Senju Pharmaceutical Co., Ltd., 6-4-3 Minatojima-Minamimachi, Chuo-Ku, Kobe, Hyogo, 650-0047, Japan.
BMC Ophthalmol. 2020 Mar 6;20(1):89. doi: 10.1186/s12886-020-01358-4.
We aimed to demonstrate the contribution of anti-inflammatory and anti-virulence effects of azithromycin (AZM) in ocular surface infection treatment.
Staphylococcus aureus was injected into the corneal stroma of rabbits to induce keratitis. AZM at concentrations of 0.01, 0.1, and 1% was instilled into the eye twice daily. The eyes were examined using a slit lamp and scored. The viable bacteria in the cornea were counted at 48 h post infection. To evaluate the anti-inflammatory efficacy of AZM, S. aureus culture supernatant-induced anterior ocular inflammation in rabbit was examined using a slit lamp and scored. To evaluate the inhibitory effect of AZM on bacterial toxin production, S. aureus was cultured with AZM and hemolytic reaction in the culture supernatant was determined.
In the bacterial keratitis model, AZM dose-dependently inhibited the increase in the clinical score. The viable bacterial count in the cornea treated with 1% AZM significantly decreased compared with that of the vehicle, whereas bacterial count in 0.01 and 0.1% AZM-treated corneas was similar to that of the vehicle. In the anterior ocular inflammation model, 0.1 and 1% AZM inhibited the increase in the clinical score. AZM inhibited hemolytic reaction at concentrations that did not inhibit bacterial growth.
The results demonstrated that AZM has not only anti-bacterial, but also anti-inflammatory effects, and inhibits bacterial toxin production leading to ocular surface damage in bacterial infection. Thus, the therapeutic effect of AZM against ocular infections is expected to be higher than that which could be assumed if it only had anti-bacterial activity.
我们旨在展示阿奇霉素（AZM）的抗炎和抗毒效应对眼表感染治疗的贡献。
将金黄色葡萄球菌注入兔角膜基质中以诱导角膜炎。将 0.01%、0.1%和 1%的 AZM 滴入眼睛，每天两次。使用裂隙灯检查并评分。感染后 48 小时计算角膜中的活菌数。为了评估 AZM 的抗炎疗效，使用裂隙灯检查 S. aureus 培养上清液诱导的兔眼前部炎症并评分。为了评估 AZM 抑制细菌毒素产生的抑制作用，用 AZM 培养 S. aureus，并测定培养上清液中的溶血反应。
在细菌性角膜炎模型中，AZM 呈剂量依赖性抑制临床评分的增加。用 1% AZM 处理的角膜中的活菌数与载体相比显著减少，而用 0.01%和 0.1% AZM 处理的角膜中的活菌数与载体相似。在眼前部炎症模型中，0.1%和 1% AZM 抑制临床评分的增加。AZM 在不抑制细菌生长的浓度下抑制溶血反应。
结果表明，AZM 不仅具有抗菌作用，而且具有抗炎作用，并抑制导致细菌感染眼表损伤的细菌毒素产生。因此，AZM 治疗眼部感染的疗效预计将高于仅具有抗菌活性时的疗效。
