Long-term supplementation with phenolic compounds from jaboticaba (Plinia jaboticaba (Vell.) Berg) reduces adiposophaty and improves glucose, lipid, and energy metabolism.

Obesity is a critical public health problem worldwide that has been associated to non-communicable diseases (NCD), such as type 2 diabetes (T2DM), non-alcoholic fatty lipid diseases (NAFLD) and inflammatory diseases. Polyphenols from several food sources have been studied as one option against these health problems. Sabara jaboticaba (Plinia jaboticaba (Vell.) Berg) is a Brazilian berry rich in ellagic acid derivatives and anthocyanins. Here we investigated the effects of a phenolic-rich extract from Sabara jaboticaba (PEJ) in a diet-induced obesity animal model. PEJ at two doses, 50 mg gallic acid equivalent (GAE)/kg body weight (BW) and 100 mg GAE/kg BW, were administered by daily gavage to obese C57BL/6J mice for 14 weeks. PEJ prevented the excessive body weight and adiposity, adipocyte hypertrophy, inflammation, hyperglycemia, glucose intolerance, insulin resistance, hypercholesterolemia, and hepatic lipid accumulation, as well as increased energy expenditure. In conclusion, polyphenols from Sabara jaboticaba presented several powerful therapeutic properties relevant for fighting obesity and associated health problems.

Response surface optimization of phenolic compounds from jabuticaba (Myrciaria cauliflora [Mart.] O.Berg) seeds: Antioxidant, antimicrobial, antihyperglycemic, antihypertensive and cytotoxic assessments.

The aim of this study was to evaluate the effects of different solvents and maximize the extraction of bioactive compounds from jabuticaba (Myrciaria cauliflora) seeds. In general, the solvent system composed of water and propanone (52:48 v/v) modified the extract polarity and increased extraction yield of bioactive compounds. The optimized extract presented antioxidant capacity measured by different chemical and biological assays. The optimized extract exerted antiproliferative and cytotoxic effects against A549 and HCT8 cells, antimicrobial and antihemolytic effects, inhibited α-amylase/α-glucosidase activities and presented in vitro antihypertensive effect. Nonetheless, the optimized extract showed no cytotoxicity in a human cell model (IMR90). Vescalagin, castalagin and ellagic acid were the major phenolic compounds in the optimized extract. Our results show that jabuticaba seed may be a potential ingredient for the development of potentially functional foods.

Clitoria ternatea L. petal bioactive compounds display antioxidant, antihemolytic and antihypertensive effects, inhibit α-amylase and α-glucosidase activities and reduce human LDL cholesterol and DNA induced oxidation.

The purpose of this study was to use a statistical approach to optimise the experimental conditions regarding the extraction of bioactive compounds, and to analyse the in vitro functional properties of crude lyophilized extracts (CLE) and partially purified (PPE) extracts of Clitoria ternatea petals. The results showed that the factors of temperature and time influenced the extraction of phenolic compounds, antioxidant activity and the physicochemical parameters. Simultaneous optimisation showed that the same levels of bioactive compounds were extracted when using temperatures from 11.7 to 68.3 °C and times from 8.47 to 51.12 min. Principal component analysis revealed the experimental conditions that provided the extraction producing the highest level of phenolic content (40 °C/30 min). The CLE showed antimicrobial activity; protective effect against hemolysis of erythrocytes; inhibition of α-amylase, α-glucosidase and angiotensin-I-converting (ACE-I) enzymes; and inhibition of lipid peroxidation. The CLE and PPE demonstrated oxygen radical absorption capacity; inhibition of DNA strand scission; inhibition of LDL cholesterol oxidation; intracellular antioxidant activity against reactive oxygen species (>100 µg/mL); and no cytotoxicity (IC50, GI50 and LC50 > 900 µg/mL) against A549, HCT8 and IMR90 cell lines.

Impact of combining acerola by-product with a probiotic strain on a gut microbiome model.

In this study, we first investigated the survival of three probiotic strains, individually and combined with acerola by-product during simulated gastrointestinal conditions. Next, we investigated the effects of acerola by-product combined with Bifidobacterium longum BB-46 on a gut microbiota model (SHIME®). Chemical composition, total phenolic compounds, antioxidant activity of the acerola by-product and microbial counts, denaturing gradient gel electrophoresis (DGGE), ammonium ions ( NH4+ ) and short-chain fatty acids (SCFAs) analysis of the SHIME® samples were performed. Acerola by-product revealed high protein and fibre, reduced lipid contents, and showed to be an excellent source of total phenolic compounds with high in vitro antioxidant activity. A decreased amount of NH4+ in the ascending colon and an increase (p < .05) in SCFAs were observed in the three regions of colon during treatment with BB-46 and acerola by-product. BB-46 combined with acerola by-product showed positive effects on the gut microbiota metabolism in SHIME® model.

