Urease inhibition potential of Di-naphthodiospyrol from Diospyros lotus roots

Nat Prod Res. 2017 May;31(10):1214-1218. doi: 10.1080/14786419.2016.1226832. Epub 2016 Sep 1.

Abstract

The dimeric napthoquione 5,8,4'-trihydroxy-1'-methoxy-6, 6'-dimethyl-7,3'-binaphtyl-1,4,5',8'-tetraone (1) was isolated from the chloroform fraction of Diospyros lotus extract. Compound 1 was screened for its inhibitory effects against four enzymes: urease, phosphodiesterase-I, carbonic anhydrase-II and α-chymotrypsin, and showed selective activity against urease enzyme with an IC50 value of 254.1 ± 3.82 μM as compared to the standard thiourea (IC50 = 21 ± 0.11 μM). Furthermore, in silico docking study was carried out to explain the molecular mechanism of compound 1 against the target receptor.

Keywords: Diospyros lotus; Ebenaceae; di-naphthodiospyrol M; molecular docking; urease inhibitory activity.

MeSH terms

  • Chymotrypsin / antagonists & inhibitors
  • Diospyros / chemistry*
  • Molecular Docking Simulation
  • Naphthoquinones / chemistry
  • Naphthoquinones / pharmacology*
  • Plant Extracts / analysis
  • Plant Roots / chemistry
  • Urease / antagonists & inhibitors*

Substances

  • Naphthoquinones
  • Plant Extracts
  • di-naphthodiospyrol
  • Chymotrypsin
  • alpha-chymotrypsin
  • Urease