Usai Donatella, Donadu Matthew, Bua Alessandra, Molicotti Paola, Zanetti Stefania, Piras Sandra, Corona Paola, Ibba Roberta, Carta Antonio
Department of Biological Science, University of Sassari, Sassari, Italy.
Department of Chemistry and Pharmacy, University of Sassari, Sassari, Italy.
J Infect Dev Ctries. 2019 Feb 28;13(2):162-164. doi: 10.3855/jidc.11102.
with the continuous emergence of pathogenic resistance to conventional drugs through efflux pumps, increasing efforts are directed toward discovering efflux inhibitory molecules.
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.
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.
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.
随着病原菌通过外排泵对传统药物的耐药性不断出现,人们越来越致力于发现外排抑制分子。
在本研究中,对10株白色念珠菌临床菌株以及12株革兰氏阳性和革兰氏阴性细菌的临床菌株和美国典型培养物保藏中心(ATCC)菌株,研究了三种属于苯氧甲基喹喔啉系列的P-糖蛋白(P13CP、P22CP、P34CP)外排抑制剂(EI),这些抑制剂能够恢复/增强阿霉素和长春新碱对人肿瘤细胞系的抗增殖活性以及不同抗生素对临床分离株的抗增殖活性。
P22CP和P34CP抑制剂使所有念珠菌菌株中氟康唑的最小杀菌浓度(MFC)值降低,P13CP抑制剂使5/10的真菌菌株中氟康唑的MFC值降低。
迫切需要具有新作用模式的新型抗生素来抑制多重耐药菌的出现。另一种方法是鉴定能够干扰外排过程的分子。