Abstract

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.

Highlights

  • Diabetes mellitus (DM) is considered one of the five leading causes of death in the world.The increased prevalence of diabetes has topped the list of global epidemic health concerns worldwide.Globally, an estimated 422 million adults were living with diabetes in 2014 compared to 108 million in1980

  • There are two types of diabetes mellitus: Type 1 is the lack of insulin due to a destructive process in pancreatic β-cells and Type 2 is a steady decline in the use of glucose due to resistance of the tissues to insulin [1]

  • The effect of it on the insulin release under a glucose challenge was significantly higher than that in the basal state. These results demonstrated that acankoreagenin increased insulin release in a dose dependent manner with 11.05 ± 0.12 ng/mL, 11.68 ± 0.11 ng/mL, and 12.92 ± 0.1 ng/mL at concentrations of 5 μM, 10 μM, and 20 μM, respectively, which were stronger than the positive control glybunide [40] at aconcentrations of 25 μM, 50 μM, and 100 μM

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Summary

Introduction

Diabetes mellitus (DM) is considered one of the five leading causes of death in the world.The increased prevalence of diabetes has topped the list of global epidemic health concerns worldwide.Globally, an estimated 422 million adults were living with diabetes in 2014 compared to 108 million in1980. Diabetes mellitus (DM) is considered one of the five leading causes of death in the world. The increased prevalence of diabetes has topped the list of global epidemic health concerns worldwide. An estimated 422 million adults were living with diabetes in 2014 compared to 108 million in. The global prevalence (age-standardized) of diabetes has nearly doubled since 1980 rising from. There are two types of diabetes mellitus: Type 1 is the lack of insulin due to a destructive process in pancreatic β-cells and Type 2 is a steady decline in the use of glucose due to resistance of the tissues to insulin [1]. Insulin-secreting β-cells failure is a common feature of diabetes, which leads to relative or absolute insulin deficiency.

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