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The Antiangiogenic Activity of Naturally Occurring and Synthetic Homoisoflavonoids from the Hyacinthaceae (sensuAPGII)

Authors :
Schwikkard, Sianne
Whitmore, Hannah
Sishtla, Kamakshi
Sulaiman, Rania S.
Shetty, Trupti
Basavarajappa, Halesha D.
Waller, Catherine
Alqahtani, Alaa
Frankemoelle, Lennart
Chapman, Andy
Crouch, Neil
Wetschnig, Wolfgang
Knirsch, Walter
Andriantiana, Jacky
Mas-Claret, Eduard
Langat, Moses K.
Mulholland, Dulcie
Corson, Timothy W.
Source :
Journal of Natural Products; 20240101, Issue: Preprints
Publication Year :
2024

Abstract

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 (GI50of 2.3 × 10–4μM).

Details

Language :
English
ISSN :
01633864 and 15206025
Issue :
Preprints
Database :
Supplemental Index
Journal :
Journal of Natural Products
Publication Type :
Periodical
Accession number :
ejs49726384
Full Text :
https://doi.org/10.1021/acs.jnatprod.8b00989