Role of dietary fats in modulating cardiometabolic risk during moderate weight gain : a randomized double-blind overfeeding trial (LIPOGAIN study)

BACKGROUND: Whether the type of dietary fat could alter cardiometabolic responses to a hypercaloric diet is unknown. In addition, subclinical cardiometabolic consequences of moderate weight gain require further study. METHODS AND RESULTS: In a 7-week, double-blind, parallel-group, randomized controlled trial, 39 healthy, lean individuals (mean age of 27±4) consumed muffins (51% of energy [%E] from fat and 44%E refined carbohydrates) providing 750 kcal/day added to their habitual diets. All muffins had identical contents, except for type of fat; sunflower oil rich in polyunsaturated fatty acids (PUFA diet) or palm oil rich in saturated fatty acids (SFA diet). Despite comparable weight gain in the 2 groups, total: high-density lipoprotein (HDL) cholesterol, low-density lipoprotein:HDL cholesterol, and apolipoprotein B:AI ratios decreased during the PUFA versus the SFA diet (-0.37±0.59 versus +0.07±0.29, -0.31±0.49 versus +0.05±0.28, and -0.07±0.11 versus +0.01±0.07, P=0.003, P=0.007, and P=0.01 for between-group differences), whereas no significant differences were observed for other cardiometabolic risk markers. In the whole group (ie, independently of fat type), body weight increased (+2.2%, P<0.001) together with increased plasma proinsulin (+21%, P=0.007), insulin (+17%, P=0.003), proprotein convertase subtilisin/kexin type 9, (+9%, P=0.008) fibroblast growth factor-21 (+31%, P=0.04), endothelial markers vascular cell adhesion molecule-1, intercellular adhesion molecule-1, and E-selectin (+9, +5, and +10%, respectively, P<0.01 for all), whereas nonesterified fatty acids decreased (-28%, P=0.001). CONCLUSIONS: Excess energy from PUFA versus SFA reduces atherogenic lipoproteins. Modest weight gain in young individuals induces hyperproinsulinemia and increases biomarkers of endothelial dysfunction, effects that may be partly outweighed by the lipid-lowering effects of PUFA. CLINICAL TRIAL REGISTRATION URL: http://ClinicalTrials.gov. Unique identifier: NCT01427140.

Efeitos de variáveis abióticas na composição química de Gelidium Crinale (Gelidiaceae, Rhodophyta) em cultivo unialgal

