Nuciferine stimulates insulin secretion from beta cells-an in vitro comparison with glibenclamide

J Ethnopharmacol. 2012 Jul 13;142(2):488-95. doi: 10.1016/j.jep.2012.05.024. Epub 2012 May 23.

Abstract

Ethnopharmacological relevance: Several Asian plants are known for their anti-diabetic properties and produce alkaloids and flavonoids that may stimulate insulin secretion.

Materials and methods: Using Vietnamese plants (Nelumbo nucifera, Gynostemma pentaphyllum, Smilax glabra, and Stemona tuberosa), we extracted two alkaloids (neotuberostemonine, nuciferine) and four flavonoids (astilbin, engeletin, smitilbin, and 3,5,3'-trihydroxy-7,4'-dimethoxyflavone), and studied their insulin stimulatory effects.

Results: Nuciferine, extracted from Nelumbo nucifera, stimulated both phases of insulin secretion in isolated islets, whereas the other compounds had no effect. The effect of nuciferine was totally abolished by diazoxide and nimodipine, and diminished by protein kinase A and protein kinase C inhibition. Nuciferine and potassium had additive effects on insulin secretion. Nuciferine also stimulated insulin secretion in INS-1E cells at both 3.3 and 16.7 mM glucose concentrations. Compared with glibenclamide, nuciferine had a stronger effect on insulin secretion and less beta-cell toxicity. However, nuciferine did not compete with glibenclamide for binding to the sulfonylurea receptor.

Conclusions: Among several compounds extracted from anti-diabetic plants, nuciferine was found to stimulate insulin secretion by closing potassium-adenosine triphosphate channels, explaining anti-diabetic effects of Nelumbo nucifera.

Publication types

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

MeSH terms

  • ATP-Binding Cassette Transporters / metabolism
  • Animals
  • Antihypertensive Agents / pharmacology
  • Aporphines / adverse effects
  • Aporphines / isolation & purification
  • Aporphines / pharmacology*
  • Cell Line
  • Cyclic AMP-Dependent Protein Kinases / pharmacology
  • Diazoxide / pharmacology
  • Glucose / pharmacology
  • Glyburide / pharmacology*
  • Hypoglycemic Agents / pharmacology*
  • Insulin / metabolism*
  • Insulin Secretion
  • Insulin-Secreting Cells / drug effects*
  • Insulin-Secreting Cells / metabolism
  • KATP Channels / metabolism
  • Mice
  • Nelumbo / chemistry*
  • Nimodipine / pharmacology
  • Plant Extracts / adverse effects
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology*
  • Potassium / pharmacology
  • Potassium Channels, Inwardly Rectifying / metabolism
  • Protein Kinase C / pharmacology
  • Receptors, Drug / metabolism
  • Sulfonylurea Receptors
  • Vietnam

Substances

  • ATP-Binding Cassette Transporters
  • Antihypertensive Agents
  • Aporphines
  • Hypoglycemic Agents
  • Insulin
  • KATP Channels
  • Plant Extracts
  • Potassium Channels, Inwardly Rectifying
  • Receptors, Drug
  • Sulfonylurea Receptors
  • Nimodipine
  • Cyclic AMP-Dependent Protein Kinases
  • Protein Kinase C
  • Glucose
  • Diazoxide
  • Potassium
  • Glyburide
  • nuciferine