: VT-1161 is a novel tetrazole antifungal agent with high specificity for fungal CYP51 (compared to human CYP enzymes) which has been proven to have fewer adverse effects and drug-drug interaction profiles due to fewer off-target inhibitors. In this study, we evaluated the anti-biofilm potential of VT-1161 against mono- and dual-species biofilms of Candida albicans, Klebsiella pneumoniae and Staphylococcus aureus. VT-1161 inhibited planktonic growth of all three strains, with an MIC value of 2 µg mL-1 for C. albicans and 0.5 µg mL-1 for K. pneumoniae and S. aureus, and killed 99.9% of the microbial populations, indicating a cytocidal action. Additionally, VT-1161 showed an excellent anti-biofilm action, since it inhibited mono-microbial biofilms by 80% at 0.5 µg mL-1, and dual-species biofilms of C. albicans/K. pneumoniae and C. albicans/S. aureus by 90% at the same concentration. Additionally, the eradication of mature biofilms after 24 h of VT-1161 exposure was excellent, reaching 90% at 2 μg mL-1 for both mono- and dual-species biofilms. In such mixed biofilms, the use of VT-1161 was revealed to be an alternative treatment because it was able to reduce the number of cells of each species during both inhibition and eradication. Since long-term therapy is necessary for most fungal biofilm infections due to their recurrence and obstinacy, VT-1161 showed low cytotoxicity against normal human cell lines and also against the invertebrate model Caenorhabditis elegans. Considering the excellent anti-biofilm potential and its GRAS (generally recognized as safe) status, VT-1161 may find use in the prevention or therapeutic treatment of mono- or poly-microbial biofilms.

VT-1161—A Tetrazole for Management of Mono- and Dual-Species Biofilms / Maione, Angela; Mileo, Aldo; Pugliese, Stefano; Siciliano, Antonietta; Cirillo, Luigi; Carraturo, Federica; DE ALTERIIS, Elisabetta; DE FALCO, Maria; Guida, Marco; Galdiero, Emilia. - In: MICROORGANISMS. - ISSN 2076-2607. - 11:2(2023), p. 237. [10.3390/microorganisms11020237]

VT-1161—A Tetrazole for Management of Mono- and Dual-Species Biofilms

Angela Maione
Primo
;
Aldo Mileo;Stefano Pugliese;Antonietta Siciliano;Federica Carraturo;Elisabetta de Alteriis;Maria De Falco;Marco Guida
Penultimo
;
Emilia Galdiero
Ultimo
2023

Abstract

: VT-1161 is a novel tetrazole antifungal agent with high specificity for fungal CYP51 (compared to human CYP enzymes) which has been proven to have fewer adverse effects and drug-drug interaction profiles due to fewer off-target inhibitors. In this study, we evaluated the anti-biofilm potential of VT-1161 against mono- and dual-species biofilms of Candida albicans, Klebsiella pneumoniae and Staphylococcus aureus. VT-1161 inhibited planktonic growth of all three strains, with an MIC value of 2 µg mL-1 for C. albicans and 0.5 µg mL-1 for K. pneumoniae and S. aureus, and killed 99.9% of the microbial populations, indicating a cytocidal action. Additionally, VT-1161 showed an excellent anti-biofilm action, since it inhibited mono-microbial biofilms by 80% at 0.5 µg mL-1, and dual-species biofilms of C. albicans/K. pneumoniae and C. albicans/S. aureus by 90% at the same concentration. Additionally, the eradication of mature biofilms after 24 h of VT-1161 exposure was excellent, reaching 90% at 2 μg mL-1 for both mono- and dual-species biofilms. In such mixed biofilms, the use of VT-1161 was revealed to be an alternative treatment because it was able to reduce the number of cells of each species during both inhibition and eradication. Since long-term therapy is necessary for most fungal biofilm infections due to their recurrence and obstinacy, VT-1161 showed low cytotoxicity against normal human cell lines and also against the invertebrate model Caenorhabditis elegans. Considering the excellent anti-biofilm potential and its GRAS (generally recognized as safe) status, VT-1161 may find use in the prevention or therapeutic treatment of mono- or poly-microbial biofilms.
2023
VT-1161—A Tetrazole for Management of Mono- and Dual-Species Biofilms / Maione, Angela; Mileo, Aldo; Pugliese, Stefano; Siciliano, Antonietta; Cirillo, Luigi; Carraturo, Federica; DE ALTERIIS, Elisabetta; DE FALCO, Maria; Guida, Marco; Galdiero, Emilia. - In: MICROORGANISMS. - ISSN 2076-2607. - 11:2(2023), p. 237. [10.3390/microorganisms11020237]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/913451
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