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学科主题物理化学
Metabolism of cephalomannine in human liver microsomes
Zhang JW(张江伟); Ge GB(葛广波); Liu Y(刘勇); Zhang YY(张延延); Liu XB(刘兴宝); Cheng J(程婕); Li W(李巍); Yang L(杨凌)
会议名称第三届中日双边药理学和临床药理学会议
会议日期2007-8-23
2007-08-23
会议地点中国
页码357/2
部门归属十八室
主办者中国药理学会
英文摘要To identify the metabolites of cephalomannine and cytochrome P450 (CYP) isoforms involved. METHODS LC/MS/MS was recruited to identify the possible structures of metabolites. Incubations were conducted with CYP isoform specific inhibitors and recombinant human CYP isoforms to ascribe individual reaction to a single CYP isoform. RESULTS After incubated with human liver microsomes (HLMs) and NADPH-generating system, two mono-hydroxylated metabolites of cephalomannine were eluted at 6.5 and 10.9 min respectively. C4'''' (6.5 min) and C6α (10.9 min) were identified as the possible hydroxylation sites by LC/MS/MS. Chemical inhibition studies and assays with recombinant CYPs suggested that 4''''-hydroxycephalomannine was produced exclusively by CYP3A4 and 6α-hydroxycephalomannine by CYP2C8. Different from the metabolism of paclitaxel, 4''''-hydroxycephalomannine by CYP3A4 became the dominant metabolite, and the mean ratio of 4''''-hydroxycephalomannine to 6α-hydroxycephalomannine was 64:36 in three liver microsomes. CONCLUSION Cephalomannine differs from paclitaxel with regard to major hydroxylation site and main metabolism enzyme. Our results confirm that substituents in C3'' greatly impact taxane metabolism. Key words: cephalomannine (taxol B); cytochrome P450 (CYP); taxane; paclitaxel
语种中文
文献类型会议论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/112718
专题中国科学院大连化学物理研究所
通讯作者Yang L(杨凌)
推荐引用方式
GB/T 7714
Zhang JW,Ge GB,Liu Y,et al. Metabolism of cephalomannine in human liver microsomes[C],2007:357/2.
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