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利卡灵 A 作为一种新型治疗炎症性眼病的药物。

Licarin A as a Novel Drug for Inflammatory Eye Diseases.

机构信息

Faculty of Pharmacy, Federal University of Minas Gerais, Belo Horizonte, Brazil.

Faculty of Medicine, Federal University of Minas Gerais, Belo Horizonte, Brazil.

出版信息

J Ocul Pharmacol Ther. 2021 Jun;37(5):290-300. doi: 10.1089/jop.2020.0129. Epub 2021 Mar 23.

Abstract

This study investigated the safety and therapeutic efficacy of licarin A (LCA) in the treatment of intraocular inflammation. safety of LCA in retinal pigmented epithelial cells (ARPE-19) and human embryonic stem cell derived-retinal pigmented epithelial cells (hES-RPE) was evaluated using CellTiter-Blue kit. The chorioallantoic membrane (CAM) assay was used to investigate LCA safety and antiangiogenic activity. safety of intravitreal LCA was accomplished by clinical examination (including assessment of intraocular pressure), electroretinography (ERG), and histopathology. Uveitis was induced in rats by subcutaneous and intravitreal injection of (BCG) antigen of . Intraocular inflammation was graded by slit-lamp and fundus examination, ERG, and histopathology. LCA was safe to cells and to the CAM at concentration below 12.0 μM. LCA significantly reduced the percentage of blood vessels in the CAM. Retinal safety and anti-inflammatory efficacy of intravitreal injection of LCA 6.0 μM were confirmed through clinical, functional, and histopathological evaluation. Significant reduction of inflammatory cytokines (tumor necrosis factor-α and interleukin-6) was also found, when compared to untreated animals. The results suggest that LCA is a potential new drug for the treatment of inflammatory eye disease.

摘要

这项研究调查了利卡灵 A(LCA)治疗眼内炎症的安全性和疗效。使用 CellTiter-Blue 试剂盒评估了 LCA 在视网膜色素上皮细胞(ARPE-19)和人胚胎干细胞衍生的视网膜色素上皮细胞(hES-RPE)中的安全性。用鸡胚尿囊膜(CAM)试验研究 LCA 的安全性和抗血管生成活性。通过临床检查(包括眼压评估)、视网膜电图(ERG)和组织病理学来评估玻璃体内 LCA 的安全性。通过皮下和玻璃体内注射牛结核分枝杆菌(BCG)抗原诱导大鼠葡萄膜炎。通过裂隙灯和眼底检查、ERG 和组织病理学评估眼内炎症程度。LCA 在浓度低于 12.0 μM 时对细胞和 CAM 是安全的。LCA 显著减少了 CAM 中的血管百分比。通过临床、功能和组织病理学评估,证实玻璃体内注射 6.0 μM 的 LCA 具有视网膜安全性和抗炎疗效。与未治疗的动物相比,还发现炎症细胞因子(肿瘤坏死因子-α和白细胞介素-6)显著减少。结果表明,LCA 是一种治疗炎症性眼病的潜在新药。

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