生理硫醇存在下硫唑嘌呤和甲硫唑嘌呤巯基解的比较动力学

Comparative kinetics of azathioprine and metazathioprine mercaptolysis in presence of physiological thiols.

作者信息

Chrzanowska Maria, Hałas Agnieszka, Kuehn Marta, Hermann Tadeusz

机构信息

Department of Physical Pharmacy and Pharmacokinetics, University of Medical Sciences, 6 Swiecickiego Str., 60 781 Poznań, Poland.

出版信息

Acta Pol Pharm. 2003 Jul-Aug;60(4):269-73.

PMID:14714854

Abstract

Kinetic parameters of mercaptolysis of azathioprine (AZA) and metazathioprine (MAZA) to 6-mercaptopurine in phosphate buffer, pH 7.4, under the influence of physiological thiols (glutathione and cysteine) at 25 degrees, 30 degrees and 37 degrees C were determined and compared. It comes out that the mercaptolysis of MAZA is significantly faster under the influence of both mentioned thiols if compared to that reaction of AZA. Furthermore, the mercaptolysis of MAZA and AZA proceeded significantly faster under the influence of cysteine than on the glutathione heterolysis.

摘要

在25℃、30℃和37℃下，研究了在生理硫醇（谷胱甘肽和半胱氨酸）影响下，硫唑嘌呤（AZA）和甲硫唑嘌呤（MAZA）在pH 7.4的磷酸盐缓冲液中巯解生成6-巯基嘌呤的动力学参数，并进行了比较。结果表明，与AZA的反应相比，在上述两种硫醇的影响下，MAZA的巯解速度明显更快。此外，与谷胱甘肽的水解作用相比，在半胱氨酸的影响下，MAZA和AZA的巯解速度明显更快。