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1.
Biomed Pharmacother ; 134: 111151, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33370629

RESUMO

Different portions (stem GIS and leaf GIL) of Garcinia linii were extracted by ethanol/water and crude extracts were employed to investigate the contents of total phenol and flavonoids, antioxidation activities, and inhibitory activities of α-amylase and α-glucosidase via enzymatic assay and OGTT and OSTT for lowering glucose levels. The data revealed that GlS and GlL contained different levels of flavonoids and total phenol. Furthermore, the results showed the extracts exhibited remarkable antioxidation activities and inhibitory activities of α-amylase and α-glucosidase. In silico docking studies were done using Gold software and the probable molecules retrieved from PubChem were docked with several anti-diabetic relate targets, the results showed several components of G. linii could potentially inhibit diabetic molecules when compared with clinic drugs. The cell glucose uptake data also confirmed that GlL and GlS could retain the active component in the regulation of insulin, AMPK, PPARγ, and DPP4. In vivo, the evidence showed G. linii extracts including syringaldehyde suppressed effect of hyperglycemia on OSTT and OGTT assays. These results suggest that G. linii extract has a potential therapeutic value for the treatment of diabetes in humans.


Assuntos
Antioxidantes/farmacologia , Glicemia/efeitos dos fármacos , Diabetes Mellitus/tratamento farmacológico , Garcinia , Inibidores de Glicosídeo Hidrolases/farmacologia , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidores , Células 3T3 , Adipócitos/efeitos dos fármacos , Adipócitos/enzimologia , Animais , Antioxidantes/isolamento & purificação , Biomarcadores/sangue , Glicemia/metabolismo , Diabetes Mellitus/sangue , Diabetes Mellitus/enzimologia , Diabetes Mellitus/etiologia , Dieta Hiperlipídica , Modelos Animais de Doenças , Garcinia/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Hepatócitos/efeitos dos fármacos , Hepatócitos/enzimologia , Masculino , Camundongos , Camundongos Endogâmicos ICR , Simulação de Acoplamento Molecular , Obesidade/etiologia , Extratos Vegetais/isolamento & purificação , Folhas de Planta , Caules de Planta , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo
2.
Medicina (Kaunas) ; 55(5)2019 May 07.
Artigo em Inglês | MEDLINE | ID: mdl-31067805

RESUMO

Background and objectives: The percutaneous route is an interesting and inventive investigation field of drug delivery. However, it is challenging for drug molecules to pass through the skins surface, which is a characterized by its permeability barrier. The purpose of this study is to look at the effect of some penetration enhancers on in vivo permeation of insulin and insulin sensitizers (curcumin and rutin) through diabetes-induced mouse skin. Materials and Methods: Sting crude extracts of Dendrocnide meyeniana, Urtica thunbergiana Sieb. and Zucc, and Alocasia odora (Lodd.) Spach were used as the penetration enhancers. Mouse skin irritation was tested by smearing the enhancers for the measurements at different time points and the cell viability of the HaCaT human skin keratinocytes, which was determined by Trypan blue exclusion and MTT assays to evaluate human biosafety for these extracts after the mouse skin permeation experiments. Results: All enhancers induced a slight erythema without edema on the mouse skin that completely recovered after 6 h from the enhancer smears as compared with normal mouse skin. Furthermore, no damaged cells were found in the HaCaT keratinocytes under sting crude extract treatments. The blood sugar level in the diabetic mice treated with the insulin or insulin sensitizers, decreased significantly (p < 0.05) in the presence of enhancers. The area under the curve (AUC) values of transdermal drug delivery (TDD) ranged from 42,000 ± 5000 mg/dL x min without enhancers, to 30,000 ± 2000 mg/dL x min in the presence of enhancers. Conclusions: This study exhibited that natural plant extracts could be preferred over the chemically synthesized molecules and are safe and potent penetration enhancers for stimulating the transdermal absorption of drugs.


Assuntos
Administração Cutânea , Hipoglicemiantes/administração & dosagem , Aizoaceae , Análise de Variância , Teste de Tolerância a Glucose/métodos , Humanos , Hipoglicemiantes/uso terapêutico , Extratos Vegetais/uso terapêutico , Rutaceae
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