Sulfonamide-chalcone hybrid compound suppresses cellular adhesion and migration: Experimental and computational insight.

In the present study, the effect of sulfonamide-chalcone 185 (SSC185) was investigated against B16-F10 metastatic melanoma cells aggressive actions, besides migration and adhesion processes, by in silico and in vitro assays. In silico studies were used to characterize the pharmacokinetic profile and possible targets of SSC185, using the pkCSM web server, and docking simulations with AutoDock Tools. Furthermore, the antimetastatic effect of SSC185 was investigated by in vitro experiments using MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide), colony, scratch, and cell adhesion assays, and atomic force microscopy (AFM). The molecular docking results show better affinity of SSC185 with the metalloproteinases-2 (MMP-2) and α5ß1 integrin. SSC185 effectively restricts the formation of colonies, migration, and adhesion of B16-F10 metastatic melanoma cells. Through the AFM images changes in cells morphology was identified, with a decrease in the filopodia and increase in the average cellular roughness. The results obtained demonstrate the potential of this molecule in inhibit the primordial steps for metastasis, which is responsible for a worse prognosis of late stage cancer, being the main cause of morbidity among cancer patients.

Impacto da COVID-19 na saúde emocional e na rotina de trabalho de fisioterapeutas oncológicos no Brasil / Impact of COVID-19 on the emotional health and work routine of oncology physiotherapists in Brazi

Introdução: A pandemia da COVID-19 vem impactando na saúde emocional e na rotina de trabalho dos profissionais de saúde. Objetivo: O objetivo deste estudo foi avaliar o efeito da pandemia da COVID-19 na saúde emocional e na rotina do trabalho dos fisioterapeutas oncológicos brasileiros. Métodos: Estudo transversal online anônimo, no qual 102 fisioterapeutas oncológicos foram recrutados de diferentes regiões do país, usando amostras de conveniência de bolas de neve nas mídias sociais. Dados sociodemográficos, referentes à formação e atuação profissional foram avaliados, além dos sintomas de Depressão, Ansiedade e Estresse. Resultados: A maioria dos fisioterapeutas era do sexo feminino (n = 89,87,3%), com média de idade de 33,8 ± 7,1 anos e especialista em fisioterapia oncológica (n = 84,82,5%). Quanto mais jovens mais estressados eram os profissionais (p = 0,022). A maioria manteve os atendimentos presenciais (n = 89, 87,3%) e o sintoma de estresse apresentou maior pontuação (6,9 ± 4,4). O aumento na jornada de trabalho e a transferência para outras unidades de trabalho resultaram em maiores sintomas de ansiedade (p = 0,016) e de estresse (p = 0,011). Conclusão: Concluímos que a pandemia afetou negativamente a rotina de trabalho e a saúde emocional de fisioterapeutas oncológicos no Brasil.

New Synthetic Sulfonamide Chalcone Induced Cell Cycle Arrest and Cell Death in Colorectal Adenocarcinoma Metastatic Cells (SW-620).

BACKGROUND: New chalcones have been developed from the insertion of organic groups, among them sulfonamides, presenting varied biological activity. OBJECTIVE: The aim of this work was to determine the antitumor potential of a new synthetic sulfonamide chalcone (SSC185) against a colorectal metastatic lymph node-derived colorectal cancer cell line (SW-620). METHODS: Synthesis and characterization, including crystallography, of SSC185 were performed. SSC185 showed a selective cytotoxic effect against colorectal cancer cell lines. Therefore, the cytotoxic effect of SSC185 against SW- 620 was further investigated. We used optical and fluorescence microscopy, flow cytometry and Western blot to determine the antitumor effects of SSC185. RESULTS: SSC185 induced cytotoxicity in SW-620 cells in a time and concentration-dependent manner. Cell cycle progression was disrupted, with increased G2/M cell number and consequent cell death, with morphological alterations associated with apoptosis and necrosis. Cell death was associated with the activation and cleavage of PARP, and with reduced expression of the pro-apoptotic Bax protein and caspase 8, depending on the SSC185 concentration tested. Expression of the necroptosis pathway proteins RIP and MLKL was also reduced. These proteins are phosphorylated during the process of necroptosis. CONCLUSION: We suggest that the mechanism involved in the cytotoxic effect of SSC185 against SW-620 in vitro may be related to the induction of cell cycle arrest in the G2/M phase and cell death by apoptosis or necroptosis, depending on the concentration used.

