| 論文名 |
In-line capillary electrophoretic evaluation of the enantioselective metabolism of verapamil by cytochrome P3A4. |
| 著者 |
L Asensi-Bernardi
Y Mart?n-Biosca
L Escuder-Gilabert
S Sagrado
M J Medina-Hern?ndez
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| キーワード |
|
| 出版年月 |
1970年1月 |
| 発表先 |
J Chromatogr A. 2013 Jul 12;1298:139-45. |
| WEBサイト |
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| 論文概要（和文） |
シトクロムP3A4によるベラパミルのエナンチオ選択的代謝のインラインキャピラリー電気泳動評価。 |
| 論文概要（英文） |
In this paper a methodology for the in-line evaluation of enantioselective metabolism by capillary electrophoresis has been developed and applied to the study of verapamil metabolism by cytochrome P3A4. The developed methodology comprises an in-capillary reaction step carried out by electrophoretically mediated microanalysis and a separation step in which highly sulfated β-cyclodextrin with partial filling technique has been employed as chiral selector for verapamil and norverapamil enantiomers resolution, joining the advantages of both methodologies in a unique assay. Kinetic parameters of the enzymatic reaction (Km and Vmax) have been evaluated for both verapamil enantiomers by non-linear fitting of experimental data obtained under intermediate precision conditions to Michaelis-Menten equation. Km and Vmax estimated values were 51±9 μM and 22±2 pmol min(-1) (pmol CYP)(-1) for S-VER and 47±9 μM and 21±2 pmol min(-1) (pmol CYP)(-1) for R-VER. Consequently, slight enantioselectivity was found for the CYP3A4 metabolism of verapamil. However, since confidence intervals of estimates overlap, we cannot assure a significant enantioselectivity. Intrinsic clearance values were also estimated from Km and Vmax for both enantiomers. |
