Anti-inflammatory effects of ozenoxacin, a topical quinolone antimicrobial agent

Abstract

Ozenoxacin is a topical quinolone showing potent antimicrobial activities against Gram-negative and Gram-positive bacteria and is widely used for the treatment of inflammatory acne. However, the anti-inflammatory activities of ozenoxacin have not been examined so far. In the present study, we investigated the in vitro and in vivo anti-inflammatory effects of ozenoxacin. The production of interleukin (IL)-6 and IL-8 by human epidermal keratinocytes stimulated by heat-killed Cutibacterium acnes was significantly inhibited by ozenoxacin at concentrations from 1 to 30 μg ml −1. Likewise, the production of IL-6, IL-8, and tumor necrosis factor alpha by stimulated THP-1 cells, a human monocyte cell line, was inhibited by ozenoxacin at concentrations from 1 to 30 μg ml −1. The production of IL-1β by THP-1 was also inhibited by ozenoxacin at the concentration of 30 μg ml −1. Phosphorylation of the mitogen-activated protein kinases and degradation of IκB-α, an inhibitory factor of NF-κB in keratinocytes and THP-1 cells, was increased by stimulation with heat-killed C. acnes. Of these activated intracellular pathways, the p38 phosphorylation pathway was remarkably reduced by ozenoxacin in both keratinocytes and THP-1 cells. In addition, the application of 2% ozenoxacin suppressed the increase in the ear thickness of rats induced by an intracutaneous injection of heat-killed C. acnes. These findings suggest that ozenoxacin possesses an antiinflammatory activity, which may contribute to its therapeutic effects on inflammatory acne.

Updated Treatment for Acne: Targeted Therapy Based on Pathogenesis

“…In addition, BPO is comedolytic. Recently, BPO has been shown to inhibit the production of C. acnes biofilms [ 47 ]. Antimicrobials have bactericidal or bacteriostatic effects on C. acnes.…”

Inhibitory Effects of a Sargassum miyabei Yendo on Cutibacterium acnes-Induced Skin Inflammation

“…Its pathogenesis is poorly understood, but inflammation has been found to be a major contributor [1]. Cutibacterium acnes (C. acnes), a gram-positive anaerobic bacterium, triggers the inflammatory response of acne vulgaris by enhancing the secretion of interleukin-1 beta (IL-1β), IL-6, IL-8, and tumor necrosis factor-alpha (TNF-α) by monocytic cells, because of which inflammatory lesions eventually develop [2,3]. Keratinocytes are the first-line responders of the skin's immune system and, along with sebocytes, produce a variety of cytokines and chemokines [4].…”

Mitigative Effects of Topical Norfloxacin on an Imiquimod-Induced Murine Model of Psoriasis

“…168 Besides, the pair of additional topically applied quinolones, nadifloxacin and ozenoxacin, alleviated ear epidermal thickening, redness, and inflammation. 55,169 It has been established that drugs belonging to the fluoroquinolone family, could potentially have many biological activities beyond those expected of classic antibiotics. 37,170 Lomefloxacin fluoroquinolone dramatically decreased the expression of pro-inflammatory activation markers in the JAK/STAT3, p38 MAPK, NF-κB, and PI3K-AKT cascades, which were persistently engaged in autoimmune and autoinflammatory conditions.…”