Influência dos Cânceres Gástrico e Hematológico na Qualidade de Vida e na Funcionalidade de Pacientes Oncológicos / Influence of Gastric and Hematological Cancers on the Quality of Life and the Functionality of Oncological Patientss / Influencia de los Cánceres Gástrico y Hematológico em la Calidad de Vida y Funcionalidad de los Pacientes Oncológico

Introdução: O câncer é uma doença complexa, sendo a segunda maior causa de morte no Brasil e no mundo, com uma média de 9,8 milhões de óbitos ao ano. Objetivo: Verificar a influência do tipo de câncer, gástrico ou hematológico, na qualidade de vida e na funcionalidade dos indivíduos. Método: Trata-se de um estudo clínico, transversal, analítico e de abordagem quantitativa. Utilizaram-se na coleta de dados uma ficha com dados demográficos, antropométricos, habituais e da doença, o Quality of Life Questionnaire-Core30 da European Organization for Research and Treatment of Cancer (EORTC QLQ-C30) e a Escala de Performance de Karnofsky (KPS). Resultados: Foram avaliados 29 pacientes no total; destes, 19 pacientes com câncer hematológico (Grupo A) e dez com câncer gástrico (Grupo B). A correlação entre idade, EORTC QLQ-C30 e KPS foi positiva entre a idade e os sintomas (r=,571, p=0,011) e a idade e a somatória total do EORTC QLQ-C30 (r=,548, p=0,015); e negativa entre a KPS e os sintomas (r=-,495, p=0,031) e a KPS e a somatória total do EORTC QLQ-C30 (r=,-580, p=0,009) no grupo A. No grupo B, não foi observada nenhuma correlação entre essas variáveis. Conclusão: Pacientes com câncer hematológico e câncer gástrico apresentam redução da qualidade de vida, sendo observada uma diminuição da funcionalidade nos pacientes com câncer hematológico quando comparado ao câncer gástrico. A redução da função nesses indivíduos pode estar diretamente relacionada com a idade e os sintomas físicos apresentados

Introduction: Cancer is a complex disease, being the second leading cause of death in Brazil and in the world, with an average of 9.8 million deaths per year. Objective: Verify the influence of the type of cancer, gastric or hematological, on the quality of life and functionality of individuals. Method: This is a clinical, cross-sectional, analytical and quantitative study. In the data collection, a form with demographic, anthropometric, habitual and disease data, the Quality-of-Life Questionnaire-Core30 da European Organization for Research and Treatment of Cancer (EORTC QLQ-C30) and the Karnofsky Performance Scale (KPS) were used. Results: 29 patients were evaluated in total, of these 19 patients with hematological cancer (Group A) and 10 with gastric cancer (Group B). The correlation between age, EORTC QLQ-C30 and KPS, was positive between age and symptoms (r=,571, p=0.011) and age and total sum of EORTC QLQ-C30 (r=,548, p=0.015); and negative between the KPS and symptoms (r=-,495, p=0.031) and the KPS and total sum of the EORTC QLQ-C30 (r =,-580, p=0.009) in group A. In group B no correlation was observed between these variables. Conclusion: Patients with hematological and gastric cancer have reduced quality of life, with a reduction in functionality in patients with hematological cancer when compared to gastric cancer. The reduction in function in these individuals may be directly y related to age and physical Symptoms

Introducción: El cáncer es una enfermedad compleja, sien dola segunda causa de muerte en Brasil y e nel mundo, con un promedio de 9,8 millones de muertes por año. Objetivo: Verificar la influencia del tipo de cáncer, gástrico o hematológico, en la calidad de vida y funcionalidad de los individuos. Método: Se trata de un estudio clínico, transversal, analítico y cuantitativo. Em la recogida de datos se utilizó un formulario con datos demográficos, antropométricos, habituales y de enfermedad, el Quality of Life Questionnaire-Core30 da European Organization for Research and Treatment of Cancer (EORTC QLQ-C30) y la Escala de Performance de Karnofsky (KPS). Resultados: Se evaluaron un total de 29 pacientes, de estos 19 pacientes con cáncer hematológico (Grupo A) y 10 con cáncer gástrico (Grupo B). La correlación entre edad, EORTC QLQ-C30 y KPS, fue positiva entre edad y síntomas (r=,571, p=0.011) y edad y suma total de EORTC QLQ-C30 (r=,548, p=0,015); y negativo entre la KPS y síntomas (r=-,495, p=0.031) y la KPS y suma total de la EORTC QLQ-C30 (r=,-580, p=0.009) e nel grupo A. Enel grupo B no se observó correlación entre estas variables. Conclusión: Los pacientes con cáncer hematológico y cáncer gástrico tienen una calidad de vida reducida, observando se una reducción de la funcionalidad en los pacientes con cáncer hematológico em comparación con el cáncer gástrico. La reducción de la funcione en estos individuos puede estar directamente relacionada con la edad y los síntomas físicos

