Enantioselectivity of microsomal and cytosolic esterases in rat intestinal mucosa

S. K. Yang, Y. Y. Hsieh, W. C. Chang, J. D. Huang

研究成果: 雜誌貢獻文章

10 引文 (Scopus)

摘要

Enantioselectivity of esterases, contained in 9,000g supernatant fraction (S9) prepared from homogenate of small intestinal mucosa of male Sprague- Dawley rats and the subsequent 105,000g supernatant (cytosol) and pellet (microsomes) prepared from S9, was studied using racemic oxazepam 3-acetate (rac-OXA) as the substrate. Esterases in S9 were enantioselective in hydrolyzing either S-OXA or R-OXA, depending on a particular subcellular preparation. Cytosolic and microsomal esterases had opposite enantioselectivity and selectively hydrolyzed S-OXA and R-OXA, respectively. Enantioselectivity of esterases solubilized from microsomes with Triton X-100 (0.1%, w/v) was identical to that of the membrane-bound microsomal esterases. Cytosolic esterases were more sensitive to temperature than either solubilized or membrane-bound microsomal esterases. In the presence of paraoxon (1 μM), the esterases selective toward R-OXA in both microsomes and S9 were completely inhibited, whereas the esterases selective toward S-OXA in cytosol were inhibited by ~6%. These results indicate that cytosolic and microsomal esterases in rat small intestinal mucosa are distinctly different enzymes, with opposite enantioselectivity in the hydrolysis of rac-OXA.

原文英語
頁(從 - 到)719-725
頁數7
期刊Drug Metabolism and Disposition
20
發行號5
出版狀態已發佈 - 1992
對外發佈Yes

指紋

Enantioselectivity
Esterases
Intestinal Mucosa
Rats
Microsomes
Cytosol
Paraoxon
Mucous Membrane
Membranes
Octoxynol
Sprague Dawley Rats
Asp(5)-oxytocin
Hydrolysis
Temperature
Enzymes

ASJC Scopus subject areas

  • Pharmacology
  • Toxicology

引用此文

Enantioselectivity of microsomal and cytosolic esterases in rat intestinal mucosa. / Yang, S. K.; Hsieh, Y. Y.; Chang, W. C.; Huang, J. D.

於: Drug Metabolism and Disposition, 卷 20, 編號 5, 1992, p. 719-725.

研究成果: 雜誌貢獻文章

Yang, S. K. ; Hsieh, Y. Y. ; Chang, W. C. ; Huang, J. D. / Enantioselectivity of microsomal and cytosolic esterases in rat intestinal mucosa. 於: Drug Metabolism and Disposition. 1992 ; 卷 20, 編號 5. 頁 719-725.
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