2017
DOI: 10.3390/antibiotics6040026
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Ubiquitous Nature of Fluoroquinolones: The Oscillation between Antibacterial and Anticancer Activities

Abstract: Fluoroquinolones are synthetic antibacterial agents that stabilize the ternary complex of prokaryotic topoisomerase II enzymes (gyrase and Topo IV), leading to extensive DNA fragmentation and bacteria death. Despite the similar structural folds within the critical regions of prokaryotic and eukaryotic topoisomerases, clinically relevant fluoroquinolones display a remarkable selectivity for prokaryotic topoisomerase II, with excellent safety records in humans. Typical agents that target human topoisomerases (su… Show more

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Cited by 75 publications
(49 citation statements)
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References 188 publications
(273 reference statements)
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“…The inability of doxorubicin to inhibit E. coli at concentrations up to 40 μ mol l −1 (21·74 mg l −1 ) was previously reported and consistent with the lack of effect we observed up to 64 mg l −1 (Panda et al ). Doxorubicin and fluoroquinolones are both topoisomerases inhibitors, acting on eukaryote type 2A and prokaryote type IIA topoisomerases, respectively (Idowu and Schweizer ). Despite this similar mechanism of action, none of the fluoroquinolone‐resistant S. pseudintermedius isolates had elevated doxorubicin MICs.…”
Section: Resultsmentioning
confidence: 99%
“…The inability of doxorubicin to inhibit E. coli at concentrations up to 40 μ mol l −1 (21·74 mg l −1 ) was previously reported and consistent with the lack of effect we observed up to 64 mg l −1 (Panda et al ). Doxorubicin and fluoroquinolones are both topoisomerases inhibitors, acting on eukaryote type 2A and prokaryote type IIA topoisomerases, respectively (Idowu and Schweizer ). Despite this similar mechanism of action, none of the fluoroquinolone‐resistant S. pseudintermedius isolates had elevated doxorubicin MICs.…”
Section: Resultsmentioning
confidence: 99%
“…Similarly, fluoroquinolones, PPIs, and NSAIDs are reported to have anti‐inflammatory effects that are associated with chemotherapeutic properties. For example, ciprofloxacin, moxifloxacin, levofloxacin, trovafloxacin, and gemifloxacin have all been shown to dose‐dependently inhibit the synthesis of IL‐1 and TNF‐α at therapeutic concentrations in LPS‐stimulated monocytes, while at the same time super‐induce interleukin‐2 (IL‐2) in vitro (Fedorowicz & Sączewski, ; Idowu & Schweizer, ).…”
Section: Discussionmentioning
confidence: 99%
“…which represent the major causes of serious hospitalized infections in the globe . Furthermore, this system can act through being an efflux pump inhibitor and/or being a membrane permeabilizer . Consequently, research groups are interested in development of multi‐component antibiotic systems.…”
Section: Recent Advances Of Quinolone Antibacterial Agentsmentioning
confidence: 99%