Therapeutic Effects of a Novel Phenylphthalimide Analog for Corneal Neovascularization and Retinal Vascular Leakage
Abstract
Neovascularization (NV) and retinal vascular leakage are major causes of impaired vision in ocular diseases. The purpose of this study was to identify novel phenylphthalimide analogs with therapeutic effects on NV and vascular leakage and to explore the mechanism of action. Antiangiogenic activities of novel phenylphthalimide analogs were assessed in vitro by using VEGF ELISA and endothelial cell proliferation assay. Their efficacies on retinal vascular leakage were evaluated using rat models of oxygen-induced retinopathy (OIR) and streptozotocin (STZ)-induced diabetes. The in vivo antiangiogenic activity was evaluated using topical administration in the alkali burn-induced corneal NV model. The expression of VEGF and intercellular adhesion molecule-1 (ICAM-1) were measured using ELISA. Thalidomide and three novel analogs all showed inhibitory effects on endothelial cell proliferation and VEGF expression in vitro. Through intravitreal injection, all of the compounds reduced retinal vascular leakage in the OIR and STZ-induced diabetic models. Among these compounds, (2,6-diisopropylphenyl)-5-amino-1H-isoindole-1,3-dione (DAID) displayed the most potent efficacy and reduced retinal vascular leakage in a dose-dependent manner in bo...Continue Reading
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