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Inhibition of the VEGFR-2 tyrosine kinase domain by witd Roman chamomile extracts and phenolic compounds

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dc.contributor.authorGuimarães, Rafaela
dc.contributor.authorCalhelha, Ricardo C.
dc.contributor.authorFroufe, Hugo J.C.
dc.contributor.authorAbreu, Rui M.V.
dc.contributor.authorCarvalho, Ana Maria
dc.contributor.authorFerreira, Isabel C.F.R.
dc.contributor.authorQueiroz, Maria João R.P.
dc.date.accessioned2015-11-23T10:51:35Z
dc.date.available2015-11-23T10:51:35Z
dc.date.issued2015
dc.description.abstractAngiogenesis 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 [1]. 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 [2]. Furthermore, it has been reported that drinking of green tea could inhibit VEGF-induced angiogenesis in vivo [3]. 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.pt_PT
dc.identifier.citationGuimarães, 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 Minhopt_PT
dc.identifier.urihttp://hdl.handle.net/10198/12378
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/pt_PT
dc.titleInhibition of the VEGFR-2 tyrosine kinase domain by witd Roman chamomile extracts and phenolic compoundspt_PT
dc.typeconference object
dspace.entity.typePublication
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBD%2F78307%2F2011/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBPD%2F68344%2F2010/PT
oaire.citation.title2nd Symposium on Medicinal Chemistry of University of Minhopt_PT
oaire.fundingStreamSFRH
oaire.fundingStreamSFRH
person.familyNameCalhelha
person.familyNameAbreu
person.familyNameCarvalho
person.familyNameFerreira
person.givenNameRicardo C.
person.givenNameRui M.V.
person.givenNameAna Maria
person.givenNameIsabel C.F.R.
person.identifierID G-7399-2011
person.identifier144781
person.identifier.ciencia-idF313-E3CE-554E
person.identifier.ciencia-id0F19-0DE2-12A2
person.identifier.ciencia-idD31A-35AF-E2A9
person.identifier.ciencia-id9418-CF95-9919
person.identifier.orcid0000-0002-6801-4578
person.identifier.orcid0000-0002-7745-8015
person.identifier.orcid0000-0001-5508-5935
person.identifier.orcid0000-0003-4910-4882
person.identifier.ridJ-2172-2014
person.identifier.ridE-8500-2013
person.identifier.scopus-author-id6507978333
person.identifier.scopus-author-id7003290613
person.identifier.scopus-author-id20336503900
person.identifier.scopus-author-id36868826600
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccesspt_PT
rcaap.typeconferenceObjectpt_PT
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