双峰驼肝脏CYP3A亚酶活性的初步研究

Preliminary Studies on CYP3A Sub-enzyme Activities of Bactrian Camel

CYP3A亚酶参与45％～60％常用药物的生物转化，在机体处置外源性物质的过程中发挥着重要作用。为了探讨双峰驼肝脏CYP3A亚酶活性，采用改进的钙离子沉淀法制备肝微粒悬液，并借助生物化学方法对双峰驼CYP3A亚酶活性进行了初步研究。结果表明，钙离子沉淀法制备的双峰驼肝微粒体蛋白含量为（1．541±0．264）mg／mL，CYP总酶含量为（0．412±0．063）nmol／mg，红霉素-N-脱甲基酶的活性为（1．159±0．001）nmol／（mg·min）。以上研究结果为今后借助探针药物检测双峰驼CYP3A亚酶的体外代谢活性的深入研究奠定了基础。

CYP3A sub-enzymes participate in biotransformation of 45%-60% of commonly used drugs, and play an important role in regulating the interaction of body and external environment and maintaining homeostasis. In order to study the activity of hepatic CYP3A sub-enzymes, the hepatic microsome was prepared by the Ca^2＋ precipitation method, and the activities of CYP3A sub-enzyme was preliminarily studied by using biochemical methods. The result showed that the protein content of hepatic microsome was （1.541±0.264） mg/mL, the content of total CYP was （0.412±0.063 ） nmol/mg, and the activity of erythromycin-N- demethylase was （1.159±0.001） nmol/（mg· min ）, respectively. The results laid a good foundation for further research of metabolic activity of CYP3A subfamily in vitro by using probe drug detection.