CB - DBQ - Artigos publicados em periódicos

URI Permanente para esta coleçãohttps://repositorio.ufrn.br/handle/1/110

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Evaluation of the antiproliferative activity of 2-amino thiophene derivatives against human cancer cells lines
(Elsevier, 2016-12) Aguiar, Andreza Conception Véras de; Moura, Ricardo Olímpio de; Mendonça Junior, Jaime Francisco Bezerra; Rocha, Hugo Alexandre de Oliveira; Câmara, Rafael Barros Gomes da; Schiavon, Manuela dos Santos Carvalho
In spite of great progress in understanding cancer biology, current therapeutic procedures remain unsatisfactory. Chemotherapy is often followed by secondary effects with cellular toxicity negatively affecting the results. The discovery and development of new safe and efficient antitumor agents is necessary. Derivatives of 2-amino thiophene have been a topic of constant investigation due to their versatile synthetic applicability and broad spectrum of biological applications; among which are antifungal and antiproliferative activity shown in prior studies of our group. In the current study, compounds 6CN09, 6CN10, 6CN12, 6CN14, 7CN09 and 7CN11 were analyzed as to antiproliferative effect in human cells of cervical adenocarcinoma (HeLa), human pancreatic adenocarcinoma (PANC-1) and mice fibroblasts (3T3), which were exposed to the compounds in concentrations of 5, 10, 25 and 50mM during 24 and 48 h. They were submitted to MTT assay. In order to elucidate the action mechanism of antitumor thiophene derivatives flow cytometry was performed to evaluate cell death and cell cycle analysis. The results showed that thiophene derivatives demonstrated great antiproliferative potential in the HeLa and PANC-1 cell lines when compared with the control, and the percentage of cell proliferation inhibition approximated or was higher than the standard drug used; doxorubicin (Dox). In highlight were the derivatives 6CN14 and 7CN09 that showed greater efficiency in the antiproliferative evaluation. Further, all compounds had a protective effect on the non-tumor 3T3 cell line. The flow cytometry analysis showed few cells in apoptosis in both the HeLa and PANC-1 lines, although the compounds interfered with the progression of the cell cycle, and avoided cell growth and multiplication in the HeLa tumor line. These thiophene derivatives demonstrated cytostatic and antiproliferative effects and may be considered as promising molecular candidates for anticancer drugs
Heterofucan from Sargassum filipendula induces apoptosis in HeLa cells
(MDPI, 2011-04-14) Costa, Leandro Silva; Telles, Cinthia Beatrice Silva; Oliveira, Ruth Medeiros; Nobre, Leonardo Thiago Duarte Barreto; Dantas-Santos, Nednaldo; Câmara, Rafael Barros Gomes da; Costa, Mariana Santana Santos Pereira; Almeida-Lima, Jailma; Melo-Silveira, Raniere Fagundes; Albuquerque, Ivan Rui Lopes; Leite, Edda Lisboa; Rocha, Hugo Alexandre de Oliveira
Fucan is a term used to denominate a family of sulfated polysaccharides rich in sulfated L-fucose. Heterofucan SF-1.5v was extracted from the brown seaweed Sargassum filipendula by proteolytic digestion followed by sequential acetone precipitation. This fucan showed antiproliferative activity on Hela cells and induced apoptosis. However, SF-1.5v was not able to activate caspases. Moreover, SF-1.5v induced glycogen synthase kinase (GSK) activation, but this protein is not involved in the heterofucan SF-1.5v induced apoptosis mechanism. In addition, ERK, p38, p53, pAKT and NFκB were not affected by the presence of SF-1.5v. We determined that SF-1.5v induces apoptosis in HeLa mainly by mitochondrial release of apoptosis-inducing factor (AIF) into cytosol. In addition, SF-1.5v decreases the expression of anti-apoptotic protein Bcl-2 and increased expression of apoptogenic protein Bax. These results are significant in that they provide a mechanistic framework for further exploring the use of SF-1.5v as a novel chemotherapeutics against human cervical cancer

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