壳聚糖包封的兔肝微粒体UDP-葡萄糖醛酸基转移酶的底物特异性及用于解毒的研究

Substrate specificity and the use of chitosan-entrapped rabbit hepatic microsomal UDP-glucuronyl transferase for detoxification.

作者信息

Zihnioğlu F, Telefoncu A

机构信息

Ege University, Faculty of Science, Biochemistry Department, Bornova-Izmir, Türkiye.

出版信息

Artif Cells Blood Substit Immobil Biotechnol. 1995;23(4):533-43. doi: 10.3109/10731199509117968.

DOI:10.3109/10731199509117968

PMID:7581838

Abstract

Rabbit hepatic microsomal UDP-Glucuronyl transferase (EC.2.4.1.17) was immobilized in chitosan, which is an ionotropic gelatation agent, and the resulting preparation was used as a biocatalyst for the glucuronidation of toxic substances and drugs such as; 1-naphthol, phenol, 4-nitrophenol, bilirubin, testesterone, estrone, lamotrigine, imipramine and chlorpromazine. For studying the drug metabolism in vitro and obtaining artificial liver support (detoxification) chitosan-entrapped UDPGT towards 1-naphthol was tested by using two model reactor system. The conversion curves of 1-naphthol to its glucuronide indicated that the column reactor system was found to be better and seems suitable for detoxification with a high yield of glucuronide formation.

摘要

兔肝微粒体UDP-葡萄糖醛酸基转移酶（EC.2.4.1.17）固定于壳聚糖中，壳聚糖是一种离子型胶凝剂，所得制剂用作生物催化剂，用于1-萘酚、苯酚、4-硝基苯酚、胆红素、睾酮、雌酮、拉莫三嗪、丙咪嗪和氯丙嗪等有毒物质和药物的葡萄糖醛酸化。为了体外研究药物代谢并获得人工肝支持（解毒），采用两种模型反应器系统测试了壳聚糖包埋的UDPGT对1-萘酚的作用。1-萘酚向其葡萄糖醛酸化物的转化曲线表明，柱式反应器系统效果更好，似乎适合以高产率形成葡萄糖醛酸化物进行解毒。