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

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
• pistagremic acid
• triterpenoid
• β-secretase
• selectivity
• acetylcholinesterase and butyrylcholinesterase

Additional information

Funding

The authors are grateful for the financial supported by Higher Education Commission of Pakistan and Institute of Chemical Sciences, University of Peshawar, Peshawar, Pakistan.