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Increased postprandial lipemia is a cardiovascular disease (CVD) risk factor. Carob fruit extract (CFE) contains condensed tannins, and their intake has been inversely related to CVD. The objective was to evaluate the in vitro pancreatic lipase activity in the presence of CFE and the in vivo effect of CFE on postprandial lipemia of healthy Wistar rats in acute and subchronic digestibility studies and to relate it with changes in fat digestion and absorption. CFE significantly reduced pancreatic lipase activity. A peak delay and a dose-dependent decrease in plasma triglyceride and cholesterol areas under the curve were observed, effects that increased after the subchronic treatment. The levels of nondigested, nonabsorbed triglycerides of the remaining intestinal lumen fat were significantly higher in the maximum dose of CFE administrated versus the control (P < 0.05). This study demonstrates for the first time the hypolipemic properties of CFE from the first administration, modifying postprandial lipemia by reducing the extents of fat digestion and absorption., Spanish Ministry of Education, Culture and Sports, Depto. de Farmacología, Farmacognosia y Botánica, Fac. de Farmacia, TRUE, pub

The mealworm (Tenebrio molitor Linnaeus 1758) is gaining importance as one of the most popular edible insects. Studies focusing on its bioactivities are increasing, although alternative forms of consumption other than the whole insect or flour, such as bioactive non-protein extracts, remain underexplored. Furthermore, the incidence of metabolic syndrome-related pathologies keeps increasing, hence the importance of seeking novel natural sources for reducing the impact of certain risk factors. The aim was to study the potential of a non-protein mealworm extract on metabolic syndrome-related pathologies, obtained with ethanol:water (1:1, v/v) by ultrasound-assisted extraction. We characterized the extract by gas-chromatography mass-spectrometry and assessed its hypolipidemic potential, its ability to scavenger free radicals, to attenuate the inflammatory response in microglial cells, to affect mitochondrial respiration and to enhance insulin sensitivity in mouse hepatocytes. The extract contained fatty acids, monoglycerides, amino acids, certain acids and sugars. The mealworm extract caused a 30% pancreatic lipase inhibition, 80% DPPH· scavenging activity and 55.9% reduction in the bioaccessibility of cholesterol (p = 0.009). The extract was effective in decreasing iNOS levels, increasing basal, maximal and ATP coupled respiration as well as enhancing insulin-mediated AKT phosphorylation at low insulin concentrations (p < 0.05). The potential of a non-protein bioactive mealworm extract against metabolic syndrome-related pathologies is shown, although further studies are needed to elucidate the mechanisms and relationship with compounds., [Simple Summary] Among edible insects, mealworm has gained attention due to its proven beneficial effects; however, mealworm products other than flour, such as concentrated forms or extracts different to proteins, are still rare. This novel food source can have a positive impact on multiple diseases such as via the metabolic syndrome. Our objective was to describe the composition of a mealworm extract and study its effect on metabolic syndrome-related pathologies. The extract interfered with the absorption of cholesterol and partially blocked the digestion of fats. It also reduced the inflammatory response, enhanced the sensitivity to insulin and showed strong antioxidant potential. Mealworm extract might be an interesting candidate for ameliorating the risk factors associated with the metabolic syndrome.

Acacia concinna (Willd.) DC. is a medicinal plant sourced mainly from Southeast Asia. The pods of Acacia concinna (A. concinna) are a potential candidate to treat or prevent obesity; however, these medicinal attributes have not been examined in detail. In this study, the anti-obesogenic compounds in A. concinna pods were investigated. Chromatographic separation of the pod extract guided by pancreatic lipase inhibitory activity led to the isolation of saponins. Decomposition analysis of the saponins revealed their chemical composition to be acacic acid, monoterpenes, and five types of sugars (glucose, xylose, rhamnose, quinovose, arabinose). The predicted structures of the saponins from decomposition analysis were confirmed by LC-MS analysis, showing that these saponins are mixture of various derivatives of monoterpenes and sugar units. These saponins inhibited pancreatic lipase activity strongly with an IC50 of 7.9 mu g/mL, and reduced lipid accumulation in 3T3-L1 adipocytes at 6.3 mu g/mL. The saponins also enhanced lipolysis of 3T3-L1 adipocytes at 3.1 or 6.3 mu g/mL by mediating the activity of protein kinase A and extracellular signal-regulated kinase pathways, suggesting that this mechanism is partly responsible for the observed reduction of lipid content in adipocytes. The results underline A. concinna as a potential source of the anti-obesogenic candidates for the future treatment and prevention of obesity.

