apr 25, 2000·Archives of Biochemistry and Biophysics·T SakumaN Nemoto

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Citations

Mar 9, 2011·Cell Biology and Toxicology·Kevin J RandallJohn R Foster
Sep 14, 2007·Journal of Pharmaceutical Sciences·Hiroshi Komura, Masahiro Iwaki
May 12, 2009·Chemico-biological Interactions·P HodekM Stiborová
Jul 2, 2003·The Journal of Pharmacy and Pharmacology·X W TengN M Davies
Feb 9, 2012·The Journal of Pharmacy and Pharmacology·Mohd Aftab AlamAbdullah M Al-Mohizea
Oct 3, 2018·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Raditya IswandanaPeter Olinga
Oct 23, 2003·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Qing-Yu ZhangLaurence S Kaminsky
Jul 30, 2005·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Esther G van de KerkhofGeny M M Groothuis
Mar 28, 2006·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Marcella MartignoniRuben de Kanter
Nov 20, 2003·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Laurence S Kaminsky, Qing-Yu Zhang
Nov 19, 2005·The Journal of Pharmacology and Experimental Therapeutics·Anita A MathiasJashvant D Unadkat

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