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Updated: Jan 27, 2026

Transient Expression in Nicotiana Benthamiana Leaves for Triterpene Production at a Preparative Scale
Published on: August 16, 2018
Triterpene-Based Carboxamides Act as Good Inhibitors of Butyrylcholinesterase
Anne Loesche1, Michael Kahnt2, Immo Serbian3
1Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany. anne.loesche@chemie.uni-halle.de.
Abstract:
A set of overall 40 carboxamides was prepared from five different natural occurring triterpenoids including oleanolic, ursolic, maslinic, betulinic, and platanic acid. All of which were derived from ethylene diamine holding an additional substituent connected to the ethylene diamine group. These derivatives were evaluated regarding their inhibitory activity of the enzymes acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) employing Ellman's assay. We further determined the type of inhibition and inhibition constants. Carboxamides derived from platanic acid have been shown to be potent and selective BChE inhibitors. Especially the mixed-type inhibitor (3β)-N-(2-pyrrolidin-1-ylethyl)-3-acetyloxy-20-oxo-30-norlupan-28-amide (35) showed a remarkably low Ki of 0.07 ± 0.01 µM (Ki' = 2.38 ± 0.48 µM) for the inhibition of BChE.
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