Acacia concinna (Willd.) DC. is a medicinal plant sourced mainly from Southeast Asia. The pods of Acacia concinna (A. concinna) are a potential candidate to treat or prevent obesity; however, these medicinal attributes have not been examined in detail. In this study, the anti-obesogenic compounds in A. concinna pods were investigated. Chromatographic separation of the pod extract guided by pancreatic lipase inhibitory activity led to the isolation of saponins. Decomposition analysis of the saponins revealed their chemical composition to be acacic acid, monoterpenes, and five types of sugars (glucose, xylose, rhamnose, quinovose, arabinose). The predicted structures of the saponins from decomposition analysis were confirmed by LC-MS analysis, showing that these saponins are mixture of various derivatives of monoterpenes and sugar units. These saponins inhibited pancreatic lipase activity strongly with an IC50 of 7.9 mu g/mL, and reduced lipid accumulation in 3T3-L1 adipocytes at 6.3 mu g/mL. The saponins also enhanced lipolysis of 3T3-L1 adipocytes at 3.1 or 6.3 mu g/mL by mediating the activity of protein kinase A and extracellular signal-regulated kinase pathways, suggesting that this mechanism is partly responsible for the observed reduction of lipid content in adipocytes. The results underline A. concinna as a potential source of the anti-obesogenic candidates for the future treatment and prevention of obesity.

Acacia concinna (Willd.) DC. is a medicinal plant sourced mainly from Southeast Asia. The pods of Acacia concinna (A. concinna) are a potential candidate to treat or prevent obesity; however, these medicinal attributes have not been examined in detail. In this study, the anti-obesogenic compounds in A. concinna pods were investigated. Chromatographic separation of the pod extract guided by pancreatic lipase inhibitory activity led to the isolation of saponins. Decomposition analysis of the saponins revealed their chemical composition to be acacic acid, monoterpenes, and five types of sugars (glucose, xylose, rhamnose, quinovose, arabinose). The predicted structures of the saponins from decomposition analysis were confirmed by LC-MS analysis, showing that these saponins are mixture of various derivatives of monoterpenes and sugar units. These saponins inhibited pancreatic lipase activity strongly with an IC50 of 7.9 mu g/mL, and reduced lipid accumulation in 3T3-L1 adipocytes at 6.3 mu g/mL. The saponins also enhanced lipolysis of 3T3-L1 adipocytes at 3.1 or 6.3 mu g/mL by mediating the activity of protein kinase A and extracellular signal-regulated kinase pathways, suggesting that this mechanism is partly responsible for the observed reduction of lipid content in adipocytes. The results underline A. concinna as a potential source of the anti-obesogenic candidates for the future treatment and prevention of obesity.

Acacia concinna (Willd.) DC. is a medicinal plant sourced mainly from Southeast Asia. The pods of Acacia concinna (A. concinna) are a potential candidate to treat or prevent obesity; however, these medicinal attributes have not been examined in detail. In this study, the anti-obesogenic compounds in A. concinna pods were investigated. Chromatographic separation of the pod extract guided by pancreatic lipase inhibitory activity led to the isolation of saponins. Decomposition analysis of the saponins revealed their chemical composition to be acacic acid, monoterpenes, and five types of sugars (glucose, xylose, rhamnose, quinovose, arabinose). The predicted structures of the saponins from decomposition analysis were confirmed by LC-MS analysis, showing that these saponins are mixture of various derivatives of monoterpenes and sugar units. These saponins inhibited pancreatic lipase activity strongly with an IC50 of 7.9 mu g/mL, and reduced lipid accumulation in 3T3-L1 adipocytes at 6.3 mu g/mL. The saponins also enhanced lipolysis of 3T3-L1 adipocytes at 3.1 or 6.3 mu g/mL by mediating the activity of protein kinase A and extracellular signal-regulated kinase pathways, suggesting that this mechanism is partly responsible for the observed reduction of lipid content in adipocytes. The results underline A. concinna as a potential source of the anti-obesogenic candidates for the future treatment and prevention of obesity.

The production of specific insect extracts with bioactive properties for human health is an emerging and innovative field for the edible insects industry, but there are unexplored extraction factors that might modulate the bioactivity of the extracts. Ultrasound-assisted extracts from T. molitor and H. illucens were produced. Effects of defatting pre-treatment and extraction solvent were evaluated on extraction yield, antioxidant activity and pancreatic lipase inhibitory effect. Chemical characterisation of defatted extracts from H. illucens was performed by GC-MS-FID. Non-defatted extracts showed higher extraction yields. Defatted extracts had similar extraction yields (around 3%). Defatted extracts had higher antioxidant activity, T. molitor being stronger than H. illucens. Antioxidant activity of T. molitor methanol extract was higher than the rest of solvents. Aqueous ethanol improved the antioxidant activity of H. illucens extracts. All extracts inhibited lipase, but no significant effect of defatting and solvent was observed for T. molitor. A significant higher inhibitory activity was observed for H. illucens, the strongest being defatted 100% and 70% ethanol H. illucens extracts. H. illucens extracts contained free amino acids and disaccharides, together with minor fractions of lipids, sterols and organic acids. These results evidence the potential of extracts obtained from edible insects as antioxidants and inhibitors of the pancreatic lipase, a simultaneous multibioactivity that might be favoured by the defatting pre-treatment of the samples and the solvent of extraction.

