Heterodimeric Diterpenoids Isolated from Euphorbia ebracteolata Roots and Their Inhibitory Effects on α-Glucosidase

J Nat Prod. 2017 Dec 22;80(12):3218-3223. doi: 10.1021/acs.jnatprod.7b00595. Epub 2017 Nov 17.

Abstract

Two heterodimeric diterpenoids (1 and 2) comprising abietane lactone and nor-rosane constituent units were isolated from Euphorbia ebracteolata roots. Compound 1 exhibited a moderate inhibitory effect on α-glucosidase (IC50 = 7.94 μM), with a Ki value of 10.8 μM. In silico molecular docking has been performed to investigate the inhibition mechanism. Compound 2 inhibited the acetyl transfer activity of Mycobacterium tuberculosis GlmU (IC50 = 41.85 μM), which is a novel tuberculosis treatment target.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Diterpenes / chemistry*
  • Diterpenes / pharmacology*
  • Euphorbia / chemistry*
  • Glycoside Hydrolase Inhibitors / chemistry*
  • Glycoside Hydrolase Inhibitors / pharmacology*
  • Lactones / chemistry
  • Lactones / pharmacology
  • Molecular Docking Simulation / methods
  • Mycobacterium tuberculosis / drug effects
  • Plant Roots / chemistry*
  • Structure-Activity Relationship
  • alpha-Glucosidases / metabolism*

Substances

  • Diterpenes
  • Glycoside Hydrolase Inhibitors
  • Lactones
  • alpha-Glucosidases