Dhami M S, Drangova R, Farkas R, Balazs T, Feuer G
Clin Chem. 1979 Jul;25(7):1263-6.
Treatment of rats with cefazolin in vivo significantly suppressed activity of alanine and aspartate aminotransferases in serum and in the liver, brain, kidney, and heart. Simultaneous administration of pyridoxal further reduced enzyme activity except in the liver, where there was no change. Pyridoxal 5'-phosphate partly reversed the decreased enzyme activity in the serum, liver, and kidney, but did not return it to the amount observed in the control animals; enzyme activity remained suppressed in the brain and heart. The effect of cefazolin was dose related, but there was no sex-related difference. In contrast to its action on am-notransferase activity, cefazolin elicited no effect on alkaline phosphatase (pyridoxal-5'-phosphate hydrolase) in serum or on pyruvate carboxylase in the liver, heart, and kidney. Cefazolin exposed to the hepatic microsomal mixed-function oxidase system in vitro was partly converted into metabolites that inhibited serum alanine aminotransferase activity in vitro. The latter inhibition was reversed by the addition of pyridoxal 5'-phosphate.
在体内用头孢唑林治疗大鼠可显著抑制血清以及肝脏、脑、肾和心脏中的丙氨酸和天冬氨酸转氨酶的活性。同时给予吡哆醛可进一步降低酶活性，但肝脏除外，肝脏中的酶活性没有变化。磷酸吡哆醛部分逆转了血清、肝脏和肾脏中酶活性的降低，但未使其恢复到对照动物中观察到的水平；脑和心脏中的酶活性仍受到抑制。头孢唑林的作用与剂量相关，但不存在性别差异。与它对氨基转移酶活性的作用相反，头孢唑林对血清中的碱性磷酸酶（磷酸吡哆醛水解酶）或肝脏、心脏和肾脏中的丙酮酸羧化酶没有影响。体外暴露于肝微粒体混合功能氧化酶系统的头孢唑林部分转化为代谢产物，这些代谢产物在体外抑制血清丙氨酸转氨酶活性。加入磷酸吡哆醛可逆转后者的抑制作用。
