Biotransformation of indomethacin by the fungus Cunninghamella blakesleeana
文献类型：期刊论文
| 作者 | Zhang, Peng; Lin, Li-hong; Huang, Hai-hua; Xu, Hai-yan; Zhong, Da-fang
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| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2006-08 |
| 卷号 | 27期号:8页码:1097-1102 |
| 关键词 | indomethacin microbial transformation Cunninghamella blakesleeana liquid chromatography mass spectrometry |
| ISSN号 | 1671-4083 |
| DOI | 10.1111/j.1745-7254.2006.00350.x |
| 文献子类 | Article |
| 英文摘要 | Aim: To investigate the biotransformation of indomethacin, the first of the newer nonsteroidal anti-inflammatory drugs, by filamentous fungus and to compare the similarities between microbial transformation and mammalian metabolism of indomethacin. Methods: Five strains of Cunninghamella (C elegans AS 3.156, C elegans AS 3.2028, C blakesleeana AS 3.153, C blakesleeana AS 3.910 and C echinulata AS 3.2004) were screened for their ability to catalyze the biotransformation of indomethacin. Indomethacin was partially metabolized by five strains of Cunninghamella, and C blakesleeana AS 3.910 was selected for further investigation. Three metabolites produced by C blakesleeana AS 3.910 were isolated using semi-preparative HPLC, and their structures were identified by a combination analysis of LC/MSn and NMR spectra. These three metabolites were separated and quantitatively assayed by liquid chromatography-ion trap mass spectrometry. Results: After 120 h of incubation with C blakesleeana AS 3.910, approximately 87.4% of indomethacin was metabolized to three metabolites: O-desmethylindomethacin (DMI, M1, 67.2%), N-deschlorobenzoylindomethacin (DBI, M2, 13.3%) and O-desmethyl-N-deschlorobenzoylindomethacin (DMBI, M3, 6.9%). Three phase I metabolites of indomethacin produced by C blakesleeana AS 3.910 were identical to those obtained in humans. Conclusion: C blakesleeana could be a useful tool for generating the mammalian phase I metabolites of indomethacin. |
| WOS关键词 | METABOLISM ; PHARMACOKINETICS ; TRANSFORMATION ; DRUG |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:2462251 |
| WOS记录号 | WOS:000239306600021 |
| 出版者 | BLACKWELL PUBLISHING |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273521]  |
| 专题 | 上海药物代谢研究中心 |
| 通讯作者 | Zhong, Da-fang |
| 作者单位 | 1.Shenyang Pharmaceut Univ, Dept Microbiol, Shenyang 110016, Peoples R China 2.Shenyang Pharmaceut Univ, Lab Drug Metab & Pharmacokinet, Shenyang 110016, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Peng,Lin, Li-hong,Huang, Hai-hua,et al. Biotransformation of indomethacin by the fungus Cunninghamella blakesleeana[J]. ACTA PHARMACOLOGICA SINICA,2006,27(8):1097-1102. |
| APA | Zhang, Peng,Lin, Li-hong,Huang, Hai-hua,Xu, Hai-yan,&Zhong, Da-fang.(2006).Biotransformation of indomethacin by the fungus Cunninghamella blakesleeana.ACTA PHARMACOLOGICA SINICA,27(8),1097-1102. |
| MLA | Zhang, Peng,et al."Biotransformation of indomethacin by the fungus Cunninghamella blakesleeana".ACTA PHARMACOLOGICA SINICA 27.8(2006):1097-1102. |
入库方式： OAI收割
来源：上海药物研究所
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