Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK)

Bioorg Med Chem Lett. 1999 Aug 2;9(15):2223-8. doi: 10.1016/s0960-894x(99)00380-7.

Abstract

Several oximes of triterpenes with a 17-beta hydroxyl and abietane derivatives are inhibitors of pyruvate dehydrogenase kinase (PDK) activity. The oxime 12 and dehydroabietyl amine 2 exhibit a blood glucose lowering effect in the diabetic ob/ob mouse after a single oral dose of 100 micromol/kg. However, the mechanism of the blood glucose lowering effect is likely unrelated to PDK inhibition.

MeSH terms

  • Administration, Oral
  • Animals
  • Blood Glucose / drug effects
  • Diabetes Mellitus, Experimental / drug therapy
  • Diabetes Mellitus, Experimental / metabolism
  • Disease Models, Animal
  • Diterpenes / chemical synthesis*
  • Diterpenes / pharmacology
  • Diterpenes / therapeutic use
  • Mice
  • Protein Kinase Inhibitors*
  • Protein Kinases*
  • Protein Serine-Threonine Kinases
  • Pyruvate Dehydrogenase Acetyl-Transferring Kinase
  • Rats
  • Rats, Sprague-Dawley
  • Structure-Activity Relationship
  • Triterpenes / chemical synthesis*
  • Triterpenes / pharmacology
  • Triterpenes / therapeutic use

Substances

  • Blood Glucose
  • Diterpenes
  • Protein Kinase Inhibitors
  • Pyruvate Dehydrogenase Acetyl-Transferring Kinase
  • Triterpenes
  • Protein Kinases
  • Protein Serine-Threonine Kinases