RESUMO
The goal of this work was to assess the usability of yeast glucan particles (GPs) as carriers for curcumin and determine the beneficial effect of a pharmacological composite of curcumin in GPs on dextran sulfate sodium induced colitis in rats. The assessment of the anti-inflammatory effect of particular substances was evaluated on the basis of the calculated disease activity index and by assessment of cytokines and enzymes from the gut tissue - tumor necrosis factor α (TNF-α), transforming growth factor ß1, interleukin (IL)-1ß, IL-6, IL-10, IL-17, catalase, superoxide dismutase 2, myeloperoxidase (MPO), and matrix metalloproteinase 9. Composites of GPs with incorporated curcumin showed promising results with the capability to lower symptoms of colitis and significantly decrease the production of pro-inflammatory cytokines TNF-α, IL-1ß, IL-6, and the activity of MPO, as well. The anti-inflammatory effect of the composites was greater than those of pure GPs or curcumin.
Assuntos
Anti-Inflamatórios/uso terapêutico , Colite/tratamento farmacológico , Curcumina/uso terapêutico , Portadores de Fármacos/uso terapêutico , Glucanos/uso terapêutico , Animais , Anti-Inflamatórios/administração & dosagem , Colite/induzido quimicamente , Curcumina/administração & dosagem , Citocinas/metabolismo , Sulfato de Dextrana , Glucanos/administração & dosagem , Interleucinas/metabolismo , Masculino , Ratos , Ratos Wistar , Saccharomyces cerevisiae/metabolismoRESUMO
Natural compounds offer a wide spectrum of potential active substances, but often they have a poor bioavailability. To increase the bioavailability and bioactivity of the natural anti-inflammatory molecules curcumin and diplacone, we used glucan particles (GPs), hollow shells from Saccharomyces cerevisiae composed mainly of ß-1,3-d-glucan. Their indigestibility and relative stability in the gut combined with their immunomodulatory effects makes them promising carriers for such compounds. This study aimed to determine how curcumin and diplacone, either alone or incorporated in GPs, affect the immunomodulatory activity of the latter by assessing the respiratory burst response and the secretion of pro-inflammatory cytokines by primary porcine innate immune cells. Incorporating curcumin and diplacone into GPs by controlled evaporation of the organic solvent substantially reduced the respiratory burst response mediated by GPs. Incorporated curcumin in GPs also reduced GPs mediated secretion of IL-1ß and TNF-α by innate immune cells. The obtained results indicate a potentially beneficial effect of the incorporation of curcumin or diplacone into GPs against inflammation.
Assuntos
Anti-Inflamatórios/farmacologia , Curcumina/farmacologia , Portadores de Fármacos , Flavanonas/farmacologia , Fatores Imunológicos/farmacologia , Leucócitos Mononucleares/efeitos dos fármacos , Neutrófilos/efeitos dos fármacos , beta-Glucanas/farmacologia , Animais , Anti-Inflamatórios/química , Células Cultivadas , Curcumina/química , Composição de Medicamentos , Flavanonas/química , Fatores Imunológicos/química , Fatores Imunológicos/isolamento & purificação , Interleucina-1beta/metabolismo , Leucócitos Mononucleares/imunologia , Leucócitos Mononucleares/metabolismo , Neutrófilos/imunologia , Neutrófilos/metabolismo , Proteoglicanas , Explosão Respiratória/efeitos dos fármacos , Saccharomyces cerevisiae/química , Solventes/química , Sus scrofa , Fator de Necrose Tumoral alfa/metabolismo , beta-Glucanas/química , beta-Glucanas/isolamento & purificaçãoRESUMO
Morusin is a prenylated flavonoid isolated from the root bark of Morus alba. Many studies have shown the ability of flavonoids to act as anti-inflammatory agents. The aim of this study was to evaluate the effect of morusin on experimentally colitis induced by 2,4,6-trinitrobenzensulfonic acid in Wistar rats and to compare it with sulfasalazine, a drug conventionally used in the treatment of inflammatory bowel disease. Morusin was administered by gavage at doses of 12.5, 25, or 50 mg/kg/day for five days. The colonic tissue was evaluated macroscopically, histologically, and by performing immunodetection and zymographic analysis to determine the levels of antioxidant enzymes [superoxide dismutase (SOD) and catalase (CAT)], interleukin (IL)-1ß, and transforming growth factor (TGF)-ß1 and the activities of matrix metalloproteinases (MMP) 2 and 9. The tissue damage scores were significantly reduced with increasing dose of morusin, however efficacy was not demonstrated at the highest dose. At the dose of 12.5 mg/kg, morusin exerted therapeutic effectivity similar to that of sulfasalazine (50 mg/kg). This was associated with significant reduction of TGF-ß1 levels and MMP2 and MMP9 activities, and slight reduction of IL-1ß. Our results suggest that morusin possesses therapeutic potential for the treatment of chronic inflammatory diseases.