In the present study, micronucleus with cytokinesis blocking and comet assays were used to evaluate the genotoxic potential of Bothrops jararacussu, Bothrops atrox, Bothrops moojeni, Bothrops alternatus (Rhinocerophis alternatus) and Bothrops brazili snake venoms, and also of some isolated toxins (MjTX-I, BthTX-I and II myotoxins, BjussuMP-II metalloprotease, and BatxLAAO l-amino acid oxidase) on human lymphocytes. Significant DNA damages were observed, indicating genotoxic potential after exposure of the lymphocytes to the toxins BthTX-I, II and BatxLAAO compared to untreated and Cisplatin-treated controls, which were able to induce greater formation of micronuclei. B. brazili, B. jararacussu and B. atrox crude venoms also presented genotoxic potential, and the latter two induced DNA breakage 5 times more often than in normal environmental conditions (control without treatment). B. jararacussu venom and its isolated toxins, as well as an LAAO from B. atrox, were able to cause lymphocyte DNA breakage in the comet test with more than 85% damage levels. The DNA damage evaluation allows a widening of the toxic-pharmacological characterization of snake venoms and their toxins and also contributes to the understanding of the mechanisms of action of these molecules in several human pathologies.
Abstract:In order to confirm the traditional use of Baccharis trimera (Less.) DC., Asteraceae, for the reduction of weight, plant extracts were evaluated on the activity of pancreatic lipase (PL), an enzyme responsible for hydrolysis of triacylglycerols in the diet for its subsequent absorption. The aqueous and infused extracts did not show inhibitory activity on the PL, the ethanol inhibited 16% (66 ALI/g) and methanol extract inhibited 78% (241 ALI/g). The methanol extract of B. trimera (MEB) was subjected to a wash with decreasing solvent polarity (n-hexane, ethyl acetate and methanol) and only the methanol fraction inhibited the lipase by 72% (230 ALI/g). We evaluated the MEB and infused inhibitory activity on the enzymes α-amylase and α and β-glycosidases. The α-amylase was not inhibited by any of the extracts, the enzyme α-glucosidase was inhibited by both extracts in the same proportion (46.9±0.1) and β-glucosidase was inhibited by 73% by the methanol extract and 65% by the infused. We also evaluated the presence of anti-nutrients. We detected the presence of saponins, polyphenols and trypsin inhibitors in the two samples. Tests performed in vivo can assess at which therapeutic concentration the presence of these anti-nutrients can be harmful to health.
Keywords Euphorbiaceae, fall armyworm, pest control, plant extract, Ricinus communis
RESUMO:A prevalência da obesidade está aumentando a um ritmo alarmante e poucos medicamentos para o tratamento estão atualmente disponíveis no mercado. A inibição da lipase pancreática é um dos mecanismos mais amplamente estudados para determinar a eficácia de produtos naturais como agentes antiobesidade. O objetivo do estudo foi avaliar in vitro a inibição de dezenove extratos aquosos e metanólicos sobre a lipase pancreática. Ensaios cinéticos foram realizados em quatro períodos de tempo com ausência e presença do extrato inibidor. Também foi avaliado a ação desses extratos após a simulação do fluido gástrico. Cymbopogon citratus apresentou a maior inibição, seguido de Costus spicatus e Baccharis trimera. Os extratos apresentam um potencial como adjuvante no tratamento da obesidade. Palavras-chave: anti obesidade, extratos vegetais, inibição de lipídeosABSTRACT: Selection of crude plant extracts with anti-obesity activity. The prevalence of obesity has been increasing at an alarming rate and only a few medications are currently available in the market. Pancreatic lipase inhibition is one of the most widely studied mechanisms for determining the efficacy of natural products as anti-obesity agents. The aim of this study was to evaluate in vitro the inhibition of nineteen aqueous and methanol extracts on pancreatic lipase. Kinetic assays were performed in four periods with the absence and the presence of the inhibitor extract. We also tested the action of these extracts after gastric fluid simulation. Cymbopogon citratus showed the highest inhibition, followed by Costus spicatus and Baccharis trimera. The extracts have the potential to act as adjuvants in the treatment of obesity.
This study was conducted to evaluate the potential induction of genotoxic effects of white bean flour using the Comet assay. The test was conducted with human lymphocytes present in whole blood immediately after collection, by incubation with white bean flour in three concentrations (3.92, 9.52 and 18.18 mg/ mL) at 37 °C for 4 h followed by preparation of slides. Samples were considered positive (above 20% damage) when the damage observed to cellular DNA was higher than the negative control. No genotoxic potential was found at the doses tested. However, it would be premature to suggest absence of risk to human health of DNA damage since the exposure of cells to the extract was restricted to four hours rather than a whole cell cycle. Additionally, further information on toxicology should be obtained in future studies.Uniterms: Genotoxicity. White bean flour/genotoxic effects. Comet assay/toxicological analysis of food. Food/toxicological analysis.Este estudo foi realizado para avaliar o potencial de indução de efeitos genotóxicos da farinha de feijão branco utilizando o teste do Cometa. O ensaio foi realizado com linfócitos humanos presentes no sangue imediatamente após a coleta, por incubação com farinha de feijão branco em três concentrações (3,92, 9,52 e 18,18 mg/mL) a 37 °C por 4 h, seguida de preparação das lâminas. As amostras foram consideradas positivas (acima de 20% de dano), quando os danos observados no DNA celular foram maiores do que o controle negativo. Verificou-se que as doses testadas não mostraram potencial genotóxico. No entanto, seria prematuro fazer recomendações sobre o padrão de riscos para a saúde humana resultantes de danos ao DNA já que exposição das células ao extrato foi restrito ao período de quatro horas e não durante um ciclo celular completo. Além disso, outras informações sobre a toxicologia devem ser obtidas no futuro.Unitermos: Genotoxicidade. Farinha de feijão branco/efeitos genotóxicos. Teste do Cometa/análise toxicológica de alimentos. Alimentos/análise toxicológica.
