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Title

Antimicrobial, Anticancer and Multidrug-Resistant Reversing Activity of Novel Oxygen-, Sulfur- and Selenoflavones and Bioisosteric Analogues

AuthorsMarć, Małgorzata Anna; Kincses, A.; Rácz, Bálint; Nasim, Muhammad Jawad; Sarfraz, Muhammad; Lázaro-Milla, Carlos; Domínguez-Álvarez, Enrique ; Jacob, C.; Spengler, G.; Almendros, Pedro CSIC ORCID
KeywordsSelenium
Flavonoids
Sulfur
Multidrug resistance (MDR)
MDR efflux pumps
P-glycoprotein (P-gp) efflux pump
Nematicidal activity
Antimicrobial
Cancer
Issue Date11-Dec-2020
PublisherMultidisciplinary Digital Publishing Institute
CitationPharmaceuticals 13(12): 453 (2020)
AbstractMultidrug resistance of cancer cells to cytotoxic drugs still remains a major obstacle to the success of chemotherapy in cancer treatment. The development of new drug candidates which may serve as P-glycoprotein (P-gp) efflux pump inhibitors is a promising strategy. Selenium analogues of natural products, such as flavonoids, offer an interesting motif from the perspective of drug design. Herein, we report the biological evaluation of novel hybrid compounds, bearing both the flavone core (compounds 1–3) or a bioisosteric analogue core (compounds 4–6) and the triflyl functional group against Gram-positive and Gram-negative bacteria, yeasts, nematodes, and human colonic adenocarcinoma cells. Results show that these flavones and analogues of flavones inhibited the activity of multidrug resistance (MDR) efflux pump ABCB1 (P-glycoprotein, P-gp). Moreover, the results of the rhodamine 123 accumulation assay demonstrated a dose-dependent inhibition of the abovementioned efflux pump. Three compounds (4, 5, and 6) exhibited potent inhibitory activity, much stronger than the positive control, verapamil. Thus, these chalcogen bioisosteric analogues of flavones become an interesting class of compounds which could be considered as P-gp efflux pump inhibitors in the therapy of MDR cancer. Moreover, all the compounds served as promising adjuvants in the cancer treatment, since they exhibited the P-gp efflux pump modulating activity.
Description© 2020 by the authors
Publisher version (URL)https://doi.org/10.3390/ph13120453
URIhttp://hdl.handle.net/10261/225703
DOI10.3390/ph13120453
E-ISSN1424-8247
Appears in Collections:(IQOG) Artículos

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