Effect of clarified Brazilian native fruit juices on postprandial glycemia in healthy subjects.

Brazilian native fruits have been shown as excellent sources of polyphenols which are associated with multiple biological activities including inhibition of carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase. Postmeal blood glucose elevations and high glycemic index diets can play a major role in the development of type 2 diabetes, therefore alternative approaches to reduce postprandial hyperglycemia are of growing interest in order to reduce diabetes risk. Here we investigated the effect of six Brazilian native clarified fruit juices from Amazon, Savannah and Atlantic Forest biomes on postprandial glycemia after consumption of a carbohydrate meal. For this, 23 healthy subjects were selected to consume seven meal tests, with a 1-week interval among them, consisting in 50g white bread plus 300mL of water (control) or cambuci, cagaita, maracujá-alho, cupuaçu, camu-camu and jaboticaba clarified fruit juices. The results showed that serum glucose concentrations were significantly lower after consumption of cambuci, cagaita, camu-camu and jaboticaba juices, whereas maracujá-alho and cupuaçu juices did not decrease the amount of glucose absorbed, compared to control (p<0.05). In addition, cagaita, cambuci, cupuaçu and jaboticaba juices increased the oxygen radical absorbance capacity in plasma, whereas all juices augmented the ferric reducing ability of plasma, except for cambuci (p<0.05). These results indicate that juices from Brazilian native fruits may be considered as adjuvant treatment for reduction of postprandial glycemia in healthy subjects.

Antioxidant effects of proanthocyanidin-rich natural extracts from grape seed and cupuassu on gastrointestinal mucosa.

BACKGROUND: The gastrointestinal tract (GI) is constantly exposed to reactive species released by the GI tract itself, and those present in food and beverages. Phenolic compounds may help in protecting the GI tract against damage produced by the reactive species. In this paper we have analyzed the effects of a grape seed proanthocyanidin extract (GSPE) on reactive oxygen species (ROS) production in two different intestinal cell types: the absorptive cell line Caco-2 and the enteroendocrine cell line STC-1. RESULTS: We show that GSPE prevents tert-butylhydroperoxide-induced oxidative stress in both cell lines, and that the effects are dose and time dependent. We have also analyzed whether GSPE has any in vivo effect, and found that 25 mg kg(-1) body weight cannot counteract the increase in intestinal ROS induced by the cafeteria diet. However, an acute (1 h) treatment of 1 g GSPE kg(-1) body weight reduced ROS in fasted animals and also decreased ROS induction by food. These effects were found only after a short-term treatment. Furthermore, we have compared the in vitro GSPE effects with those of another proanthocyanidin-rich extract from cupuassu seeds, though it has compounds with different structures. Cupuassu extract also shows antioxidant effects in both cell types, which suggests different mechanisms from those of GSPE. CONCLUSION: Natural proanthocyanidin-rich extracts have an antioxidant effect in the GI tract, acting on absorptive cells and enterohormone-secreting cells, although the effects depend on the dose and period of treatment. © 2015 Society of Chemical Industry.

Aqueous extract of Rosmarinus officinalis L. inhibits neutrophil influx and cytokine secretion.