Diabetes and obesity represent major public health problems worldwide. High cost of medicines and drug treatments propose the research for less expensive alternatives, such as enzymatic inhibitors present in medicinal plants from natural sources. An example of such medicinal plant is the jambolan Syzygium sp., which is referred to be hypoglycemic and efficient in weight loss. With this in mind, we identified the bioactive compounds from Syzygium sp. commercial teas and evaluated the inhibitory potential and the antioxidant activity of digestive enzymes from a simulated gastric fluid. Syzygium sp. samples showed low percentages of enzymatic inhibition at 1 : 200 dilution. Antioxidant activity was significant, although it was not expressive of the contents of total phenolic compounds, tannins, flavonoids, flavones, and alkaloids. Maldi-Tof spectroscopy suggested the presence of luteolin in Syzygium sp. samples. Molecular docking predicted that luteolin binds at the α-amylase catalytic site in a similar manner as acarbose, the carbohydrate inhibitor from the enzyme crystallographic structure. The phytochemical content and biological activity were distinct among samples from commercial teas. Thus, additional studies should be conducted to elucidate efficacy and safety of Syzygium sp. extracts, especially in vivo experiments. Syzygium sp. might be in the near future recommended as a medicinal plant in low cost diabetes and obesity treatments.
Várias plantas têm sido consideradas produtos terapêuticos, dentre elas destacam-se os chás verde e preto, popularmente utilizados para controle da hiperglicemia e obesidade. Objetivou-se neste trabalho avaliar o potencial inibitório sobre as enzimas α-amilase, α e β-glicosidases e o teor de compostos fenólicos do chá verde e do chá preto. O teor de compostos fenólicos encontrados foram de 80,8 ± 0,43 mg g-1 no chá preto e 32,0 ± 0,12 mg g-1 no chá verde. O chá verde e o chá preto, em condições de consumo, inibiram as enzimas em estudo, porém, após a simulação do fluido gástrico o inibidor presente no chá verde perdeu a ação. O chá preto deixou de inibir a α-amilase e apresentou inibição inalterada para α e β-glicosidases. Tais resultados sugerem que o chá preto pode ser auxiliar em dietas de restrição de carboidratos.
RESUMO:A obesidade é atualmente o principal problema de saúde em países desenvolvidos e em desenvolvimento. Diversos recursos terapêuticos têm sido empregados para o tratamento da obesidade destacando-se os fitoterápicos, consagrados pelo conhecimento popular. Nesse contexto, a planta Hoodia gordonii tem despertado atualmente grande interesse mundial, principalmente pelas recentes descobertas e comprovações científicas da inibição do apetite e da sede pelo glicosídeo ativo P57 isolado de espécies da planta. Apesar disso, tais efeitos ainda não foram avaliados e comprovados em amostras comerciais do pó de H. gordonii (PHG), não existindo evidências científicas que garantam a sua eficácia e segurança. Portanto, o objetivo deste trabalho foi realizar ensaios biológicos com ratos para avaliar a atividade farmacológica e a toxicidade de amostras comerciais do pó de H. gordonii. As amostras foram administradas por gavagem em doses equivalentes a 20 vezes as recomendadas para humanos em ratas Wistar durante 4 semanas sendo avaliados os parâmetros indicadores do efeito terapêutico. Após as 4 semanas, os animais foram sacrificados, e amostras de sangue e órgãos foram coletados e submetidos à avaliação dos indicadores metabólicos, endócrinos, hematológicos e histopatológicos. Os resultados demonstraram que para todos os parâmetros avaliados não houve diferenças significativas entre o grupo controle que recebeu somente solução salina estéril e os grupos tratados com PHG indicando que os mesmos, apesar de não apresentarem quaisquer indícios de toxicidade, são incapazes de produzir os supostos efeitos de inibição de apetite e consequente tratamento da obesidade. Palavras-chave:Hoodia, eficácia, toxicidade, obesidade ABSTRACT: Efficacy and toxicity of Hoodia gordonii commercial powder used to combat obesity. Obesity is currently the main health problem in developed and developing countries. Several therapeutic methods have been employed for the treatment of obesity, especially herbal medicines, highlighted by popular knowledge. In this context, the plant Hoodia gordonii has currently aroused great interest worldwide, especially for recent discoveries and scientific proof of inhibition of appetite and thirst by the active glycoside P57 isolated from plant species. Nevertheless, such effects have not been evaluated and proven for commercial samples of H. gordonii powder (PHG), with no scientific evidence to ensure its effectiveness and safety. Therefore, the aim of this study was to conduct biological tests with rats to evaluate the pharmacological activity and toxicity of commercial samples of H. gordonii powder. The samples were administered through gavage, at doses equivalent to 20 times those recommended for humans, in female Wistar rats during 4 weeks for evaluation of the parameters indicative of therapeutic efficacy. After 4 weeks, the animals were sacrificed and blood and organ samples were collected and subjected to the evaluation of metabolic, endocrine, hematological and histopathological indicators. Results showed t...
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