Abstract
As vosaroxin as a fluoroquinolone (FQ) had anticancer effectiveness; this study aimed to screen new lipophilic FQs for their dual antimicrobial-antiproliferative activities. Using sulforhodamine B assay; 36 lipophilic FQs have been screened for antimicrobial propensities against S. aureus, E. coli, and C. albicans vs. the respective references ciprofloxacin and fluconazole. They were also explored against a battery of cancer cell lines. Normal periodontal ligament fibroblasts (PDL) were tested for safety examination in comparison to the cisplatin. Reduced FQ compound 4g (R-2, 4-DMeOACA) highly scored nanomolar potency with MIC value of 0.004 µM against gram-positive bacteria. The highest activity of the 36 lipophilic FQs was noted on Leukaemia K562, cervical HELA and pancreatic PANC-1 cancer cell lines with respective IC50 value of 0.005 µM for compound R-4-BuACA (4e), 0.40 µM with CHxCA (7a) and 0.11 µM for R-4-HxACA (4f). Tested FQs exhibited cytotoxicity in A549 lung cancer, MCF-7 and T47D breast cancer cell lines. The reduced 4e and 4f compounds have shown nanomolar inhibition against K562 (as of 4e), PANC-1 and MCF-7 (as of 4f) with IC50 values of 0.005, 0.11 and 0.30 µM, respectively. Succinctly FQs’ dual gram-positive antibacterial-antineoplastic capacities expand on of drug design scaffolds in lead generation.
Highlights
The fight against cancer is an unbreakable continuous challenge
Using sulforhodamine B assay; 36 lipophilic FQs have been screened for antimicrobial propensities against S. aureus, E. coli, and C. albicans vs. the respective references ciprofloxacin and fluconazole
The anti-proliferative activity was tested against 7 different cancer cell lines A549, A374.S2, MCF7, HELA, K562, PANC 1, and T47D
Summary
The fight against cancer is an unbreakable continuous challenge. Cancer statistics are overwhelming and new cases are arising each year. Several reports have mentioned that FQs have anti-proliferative activity in certain types of human cancer cell lines such as moxifloxacin and ciprofloxacin and gemifloxacin (Kan et al, 2013). Vosaroxin and all anticancer quinolone do inhibit eukaryotic type II topoisomerases (A2) that is highly expressed in many eukaryotic proliferating cells (Abbas et al, 2015; Hotinski et al, 2015). This anticancer FQ drug does justify and rationalize our aims toward antineoplastic FQs. Additional rationalization for this research comes from the fact that FQs class was in general regarded as quite safe overall, without any significant cardio toxicity (Owens and Ambrose, 2005). Quinolones are formulated as both oral and parenteral preparations
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