Donatella Usai1, Matthew Donadu2, Alessandra Bua3, Paola Molicotti4, Stefania Zanetti5, Sandra Piras6, Paola Corona7, Roberta Ibba8, Antonio Carta9. 1. Department of Biological Science, University of Sassari, Sassari, Italy. dusai@uniss.it. 2. Department of Biological Science, University of Sassari, Sassari, Italy. mdonadu@jidc.org. 3. Department of Biological Science, University of Sassari, Sassari, Italy. albua@uniss.it. 4. Department of Biological Science, University of Sassari, Sassari, Italy. molicott@uniss.it. 5. Department of Biological Science, University of Sassari, Sassari, Italy. zanettis@uniss.it. 6. Department of Chemistry and Pharmacy, University of Sassari, Sassari, Italy. piras@uniss.it. 7. Department of Chemistry and Pharmacy, University of Sassari, Sassari, Italy. pcorona@uniss.it. 8. Department of Chemistry and Pharmacy, University of Sassari, Sassari, Italy. ribba@uniss.it. 9. Department of Chemistry and Pharmacy, University of Sassari, Sassari, Italy. acarta@uniss.it.
Abstract
INTRODUCTION: with the continuous emergence of pathogenic resistance to conventional drugs through efflux pumps, increasing efforts are directed toward discovering efflux inhibitory molecules. METHODOLOGY: in this study three P-glycoprotein (P13CP, P22CP, P34CP) efflux-inhibitors (EIs), belonging to the series of phenoxymethylquinoxalines capable to restore/potentiate the antiproliferative activity of doxorubicin and vincristine against human tumor cell lines and different antibiotics against clinical isolates, were investigated on 10 clinical strains of Candida and 12 clinical and ATCC strains of Gram positive and Gram-negative bacteria. RESULTS: MFC values of FLC were reduced in all Candida strains by the P22CP and P34CP inhibitors, and in 5/10 fungal strains by the P13CP inhibitor. CONCLUSION: novel antibiotics with new modes of action are urgently required to suppress the rise of MDR bacteria. An alternative approach would be to identify molecules that can interfere with the process of efflux. Copyright (c) 2019 Donatella Usai, Matthew Donadu, Alessandra Bua, Paola Molicotti, Stefania Zanetti, Sandra Piras, Paola Corona, Roberta Ibba, Antonio Carta.
INTRODUCTION: with the continuous emergence of pathogenic resistance to conventional drugs through efflux pumps, increasing efforts are directed toward discovering efflux inhibitory molecules. METHODOLOGY: in this study three P-glycoprotein (P13CP, P22CP, P34CP) efflux-inhibitors (EIs), belonging to the series of phenoxymethylquinoxalines capable to restore/potentiate the antiproliferative activity of doxorubicin and vincristine against humantumor cell lines and different antibiotics against clinical isolates, were investigated on 10 clinical strains of Candida and 12 clinical and ATCC strains of Gram positive and Gram-negative bacteria. RESULTS: MFC values of FLC were reduced in all Candida strains by the P22CP and P34CP inhibitors, and in 5/10 fungal strains by the P13CP inhibitor. CONCLUSION: novel antibiotics with new modes of action are urgently required to suppress the rise of MDR bacteria. An alternative approach would be to identify molecules that can interfere with the process of efflux. Copyright (c) 2019 Donatella Usai, Matthew Donadu, Alessandra Bua, Paola Molicotti, Stefania Zanetti, Sandra Piras, Paola Corona, Roberta Ibba, Antonio Carta.
Authors: Shereen A Sayed; Ehsan A B Hassan; Muhamad R Abdel Hameed; Michael N Agban; Mostafa F Mohammed Saleh; Hayam H Mohammed; Abu-Baker M Abdel-Aal; Sherein G Elgendy Journal: J Blood Med Date: 2021-06-15