title: Wild Roman chamomile extracts and phenolic compounds: enzymatic assays and molecular modelling studies with VEGFR-2 tyrosine kinase.
abstract: Angiogenesis is a process by which new blood vessels are formed from the pre-existing vasculature, and it is a key process that leads to tumour development. Some studies have recognized phenolic compounds as chemopreventive agents; flavonoids, in particular, seem to suppress the growth of tumor cells modifying the cell cycle. Herein, the antiangiogenic activity of Roman chamomile (Chamaemelum nobile L.) extracts (methanolic extract and infusion) and the main phenolic compounds present (apigenin, apigenin-7-O-glucoside, caffeic acid, chlorogenic acid, luteolin, and luteolin-7-O-glucoside) was evaluated through enzymatic assays using the tyrosine kinase intracellular domain of the Vascular Endothelium Growth Factor Receptor-2 (VEGFR-2), which is a transmembrane receptor expressed fundamentally in endothelial cells involved in angiogenesis, and molecular modelling studies. The methanolic extract showed a lower IC50 value (concentration that provided 50% of VEGFR-2 inhibition) than the infusion, 269 and 301 μg mL(-1), respectively. Regarding phenolic compounds, luteolin and apigenin showed the highest capacity to inhibit the phosphorylation of VEGFR-2, leading us to believe that these compounds are involved in the activity revealed by the methanolic extract.
authors.affiliation: Centro de Investigação de Montanha, Escola Superior Agrária, Campus de Santa Apolónia, apartado 1172, 5301-854 Bragança, Portugal. iferreira@ipb.pt and Centro de Química da Universidade do Minho, Campus de Gualtar, 4710-057 Braga, Portugal.
authors.forename: Rafaela
authors.initials: R
authors.lastname: Guimarães
authors.affiliation: Centro de Investigação de Montanha, Escola Superior Agrária, Campus de Santa Apolónia, apartado 1172, 5301-854 Bragança, Portugal. iferreira@ipb.pt and Centro de Química da Universidade do Minho, Campus de Gualtar, 4710-057 Braga, Portugal.
authors.forename: Ricardo C
authors.initials: RC
authors.lastname: Calhelha
authors.affiliation: Centro de Investigação de Montanha, Escola Superior Agrária, Campus de Santa Apolónia, apartado 1172, 5301-854 Bragança, Portugal. iferreira@ipb.pt.
authors.forename: Hugo J C
authors.initials: HJ
authors.lastname: Froufe
authors.affiliation: Centro de Investigação de Montanha, Escola Superior Agrária, Campus de Santa Apolónia, apartado 1172, 5301-854 Bragança, Portugal. iferreira@ipb.pt.
authors.forename: Rui M V
authors.initials: RM
authors.lastname: Abreu
authors.affiliation: Centro de Investigação de Montanha, Escola Superior Agrária, Campus de Santa Apolónia, apartado 1172, 5301-854 Bragança, Portugal. iferreira@ipb.pt.
authors.forename: Ana Maria
authors.initials: AM
authors.lastname: Carvalho
authors.affiliation: Centro de Química da Universidade do Minho, Campus de Gualtar, 4710-057 Braga, Portugal.
authors.forename: Maria João R P
authors.initials: MJ
authors.lastname: Queiroz
authors.affiliation: Centro de Investigação de Montanha, Escola Superior Agrária, Campus de Santa Apolónia, apartado 1172, 5301-854 Bragança, Portugal. iferreira@ipb.pt.
authors.forename: Isabel C F R
authors.initials: IC
authors.lastname: Ferreira
mesh_terms: D047310:Apigenin / Q000494:pharmacology; D020843:Chamomile / Q000737:chemistry*; D005419:Flavonoids / Q000494:pharmacology; D006801:Humans; D047311:Luteolin / Q000494:pharmacology; D000432:Methanol; D008958:Models, Molecular; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D009389:Neovascularization, Pathologic / Q000517:prevention & control; D010636:Phenols / Q000494:pharmacology; D010766:Phosphorylation / Q000187:drug effects; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors*
chemical_list: D005419:Flavonoids; D010636:Phenols; D010936:Plant Extracts; D047310:Apigenin; D011505:Protein-Tyrosine Kinases; D040301:Vascular Endothelial Growth Factor Receptor-2; D047311:Luteolin; D000432:Methanol