Copaifera langsdorffii Desf. tree oleoresin-induced antinociception recruits µ1- and κ -opioid receptors in the ventrolateral columns of the periaqueductal gray matter.

Popular medicine has been using oleoresin from several species of copaíba tree for the treatment of various diseases and its clinical administration potentially causes antinociception. Electrical stimulation of ventrolateral (vlPAG) and dorsolateral (dlPAG) columns of the periaqueductal gray matter also causes antinociception. The aim this study was to verify the antinociceptive effect of oleoresin extracted from Copaifera langsdorffii tree and to test the hypothesis that oleoresin-induced antinociception is mediated by µ1- and κ-opioid receptors in the vlPAG and dlPAG. Nociceptive thresholds were determined by the tail-flick test in Wistar rats. The copaíba tree oleoresin was administered at different doses (50, 100 and 200 mg/kg) through the gavage technique. After the specification of the most effective dose of copaíba tree oleoresin (200 mg/kg), rats were pretreated with either the µ1-opioid receptor selective antagonist naloxonazine (at 0.05, 0.5 and 5 µg/ 0.2 µl in vlPAG, and 5 µg/ 0.2 µl in dlPAG) or the κ-opioid receptor selective antagonist nor-binaltorphimine (at 1, 3 and 9 nmol/ 0.2 µl in vlPAG, and 9 nmol/ 0.2 µl in dlPAG). The blockade of µ1 and κ opioid receptors of vlPAG decreased the antinociception produced by copaíba tree oleoresin. However, the blockade of these receptors in dlPAG did not alter copaíba tree oleoresin-induced antinociception. These data suggest that vlPAG µ1 and κ opioid receptors are critically recruited in the antinociceptive effect produced by oleoresin extracted from Copaifera langsdorffii.

Use of bacaba peel for the development of hydroelectrolytic beverages and their consumer acceptance

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.

30th Brazilian Society for Virology 2019 Annual Meeting-Cuiabá, Mato Grosso, Brazil.

The 30th meeting of the Brazilian Society for Virology (SBV) was held, for the first time in its 30 years of existence, in Cuiabá, the capital of Mato Grosso State, Central Western Brazil, a tropical region between the three richest biomes in the world: Amazon Florest, Cerrado and Pantanal. In recent years, the field of virology has been built in the State. The aim of this report is to support participants and virologists to receive the most up-to-date information about the meeting, which occurred from 16 to 19 October 2019. National and international speakers gave SBV the opportunity to learn about their experience on their virology fields, sharing recent scientific findings, compiling conferences, round table presentations and work presentations in oral and poster sessions. The meeting held over 300 attendants, who were also involved on oral and poster presentations, showing a great variety of recent unpublished studies on environmental, basic, animal, human, plant and invertebrate virology. In addition, SBV offered the Helio Gelli Pereira award for the best research studies in each field presented during the meeting. The 30th meeting of SBV was very productive and has also encouraged scientific partnership and collaboration among virologists worldwide.

Centesimal and mineral composition and antioxidant activity of the bacaba fruit peel / Composição centesimal, mineral e potencial antioxidante da casca do fruto de bacaba

Oenocarpus bacaba Mart. is a palm tree native from Amazon with highlighted antioxidant activities. Its fruit (bacaba) processing dismisses the peel, which has nutrients that can collaborate for its antioxidant activity and preventing diseases. Thus, this study assessed the centesimal and mineral composition, physicochemical characterization (acidity, total soluble solids, pH, and color), total phenolics (Folin-Ciocalteu method), anthocyanins and antioxidant activity by DPPH (2,2 difenil-1-picril hidrazil) method in bacaba peels. For the centesimal composition, it was found 4.87, 1.42, 29.13, 1.08 and 63.32 g 100 g-1 for water content, ashes, lipids, proteins, and total carbohydrates, respectively. For the mineral composition, it was found 582.97, 79.00, 51.79, 0.625, 37.02, 2.37 and 77.12 mg 100g-1 contents for potassium, sodium, magnesium, copper, calcium, manganese, and phosphorus, respectively. The physicochemical characterization showed pH 5.66, titratable acidity 0.306% of citric acid, total soluble solids 9,75, and coordinates L* a* e b* of 19.03, 8.07 and 9.25, respectively. Phenolic contents were 42.07 mg EAG g-1. The antioxidant potential IC50 was 1.07 mg mL-1 and anthocyanins 37.31 mg 100 g-1. Results show that bacaba peels are an alternate source of nutrients suggesting their use in food as well cosmetic industries, especially for their antioxidant activity and mineral composition

