Enoxacin (AT 2266) is a fluoroquinolone antibiotic, which disrupts bacterial DNA by inhibiting DNA gyrase and topoisomerase IV, with IC50 values of 126 µg/ml and 26.5 µg/ml, respectively. It also functions as a miRNA processing activator, enhancing siRNA-mediated mRNA degradation and promoting the biogenesis of endogenous miRNAs. Enoxacin exhibits potent antibacterial activity against both gram-positive and gram-negative bacteria and acts as a cancer-specific growth inhibitor by boosting TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing[1].[2].[3].[4].
体内研究
Furthermore, in an in vivo study, in GFP transgenic mice, Enoxacin administered at 100 µM in a volume of 2 µl directly into the ear once a day for three consecutive days (days 12, 13, and 14), significantly enhances GFP mRNA knockdown efficiency mediated by Lv-siGFP (from 80% to 60%; leaving 40% GFP mRNA levels), while having no effect on GFP expression when administered alone in the GFP transgenic line C57BL/6-Tg(ACTB-EGFP)1Osb/J (aged 10 days) with lentivirus expressing shGFP (Lv-siGFP; injected into the ear for 10 days)[3].
体外研究
In cell-based assays, Enoxacin increases siGFP-mediated gene knockdown in a dose-dependent manner within a HEK293 cells-based reporter system, showing an effective concentration (EC50) of about 30 µM. It specifically enhances the processing of miRNAs and the loading of siRNA duplexes onto RISCs in these cells at a concentration of 50 µM[3].
Enoxacin does not affect the processing of pre-let-7 or pre-miR-30a by Dicer alone, but when combined with TRBP, it enhances their processing by Dicer[3].
Enoxacin is effective against various bacterial strains, inhibiting 90% of pathogens like Escherichia coli, Klebsiella sp., Aeromonas sp., Enterobacter spp., Serratia spp., Proteus mirabilis, and Morganella morganii at concentrations less than or equal to 0.8 micrograms/ml[5].
United States, Kentucky
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University of Louisville
Recruiting
Louisville, Kentucky, United States, 40202
Contact: Julio A Ramirez, MD 502-852-1148 jarami01@louisville.edu
Contact: David Seligson, MD 502-852-0923 d0seli01@louisville.edu
Sub-Investigator: Forest Arnold, DO
Sub-Investigator: Timothy Wiemkwn, PhD
Sub-Investigator: Robert Kelley, PhD
Sub-Investigator: James Summersgill, PhD
Sub-Investigator: Ruth Carrico, PhD
Sub-Investigator: Julie Harting, PharmD
Sub-Investigator: Paula Peyrani, MD
Principal Investigator: David Seligson, MD
Sub-Investigator: Craig Roberts, MD
Principal Investigator: Julio Ramirez, MD 收起 <<
CI 919;AT 2266;Sesquihydrate, Enoxacin;Rhône-Poulenc Rorer Brand of Enoxacin Sesquihydrate;Brand of Enoxacin Sesquihydrate;Sesquihydrate Rhône Poulenc Rorer;Pierre Fabre Brand of Enoxacin;Enoxacino;Comprecin;Enoxacine;Penetrex;NSC 629661;Pd107779
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蓝冰
存储条件
液体-20°C:3-6个月-80°C:12个月
粉末Keep in dark place,Sealed in dry,Room Temperature
United States, Kentucky
... 展开 >>
University of Louisville
Recruiting
Louisville, Kentucky, United States, 40202
Contact: Julio A Ramirez, MD 502-852-1148 jarami01@louisville.edu
Contact: David Seligson, MD 502-852-0923 d0seli01@louisville.edu
Sub-Investigator: Forest Arnold, DO
Sub-Investigator: Timothy Wiemkwn, PhD
Sub-Investigator: Robert Kelley, PhD
Sub-Investigator: James Summersgill, PhD
Sub-Investigator: Ruth Carrico, PhD
Sub-Investigator: Julie Harting, PharmD
Sub-Investigator: Paula Peyrani, MD
Principal Investigator: David Seligson, MD
Sub-Investigator: Craig Roberts, MD
Principal Investigator: Julio Ramirez, MD 收起 <<
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