Boerhaavia diffusa inhibits key enzymes linked to type 2 diabetes in vitro and in silico; and modulates abdominal glucose absorption and muscle glucose uptake ex vivo

Biomed Pharmacother. 2018 Oct:106:1116-1125. doi: 10.1016/j.biopha.2018.07.053. Epub 2018 Jul 17.

Abstract

The present study investigated the in vitro and ex vivo antioxidant, anti-diabetic and anti-obesogenic potentials of different solvent (ethyl acetate, ethanol and water) extracts from the aerial parts of Boerhaavia diffusa. The ferric reducing antioxidant power (FRAP), DPPH scavenging activity and the ameliorative effects of the extracts on Fe2+-induced oxidative injury was investigated both in vitro and ex vivo. Alpha glucosidase and pancreatic lipase inhibitory potentials of the extracts were examined in vitro, while the effects of the ethanol extract on abdominal glucose intake and muscle glucose uptake were determined in freshly harvested tissues ex vivo. The extracts were subjected to Gas Chromatography-Mass Spectrometry (GC-MS) analysis to identify their possible bioactive components. The ethanol extract showed the most potent FRAP and DPPH radical scavenging activities compared to other extracts. All extracts increased catalase and SOD activities, and GSH levels in oxidative pancreatic injury. Both ethanol and aqueous extracts exhibited remarkable enzyme inhibitory activities, which was significantly higher than ethyl acetate extract and acarbose but was not comparable to orlistat. The ethanol extract portrayed a dose-dependent inhibitory effect on jejunal glucose uptake and enhancement of muscle glucose uptake. 9-(4 methoxyphenyl) xanthene, xanthone and stigmasterol showed strong binding affinities for α-glucosidase and lipase enzymes tested. Data from this study suggest that aerial parts of B. diffusa (particularly the ethanol extract) may not only exhibit antioxidant potentials but may also mediate anti-lipidemic and anti-hyperglycemic effects via inhibiting fat and carbohydrate digestion as well as abdominal glucose intake and enhancing muscle glucose uptake.

Keywords: Antioxidant; Boerhaavia diffusa; Enzyme inhibition; Glucose absorption; Glucose uptake.

Publication types

  • Comparative Study

MeSH terms

  • Acetates / chemistry
  • Animals
  • Anti-Obesity Agents / pharmacology
  • Antioxidants / pharmacology
  • Biomarkers / blood
  • Blood Glucose / drug effects
  • Blood Glucose / metabolism
  • Diabetes Mellitus, Type 2 / blood
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / isolation & purification
  • Enzyme Inhibitors / pharmacology*
  • Ethanol / chemistry
  • Glycoside Hydrolase Inhibitors / pharmacology
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / isolation & purification
  • Hypoglycemic Agents / pharmacology*
  • Intestinal Absorption / drug effects*
  • Jejunum / drug effects*
  • Jejunum / metabolism
  • Lipase / antagonists & inhibitors
  • Lipase / metabolism
  • Male
  • Models, Biological
  • Molecular Docking Simulation
  • Muscle, Skeletal / drug effects*
  • Muscle, Skeletal / metabolism
  • Nyctaginaceae* / chemistry
  • Oxidative Stress / drug effects
  • Pancreas / drug effects
  • Pancreas / enzymology
  • Phytotherapy
  • Plant Components, Aerial
  • Plant Extracts / chemistry
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology*
  • Plants, Medicinal
  • Rats, Sprague-Dawley
  • Solvents / chemistry
  • Structure-Activity Relationship
  • Water / chemistry

Substances

  • Acetates
  • Anti-Obesity Agents
  • Antioxidants
  • Biomarkers
  • Blood Glucose
  • Enzyme Inhibitors
  • Glycoside Hydrolase Inhibitors
  • Hypoglycemic Agents
  • Plant Extracts
  • Solvents
  • Water
  • Ethanol
  • ethyl acetate
  • Lipase