The Molecular Targets of Swertiamarin and its Derivatives Confer Anti- Diabetic and Anti-Hyperlipidemic Effects

Curr Drug Targets. 2018;19(16):1958-1967. doi: 10.2174/1389450119666180406113428.

Abstract

The herbal plant extract of Enicostemma littorale is widely used to medicate and treat type II Diabetes. This extract in medicine has shown its value in reducing blood glucose & lipid levels, and improving the kidney functioning, lipid profile, controlling blood pressure and heart rate. The well characterized chemical components such as iridoid and secoiridoid glycosides are present in aqueous and ethanolic extracts of the plant. Swertiamarin, a secoiridoid glycoside, is identified as the lead compound that confers anti-hyperglycemic & anti-hyperlipidemic effects. The swertiamarin binds with one or more molecular targets to alter their expression and/or activity. The in silico, in vivo and in vitro studies have been carried out to uncover the underlying molecular mechanism of action of swertiamarin and its derivatives for showing the better anti-diabetic & anti-hyperlipidemic activities. In brief, the present review focuses on unraveling the information about molecular targets of swertiamarin. Our review will open new avenues to develop therapeutic approaches and drugs to treat diabetes and other inflammatory diseases.

Keywords: Enicostemma littorale; Swertiamarin; anti-diabetic; anti-hyperlipidemic; insulin sensitizer; semi-synthetic derivatives; type 2 diabetes mellitus..

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Computer Simulation
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Diabetes Mellitus, Type 2 / metabolism
  • Disease Models, Animal
  • Gentianaceae / chemistry
  • Glucose / metabolism
  • Humans
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacology*
  • Hypoglycemic Agents / therapeutic use
  • Hypolipidemic Agents / chemistry
  • Hypolipidemic Agents / pharmacology*
  • Hypolipidemic Agents / therapeutic use
  • Insulin / metabolism
  • Iridoid Glucosides / chemistry
  • Iridoid Glucosides / pharmacology*
  • Iridoid Glucosides / therapeutic use
  • Lipid Metabolism / drug effects
  • Metabolic Networks and Pathways / drug effects
  • Metabolic Syndrome / drug therapy*
  • Metabolic Syndrome / metabolism
  • Molecular Targeted Therapy / methods
  • Pyrones / chemistry
  • Pyrones / pharmacology*
  • Pyrones / therapeutic use
  • Signal Transduction / drug effects
  • Structure-Activity Relationship

Substances

  • Hypoglycemic Agents
  • Hypolipidemic Agents
  • Insulin
  • Iridoid Glucosides
  • Pyrones
  • swertiamarin
  • Glucose