Excretion of [H-3] triptolide and its metabolites in rats after oral administration
文献类型：期刊论文
| 作者 | Liu, Jia ; Zhou, Xin; Chen, Xiao-yan; Zhong, Da-fang
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2014-04 |
| 卷号 | 35期号:4页码:549-554 |
| 关键词 | triptolide immunosuppressant pharmacokinetics excretion pathway gender difference |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2013.192 |
| 文献子类 | Article |
| 英文摘要 | Aim: To investigate the routes of elimination and excretion for triptolide recovered in rats. Methods: After a single oral administration of [H-3] triptolide (0.8 mg/kg, 100 mu Ci/kg) in Sprague Dawley rats, urine and fecal samples were collected for 168 h. To study biliary excretion, bile samples were collected for 24 h through bile duct cannulation. Radioactivity was measured using a liquid scintillation analyzer, and excretion pathway analysis was performed using an HPLC/on-line radioactivity detector. Results: The total radioactivity recovered from the urine and feces of rats without bile duct ligation ranged from 86.6%-89.1%. Most of the radioactivity (68.6%-72.0%) was recovered in the feces within 72 h after oral administration, while the radioactivity recovered in the urine and bile was 17.1%-18.0% and 39.0%-39.4%, respectively. The HPLC/on-line radiochromatographic analysis revealed that most of the drug-related radioactivity was in the form of metabolites. In addition, significant gender differences in the quantity of these metabolites were found: monohydroxytriptolide sulfates were the major metabolites detected in the urine, feces, and bile of female rats, while only traces of these metabolites were found in male rats. Conclusion: Radiolabeled triptolide is mainly secreted in bile and eliminated in feces. The absorbed radioactivity is primarily eliminated in the form of metabolites, and significant gender differences are observed in the quantity of recovered metabolites, which are likely caused by the gender-specific expression of sulfotransferases. |
| WOS关键词 | WILFORDII HOOK F ; SEX-DIFFERENCES ; SULFATION ; TOXICITY ; CELLS |
| 资助项目 | National Natural Science Foundation of China[30901831] ; National Natural Science Foundation of China[81373479] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:5106727 |
| WOS记录号 | WOS:000334417500013 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277139]  |
| 专题 | 上海药物代谢研究中心 |
| 通讯作者 | Zhong, Da-fang |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Materia Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Jia,Zhou, Xin,Chen, Xiao-yan,et al. Excretion of [H-3] triptolide and its metabolites in rats after oral administration[J]. ACTA PHARMACOLOGICA SINICA,2014,35(4):549-554. |
| APA | Liu, Jia,Zhou, Xin,Chen, Xiao-yan,&Zhong, Da-fang.(2014).Excretion of [H-3] triptolide and its metabolites in rats after oral administration.ACTA PHARMACOLOGICA SINICA,35(4),549-554. |
| MLA | Liu, Jia,et al."Excretion of [H-3] triptolide and its metabolites in rats after oral administration".ACTA PHARMACOLOGICA SINICA 35.4(2014):549-554. |
入库方式： OAI收割
来源：上海药物研究所
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