title: 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).
authors.affiliation: a Institute of Chemical Sciences, University of Peshawar , Peshawar 25120 , KPK , Pakistan.
authors.forename: Abdur
authors.initials: A
authors.lastname: Rauf
authors.forename: Ghias
authors.initials: G
authors.lastname: Uddin
authors.forename: Ajmal
authors.initials: A
authors.lastname: Khan
authors.forename: Bina S
authors.initials: BS
authors.lastname: Siddiqui
authors.forename: Mohammad
authors.initials: M
authors.lastname: Arfan
authors.forename: Kourosh
authors.initials: K
authors.lastname: Dalvandi
authors.forename: Taibi
authors.initials: T
authors.lastname: Ben Hadda
mesh_terms: D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D027927:Pistacia / Q000737:chemistry*; D024301:Plant Bark / Q000737:chemistry; D014315:Triterpenes / Q000737:chemistry* / Q000302:isolation & purification
chemical_list: D014315:Triterpenes; C581170:pistagremic acid; D053829:Amyloid Precursor Protein Secretases
keywords: Pistacia integerrima; acetylcholinesterase and butyrylcholinesterase; pistagremic acid; selectivity; triterpenoid; β-secretase