Os efeitos individuais e interativos dos parâmetros ambientais físicos e químicos, como temperatura, intensidade luminosa, salinidade e concentração de fósforo inorgânico dissolvido na água do mar, na produção de proteínas, carboidratos, acúmulo de fósforo tecidual e taxa de absorção do fósforo inorgânico disponível no meio de cultura em Gelidium crinale (Turner) Lamouroux, foram investigados durante um período de sete dias de cultivo laboratorial, em condições controladas. A ação dos parâmetros abióticos foi analisada de três maneiras diferentes. A primeira avaliação integrou a ação de temperatura, intensidade luminosa e fósforo inorgânico dissolvido, mantendo-se fixa a salinidade em 25 ups, onde se constatou que em todos os componentes químicos algais ocorreram interações de terceira ordem. O incremento de 2,28 a 2,67 % nos teores de proteínas foram obtidos à temperatura de 25 °C e 12 μmol m-2 s-1 de intensidade luminosa, diminuindo com a elevação da intensidade luminosa para 40 μmol m-2 s-1. Para carboidratos, ocorreram interações significativas entre os três parâmetros, com um aumento de 6,85 % sendo registrado a 25 °C de temperatura, 24 μmol m-2 s-1 de intensidade luminosa e 10,0 μM de fósforo inorgânico. O aumento máximo na taxa de fósforo tecidual (0,56 %) ocorreu em talos cultivados nas menores temperatura e intensidade luminosa e na maior concentração de fósforo inorgânico dissolvido. Com relação à intensidade luminosa, foi observada uma correlação negativa entre proteínas e carboidratos. A segunda avaliação estabeleceu a ação independente e sinérgica de temperatura, salinidade e fósforo inorgânico disponível no meio de cultivo, fixando-se a intensidade luminosa em 24 μmol m-2s-1. A maior produção de proteínas ocorreu em cultivos onde a temperatura foi de 25 °C, com uma concentração de 5,0 e 10,0 μM de fósforo inorgânico dissolvido e salinidade entre 15 e 20 ups, cujos valores médios do incremento variaram entre 2,62 a 2,83 % peso seco de alga, resultando em uma interação de terceira ordem altamente significativa. Para carboidratos a elevação de 6,85 % em sua concentração está associada à maior temperatura (25 °C), maior salinidade (25 ups) e maior quantidade de fósforo inorgânico disponível no meio de cultivo (10,0 μM). Contudo, não foi observada uma interação de terceira ordem através da análise estatística. Para esta biomolécula observaram-se interações de segunda ordem altamente significativa (P < 0,005) entre temperatura e diferentes concentrações de fósforo inorgânico e entre temperatura e salinidade (P < 0,000). O acúmulo de fósforo nos talos da alga foi menor durante os cultivos em que a salinidade foi de 25 ups,nas temperaturas de 20 e 25 °C e concentração de fósforo disponível de 2,5 μM, com percentuais entre 0,08 a 0,11 % em peso de cinzas. O maior incremento ocorreu na menor temperatura, associada à baixa salinidade e alta concentração de fósforo inorgânico no meio. O coeficiente de correlação de Pearson revelou correlações positivas, altamente significativas (P < 0,001) entre teor de proteína, temperatura e disponibilidade de fósforo inorgânico no meio de cultivo. Para carboidratos, as correlações foram positivas com os três parâmetros abióticos. Para fósforo tecidual somente com o fósforo inorgânico disponível no cultivo foi que ocorreu uma relação positiva; com os outros dois parâmetros esta correlação foi negativa. Entre os componentes químicos encontrados nas algas, proteínas e carboidratos apresentaram uma relação positiva, porém fósforo tecidual apresentou uma correlação negativa com ambos, embora com proteínas esta relação não tenha sido significativa. A terceira avaliação estudou a ação individual e o sinergismo entre os parâmetros ambientais, temperatura, intensidade luminosa e salinidade, a uma concentração fixa de fósforo inorgânico disponível no meio de cultivo (10,0 μM), sobre a composição química, bem como na taxa de absorção de fósforo inorgânico disponível. Observou-se a ocorrência de interações de terceira ordem em todos as variáveis estudadas. O teor de proteínas apresentou um aumento de 3,72 % durante o período de cultivo, passando de 20,63 % antes do cultivo, para 24,35 % após o término do experimento, principalmente nas condições de 25 °C de temperatura, 12 μmol m-2s-1 de intensidade luminosa e 15 ups de salinidade. Para carboidratos, nas condições de baixa intensidade luminosa (12 μmol m-2s- 1), a uma temperatura de 20 °C e salinidades de 10 e 15 ups, foram registrados valores inferiores à amostra controle, caracterizando um consumo desta biomolécula por parte das algas. Nestas mesmas condições ambientais, foram registrados os maiores teores de fósforo tecidual, variando entre 0,86 a 1,09 % do peso das cinzas. As maiores taxas de absorção do fósforo do meio ocorreram na salinidade de 25 ups e 25 °C de temperatura, diminuindo da intensidade luminosa de 12 μmol m-2s-1 para 40 μmol m-2s-1. As maiores concentrações de fósforo inorgânico residual na água do meio de cultivo ocorreram nas salinidades de 10 e 15 ups, em todas as intensidade luminosas e temperaturas estudadas. Através do coeficiente de correlação de Pearson, observou-se que os teores de proteínas apresentaram uma forte correlação negativa com a intensidade luminosa e positiva com a temperatura e salinidade, embora com esta última não tenha sido significativa. Para carboidratos, as correlações com os parâmetros abióticos foram todas positivas. Correlações negativa e positiva, não significativas, foram observadas entre esta biomolécula e o teor de proteínas e a taxa de absorção de fósforo disponível no meio, respectivamente. Por outro lado, com fósforo tecidual, ocorreu uma correlação negativa, altamente significativa. Este estudo mostra o estado fisiológico de Gelidium crinale e contribui para o estabelecimento das melhores condições de cultivo para produção de proteína, carboidrato e fósforo tecidual e indicação do uso racional de nutrientes, fornecendo informações para a otimização de processos de maricultura, tanto em termos de cultivo bem sucedido de algas, quanto de redução no impacto sobre o ambiente.

