161722 20251017144651.0 doi 10.1186/s13065-025-01538-7 sideral 144366 ART-2025-144366 eng Bescós-Ramo, Sara Universidad de Zaragoza (orcid)0009-0008-6456-4856 Catechol-substituted siderophore colistin exhibits superior antimicrobial activity than its unmodified polypeptide counterpart 2025 Access copy available to the general public Unrestricted Catechol moieties have been covalently coupled to the last-resort polypeptide antibiotic colistin via esterification and amidation reactions, inspired by the superior antimicrobial action of cefiderocol, i.e., a catechol-substituted siderophore cephalosporin. Among the tested strategies, the incorporation of the catechol motif by amidation reduces by 50% the minimum concentration to inhibit the growth of a clinical strain of uropathogenic Escherichia coli (E. coli) in its planktonic form. Its minimum bactericidal concentration is reduced by 25% after chemical modification. The tested modified antibiotic did not show cytotoxicity against human fibroblasts and keratinocytes at bactericidal doses. Additionally, due to the potential nephrotoxicity of colistin, the cytotoxicity of this catechol-substituted siderophore colistin was evaluated in a 3D model of human renal organoids showing no cytotoxicity at the doses tested. The chemical incorporation of catechol groups to existing antibiotics can reduce the doses to exert a fast antimicrobial action reducing the chances to develop antibiotic resistance. info:eu-repo/grantAgreement/ES/DGA/E47-23R info:eu-repo/grantAgreement/ES/MICINN/PID2021-126132NB-I00 info:eu-repo/grantAgreement/ES/MICINN/PID2023-146091OB-I00 info:eu-repo/grantAgreement/ES/MICIU/CEX2023-001286-S info:eu-repo/semantics/openAccess by-nc-nd https://creativecommons.org/licenses/by-nc-nd/4.0/deed.es info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion Gámez, Enrique (orcid)0000-0002-0272-3152 Encabo-Berzosa, María del Mar (orcid)0000-0003-4891-105X Piñol, Milagros Universidad de Zaragoza (orcid)0000-0001-5556-2172 Oriol, Luis Universidad de Zaragoza (orcid)0000-0002-0922-5615 Arruebo, Manuel Universidad de Zaragoza (orcid)0000-0003-3165-0156 5005 555 Universidad de Zaragoza Dpto. Ing.Quím.Tecnol.Med.Amb. Área Ingeniería Química 2013 765 Universidad de Zaragoza Dpto. Química Orgánica Área Química Orgánica 19 (2025), 162 [14 pp.] BMC Chemistry 2661-801X 2298063 http://zaguan.unizar.es/record/161722/files/texto_completo.pdf Versión publicada 2464501 http://zaguan.unizar.es/record/161722/files/texto_completo.jpg?subformat=icon icon Versión publicada oai:zaguan.unizar.es:161722 articulos driver 2025-10-17-14:36:30 ARTICLE