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https://hdl.handle.net/1822/48095
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Campo DC | Valor | Idioma |
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dc.contributor.author | Pereira, David M. | por |
dc.contributor.author | Videira, Romeu A. | por |
dc.contributor.author | Andrade, Paula B. | por |
dc.contributor.author | Monteiro, Luís S. | por |
dc.contributor.author | Valentão, Patrícia | por |
dc.contributor.author | Ferreira, Paula M. T. | por |
dc.date.accessioned | 2017-12-07T14:29:01Z | - |
dc.date.available | 2017-12-07T14:29:01Z | - |
dc.date.issued | 2018 | - |
dc.identifier.citation | Romeu A. Videira, Paula B. Andrade, Luís S. Monteiro, Patrícia Valentão, Paula M.T. Ferreira, David M. Pereira, Toxicology in Vitro 47 (2018) 26–37 | por |
dc.identifier.issn | 0887-2333 | por |
dc.identifier.uri | https://hdl.handle.net/1822/48095 | - |
dc.description.abstract | A library of N-protected dehydroamino acids, namely dehydroalanine, dehydroaminobutyric acid and dehydrophenylalanine derivatives, was screened in three human cancer cell lines [(lung (A549), gastric (AGS) and neuroblastoma (SH-SY5Y)] in order to characterize their toxicological profile and identify new molecules with potential anticancer activity. Results showed N-protected dehydrophenylalanine and dehydroaminobutyric acid derivatives have no or low toxicity for all tested cell lines. The N-protected dehydroalanines exhibit significant toxic effects and the AGS and SH-SY5Y cells were significantly more vulnerable than A549 cells. Four α,β- dehydroalanine derivatives, with IC50 < 62.5 μM, were selected to investigate the pathways by which these compounds promote cell death. All compounds, at their IC50 concentrations, were able to induce apoptosis in both AGS and SH-SY5Y cell lines. In both cell lines, loss of mitochondrial membrane potential (ΔΨm) was found and caspase activity was increased, namely endoplasmic reticulum-resident caspase-4 in AGS cells and caspase-3/7 in SH-SY5Y cells. When evaluated in a non-cancer cell line, the molecules displayed no to low toxicity, thus suggesting some degree of selectivity for cancer cells. The results indicate that α,β-dehydroalanine derivatives can be considered a future resource of compounds able to work as anticancer drugs. | por |
dc.description.sponsorship | This work received financial support from National Funds (FCT/MEC) through Project UID/QUI/50006/2013, co-financed by European Union (FEDER under the Partnership Agreement PT2020); and from Norte Portugal Regional Operational Programme (NORTE 2020), under the PORTUGAL 2020 Partnership Agreement, through the European Regional Development Fund (ERDF) (project NORTE-01-0145-FEDER 000024). | por |
dc.language.iso | eng | por |
dc.publisher | Elsevier 1 | por |
dc.relation | info:eu-repo/grantAgreement/FCT/5876/147218/PT | por |
dc.rights | openAccess | por |
dc.subject | Dehydroamino acids | por |
dc.subject | Toxicological profile | por |
dc.subject | Apoptosis | por |
dc.subject | Caspases | por |
dc.subject | Therapeutic agents | por |
dc.subject | Structure-activity relationship (SAR) | por |
dc.title | Toxicity and structure-activity relationship (SAR) of α, β-dehydroamino acids against human cancer cell lines | por |
dc.type | article | por |
dc.peerreviewed | yes | por |
oaire.citationStartPage | 26 | por |
oaire.citationEndPage | 37 | por |
oaire.citationVolume | 47 | por |
dc.identifier.doi | 10.1016/j.tiv.2017.10.027 | por |
dc.identifier.pmid | 29107685 | por |
dc.subject.fos | Ciências Naturais::Ciências Químicas | por |
dc.description.publicationversion | info:eu-repo/semantics/publishedVersion | por |
dc.subject.wos | Science & Technology | por |
sdum.journal | Toxicology in Vitro | por |
Aparece nas coleções: | CDQuim - Artigos (Papers) |
Ficheiros deste registo:
Ficheiro | Descrição | Tamanho | Formato | |
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2018-Toxicology in vitro.pdf | 206,87 kB | Adobe PDF | Ver/Abrir |