Obesity is associated with metabolic and physiological effects in the gut. In this study, we evaluated the anti-inflammatory effect of trypsin inhibitor isolated from tamarind seeds (TTI) in vitro ...(interaction with lipopolysaccharide (LPS) and inhibitory activity against human neutrophil elastase (HNE)), and using intestinal co-cultures of Caco-2:HT29-MTX cell lines inflamed with TNF-α (50 ng/mL) and a Wistar rat model of diet-induced obesity (n = 15). TTI was administered to animals by gavage (10 days), and the treated group (25 mg/kg/day) was compared to animals without treatment or treated with a nutritionally adequate diet. In the in vitro study, it showed inhibitory activity against HNE (93%). In co-cultures, there was no protection or recovery of the integrity of inflamed cell monolayers treated with TTI (1.0 mg/mL). In animals, TTI led to lower plasma concentrations of TNF-α and IL-6, total leukocytes, fasting glucose, and LDL-c (p < 0.05). The intestines demonstrated a lower degree of chronic enteritis, greater preservation of the submucosa, and greater intestinal wall thickness than the other groups (p = 0.042). Therefore, the better appearance of the intestine not reflected in the intestinal permeability added to the in vitro activity against HNE point to possibilities for new studies and applications related to this activity.
The present study investigated the effect of gelatin-based nanoparticles (EPG) loaded with a carotenoid-rich crude extract (CE) on systemic and adipose tissue inflammatory response in a model with ...inflammation induced by a high glycemic index and high glycemic load diet (HGLI). Nanoparticles synthesized were characterized by different physical and chemical methods. The in vivo investigation evaluated Wistar rats (n = 20, 11 days, adult male with 21 weeks) subdivided into untreated (HGLI diet), conventional treatment (nutritionally adequate diet), treatment 1 (HGLI + crude extract (12.5 mg/kg)), and treatment 2 (HGLI + EPG (50 mg/kg)) groups. Dietary intake, caloric intake and efficiency, weight, inflammatory cytokines tissue concentration, visceral adipose tissue (VAT) weight, histopathological analysis, and antioxidant activity in plasma and VAT were investigated. EPG showed the same physical and chemical characteristics as previous batches (95.2 nm, smooth surface, and chemical interactions between materials). The EPG-treated group was the only group promoting negative ∆dietary intake, ∆caloric efficiency, and ∆weight. In addition, it presented a significant reduction (
< 0.05) in IL-6 and leptin levels and a greater presence of multilocular adipocytes. The results suggest that EPG can act as a nutraceutical in adjuvant therapy for treating inflammatory diseases associated with adipose tissue accumulation.
In tropical America, principally in Northeastern Brazil, the leaf extract of Anacardium occidentale is traditionally used for treatment of different diseases. However, chemical and biological ...properties and activities of Anacardium occidentale are poorly investigated and known. Here, we evaluated the antioxidant and anti-inflammatory activities “in vitro” of leaf extract from Anacardium occidentale. Our results show that leaf extract exhibits antioxidant activity when used to treat RAW 264.7 macrophage cells. Antioxidant effects were observed by decrease in oxidative damage in macrophage cells treated with 0.5 µg/mL and 5 µg/mL of leaf extract. Moreover, leaf extract reversed oxidative damage and inflammatory parameters induced in LPS-stimulated RAW 264.7 macrophage cells. Leaf extract at 0.5 µg/mL and 5 µg/mL was able to inhibit release of TNF-α and IL-1β in LPS-stimulated cells. Taken together, our results indicate antioxidant and anti-inflammatory effects of leaf extract from Anacardium occidentale and reveal the positive effects that intake of these products can mediate in biological system.
Trypsin and chymotrypsin inhibitors from Erythrina velutina seeds have been previously isolated by our group. In previous studies using a sepsis model, we demonstrated the antitumor and ...anti-inflammatory action of these compounds. This study aimed to evaluate the gastroprotective and antielastase effects of protein inhibitors from E. velutina seeds in an experimental stress-induced ulcer model. Two protein isolates from E. velutina seeds, with antitrypsin (PIAT) and antichymotrypsin (PIAQ) activities, were tested. Both protein isolates showed a high affinity and inhibitory effect against human neutrophil elastase, with 84% and 85% inhibition, respectively. Gastric ulcer was induced using ethanol (99%) in 6 groups of animals (female Wistar rats, n = 6). Before ulcer induction, these animals were treated for 5 days with one of the following: (1) PIAT (0.2 mg·kg
−1
), (2) PIAT (0.4 mg·kg
−1
), (3) PIAQ (0.035 mg·kg
−1
), (4) ranitidine hydrochloride (50 mg·kg
−1
), (5) saline solution (0.9%), or (6) no intervention (sham). Both PIAT and PIAQ protected gastric mucosa, preventing hemorrhagic lesions, edema, and mucus loss. No histologic toxic effects of PIAT or PIAQ were seen in liver and pancreatic cells. Our results show that protein isolates from E. velutina seeds have potential gastroprotective effects, placing these compounds as natural candidates for gastric ulcer prevention.