Oenocarpus bacaba MART. (bacaba) é uma palmeira nativa da Amazônia que se destaca por suas propriedades antioxidantes. O processamento de seu fruto gera a casca como produto de descarte, que possui nutrientes que podem colaborar na ação antioxidante e na prevenção de doenças. Assim, o presente trabalho avaliou a composição centesimal e mineral, caracterização físico-química (acidez, sólidos solúveis totais, pH e cor), fenóis totais (método de Folin-Ciocalteu), antocianinas e potencial antioxidante pelo método do DPPH (2,2 difenil-1-picril hidrazil) em cascas de bacaba. Para a composição centesimal verificou-se teores (%) de 4.87, 1.42, 29.13, 1.08 e 63.32 para o teor de água, cinzas, lipídeos, proteínas e carboidratos totais, respectivamente. Para a composição mineral foi encontrado teores (mg100g-1) de 582.97, 79.00, 51.79, 0.625, 37.02, 2.37 e 77.12 para potássio, sódio, magnésio, cobre, cálcio, manganês e fósforo, respectivamente. A caracterização físico-química apresentou valores de pH de 5.66, acidez titulável de 0.306% de ácido cítrico, sólido solúveis totais de 9.75 e cor nas coordenadas L* a* e b* com valores de 19.03, 8.07 e 9.25 . Para o teor de fenóis foi encontrado 42.07 mg EAG.g-1. O EC50 para a potencial antioxidante foi de 1.07 mg.mL-1 e o teor de antocianinas foi de 37.31 mg.100g-1. Os resultados mostram que as cascas de bacaba são uma fonte alternativa de nutrientes sugerindo seu aproveitamento na indústria alimentícia e cosmética, principalmente pela sua potencial atividade antioxidante e composição em minerais.

Determination and validation of secnidazole in tablets by UV spectrophotometric / Determinação e validação do secnidazol em comprimidos por espectrofotometria na região do ultravioleta

Secnidazole, a 5-nitroimidazole, is a drug used in the treatment against protozoa, and several bacterial infections. This study purpose was to develop and validate a UV spectrophotometric method to determine secnidazole in pharmaceutical tablet dosage forms once there is no method reported in the pharmacopoeia yet. The quantification was performed using methanol as solvent at 325 nm (maximum wavelength) and three kinds of products marketed in Brazil (reference, generic and similar tablets) containing 1g of secnidazole. The method obeyed Beer's law in the concentration range of 4 - 20 µgmL-1 respectively. The method was validated according to the International Conference on Harmonization (ICH) and Brazil National Health Surveillance Agency (ANVISA) guidelines, showing accuracy, precision, selectivity, robustness and linearity. Tests such as weight range, friability, disintegration, hardness and dissolution were carried out to check tablets' quality and all the trials showed to be in accordance with the general test guidelines of the Brazilian Pharmacopoeia. The dissolution test was carried out and the developed method was applied. The method developed is suitable for the estimation of secnidazole in tablets without any interference from the excipients and can be used for routine in quality control. Still, it's a simple, fast and low cost method.

Secnidazol, um nitroimidazólico, é um fármaco utilizado no tratamento para protozoários, e várias infecções bacterianas. Este trabalho propôs o desenvolvimento e validação de um método espectrofotométrico na região do ultravioleta para a determinação de Secnidazol na forma farmacêutica de comprimidos, uma vez que não há nenhum método relatado nas farmacopeias. A quantificação foi realizada utilizando metanol como solvente a 325 nm (máximo de comprimento de onda) e usando três tipos de produtos comercializados no Brasil (de referência, genéricos e comprimidos similares) contendo 1g de Secnidazol. O método obedeceu a lei de Beer no intervalo de concentração de 4 - 20 µgmL-1, respectivamente. O método foi validado de acordo com a Conferência Internacional de Harmonização (ICH) e diretrizes da Agência Nacional de Vigilância Sanitária do Brasil (ANVISA), apresentando exatidão, precisão, seletividade, robustez e linearidade. Testes como variação de peso, friabilidade, desintegração, dureza e dissolução foram realizados para verificar a qualidade de comprimidos e mostrou-se de acordo com os testes gerais da Farmacopeia Brasileira. O teste de dissolução realizado e o método desenvolvido pode ser aplicado. O método desenvolvido é adequado para a estimativa de secnidazole em comprimidos sem qualquer interferência dos excipientes e pode ser usado para a rotina de controlo de qualidade. Ainda, é um método simples, rápido e de baixo custo.

