Anti-VEGF Effect of Bioactive Indolic Compounds and Hydroxytyrosol Metabolites
Angiogenesis is a key process involved in both cancer and cardiovascular diseases, the vascular endothelial growth factor (VEGF) and its VEGF receptor-2 (VEGFR-2) being the main triggers. The aim of this study was to determine the molecular mechanism underlying the potent inhibition of VEGF signalin...
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ftpubmed:oai:pubmedcentral.nih.gov:8871452 2023-05-15T16:55:47+02:00 Anti-VEGF Effect of Bioactive Indolic Compounds and Hydroxytyrosol Metabolites Gallardo-Fernández, Marta Cerezo, Ana B. Hornedo-Ortega, Ruth Troncoso, Ana M. Garcia-Parrilla, M. Carmen 2022-02-11 http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8871452/ https://doi.org/10.3390/foods11040526 en eng MDPI http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8871452/ http://dx.doi.org/10.3390/foods11040526 © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). CC-BY Foods Article Text 2022 ftpubmed https://doi.org/10.3390/foods11040526 2022-02-27T01:58:27Z Angiogenesis is a key process involved in both cancer and cardiovascular diseases, the vascular endothelial growth factor (VEGF) and its VEGF receptor-2 (VEGFR-2) being the main triggers. The aim of this study was to determine the molecular mechanism underlying the potent inhibition of VEGF signaling by hydroxytyrosol (HT) metabolites and indolic compounds and establish a relation between their structure and bioactivity. Experiments involved the evaluation of their potential to inhibit VEGF on human umbilical vein endothelial cells (HUVECs) by ELISA assay and their subsequent effect on the downstream signaling pathway (PLCγ1, Akt, and endothelial nitric oxide synthetase (eNOS)) by Western blot. Respectively, 3,4-dihydroxyphenylacetaldehyde (DOPAL) (100 µM) and indole pyruvic acid (IPy) (1 mM) were capable of inhibiting VEGFR-2 activation with an IC(50) value of 119 µM and 1.037 mM. The anti-angiogenic effect of DOPAL and IPy is mediated via PLCγ1. Additionally, DOPAL significantly increases eNOS phosphorylation, while IPy maintained it. These data provide for the first time evidence of the anti-angiogenic effect of DOPAL and IPy for future use as potential bioactive food ingredients. Text IPY PubMed Central (PMC) Foods 11 4 526 |
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Article Gallardo-Fernández, Marta Cerezo, Ana B. Hornedo-Ortega, Ruth Troncoso, Ana M. Garcia-Parrilla, M. Carmen Anti-VEGF Effect of Bioactive Indolic Compounds and Hydroxytyrosol Metabolites |
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Angiogenesis is a key process involved in both cancer and cardiovascular diseases, the vascular endothelial growth factor (VEGF) and its VEGF receptor-2 (VEGFR-2) being the main triggers. The aim of this study was to determine the molecular mechanism underlying the potent inhibition of VEGF signaling by hydroxytyrosol (HT) metabolites and indolic compounds and establish a relation between their structure and bioactivity. Experiments involved the evaluation of their potential to inhibit VEGF on human umbilical vein endothelial cells (HUVECs) by ELISA assay and their subsequent effect on the downstream signaling pathway (PLCγ1, Akt, and endothelial nitric oxide synthetase (eNOS)) by Western blot. Respectively, 3,4-dihydroxyphenylacetaldehyde (DOPAL) (100 µM) and indole pyruvic acid (IPy) (1 mM) were capable of inhibiting VEGFR-2 activation with an IC(50) value of 119 µM and 1.037 mM. The anti-angiogenic effect of DOPAL and IPy is mediated via PLCγ1. Additionally, DOPAL significantly increases eNOS phosphorylation, while IPy maintained it. These data provide for the first time evidence of the anti-angiogenic effect of DOPAL and IPy for future use as potential bioactive food ingredients. |
format |
Text |
author |
Gallardo-Fernández, Marta Cerezo, Ana B. Hornedo-Ortega, Ruth Troncoso, Ana M. Garcia-Parrilla, M. Carmen |
author_facet |
Gallardo-Fernández, Marta Cerezo, Ana B. Hornedo-Ortega, Ruth Troncoso, Ana M. Garcia-Parrilla, M. Carmen |
author_sort |
Gallardo-Fernández, Marta |
title |
Anti-VEGF Effect of Bioactive Indolic Compounds and Hydroxytyrosol Metabolites |
title_short |
Anti-VEGF Effect of Bioactive Indolic Compounds and Hydroxytyrosol Metabolites |
title_full |
Anti-VEGF Effect of Bioactive Indolic Compounds and Hydroxytyrosol Metabolites |
title_fullStr |
Anti-VEGF Effect of Bioactive Indolic Compounds and Hydroxytyrosol Metabolites |
title_full_unstemmed |
Anti-VEGF Effect of Bioactive Indolic Compounds and Hydroxytyrosol Metabolites |
title_sort |
anti-vegf effect of bioactive indolic compounds and hydroxytyrosol metabolites |
publisher |
MDPI |
publishDate |
2022 |
url |
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8871452/ https://doi.org/10.3390/foods11040526 |
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IPY |
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IPY |
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Foods |
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8871452/ http://dx.doi.org/10.3390/foods11040526 |
op_rights |
© 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
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CC-BY |
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https://doi.org/10.3390/foods11040526 |
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Foods |
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11 |
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526 |
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1766046836656701440 |