紫杉醇及其人血浆中代谢物的电喷雾串联质谱研究  

Study on paclitaxel and its metabolites in human plasma by electrospray ionization tandem mass spectrometry

作　　者：钱隽[1,2] 王漪璇[2] 郁韵秋[1] 

机构地区：[1]复旦大学药学院药物分析学教研室,上海201203 [2]复旦大学附属肿瘤医院化疗科,上海200032

出　　处：《药学服务与研究》2012年第6期418-422,共5页Pharmaceutical Care and Research

摘　　要：目的:采用电喷雾串联质谱(ESI-MSn)法研究紫杉醇的离子化方式、结构裂解方式及在人血浆中的主要代谢物。方法:紫杉醇对照品溶液经质谱进样,探索其一级质谱的电离规律和二级质谱的裂解规律。通过液相色谱-质谱联用技术分离和鉴定紫杉醇在人体中的代谢物。结果:溶液中的添加剂对紫杉醇的离子化效率有明显促进作用,在ESI正离子模式下紫杉醇以m/z854的[M+H]+丰度最高。紫杉醇裂解过程以脱水和酯键断裂为主,产生多个碎片离子,其中m/z286信号最强并具有较好的稳定性。紫杉醇在人血浆中的代谢物有3个,以6α-羟基紫杉醇为主。结论:紫杉醇及其人血浆中代谢物的质谱行为研究,可为紫杉醇的质谱定性和定量分析以及药物代谢研究提供重要参考。Objective： To investigate the ionization effect,structural fragmentation pathways of paclitaxel and its major metabolites in human plasma by electrospray ionization tandem mass spectrometry（ESI-MSn）.Methods：The reference solution of paclitaxel was infused into mass spectrometer for studying its ionization and fragmentation in MS and MS2 mode.Paclitaxel metabolites in human body were separated and identified by LC-MS/MS method.Results： The ionization efficiency of paclitaxel was greatly enhanced by the additives in the solution.The protonated ion（~） at m/z 854 was the most abundant under positive ESI condition.Dehydration and ester bond cleavage were the main fragmentation procedures of paclitaxel.Various fragment ions were formed,and the fragment ion at m/z 286 was the most prominent and stable.Three metabolites of paclitaxel were found in human plasma and 6α-hydroxy paclitaxel was the main metabolite.Conclusion： The study on mass spectrometric behavior of paclitaxel and its primary metabolites in human plasma provided an important evidence for qualitative and quantitative analysis of paclitaxel by mass spectrometry and research on its metabolism.

关 键 词：紫杉醇 代谢物 质谱法 离子碎片 

分 类 号：R979.1[医药卫生—药品] TQ460.7[医药卫生—药学]