In Algeria, Fraxinus angustifolia Vahl (Oleaceae) is a prominent ingredient for the treatment of inflammatory diseases caused by oxidative stress. This study aimed to make a comparison between the phenolic compound compositions of the ethanolic and aqueous extracts (decoction and infusion) of this plant and to test the antioxidant, cytotoxic and anti-pancreatic lipase activities of the ethanolic extracts from the leaf and bark. The identification and quantification of phenolic compounds was carried out by HPLC-DAD-MS and the antioxidant activity was assessed according to three methods: Ferric Reducing Antioxidant Power (FRAP), 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) free radical scavenging activity and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) scavenging activity. The cytotoxic effect was investigated using the human colon adenocarcinoma cell line HCT-116; while pancreatic lipase inhibitory activity was examined using 4-nitrophenyl butyrate (NPB) as a substrate. A large variety of phenolic compounds were detected and the content of the leaf was much higher than that of the bark. The ethanolic extracts from the leaf had a higher antioxidant capacity than those of the bark, however, the latter showed greater antilipase activity and cytotoxicity than the former. These results suggest that this plant may be an important source of active compounds with a variety of biological activities which justify its use in traditional medicine.

The aim of this study was to determine the pancreatic lipase (PL) inhibitory effect of cocoa protein (CP) hydrolysates (CPH) using in silico and in vitro approaches, and an in vivo high-fat diet (HF) obese rat model. The results showed better theoretical affinity on PL for cocoa peptides EEQR, GGER, QTGVQ, and VSTDVNIE released from vicilin and albumins (−6.5, −6.3, −6.2, and −6.1 kcal/mol, respectively). Absorption, distribution, metabolism, and excretion (ADMET) prediction showed the human intestinal absorption (HIA) capacity of orlistat and eight cocoa peptides, demonstrating that they presented a low probability of toxicity with values lower than 0.6, while the orlistat has a high probability of hepatotoxicity with a mean value of 0.9. CPH (degree of hydrolysis of 55%) inhibited PL with an IC50 (concentration needed to inhibit 50% of enzyme activity) value of 1.38 mg/mL. The intragastric administration of 150 mg CP/kg/day to rats increased total lipids and triglycerides excretion in feces, ranging from 11% to 15% compared to the HF-diet. The HF + CP-diet also significantly decreased (p < 0.05) the apparent rate of fat absorption compared with the HF group. These results suggest that CP has anti-obesity potential by inhibiting PL, thus helping to prevent the development of non-communicable diseases.

The main objective of this study was the formulation of food-grade water-in-oil (W/O) nano-dispersions based mainly on medium or long-chain triglycerides. Two types of dispersions were formulated and structurally compared, namely emulsions and microemulsions. The systems were used as matrices for encapsulating targeted bioactive molecules with specific characteristics such as antioxidants or peptides. The structural characterization of the formulated systems was investigated using techniques such as Electron Paramagnetic Resonance (EPR) spectroscopy, Dynamic Light Scattering (DLS), Cryogenic Transmission Electron Microscopy (Cryo-TEM) and Small Angle Xray Scattering (SAXS). The existence of swollen inverse micelles was revealed for the case of microemulsions whereas larger droplets still at the nano-scale were observed for the case of emulsions. Structural differences in the presence of the bioactive molecules or induced by the alteration of components were also observed. In order to study the efficacy of the formulations, the proposed loaded systems were assessed either using EPR spectroscopy or Well Diffusion Assay (WDA) depending on the bioactive molecule. It was found that the encapsulated molecules retained their claimed characteristics when encapsulated to the proposed matrices. Finally, some of the formulated dispersions were investigated for their behavior under gastrointestinal (GI) conditions. A two-step digestion model using recombinant Dog Gastric Lipase (rDGL) and Porcine Pancreatic Lipase (PPL) was proposed to simulate lipid hydrolysis in humans. The studies revealed significant decrease of the rDGL specific activity in the presence of the microemulsion while in the presence of lower percent of surfactants (case of emulsion) no alterations were observed.

The main objective of this study was the formulation of food-grade water-in-oil (W/O) nano-dispersions based mainly on medium or long-chain triglycerides. Two types of dispersions were formulated and structurally compared, namely emulsions and microemulsions. The systems were used as matrices for encapsulating targeted bioactive molecules with specific characteristics such as antioxidants or peptides. The structural characterization of the formulated systems was investigated using techniques such as Electron Paramagnetic Resonance (EPR) spectroscopy, Dynamic Light Scattering (DLS), Cryogenic Transmission Electron Microscopy (Cryo-TEM) and Small Angle Xray Scattering (SAXS). The existence of swollen inverse micelles was revealed for the case of microemulsions whereas larger droplets still at the nano-scale were observed for the case of emulsions. Structural differences in the presence of the bioactive molecules or induced by the alteration of components were also observed. In order to study the efficacy of the formulations, the proposed loaded systems were assessed either using EPR spectroscopy or Well Diffusion Assay (WDA) depending on the bioactive molecule. It was found that the encapsulated molecules retained their claimed characteristics when encapsulated to the proposed matrices. Finally, some of the formulated dispersions were investigated for their behavior under gastrointestinal (GI) conditions. A two-step digestion model using recombinant Dog Gastric Lipase (rDGL) and Porcine Pancreatic Lipase (PPL) was proposed to simulate lipid hydrolysis in humans. The studies revealed significant decrease of the rDGL specific activity in the presence of the microemulsion while in the presence of lower percent of surfactants (case of emulsion) no alterations were observed.

