RESUMEN
The aim of the present study was to develop a self-emulsifying drug delivery system (SEDDS) containing the extract of S oleraceus Linn (SOL) with improved intestinal stability in order to increase oral bio-potency. SOL was effectively incorporated into emulsions, which showed resistance to in vitro digestion without any destruction of its phenolic acids, glycosides and aglycone. SEDDS and SOL were also prepared for the comparison of in vivo anti-diabetic effects. Four weeks of daily treatments of SEDDS dramatically improved the quality of life for diabetic rats. Streptozotocin (STZ) caused body weight reduction, which was reversed by SEDDS at a low dose (100 mg kg-1), and it was more effective than SOL at a high dose (200 mg kg-1). SEDDS also improved the response to glucose tolerance, which was significantly higher than that of SOL. On the basis of these findings, the SEDDS approach might be an efficacious dosage option to enhance the nutraceutical properties of SOL.
Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Hipoglucemiantes/uso terapéutico , Extractos Vegetales/uso terapéutico , Sonchus , Administración Oral , Animales , Modelos Animales de Enfermedad , Composición de Medicamentos , Emulsionantes/química , Hipoglucemiantes/administración & dosificación , Hipoglucemiantes/química , Masculino , Fitoterapia , Extractos Vegetales/administración & dosificación , Extractos Vegetales/química , Distribución Aleatoria , Ratas , Ratas Sprague-Dawley , EstreptozocinaRESUMEN
The extracts of S. oleraceus Linn (SOL) and its main phenolic compounds have shown anti-diabetic effects, but their underlying mechanisms for glucose homeostasis remain unclear. The aim of this study is to evaluate the anti-diabetic mechanism of SOL by using the streptozocin (STZ) induced diabetic rat model. When diabetic rats were fed with SOL at a dose of 400 mg/kg/day for 6 weeks, the concentrations of triglycerides (TG), total cholesterol (TC), and low-density lipoprotein cholesterol (LDL-C) were reduced by 43%, 22%, and 16%, respectively. Meanwhile, it was also found that daily feeding of SOL to diabetic rats led to a decrease in plasma glucose level by approximately 23%. Positive effects were observed on glucose homeostasis due to the down-regulation of AMPK/Akt/GSK-3ß pathway, as indicated by the suppressions of adenosine 5'-monophosphate (AMP)-activated protein kinase (AMPK), protein kinase (Akt) phosphorylation, glycogen synthase kinase 3 beta (GSK-3ß), and the hepatic insulin resistance. In HepG2 cells, AMPK, Akt and GSK-3ß showed a consistent transcript regulation. SOL at dose of 400 mg/kg/day feeding for 6 weeks showed a positive effect comparable to metformin.
Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/administración & dosificación , Extractos Vegetales/administración & dosificación , Sonchus/química , Proteínas Quinasas Activadas por AMP/genética , Proteínas Quinasas Activadas por AMP/metabolismo , Animales , Diabetes Mellitus Experimental/metabolismo , Glucosa/metabolismo , Glucógeno Sintasa Quinasa 3 beta/genética , Glucógeno Sintasa Quinasa 3 beta/metabolismo , Células Hep G2 , Homeostasis/efectos de los fármacos , Humanos , Hígado/efectos de los fármacos , Hígado/metabolismo , Masculino , Proteínas Proto-Oncogénicas c-akt/genética , Proteínas Proto-Oncogénicas c-akt/metabolismo , Ratas Sprague-Dawley , Transducción de Señal/efectos de los fármacosRESUMEN
Edible Sonchus oleraceus Linn is a medicinal plant with many bioactivities such as anti-diabetic activity and anti-inflammatory activity. However, the main bioactive components such as polyphenols in S. oleraceus Linn are poorly absorbed in gastrointestinal tract and rapidly metabolized. Thereby, a self-emulsifying delivery system containing S. oleraceus Linn extracts (SSEDDS) was introduced to evade these problems. Herein, the anti-inflammatory effect of SSEDDS on streptozotocin-induced diabetic rats was investigated. The plasma glucose level was increased and plasma insulin level was decreased in diabetic rats. The levels of NF-κB, TNF-α, and IL-6 in the liver were significantly improved in diabetic rats (pâ¯<â¯0.05). Conversely, daily fed diabetic rats with 100, 200 and 400â¯mg/kg/day of SSEDS and 1â¯mg/kg/day metformin for 4 weeks, significantly (pâ¯<â¯0.05) restored all the above mentioned parameters to near normal levels. The immuno-histochemical studies confirmed the anti-inflammatory effects of SSEDDS.
