Chemical Constituents from Solenostemma argel and their Cholinesterase Inhibitory Activity

Abstract

− 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(1→6)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-15β-D-glucopyranoside (7) and solargin I (8). Two of them (compounds 2 and 3) could inhibit over 50 % of butyrylcholinesterase activity at 100 µM. 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 π-π stacking interactions which could explain the compound potency to inhibit AChE and BChE.

Bioguided Isolation of Active Compounds from Rhamnus alaternus against Methicillin-Resistant Staphylococcus aureus (MRSA) and Panton-Valentine Leucocidin Positive Strains (MSSA-PVL)

“…NMR analyses ( 1 H and 13 C) of these compounds led to the identification of emodin ( 1 ) kaempferol ( 2 ) ( Figure 2 ). The spectroscopic data from the NMR spectra ( Figures S3 and S4 ) corroborate those previously reported in the literature [ 29 , 30 ]. In addition, mass spectrometry analyses were performed to confirm the structures obtained ( Figures S5–S8 ).…”

Myricetin Amorphous Solid Dispersions—Antineurodegenerative Potential

“…This structural difference may contribute to the higher affinity of myricetin towards BChE. Molecular docking (MD) is a key technique in structural molecular biology, as confirmed by numerous literature reports [96][97][98][99][100]. MD was used to observe and confirm possible interactions between MYR and AChE/BChE, which are important targets for neuroprotection.…”

Enhancing Therapeutic Efficacy of Donepezil, an Alzheimer’s Disease Drug, by Diplazium esculentum (Retz.) Sw. and Its Phytochemicals

“…These neuroprotective effects resulted from the plant’s bioactive compounds, quercetin and kaempferol. Kaempferol also inhibited AChE in a reversible mixed mode manner with an IC 50 value of 12.43 µM [ 33 ], exhibited 2-fold higher inhibitory activity against BChE than AChE [ 34 ], and also delayed memory loss by maintaining climbing ability and reducing AChE activity in a transgenic Drosophila model for AD [ 35 ]. Quercetin also acted as a reversible mixed inhibitor against AChE with an IC 50 value of 4.59 µM [ 36 ], while a 2.9-fold lower IC 50 value against BChE was observed [ 37 ], suggesting greater quercetin inhibitory capacity against BChE.…”