The main objective of this study was the formulation of food-grade water-in-oil (W/O) nano-dispersions based mainly on medium or long-chain triglycerides. Two types of dispersions were formulated and structurally compared, namely emulsions and microemulsions. The systems were used as matrices for encapsulating targeted bioactive molecules with specific characteristics such as antioxidants or peptides. The structural characterization of the formulated systems was investigated using techniques such as Electron Paramagnetic Resonance (EPR) spectroscopy, Dynamic Light Scattering (DLS), Cryogenic Transmission Electron Microscopy (Cryo-TEM) and Small Angle Xray Scattering (SAXS). The existence of swollen inverse micelles was revealed for the case of microemulsions whereas larger droplets still at the nano-scale were observed for the case of emulsions. Structural differences in the presence of the bioactive molecules or induced by the alteration of components were also observed. In order to study the efficacy of the formulations, the proposed loaded systems were assessed either using EPR spectroscopy or Well Diffusion Assay (WDA) depending on the bioactive molecule. It was found that the encapsulated molecules retained their claimed characteristics when encapsulated to the proposed matrices. Finally, some of the formulated dispersions were investigated for their behavior under gastrointestinal (GI) conditions. A two-step digestion model using recombinant Dog Gastric Lipase (rDGL) and Porcine Pancreatic Lipase (PPL) was proposed to simulate lipid hydrolysis in humans. The studies revealed significant decrease of the rDGL specific activity in the presence of the microemulsion while in the presence of lower percent of surfactants (case of emulsion) no alterations were observed.

The main objective of this study was the formulation of food-grade water-in-oil (W/O) nano-dispersions based mainly on medium or long-chain triglycerides. Two types of dispersions were formulated and structurally compared, namely emulsions and microemulsions. The systems were used as matrices for encapsulating targeted bioactive molecules with specific characteristics such as antioxidants or peptides. The structural characterization of the formulated systems was investigated using techniques such as Electron Paramagnetic Resonance (EPR) spectroscopy, Dynamic Light Scattering (DLS), Cryogenic Transmission Electron Microscopy (Cryo-TEM) and Small Angle Xray Scattering (SAXS). The existence of swollen inverse micelles was revealed for the case of microemulsions whereas larger droplets still at the nano-scale were observed for the case of emulsions. Structural differences in the presence of the bioactive molecules or induced by the alteration of components were also observed. In order to study the efficacy of the formulations, the proposed loaded systems were assessed either using EPR spectroscopy or Well Diffusion Assay (WDA) depending on the bioactive molecule. It was found that the encapsulated molecules retained their claimed characteristics when encapsulated to the proposed matrices. Finally, some of the formulated dispersions were investigated for their behavior under gastrointestinal (GI) conditions. A two-step digestion model using recombinant Dog Gastric Lipase (rDGL) and Porcine Pancreatic Lipase (PPL) was proposed to simulate lipid hydrolysis in humans. The studies revealed significant decrease of the rDGL specific activity in the presence of the microemulsion while in the presence of lower percent of surfactants (case of emulsion) no alterations were observed.

The main objective of this study was the formulation of food-grade water-in-oil (W/O) nano-dispersions based mainly on medium or long-chain triglycerides. Two types of dispersions were formulated and structurally compared, namely emulsions and microemulsions. The systems were used as matrices for encapsulating targeted bioactive molecules with specific characteristics such as antioxidants or peptides. The structural characterization of the formulated systems was investigated using techniques such as Electron Paramagnetic Resonance (EPR) spectroscopy, Dynamic Light Scattering (DLS), Cryogenic Transmission Electron Microscopy (Cryo-TEM) and Small Angle Xray Scattering (SAXS). The existence of swollen inverse micelles was revealed for the case of microemulsions whereas larger droplets still at the nano-scale were observed for the case of emulsions. Structural differences in the presence of the bioactive molecules or induced by the alteration of components were also observed. In order to study the efficacy of the formulations, the proposed loaded systems were assessed either using EPR spectroscopy or Well Diffusion Assay (WDA) depending on the bioactive molecule. It was found that the encapsulated molecules retained their claimed characteristics when encapsulated to the proposed matrices. Finally, some of the formulated dispersions were investigated for their behavior under gastrointestinal (GI) conditions. A two-step digestion model using recombinant Dog Gastric Lipase (rDGL) and Porcine Pancreatic Lipase (PPL) was proposed to simulate lipid hydrolysis in humans. The studies revealed significant decrease of the rDGL specific activity in the presence of the microemulsion while in the presence of lower percent of surfactants (case of emulsion) no alterations were observed.

