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Effects of breast cancer resistance protein inhibitors and pharmaceutical excipients on decreasing gastrointestinal toxicity of camptothecin analogs

文献类型：期刊论文

作者Zhang, Xin-xin1,2; Pan, Wei-san2; Gan, Li1; Zhu, Chun-liu1; Gan, Yong1
刊名ACTA PHARMACOLOGICA SINICA
出版日期2008-11
卷号29期号:11页码:1391-1398
关键词breast cancer resistance protein irinotecan CPT-11 hydroxycamptothecin biliary excretion diarrhea gastrointestinal toxicity
ISSN号1671-4083
DOI10.1111/j.1745-7254.2008.00883.x
文献子类Article
英文摘要Aim: To investigate the effect of breast cancer resistance protein (BCRP) inhibitors and pharmaceutical excipients on reducing the biliary excretion of camptothecins (CPT), ameliorating delayed-type diarrhea and intestinal mucosa damage induced by CPT. Methods: The cumulative biliary excretion of irinotecan (CPT-11) and hydroxycamptothecin (HCPT) with or without BCRP inhibitors and excipients was investigated in rats. The gastrointestinal toxicity, assessed as the diarrheal score, body weight change and microscopic pathological damage was also determined in rats. Results: Breast cancer resistance protein (BCRP) exhibited important effects on the biliary excretion of CPT. Coadministration of BCRP inhibitors such as GF120918 and cyclosporin A reduced the biliary excretion of CPT-11 and HCPT. Pharmaceutical excipients such as Pluronic F68 and PEG 2000 stearate also showed inhibitory effects on BCRP and similarly reduced CPT biliary excretion. The observed gastrointestinal toxicity was ameliorated by coadministration of BCRP inhibitors and excipients compared with injection of CPT-11 and HCPT alone. Conclusion: The use of excipients as inhibitors of BCRP is safe and relatively non-toxic, and may lead to important pharmacotherapeutic benefits by decreasing the gastrointestinal toxicity of CPT.
WOS关键词CELL LUNG-CANCER ; MULTIDRUG-RESISTANCE ; BILIARY-EXCRETION ; HALF-TRANSPORTER ; TOPOISOMERASE-I ; PHASE-II ; IRINOTECAN ; TOPOTECAN ; CPT-11 ; PHARMACOKINETICS
资助项目Knowledge Innovation Program of the Chinese Academy of Sciences[SIMM0709QN-10]
WOS研究方向Chemistry ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000260527300015
出版者SHANGHAI INST MATERIA MEDICA
源URL[http://119.78.100.183/handle/2S10ELR8/279439]  
专题药物制剂研究中心
通讯作者Gan, Yong
作者单位1.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
2.Shenyang Pharmaceut Univ, Sch Pharm, Shenyang 110016, Peoples R China
推荐引用方式
GB/T 7714		 Zhang, Xin-xin,Pan, Wei-san,Gan, Li,et al. Effects of breast cancer resistance protein inhibitors and pharmaceutical excipients on decreasing gastrointestinal toxicity of camptothecin analogs[J]. ACTA PHARMACOLOGICA SINICA,2008,29(11):1391-1398.
APA Zhang, Xin-xin,Pan, Wei-san,Gan, Li,Zhu, Chun-liu,&Gan, Yong.(2008).Effects of breast cancer resistance protein inhibitors and pharmaceutical excipients on decreasing gastrointestinal toxicity of camptothecin analogs.ACTA PHARMACOLOGICA SINICA,29(11),1391-1398.
MLA Zhang, Xin-xin,et al."Effects of breast cancer resistance protein inhibitors and pharmaceutical excipients on decreasing gastrointestinal toxicity of camptothecin analogs".ACTA PHARMACOLOGICA SINICA 29.11(2008):1391-1398.

入库方式： OAI收割

来源：上海药物研究所

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