ABSTRACT The herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) occur worldwide. Infections caused by these viruses have great public health importance due to the growing resistance to the first-choice drug, acyclovir, especially in immunosuppressed patients. Alkaloids derived from species of Annonaceae have been reported as antiviral agents against HSV and others viruses. Within this context, we evaluated the antiviral activity of the total alkaloid fraction (TAF) extracted from the branches of Fusaea longifolia (Aubl.) Saff. (Annonaceae), a species native to the Amazon region, against the HSV-1 and HSV-2 viruses. The antiviral activity was evaluated through the plate reduction assay and the mode of action was investigated by a set of other assays. The TAF was active against the HSV-2 strain 333 and against the HSV-1 strains KOS and 29R (acyclovir resistant), with selectivity index values (SI = 50% cytotoxic concentration/50% effective concentration) of 5, 4 and 3, respectively. In the preliminary study of the anti-HSV-2 mode of action, TAF showed viral inhibitory effects if added up to 12 h post-infection, had virucidal activity and did not present viral inhibition in pre-treatment. Our results showed that the TAF exhibited anti-HSV activity. Regarding HSV-2, TAF acted after the viral infection and had virucidal activity. A mass spectrometry analysis revealed the presence of nine alkaloids in the TAF that had previously been reported for Annonaceae, including liriodenine, lysicamine and isoboldine, which have been described as potential anti-HSV-1 agents.

RESUMO Os vírus herpes simplex tipo 1 (HSV-1) e tipo 2 (HSV-2) têm ampla ocorrência global. As infecções causadas por esses vírus têm grande importância em saúde pública devido à crescente resistência ao fármaco de primeira linha, aciclovir, principalmente em pacientes imunossuprimidos. Alcaloides derivados de espécies de Annonaceae têm sido relatados como agentes antivirais contra o HSV e outros vírus. Neste contexto, nós avaliamos a atividade antiviral da fração alcaloide total (TAF) dos ramos de Fusaea longifolia (Aubl.) Saff. (Annonaceae), uma espécie nativa da região amazônica, contra os vírus HSV-1 e HSV-2. A atividade antiviral foi avaliada através do ensaio de redução em placa e o modo de ação foi investigado por um conjunto de ensaios. O TAF foi ativo contra a cepa HSV-2 333 e contra as cepas HSV-1 KOS e 29R (resistente ao aciclovir), com valores de índice de seletividade (IS = 50% concentração citotóxica/50% concentração efetiva) de 5, 4 e 3, respectivamente. No estudo preliminar do modo de ação da atividade anti-HSV-2, o TAF inibiu a replicação viral quando adicionados até 12 h pós-infecção, apresentou atividade virucida e não apresentou inibição viral no pré-tratamento. Nossos resultados mostraram que o TAF exibiu atividade anti-HSV. Em relação ao HSV-2, o TAF atuou após a infecção viral e apresentou atividade virucida. Uma análise do TAF por espectrometria de massas identificou a presença de nove alcaloides, incluindo liriodenina, lisicamina e isoboldina, que já foram descritos como potenciais agentes anti-HSV-1.

Abstract The hydroelectrolytic beverages segment has been expading its market and introducing new flavors in order to meet the demand for new products. However, experimental studies find concerns about the chemical compositions of these drinks. The aim of this study was to develop a drink without synthetic coloring or flavoring, with functional attributes based on the bacaba (Oenocarpus bacaba Mart.) peel extract. Two hydroelectrolytic drinks were developed, one hypotonic and the other isotonic, containing 0.5 and 1.0% of bacaba peel extract. Physicochemical characterization, determination of total phenolic compounds, anthocyanins, and antioxidant capacity were perfomed, in addition to color evaluation, as well as sensory analysis by means of preference tests. The developed formulations showed potential antioxidant activity and natural red coloring due to the phenolic compounds and anthocyanins present in the beverages. The sensory evaluation indicated positive acceptance by the tasters regarding the addition of the bacaba peel extract to the beverage formulations. The developed formulations demonstrated that the use of the bacaba peel is a viable option for the production of sports drinks, acting as a natural dye and offering health benefits due to its bioactive compounds.

RESUMO Obesidade leva ao acúmulo de gordura e disfunção do tecido adiposo. Compostos ativos foram descritos no óleo-resina de copaíba, que apresenta efeitos anti-inflamatórios, antimicrobiais e antioxidantes. Contudo, não há dados sobre os efeitos do óleo-resina de copaíba sobre o tecido adiposo. Assim, testamos a hipótese de que o óleo-resina de copaíba pode prevenir ou minimizar a obesidade, e inflamação e estresse oxidativo no tecido adiposo em resposta à dieta rica em sacarose. Ratos Wistar machos foram casualmente divididos para receber dieta padrão (C, n = 8), dieta padrão e 30% de sacarose na água de beber (S, n = 8), e dieta padrão e 30% de sacarose na água de beber + óleo-resina de copaíba (S+CO, n = 8). O óleo-resina de copaíba foi administrado via gavagem (200 mg kg-1 dia-1), por oito semanas. Animais dos grupos não suplementados (C e S) receberam veículo via gavagem, em volume equivalente ao oferecido ao grupo S+CO. Ao final do experimento, amostras de sangue e tecido adiposo epididimal foram coletadas para análises bioquímicas, inflamatórias e de estresse oxidativo. A suplementação com óleo-resina preveniu ganho de peso, adiposidade, resistência à insulina e aumento de IL-1β, inibiu parcialmente o aumento nos níveis de glicemia de jejum, lipídeos e níveis de IL-6 no tecido adiposo, além de melhorar o sistema de defesa antioxidante no tecido. Nossos resultados sugerem que o óleo-resina de copaíba pode ser usado como uma boa estratégia para a prevenção da obesidade e suas complicações.

