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

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Version 2 2015-08-04, 14:27
Version 1 2015-08-04, 14:27
journal contribution
posted on 2015-08-04, 14:27 authored by Abdur Rauf, Ghias Uddin, Ajmal Khan, Bina S. Siddiqui, Mohammad Arfan, Kourosh Dalvandi, Taibi Ben Hadda

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).

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