Asunto(s)
Antiinflamatorios/uso terapéutico , Diabetes Mellitus Experimental/tratamiento farmacológico , Emulsiones/uso terapéutico , Extractos Vegetales/uso terapéutico , Sonchus/química , Animales , Glucemia/metabolismo , Citocinas/metabolismo , Diabetes Mellitus Experimental/inducido químicamente , Hipoglucemiantes/uso terapéutico , Insulina/metabolismo , Hígado/efectos de los fármacos , Hígado/patología , Masculino , Ratas Sprague-Dawley , EstreptozocinaRESUMEN
The aim of this study was to assess the inhibitory effects of Sonchus olearleu extract on the generation of heterocyclic amines in roasted pork patties cooked by pan-frying. All samples were cooked for two different durations (45â¯min and 105â¯min) under 200⯰C and 230⯰C. 2-amino-3-methylimidazo[4,5-f]quinoline (IQ), 2-ami- no-3,8-dimethylimidazo[4,5-f]quinoxaline (MeIQx), 2-amino-3,4,8-trimethylimidazo[4,5-f]quinox-aline (4,8-DiMeIQx), harman, and norharman were detected and quantified. In patties cooked at 230⯰C for 105â¯min, S. olearleu extract (0.5%) significantly inhibited the formation of IQ, harman, and norharman by 39%, 67%, and 63%, respectively. In contrast to IQ, the levels of harman and norharman were significantly reduced by the extracts tested. However, no such effects were observed for MeIQx and 4, 8-DiMeIQx. Notably, the inhibitory effect on heterocyclic amines is significantly correlated with the antioxidant potential and total phenolic content of S. olearleu extract.
Asunto(s)
Aminas/análisis , Carcinógenos/toxicidad , Culinaria , Compuestos Heterocíclicos/análisis , Productos de la Carne/análisis , Extractos Vegetales/farmacología , Sonchus/química , Animales , Cromatografía Líquida de Alta Presión/métodos , Espectrometría de Fluorescencia/métodos , PorcinosRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Sonchus oleraceus Linn (SOL) belongs to family of Asteraceae, is a traditional medicinal plant, which has been used to treat tumor, inflammatory diseases, infection and so on in Chinese folk culture. AIM OF THE STUDY: This work investigated the influence of aqueous ethanol extract of whole plant of SOL and contribution of its main components on inflammation METHODS AND RESULTS: Oral administration of SOL (10â¯mg/kg) to mice reduced the expression of inflammatory cytokines including IL-6, IL-1ß, and TNF-α, in the LPS-induced sepsis mouse model. Major phenolics in SOL were isolated and determined by HPLC. Results indicate that SOL at the concentration range from 25 to 100⯵g/mL and its main components, chlorogenic acid, caffeic acid (25-100⯵M) significantly reduced the pro-inflammatory cytokine IL-1ß, IL-6, TNF-α, attenuated iNOS and COX-2 expression in LPS-stimulated Macrophages. In addition, western blot analysis showed SOL suppressed inducible nitric oxide synthase (iNOS) protein expression and the phosphorylation of extracellular signal-regulated kinase (ERK), p38, c-Jun N-terminal kinase (JNK). CONCLUSION: The underlying mechanism of anti-inflammation might be in according with the inhibition of MAPKs activation as well as down regulation of iNOS and cyclooxygenase-2 (COX-2).