Ability Of Ciprofloxacin Research Articles

Ciprofloxacin and Moxifloxacin Could Interact with SARS-CoV-2 Protease: Preliminary <i>In Silico</i> Analysis

Background: A serious of actions have been taken to control the epidemic of the 2019-nCoV virus, and the effective therapeutic methods are in urgent needs to prevent infection. Fluoroquinolones are known synthetic group of antibiotics that have been the subject of many research interests. It was shown that this class of drugs could possess antiviral activity as a broad range of anti-infective activities. Based on these findings, we performed in silico molecular docking analysis to provide, for the first time, the basis for the potential evidence pointing ciprofloxacin and moxifloxacin ability to interact with COVID-19 Main Protease. Methods: In silico molecular docking analysis was applied to assess the possible ability of ciprofloxacin and moxifloxacin to interact with COVID-19 Main Protease (Mpro). Genetic Optimization for Ligand Docking (GOLD) 5.6.3 was used for the docking studies. Moreover, chloroquine and nelfinavir were used as positive controls for comparison. Findings: The obtained results pointed out that the tested antibiotics exert strong capacity for binding to COVID-19 Main Protease (Mpro). The analysis of the docking results showed that ciprofloxacin and moxifloxacin bound to the protein active site more strongly than native ligand. When comparing with positive controls, a detailed analysis of the ligand-protein interactions shows the tested fluoroquinolones exert a greater number of protein interactions than chloroquine and nelfinavir. It is worth emphasizing that ciprofloxacin binds to the protein with four strong hydrogen bonds (compared to one and two hydrogen bonds for chloroquine and nelfinavir, respectively) and a significant number of hydrophobic interactions. However, lower binding energy values were stated when compared to chloroquine and nelfinavir. Interpretation: Herein, for the first time, we have demonstrated that ciprofloxacin and moxifloxacin may interact with COVID-19 Main Protease (Mpro) which indicates that both fluoroquinolone antibiotics may be potential inhibitors of the tested protease. Funding Statement: Medical University of Silesia Grants no. KNW-1-037/K/9/O, KNW-1-055/K/9/O. Energy-minimization calculations have been carried out using resources provided by Wroclaw Centre for 818 Networking and Supercomputing (http://wcss.pl), Grant No. 382. Declaration of Interests: The authors declare no competing interests.

Mutant prevention concentrations of ciprofloxacin against urinary isolates of Escherichia coli and Klebsiella pneumoniae

The aim of this work was to study the ability of ciprofloxacin to restrict the development of resistant mutants of Escherichia coli and Klebsiella pneumoniae through determination of the Mutant Prevention Concentration (MPC). We studied 140 strains of E. coli and 86 strains of K. pneumoniae with different profiles of sensitivity to fluoroquinolones and extended spectrum beta lactamase (ESBL) production. The MPCs were determined using an inoculum of 1010 CFU/ml in Mueller-Hinton agar plates with serial concentrations of ciprofloxacin. Ciprofloxacin-susceptible ESBL-producing strains showed a higher MPC for ciprofloxacin (P <0.001) than ciprofloxacin-susceptible non ESBL-producing strains, while ciprofloxacin-resistant ESBL-producing and non ESBL-producing strains did not significantly differ. The presence of qnr variants was associated with elevated MPCs. This was observed for both tested organisms. Our study helps to explain the frequent finding of resistance to fluoroquinolones in ESBL-producing strains. Consequently, the use of concentrations of ciprofloxacin higher than the MIC in order to prevent the recovery and growth of resistant mutants is recommended.

Interaction between ciprofloxacin and melanin: The effect on proliferation and melanization in melanocytes

There have been described serious adverse events caused by ciprofloxacin in pigmented tissues. It is known that some fluoroquinolones bind well to melanin rich tissues, but the relation between their affinity to melanin and the skin or eye toxicity is not well documented. The aim of this study was to examine whether ciprofloxacin binds to melanin, and how this interaction affects the proliferation and melanization in melanocytes. We have demonstrated that complexes which ciprofloxacin forms with melanin possess at least two classes of independent binding sites. Their association constants are K(1)~10(5) M(-1) and K(2)~10(2) M(-1), respectively. Ciprofloxacin has induced evident concentration-dependent loss in melanocytes viability. The value of ED(50) was found to be ~0.5 mM. It has also been shown that ciprofloxacin reduces melanin content, and decreases tyrosinase activity in human skin melanocytes. The ability of ciprofloxacin to interact with melanin and its inhibitory effect on melanization in melanocytes in vitro may explain a potential role of melanin in the mechanisms of ciprofloxacin toxic effects in vivo.

Fluoroquinolone−Biomembrane Interaction at the DPPC/PG Lipid−Bilayer Interface

The interaction of two fluoroquinolones, ciprofloxacin (CPX) and its N-4-butylpiperazinyl derivative (BCPX), with liposomes bearing negative surface charge was studied by fluorescence methods. Binding of 1-anilino-8-naphthalenesulfonate to the liposome surface and diphenylhexatriene (DPH) and diphenylhexatriene−propionic (DPH−AP) acid fluorescence anisotropy measurements were differently affected by the two. On the basis of the variations of the surface potential and phase transition temperature (Tm) of the phospholipids studied, it was concluded that (i) both drugs interact electrostatically at the lipid membrane interface and (ii) the butyl side chain of BCPX led to a different interaction with the lipid headgroups. This behavior is then related to the activity of an efflux pump Serratia marcescens NIMA, which appear to be affected by the ability of CPX and BCPX to interact with the inner surface of the plasma membrane.

Ability of ciprofloxacin but not pipemidic acid to differentiate all three biovariants of Mycobacterium fortuitum from Mycobacterium chelonae.

When tested against 312 clinical isolates of rapidly growing mycobacteria, the quinolone pipemidic acid correctly separated Mycobacterium chelonae (M. chelonei) from Mycobacterium fortuitum biovar fortuitum but not from biovar peregrinum or the third biovar complex. The new 4-quinolone ciprofloxacin correctly separated all three biovars of M. fortuitum from M. chelonae and appears to provide a better taxonomic test.