The Antiangiogenic Activity of Naturally Occurring and Synthetic Homoisoflavonoids from the Hyacinthaceae (sensu APGII)
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 and Corson, Timothy W. (2019) The Antiangiogenic Activity of Naturally Occurring and Synthetic Homoisoflavonoids from the Hyacinthaceae (sensu APGII) Journal of Natural Products.
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The Antiangiogenic Activity of Naturally-occurring and synthetic Homoisoflavonoids from the Hyacinthaceae (sensu APGII).docx - Accepted version Manuscript Download (7MB) |
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 (GI50 of 2.3 × 10–4 μM).
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Divisions : | Faculty of Engineering and Physical Sciences > Chemistry | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Date : | 2019 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Funders : | University of Surrey, National Institutes of Health | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||
DOI : | 10.1021/acs.jnatprod.8b00989 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Copyright Disclaimer : | Copyright © 2019 American Chemical Society and American Society of Pharmacognosy | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Depositing User : | Clive Harris | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Date Deposited : | 26 Apr 2019 09:59 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Last Modified : | 03 Sep 2020 18:55 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||
URI: | http://epubs.surrey.ac.uk/id/eprint/851698 |
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