Rosmarinus officinalis L. phenolic compounds have attracted considerable attention because of their antioxidant and antimicrobial properties, including its ability to treat inflammatory disorders. In this work, we investigated the in vivo and in vitro effects of R. officinalis aqueous extract on neutrophil trafficking from the blood into an inflamed tissue, on cell-derived secretion of chemical mediators, and on oxidative stress. Anti-inflammatory activity was investigated using carrageenan-induced inflammation in the subcutaneous tissue of male Wistar rats orally treated with the R. officinalis extract (100, 200, or 400 mg/kg). The leukocyte influx (optical microscopy), secretion of chemical mediators (prostaglandin E2 (PGE2), TNF-α, interleukin 6 (IL-6), leukotriene B4 (LTB4), and cytokine-induced neutrophil chemoattractant 1 by enzyme-linked immunosorbent assay), and the anti-oxidative profile (super oxide dismutase (SOD), glutathione peroxidase, and thiobarbituric acid reactive substance (TBARS) spectrophotometry) were quantified in the inflamed exudate. N-Formyl-methionine-leucine-phenylalanine-induced chemotaxis, lipopolysaccharide-induced NO2 (-) production (Greiss reaction), and adhesion molecule expression (flow cytometry) were in vitro quantified using oyster glycogen recruited peritoneal neutrophils previous treated with the extract (1, 10, or 100 µg/mL). Animals orally treated with phosphate-buffered saline and neutrophils incubated with Hank's balanced salt solution were used as control. R. officinalis extract oral treatment caused a dose-dependent reduction in the neutrophil migration as well as decreased SOD, TBARS, LTB4, PGE2, IL-6, and TNF-α levels in the inflamed exudate. In vitro treatment with R. officinalis decreased neutrophil chemotaxis, NO2 (-) production, and shedding of L-selectin and ß2 integrin expressions. Results here presented show that R. officinalis aqueous extract displays important in vivo and in vitro anti-inflammatory actions by blocking pathways of neutrophil migration and secretion, suggesting its therapeutic application to acute inflammatory reactions.

Antioxidant capacity and mineral content of pulp and peel from commercial cultivars of citrus from Brazil.

Four Citrus species (C. sinensis, cvs. Pera and Lima; C. latifolia Tanaka cv. Tahiti; C. limettioides Tanaka cv. Sweet lime and C. reticulate, cv. Ponkan) grown in Brazil were characterised in relation to contents of minerals, ascorbic acid, total polyphenols and antioxidant capacity of pulps and peels. In general, the peels demonstrated significantly higher contents of all compounds than the pulps (p<0.05), with the exception of the Pera orange pulp that presented the highest acid ascorbic content (68 mg/100 ml), while the Tahiti lime peel presented the lowest (8 mg/100 g). Citrus showed high levels of potassium, calcium and magnesium, and the peels were considered sources of these minerals. The Ponkan mandarin peel presented the highest antioxidant capacity. The antioxidant capacity of citrus was correlated both to vitamin C and phenolics. Aside from citrus pulps, the peels are also good sources of bioactive compounds and minerals, and can be explored for their health promoting values in food products.

Evaluation of antiproliferative, anti-type 2 diabetes, and antihypertension potentials of ellagitannins from strawberries (Fragaria × ananassa Duch.) using in vitro models.

Strawberries represent the main source of ellagic acid derivatives in the Brazilian diet, corresponding to more than 50% of all phenolic compounds found in the fruit. There is a particular interest in the determination of the ellagic acid content in fruits because of possible chemopreventive benefits. In the present study, the potential health benefits of purified ellagitannins from strawberries were evaluated in relation to the antiproliferative activity and in vitro inhibition of α-amylase, α-glucosidase, and angiotensin I-converting enzyme (ACE) relevant for potential management of hyperglycemia and hypertension. Therefore, a comparison among ellagic acid, purified ellagitannins, and a strawberry extract was done to evaluate the possible synergistic effects of phenolics. In relation to the antiproliferative activity, it was observed that ellagic acid had the highest percentage inhibition of cell proliferation. The strawberry extract had lower efficacy in inhibiting the cell proliferation, indicating that in the case of this fruit there is no synergism. Purified ellagitannins had high α-amylase and ACE inhibitory activities. However, these compounds had low α-glucosidase inhibitory activity. These results suggested that the ellagitannins and ellagic acid have good potential for the management of hyperglycemia and hypertension linked to type 2 diabetes. However, further studies with animal and human models are needed to advance the in vitro assay-based biochemical rationale from this study.

Chemical composition and antioxidant/antidiabetic potential of Brazilian native fruits and commercial frozen pulps.

Foods provide essential and bioactive compounds with health-promoting properties such as antioxidant, anti-inflammatory, and hypocholesterolemic activities, which have been related to vitamins A, C, and E and phenolic compounds such as flavonoids. Therefore, the aim of this work was to identify potential sources of bioactive compounds through the determination of flavonoids and ellagic acid contents and the in vitro antioxidant capacity and alpha-glucosidase and alpha-amylase inhibitory activities of Brazilian native fruits and commercial frozen pulps. Camu-camu, cambuci, uxi, and tucuma and commercial frozen pulps of cambuci, cagaita, coquinho azedo, and araca presented the highest antioxidant capacities. Cambuci and cagaita exhibited the highest alpha-glucosidase and alpha-amylase inhibitory activities. Quercetin and kaempferol derivatives were the main flavonoids present in most of the samples. Ellagic acid was detected only in umbu, camu-camu, cagaita, araca, and cambuci. According to the results, native Brazilian fruits can be considered as excellent sources of bioactive compounds.

