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.
Korean Medicine Based Herbal Drug Development Group, Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon, South Korea.
Yun Mi
YM
Lee
Korean Medicine Based Herbal Drug Development Group, Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon, South Korea.
Junghyun
J
Kim
Korean Medicine Based Herbal Drug Development Group, Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon, South Korea.
Chan-Sik
CS
Kim
Korean Medicine Based Herbal Drug Development Group, Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon, South Korea.
Kyuhyung
K
Jo
International Ginseng & Herb Research Institute, Geumsan, South Korea.
Nam Hee
NH
Yoo
Korean Medicine Based Herbal Drug Development Group, Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon, South Korea.
Eunjin
E
Sohn
Korean Medicine Based Herbal Drug Development Group, Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon, South Korea. Electronic address: jskim@kiom.re.kr.
Jin Sook
JS
Kim
D020533:Angiogenesis Inhibitors / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D001813:Blood-Retinal Barrier / Q000187:drug effects / Q000378:metabolism; D002199:Capillary Permeability / Q000187:drug effects / Q000502:physiology; D003930:Diabetic Retinopathy / Q000188:drug therapy / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D017127:Glycation End Products, Advanced / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D064209:Phytochemicals / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D018515:Plant Leaves; D018547:Plant Stems; D051381:Rats; D017207:Rats, Sprague-Dawley; D027824:Rosaceae; D042461:Vascular Endothelial Growth Factor A / Q000378:metabolism
D020533:Angiogenesis Inhibitors; D017127:Glycation End Products, Advanced; D064209:Phytochemicals; D010936:Plant Extracts; D042461:Vascular Endothelial Growth Factor A
5′-Methoxybiphenyl-3,4,3′-triol; Advanced glycation end products; Blood–retinal barrier; Oxygen-induced retinopathy; Vascular endothelial growth factor