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Open AccessArticle

Ciprofloxacin Enhances the Chemosensitivity of Cancer Cells to ABCB1 Substrates

Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John’s University, Queens, NY 11439, USA
Department of Histology and Embryology, Weifang Medical University, Weifang 261053, China
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Int. J. Mol. Sci. 2019, 20(2), 268;
Received: 20 December 2018 / Revised: 4 January 2019 / Accepted: 7 January 2019 / Published: 11 January 2019
(This article belongs to the Special Issue Drug Resistance: Mechanisms and New Strategies)
ABCB1 is one of the major drug efflux transporters that is known to cause multidrug resistance (MDR) in cancer patients receiving chemotherapy for the treatment of solid tumors and hematological malignancies. Inhibition of ABCB1 efflux function is important for maintaining the intracellular concentration of chemotherapeutic drugs. Here, we evaluated ciprofloxacin for its ability to reverse MDR caused by the overexpression of ABCB1. Cytotoxicity of ciprofloxacin was determined by the MTT assay. The chemosensitizing effects of ciprofloxacin were determined in combination with ABCB1 substrates. The intracellular accumulation and efflux of ABCB1 substrates was measured by a scintillation counter, and protein expression was determined by the Western blotting. Vanadate-sensitive ATPase assay was performed to determine the effect of ciprofloxacin on the ATPase activity of ABCB1, and docking analysis was done to determine the interaction of ciprofloxacin with ABCB1. Ciprofloxacin significantly potentiated the cytotoxic effects of ABCB1 substrates in ABCB1-overexpressing cells. Furthermore, ciprofloxacin increased the intracellular accumulation and decreased the efflux of [3H]-paclitaxel without altering the expression of ABCB1. Ciprofloxacin stimulated the ATPase activity of ABCB1 in a concentration-dependent manner. Our findings showed that ciprofloxacin potently inhibits the ABCB1 efflux function and it has potential to be developed as a combination anticancer therapy. View Full-Text
Keywords: ciprofloxacin; ABCB1 transporter; paclitaxel; multidrug-resistance ciprofloxacin; ABCB1 transporter; paclitaxel; multidrug-resistance
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Gupta, P.; Gao, H.-L.; Ashar, Y.V.; Karadkhelkar, N.M.; Yoganathan, S.; Chen, Z.-S. Ciprofloxacin Enhances the Chemosensitivity of Cancer Cells to ABCB1 Substrates. Int. J. Mol. Sci. 2019, 20, 268.

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