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Molecules ; 23(4)2018 Apr 19.
Artigo em Inglês | MEDLINE | ID: mdl-29671829

RESUMO

Diabetes mellitus is a chronic degenerative disease that causes long-term complications and represents a serious public health problem. In this manuscript, acankoreagenin isolated from the leaves of Acanthopanax gracilistylus (LAG) is thought to possess excellent anti-diabetic properties. In vitro, anti-diabetic activities were assessed based on the inhibitory activities with α-glucosidase (IC50 13.01 µM), α-amylase (IC50 30.81 µM), and PTP1B (IC50 16.39 µM). Acankoreagenin showed better anti-diabetic effects. Then, an investigation was performed to analyze the insulin secretion effects of the insulin-secreting cell line in RIN-m5F cells. It was found that acankoreagenin could increase the insulin release in RIN-m5F cells. It was also found that acankoreagenin reduced NO production, activity of caspase-3, and the reactive oxygen species levels in the cells injured by processing of cytokines. In western blotting, inactivation of NF-κB signaling was confirmed. Acankoreagenin (20 µM) showed a higher I-κBα expression and lower NF-κB expression than the control group and showed a better expression than the positive control L-NAME (1 mM) (p < 0.05). This study demonstrates the anti-diabetic effects of acankoreagenin in vitro and suggests acankoreagenin might offer therapeutic potential for treating diabetes mellitus.


Assuntos
Eleutherococcus/química , NF-kappa B/metabolismo , Folhas de Planta/química , Triterpenos/farmacologia , Animais , Humanos , Hipoglicemiantes/farmacologia , Proteína Tirosina Fosfatase não Receptora Tipo 1/metabolismo , Transdução de Sinais/efeitos dos fármacos , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo
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