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Two fast screening methods (GC-MS and TLC-ChEI assay) for rapid evaluation of potential anticholinesterasic indole alkaloids in complex mixtures

Overview of attention for article published in Anais da Academia Brasileira de Ciências, September 2008
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Title
Two fast screening methods (GC-MS and TLC-ChEI assay) for rapid evaluation of potential anticholinesterasic indole alkaloids in complex mixtures
Published in
Anais da Academia Brasileira de Ciências, September 2008
DOI 10.1590/s0001-37652008000300003
Pubmed ID
Authors

Ivo J.C. Vieira, Walter L.B. Medeiros, Cecilia S. Monnerat, Jucimar J. Souza, Leda Mathias, Raimundo Braz-Filho, Angelo C. Pinto, Priscila M. Sousa, Claudia M. Rezende, Rosângela De A. Epifanio

Abstract

The pharmacotherapy for Alzheimer's disease (AD) includes the use of acetylcholinesterase inhibitors (AChEI). Recent investigations for novel AD therapeutic agents from plants suggested that Tabernaemontana genus is a promising source of novel anticholinesterasic indole alkaloids. In this work two fast screening techniques were combined in order to easily identify novel cholinesterase inhibitors (ChEI). Gas chromatography-mass spectrometry (GC-MS) of the less polar alkaloidic fractions obtained from the acid-base extraction of the stalk of T. laeta revealed thirteen monoindole alkaloids, four of them confirmed by co-injection with previously isolated alkaloids. The others were tentatively identified by mass fragmentation analysis. By gas chromatography with flame ionization detection (GC-FID) and using isatin as internal standard, affinisine and voachalotine were determined as major compounds. These fractions and fourteen previously isolated alkaloids, obtained from root bark of T. laeta and T. hystrix were investigated for acetyl (AChE) and butyrylcholinesterase (BuChE) inhibitory activities by the modified Ellman's method in thin layer chromatography(TLC-ChEI). Results showed selective inhibition of the alkaloids heyneanine and Nb-methylvoachalotine for BuChE, and 19-epi-isovoacristine for AChE, whereas olivacine, affinisine, ibogamine, affinine, conodurine and hystrixnine inhibited both enzymes. In addition to confirming that monoterpenoid indole alkaloids can be novel therapeutic agents for AD, this is the first report of the ChEI activity of olivacine, a pyridocarbazole alkaloid.

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Mendeley readers

The data shown below were compiled from readership statistics for 50 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Algeria 1 2%
Brazil 1 2%
Unknown 48 96%

Demographic breakdown

Readers by professional status Count As %
Student > Master 7 14%
Researcher 6 12%
Student > Bachelor 5 10%
Student > Ph. D. Student 5 10%
Student > Doctoral Student 4 8%
Other 13 26%
Unknown 10 20%
Readers by discipline Count As %
Chemistry 11 22%
Agricultural and Biological Sciences 7 14%
Biochemistry, Genetics and Molecular Biology 3 6%
Pharmacology, Toxicology and Pharmaceutical Science 3 6%
Neuroscience 2 4%
Other 7 14%
Unknown 17 34%