@article{APS3666,
author = {Zheng Hou and Jing-ru Meng and Jin-rong Zhao and Ben-quan Hu and Jie Liu and Xiao-jun Yan and Min Jia and Xiao-xing Luo},
title = {Inhibition of β-lactamase-mediated oxacillin resistance in Staphylococcus aureus by a deoxyribozyme},
journal = {Acta Pharmacologica Sinica},
volume = {28},
number = {11},
year = {2016},
keywords = {},
abstract = {Aim: To investigate the oxacillin susceptibility restoration of methicillin-resistant Staphylococcus aureus (MRSA) by targeting the signaling pathway of blaR1-blaZ with a DNAzyme.
Methods: A DNAzyme (named PS-DRz602) targeting blaR1 mRNA was designed and synthesized. After DRz602 was introduced into a MRSA strain WHO-2, the colony-forming units of WHO-2 on the Mueller-Hinton agar containing 6 mg/L oxacillin and the minimum inhibitory concentrations of oxacillin were determined. The inhibitory effects of DRz602 on the expressions of antibiotic-resistant gene blaR1 and its downstream gene blaZ were detected by real time RT-PCR.
Results: PS-DRz602 significantly decreased the transcription of blaR1 mRNA and led to the significant reduction of blaZ in a concentration-dependent manner. Consequently, the resistance of S aureus WHO-2 to the β-lactam antibiotic oxacillin was significantly inhibited.
Conclusion: Our results indicated that blocking the blaR1-blaZ signaling pathway via DNAzyme might provide a viable strategy for inhibiting the resistance of MRSA to β-lactam antibiotics and that BlaR1 might be a potential target for pharmacological agents combating MRSA.},
issn = {1745-7254}, url = {http://www.chinaphar.com/article/view/3666}
}