A mixture of sphingoid esters was isolated (1.4% w/w) from the molecular distillation of crude squid visceral oil. A preliminary investigation on the bioactivity profile and toxic potential of this residue was carried out by in vitro experiments. No cytotoxicity and a moderate lipase inhibition activity were highlighted.

Tato diplomová práce se zabývala sledováním aktivity pankreatické lipázy a možnostmi jejího ovlivnění. Aktivita pankreatické lipázy byla stanovena v závislosti na teplotě, pH, koncentraci substrátu a přítomnosti karbamátových a salicylanilidových inhibitorů. Mezní rychlost reakce (Vm), Michaelisova konstanta (Km) a hodnota IC50 byly stanoveny spektrofotometrickou metodou. V důsledku různých reakčních podmínek byly získány rozdílné výsledky. Na základě získaných výsledků bylo možné určit, za jakých podmínek je rychlost reakce nejvyšší a jaký inhibitor je nejúčinnější., This thesis dealt with a monitoring of pancreatic lipase activity and possibility of its affection. Pancreatic lipase activity was determined depending of the temperature, pH, concentration of substrate and presence of carbamate and salicylanilide inhibitors. Maximum rate (Vm), the Michaelis constant (Km) and the IC50 were determined using the spectrophotometric method. Consequently for different reaction conditions different results were obtained. Based on the obtained results, it was possible to determine the conditions under which the reaction rate is high, and what is the most effective inhibitor., Katedra biologických a biochemických věd, 1. Prezentace výsledků diplomové práce.2. Diskuze k posudku vedoucího diplomové práce.3. Studentka zodpověděla vaechny dotazy a připomínky k DP.

Dietary triglycerides are hydrolyzed in the small intestine principally by pancreatic lipase. Following uptake by enterocytes and secretion as chylomicrons, dietary lipids are cleared from the bloodstream via lipoprotein lipase. Whereas lipoprotein lipase is inhibited by several proteins including Angiopoietin-like 4 (Angptl4), no endogenous regulator of pancreatic lipase has yet been identified. Here we present evidence that Angptl4 is an endogenous inhibitor of dietary lipid digestion. Angptl4-/- mice were heavier compared to their wild-type counterparts without any difference in food intake, energy expenditure or locomotor activity. However, Angptl4-/- mice showed decreased lipid content in the stools and increased accumulation of dietary triglycerides in the small intestine, which coincided with elevated luminal lipase activity in Angptl4-/- mice. Furthermore, recombinant Angptl4 reduced the activity of pancreatic lipase as well as the lipase activity in human ileostomy output. In conclusion, our data suggest that Angptl4 is an endogenous inhibitor of intestinal lipase activity.

© 2014 Elsevier Ltd. Addition of lutein to dairy products is an alternative that widens the range of foods which could be lutein sources. However, bioaccessibility is an essential aspect to be considered during the development of products with added bioactive substances. We evaluated the in vitro bioaccessibility of lutein esters added to milk and yogurt with different fat contents, and determined the efficiency of enzymatic hydrolysis of the esters during digestion. Bioaccessibility of lutein and efficiency of hydrolysis were significantly lower in skimmed products than semi-skimmed and whole products, indicating that a minimal amount of fat is required to allow micellization and hydrolysis. The efficiency of ester hydrolysis ranged between 12 and 35%, which was attributed to pancreatic lipase. Whole and semi-skimmed samples were shown to be good vehicles for the addition of lutein, since presented bioaccessibility indices (38.3-47.5%) are similar to those found in natural food sources of xanthophylls.

One of the strategies in prevention or treatment of obesity is altering metabolism of lipids by inhibition of dietary fat absorption. The extracts obtained with methanol, water and methanol:water (1:1) from 21 mushroom species were screened as potential sources of pancreatic lipase (PL) inhibitors using a standardised in vitro test. Lepiota procera methanol:water (1:1) extracts showed the highest inhibition activity closely followed by Grifola frondosa, Pleurotus eryngii and Lyophyllum shimeji. Other mushroom strains such as Morchella conica, Marasmius oreades, Lentinula edodes, Amanita ponderosa and Boletus edulis also showed a certain inhibitory activity. However, when the PL inhibitory activity was evaluated using an in vitro digestion model mimicking gut conditions, none of the selected mushroom extracts were able to inhibit PL activity. On the contrary, stimulation of the lipase activity levels was observed and it was not due to endogenous mushroom lipases activities. © 2012 The Authors. International Journal of Food Science and Technology © 2012 Institute of Food Science and Technology.