We investigated the inflammatory effect of a pellet-diet with high glycemic index and load (HGLI) on the histological organization of adipocytes, intestinal epithelium, and fat in liver and pancreas ...in adult male
rats. Two groups (
=10) received for 17 weeks: (1) HGLI diet or (2) Standard diet (Labina®). Histological analyses of adipose tissue, jejunum, liver, and pancreas were performed. Stereology analysis, visceral adiposity index, gene expression, and immunohistochemistry of tumor necrosis factor-α (TNF-α) in visceral adipose tissue and plasma TNF-α were also assessed. The HGLI diet-induced hypertrophy of adipocytes with adipocyte volume density equal to 97.0%, cross-sectional area of adipocytes equivalent to 1387 µm² and a total volume of adipocytes of 6.97 cm³ an elevation of 8%, 25%, and 58%, respectively. Furthermore, the HGLI diet increased liver and pancreatic fat deposition, altered and inflamed the intestinal epithelia, and increased TNF-α gene expression (
=0.014) with a positive immunostaining in visceral adipose tissue and high plasma TNF-α in comparison with standard diet. The results suggest that this diet was able to generate changes commonly caused to solid diets with high fat or fructose-rich beverages. To the best of our knowledge, this is the first report in the literature concerning the properties of low-cost, sucrose-rich pellet-diet presenting high glycemic index and high glycemic load efficient on the development of obesity complications in
rats that were subjected to diet-induced obesity. Therefore, the HGLI pellet-diet may be considered an effective tool to be used by the scientific community in experimental research.
•Carotenoids present anti-inflammatory effects in healthy and overweight adults.•Nanotechnology can enhance carotenoid's bioactive potential.•Nanoparticles loaded with carotenoids from Cantaloupe ...melon were used in obese rats.•Animals receiving the nanoparticles showed no signs of toxicity.•Animals treated with nanoparticles had organs better aspect compared to untreated.
The safety and bioactive potential of crude carotenoid extract from Cantaloupe melon nanoencapsulated in porcine gelatin (EPG) were evaluated in a chronic inflammatory experimental model. Animals were fed a high glycemic index and high glycemic load (HGLI) diet for 17 weeks and treated for ten days with 1) HGLI diet, 2) standard diet, 3) HGLI diet + crude carotenoid extract (CE) (12.5 mg/kg), and 4) HGLI diet + EPG (50 mg/kg). General toxicity signals were investigated, considering body weight, food intake, hematological, biochemical parameters, relative weight, morphology, and histopathology of organs. The biochemical parameters indicated the low toxicity of EPG. Acute hepatitis was observed in animals' livers, but CE and EPG groups presented improved tissue appearance. Chronic enteritis was observed in animals, with villi and intestinal glands preservation in the EPG group. The results suggest the safety and the bioactive effect of EPG, possibly related to its anti-inflammatory potential.
Drug delivery systems based on carbohydrate polymers have shown promising results for the colonic release of drugs due to the selective degradation by the local microbiota and physical resistance to ...the physiological conditions of the gastrointestinal tract. This work aimed to obtain and characterize a novel particulate system (PS) based on chitosan and guar gum polymers (CHI-GG) for the release of triamcinolone (TRI) and evaluate the in vivo anti-inflammatory activity of ulcerative colitis. PS were prepared by combining coacervation and spray drying techniques using different CHI-GG and drug-polymer ratios. For obtained, PS CHI-GG-TRI systems were characterized. To evaluate the in vivo activity of PS containing TRI, we used Wistar rats to observe the anti-inflammatory response in macroscopic and microscopic parameters of the intestinal mucosa. PS-TRI demonstrated improvements in the aspects related to reducing adverse effects of the drugs when administered in their free form. PS-TRI release occurred in only 69 % of the active in 24 h; the macro and microscopic parameters and the activity of the experimental ulcerative colitis were softened, and an excellent potential anti-inflammatory effect was observed. Infrared data evidenced the incorporation of TRI on the PS. DSC analysis showed the compatibility between TRI and the polymers of the PS. The release kinetics showed an initial burst release of TRI followed by a controlled release profile for up to 30 h. Therefore, a new PS for TRI release was obtained that can swell and control TRI release and that showed anti-inflammatory activity in an animal model, also reducing adverse effects present in conventional treatments.
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•Chitosan-guar gum particulate systems (PS) have enhanced colonic drug delivery.•The ulcerative colitis was softened, indicating an anti-inflammatory effect.•PS exhibits controlled release kinetics, sustained action for 30 h•PS reduced the adverse effects of the TRI compared with their free form.
This study aimed to evaluate the effect of supplementation of sucralose and fructose on the metabolism of adolescent rats. Eighteen male Wistar rats were divided into 3 groups: control group (GC), ...fructose group (GF) treated with 50 mg/kg of fructose, and sucralose group (GS) receiving 50 mg/kg of sucralose for 24 days. The weight and feed intake were measured weekly. At the end of the experiment, some biochemical parameters, histopathology of the liver and biodistribution of the radiotracer super(99m)Tc-sodium phytate in liver and blood were analyzed. The GF showed higher body weight only in the first week compared with GS and GC (p<0.05). Histopathology and % ATI/g radiotracer super(99m)Tc-sodium phytate in liver and blood were not different between the groups. The GF showed higher values of aspartate aminotransferase activity, bilirubin, alkaline phosphatase activity and gamma glutamyl transferase activity, compared with the other groups (GC and GS) (p<0.05). Activity of alanine aminotransferase and albumin level of GF were higher than GS (p<0.05). For other parameters, no statistical difference was observed. It was concluded that the use of fructose during the experiment was able to alter hepatic enzymes, but on the other hands, the use of sucralose caused no change.
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