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Absorption, Distribution, Metabolism, and Excretion of [14C]BS1801, a Selenium-Containing Drug Candidate, in Rats

文献类型：期刊论文

作者Yang, Cheng3,4; Xue, Mingzhen2; He, Yifei3; Yin, Hanwei1; Yang, Chen3; Zhong, Dafang3; Zeng, Huihui1; Zheng, Yuandong3; Diao, Xingxing3,4
刊名MOLECULES
出版日期2023-12-01
卷号28期号:24页码:16
关键词[C-14]BS1801 BS1801 (butaselen) tissue distribution metabolism mass balance selenium
DOI10.3390/molecules28248102
通讯作者Zeng, Huihui(zenghh@bjmu.edu.cn) ; Zheng, Yuandong(ydzheng@simm.ac.cn) ; Diao, Xingxing(xxdiao@simm.ac.cn)
英文摘要BS1801 is a selenium-containing drug candidate with potential for treating liver and lung fibrosis. To fully elucidate the biotransformation of BS1801 in animals and provide sufficient preclinical drug metabolism data for human mass balance study, the metabolism of BS1801 in rats was investigated. We used radiolabeling techniques to investigate the mass balance, tissue distribution, and metabolite identification of BS1801 in Sprague-Dawley/Long-Evans rats after a single oral dose of 100 mg/kg (100 mu Ci/kg) [C-14]BS1801: 1. The mean recovery of radioactive substances in urine and feces was 93.39% within 168 h postdose, and feces were the main excretion route. 2. Additionally, less than 1.00% of the dose was recovered from either urine or bile. 3. BS1801-related components were widely distributed throughout the body. 4. Fifteen metabolites were identified in rat plasma, urine, feces, and bile, and BS1801 was detected only in feces. 5. BS1801-M484, the methylation product obtained via a N-Se bond reduction in BS1801, was the most abundant drug-related component in plasma. The main metabolic pathways of BS1801 were reduction, amide hydrolysis, oxidation, and methylation. Overall, BS1801 was distributed throughout the body, and excreted mainly as an intact BS1801 form through feces. No differences were observed between male and female rats in distribution, metabolism, and excretion of BS1801.
WOS关键词THIOREDOXIN REDUCTASE INHIBITOR ; PLASMA ; APOPTOSIS ; COMPOUND ; BINDING ; EBSELEN ; BBSKE
资助项目Shanghai Yuanxi Medicine Corp
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
语种英语
出版者MDPI
WOS记录号WOS:001132648300001
源URL[http://119.78.100.183/handle/2S10ELR8/308383]  
专题中国科学院上海药物研究所
通讯作者Zeng, Huihui; Zheng, Yuandong; Diao, Xingxing
作者单位1.Shanghai Yuanxi Pharmaceut Technol Co Ltd, Shanghai 201203, Peoples R China
2.Nanjing Univ Chinese Med, Jiangsu Key Lab Funct Subst Chinese Med, Nanjing 210023, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201210, 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		 Yang, Cheng,Xue, Mingzhen,He, Yifei,et al. Absorption, Distribution, Metabolism, and Excretion of [14C]BS1801, a Selenium-Containing Drug Candidate, in Rats[J]. MOLECULES,2023,28(24):16.
APA Yang, Cheng.,Xue, Mingzhen.,He, Yifei.,Yin, Hanwei.,Yang, Chen.,...&Diao, Xingxing.(2023).Absorption, Distribution, Metabolism, and Excretion of [14C]BS1801, a Selenium-Containing Drug Candidate, in Rats.MOLECULES,28(24),16.
MLA Yang, Cheng,et al."Absorption, Distribution, Metabolism, and Excretion of [14C]BS1801, a Selenium-Containing Drug Candidate, in Rats".MOLECULES 28.24(2023):16.

入库方式： OAI收割

来源：上海药物研究所

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