Anti-VEGF Effect of Bioactive Indolic Compounds and Hydroxytyrosol Metabolites
|Author/s||Gallardo Fernández, Marta
Cerezo López, Ana Belén
Hornedo Ortega, Ruth
Troncoso González, Ana María
García Parrilla, María del Carmen
|Department||Universidad de Sevilla. Departamento de Nutrición y Bromatología, Toxicología y Medicina Legal|
|Abstract||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 ...
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 IC50 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.
|Funding agencies||Ministerio de Ciencia e Innovación (MICIN). España
Junta de Andalucía
|Citation||Gallardo Fernández, M., Cerezo López, A.B., Hornedo Ortega, R., Troncoso González, A.M. y García Parrilla, M.d.C. (2022). Anti-VEGF Effect of Bioactive Indolic Compounds and Hydroxytyrosol Metabolites. Foods, 11 (4), 526.|