Selective dual cholinesterase inhibitors from Aconitum laeve

Ahmad H 1 , Ahmad S 1 , Shah SAA 2 , Khan HU 3 , Khan FA 4 , Ali M 1 Show all authors , Latif A 1 , Shaheen F 5 , Ahmad M 1

Affiliations 

  • 1 a Department of Chemistry , University of Malakand , Dir (Lower) 18550 , Pakistan
  • 2 c Faculty of Pharmacy , Universiti Teknologi MARA , Bandar Puncak Alam 42300 , Malaysia
  • 3 e Department of Biotechnology, University of Science and Technology , Bannu 28100 , Pakistan
  • 4 g Department of Chemistry , Shaheed Benazir Bhutto University Sheringal , Dir (Upper) 18000 , Pakistan
  • 5 f HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences (ICCBS), University of Karachi , Karachi 75270 , Pakistan
J Asian Nat Prod Res, 2018 Feb;20(2):172-181.
PMID: 28463565 DOI: 10.1080/10286020.2017.1319820

Abstract

New lycoctonine-type dual cholinesterase inhibitor, swatinine-C (1), along with three known norditerpenoid alkaloids, hohenackerine (2), aconorine (5) and lappaconitine (6) and two synthetically known but phytochemically new benzene derivatives, methyl 2-acetamidobenzoate (3) and methyl 4-[2-(methoxycarbonyl)anilino]-4-oxobutanoate (4), was isolated from the roots of A. laeve. Structures of new and known compounds (1-6) were established on the basis of latest spectroscopic techniques and by close comparison with the data available in literature. In vitro, compounds (1-6) were tested against AChE and BChE inhibitory activities. Compounds 1 and 2 showed competitive inhibition against AChE (IC50 = 3.7 μM, 4.53 μM) and BChE (IC50 = 12.23 μM, 9.94 μM), respectively. Compounds 5 and 6 showed promising noncompetitive type of inhibitory profile against AChE (IC50 = 2.51 and 6.13 μM) only. Compounds 3 and 4 showed weak inhibitory profile against both AChE and BChE.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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