effectsofbreastcancerresistanceproteininhibitorsandpharmaceuticalexcipientsondecreasinggastrointestinaltoxicityofcamptothecinanalogs
文献类型：期刊论文
| 作者 | Xinxin ZHANG1 ; Weisan PAN2; Li GAN1; Chunliu ZHU1; Yong GAN1
|
| 刊名 | actapharmacologicasinica
 |
| 出版日期 | 2008 |
| 卷号 | 29期号:11页码:1391 |
| 关键词 | CELL LUNG-CANCER MULTIDRUG-RESISTANCE BILIARY-EXCRETION HALF-TRANSPORTER TOPOISOMERASE-I PHASE-II IRINOTECAN TOPOTECAN CPT-11 PHARMACOKINETICS breast cancer resistance protein irinotecan CPT-11 hydroxycamptothecin biliary excretion diarrhea gastrointestinal toxicity |
| ISSN号 | 1671-4083 |
| DOI | 10.1111/j.1745-7254.2008.00883.x |
| 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. |
| 资助项目 | [Knowledge Innovation Program of the Chinese Academy of Sciences] |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/287418]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.中国科学院上海药物研究所 2.沈阳药科大学 |
| 推荐引用方式 GB/T 7714 | Xinxin ZHANG,Weisan PAN,Li GAN,et al. effectsofbreastcancerresistanceproteininhibitorsandpharmaceuticalexcipientsondecreasinggastrointestinaltoxicityofcamptothecinanalogs[J]. actapharmacologicasinica,2008,29(11):1391. |
| APA | Xinxin ZHANG,Weisan PAN,Li GAN,Chunliu ZHU,&Yong GAN.(2008).effectsofbreastcancerresistanceproteininhibitorsandpharmaceuticalexcipientsondecreasinggastrointestinaltoxicityofcamptothecinanalogs.actapharmacologicasinica,29(11),1391. |
| MLA | Xinxin ZHANG,et al."effectsofbreastcancerresistanceproteininhibitorsandpharmaceuticalexcipientsondecreasinggastrointestinaltoxicityofcamptothecinanalogs".actapharmacologicasinica 29.11(2008):1391. |
入库方式： OAI收割
来源：上海药物研究所
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