Rosemary (Rosmarinus officinalis L.) extracts (RE) are natural antioxidants that are used in food, food supplements and cosmetic applications; exert anti-inflammatory and anti-hyperglycaemic effects; and promote weight loss, which can be exploited to develop new preventive strategies against metabolic disorders. Therefore, the aim of the present study was to evaluate the preventive effects of rosemary leaf extract that was standardised to 20 % carnosic acid (RE) on weight gain, glucose levels and lipid homeostasis in mice that had begun a high-fat diet (HFD) as juveniles. The animals were given a low-fat diet, a HFD or a HFD that was supplemented with 500 mg RE/kg body weight per d (mpk). Physiological and biochemical parameters were monitored for 16 weeks. Body and epididymal fat weight in animals on the HFD that was supplemented with RE increased 69 and 79 % less than those in the HFD group. Treatment with RE was associated with increased faecal fat excretion but not with decreased food intake. The extract also reduced fasting glycaemia and plasma cholesterol levels. In addition, we evaluated the inhibitory effects of RE in vitro on pancreatic lipase and PPAR-¿ agonist activity; the in vitro findings correlated with our observations in the animal experiments. Thus, the present results suggest that RE that is rich in carnosic acid can be used as a preventive treatment against metabolic disorders, which merits further examination at physiological doses in randomised controlled trials. © Copyright © The Authors 2011.

Rosemary (Rosmarinus officinalis L.) extracts (RE) are natural antioxidants that are used in food, food supplements and cosmetic applications; exert anti-inflammatory and anti-hyperglycaemic effects; and promote weight loss, which can be exploited to develop new preventive strategies against metabolic disorders. Therefore, the aim of the present study was to evaluate the preventive effects of rosemary leaf extract that was standardised to 20 % carnosic acid (RE) on weight gain, glucose levels and lipid homeostasis in mice that had begun a high-fat diet (HFD) as juveniles. The animals were given a low-fat diet, a HFD or a HFD that was supplemented with 500 mg RE/kg body weight per d (mpk). Physiological and biochemical parameters were monitored for 16 weeks. Body and epididymal fat weight in animals on the HFD that was supplemented with RE increased 69 and 79 % less than those in the HFD group. Treatment with RE was associated with increased faecal fat excretion but not with decreased food intake. The extract also reduced fasting glycaemia and plasma cholesterol levels. In addition, we evaluated the inhibitory effects of RE in vitro on pancreatic lipase and PPAR-¿ agonist activity; the in vitro findings correlated with our observations in the animal experiments. Thus, the present results suggest that RE that is rich in carnosic acid can be used as a preventive treatment against metabolic disorders, which merits further examination at physiological doses in randomised controlled trials. © Copyright © The Authors 2011.

The present study was aimed to screen the possible antiobesity effects of ethanol extract of Alpinia galanga rhizomes in cafeteria diet fed obese rats. Obesity was induced in albino rats by feeding cafeteria diet daily for 6 weeks in addition to normal diet. The ethanol extract of rhizomes was administered at a daily dose of 500 mg/kg orally for 6 weeks. Body weight and food intake was measured initially and then every week thereafter. On day 42, serum glucose, lipids and leptin levels were estimated and then the weight of liver and parametrial adipose tissues was determined. The liver triglyceride content was estimated. The in vitro pancreatic lipase inhibitory activity of the extract was also determined. The extract produced inhibition of increase in body weight, energy intake and parametrial adipose tissue weight induced by cafeteria diet. The extract significantly reduced serum lipid and leptin levels, which were elevated by feeding cafeteria diet. In addition, the extract significantly inhibited the increase in liver weight and accumulation of hepatic triglycerides. The extract also produced dose dependent inhibition of in vitro pancreatic lipase activity. The present study concludes that, ethanol extract of Alpinia galanga rhizomes is useful for treatment of cafeteria diet induced obesity in rats.

La prevalencia de los trastornos metabólicos está creciendo a nivel mundial. Botánicos, como el romero (Rosmarinus officinalis L.) y las semillas de fresno (Fraxinus excelsior L.), pueden ser una alternativa para mejorar estos trastornos. El objetivo de esta tesis doctoral fue generar extractos industriales de las partes comestibles de estas plantas, identificar sus compuestos por HPLC, HPLC-MS y RMN, y determinar su eficacia y seguridad. Se desarrollaron tres extractos de romero - estandarizados al 20% de ácido carnósico, 20% de ácido rosmarínico, y 40% de ácido ursólico. El extracto rico en ácido ursólico mostró la menor capacidad antioxidante en modelos ORAC y FRAP in vitro, mientras que los otros dos extractos tuvieron capacidades más elevadas. Sin embargo, el extracto rico en ácido carnósico (RE) fue superior en la inhibición de la oxidación de LDL ex vivo, y fue el único seleccionado para estudios posteriores. Se desarrolló un extracto de semilla de fresno (FE) de acuerdo a su uso tradicional en Marruecos, siendo identificados salidrosido y 9 glucósidos secoiridoides, dos de ellos fueron descubiertos por primera vez: Excelside A y Excelside B. En estudios in vitro, RE y FE activaron receptores nucleares que regulan la homeostasis de la glucosa y la energía, y actuaron sobre mecanismos contra la obesidad y la dislipidemia - RE activa PPAR? e inhibe la lipasa pancreática, y FE estimula PPAR? y evita la diferenciación de preadipocitos. La eficacia de ambos extractos para el control de trastornos metabólicos fue confirmada en ratones C57BL/6J administrados con una dieta baja en grasa, una dieta alta en grasa, o una dieta alta en grasa más 0.5% RE (HFD.RE) o 0.5% FE (FED) durante 16 semanas. HFD.RE limitó el aumento del peso corporal y grasa en el epidídimo en un 69% (P<0.01) y 79% (P<0.001), respectivamente. HFD.RE también redujo la glucemia (72%, P<0.01) y los niveles de colesterol (68%, P<0.001). FED redujo la glucemia (76.52%, P<0.001), insulinemia (53.43%, P

