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|Título:||Inhibition of the VEGFR-2 tyrosine kinase domain by witd Roman chamomile extracts and phenolic compounds|
Calhelha, Ricardo C.
Froufe, Hugo J.C.
Abreu, Rui M.V.
Carvalho, Ana Maria
Ferreira, Isabel C.F.R.
Queiroz, Maria João R.P.
|Citação:||Guimarães, Rafaela; Calhelha, Ricardo C.; Froufe, Hugo J.C.; Abreu, Rui M.V.; Carvalho, Ana Maria; Ferreira, Isabel C.F.R.; Queiroz, Maria João R.P. (2015) - Inhibition of the VEGFR-2 tyrosine kinase domain by witd Roman chamomile extracts and phenolic compounds. In 2nd Symposium on Medicinal Chemistry of University of Minho|
|Resumo:||Angiogenesis results from new blood vessels growing excessively (e. g. câncer). The Vascular Endothelial Growth Factor (VEGF) is secreted by the tumor cells and plays a crucial role in angiogenesis; low oxygen tension dramatically induces the expression of this major angiogenic factor that when linked to the transmembrane tyrosine kinase receptor VEGFR-2, which is present in endothelial cells, signalizes for the proliferation of these cells towards the tumor. Treatments using small molecules with anti-tyrosine kinase activity (e. g., sorafenib) can block angiogenic signalling, reduce blood tumoral irrigation, and improve chemotherapy distribution . Some studies recognized phenolic compounds as chemopreventive agents, especially flavonoids. Other plant-derived anticancer drugs (e. g. Taxol) proved to be anti-angiogenic. In traditional Chinese medicine, many herbs are used in the treatment of angiogenic diseases such as chronic wounds and rheumatoid arthritis . Furthermore, it has been reported that drinking of green tea could inhibit VEGF-induced angiogenesis in vivo . In the present work, the anti-angiogenic activity of Roman chamomile (Chamaemelum nobile L.) extracts (methanolic extract and infusion) and main phenolic compounds (apigenin, apigenin-7-O-glucoside, caffeic acid, chlorogenic acid, luteolin, luteolin-7-O-glucoside) was evaluated through an enzymatic assay using the VEGFR-2 tyrosine kinase domain. To better understand the inhibition phosphorylation mechanism of the tyrosine kinase receptor by luteolin, apigenin and apigenin-7- 0-glucoside, docking studies were performed. The methanolic extract showed higher phosphorylation inhibition than the infusion (IC50 values of 269 and 301 μg/mL, respectively). Regarding phenolic compounds, luteolin (IC50 2.10 μM) and apigenin (IC50 4.78 μM) were the most potent in inhibiting VEGFR-2 phosphorylation, leading us to believe that these compounds are involved in the anti-angiogenic activity revealed by the methanolic extract.|
|Aparece nas colecções:||CIMO - Resumos em Proceedings Não Indexados à WoS/Scopus|
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