Paullinia cupana (Guarana) is a native plant of Amazon region that has very traditional importance. Its seeds are rich in bioactive compounds, including tannins, which exhibit relevant properties. Objective. This study aimed to evaluate antibacterial, antineoplastic, and immunomodulatory activity of P. cupana seeds crude extract (CE) and ethyl-acetate fraction (EAF). Methods. Antibacterial activity was evaluated by determination of minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC). Antineoplastic activity was evaluated by MTT assays in hepatocellular carcinoma (HepG2), breast adenocarcinoma (MCF-7), ductal carcinoma (T47-D), non-Hodgkin's B cell lymphoma (Toledo), T cell leukemia (Jukart), and Acute Leukemia (HL-60) cell lines. BALB/c mice splenocytes were treated to assess IFN-γ, IL-6, IL-17, and IL-10 levels by sandwich ELISA. Results. CE and EAF were not toxic to peripheral blood cells and splenocytes. CE and EAF fractions showed a bacteriostatic activity (MIC = 250 μg/mL) and presented IC50 values of 70.25 μg/mL and 61.18 μg/mL in HL-60 leukemia cell line. All cytokines evaluated had their levels reduced after treatment, following dose-response model. Discussion and Conclusion. Different biological activities were observed for both CE and EAF, suggesting P. cupana as a source of bioactive substances, especially tannins that may be used for several diseases treatments.

No abstract

Background: Oxazolidinones display several biological effects including anticancer activity. The purpose of this present work was to investigate a series of novel oxazolidinone derivatives with potential antineoplastic activity. It was evaluated its mechanism of death induction and cell cycle effects. Molecular docking study was accomplished through proteins of Cyclin-Dependent Kinases family (CDK). The new compound LPSF/NBM-2 appear to promote cell cycle arresting at G2/M phase and increased the percentage of apoptotic cells. Methods: : Oxazolidinone derivatives were obtained through Knoevenagel condensation. Cytotoxic assay was evaluated through MTT method. Flow cytometry was performed in order to investigate the effects of the new compounds in the cell cycle stages, induction of cell death and apoptosis. A blind docking was performed through the swissdock online server and the analysis of the results was performed using the UCSF Chimera and discovery studio biovia software. Results: LPSF/NBM-1 and LPSF/NBM-2 displayed the most cytotoxic activity against HL-60 (IC50 = 54.83 µM) and MOLT-4 (IC50 = 51.61 µM) cell lines. LPSF/NBM-2 showed an increased percentage of cell population at G2/M phase. Molecular-docking results of LPSF/NBM-1 and LPSF/NBM-2 suggested binding affinity with the evaluated CDK proteins. Conclusion: LPSF/NBM-1 and LPSF/NBM-2 displayed cytotoxic profile against Hl-60 and MOLT-4. LPSF/NBM-2 increased cell population percentage at G2/M phase and promoted induction of cell death when compared to non-treated cells in MOLT-4 cell line. Based on these findings, oxazolidinone derivatives could be highlighted as possible cytostatic agent against lymphoma cells. Molecular docking results suggest the action of LPSF/NBM-1 and LPSF/NBM-2 compounds on enzymes of cyclin-dependent kinases family, however more studies are demanded in order to stablish this correlation.

Direitos para esta edição cedidos à Atena Editora pelos autores. Open access publication by Atena Editora Todo o conteúdo deste livro está licenciado sob uma Licença de Atribuição Creative Commons. Atribuição-Não-Comercial-NãoDerivativos 4.0 Internacional (CC BY-NC-ND 4.0). O conteúdo dos artigos e seus dados em sua forma, correção e confiabilidade são de responsabilidade exclusiva dos autores, inclusive não representam necessariamente a posição oficial da Atena Editora. Permitido o download da obra e o compartilhamento desde que sejam atribuídos créditos aos autores, mas sem a possibilidade de alterá-la de nenhuma forma ou utilizá-la para fins comerciais.Todos os manuscritos foram previamente submetidos à avaliação cega pelos pares, membros do Conselho Editorial desta Editora, tendo sido aprovados para a publicação com base em critérios de neutralidade e imparcialidade acadêmica.A Atena Editora é comprometida em garantir a integridade editorial em todas as etapas do processo de publicação, evitando plágio, dados ou resultados fraudulentos e impedindo que interesses financeiros comprometam os padrões éticos da publicação. Situações suspeitas de má conduta científica serão investigadas sob o mais alto padrão de rigor acadêmico e ético.