ES2 enhances the efficacy of chemotherapeutic agents in ABCB1-overexpressing cancer cells in vitro and in vivo
文献类型：期刊论文
| 作者 | Fang, Yanfen1,3; Sun, Juanjuan3,4; Zhong, Xing3; Hu, Rui2; Gao, Jie2; Duan, Guanfu3; Ji, Changge3; Chen, Lijuan3; Zhang, Wanli3; Miao, Chunxiao3 |
| 刊名 | PHARMACOLOGICAL RESEARCH
 |
| 出版日期 | 2018-03 |
| 卷号 | 129页码:388-399 |
| 关键词 | MDR ABCB1 Jatrophane diterpenoid ester Chemotherapeutic agents |
| ISSN号 | 1043-6618 |
| DOI | 10.1016/j.phrs.2017.11.001 |
| 文献子类 | Article |
| 英文摘要 | ES2 is a new type of jatrophane diterpenoid ester isolated from the fructus E. sororia, a traditional Uyghur medicine in China. Here we reported the multidrug resistance (MDR) reversal effect of ES2 in vitro and in vivo by modulating the function of ATP-binding cassette subfamily B member 1 (ABCB1). ES2 exhibited low cytotoxicity to ABCB1-overexpressing MDR cells and their parental sensitive cells, but sensitized the MDR cells and ABCB1-transfected HEK293 cells to chemotherapeutic drugs that are ABCB1 substrates. The reversal ability of ES2 was primarily due to the inhibition of the efflux function of ABCB1. Moreover, ES2 stimulated the ATPase activity of ABCB1 in a concentration-dependent manner. There was no change in the expression of ABCB1 in the presence of ES2. The molecular docking analysis indicated that ES2 bond to the drug-binding site of ABCBI transporter. Importantly, ES2 significantly enhanced the anti-tumor effect of vinorelbine against KBv200 cell xenografts in nude mice. Overall, these findings demonstrate that ES2 inhibits the ABCB1 transporter function and consequently reverses ABCB1-mediated MDR, indicating the potential use of ES2 in combination therapy with conventional chemotherapeutic drugs for cancer treatment. (C) 2017 Elsevier Ltd. All rights reserved. |
| WOS关键词 | MULTIDRUG-RESISTANCE ; P-GLYCOPROTEIN ; MOLECULAR-BASIS ; TRANSPORTER ; BINDING ; ABCB1 ; INHIBITORS ; APOPTOSIS |
| 资助项目 | National Natural Science Foundation of China[21572263] ; National Natural Science Foundation of China[81373964] ; National Natural Science Foundation of China[81402953] ; Shanghai Science & Technology Innovation Action Program[15140904800] ; Shanghai Science & Technology Innovation Action program[14431902700] ; National Science & Technology Major Project of China[2014ZX09301-306-03] ; China Postdoctoral Science Foundation[2015T80416] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000428102600036 |
| 出版者 | ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279869]  |
| 专题 | 药理学第一研究室 |
| 通讯作者 | Aisa, Haji Akber; Zhang, Xiongwen |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, Shanghai, Peoples R China; 2.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, Key Lab Plant Resources & Chem Arid Zone, Urumqi, Peoples R China 3.East China Normal Univ, Sch Chem & Mol Engn, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Shanghai, Peoples R China; 4.Chinese Acad Sci, Shanghai Inst Biochem & Cell Biol, Ctr Excellence Mol & Cell Biol, State Key Lab Cell Biol, Shanghai, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Fang, Yanfen,Sun, Juanjuan,Zhong, Xing,et al. ES2 enhances the efficacy of chemotherapeutic agents in ABCB1-overexpressing cancer cells in vitro and in vivo[J]. PHARMACOLOGICAL RESEARCH,2018,129:388-399. |
| APA | Fang, Yanfen.,Sun, Juanjuan.,Zhong, Xing.,Hu, Rui.,Gao, Jie.,...&Zhang, Xiongwen.(2018).ES2 enhances the efficacy of chemotherapeutic agents in ABCB1-overexpressing cancer cells in vitro and in vivo.PHARMACOLOGICAL RESEARCH,129,388-399. |
| MLA | Fang, Yanfen,et al."ES2 enhances the efficacy of chemotherapeutic agents in ABCB1-overexpressing cancer cells in vitro and in vivo".PHARMACOLOGICAL RESEARCH 129(2018):388-399. |
入库方式： OAI收割
来源：上海药物研究所
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