Organização de produtores rurais para a gestão da cadeia produtiva da mandioca no nordeste paraense: um estudo de caso na Associação de Desenvolvimento Comunitário e Rural Bom Jesus

A mandioca (Manihot esculenta Crantz) é uma planta cultivada predominantemente para a subsistência dos trabalhadores rurais sendo uma das principais fontes de carboidratos disponíveis aos estratos sociais de baixa renda e tem importante participação na geração de emprego e renda. O Estado do Pará destaca-se pelo volume de produção de mandioca, mas o cultivo ainda está voltado essencialmente para a subsistência sendo pouco explorado como matéria prima em derivados industriais e insumo para enfrentar problemas globais como a fome, a degradação ambiental e a produção de energia, gerando emprego e renda para comunidades locais e rurais. Este estudo tem como objetivo avaliar como está se desenvolvendo a organização de produtores rurais de mandioca da Associação de Desenvolvimento Comunitário e Rural Bom Jesus, através do modelo de gestão de cadeia produtiva e compreender em que medida se justifica economicamente o cultivo de mandioca. A pesquisa é de natureza exploratória e descritiva e por meio do questionário e entrevista aplicado a 17 produtores rurais juntamente com a fundamentação teórica sobre o entendimento contemporâneo de cadeia produtiva foram percebidos evidências que justificam economicamente, em parte, o cultivo da mandioca. A geração de postos de trabalhos para as mulheres, a utilização de resíduos como incremento no arranjo produtivo, a apoio da extensão e do crédito rural, e as vantagens advindas da organização dos produtores rurais proporcionando renda e produção constantes no campo, foram os fatores considerados. Porém, a necessidade de inovações tecnológicas, parcerias com os setores industriais, arranjos produtivos mais rentáveis, mecanização do plantio e da colheita, os problemas ambientais (resíduos tóxicos e desmatamento) e de acesso à pesquisa, o nível de escolaridade, e a cooperação entre os agricultores, são desafios reais a serem enfrentados e o fator decisivo é o apoio governamental. Este estudo demonstra a realidade de uma sociedade quase sempre marginalizada e esquecida pelas políticas públicas. Além da variável econômica, a avaliação das culturas produtivas deve passar pelos filtros de análise social e ambiental, pois assim, nos permite com maior exatidão compreender os problemas reais da nossa sociedade, em especial da vida na Amazônia.

