Identification of cytochrome P450 1A2 as enzyme involved in the microsomal metabolism of Huperzine A
文献类型：期刊论文
| 作者 | Ma, XC; Wang, HX; Xin, H; Zhang, T; Tu, ZH |
| 刊名 | EUROPEAN JOURNAL OF PHARMACOLOGY
 |
| 出版日期 | 2003-02-14 |
| 卷号 | 461期号:2-3页码:89-92 |
| 关键词 | Huperzine A metabolism cytochrome p450 microsome |
| ISSN号 | 0014-2999 |
| DOI | 10.1061/S0014-2999(03)01290-1 |
| 文献子类 | Article |
| 英文摘要 | Huperzine A is a reversible and selective cholinesterase inhibitor approved for the treatment of Alzheimer's disease. To identify which cytochrome P450 (CYP) isoenzymes are involved in the metabolism of Huperzine A, an in vitro study was performed with rat liver microsomes and immunoinhibition and chemical inhibition methods. Huperzine A metabolism was analyzed with high-performance liquid chromatography (HPLC) and expressed as Huperzine A disappearance rate. Result showed that 76.2% of Huperzine A metabolism was inhibited by CYP1A2 antibody and 17.8% by CYP3A1/2 antibody. Inhibitory effects produced by CYP2Cl1 and 2E1 antibodies were minor. The CYP1A2 substrate phenacetin showed an inhibitory effect of 70.3%. In conclusion, Huperzine A metabolism in rat liver microsomes is mediated primarily by CYP1A2, with a probable secondary contribution of CYP3A1/2. CYP2Cl1 and 2E1 are likely not involved in Huperzine A metabolism. (C) 2003 Elsevier Science B.V. All rights reserved. |
| WOS关键词 | MONOCLONAL-ANTIBODIES ; DRUG-METABOLISM ; OXIDATION ; CHEMICALS |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000181067700002 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274264]  |
| 专题 | 新药研究国家重点实验室 中科院受体结构与功能重点实验室 |
| 通讯作者 | Tu, ZH |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Medica, State Key Lab Drug Res, Shanghai 200031, Peoples R China 2.Fudan Univ, Sch Pharm, Dept Pharmacol, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ma, XC,Wang, HX,Xin, H,et al. Identification of cytochrome P450 1A2 as enzyme involved in the microsomal metabolism of Huperzine A[J]. EUROPEAN JOURNAL OF PHARMACOLOGY,2003,461(2-3):89-92. |
| APA | Ma, XC,Wang, HX,Xin, H,Zhang, T,&Tu, ZH.(2003).Identification of cytochrome P450 1A2 as enzyme involved in the microsomal metabolism of Huperzine A.EUROPEAN JOURNAL OF PHARMACOLOGY,461(2-3),89-92. |
| MLA | Ma, XC,et al."Identification of cytochrome P450 1A2 as enzyme involved in the microsomal metabolism of Huperzine A".EUROPEAN JOURNAL OF PHARMACOLOGY 461.2-3(2003):89-92. |
入库方式： OAI收割
来源：上海药物研究所
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