Avaliação da qualidade de medicamentos contendo clortalidona / Quality Assessment of medication containing chlorthalidone

Os diuréticos são a classe de fármacos mais utilizados no tratamento da hipertensão devido a sua eficácia terapêutica e ao baixo custo. Isto faz com que uma grande variedade de medicamentos esteja disponível no comercio e atrelado a este fator muitas empresas tem seus lotes de medicamentos suspensos devido a desvios de qualidade e das modificações realizadas nas formulações após o seu registro. A clortalidona é um diurético tiazídico indicada para o tratamento de hipertensão arterial leve ou moderada e com normalidade das funções cardíacas e renal. Este trabalho teve como objetivo verificar a qualidade de comprimidos de clortalidona comercializados no município de Sinop/ MT. O controle de qualidade foi realizado como estabelecido na Farmacopeia Brasileira quinta edição (ensaios de identificação, pureza, doseamento, ensaios referentes a forma farmacêutica de comprimidos e perfil de dissolução), de cinco produtos contendo clortalidona 25 mg sendo um produto de medicamento referência, dois de medicamentos genéricos e dois de medicamentos similares. Verificou-se que todos os produtos foram aprovados, cumprindo com todos os requisitos exigidos nos ensaios de qualidade e que estudos referentes ao perfil de dissolução nos lotes de produção de medicamentos são importantes para prever a absorção adequada do princípio ativo

Diuretics are the most used class of drugs that are used to treat hypertension because of their therapeutic efficiency and low cost. This makes a wide variety of medicines commercially available and, linked to this factor, many companies have their batches of medicines suspended due to deviations of quality and modifications made in the formulas after their registration. Chlorthalidone, is a thiazide diuretic drug indicated for treatment of hypertension of patients with mild or moderate hypertension, and with normal cardiac and renal function. This work aimed to assess and compare the quality of medicines containing chlorthalidone commercialized in Sinop-MT. The quality control was performed as established in the fifth edition of the Brazilian Pharmacopoeia (identification, purity and dosage assays, tests referring to the pharmaceutical form of the tablets and their dissolution profile). Among five products containing 25 mg of chlortalidone, one was a reference drug product, two were generic and two were similar drugs. It was found that all products were approved, meeting all the requirements required in the quality tests, and that studies concerning the dissolution profile in batches of drug production are important to predict adequate absorption of the active principle

Antiplasmodial and Cytotoxic Activities of Toad Venoms from Southern Amazon, Brazil.

The drug-resistance of malaria parasites is the main problem in the disease control. The huge Brazilian biodiversity promotes the search for new compounds, where the animal kingdom is proving to be a promising source of bioactive compounds. The main objective of this study was to evaluate the antiplasmodial and cytotoxic activity of the compounds obtained from the toad venoms of Brazilian Amazon. Toad venoms were collected from the secretion of Rhinella marina and Rhaebo guttatus in Mato Grosso State, Brazil. The powder was extracted at room temperature, yielding 2 extracts (RG and RM) and a substance ('1') identified as a bufadienolide, named telocinobufagin. Growth inhibition, intraerythrocytic development, and parasite morphology were evaluated in culture by microscopic observations of Giemsa-stained thin blood films. Cytotoxicity was determined against HepG2 and BGM cells by MTT and neutral red assays. The 2 extracts and the pure substance ('1') tested were active against chloroquine-resistant Plasmodium falciparum strain, demonstrating lower IC50 values. In cytotoxic tests, the 2 extracts and substance '1' showed pronounced lethal effects on chloroquine-resistant P. faciparum strain and low cytotoxic effect, highlighting toad parotoid gland secretions as a promising source of novel lead antiplasmodial compounds.

Antimalarial activity of 4-metoxychalcones: docking studies as falcipain/plasmepsin inhibitors, ADMET and lipophilic efficiency analysis to identify a putative oral lead candidate.

Herein, we report the antimalarial activity of nine 4-methoxychalcone derivatives 1a-i and an initial analysis of their ADMET properties. All compounds showed potent activity against the P. falciparum chloroquine-resistant clone W2, with IC50 values ranging from 1.96 µM to 10.99 µM, with moderate or low cytotoxicity against the HeLa cell line. The compound 1a (IC50 = 2.06 µM) had the best selectivity index (9.0). All the sulfonamide 4-metychalcone derivatives synthesized had cLogP values between 2 and 5 (mean value 3.79) and molecular weights (MWs) below 500. The substitution of the pyrrolidine group in 1i by a morpholine group in 1a reduced the cLogP value from 3.05 in compound 1i to 2.34 in compound 1a. Indeed, compound 1a had the highest LipE value. The binding free energy of compound 1a showed it to be the most optimal chalcone derivative for plasmepsin-2 (-7.3 Kcal/mol). The physicochemical properties and LipE analysis of the dataset allowed us to establish that compound 1a is the highest quality compound of the series and a potential oral lead candidate.