La prevalencia de los trastornos metabólicos está creciendo a nivel mundial. Botánicos, como el romero (Rosmarinus officinalis L.) y las semillas de fresno (Fraxinus excelsior L.), pueden ser una alternativa para mejorar estos trastornos. El objetivo de esta tesis doctoral fue generar extractos industriales de las partes comestibles de estas plantas, identificar sus compuestos por HPLC, HPLC-MS y RMN, y determinar su eficacia y seguridad. Se desarrollaron tres extractos de romero - estandarizados al 20% de ácido carnósico, 20% de ácido rosmarínico, y 40% de ácido ursólico. El extracto rico en ácido ursólico mostró la menor capacidad antioxidante en modelos ORAC y FRAP in vitro, mientras que los otros dos extractos tuvieron capacidades más elevadas. Sin embargo, el extracto rico en ácido carnósico (RE) fue superior en la inhibición de la oxidación de LDL ex vivo, y fue el único seleccionado para estudios posteriores. Se desarrolló un extracto de semilla de fresno (FE) de acuerdo a su uso tradicional en Marruecos, siendo identificados salidrosido y 9 glucósidos secoiridoides, dos de ellos fueron descubiertos por primera vez: Excelside A y Excelside B. En estudios in vitro, RE y FE activaron receptores nucleares que regulan la homeostasis de la glucosa y la energía, y actuaron sobre mecanismos contra la obesidad y la dislipidemia - RE activa PPAR? e inhibe la lipasa pancreática, y FE estimula PPAR? y evita la diferenciación de preadipocitos. La eficacia de ambos extractos para el control de trastornos metabólicos fue confirmada en ratones C57BL/6J administrados con una dieta baja en grasa, una dieta alta en grasa, o una dieta alta en grasa más 0.5% RE (HFD.RE) o 0.5% FE (FED) durante 16 semanas. HFD.RE limitó el aumento del peso corporal y grasa en el epidídimo en un 69% (P<0.01) y 79% (P<0.001), respectivamente. HFD.RE también redujo la glucemia (72%, P<0.01) y los niveles de colesterol (68%, P<0.001). FED redujo la glucemia (76.52%, P<0.001), insulinemia (53.43%, P

In view of the reported association of insulin-dependent diabetes mellitus (IDDM) with viral infections, (non-) islet-specific immune changes, and partial immunodeficiencies, we used immunonephelometry to measure circulating levels of IgM, IgG, and IgA in a registry-based group of IDDM patients under age 40 years at clinical onset (n = 397) and in age-matched nondiabetic siblings (n = 316) and control subjects (n = 322). Overall, IgM and IgA concentrations were higher, and IgG concentrations lower, in patients than in control subjects or siblings (P < 0.001). In siblings, IgM concentrations were higher than in control subjects (P < 0.001). Using age- adjusted reference intervals, abnormal Ig concentrations were noted in 27% of the patients at onset versus only 10% of the siblings and 7% of the control subjects (P < 0.001). For onset between 20 and 40 years (n = 220), 30% of the patients presented either increased IgM levels (21%) or decreased IgG levels (11%). Both independent phenomena occurred regardless of diabetes-associated immune and genetic markers. In patients and siblings, IgM levels were positively correlated with pancreatic lipase activity. In diabetic children (0-9 years; n = 65), a subgroup presented increased IgA levels (15%) in association with the highest HLA DQ-linked genetic risk and elevated IgM levels. The changes in total Ig concentrations at onset were largely reversed under insulin therapy. They may reflect exposure to environmental triggers, such as viral infections, or to (relative) insulinopenia prior to clinical disease onset. Whatever their cause, different serum Ig levels exist in different age groups of recent-onset IDDM patients., SCOPUS: cp.j, info:eu-repo/semantics/published