Potencial de produção de cana-energia em áreas agrícolas marginais no Brasil

A descoberta e utilização do petróleo provocaram significativas mudanças na sociedade ao longo do tempo, sendo ele um dos mais importantes fatores de transformação socioambiental e cultural no mundo ao longo do ultimo século. Sua grande gama de possibilidades de utilização acabou criando um sistema de produção baseado em um único agente energético, principalmente nos países que não possuem recursos hídricos nem outras fontes renováveis. Porém, nas ultimas décadas do século passado, começaram a surgir inúmeras discussões sobre a necessidade de se alterar a composição da matriz energética global. Como resultados das preocupações quanto à escassez daquele recurso natural, vários pesquisadores direcionaram seus estudos para a busca de alternativas que pudessem de forma sustentável se prestar como substituto ao petróleo. Uma delas seria o uso de biomassa, de forma a aproveitar a capacidade das plantas em transformar a energia solar em carbohidratos. O Brasil, além de possuir uma das matrizes energéticas mais diversificadas e limpas do mundo, possui grande extensão de terras agricultáveis o que o coloca em lugar de destaque quanto ao potencial de produção de culturas agroenergéticas. Considerando as características da cana-de-açúcar e a sua adaptação a áreas de cultivo do Brasil e impulsionados pela demanda de produção de biomassa moderna, a ser aplicada em processos de transformação mais complexos e que possibilitem a obtenção de outros produtos além de açúcar, álcool e energia, estudou-se neste trabalho plantas de cana-de-açúcar melhoradas com a finalidade exclusiva de produzir biomassa moderna, a chamada “cana- energia”. Esta é uma planta que, contrariamente à tradicional cana-de-açúcar, melhorada para produzir sacarose, é direcionada para produzir fibra, e que, além disso, por possuir maior participação de espécies ancestrais de maior rusticidade, estão aptas a suportar condições ambientais mais estressantes. Os resultados obtidos demonstraram que os híbridos de cana-energia apresentam grande potencial de produção de biomassa e massa seca por área, a custos altamente competitivos considerando as análises comparativas de custo de produção de massa seca por área. Quanto a produção foi possível observar que além de ser mais produtiva em primeiro corte, nos resultados de colheita de soqueira (segundo corte), o melhor híbrido de cana- energia chegou a produzir uma vez e meia mais massa seca que a cana-de-açúcar tradicional, e apresentou maiores produtividades que outras culturas energéticas tais como o eucalipto e o capim-elefante, sendo que, considerando as produtividades médias observadas, a partir do terceiro corte com estes níveis de produtividade, a cana-energia passa a ser a matéria prima de mais baixo custo de produção de massa seca por área, denotando o seu alto potencial como matéria prima para a produção de bioenergia. No Zoneamento agroecológico realizado para a cana energia foi possível identificar 32,3 milhões de hectares de áreas de produção agrícola marginais aptas ao cultivo deste material, sendo que de acordo com os resultados do zoneamento agrícola e as características das regiões em estudos, identifica-se que deste total, pode-se considerar que os materiais que se destacaram em produtividade neste estudo, apresentam boas condições de ocupar uma área de 2,0 a 8,0 milhões de hectares.

Enzymatic inhibitory activity of hydroxycinnamates (HCs): in silico studies

Diabetes is a worldwide health issue that has been expanding mainly in developed countries. It is characterized by abnormal levels of blood sugar due to several factors. The most common are resistance to insulin and the production of defective insulin which exerts little or no effect. Its most common symptoms include tissue damage to several systems due to elevated levels of blood sugar. One of the key enzymes in hydrocarbon metabolism is α-glucosidase (EC 3.2.1.20). It catalyzes the breakdown of complex carbohydrates into their respective monomers (glucose) which allows them to be absorbed. In this work, caffeoyl quinic acids and their metabolites were analyzed as potential inhibitors for α-glucosidase. The search for the best inhibitor was conducted using molecular docking. The affinity of each compound was compared to the inhibitor present in the crystal structure of the protein. As no inhibitor with a similar affinity was´found, a new approach was used, in situ drug design. It was not possible to achieve an inhibitor capable of competing with the one present in the crystal structure of the enzyme, which is also its current commercial inhibitor. It is possible to draw some conclusions as to which functional groups interact best with certain residues of the active site. This work was divided into three main sections. The first section, Diabetes, serves as an introduction to what is Diabetes, its symptoms and/or side effects and how caffeoyl quinic acids could be used as a treatment. The second section, Caffeoylquinic acids and their metabolites as inhibitors for Alfa-glucosidase, corresponds to the search through molecular docking of caffeoyl quinic acids as inhibitors for α-glucosidase and what was possible to draw from this search. The last section, In situ design of an inhibitor for α-glucosidase (EC 3.2.1.20), corresponds to the in situ drug design study and what it achieved. The representation of each of the molecules used as a ligand can be found in the Annexes.

