Pharmacokinetics, Mass Balance, Tissue Distribution, and Metabolism of [3H]Catalpol in Rats: the Main Bioactive Component of Rehmannia glutinosa for the Treatment of Ischemic Stroke
文献类型：期刊论文
| 作者 | Ge, Xinyu3,4; Zheng, Yuandong3; He, Yifei3; Chen, Chong3,4; Yang, Chen3; Lu, Saiwei1; Xuan, Zhenyu1,2; Zhong, Dafang3 ; Diao, Xingxing3,4
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| 刊名 | CURRENT DRUG METABOLISM
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| 出版日期 | 2023-07-17 |
| 页码 | 10 |
| 关键词 | [H-3]catalpol Rehmannia glutinosa mass balance tissue distribution metabolism intestinal flora ischemic stroke. |
| ISSN号 | 1389-2002 |
| DOI | 10.2174/1389200224666230705142901 |
| 通讯作者 | Xuan, Zhenyu(xuanzhenyu@163.com) ; Zhong, Dafang(dfzhong@simm.ac.cn) ; Diao, Xingxing(xxdiao@simm.ac.cn) |
| 英文摘要 | \Background: Catalpol, one of the main bioactive components isolated from Rehmannia glutinosa, was developed by Suzhou Youseen for the treatment of ischemic stroke; however, preclinical information about its absorption, distribution, metabolism, and excretion (ADME) in animals is inadequate. Objective: This study aimed to illuminate the pharmacokinetics (PK), mass balance (MB), tissue distribution (TD), and metabolism of catalpol after a single intragastric administration of 30 mg/kg (300 mu Ci/kg) [H-3]catalpol in rats. Methods: Radioactivity in plasma, urine, feces, bile, and tissues was measured by liquid scintillation counting ( LSC), and metabolite profiling was characterized by UHPLC-beta-ram and UHPLC-Q-Exactive plus MS. Results: The radio pharmacokinetic results showed that catalpol was rapidly absorbed by Sprague-Dawley (SD) rats, with a median T-max of 0.75 h and an arithmetic mean half-life (t(1/2)) of the total radioactivity of approximately 1.52 h in plasma. The mean recovery of the total radioactive dose was 94.82%+/- 1.96% over 168 h postdose ( 57.52%+/- 12.50% in the urine and 37.30%+/- 12.88% in the feces). The parent drug catalpol was the predominant drug-related substance in rat plasma and urine, while M1 and M2, two unidentified metabolites, were detected in feces. When [3H]catalpol was incubated with beta-glucosidase and rat intestinal flora, we found that the same metabolites M1 and M2 were produced in both incubation systems. Conclusions: Catalpol was excreted mainly through the urine. The drug-related substances were primarily concentrated in the stomach, large intestine, bladder, and kidney. Only the parent drug was detected in the plasma and urine, and M1 and M2 were detected in the feces. We speculate that the metabolism of catalpol in rats was mainly mediated by the intestinal flora, resulting in an aglycone-containing hemiacetal hydroxyl structure. |
| WOS关键词 | CATALPOL ; PLASMA ; AUCUBIN ; FECES |
| 资助项目 | Declared none. |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001069609400001 |
| 出版者 | BENTHAM SCIENCE PUBL LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/307300]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Xuan, Zhenyu; Zhong, Dafang; Diao, Xingxing |
| 作者单位 | 1.SuZhou Youseen New Drug R&D Co Ltd, Suzhou 215123, Peoples R China 2.Soochow Univ, Coll Pharmaceut Sci, Suzhou 215127, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 4.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ge, Xinyu,Zheng, Yuandong,He, Yifei,et al. Pharmacokinetics, Mass Balance, Tissue Distribution, and Metabolism of [3H]Catalpol in Rats: the Main Bioactive Component of Rehmannia glutinosa for the Treatment of Ischemic Stroke[J]. CURRENT DRUG METABOLISM,2023:10. |
| APA | Ge, Xinyu.,Zheng, Yuandong.,He, Yifei.,Chen, Chong.,Yang, Chen.,...&Diao, Xingxing.(2023).Pharmacokinetics, Mass Balance, Tissue Distribution, and Metabolism of [3H]Catalpol in Rats: the Main Bioactive Component of Rehmannia glutinosa for the Treatment of Ischemic Stroke.CURRENT DRUG METABOLISM,10. |
| MLA | Ge, Xinyu,et al."Pharmacokinetics, Mass Balance, Tissue Distribution, and Metabolism of [3H]Catalpol in Rats: the Main Bioactive Component of Rehmannia glutinosa for the Treatment of Ischemic Stroke".CURRENT DRUG METABOLISM (2023):10. |
入库方式： OAI收割
来源：上海药物研究所
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