Apigenin Inhibits Laser-Induced Choroidal Neovascularization and Regulates Endothelial Cell Function

Abstract

PURPOSE: The aim of this study is to evaluate the effect of apigenin on laser-induced experimental choroidal neovascularization (CNV) rat model and endothelial cell proliferation and migration. METHODS: Male Brown Norway rats were anesthetized to receive Nd:YAG laser to break the Bruch's membrane. Apigenin at 5, 15, or 30 mg/kg was given once-daily through intraperitoneal injection after laser treatment for 4 weeks. The development of CNV was determined by fluorescein angiography performed on weeks 2 and 4. Endothelial cell function was evaluated with proliferation assay and migration assay. RESULTS: The intensity of fluorescein leakage from the photocoagulated lesions decreased significantly, compared to the control group, following apigenin treatment. Four (4) weeks after administration, apigenin, at 15 and 30 mg/kg, inhibited CNV development to 84.5% and 83.6% of the control group, respectively (P<0.05). Apigenin also interfered with the endothelial cells' proliferation and migration. At 3 and 10 microg/ml, apigenin inhibited the growth of human umbilical vein endothelial cells (HUVEC) to 54% and 46% of the control group, respectively (P<0.01); inhibited the growth of choroidal endothelial cells to 47% and 8% of the control group, respectively (P<0.01); and inhibited HUVEC migration over 50%, compared with the control (P<0.01). CONCLUSIONS: Apigenin exerts an inhibitory effect on choroidal angiogenesis in vitro and in vivo. It should be further evaluated for its potential as a novel therapy for CNV.