Enrichment of bioactive compounds in microalgae for aquaculture

Microalgae are promising microorganisms for the production of food and fine chemicals. Several species of microalgae are used in aquaculture with the purpose of transfer bioactive compounds up to the aquatic food chain. The main objective of this project was to develop a stress–inducement strategy in order to enhance the biochemical productivity of Nannochloropsis gaditana, Rhodomonas marina and Isochrysis sp. for aquaculture purposes having in account their growth and organizational differences. In this regard, two experiments were design: the first one consisted on the alteration of overall nutrient availabilities in growth medium; and the second one comprised changes in nitrogen and sulfur concentrations maintaining the concentrations of the other nutrients present in a commercial growth medium (Nutribloom plus), which is frequently used in aquaculture. Microalgae dried biomass was characterized biochemically and elemental analysis was also performed for all samples. In first experimental design: linear trends between nutrient availability in growth media and microalgae protein content were obtained; optimum productivities of eicosapentaenoic (EPA) and docosahexaenoic acids (DHA) were attained for both R. marina and N. gaditana in growth media enriched with 1000 L L-1 of nutrient solution whereas for Isochrysis sp. the double of Nutribloom plus was needed; the decrease of glucans and total monosaccharides with nutrient availability for R. marina and Isochrysis sp. showed the occurrence of a possible depletion of carbohydrates towards lipids and proteins biosynthesis. Second experimental desing: N. gaditana exhibited the highest variation in their biochemical composition against the applied perturbation; variations observed for microalgae in their biochemical composition were reflected in their elemental stoichiometry; in N. gaditana the highest nitrogen concentrations lead to overall maximum productivities of the biochemical parameters. The results of the present work show two stress-inducement strategies for microalgae that may constitute a base for further investigations on their biochemical enhancement.

Effects of Purified Saccharomyces cerevisiae (1→3)-β-Glucan on Venous Ulcer Healing

Water-insoluble glucan was isolated from the baker’s yeast Saccharomyces cerevisiae. The yeast cells were treated with alkali and the residue then with acid. Chemical and NMR (1D and 2D) analyses showed that a linear (1→3)-β-glucan was purified that was not contaminated with other carbohydrates, proteins or phenolic compounds. The effects of the glucan on wound healing were assessed in human venous ulcers by histopathological analysis after 30 days of topical treatment. (1→3)-β-glucan enhanced ulcer healing and increased epithelial hyperplasia, as well as increased inflammatory cells, angiogenesis and fibroblast proliferation. In one patient who had an ulcer that would not heal for over 15 years, glucan treatment caused a 67.8% decrease in the area of the ulcer. This is the first study to investigate the effects of (1→3)-β-glucan on venous ulcer healing in humans; our findings suggest that this glucan is a potential natural biological response modifier in wound healing

Effects of Purified Saccharomyces cerevisiae (1→3)-β-Glucan on Venous Ulcer Healing

Water-insoluble glucan was isolated from the baker’s yeast Saccharomyces cerevisiae. The yeast cells were treated with alkali and the residue then with acid. Chemical and NMR (1D and 2D) analyses showed that a linear (1→3)-β-glucan was purified that was not contaminated with other carbohydrates, proteins or phenolic compounds. The effects of the glucan on wound healing were assessed in human venous ulcers by histopathological analysis after 30 days of topical treatment. (1→3)-β-glucan enhanced ulcer healing and increased epithelial hyperplasia, as well as increased inflammatory cells, angiogenesis and fibroblast proliferation. In one patient who had an ulcer that would not heal for over 15 years, glucan treatment caused a 67.8% decrease in the area of the ulcer. This is the first study to investigate the effects of (1→3)-β-glucan on venous ulcer healing in humans; our findings suggest that this glucan is a potential natural biological response modifier in wound healing

Avaliação do extrato do fungo caripia montagnei e de agonistas de PPAR - α no processo inflamatório