ABSTRACT Obesogenic diets lead to fat accumulation and dysfunctional adipose tissue. Active compounds were described in copaiba oleoresin, which presents anti-inflammatory, antimicrobial, and antioxidant properties. However, there are no data regarding the effects of copaiba oleoresin in adipose tissue. Therefore, we tested the hypothesis that the copaiba oleoresin could prevent or minimize obesity and adipose tissue inflammation and oxidative stress in response to a high sucrose diet. Male Wistar rats were randomly assigned to receiving commercial chow (C, n = 8), commercial chow and 30% sucrose added to the drinking water (S, n = 8), or commercial chow and 30% sucrose added to the drinking water + copaiba oleoresin (S+CO, n = 8). Copaiba oleoresin was given at a dose of 200 mg kg-1 day-1 by gavage for eight weeks. C and S animals received vehicle, at equivalent volume, by gavage. At the end of the experiment, blood samples and epididymal adipose tissue were collected for biochemical, inflammatory, and oxidative stress analyses. Copaiba oleoresin supplementation prevented weight gain, adiposity, insulin resistance, and increased IL-1β levels. Additionally, copaiba oleoresin partially attenuated the increase in fasting glucose levels, lipids, and IL-6 levels, and improved the redox status in adipose tissue. Our results suggest that the use of copaiba oleoresin could be a good strategy for prevention of obesity and its complications.

Pomegranate (Punica granatum L.) is a fruit which has important pharmacological activities and has been attracting attention due to its important antioxidant activity, a significant feature in relation to cosmetics. Formulations containing different concentrations of an ethanolic extract of pomegranate (0.1, 1.0 and 5.0%) (w/w) as an antioxidant agent showed that this is an interesting alternative for the use of natural products with biological activity. The stability and rheology of semissolid systems containing an extract of this plant were evaluated. Preliminary stability studies showed greater physico-chemical stability of the formulation, and thus it was used in an accelerated stability study, as well the quantification of total phenolic compounds and the determination of antioxidant activity. It was observed that different concentrations of the extract did not significantly influence the stability. Moreover, the formulation was found to have better stability when stored at room temperature than under heated or cooled conditions. Formulations containing 0.1 and 5.0% of extract showed more stable rheological behavior, due to the absence of a solid/liquid transition in the rheogram. Tests confirmed the high phenolic content and antioxidant activity, demonstrating the potential of this plant for use in cosmetology as an antioxidant.

RESUMO Analisou-se a concentração de fenóis totais presentes nas folhas de Vochysia divergens Pohl. (Vochysiaceae) na região norte do Pantanal, coletadas entre setembro de 2012 e junho de 2013, compreendendo o período de seca (setembro/2012), o começo do período de inundação (dezembro/2012), período de cheia (março/2013) seguido pela vazante (junho/2013). Para a coleta foram selecionadas 15 árvores, cinco em cada área amostral. A concentração de fenóis nas folhas foi obtida com as amostras secas à 40ºC, maceradas com etanol: água e centrifugada. O extrato foi usado para determinação da concentração de fenóis totais utilizando-se o método espectrométrico de Folin-Ciocalteu. Não houve diferença entre as áreas amostrais, entretanto os valores foram diferentes em relação aos períodos sazonais. A menor concentração foi registrada no período da seca (folhas jovens) aumentando gradativamente no início do período de enchente com maiores níveis no final do período de inundação. A maior concentração de fenóis ocorreu durante a vazante (final do ciclo de vida das folhas de V. divergens), seguida pela cheia e enchente. O aumento na concentração de fenóis, provavelmente, está associado ao ciclo de inundações do Pantanal, e relacionado com a fenologia das folhas de V. divergens.

ABSTRACT The total phenol concentration present in Vochysia divergens Pohl. (Vochysiaceae) leaves in the Pantanal was analyzed. Work was carried out between September/2012 and June/2013 which is made up by the dry season (September/2012), the beginning of the rising water (December/2012), the high water (March/2013) followed by the receding water period (June/2013). For the purpose of the research fifteen trees were selected, five from each sample area. The phenolic content in the leaves was obtained from the samples which were dried, steeped with ethanol: water and centrifuged. The extract was used to determine the concentration of total phenols using the Folin-Ciocalteu spectrometric method. There was no difference among the sampling areas; however the values were different in relation to seasonal periods. The lowest concentration was recorded in the dry season (young leaves) increasing gradually at the beginning of the rising water, with higher levels at the end of high water and receding water season. The highest concentration of phenols occurred during the receding water period (end of the life cycle of V. divergens leaves), followed by high and rising water periods. The increase in phenol concentration is associated with the Pantanal flood cycle, and related to the phenology of the V. divergens leaves.

The synthetic n-alkyl esters of gallic acid (GA), also known as gallates, especially propyl, octyl and dodecyl gallates, are widely employed as antioxidants by food and pharmaceutical industries. The inhibitory effects of GA and 15 gallates on Herpes Simplex Virus type 1 (HSV-1) and Human Immunodeficiency Virus (HIV-1) replication were investigated here. After a preliminary screening of these compounds, GA and pentyl gallate (PG) seemed to be the most active compounds against HSV-1 replication and their mode of action was characterized through a set of assays, which attempted to localize the step of the viral multiplication cycle where impairment occurred. The detected anti-HSV-1 activity was mediated by the inhibition of virus attachment to and penetration into cells, and by virucidal properties. Furthermore, an anti-HIV-1 activity was also found, to different degrees. In summary, our results suggest that both compounds could be regarded as promising candidates for the development of topical anti-HSV-1 agents, and further studies concerning the anti-HIV-1 activity of this group of molecules are merited.