ES2 enhances the efficacy of chemotherapeutic agents in ABCB1-overexpressing cancer cells in vitro and in vivo
Fang, YF (Fang, Yanfen); Sun, JJ (Sun, Juanjuan); Zhong, X (Zhong, Xing); Hu, R (Hu, Rui); Gao, J (Gao, Jie); Duan, GF (Duan, Guanfu); Ji, CG (Ji, Changge); Chen, LJ (Chen, Lijuan); Zhang, WL (Zhang, Wanli); Miao, CX (Miao, Chunxiao); Aisa, HA (Aisa, Haji Akber); Zhang, XW (Zhang, Xiongwen)
2018
发表期刊PHARMACOLOGICAL RESEARCH
卷号129期号:3页码:388-399
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.

关键词Mdr Abcb1 Jatrophane Diterpenoid Ester Chemotherapeutic Agents
DOI10.1016/j.phrs.2017.11.001
收录类别SCI
WOS记录号WOS:000428102600036
引用统计
文献类型期刊论文
条目标识符http://ir.xjipc.cas.cn/handle/365002/5276
专题省部共建新疆特有药用资源利用重点实验室
作者单位1.East China Normal Univ, Sch Chem & Mol Engn, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Shanghai, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, Shanghai, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Biochem & Cell Biol, Ctr Excellence Mol & Cell Biol, State Key Lab Cell Biol, Shanghai, Peoples R China
4.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, Key Lab Plant Resources & Chem Arid Zone, Urumqi, Peoples R China
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Fang, YF ,Sun, JJ ,Zhong, X ,et al. ES2 enhances the efficacy of chemotherapeutic agents in ABCB1-overexpressing cancer cells in vitro and in vivo[J]. PHARMACOLOGICAL RESEARCH,2018,129(3):388-399.
APA Fang, YF .,Sun, JJ .,Zhong, X .,Hu, R .,Gao, J .,...&Zhang, XW .(2018).ES2 enhances the efficacy of chemotherapeutic agents in ABCB1-overexpressing cancer cells in vitro and in vivo.PHARMACOLOGICAL RESEARCH,129(3),388-399.
MLA Fang, YF ,et al."ES2 enhances the efficacy of chemotherapeutic agents in ABCB1-overexpressing cancer cells in vitro and in vivo".PHARMACOLOGICAL RESEARCH 129.3(2018):388-399.
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