The Antiangiogenic Activity of Naturally Occurring and Synthetic Homoisoflavonoids from the Hyacinthaceae (sensu APGII)
Autor: | Andy M. Chapman, Wolfgang Wetschnig, Halesha D. Basavarajappa, Sianne Schwikkard, Neil R. Crouch, Catherine Waller, Moses K. Langat, Timothy W. Corson, Dulcie A. Mulholland, Trupti Shetty, Lennart Frankemoelle, Alaa Alqahtani, Rania S. Sulaiman, Walter Knirsch, Eduard Mas-Claret, Jacky Andriantiana, Hannah Whitmore, Kamakshi Sishtla |
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Rok vydání: | 2019 |
Předmět: |
Cell type
genetic structures Pharmaceutical Science Angiogenesis Inhibitors Retinal Neovascularization Pharmacology chemistry Plant Roots 01 natural sciences Article Analytical Chemistry Structure-Activity Relationship chemistry.chemical_compound In vivo Drug Discovery Human Umbilical Vein Endothelial Cells medicine Humans Structure–activity relationship Asparagaceae Cell Proliferation Flavonoids Molecular Structure Plant Extracts 010405 organic chemistry Chemistry Organic Chemistry Endothelial Cells Diabetic retinopathy Macular degeneration medicine.disease eye diseases In vitro 0104 chemical sciences 010404 medicinal & biomolecular chemistry medicine.anatomical_structure Complementary and alternative medicine Molecular Medicine Chromane sense organs Blood vessel |
Zdroj: | J Nat Prod |
ISSN: | 1520-6025 0163-3864 |
Popis: | 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). |
Databáze: | OpenAIRE |
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