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doi:10.22028/D291-32965
Titel: | Antimicrobial, Anticancer and Multidrug-Resistant Reversing Activity of Novel Oxygen-, Sulfur- and Selenoflavones and Bioisosteric Analogues |
VerfasserIn: | Marć, Małgorzata Anna Kincses, Annamária Rácz, Bálint Nasim, Muhammad Jawad Sarfraz, Muhammad Lázaro-Milla, Carlos Domínguez-Álvarez, Enrique Jacob, Claus Spengler, Gabriella Almendros, Pedro |
Sprache: | Englisch |
Titel: | Pharmaceuticals |
Bandnummer: | 13 |
Heft: | 12 |
Verlag/Plattform: | MDPI |
Erscheinungsjahr: | 2020 |
Freie Schlagwörter: | selenium flavonoids sulfur multidrug resistance (MDR) MDR efflux pumps P-glycoprotein (P-gp) efflux pump nematicidal activity antimicrobial cancer |
DDC-Sachgruppe: | 500 Naturwissenschaften 600 Technik 610 Medizin, Gesundheit |
Dokumenttyp: | Journalartikel / Zeitschriftenartikel |
Abstract: | Multidrug 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. |
DOI der Erstveröffentlichung: | 10.3390/ph13120453 |
Link zu diesem Datensatz: | urn:nbn:de:bsz:291--ds-329657 hdl:20.500.11880/30486 http://dx.doi.org/10.22028/D291-32965 |
ISSN: | 1424-8247 |
Datum des Eintrags: | 29-Jan-2021 |
Bezeichnung des in Beziehung stehenden Objekts: | Supplementary Materials |
In Beziehung stehendes Objekt: | http://www.mdpi.com/1424-8247/13/12/453/s1 |
Fakultät: | NT - Naturwissenschaftlich- Technische Fakultät |
Fachrichtung: | NT - Pharmazie |
Professur: | NT - Prof. Dr. Claus Jacob |
Sammlung: | SciDok - Der Wissenschaftsserver der Universität des Saarlandes |
Dateien zu diesem Datensatz:
Datei | Beschreibung | Größe | Format | |
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pharmaceuticals-13-00453.pdf | 875,05 kB | Adobe PDF | Öffnen/Anzeigen |
Diese Ressource wurde unter folgender Copyright-Bestimmung veröffentlicht: Lizenz von Creative Commons