Please use this identifier to cite or link to this item:
PIRA download icon_1.1View/Download Full Text
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
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 (
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
Appears in Collections:Journal/Magazine Article

Files in This Item:
File Description SizeFormat 
Zhou_Development_Novel_Quinoline.pdf4.3 MBAdobe PDFView/Open
Open Access Information
Status open access
File Version Version of Record
View full-text via PolyU eLinks SFX Query
Show full item record

Page views

Last Week
Last month
Citations as of May 28, 2023


Citations as of May 28, 2023


Citations as of May 25, 2023


Citations as of May 25, 2023

Google ScholarTM



Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.