The mushrooms have been object of intense research in view of its potential raising of application in different sectors of the pharmacology and alimentary industry. Among diverse bioactive composites of polyssacharides nature that exist in the fungus the glucans are much searched. These are polymers of glucose and classified as the type of glicosidic linking [α, β]. Peroxisome proliferator-activated receptors (PPARs), ranscription factors belonging to the family of nuclear receptors that bind themselves o specific agonists, have shown their importance in controlling the inflammatory process. The aim of this study was to perform a chemical characterization of extract rom the mushroom Caripia montagnei, assess its antiinflammatory and antibacterial effect and determine if this effect occurs via PPAR. This mushroom is composed of carbohydrates (63.3±4.1%), lipids (21.4l±0.9%) and proteins (2.2± 0.3%). The aqueous solution resulting from the fractionation contained carbohydrates (98.7±3.3%) and protein (1.3±0.25%). Analyses of infrared spectrophotometry and of nuclear magnetic esonance demonstrated that the extract of mushroom C. montagnei is rich in β-glucans. In hioglycolate-induced peritonitis, the C. montagnei glucans (50 mg/kg) educed the inflammatory process in 65.5±5.2% and agonists, pharmacological igands, for PPAR: Wy-14643 (49.3±6.1%), PFOA (48.9±3.8%) and clofibrate in 45.2±3.2%. Sodium diclofenac showed a reduction of 81.65±0.6%. In the plantar edema, the glucans from C. montagnei (50 mg/kg) and L-NAME reduced the edema to a similar degree 91.4±0.3% and 92.8±0,5 %, respectively. In all the groups tested, nitric oxide (NO), an inflammation mediator, showed a significant reduction in the nitrate/nitrite levels when compared to the positive control (P<0.001). The C. montagnei glucans did not show cytotoxicity in the concentrations tested (2.5, 5.0, 10.0, 20.0 and 40.0 µg/100 µL). Antibacterial activity demonstrated that, unlike total extract, there was no inhibition of bacterial growth. The C. montagnei glucans show great potential for antiinflammatory applications. This effect suggests that it is mediated by PPAR activation and by COX and iNOS inhibition

Avaliação das propriedades farmacológicas de polissacarídeos do fungo Scleroderma nitidum

Several pharmacological properties have been attributed to isolated compounds from mushroom. Recently, have these compounds, especially the polysaccharides derived from mushrooms, modulate the immune system, and its antitumor, antiviral, antibiotic and antiinflammatory activities. This study assesses the possible pharmacological properties of the polysaccharides from Scleroderma nitidum mushroom. The centesimal composition of the tissue showed that this fungus is composed mainly of fibers (35.61%), ash (33.69%) and carbohydrates (25.31%). The chemical analysis of the polysaccharide fraction showed high levels of carbohydrates (94.71%) and low content of protein (5.29%). These polysaccharides are composed of glucose, galactose, mannose and fucose in the following molar ratios 0.156, 0.044, 0.025, 0.066 and the infrared analysis showed a possible polysaccharide-protein complex. The polysaccharides from Scleroderma nitidum showed antioxidant potential with concentration-dependent antioxidant activity compared to ascorbic acid. The analysis scavenging of superoxide radical and inhibition of lipid peroxidation showed that the polysaccharides from S. nitidum have an IC50 of 12.70 mg/ml and EC50 10.4 μg/ml, respectively. The antioxidant activity was confirmed by the presence of reducing potential of these polysaccharides. The effect of these polymers on the inflammatory process was tested using the carrageenan or histamine-induced paw edema model and the sodium thioglycolate or zymosan-induced model. The polysaccharides were effective in reducing edema (73% at 50 mg/kg) and cell infiltrate (37% at 10 mg/kg) in both inflammation models tested. Nitric oxide, a mediator in the inflammatory process, showed a reduction of around 26% at 10 mg/kg of body weight. Analysis of pro- and anti-inflammatory cytokines showed that in the groups treated with polysaccharides from S. nitidum there was an increase in cytokines such as IL-1ra, IL-10, and MIP-1β concomitant with the decrease in INF-γ (75%) and IL-2 (22%). We observed the influence of polysaccharides on the modulation of the expression of nuclear factor κB. Thus, polysaccharides from S. nitidum reduced the expression of NF-κB by up to 64%. The results obtained suggest that NF-κB modulation is one of the possible mechanisms that explain the anti-inflammatory effect of polysaccharides from the fungus S. nitidum.

