000161722 001__ 161722
000161722 005__ 20251017144651.0
000161722 0247_ $$2doi$$a10.1186/s13065-025-01538-7
000161722 0248_ $$2sideral$$a144366
000161722 037__ $$aART-2025-144366
000161722 041__ $$aeng
000161722 100__ $$0(orcid)0009-0008-6456-4856$$aBescós-Ramo, Sara$$uUniversidad de Zaragoza
000161722 245__ $$aCatechol-substituted siderophore colistin exhibits superior antimicrobial activity than its unmodified polypeptide counterpart
000161722 260__ $$c2025
000161722 5060_ $$aAccess copy available to the general public$$fUnrestricted
000161722 5203_ $$aCatechol 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.
000161722 536__ $$9info:eu-repo/grantAgreement/ES/DGA/E47-23R$$9info:eu-repo/grantAgreement/ES/MICINN/PID2021-126132NB-I00$$9info:eu-repo/grantAgreement/ES/MICINN/PID2023-146091OB-I00$$9info:eu-repo/grantAgreement/ES/MICIU/CEX2023-001286-S
000161722 540__ $$9info:eu-repo/semantics/openAccess$$aby-nc-nd$$uhttps://creativecommons.org/licenses/by-nc-nd/4.0/deed.es
000161722 655_4 $$ainfo:eu-repo/semantics/article$$vinfo:eu-repo/semantics/publishedVersion
000161722 700__ $$0(orcid)0000-0002-0272-3152$$aGámez, Enrique
000161722 700__ $$0(orcid)0000-0003-4891-105X$$aEncabo-Berzosa, María del Mar
000161722 700__ $$0(orcid)0000-0001-5556-2172$$aPiñol, Milagros$$uUniversidad de Zaragoza
000161722 700__ $$0(orcid)0000-0002-0922-5615$$aOriol, Luis$$uUniversidad de Zaragoza
000161722 700__ $$0(orcid)0000-0003-3165-0156$$aArruebo, Manuel$$uUniversidad de Zaragoza
000161722 7102_ $$15005$$2555$$aUniversidad de Zaragoza$$bDpto. Ing.Quím.Tecnol.Med.Amb.$$cÁrea Ingeniería Química
000161722 7102_ $$12013$$2765$$aUniversidad de Zaragoza$$bDpto. Química Orgánica$$cÁrea Química Orgánica
000161722 773__ $$g19 (2025), 162 [14 pp.]$$tBMC Chemistry$$x2661-801X
000161722 8564_ $$s2298063$$uhttps://zaguan.unizar.es/record/161722/files/texto_completo.pdf$$yVersión publicada
000161722 8564_ $$s2464501$$uhttps://zaguan.unizar.es/record/161722/files/texto_completo.jpg?subformat=icon$$xicon$$yVersión publicada
000161722 909CO $$ooai:zaguan.unizar.es:161722$$particulos$$pdriver
000161722 951__ $$a2025-10-17-14:36:30
000161722 980__ $$aARTICLE