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J Nat Prod. 2019 Apr 5. doi: 10.1021/acs.jnatprod.8b00989. [Epub ahead of print]

The Antiangiogenic Activity of Naturally Occurring and Synthetic Homoisoflavonoids from the Hyacinthaceae ( sensu APGII).

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School of Life Sciences, Pharmacy and Chemistry , Kingston University , Kingston-upon-Thames , KT1 2EE , U.K.
Natural Products Research Group, Department of Chemistry, Faculty of Engineering and Physical Sciences , University of Surrey , Guildford , GU2 7XH , U.K.
Department of Biochemistry, Faculty of Pharmacy , Cairo University , Cairo , Egypt.
Biodiversity Economy , South African National Biodiversity Institute , P.O. Box 52099, 4007 Berea Road , Durban , South Africa.
School of Chemistry and Physics , University of KwaZulu-Natal , Durban , 4041 , South Africa.
Institute of Biology, NAWI Graz , University of Graz , 8010 Graz , Austria.
Parc Botanique et Zoologique de Tsimbazaza , Rue Fernand Kassanga , Antananarivo 101 , Madagascar.


Excessive blood vessel formation in the eye is implicated in wet age-related macular degeneration, proliferative diabetic retinopathy, neovascular glaucoma, and retinopathy of prematurity, which are major causes of blindness. Small molecule antiangiogenic drugs are strongly needed to supplement existing biologics. Homoisoflavonoids have been previously shown to have potent antiproliferative activities in endothelial cells over other cell types. Moreover, they demonstrated a strong antiangiogenic potential in vitro and in vivo in animal models of ocular neovascularization. Here, we tested the antiangiogenic activity of a group of naturally occurring homoisoflavonoids isolated from the family Hyacinthaceae and related synthetic compounds, chosen for synthesis based on structure-activity relationship observations. Several compounds showed interesting antiproliferative and antiangiogenic activities in vitro on retinal microvascular endothelial cells, a disease-relevant cell type, with the synthetic chromane, 46, showing the best activity (GI50 of 2.3 × 10-4 μM).

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