Metabolite identification of a new antitumor agent icotinib in rats using liquid chromatography/tandem mass spectrometry
文献类型：期刊论文
| 作者 | Guan, Zhongmin1,3; Chen, Xiaoyan1 ; Wang, Yinxiang2; Zhong, Dafang1,3
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| 刊名 | RAPID COMMUNICATIONS IN MASS SPECTROMETRY
 |
| 出版日期 | 2008-07 |
| 卷号 | 22期号:14页码:2176-2184 |
| ISSN号 | 0951-4198 |
| DOI | 10.1002/rcm.3599 |
| 文献子类 | Article |
| 英文摘要 | Icotinib, 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-4-quinazoline, is a new antitumor agent. The metabolic pathway of icotinib in rats was studied using liquid chromatography/tandem mass spectrometry (LC/MSn) analysis. Full scan and selected ion monitoring modes were used to profile the possible metabolites of icotinib in rat urine, feces and bile samples. Four phase I metabolites (M1-M4) and two phase II metabolites (M5, M6) were detected and characterized. Multiple-stage mass spectrometry and nuclear magnetic resonance (NMR) spectrometry were employed to elucidate structures of metabolites. Icotinib was metabolized to open the crown ether ring to form the main phase I metabolites. During metabolism, a reactive metabolite was formed. Using semicarbazide as a trapping agent, an intermediate arising from opening of the crown ether ring was detected as an aldehyde product by LC/MS/MS. These data indicated that ring opening of the crown ether was triggered by hydroxylation at the 8 ''-position of the ring to form a hemiacetal intermediate, which was further oxidized or reduced. Finally, the metabolic pathway of icotinib in rats was proposed. Copyright (C) 2008 John Wiley & Sons, Ltd. |
| WOS关键词 | GROWTH-FACTOR RECEPTOR ; CANCER ; GEFITINIB |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry ; Spectroscopy |
| 语种 | 英语 |
| WOS记录号 | WOS:000257863500004 |
| 出版者 | JOHN WILEY & SONS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272884]  |
| 专题 | 上海药物代谢研究中心 |
| 通讯作者 | Zhong, Dafang |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.Zhejiang Bata Pharma Inc, Hangzhou 310004, Zhejiang, Peoples R China 3.Shenyang Pharmaceut Univ, Lab Drug Metab & Pharmacokinet, Shenyang 110016, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Guan, Zhongmin,Chen, Xiaoyan,Wang, Yinxiang,et al. Metabolite identification of a new antitumor agent icotinib in rats using liquid chromatography/tandem mass spectrometry[J]. RAPID COMMUNICATIONS IN MASS SPECTROMETRY,2008,22(14):2176-2184. |
| APA | Guan, Zhongmin,Chen, Xiaoyan,Wang, Yinxiang,&Zhong, Dafang.(2008).Metabolite identification of a new antitumor agent icotinib in rats using liquid chromatography/tandem mass spectrometry.RAPID COMMUNICATIONS IN MASS SPECTROMETRY,22(14),2176-2184. |
| MLA | Guan, Zhongmin,et al."Metabolite identification of a new antitumor agent icotinib in rats using liquid chromatography/tandem mass spectrometry".RAPID COMMUNICATIONS IN MASS SPECTROMETRY 22.14(2008):2176-2184. |
入库方式： OAI收割
来源：上海药物研究所
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