Metabolic assessment in liver microsomes by co-activating cytochrome P450s and UDP-glycosyltransferases
Metabolic assessment in liver microsomes by co-activating cytochrome P450s and UDP-glycosyltransferases
复制标题
DOI：
10.1007/bf03190489
复制
发表时间：
2003-07-01
影响因子：
1.9
通讯作者：
Caldwell, GW
中科院分区：
文献类型：
--
作者：
Yan, Z;Caldwell, GW
对CYP和UGT均具有活性的“双活性”微粒体系统进行了评价，以用于代谢稳定性和体外代谢物谱研究。在该“双活性”系统中，使用成孔肽丙甲霉素来激活人肝微粒体中的UGT，而不影响UGT活性。干扰研究表明，通过对乙酰氨基酚和三氟拉嗪的葡萄糖醛酸化测定，抗凝血剂对UGT替代活性几乎没有影响。2019 - 04 - 22 00：00：00 00：00
A "dual-activity" microsomal system in which both CYPs and UGTs were active was evaluated for studies of metabolic stability and in-vitro metabolite profiling. in this "dual-activity" system, alamethicin, a pore-forming peptide, was used to activate UGTs in human liver microsomes without affecting CYP activity. Interference studies indicated that CYP colactors had little effect on UGT surrogate activity as measured by glucuronidation of acetaminophen and trifluoperazine. Further, UGT cofactor, UDPGA (