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1.
J Int Med Res ; 48(5): 300060520903612, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32475187

RESUMO

OBJECTIVES: The objective was to observe the effects of Astragalus polysaccharides on diabetes and on regulation of the TGF-ß/Smad signaling pathway. METHODS: A type 2 diabetic rat model was established with a high-fat diet in combination with low-dose streptozotocin (35 mg/kg). Astragalus polysaccharides were applied as treatment intervention and changes in blood glucose and kidney morphology and function were assessed. RESULTS: Eight weeks after model establishment, kidney weight as a proportion of total weight (KW/TW) in the high-, medium-, and low-dose Astragalus polysaccharide groups was significantly lower than that in the model group, and the KW/TW value gradually decreased with increasing dose of polysaccharides in each treatment group. Fasting blood glucose in the low- and medium-dose Astragalus polysaccharide groups was numerically lower than that in the model group and fasting blood glucose in rats in the high-dose group was significantly lower than that in the model group. Levels of 24-hour urinary microalbumin, creatinine, blood urea nitrogen, collagens I, III, and IV, α-smooth muscle actin, transforming growth factor-ß1, and Smad3 in Astragalus polysaccharide groups (all doses) were significantly lower than those in the model group. CONCLUSIONS: Astragalus polysaccharide significantly improved blood glucose and protected kidney function in a rat diabetes model.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Rim/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Astrágalo/metabolismo , Glicemia/metabolismo , Creatinina/sangue , Nefropatias Diabéticas/sangue , Dieta Hiperlipídica , Modelos Animais de Doenças , Rim/metabolismo , Masculino , Polissacarídeos/farmacologia , Ratos , Ratos Sprague-Dawley , Estudos Retrospectivos , Transdução de Sinais/efeitos dos fármacos , Proteínas Smad Reguladas por Receptor/metabolismo , Estreptozocina/metabolismo , Estreptozocina/farmacologia , Fator de Crescimento Transformador beta1/metabolismo
2.
AAPS PharmSciTech ; 21(4): 123, 2020 Apr 26.
Artigo em Inglês | MEDLINE | ID: mdl-32337654

RESUMO

The objective of this work was to investigate the capacity of mogroside V (MOG-V), a food additive, as a novel carrier to improve the bioavailability and liver distribution of silybin (SLY). Solid dispersion particles (SDPs) of SLY/MOG-V were prepared utilizing the solvent evaporation method. The physicochemical characterizations of SDPs were evaluated by using dynamic light scattering (DLS), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) measurements. DLS results demonstrated the formation of nanoparticles (206 nm) of SDPs in water. DSC and PXRD analysis revealed that SLY was in amorphous form or molecularly dispersed in SDPs. SDPs also exhibited a major increase in both dissolution rate and saturation solubility, as evidenced by a 1931-fold improvement (2201 µg/mL) in solubility compared with pure SLY (1.14 µg/mL). The pharmacokinetic study in rats showed that oral absorption of SLY/MOG-V SDPs was dramatically increased. The mean value of AUC until 12 h for SLY/MOG-V SDPs (27,481 ng·min/mL) was 24.5-fold higher than that of pure SLY (1122 ng·min/mL). In vivo tissue distribution experiment in mice confirmed that the major distribution tissue was changed from lungs to liver after SLY was loaded into MOG-V. In addition, even orally administrated to mice at a high dose (4.2 g/kg), MOG-V exhibited no undesirable effect on the plasma glucose concentrations. Thus, MOG-V may have the applicability to serve as an ideal excipient for solubilization or as a novel liver targeting carrier for the delivery of SLY.


Assuntos
Portadores de Fármacos/metabolismo , Sistemas de Liberação de Medicamentos/métodos , Fígado/metabolismo , Silibina/metabolismo , Triterpenos/metabolismo , Administração Oral , Animais , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/metabolismo , Disponibilidade Biológica , Portadores de Fármacos/administração & dosagem , Avaliação Pré-Clínica de Medicamentos/métodos , Fígado/efeitos dos fármacos , Masculino , Camundongos , Camundongos Endogâmicos ICR , Ratos , Ratos Sprague-Dawley , Silibina/administração & dosagem , Edulcorantes/administração & dosagem , Edulcorantes/metabolismo , Triterpenos/administração & dosagem , Difração de Raios X/métodos
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