ADMET study, spectroscopic characterization and effect of synthetic nitro chalcone in combination with norfloxacin, ciprofloxacin, and ethidium bromide against Staphylococcus aureus efflux pumps.

Autor: Rocha JE; Departamento de Química Biológica, Universidade Regional do Cariri, Crato, Ceará, Brasil., de Freitas TS; Departamento de Química Biológica, Universidade Regional do Cariri, Crato, Ceará, Brasil., Xavier JC; Departamento de Química Biológica, Universidade Regional do Cariri, Crato, Ceará, Brasil., Pereira RLS; Departamento de Química Biológica, Universidade Regional do Cariri, Crato, Ceará, Brasil., Pereira Junior FN; Centro de Ciências Agrárias e da Biodiversidade, Universidade Federal do Cariri, Crato, Ceará, Brasil., Nogueira CES; Departamento de Química Biológica, Universidade Regional do Cariri, Crato, Ceará, Brasil., Marinho MM; Faculdade de Educação, Ciência e Letras de Iguatu, Universidade Estadual do Ceará, Iguatu, Ceará, Brasil., Bandeira PN; Centro de Ciencias Exatas e Tecnologia, Universidade Estadual do Vale do Acaraú, Sobral, Ceará, Brasil., Rodrigues LG; Centro de Ciencias Exatas e Tecnologia, Universidade Estadual do Vale do Acaraú, Sobral, Ceará, Brasil., Marinho ES; Faculdade de Filosofia Dom Aureliano Mato, Universidade Estadual do Ceará, Limoeiro do Norte, Ceará, Brasil., de Lacerda BCGV; Faculdade Cecape, Juazeiro do Norte, Ceará, Brasil., de Andrade EM; Faculdade Cecape, Juazeiro do Norte, Ceará, Brasil., Teixeira AMR; Departamento de Química Biológica, Universidade Regional do Cariri, Crato, Ceará, Brasil., Dos Santos HS; Centro de Ciencias Exatas e Tecnologia, Universidade Estadual do Vale do Acaraú, Sobral, Ceará, Brasil., Coutinho HDM; Departamento de Química Biológica, Universidade Regional do Cariri, Crato, Ceará, Brasil.
Jazyk: angličtina
Zdroj: Fundamental & clinical pharmacology [Fundam Clin Pharmacol] 2023 Feb; Vol. 37 (1), pp. 163-173. Date of Electronic Publication: 2022 Sep 16.
DOI: 10.1111/fcp.12830
Abstrakt: Chalcones are present in a wide variety of plants, having in their structure two aromatic rings that are linked together by a chain composed of three carbon atoms with α, β-unsaturated to carbonyl system. Bacteria have several drug resistance mechanisms, among them the efflux pump; this mechanism, when active, is able to expel different compounds from inside bacterial cells. Several efflux pumps have already been identified for Staphylococcus aureus bacteria, including MepA and NorA. Many chalcones have been isolated and identified with various activities, such as antimicrobial. In view of this, this article aimed to evaluate the antibiotic modifying effect of chalcone (E)-1-(2-hydroxyphenyl)-3-(3-nitrophenyl)prop-2-en-1-one against S. aureus carrier of NorA and MepA efflux pump. Regarding the antibiotic, there was a synergism when associated with ciprofloxacin in SA-K2068 strain, showing this chalcone as an alternative to reverse the resistance to this medicine. The physicochemical properties calculated were fundamental in the description of the predicted pharmacokinetic properties. Despite the mutagenic risk caused by the metabolic activation of nitrochalcone, it is possible to notice a pharmacological principle in a longer half-life for the performance of biological activities. The compound has a good bioavailability, as it is highly absorbed in the intestine and easily transported by plasma proteins, in addition to not presenting neurotoxic, hepatotoxic, and cardiotoxic damage.
(© 2022 Société Française de Pharmacologie et de Thérapeutique. Published by John Wiley & Sons Ltd.)
Databáze: MEDLINE
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