Health impacts on cancer patients: an overview of the COVID-19 pandemic in Brazil / Impactos na saúde do paciente oncológico: um panorama da pandemia por COVID-19 no Brasil

Introduction: Because of the social isolation during the COVID-19 pandemic, the use of health services and the participation in social activities of cancer patients have been reduced, which can have a direct impact on their health. Objective: To identify the repercussions on the cancer treatment, participation in social activities and emotional state of cancer patients in Brazil during COVID-19 pandemic. Methods: This is a cross-sectional study using an online questionnaire for cancer patients. A non-probability sample was recruited by convenience. Sociodemographic and clinical data, physical activity levels and emotional state (DASS-21) during the pandemic were collected. Quantitative data were analyzed and the significance level set at 95% (p < 0.05). Results: A total of 105 individuals participated in the study. Results indicated that younger participants were more stressed; 16.2% reported interrupting cancer treatment and 42.9% cancelled examinations or appointments during the pandemic, associated with a higher rate of stress, anxiety, and depression. More than half of the individuals engaged in exercise before the pandemic, but only 35.2% did so in the previous 2 months. Physical exercise during the pandemic was associated with lower depression score. Conclusion: As observed worldwide, the COVID-19 pandemic has had a direct impact on the physical and mental health of cancer patients in Brazil. (AU)

Introdução: Como consequência do isolamento social durante a pandemia de COVID-19, reduziu-se a utilização de serviços de saúde e a participação em atividades sociais de pacientes com câncer, o que pode impactar diretamente em sua saúde. Objetivo: Identificar as repercussões no tratamento do câncer, na participação em atividades sociais e no estado emocional de pacientes com câncer no Brasil durante a pandemia de COVID-19. Métodos: Trata-se de um estudo transversal com questionário online para pacientes com câncer. Uma amostra não probabilística foi recrutada por conveniência. Dados sociodemográficos e clínicos, níveis de atividade física e estado emocional (DASS-21) durante a pandemia foram coletados. Os dados quantitativos foram analisados e o nível de significância estabelecido em 95% (p <0,05). Resultados: Participaram do estudo 105 indivíduos. Os resultados indicaram que os participantes mais jovens estavam mais estressados; 16,2% relataram interrupção do tratamento contra o câncer e 42,9% cancelaram exames ou consultas durante a pandemia, associado a maior índice de estresse, ansiedade e depressão. Mais da metade dos indivíduos praticou exercícios antes da pandemia, mas apenas 35,2% o fizeram nos 2 meses anteriores. O exercício físico durante a pandemia foi associado a menor escore de depressão. Conclusão: Conforme observado em todo o mundo, a pandemia de COVID-19 teve impacto direto na saúde física e mental de pacientes com câncer no Brasil. (AU)

Diterpenoids from Leaves of Cultivated Plectranthus ornatus.

Two new diterpenoid derivatives 7α,12ß,17-triacetoxy-6ß,19-dihydroxy-13ß,16-spirocicloabiet-8-ene-11,14-dione ( 1: ) and 6ß-acetoxy-3ß,7α,12α-trihydroxy-13ß,16-spirocicloabiet-8-ene-11,14-dione ( 2: ) along with 11 ( 3: - 13: ) miscellaneous compounds were isolated from the leaves of Plectranthus ornatus Codd. Their structures were elucidated by spectroscopic analysis and gauge independent atomic orbitals 13C NMR calculations. The isolated compounds were screened for their effects on intestinal motility using guinea-pig ileum and duodenum and by their cytotoxicity against 4 human cancer cell lines (HCT-116, SF-295, PC-3, and HL-60). Compounds 6: and 9: were moderately cytotoxic against HL-60, whereas 6: and 13: were more active on SF-295 and HCT-116.

Synthesis of PJOV56, a new quinoxalinyl-hydrazone derivative able to induce autophagy and apoptosis in colorectal cancer cells, and related compounds.

Quinoxaline derivatives are reported as antineoplastic agents against a variety of human cancer cell lines, with some compounds being submitted to clinical trials. In this work, we report the synthesis, characterization and cytotoxicity potential of a new series of quinoxalinyl-hydrazones. The most cytotoxic compound was (E)-2-[2-(2-pyridin-2-ylmethylene)hydrazinyl]quinoxaline (PJOV56) that presented a time-dependent effect against HCT-116 cells. After 48 h of incubation, PJOV56 was able to induce autophagy and apoptosis of HCT-116 cells, mediated by upregulation of Beclin 1, upregulation of LC3A/B II and activation of caspase 7. Apoptosis was induced along with G0/G1 cell cycle arrest at the highest concentration of PJOV56 (6.0 µM). Thus, PJOV56 showed a dose-dependent mode of action related to induction of autophagy and apoptosis in HCT-116 cells.