Efeito de glucanas do fungo Caripia montagnei em modelo de inflamação intestinal induzida por tnbs em ratos Wistar e em células de carcinoma de cólon humano HT-29

Compounds derived from fungi has been the subject of many studies in order to broaden the knowledge of their bioactive potential. Polysaccharides from Caripia montagnei have been described to possess anti-inflammatory and antioxidant properties. In this study, glucans extracted from Caripia montagnei mushroom were chemically characterized and their effects evaluated at different doses and intervals of treatment. It was also described their action on colonic injury in the model of colitis induced by 2,4,6-trinitrobenzene sulfonic acid (TNBS), and its action on cells of the human colon carcinoma (HT-29). Compounds extracted of C. montagnei contain high level of carbohydrates (96%), low content of phenolic compounds (1.5%) and low contamination with proteins (2.5%). The (FT-IR) and (NMR) analysis showed that polysaccharides from this species of mushroom are composed of α- and β-glucans. The colonic damage was evaluated by macroscopic, histological, biochemical and immunologic analyses. The results showed a reduction of colonic lesions in all groups treated with the glucans of Caripia montagnei (GCM). GCM significantly reduced the levels of IL-6 (50 and 75 mg/kg, p < 0.05), a major inflammatory cytokine. Biochemical analyses showed that such glucans acted on reducing levels of alkaline phosphatase (75 mg/kg, p < 0.01), nitric oxide (p < 0.001), and myeloperoxidase (p < 0.001). These results were confirmed microscopically by the reduction of cellular infiltration. The increase of catalase activity suggest a protective effect of GCM on colonic tissue, confirming their anti-inflammatory potential. GCM displayed cytostatic activity against HT-29 cells, causing accumulation of cells in G1 phase, blocking the cycle cell progression. Those glucans also showed ability to modulate the adhesion of HT-29 cells to Matrigel® and reduced the oxidative stress. The antiproliferative activity against HT-29 cells displayed by GCM (p <0.001) can be attributed to its cytostatic activity and induction of apoptosis by GCM

Propriedades antioxidante, anti-hemostástica e antiproliferativa de galactanas sulfatadas da alga vermelha hypnea musciformis (wulfen) j. V. Lamouroux

Marine algae are one of the major sources of biologic compounds. In extracellular matrix of these organisms there are sulfated polysaccharides that functions as structural components and provides protection against dehydration. The fraction 1.0 (F1.0) rich in sulfated galactans obtained from red seaweed Hypnea musciformis was physicochemical characterized and evaluated for pharmacologic activity through antioxidant activity, cytotoxic action on erythrocytes, anticoagulant, stimulatory action under antithrombotic heparan sulfate synthesis and their effects on cell proliferation and cycle cell progression. The main components of F1.0 were carbohydrates (49.70 ± 0.10%) and sulfate (44.59 ± 0.015%), presenting phenolic compounds (4.79 ± 0.016%) and low protein contamination (0.92 ± 0.001%). Fraction 1.0 showed polidisperse profile and signs in infrared analysis in 1262, 1074 and 930, 900 and 850 attributed to sulfate esters S=O bond, presence of a 3,6- anidrogalactose C-O bond, non-sulfated β-D-galactose and a C-O-SO4 bond in galactose C4, respectively. The fraction rich in sulfated galactans exhibited strong antioxidant action under lipid peroxidation assay with IC50 of 0.003 mg/mL. Besides the inhibition of hemolysis induced by H2O2 in erythrocytes treated with F1.0, this fraction did not promote significant cytotoxity under erythrocytes membranes. F1.0 exhibited low anticoagulant activity causing moderate direct inhibition of enzimatic activity of thrombin. This fraction promoted stimulation around of 4.6 times on this synthesis of heparan sulfate (HS) by rabbit aortic endothelial cells (RAEC) in culture when was compared with non treated cells. The fraction of this algae displayed antiproliferative action under RAEC cells causing incresing on cell number on S fase, blocking the cycle cell progression. Thus F1.0 presented cytostatic and no cytotoxic action under this cell lineage. These results suggest that F1.0 from H. musciformis have antioxidant potential which is a great effect for a compound used as food and in food industry which could be an alternative to food industry to prevent quality decay of lipid containing food due to lipid peroxidation. These polysaccharides prevent the lipid peroxidation once the fraction in study exhibited strong inhibitory action of this process. Furthermore that F1.0 present strong antithrombotic action promoting the stimulation of antithrombotic HS synthesis by endothelial cells, being important for thrombosis preventing, by its inhibitory action under reactive oxygen species (ROS) in some in vitro methods, being involved in promotion of hypercoagulability state.

