RESUMO
PURPOSE: Anthocyanins (ACNs) are polyphenols that might reduce pathological processes associated with type 2 diabetes mellitus and other chronic diseases, but their bioavailability is still controversial. In this study, the metabolic activity of oral delivery of ACN-loaded niosomes was investigated and evaluated in a diet-induced obesity (DIO) mice model. METHODS: ACNs extracted from Vaccinium Meridionale by the supercritical fluid extraction method were loaded in niosomes. The niosomal formulation was physically characterized and further administrated in drinking water to obese, insulin resistant mouse. We evaluated the effect of ACN loaded niosomes on hyperglycemia, glucose and insulin intolerance and insulin blood levels in C57BL/6 J mice fed with a high-fat diet. RESULTS: The ACN-loaded particles were moderately monodisperse, showed a negative surface charge and 57% encapsulation efficiency. The ACN-loaded niosomes ameliorated the insulin resistance and glucose intolerance in the DIO mice model. Additionally, they reduced animal weight and plasma insulin, glucose, leptin and total cholesterol levels in obese mice. CONCLUSION: ACN-loaded niosomes administration, as a functional drink, had a beneficial effect on the reversal of metabolic abnormalities associated with obesity.
Assuntos
Antocianinas/química , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/química , Lipossomos/química , Nanocápsulas/química , Extratos Vegetais/química , Estreptófitas/química , Animais , Antocianinas/administração & dosagem , Glicemia/efeitos dos fármacos , Peso Corporal/efeitos dos fármacos , Colesterol/sangue , Colesterol/metabolismo , Diabetes Mellitus Experimental , Dieta Hiperlipídica , Composição de Medicamentos , Liberação Controlada de Fármacos , Humanos , Hipoglicemiantes/administração & dosagem , Insulina/sangue , Insulina/metabolismo , Insulina/farmacologia , Resistência à Insulina , Leptina/sangue , Leptina/metabolismo , Masculino , Camundongos Endogâmicos C57BL , Camundongos Obesos , Obesidade/tratamento farmacológico , Extratos Vegetais/administração & dosagemRESUMO
Leishmaniasis comprises a group of infectious diseases with worldwide distribution, of which both the visceral and cutaneous forms are caused by Leishmania parasites. In the absence of vaccines, efficacious chemotherapy remains the basis for leishmaniasis control. The available drugs are expensive and associated with several secondary adverse effects. Due to these limitations, the development of new antileishmanial compounds is imperative, and plants offer various perspectives in this regard. The present study evaluated the in vitro leishmanicidal activity of flavonoids isolated from Solanum paludosum Moric. and investigated the mechanisms of cell death induced by them. These compounds were evaluated in vitro for their antileishmanial activity against Leishmania amazonensis promastigotes and they showed prominent leishmanicidal activity. The EtOAc fraction, gossypetin 3,7,8,4'-tetra-O-methyl ether (1), and kaempferol 3,7-di-O-methyl ether (3) were selected to be used in an in vitro assay against L. amazonensis amastigotes and cell death assays. The flavonoids (1) and (3) presented significant activity against L. amazonensis amastigotes, exhibiting the IC50 values of 23.3 ± 4.5 µM, 34.0 ± 9.6 µM, and 10.5 ± 2.5 µM for the EtOAc fraction, (1), and (3), respectively, without toxic effects to the host cells. Moreover, (1) and (3) induced blocked cell cycle progression at the G1/S transition, ultimately leading to G1/G0 arrest. Flavonoid (3) also induced autophagy. Using Raman spectroscopy in conjunction with principal component analysis, the biochemical changes in the cellular components induced by flavonoids (1) and (3) were presented. The obtained results indicated that the mechanisms of action of (1) and (3) occurred through different routes. The results support that the flavonoids derived from S. paludosum can become lead molecules for the design of antileishmanial prototypes.
Assuntos
Antiprotozoários/farmacologia , Morte Celular/efeitos dos fármacos , Flavonoides/farmacologia , Citometria de Fluxo/métodos , Leishmania/efeitos dos fármacos , Animais , Antiprotozoários/química , Autofagia/efeitos dos fármacos , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Flavonoides/química , Quempferóis/química , Quempferóis/farmacologia , Leishmania/citologia , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Camundongos , Análise Espectral Raman , Estreptófitas/químicaRESUMO
The rheological behavior, thermogravimetric analysis (TGA), and atomic force microscopy (AFM) of the Pereskia aculeata Miller (OPN) mucilage treated with sodium chloride (NaCl), calcium chloride (CaCl2), and sucrose were evaluated. The experimental design was divided in a fractional factorial 25-1 for the screening of factors (OPN, sucrose, NaCl, CaCl2, and pH) and then in a 5â¯×â¯3â¯×â¯3 full factorial (OPN, sucrose, and NaCl). The model solutions used for the screening of factors presented shear-thinning behavior and the OPN mucilage concentrations were the factors that had significant effect on the apparent viscosity. Sucrose addition increased the thermal stability of the OPN mucilage solutions. OPN mucilage, sucrose, and NaCl were the variables with significant effect on thermogravimetric responses. The samples presented Newtonian behavior in 0-1.25% OPN mucilage concentrations and non-Newtonian behavior adjusted by power-law in 2.50-5.00% OPN mucilage concentrations with predominance of elastic behavior, contributing to the formation of stronger gels. The presence of sucrose in the systems containing OPN mucilage changed their rheological properties and salt additions caused reduction in viscosity. The AFM results provided a better understanding of the mechanism of OPN mucilage interactions in different solutions that justify the changes in viscosities.
Assuntos
Mucilagem Vegetal/química , Reologia , Sais/química , Estreptófitas/química , Sacarose/química , Microscopia de Força Atômica , Estrutura Molecular , Mucilagem Vegetal/análise , Cloreto de Sódio/química , Temperatura , TermogravimetriaRESUMO
Nectandra grandiflora Nees (Lauraceae) is a Brazilian native tree recognized by its durable wood and the antioxidant compounds of its leaves. Taking into account that the forest industry offers the opportunity to recover active compounds from its residues and by-products, this study identifies and underlines the potential of natural products from Nectandra grandiflora that can add value to the forest exploitation. This study shows the effect of three different extraction methods: conventional (CE), ultrasound-assisted (UAE) and microwave-assisted (MAE) on Nectandra grandiflora leaf extracts (NGLE) chemical yields, phenolic and flavonoid composition, physical characteristics as well as antioxidant and antifungal properties. Results indicate that CE achieves the highest extraction phytochemical yield (22.16%), but with similar chemical composition to that obtained by UAE and MAE. Moreover, CE also provided a superior thermal stability of NGLE. The phenolic composition of NGLE was confirmed firstly, by colorimetric assays and infrared spectra and then by chromatographic analysis, in which quercetin-3-O-rhamnoside was detected as the major compound (57.75-65.14%). Furthermore, the antioxidant capacity of the NGLE was not altered by the extraction methods, finding a high radical inhibition in all NGLE (>80% at 2 mg/mL). Regarding the antifungal activity, there was observed that NGLE possess effective bioactive compounds, which inhibit the Aspergillus niger growth.