Besifloxacin is the Hydrochloride salt form of Besifloxacin a broad-spectrum, fourth-generation, 8-chloro-fluoroquinolone antibiotic agent. Besifloxacin Hydrochloride is the commercially available form developed by SSP Co Ltd, Japan. It is active against both Gram-positive and Gram-negative, aerobic and anaerobic bacteria. It is primarily used against bacteria causing bacterial conjunctivitis. Besifloxacin stops the production of pro-inflammatory cytokines in vitro.
| Mechanism of Action | Besifloxacin has a uniquely balanced dual-targeting activity that inhibits both DNA gyrase and topoisomerase IV at nearly equal concentrations. It is associated with a lower incidence of resistance development. Fluoroquinolones stabilize DNA strand breaks created by DNA gyrase and topoisomerase IV by binding to the enzyme-DNA complex generating persistent, covalent enzyme–DNA adducts, inhibiting DNA synthesis. |
| Spectrum | Besifloxacin Hydrochloride displays activity against both Gram-positive and Gram-negative bacteria including ocular bacteria Streptococcus pneumonia, Staphylococcus aureus, S. epidermidis, Haemophilus influenza, Moraxella catarrhalis and Corynebacterium spp. |
| Microbiology Applications | In vitro, Besifloxacin has demonstrated equivalent or superior activity compared with other commonly used topical antibiotics. In vivo, besifloxacin has consistently demonstrated efficacy and safety against bacterial conjunctivitis. Besifloxacin is not marketed in other formulations, ensuring that its exposure is limited to bacterial populations in and around the eye. Basifloxacin is effective against ocular pathogens such as Corynebacterium pseudodiphtheriticum, Moraxella lacunata, Staphylococcus spp. and Streptococcus spp. |
| Eukaryotic Cell Culture Applications | Besifloxacin acts as an anti-inflammatory agent in monocytes in vitro. Cytokine expression in human THP-1 monocytes was stimulated by lipopolysaccharide (LPS). Cytokine expression in human THP-1 monocytes was stimulated by LPS (Zhang and Ward, 2008). |
| Molecular Formula | C19H21ClFN3O3 · HCl |
| References |
Comstock TL, Karpecki PM, Morris TW, Zhang JZ (2010) Besifloxacin: a novel anti-infective for the treatment of bacterial conjunctivitis. Clin Ophthalmol. 2010;4:215-225 Haas W et al (2009) Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria. Antimicrob .Agents Chemother. 53(8):3552-3560 Singh CL, Singh A, Kumar S, Majumdar DK (2014) Besifloxacin the fourth generation fluoroquinolone: A review. JDDT 4(6):39-4 Zhang JZ and Ward KW (2008) Besifloxacin, a novel fluoroquinolone antimicrobial agent, exhibits potent inhibition of pro-inflammatory cytokines in human THP-1 monocytes. J Antimicrob. Chemother. 61(1):111-116 |
