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1.
Mol Biol Rep ; 47(7): 5273-5283, 2020 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-32642916

RESUMEN

Type 2 diabetes mellitus (T2DM) is a metabolic disorder caused due to varied genetic and lifestyle factors. The search for a potential natural compound to enhance the treatment of diabetes is the need of the hour. Butein, a flavonoid, found sufficiently in Faba bean, is said to possess an anti-diabetic property. In-silico analysis, Butein is predicted as a potential anti-diabetic compound, due to its regulatory action on PPAR-Gamma. Based on this evidence, the Butein's anti-diabetic action is studied in diabetic induced rat models. The drug property of Butein is studied through in-silico analysis to determine the metabolic properties. In animal models, the biochemical analysis, histopathological and gene expression against PPAR-Gamma were studied comparatively. Butein being a hydrophobic compound, the bioavailability is said to be minimum. Hence, Butein formulation was made using biopolymer Chitosan for the synergistic anti-diabetic action. The Butein Chitosan formulation was optimized and characterized using analytical techniques. Further, the anti-diabetic activity of Butein and Butein Chitosan formulation was studied in diabetic induced rats. The obtained in-silico analysis results showed that Butein is the most favorable drug. Apparently, in the rat model, Butein and Butein Chitosan formulation effectively controlled the blood glucose levels without any side effects. The histopathological observations of the tissue samples showed nontoxic activity. Additionally, the gene expression analysis predicted the possible mechanism of anti-diabetic action exhibited through the down regulation of PPAR-Gamma. Whereas, the Butein Chitosan formulation failed, to show synergetic anti-diabetic activity as expected. This study is vital in introducing Butein as a safe anti-diabetic compound, which can be used in the treatment of T2DM.


Asunto(s)
Chalconas/farmacología , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/farmacología , PPAR gamma/metabolismo , Animales , Chalconas/administración & dosificación , Chalconas/uso terapéutico , Quitosano/análogos & derivados , Diabetes Mellitus Experimental/metabolismo , Portadores de Fármacos/química , Hipoglucemiantes/administración & dosificación , Hipoglucemiantes/uso terapéutico , Riñón/efectos de los fármacos , Riñón/metabolismo , Hígado/efectos de los fármacos , Hígado/metabolismo , Masculino , PPAR gamma/genética , Páncreas/efectos de los fármacos , Páncreas/metabolismo , Ratas , Ratas Wistar
2.
J Cell Biochem ; 119(9): 7729-7737, 2018 09.
Artículo en Inglés | MEDLINE | ID: mdl-29923224

RESUMEN

The agonists of peroxisome proliferator-activated receptor gamma (PPARγ) from natural victual products were used as antidiabetic agents. Faba bean (Vicia faba L.) is a consequential legume that was known to possess potential antidiabetic activity, whose mechanism of action was unknown. The current study was focused to ascertain gene expression of the nuclear receptor PPARγ by Faba bean pod extract in rat cell lines (RINm5F).The real-time polymerase chain reaction analysis demonstrated that Faba bean pod extract in concentrations of 160 µg/mL have shown 4.97-fold stimulation compared with control. The cells treated with 320 µg/mL has shown 5.89-fold upregulation, respectively. Furthermore, in silico docking analysis was carried out against PPARγ, using the bioactive compounds identified from Faba bean pod extracts, which were known reported compounds from the literature. The results suggest that gene expression of PPARγ was inhibited by the constituents in Faba bean. In silico analysis prognosticates, butein has a high binding energy (-8.6 kcal/mol) with an atomic contact energy of -214.10, followed by Apigenin and Quercetin against PPARγ. Similarly, the percentage of interaction was high for butein, followed by Apigenin and Quercetin than other compounds comparatively. Hence, the results conclude inhibition of PPARγ by the bioactive compounds from Faba bean, which may provide insights into developing future therapeutic molecules for diabetes mellitus.


Asunto(s)
Línea Celular/química , Hipoglucemiantes/farmacología , PPAR gamma/genética , Extractos Vegetales/farmacología , Regulación hacia Arriba , Animales , Apigenina/química , Apigenina/farmacología , Chalconas/química , Chalconas/farmacología , Simulación por Computador , Relación Dosis-Respuesta a Droga , Hipoglucemiantes/química , Modelos Biológicos , Modelos Moleculares , Simulación del Acoplamiento Molecular , PPAR gamma/agonistas , PPAR gamma/química , Extractos Vegetales/química , Quercetina/química , Ratas , Vicia faba
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