Evaluation of indigenous grains from the Peruvian Andean region for antidiabetes and antihypertension potential using in vitro methods.

The health-relevant functionality of 10 thermally processed Peruvian Andean grains (five cereals, three pseudocereals, and two legumes) was evaluated for potential type 2 diabetes-relevant antihyperglycemia and antihypertension activity using in vitro enzyme assays. Inhibition of enzymes relevant for managing early stages of type 2 diabetes such as hyperglycemia-relevant alpha-glucosidase and alpha-amylase and hypertension-relevant angiotensin I-converting enzyme (ACE) were assayed along with the total phenolic content, phenolic profiles, and antioxidant activity based on the 1,1-diphenyl-2-picrylhydrazyl radical assay. Purple corn (Zea mays L.) (cereal) exhibited high free radical scavenging-linked antioxidant activity (77%) and had the highest total phenolic content (8 +/- 1 mg of gallic acid equivalents/g of sample weight) and alpha-glucosidase inhibitory activity (51% at 5 mg of sample weight). The major phenolic compound in this cereal was protocatechuic acid (287 +/- 15 microg/g of sample weight). Pseudocereals such as Quinoa (Chenopodium quinoa Willd) and Kañiwa (Chenopodium pallidicaule Aellen) were rich in quercetin derivatives (1,131 +/- 56 and 943 +/- 35 microg [expressed as quercetin aglycone]/g of sample weight, respectively) and had the highest antioxidant activity (86% and 75%, respectively). Andean legumes (Lupinus mutabilis cultivars SLP-1 and H-6) inhibited significantly the hypertension-relevant ACE (52% at 5 mg of sample weight). No alpha-amylase inhibitory activity was found in any of the evaluated Andean grains. This in vitro study indicates the potential of combination of Andean whole grain cereals, pseudocereals, and legumes to develop effective dietary strategies for managing type 2 diabetes and associated hypertension and provides the rationale for animal and clinical studies.

Potential of Ginkgo biloba L. leaves in the management of hyperglycemia and hypertension using in vitro models.

Leaves from four different Ginkgo biloba L. trees (1 and 2--females; 3 and 4--males), grown at the same conditions, were collected during a period of 5 months (from June to October, 2007). Water and 12% ethanol extracts were analyzed for total phenolics content, antioxidant activity, phenolic profile, and the potential in vitro inhibitory effects on alpha-amylase, alpha-glucosidase, and Angiotensin I-Converting Enzyme (ACE) enzymes related to the management of diabetes and hypertension. The results indicated a significant difference among the trees in all functional benefits evaluated in the leaf extracts and also found important seasonal variation related to the same functional parameters. In general, the aqueous extracts had higher total phenolic content than the ethanolic extracts. Also, no correlation was found between total phenolics and antioxidant activity. In relation to the ACE inhibition, only ethanolic extracts had inhibitory activity.

Evaluation of antihyperglycemia and antihypertension potential of native Peruvian fruits using in vitro models.

Local food diversity and traditional crops are essential for cost-effective management of the global epidemic of type 2 diabetes and associated complications of hypertension. Water and 12% ethanol extracts of native Peruvian fruits such as Lucuma (Pouteria lucuma), Pacae (Inga feuille), Papayita arequipeña (Carica pubescens), Capuli (Prunus capuli), Aguaymanto (Physalis peruviana), and Algarrobo (Prosopis pallida) were evaluated for total phenolics, antioxidant activity based on 2, 2-diphenyl-1-picrylhydrazyl radical scavenging assay, and functionality such as in vitro inhibition of alpha-amylase, alpha-glucosidase, and angiotensin I-converting enzyme (ACE) relevant for potential management of hyperglycemia and hypertension linked to type 2 diabetes. The total phenolic content ranged from 3.2 (Aguaymanto) to 11.4 (Lucuma fruit) mg/g of sample dry weight. A significant positive correlation was found between total phenolic content and antioxidant activity for the ethanolic extracts. No phenolic compound was detected in Lucuma (fruit and powder) and Pacae. Aqueous extracts from Lucuma and Algarrobo had the highest alpha-glucosidase inhibitory activities. Papayita arequipeña and Algarrobo had significant ACE inhibitory activities reflecting antihypertensive potential. These in vitro results point to the excellent potential of Peruvian fruits for food-based strategies for complementing effective antidiabetes and antihypertension solutions based on further animal and clinical studies.

