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Chemical Constituents from Solenostemma argel and their Cholinesterase Inhibitory Activity

  • Demmak, Rym Gouta (Laboratoire de Biochimie Appliquee, Departement des Sciences de la Nature et de la Vie, Universite Freres Mentouri-Constantine) ;
  • Bordage, Simon (Laboratoire de Pharmacognosie, Univ. Lille) ;
  • Bensegueni, Abederrahmane (Laboratoire de Biochimie Appliquee, Departement des Sciences de la Nature et de la Vie, Universite Freres Mentouri-Constantine) ;
  • Boutaghane, Naima (Laboratoire d'Obtention des Substances Therapeutiques (LOST), Campus Chaabet-Ersas, Departement de chimie, Universite des Freres Mentouri-Constantine) ;
  • Hennebelle, Thierry (Laboratoire de Pharmacognosie, Univ. Lille) ;
  • Mokrani, El Hassen (Laboratoire de Biochimie Appliquee, Departement des Sciences de la Nature et de la Vie, Universite Freres Mentouri-Constantine) ;
  • Sahpaz, Sevser (Laboratoire de Pharmacognosie, Univ. Lille)
  • 투고 : 2018.11.12
  • 심사 : 2018.12.09
  • 발행 : 2019.06.30

초록

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($1{\rightarrow}6$)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-$15{\beta}$-D-glucopyranoside (7) and solargin I (8). Two of them (compounds 2 and 3) could inhibit over 50 % of butyrylcholinesterase activity at $100{\mu}M$. 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 ${\pi}-{\pi}$ stacking interactions which could explain the compound potency to inhibit AChE and BChE.

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