Onze derivados da ftalimida foram avaliados quanto a sua atividade antiproliferativa em células tumorais e normais e possíveis efeitos tóxicos. Avaliou-se a citotoxicidade contra tumores murinos (células de Sarcoma 180 e B-16/F-10) e células mononucleares do sangue perférico (CMSP) usando os ensaios de MTT e Alamar Blue. Em seguida, a investigação de citotoxicidade foi executada por citometria de fluxo e potencial antitumoral e toxicológico por meio de métodos in vivo. As moléculas 3b, 3c, 4 e 5 revelaram citotoxicidade in vitro contra Sarcoma 180, B-16/F-10 e PBMC. Uma vez que o composto 4 foi o derivado mais efetivo, ele foi escolhido para detalhar o mecanismo de ação após 24, 48 e 72h de exposição (22.5 e 45 µM). Células de Sarcoma 180 tratadas com o composto 4 mostraram desintegração de membrana, fragmentação de DNA e despolarização mitocondrial de maneira tempo e concentracão dependente. Os compostos 3c, 4 e 5 (50 mg/kg/dia) não inibiu o crescimento tumoral in vivo. Os animals tratados com o composto 4 exibiram aumento do total de leucócitos, linfócitos e no peso relativo do baço, diminuição de neutrófilos e hiperplasia da polpa branca esplênica. Os animais tratados apresentaram alterações histológicas reversíveis. A molécula 4 tem ação antiproliferativa in vitro provavelmente por ativação de apoptose, efeitos tóxicos reversíveis e exibiu propriedades imunoestimulantes que podem ser exploradas para atacar células neoplásicas.

Eleven phthalimide derivatives were evaluated with regards to their antiproliferative activity on tumor and normal cells and possible toxic effects. Cytotoxic analyses were performed against murine tumors (Sarcoma 180 and B-16/F-10 cells) and peripheral blood mononuclear cells (PBMC) using MTT and Alamar Blue assays. Following, the investigation of cytotoxicity was executed by flow cytometry analysis and antitumoral and toxicological potential by in vivo techniques. The molecules 3b, 3c, 4 and 5 revealed in vitro cytotoxicity against Sarcoma 180, B-16/F-10 and PBMC. Since compound 4 was the most effective derivative, it was chosen to detail the mechanism of action after 24, 48 and 72 h exposure (22.5 and 45 µM). Sarcoma 180 cells treated with compound 4 showed membrane disruption, DNA fragmentation and mitochondrial depolarization in a time- and dose-dependent way. Compounds 3c, 4 and 5 (50 mg/kg/day) did not inhibit in vivotumor growth. Compound 4-treated animals exhibited an increase in total leukocytes, lymphocytes and spleen relative weight, a decreasing in neutrophils and hyperplasia of spleen white pulp. Treated animals presented reversible histological changes. Molecule 4 had in vitro antiproliferative action possibly triggered by apoptosis, reversible toxic effects on kidneys, spleen and livers and exhibited immunostimulant properties that can be explored to attack neoplasic cells.

This study aimed to characterize the chemical composition, determine the fatty acid profile, and quantify the bioactive compounds present in guava seed powder (Psidium guajava L.). The powder resulted from seeds obtained from guava pulp processing. The agro-industrial seeds from red guava cv. paluma were used, and they were donated by a frozen pulp fruit manufacturer. They contain varying amounts of macronutrients and micronutrients, with a high content of total dietary fiber (63.94 g/100g), protein (11.19 g/100g), iron (13.8 mg/100g), zinc (3.31 mg/100g), and reduced calorie content (182 kcal/100g). Their lipid profile showed a predominance of unsaturated fatty acids (87.06%), especially linoleic acid (n6) and oleic acid (n9). The powder obtained contained significant amounts of bioactive compounds such as ascorbic acid (87.44 mg/100g), total carotenoids (1.25 mg/100 g) and insoluble dietary fiber (63.55 g/100g). With regard to their microbiological quality, the samples were found suitable for consumption. Based on these results, it can be concluded that the powder produced has favorable attributes for industrial use, and that use of these seeds would be a viable alternative to prevent various diseases and malnutrition in our country and to reduce the environmental impact of agricultural waste.

Grape pomace (Vitis vinifera L.), Benitaka variety, grown in the semiarid region of Northeast Brazil was evaluated in relation to chemical composition, and content of minerals and functional properties. Its microbiological quality and toxic potential, using Artemia salina sp, were also investigated. The results showed that the flour obtained from these residues had below neutral pH (3.82), moisture (3.33g/100g), acidity of (0.64g of citric acid/100g), and ash (4.65 g/100g). The amount of total dietary fiber (46.17g/100g) stood out quantitatively compared to the content of carbohydrate (29.2g/100 g), protein (8.49g/100g), and lipids (8.16g/100g). The total energy was 224Kcal/100g. With regard to the compounds with functional properties, higher values of insoluble fiber 79% (36.4 g/100 g); vitamin C (26.25 mg of acid ascorbic/100g), and anthocyanins (131mg/100g) were found. The minerals iron, potassium, zinc, manganese, and calcium were present in higher concentrations. There were no significant copper values. The results showed that the grape residues are an important source of nutrients and compounds with functional properties suggesting that they can be incorporated as an ingredient in the diet and/or used as a dietary supplement aiming at health benefits. The residues did not show microbiological contamination and were considered nontoxic.