Absorption and metabolism of cyanidin-3-glucoside and cyanidin-3-rutinoside extracted from wild mulberry (Morus nigra L.) in rats.

The mechanism of uptake of anthocyanins (as well as the type) from food in the intestine is not clear. Anthocyanin-rich extract from wild mulberry, composed of cyanidin-3-glucoside (79%) and cyanidin-3-rutinoside (cy-3-rut) (19%), was orally administered to Wistar rats, and their concentrations were determined in plasma, kidney, and the gastrointestinal (GI) tract. The 2 glycosylated forms showed maximum concentration at 15 minutes after oral administration, both in plasma and kidney. The cyanidin-3-glucoside and cy-3-rut were found in plasma as glucuronides, as sulfates of cyanidin, and as unchanged forms. The area under the curve of concentration vs time (AUC(0-8h)) was 2.76 +/- 0.88 microg hour/mL and 9.74 +/- 0.75 microg hour/g for plasma and kidney, respectively. In spite of the low absorption, the increase in plasma anthocyanin level resulted in a significant increase in antioxidant capacity (P < .05). In the GI tract (stomach and small and large intestines), cyanidin glycosides were found unchanged, but a low amount of the aglycone form was present. Anthocyanin glycosides were no longer detected in the GI tract after 8 hours of administration. In vitro fermentation showed that the 2 cyanidin glycosides were totally metabolized by the rat colonic microflora, explaining their disappearance. In addition, the 2 products of their degradation, cyanidin and protocatechuic acid, were not detected in plasma and probably do not influence plasma antioxidant capacity. As found by the everted sac model, anthocyanins were transported across the enterocyte by the sodium-dependent glucose transporter.

Antidiabetes and antihypertension potential of commonly consumed carbohydrate sweeteners using in vitro models.

Commonly consumed carbohydrate sweeteners derived from sugar cane, palm, and corn (syrups) were investigated to determine their potential to inhibit key enzymes relevant to Type 2 diabetes and hypertension based on the total phenolic content and antioxidant activity using in vitro models. Among sugar cane derivatives, brown sugars showed higher antidiabetes potential than white sugars; nevertheless, no angiotensin I-converting enzyme (ACE) inhibition was detected in both sugar classes. Brown sugar from Peru and Mauritius (dark muscovado) had the highest total phenolic content and 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity, which correlated with a moderate inhibition of yeast alpha-glucosidase without showing a significant effect on porcine pancreatic alpha-amylase activity. In addition, chlorogenic acid quantified by high-performance liquid chromatography was detected in these sugars (128 +/- 6 and 144 +/- 2 microg/g of sample weight, respectively). Date sugar exhibited high alpha-glucosidase, alpha-amylase, and ACE inhibitory activities that correlated with high total phenolic content and antioxidant activity. Neither phenolic compounds or antioxidant activity was detected in corn syrups, indicating that nonphenolic factors may be involved in their significant ability to inhibit alpha-glucosidase, alpha-amylase, and ACE. This study provides a strong biochemical rationale for further in vivo studies and useful information to make better dietary sweetener choices for Type 2 diabetes and hypertension management.

Avaliação do teor de isoflavonas de "suplementos nutricionais à base de soja" / Isoflavone content of soy dietary supplements

Devido aos possíveis efeitos benéficos, diversos produtos à base de soja (gérmen, extrato), na forma de cápsulas ou comprimidos, surgiram recentemente no mercado como fontes de isoflavonas. Neste trabalho avaliaram-se o teor e o perfil de isoflavonas dos produtos comercializados em drogarias e farmácias locais (São Paulo), para verificar se estavam de acordo com o especificado pelos fabricantes. A determinação foi realizada através de cromatografia líquida de alta eficiência com detetor com arranjo de diodos, de acordo com Genovese & lajolo (2001b). Os resultados mostraram que os produtos à base de soja apresentam teor de isoflavonas muito abaixo do valor indicado nos rótulos, entre 27 por cento e 86 por cento a menos...