黄连素和氯硝柳胺对眼部蠕形螨的体外杀灭作用。

In vitro killing effect of berberine and niclosamide on ocular Demodex folliculorum.

作者信息

Guo Shujia, Wang Yuqian, Li Jiani, Liu Yuwen, Han Yi, Huang Caihong, Wu Huping, Hu Jiaoyue, Liu Zuguo

机构信息

Xiamen University affiliated Xiamen Eye Center, Fujian Provincial Key Laboratory of Ophthalmology and Visual Science, Fujian Engineering and Research Center of Eye Regenerative Medicine, Eye Institute of Xiamen University, School of Medicine, Xiamen University, Xiamen, Fujian 361005, China.

Department of Ophthalmology, The First Affiliated Hospital of University of South China, Hengyang, Hunan 421001, China.

出版信息

Cont Lens Anterior Eye. 2025 Apr;48(2):102336. doi: 10.1016/j.clae.2024.102336. Epub 2024 Nov 30.

DOI:10.1016/j.clae.2024.102336

PMID:39616005

Abstract

PURPOSE

To explore the in vitro killing effect of water-soluble berberine and lipid-soluble niclosamide against ocular Demodex folliculorum.

METHODS

Demodex with good vigor were collected from patients' eyelashes. These mites were randomly distributed into different groups with 20 mites in each group. Saline, Double Distilled Water (DDW), Polysorbate 80 (TWEEN 80), Polyethylene glycol 300 (PEG 300) and Castor Oil were used to screen solvents and cosolvents. 20 % Tea Tree Oil (TTO) and Anhydrous Ethanol (EtOH) were used as positive controls. 0.2 % Berberine, 0.25 % Niclosamide and 0.5 % Niclosamide, were designated as experimental groups. Following treatment, the analysis of Kaplan-Meier survival curves and survival time of mites and safety of drugs were then performed.

RESULTS

The survival of Demodex in vitro in Saline and DDW, was not significant different. Therefore, DDW, which was more conducive to the dissolution of berberine, was chosen as the solvent for berberine. 0.2 % Berberine significantly inhibited the survival distribution and survival time (P < 0.001) of Demodex in vitro compared with the DDW group. Through the evaluation of several cosolvents, PEG300 had milder effects on Demodex. Hence, the proportion of PEG300 in the niclosamide solvent group was increased to reduce the irritability of the vehicle. Furthermore, niclosamide could significantly inhibit the survival of Demodex compared with the vehicle group, and the effect of 0.5 % Niclosamide was more obvious (P < 0.001), and was better than 20 %TTO (P < 0.001). In addition, after niclosamide administration, Demodex bodies exhibited gradual distortion along with increased transparency and the presence of blurred dark particles compared to those in the vehicle group. Moreover, both drugs showed good subjective tolerability and safety in a mouse model.

CONCLUSION

0.2 % berberine and 0.5 % niclosamide effectively inhibited Demodex survival in vitro, with 0.5 % niclosamide superior to 20 % TTO. These two drugs, with anti-Demodex, anti-bacterial, and anti-inflammatory properties, may offer alternative treatment for Demodex blepharitis.

摘要

目的

探讨水溶性黄连素和脂溶性氯硝柳胺对眼部蠕形螨的体外杀灭作用。

方法

从患者睫毛上采集活力良好的蠕形螨。将这些螨虫随机分成不同组，每组20只。使用生理盐水、双蒸水（DDW）、聚山梨酯80（吐温80）、聚乙二醇300（PEG 300）和蓖麻油筛选溶剂和助溶剂。20%茶树油（TTO）和无水乙醇（EtOH）用作阳性对照。0.2%黄连素、0.25%氯硝柳胺和0.5%氯硝柳胺设为实验组。处理后，分析螨的Kaplan-Meier生存曲线、生存时间及药物安全性。

结果

蠕形螨在生理盐水和双蒸水中的体外存活率无显著差异。因此，选择更有利于黄连素溶解的双蒸水作为黄连素的溶剂。与双蒸水组相比，0.2%黄连素显著抑制蠕形螨的体外生存分布和生存时间（P<0.001）。通过对几种助溶剂的评估，PEG300对蠕形螨的影响较温和。因此，增加氯硝柳胺溶剂组中PEG300的比例以降低赋形剂的刺激性。此外，与赋形剂组相比，氯硝柳胺可显著抑制蠕形螨的生存，0.5%氯硝柳胺的效果更明显（P<0.001），且优于20%TTO（P<0.001）。此外，与赋形剂组相比，给予氯硝柳胺后，蠕形螨体逐渐变形，透明度增加，出现模糊的暗颗粒。此外，两种药物在小鼠模型中均表现出良好的主观耐受性和安全性。