Assessment of anti-cholinesterase activity and cytotoxicity of cagaita (Eugenia dysenterica) leaves

Food Chem Toxicol. 2017 Nov;109(Pt 2):996-1002. doi: 10.1016/j.fct.2017.02.032. Epub 2017 Feb 24.

Abstract

Eugenia dysenterica ex DC Mart. (Myrtaceae) is a Brazilian tree with pharmacological and biological properties. The aqueous leaf extract, rich in polyphenols, was tested in the human neuroblastoma cell line SH-SY5Y to evaluate its effect on cell viability. The extract and two isolated compounds were also assessed for the potential inhibitory activity on acetylcholinesterase, an enzyme related to Alzheimer's disease. A simple chromatographic method using Sephadex LH-20 was developed to separate catechin and quercetin from the aqueous leaf extract of E. dysenterica. Identification was carried out by spectroscopic techniques IR, UV, and 1H and 13C NMR. The IC50 values were obtained by constructing dose-response curves on a graph with percentage inhibition versus log of inhibitor concentration and compared with physostigmine, a well-known AChE inhibitor. The extract was toxic for SH-SY5Y cells at concentrations higher than 7.8 μg/ml given for 24 h. The decline in SH-SY5Y cell viability appears to be related to its antiproliferative activity. The extract also showed relatively moderate acetylcholinesterase inhibitory activity of 66.33% ± 0.52% at 1.0 mg/ml with an IC50 value of 155.20 ± 2.09 μg/ml. Physostigmine, quercetin, and catechin showed IC50 values of 18.69 ± 0.07, 46.59 ± 0.49, and 42.39 ± 0.67 μg/ml, respectively.

Keywords: Acetylcholinesterase; Alzheimer's disease; Catechin; Cerrado; Quercetin.

MeSH terms

  • Brazil
  • Cell Line
  • Cell Survival / drug effects
  • Cholinesterase Inhibitors / chemistry*
  • Cholinesterase Inhibitors / isolation & purification
  • Cholinesterase Inhibitors / pharmacology
  • Cholinesterases / chemistry
  • Eugenia / chemistry*
  • Humans
  • Kinetics
  • Phenols / chemistry
  • Phenols / isolation & purification
  • Phenols / pharmacology
  • Plant Extracts / chemistry*
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology
  • Plant Leaves / chemistry

Substances

  • Cholinesterase Inhibitors
  • Phenols
  • Plant Extracts
  • Cholinesterases