Natural Product Sciences · 2019 · 19 citations · 23 references
MedicineMedicinal ChemistryPharmacologyEnzymologyNeurochemistryNeuropharmacologyCholinergic NeurochemistryCholinergic PharmacologyCholinergic SignalingEnzyme InhibitionNeurochemical PharmacologyNeurodegenerative Disease PharmacologyAcetylcholinesterase FunctionAcetylcholinesterase InhibitorsAcetylcholinesterase TargetsBioactive ConstituentsButyrylcholinesterase InhibitionCholine Acetyltransferase Activity
Alzheimer's disease is a chronic neurodegenerative disorder with no curative treatment. The commercially available drugs, which target acetylcholinesterase, are not satisfactory. The aim of this study was to investigate the cholinesterase inhibitory activity of Solenostemma argel aerial part. Eight compounds were isolated and identified by NMR: kaempferol-3-O-glucopyranoside (1), kaempferol (2), kaempferol-3-glucopyranosyl(16)rhamnopyranose (3) p-hydroxybenzoic acid (4), dehydrovomifoliol (5), 14,15-dihydroxypregn-4-ene-3,20-dione (6), 14,15-dihydroxy-pregn-4-ene-3,20-dione-15-D-glucopyranoside (7) and solargin I (8). Two of them (compounds 2 and 3) could inhibit over 50 % of butyrylcholinesterase activity at 100 M. Compound (2) displayed the highest inhibitory effect against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with a slight selectivity towards the latter. Molecular docking studies supported the in vitro results and revealed that (2) had made several hydrogen and - stacking interactions which could explain the compound potency to inhibit AChE and BChE.
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VMD: Visual molecular dynamics
William Humphrey, Andrew Dalke, Klaus Schulten · Journal of Molecular Graphics · 1996 · 66.6K citations
Saviana Di Giovanni, A. Borloz, Aurélie Urbain et al. · European Journal of Pharmaceutical Sciences · 2007 · 123 citations