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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
Source PublicationPHARMACOLOGICAL RESEARCH
ISSN1043-6618
Volume129Issue:3Pages:388-399
Abstract

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.

KeywordMdr Abcb1 Jatrophane Diterpenoid Ester Chemotherapeutic Agents
DOI10.1016/j.phrs.2017.11.001
Indexed BySCI
WOS IDWOS:000428102600036
Citation statistics
Cited Times:2[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.xjipc.cas.cn/handle/365002/5276
Collection省部共建新疆特有药用资源利用重点实验室
资源化学研究室
Corresponding AuthorAisa, HA (Aisa, Haji Akber)
Affiliation1.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
Recommended Citation
GB/T 7714
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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