Caracterização físico-química e ações farmacológicas hepatoprotetora, antiinflamatória, pró-angiogênica, antioxidante e anticoagulante da fração rica em fucana 0,8FRF 0,8 da alga marrom Lobophora variegata

This study examines the physical and chemical composition and the pharmacological effects of brown seaweed FRF 0.8 Lobophora variegata. Fractionation of the crude extract was done with the concentration of 0.8 volumes of acetone, obtaining the FRF 0.8. The physicochemical characterization showed that it was a fucana sulfated. Anti-inflammatory activity was assessed by paw edema model by the high rates of inhibition of the edema and the best results were in the fourth hour after induction (100 ± 1.4% at the dose of 75 mg / kg) and by the strong inhibitory activity of the enzyme myeloperoxidase (91.45% at the dose of 25 mg / kg). The hepataproteção was demonstrated by measurements of enzymatic and metabolic parameters indicative of liver damage, such as bilirubin (reduction in 68.81%, 70.68% and 68.21% for bilirubin total, direct and indirect, respectively at a dose of 75 mg / kg), ALT, AST and γ-GT (decrease of 76.93%, 44.58% and 50% respectively at a dose of 75 mg / kg) by analysis of histological slides of liver tissue, confirming that hepatoprotective effect the polymers of carbohydrates, showing a reduction in tissue damage caused by CCl4 and the inhibition of the enzyme complex of cytochrome P 450 (increasing sleep time in 54.6% and reducing the latency time in 71.43%). The effectiveness of the FRF 0.8 angiogenesis was examined in chorioallantoic membrane (CAM) of fertilized eggs, with the density of capillaries evaluated and scored, showing an effect proangigênico at all concentrations tested FRF (10 mg- 1000 mg). The FRF showed antioxidant activity on free radicals (by inhibiting Superoxide Radical in 55.62 ± 2.10%, Lipid Peroxidation in 100.15 ± 0.01%, Hydroxyl Radical in 41.84 ± 0.001% and 71.47 Peroxide in ± 2.69% at concentration of 0.62 mg / mL). The anticoagulant activity was observed with prolongation of activated partial thromboplastin time (aPTT) at 50 mg (> 240 s), showing that its action occurs in the intrinsic pathway of the coagulation cascade. Thus, our results indicate that these sulfated polysaccharides are an important pharmacological target

Lectina da esponja marinha Tedania ignis: purificação, caracterização e interação com leishmanias

Lectin obtained from the marine sponge Tedania ignis was purified and characterized by extraction of soluble proteins (crude extract) in 50mM Borax, pH 7.5. The purification procedure was carried out by crude extract precipitation with ammonium sulfate 30% (FI). The precipitated was resuspended in the same buffer and fractionated with acetone 1.0 volume (F1.0). A lectin was purified from this specific fraction by using an affinity chromatography Sepharose 6B. This lectin preferentially agglutinated human erythrocytes from B type previously treated with papain enzyme. The hemagglutinating activity lectin was dependent of divalent Mn2+ cation and was inhibited by the carbohydrates galactose, xylose and fructose. SDS-PAGE analysis indicated a molecular mass of the lectin around 45 kDa. This protein showed stability until 40°C for 1 h. Further, it showed activity between pH 2.5 and 11.5, with an enhanced activity at pH 7.5. Leishmania chagasi promastigotes stained with Coomassie brilliant blue R-250 were agglutinated by F1,0 and in the presence of galactose this interaction was abolished. These results show that this lectin could be implicated in defense procedures and it will can be used as biological tools in studies with this protozoon