Pistagremic acid, a novel β-secretase enzyme (BACE1) inhibitor from Pistacia integerrima Stewart

Nat Prod Res. 2015;29(18):1735-8. doi: 10.1080/14786419.2014.997231. Epub 2015 Jan 15.

Abstract

A new triterpenic compound named pistagremic acid (PA) was once again isolated from Pistaciaintegerrima. The β-secretase inhibition study was carried out. Compound PA was found significantly active against β-secretase enzyme (BACE1) with IC50 value of 350 ± 2 nM in comparison to the standard inhibitors [Asn670, Sta671, Val672]-amyloid-β/A4 precursor protein 770 fragment 662-675 (IC50 = 290.71 ± 1 nM). The selectivity of this compound was also evaluated against the acetylcholinesterase and butyrylcholinesterase enzymes. Interestingly compound PA was found to be inactive against them and showed selectivity towards β-secretase enzyme (BACE1).

Keywords: Pistacia integerrima; acetylcholinesterase and butyrylcholinesterase; pistagremic acid; selectivity; triterpenoid; β-secretase.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amyloid Precursor Protein Secretases / antagonists & inhibitors*
  • Inhibitory Concentration 50
  • Molecular Structure
  • Pistacia / chemistry*
  • Plant Bark / chemistry
  • Triterpenes / chemistry*
  • Triterpenes / isolation & purification

Substances

  • Triterpenes
  • pistagremic acid
  • Amyloid Precursor Protein Secretases