Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa

Bioorg Med Chem Lett. 2010 Jan 15;20(2):513-5. doi: 10.1016/j.bmcl.2009.11.109. Epub 2009 Nov 26.

Abstract

Five iridoid glycosides were isolated from the MeOH extract of Hedyotis diffusa, and their structures were elucidated as E-6-O-p-methoxycinnamoyl scandoside methyl ester (1), Z-6-O-p-methoxycinnamoyl scandoside methyl ester (2), E-6-O-p-feruloyl scandoside methyl ester (3), E-6-O-p-coumaroyl scandoside methyl ester (4), and Z-6-O-p-coumaroyl scandoside methyl ester (5) by interpretation of their spectroscopic data. All the isolated compounds were evaluated for human neutrophil elastase inhibitory effect, and compound 1 showed potent activity with an IC(50) value of 18.0muM. The molecular docking simulation suggested a structural model for the inhibition of human neutrophil elastase by compound 1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding Sites
  • Computer Simulation
  • Hedyotis / chemistry*
  • Humans
  • Iridoids / chemistry*
  • Iridoids / isolation & purification
  • Iridoids / pharmacology
  • Leukocyte Elastase / antagonists & inhibitors*
  • Leukocyte Elastase / metabolism
  • Plant Extracts / chemistry
  • Protease Inhibitors / chemistry*
  • Protease Inhibitors / isolation & purification
  • Protease Inhibitors / pharmacology

Substances

  • 6-O-p-methoxycinnamoyl scandoside methyl ester
  • Iridoids
  • Plant Extracts
  • Protease Inhibitors
  • Leukocyte Elastase