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沙匹替尼逆转过表达ABCB1转运蛋白的结肠癌细胞中的抗癌药物耐药性。

Sapitinib Reverses Anticancer Drug Resistance in Colon Cancer Cells Overexpressing the ABCB1 Transporter.

作者信息

Gao Hai-Ling, Gupta Pranav, Cui Qingbin, Ashar Yunali V, Wu Zhuo-Xun, Zeng Leli, Lei Zi-Ning, Teng Qiu-Xu, Ashby Charles R, Guan Yingjun, Chen Zhe-Sheng

机构信息

Department of Histology and Embryology, Weifang Medical University, Weifang, China.

Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, NY, United States.

出版信息

Front Oncol. 2020 Oct 9;10:574861. doi: 10.3389/fonc.2020.574861. eCollection 2020.

DOI:10.3389/fonc.2020.574861
PMID:33163405
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7581728/
Abstract

The efficacy of anti-cancer drugs in patients can be attenuated by the development of multi-drug resistance (MDR) due to ATP-binding cassette (ABC) transporters overexpression. In this study, we determined the reversal efficacy of the epidermal growth factor receptor (EFGR) inhibitor, saptinib, in SW620 and SW720/Ad300 colon cancer cells and HEK293/ABCB1 cells which overexpress the ABCB1 transporter. Sapitinib significantly increased the efficacy of paclitaxel and doxorubicin in ABCB1 overexpressing cells without altering the expression or the subcellular location of the ABCB1 transporter. Sapitinib significantly increased the accumulation of [H]-paclitaxel in SW620/AD300 cells probably by stimulating ATPase activity which could competitively inhibit the uptake of [H]-paclitaxel. Furthermore, sapitinib inhibited the growth of resistant multicellular tumor spheroids (MCTS). The docking study indicated that sapitinib interacted with the efflux site of ABCB1 transporter by π-π interaction and two hydrogen bonds. In conclusion, our study suggests that sapitinib surmounts MDR mediated by ABCB1 transporter in cancer cells.

摘要

由于ATP结合盒（ABC）转运蛋白的过表达导致多药耐药（MDR）的出现，抗癌药物在患者体内的疗效可能会减弱。在本研究中，我们测定了表皮生长因子受体（EFGR）抑制剂沙铂替尼对过表达ABCB1转运蛋白的SW620和SW720/Ad300结肠癌细胞以及HEK293/ABCB1细胞的逆转疗效。沙铂替尼显著提高了过表达ABCB1的细胞中紫杉醇和阿霉素的疗效，而没有改变ABCB1转运蛋白的表达或亚细胞定位。沙铂替尼可能通过刺激ATP酶活性显著增加了[H]-紫杉醇在SW620/AD300细胞中的蓄积，这可以竞争性抑制[H]-紫杉醇的摄取。此外，沙铂替尼抑制了耐药多细胞肿瘤球体（MCTS）的生长。对接研究表明，沙铂替尼通过π-π相互作用和两个氢键与ABCB1转运蛋白的外排位点相互作用。总之，我们的研究表明沙铂替尼克服了癌细胞中由ABCB1转运蛋白介导的MDR。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/11a0/7581728/93bfaeb1f663/fonc-10-574861-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/11a0/7581728/5f87881dacd3/fonc-10-574861-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/11a0/7581728/cb677ce15c6c/fonc-10-574861-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/11a0/7581728/3adf1146d1a4/fonc-10-574861-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/11a0/7581728/130b9330be99/fonc-10-574861-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/11a0/7581728/0b1efe886c97/fonc-10-574861-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/11a0/7581728/93bfaeb1f663/fonc-10-574861-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/11a0/7581728/5f87881dacd3/fonc-10-574861-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/11a0/7581728/cb677ce15c6c/fonc-10-574861-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/11a0/7581728/3adf1146d1a4/fonc-10-574861-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/11a0/7581728/130b9330be99/fonc-10-574861-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/11a0/7581728/0b1efe886c97/fonc-10-574861-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/11a0/7581728/93bfaeb1f663/fonc-10-574861-g006.jpg

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