In view of the reported association of insulin-dependent diabetes mellitus (IDDM) with viral infections, (non-) islet-specific immune changes, and partial immunodeficiencies, we used immunonephelometry to measure circulating levels of IgM, IgG, and IgA in a registry-based group of IDDM patients under age 40 years at clinical onset (n = 397) and in age-matched nondiabetic siblings (n = 316) and control subjects (n = 322). Overall, IgM and IgA concentrations were higher, and IgG concentrations lower, in patients than in control subjects or siblings (P < 0.001). In siblings, IgM concentrations were higher than in control subjects (P < 0.001). Using age- adjusted reference intervals, abnormal Ig concentrations were noted in 27% of the patients at onset versus only 10% of the siblings and 7% of the control subjects (P < 0.001). For onset between 20 and 40 years (n = 220), 30% of the patients presented either increased IgM levels (21%) or decreased IgG levels (11%). Both independent phenomena occurred regardless of diabetes-associated immune and genetic markers. In patients and siblings, IgM levels were positively correlated with pancreatic lipase activity. In diabetic children (0-9 years; n = 65), a subgroup presented increased IgA levels (15%) in association with the highest HLA DQ-linked genetic risk and elevated IgM levels. The changes in total Ig concentrations at onset were largely reversed under insulin therapy. They may reflect exposure to environmental triggers, such as viral infections, or to (relative) insulinopenia prior to clinical disease onset. Whatever their cause, different serum Ig levels exist in different age groups of recent-onset IDDM patients., SCOPUS: cp.j, info:eu-repo/semantics/published

The need for stable fats in military rations that are nutritionally and physiologically adequate is well recognized. Concerns have been raised regarding the digestibility of some solid fats that were considered as candidate fats to be used in calorically dense rations for short-term military feeding. The nutritional effect of fats is commonly evaluated by animal experimentation. The closing of animal facilities at the U.S. Army Natick Research, Development and Engineering Center in 1982 provided a challenge as well as an opportunity to seriously consider nonanimal assay techniques to determine the bioavailability of fats and other nutrients. The present study was undertaken to develop a simple and rapid enzymatic digestion method to meet the unique reaction requirements of solid fats. In addition, the effect of various factors such as the source of lipase, the structure of the fat, and the effect of certain additives, on the in vitro digestibility of fats was examined. It is anticipated that this study would be beneficial in screening various commercial fats prior to animal and human experimentation to meet the special requirements of energy- dense foods

peer-reviewed, Lipid cubic phase (LCP) formulations enhance the intestinal solubility and bioavailability of hydrophobic drugs by reducing precipitation and facilitating their mass transport to the intestinal surface for absorption. LCPs with an ester linkage connecting the acyl chain to the glycerol backbone (monoacylglycerols), are susceptible to chemical digestion by several lipolytic enzymes including lipases, accelerating the release of hydrophobic agents from the lipid bilayers of the matrix. Unlike regular enzymes that transform soluble substrates, lipolytic enzymes act at the interface of water and insoluble lipid. Therefore, compounds that bind to this interface can enhance or inhibit the activity of enzymes to varying extent. Here, we explore how the lipolysis rate can be tuned by the interfacial interaction of porcine pancreatic lipase with monoolein LCPs containing a known lipase inhibitor, tetrahydrolipstatin. Release of the Biopharmaceutical Classification System (BCS) class IV drug, paclitaxel, from the inhibitor-modified LCP was examined in the presence of lipase and its effectors colipase and calcium. By combining experimental dynamic digestion studies, thermodynamic measurements and molecular dynamics simulations of the competitive inhibition of lipase by tetrahydrolipstatin, we reveal the role and mode of action of lipase effectors in creating a precisely-balanced degradation-controlled LCP release system for the poorly soluble paclitaxel drug

© 2015 Pleiades Publishing, Ltd. Esters of fatty acids (FAs) and polyethylene glycol-400 (PEG) are valuable chemically derived surfactants. In this work, it is shown that the chemical synthesis of PEG esters can be replaced by enzymatic synthesis under milder conditions and using simpler and more environmentally friendly technology. The main obstacles to enzymatic catalysis in a system of PEG and higher FAs are the high viscosity of the former and the low water solubility of the latter. These problems are solved by selecting organic media and other conditions of the process mediated by pancreatic lipase. The optimum conditions for the synthesis of PEG esters of FAs are determined: reaction medium, benzene/hexane in a ratio of 2: 3; optimum temperature, 25°C; water content in the system, no more than 0.2%; FA: PEG molar ratio, 1: 1.8; reaction time, 48 h. Under these conditions, the yields in synthesizing PEG esters of capric, lauric, and palmitic acids are 80, 78, and 44%, respectively.

© 2015 Pleiades Publishing, Ltd. Esters of fatty acids (FAs) and polyethylene glycol-400 (PEG) are valuable chemically derived surfactants. In this work, it is shown that the chemical synthesis of PEG esters can be replaced by enzymatic synthesis under milder conditions and using simpler and more environmentally friendly technology. The main obstacles to enzymatic catalysis in a system of PEG and higher FAs are the high viscosity of the former and the low water solubility of the latter. These problems are solved by selecting organic media and other conditions of the process mediated by pancreatic lipase. The optimum conditions for the synthesis of PEG esters of FAs are determined: reaction medium, benzene/hexane in a ratio of 2: 3; optimum temperature, 25°C; water content in the system, no more than 0.2%; FA: PEG molar ratio, 1: 1.8; reaction time, 48 h. Under these conditions, the yields in synthesizing PEG esters of capric, lauric, and palmitic acids are 80, 78, and 44%, respectively.