Anti-glycation and anti-angiogenic activities of 5′-methoxybiphenyl-3,4,3′-triol, a novel phytochemical component of Osteomeles schwerinae

Advanced glycation end products (AGEs) are involved in the development of diabetic complications such as diabetic retinopathy. 5′-methoxybiphenyl-3,4,3′-triol (referred to as K24) was isolated using bioactivity-guided fractionation of Osteomeles schwerinae C. K. Schneid. and identified as a potent AGE inhibitor. To identify the protective effect of K24 on disruption of the blood–retinal barrier, AGE-RSA was intravitreally injected into rat eyes. K24 had an inhibitory effect on AGE-RSA-induced retinal vascular leakage by suppressing the expression of vascular endothelial growth factor (VEGF) and decreasing the loss of occludin. In addition, we examined whether K24 has a preventive effect against retinal pathogenic angiogenesis in an oxygen-induced retinopathy (OIR) mouse model. K24 significantly reduced the retinal non-perfused area and neovascular tufts in the OIR mice. These data indicate that K24 could serve as an innovative pharmaceutical agent to prevent blood–retinal barrier breakage and retinal pathogenic angiogenesis through an anti-VEGF mechanism.