论文部分内容阅读
综述了葡萄糖醛酸轭合反应在药物代谢转化中的作用研究进展。论述了催化药物葡萄糖醛酸轭合反应的葡萄糖醛酸转移酶(UDP-Glucuronosyltransferases,UGTs)的分布、分类及其底物多样性,药物葡萄糖醛酸轭合反应的产物类型,药物葡萄糖醛酸轭合反应的毒理药理效应等;阐述了药物代谢中的去葡萄糖醛酸轭合反应的风险和意义,脑部葡萄糖醛酸转移酶的分布活性及功能,葡萄糖醛酸轭合产物的分析方法,葡萄糖醛酸轭合反应过程的个体差异、种间差异等。研究表明,葡萄糖醛酸轭合反应是重要的药物清除与代谢反应,与药物代谢、药效、毒副作用及癌症的发生等关系密切。
The research progress on the role of glucuronide conjugation in drug metabolism and transformation was reviewed. The distribution, classification and substrate diversity of glucuronosyltransferases (UGTs) catalyzed by glucuronide conjugation catalyzed by glucuronidase were discussed. The product type of glucuronide conjugation of drug glucuronide Toxicology and pharmacological effects of co-reaction; described the risk and significance of the glucuronide conjugation reaction in the drug metabolism, the distribution activity and function of glucuronic acid transferase in the brain, the analysis method of glucuronic acid conjugate, Glucuronic acid conjugation reaction of individual differences, species differences and so on. Studies have shown that glucuronide conjugation reaction is an important drug clearance and metabolic reactions, and drug metabolism, efficacy, side effects and the occurrence of cancer are closely related.