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The Effect of Conjugation of Ciprofloxacin and Moxifloxacin with Fatty Acids on Their Antibacterial and Anticancer Activity

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cris.lastimport.scopus2024-02-12T20:26:53Z
dc.abstract.enNovel conjugates (CP) of moxifloxacin (MXF) with fatty acids (1m–16m) were synthesized with good yields utilizing amides chemistry. They exhibit a more pronounced cytotoxic potential than the parent drug. They were the most effective for prostate cancer cells with an IC50 below 5 µM for respective conjugates with sorbic (2m), oleic (4m), 6-heptenoic (10m), linoleic (11m), caprylic (15m), and stearic (16m) acids. All derivatives were evaluated against a panel of standard and clinical bacterial strains, as well as towards mycobacteria. The highest activity towards standard isolates was observed for the acetic acid derivative 14m, followed by conjugates of unsaturated crotonic (1m) and sorbic (2m) acids. The activity of conjugates tested against an expanded panel of clinical coagulase-negative staphylococci showed that the compound (14m) was recognized as a leading structure with an MIC of 0.5 μg/mL denoted for all quinolone-susceptible isolates. In the group of CP derivatives, sorbic (2) and geranic (3) acid amides exhibited the highest bactericidal potential against clinical strains. The M. tuberculosis Spec. 210 strain was the most sensitive to sorbic (2m) conjugate and to conjugates with medium- and long-chain polyunsaturated acids. To establish the mechanism of antibacterial action, selected CP and MXF conjugates were examined in both topoisomerase IV decatenation assay and the DNA gyrase supercoiling assay, followed by suitable molecular docking studies.
dc.affiliationUniwersytet Warszawski
dc.contributor.authorBielenica, Anna
dc.contributor.authorWrzosek, Małgorzata
dc.contributor.authorAugustynowicz-Kopeć, Ewa
dc.contributor.authorStefańska, Joanna
dc.contributor.authorZabost, Anna
dc.contributor.authorJałbrzykowska, Karolina
dc.contributor.authorKmiecik, Sebastian
dc.contributor.authorKoliński, Michał
dc.contributor.authorRoszkowski, Piotr
dc.contributor.authorStruga, Marta
dc.contributor.authorChrzanowska, Alicja
dc.date.accessioned2024-01-26T10:11:20Z
dc.date.available2024-01-26T10:11:20Z
dc.date.copyright2022-06-02
dc.date.issued2022
dc.description.accesstimeAT_PUBLICATION
dc.description.financePublikacja bezkosztowa
dc.description.number11
dc.description.versionFINAL_PUBLISHED
dc.description.volume23
dc.identifier.doi10.3390/IJMS23116261
dc.identifier.issn1422-0067
dc.identifier.urihttps://repozytorium.uw.edu.pl//handle/item/122181
dc.identifier.weblinkhttps://www.mdpi.com/1422-0067/23/11/6261/pdf
dc.languageeng
dc.pbn.affiliationchemical sciences
dc.relation.ispartofInternational Journal of Molecular Sciences
dc.relation.pages6261
dc.rightsCC-BY
dc.sciencecloudnosend
dc.subject.enfluoroquinolone
dc.subject.enconjugation
dc.subject.enfatty acids
dc.subject.encytotoxicity
dc.subject.enantibacterial activity
dc.titleThe Effect of Conjugation of Ciprofloxacin and Moxifloxacin with Fatty Acids on Their Antibacterial and Anticancer Activity
dc.typeJournalArticle
dspace.entity.typePublication