Anti-Diabetic Effects of Acankoreagenin from the Leaves of Acanthopanax Gracilistylus Herb in RIN-m5F Cells via Suppression of NF-κB Activation

Molecules. 2018 Apr 19;23(4):958. doi: 10.3390/molecules23040958.

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.

Keywords: Acanthopanax gracilistylus; PTP1B; RIN-m5F cells; acankoreagenin; anti-diabetic effects; α-amylase; α-glucosidase.

MeSH terms

  • Animals
  • Eleutherococcus / chemistry*
  • Humans
  • Hypoglycemic Agents / pharmacology
  • NF-kappa B / metabolism*
  • Plant Leaves / chemistry*
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1 / metabolism
  • Signal Transduction / drug effects
  • Triterpenes / pharmacology*
  • alpha-Amylases / metabolism
  • alpha-Glucosidases / metabolism

Substances

  • Hypoglycemic Agents
  • NF-kappa B
  • Triterpenes
  • acankoreagenin
  • PTPN1 protein, human
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1
  • alpha-Amylases
  • alpha-Glucosidases