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Low-Generation Cationic Phosphorus Dendrimers: Novel Approach to Tackle Drug-Resistant S. aureus In Vitro and In Vivo

dc.rights.licenseopenen_US
hal.structure.identifierChimie et Biologie des Membranes et des Nanoobjets [CBMN]
dc.contributor.authorAPARTSIN, Evgeny
dc.contributor.authorAKHIR, Abdul
dc.contributor.authorKAUL, Grace
dc.contributor.authorSAXENA, Deepanshi
dc.contributor.authorLAURENT, Regis
dc.contributor.authorSRIVASTAVA, Kishore Kumar
dc.contributor.authorMIGNANI, Serge
dc.contributor.authorMAJORAL, Jean-Pierre
dc.contributor.authorCHOPRA, Sidharth
dc.date.accessioned2024-04-23T09:57:01Z
dc.date.available2024-04-23T09:57:01Z
dc.date.issued2023-07-10
dc.identifier.issn1525-7797en_US
dc.identifier.urihttps://oskar-bordeaux.fr/handle/20.500.12278/199274
dc.description.abstractEnThe incessant, global increase in antimicrobial resistance (AMR) is a very big challenge for healthcare systems. AMR is predicted to grow at an alarming pace, with a dramatic increase in morbidity, mortality, and a 100 trillion US$ loss to the global economy by 2050. The mortality rate caused by methicillin-resistant S. aureus (MRSA) is much higher as compared to infections caused by drug-susceptible S. aureus. Additionally, there is a big paucity of therapeutics available for treatment of serious infections caused by MRSA. Thus, the discovery and development of novel therapies is an urgent, unmet medical need. In this context, we synthesized AE4G0, a low-generation cationic-phosphorus dendrimer expressing potent antimicrobial activity against S. aureus and Enterococcus sp., and demonstrating a broad selectivity index against eukaryotic cells. AE4G0 exhibits concentration-dependent, bactericidal activity and synergizes with gentamicin, especially against gentamicin-resistant MRSA NRS119. Fluorescence and scanning electron microscopy demonstrate that treatment with AE4G0 led to the utter destruction of S. aureus ATCC 29213 without inducing resistance, despite repeated exposure. When tested in vivo, AE4G0 demonstrates significant efficacy against S. aureus ATCC 29213, alone and in combination with gentamicin against gentamicin-resistant S. aureus NRS119 in the murine skin model of infection. Taken together, AE4G0 demonstrates the potential to be translated as a novel therapeutic option for the treatment of topical, drug-resistant S. aureus infections.
dc.language.isoENen_US
dc.subject.enAromatic compounds
dc.subject.enBacteria
dc.subject.enDendrons
dc.subject.enHydrocarbons
dc.subject.enInfectious diseases
dc.title.enLow-Generation Cationic Phosphorus Dendrimers: Novel Approach to Tackle Drug-Resistant S. aureus In Vitro and In Vivo
dc.typeArticle de revueen_US
dc.identifier.doi10.1021/acs.biomac.3c00266en_US
dc.subject.halSciences du Vivant [q-bio]/Biochimie, Biologie Moléculaireen_US
bordeaux.journalBiomacromoleculesen_US
bordeaux.page3215-3227en_US
bordeaux.volume24en_US
bordeaux.hal.laboratoriesCBMN : Chimie & de Biologie des Membranes & des Nano-objets - UMR 5248en_US
bordeaux.issue7en_US
bordeaux.institutionUniversité de Bordeauxen_US
bordeaux.institutionBordeaux INPen_US
bordeaux.institutionCNRSen_US
bordeaux.peerReviewedouien_US
bordeaux.inpressnonen_US
bordeaux.import.sourcehal
hal.identifierhal-04174818
hal.version1
hal.popularnonen_US
hal.audienceInternationaleen_US
hal.exportfalse
workflow.import.sourcehal
dc.rights.ccPas de Licence CCen_US
bordeaux.COinSctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Biomacromolecules&rft.date=2023-07-10&rft.volume=24&rft.issue=7&rft.spage=3215-3227&rft.epage=3215-3227&rft.eissn=1525-7797&rft.issn=1525-7797&rft.au=APARTSIN,%20Evgeny&AKHIR,%20Abdul&KAUL,%20Grace&SAXENA,%20Deepanshi&LAURENT,%20Regis&rft.genre=article


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