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dc.contributor.authorZhou, Y
dc.contributor.authorChung, PY
dc.contributor.authorMa, JYW
dc.contributor.authorLam, AKY
dc.contributor.authorLaw, S
dc.contributor.authorChan, KW
dc.contributor.authorChan, ASC
dc.contributor.authorLi, X
dc.contributor.authorLam, KH
dc.contributor.authorChui, CH
dc.contributor.authorTang, JCO
dc.date.accessioned2019-11-26T05:13:50Z
dc.date.available2019-11-26T05:13:50Z
dc.date.issued2019
dc.identifier.issn2079-7737
dc.identifier.doi10.3390/biology8040075
dc.identifier.urihttp://hdl.handle.net/10072/389290
dc.description.abstractMultidrug 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.
dc.description.peerreviewedYes
dc.languageEnglish
dc.language.isoeng
dc.publisherMDPI
dc.publisher.placeSwitzerland
dc.relation.ispartofpagefrom75:1
dc.relation.ispartofpageto75:19
dc.relation.ispartofissue4
dc.relation.ispartofjournalBiology
dc.relation.ispartofvolume8
dc.subject.fieldofresearchBiochemistry and Cell Biology
dc.subject.fieldofresearchBiological Sciences
dc.subject.fieldofresearchcode0601
dc.subject.fieldofresearchcode06
dc.subject.keywordsanticancer
dc.subject.keywordsmultidrug resistance
dc.subject.keywordsp-glycoprotein
dc.subject.keywordsquinoline compounds
dc.titleDevelopment of a novel quinoline derivative as a P-glycoprotein inhibitor to reverse multidrug resistance in cancer cells
dc.typeJournal article
dc.type.descriptionC1 - Articles
dcterms.bibliographicCitationZhou, Y; Chung, PY; Ma, JYW; Lam, AKY; Law, S; Chan, KW; Chan, ASC; Li, X; Lam, KH; Chui, CH; Tang, JCO, Development of a novel quinoline derivative as a P-glycoprotein inhibitor to reverse multidrug resistance in cancer cells, Biology, 2019, 8 (4), pp. 75:1-75:19
dcterms.dateAccepted2019-09-27
dcterms.licensehttp://creativecommons.org/licenses/by/4.0/
dc.date.updated2019-11-26T02:13:15Z
dc.description.versionVersion of Record (VoR)
gro.rights.copyright© 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/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited
gro.hasfulltextFull Text
gro.griffith.authorLam, Alfred K.


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