Fujihara Tsutomu, Murakami Tadahiro, Nagano Takashi, Nakamura Masatsugu, Nakata Katsuhiko
Santen Pharmaceutical Co, Ltd Ophthalmic Division, Nara, Japan.
J Ocul Pharmacol Ther. 2002 Aug;18(4):363-70. doi: 10.1089/10807680260218524.
P2Y2 receptor agonists, like UTP and ATP, stimulate mucin secretion from goblet cells in vitro. Therefore, mucin stimulants could be good candidates for the treatment of dry eye syndrome because mucin increases the tear film stability and protects against desiccation of ocular surface. INS365 is a more stable P2Y2 receptor agonist than UTP. In the present study, we evaluated, in normal rabbit eyes, its effectiveness to release mucin from goblet cells and to protect the corneal damage induced by desiccation. For mucin secretion, impression cytology was performed following the instillation of INS365 solution or saline into the conjunctival sac. The specimens were stained with periodic acid and Schiff (PAS) reagent, and then the staining area was calculated using computer software. INS365 dose-dependently decreased the PAS staining area of conjunctival goblet cells from 2 to 15 min post-application. Furthermore, we utilized the rabbit short-term dry eye model to evaluate if INS365 eyedrops could protect against any of the damage produced by blockage of blinking with ocular speculum. INS365 significantly suppressed corneal damage at concentrations of more than 0.1% w/v. These results suggest that this P2Y2 agonist is a good candidate for the treatment of dry eye disease.
P2Y2受体激动剂,如尿苷三磷酸(UTP)和三磷酸腺苷(ATP),在体外可刺激杯状细胞分泌黏蛋白。因此,黏蛋白刺激剂有望成为治疗干眼症的理想药物,因为黏蛋白可增强泪膜稳定性并防止眼表干燥。INS365是一种比UTP更稳定的P2Y2受体激动剂。在本研究中,我们评估了在正常兔眼中,它从杯状细胞释放黏蛋白以及保护干燥诱导的角膜损伤的效果。对于黏蛋白分泌,在结膜囊中滴入INS365溶液或生理盐水后进行印迹细胞学检查。标本用高碘酸和席夫(PAS)试剂染色,然后使用计算机软件计算染色面积。应用后2至15分钟,INS365剂量依赖性地减少了结膜杯状细胞的PAS染色面积。此外,我们利用兔短期干眼模型评估INS365滴眼液是否能预防开睑器阻断眨眼所产生的任何损伤。浓度高于0.1% w/v时,INS365可显著抑制角膜损伤。这些结果表明,这种P2Y2激动剂有望成为治疗干眼病的理想药物。