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一种新的眼科药物制剂,局部苏糖赖氨酸,可增强干燥应激介导的干眼症中的眼粘液分泌。

A New Ophthalmic Pharmaceutical Formulation, Topical Sulglycotide, Enhances the Ocular Mucin Secretion in Desiccation Stress-Mediated Dry Eye Disease.

机构信息

T2B Infrastructure Center for Ocular Diseases, Inje University Busan Paik Hospital, Busanjin-gu, Busan, Republic of Korea.

College of Pharmacy, Ajou University, Yeongtong-gu, Suwon City, Republic of Korea.

出版信息

Invest Ophthalmol Vis Sci. 2019 Mar 1;60(4):1076-1087. doi: 10.1167/iovs.18-24935.

DOI:10.1167/iovs.18-24935
PMID:30901389
Abstract

PURPOSE

The aim of this study was the investigation of the effect of sulglycotide (SOS), a polysulfated glycopeptide derived from porcine duodenal mucin, for the treatment of dry eye disease.

METHODS

NOD.B10.H2b mice were exposed to an air draft for 10 days, and, simultaneously, scopolamine hydrobromide was injected subcutaneously. The mice were randomly divided into nine groups as follows: four kinds of SOS formulations and three kinds of commercial medicine. After 10 days of treatment, we estimated the effect of treatment on tear production, epithelium stabilization, mucin secretion, and inflammation.

RESULTS

The desiccation stress significantly decreased tear production and corneal epithelium stabilization, as well as markedly decreased the numbers of goblet cells and mucin-stained cells in conjunctiva. However, the topical 4% SOS eye drops markedly increased tear production and corneal stabilization, which recovered to baseline levels. In addition, topical 4% SOS significantly induced an increase in the numbers of goblet cells and the expression of membrane-associated mucins including MUC1, MUC4, and MUC16, as well as the gel-forming mucin, MUC5AC. Furthermore, SOS formulations provided anti-inflammatory improvement in a dose-dependent manner.

CONCLUSIONS

In summary, we suggest that a new ophthalmic pharmaceutical formulation, topical sulglycotide, enhances the ocular mucin secretion in dry eye disease and can be used as a new ophthalmic pharmaceutical material to treat dry eye disease.

摘要

目的

本研究旨在探讨源自猪十二指肠黏蛋白的多糖硫酸化糖肽(SOS)治疗干眼症的效果。

方法

NOD.B10.H2b 小鼠暴露于气流中 10 天,同时皮下注射氢溴酸东莨菪碱。将小鼠随机分为九组:四种 SOS 制剂和三种商业药物。治疗 10 天后,评估治疗对泪液产生、上皮稳定、黏蛋白分泌和炎症的影响。

结果

干燥应激显著降低泪液产生和角膜上皮稳定,同时显著减少结膜中杯状细胞和黏蛋白染色细胞的数量。然而,局部使用 4%SOS 眼药水可显著增加泪液产生和角膜稳定,使其恢复到基线水平。此外,局部使用 4%SOS 显著诱导杯状细胞数量增加,以及包括 MUC1、MUC4 和 MUC16 在内的膜相关黏蛋白和凝胶形成黏蛋白 MUC5AC 的表达增加。此外,SOS 制剂以剂量依赖的方式提供抗炎改善。

结论

总之,我们建议一种新的眼科药物制剂,局部使用多糖硫酸化糖肽可增强干眼症中的眼黏蛋白分泌,可作为治疗干眼症的新型眼科药物材料。

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