Therapeutic effect of astragaloside-IV on bradycardia is involved in up-regulating klotho expression

Life Sci. 2016 Jan 1:144:94-102. doi: 10.1016/j.lfs.2015.11.021. Epub 2015 Nov 22.

Abstract

Aims: In order to determine whether klotho is involved in the therapeutic effects of Astragaloside-IV on bradycardia, we evaluated the effect of ASG-IV on klotho and the effect of klotho on HCN4 and If.

Main methods: Administrating isoproterenol (5 mg/kg) for 15 days to establish a rat bradycardia model randomized SD rats into control, model (ISO) and ASG-IV (5 mg/kg/day) groups to explore the effect of ASG-IV on klotho. Rats were sacrificed on day 15 after heart rate and heart function were measured; SAN tissues were collected to measure the expression of klotho and HCN4. In vitro, neonatal rat myocardial cells were incubated with LPS for 24 h to inhibit the expression of HCN4 and incubated with LPS+ klotho to explore the effect of klotho on HCN4 expression. We also adopted full-patch-clamp technique to explore the effect of klotho on If.

Key findings: Heart rate in model group was significantly decreased (356.6±19.7 vs. 428.9±19.9 in control group, P<0.01) and ASG-IV can increase heart rate (401.4±12.0 vs. 356.6±19.7 in model group, P<0.01). The expression of klotho was also up-regulated (P<0.05). In vitro, after incubation with LPS for 24h, HCN4 expression was significantly decreased in neonatal rat myocardial cells (0.6±0.07 vs. 1.0, P<0.01) and If was significantly declined. Exogenous klotho showed protective effect on HCN4 expression (1.58±0.16 in ASG-IV group vs. 0.6±0.07 in LPS group, P<0.05) and If.

Significance: Klotho is involved in the treatment mechanism of ASG-IV.

Keywords: Astragaloside IV; Bradycardia; HCN4; ISO; Klotho.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic beta-Agonists
  • Animals
  • Animals, Newborn
  • Bradycardia / chemically induced
  • Bradycardia / drug therapy*
  • Bradycardia / genetics*
  • Glucuronidase / biosynthesis*
  • Glucuronidase / genetics*
  • Heart Function Tests
  • Heart Rate / drug effects
  • Hyperpolarization-Activated Cyclic Nucleotide-Gated Channels / biosynthesis
  • Hyperpolarization-Activated Cyclic Nucleotide-Gated Channels / genetics
  • Isoproterenol
  • Klotho Proteins
  • Lipopolysaccharides / pharmacology
  • Myocytes, Cardiac / drug effects
  • Myocytes, Cardiac / metabolism
  • Patch-Clamp Techniques
  • Potassium Channels / biosynthesis
  • Potassium Channels / genetics
  • Rats
  • Rats, Sprague-Dawley
  • Saponins / pharmacology
  • Saponins / therapeutic use*
  • Triterpenes / pharmacology
  • Triterpenes / therapeutic use*
  • Up-Regulation / drug effects

Substances

  • Adrenergic beta-Agonists
  • HCN4 protein, rat
  • Hyperpolarization-Activated Cyclic Nucleotide-Gated Channels
  • Lipopolysaccharides
  • Potassium Channels
  • Saponins
  • Triterpenes
  • astragaloside A
  • Glucuronidase
  • Klotho Proteins
  • Isoproterenol