[关键词]
[摘要]
葡萄糖醛酸结合反应是机体内重要的一类代谢反应, 其中O-葡萄糖醛酸结合是最常见的反应类型。O-葡萄糖醛酸苷的制备对于准确评估葡萄糖醛酸代谢产物的药理活性及安全性、药物代谢和药动学定量分析等研究至关重要。利用尿苷二磷酸葡萄糖醛酸转移酶(UGT)生物合成目标代谢物是制备葡萄糖醛酸苷的重要手段之一。综述了近年来利用生物转化技术制备O-葡萄糖醛酸苷的研究进展, 包括利用植物、微生物、动物来源及人重组UGT酶等不同方法制备O-葡萄糖醛酸苷的最新进展, 同时还综述了近年来国内外通过对生物反应体系和转化工艺的改进与优化, 实现葡萄糖醛酸苷高效制备的相关技术和工艺特点。
[Key word]
[Abstract]
Glucuronidation is one of the most important metabolic reactions in vivo, while O-glucuronidation is the major reaction type. The synthesis of O-glucuronides is very helpful for the further studies on the evaluation of biological activity and safety of O-glucuronids, as well as drug metabolism and pharmacokinetic studies. The enzymatic catalysis process using UDP-glucuronosyltransferases (UGTs) is the major method for O-glucuronides biosynthesis. This review summarized the recent progress in enzymatic preparation of O-glucuronides by using different enzyme sources including plants, microorganisms, animals, and recombinant human UGTs. Furthermore, this review also summarized several new techniques to improve the efficacy for biosynthesis of O-glucuronides.
[中图分类号]
[基金项目]
国家自然科学基金资助项目(81273590, 81302793);“973”计划(2013CB531800);辽宁省教育厅科研项目(L2013345);辽宁省科技厅自然科学基金(2013023049);辽宁省大学生创新创业计划项目(201310161046)
