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Title: Development of a novel quinoline derivative as a P-glycoprotein inhibitor to reverse multidrug resistance in cancer cells
Authors: Zhou, Y
Chung, PY
Ma, JYW 
Lam, AKY
Law, S
Chan, KW
Chan, ASC
Li, X
Lam, KH
Chui, CH
Tang, JCO
Issue Date: 2019
Source: Biology, 2019, v. 8, no. 4, 75
Abstract: Multidrug resistance (MDR) is one of conventional cancer chemotherapy’s limitations. Our group previously synthesized a series of quinoline-based compounds in an attempt to identify novel anticancer agents. With a molecular docking analysis, the novel compound 160a was predicted to target p-glycoprotein, an MDR candidate. The purpose of this study is to evaluate 160a’s MDR reversal effect and investigate the underlying mechanism at the molecular level. To investigate 160a’s inhibitory effect, we used a series of parental cancer cell lines (A549, LCC6, KYSE150, and MCF-7), the corresponding doxorubicin-resistant cell lines, an MTS cytotoxicity assay, an intracellular doxorubicin accumulation test, and multidrug resistance assays. The Compusyn program confirmed, with a combination index (CI) value greater than 1, that 160a combined with doxorubicin exerts a synergistic effect. Intracellular doxorubicin accumulation and transported calcein acetoxymethyl (AM) (a substrate for p-glycoprotein) were both increased when cancer cells with MDR were treated with compound 160a. We also showed that compound 160a’s MDR reversal effect can persist for at least 1 h. Taken together, these results suggest that the quinoline compound 160a possesses high potential to reverse MDR by inhibiting p-glycoprotein-mediated drug efflux in cancer cells with MDR.
Keywords: Anticancer
Multidrug resistance
P-glycoprotein
Quinoline compounds
Publisher: MDPI AG
Journal: Fire safety journal 
ISSN: 2079-7737
EISSN: 2079-7737
DOI: 10.3390/biology8040075
Rights: © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
The following publication Zhou, Y., Chung, P. Y., Ma, J. Y. W., Lam, A. K. Y., Law, S., Chan, K. W., ... & Tang, J. C. O. (2019). Development of a Novel Quinoline Derivative as a P-Glycoprotein Inhibitor to Reverse Multidrug Resistance in Cancer Cells. Biology, 8(4), 75 is available at https://doi.org/10.3390/biology8040075
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