2. Academic Validation
  3. Caffeic acid phenethyl ester (CAPE)-derivatives act as selective inhibitors of acetylcholinesterase

Caffeic acid phenethyl ester (CAPE)-derivatives act as selective inhibitors of acetylcholinesterase

  • Eur J Med Chem. 2019 Sep 1:177:259-268. doi: 10.1016/j.ejmech.2019.05.059.
Josephine M Gießel 1,  Anne Loesche 1,  René Csuk 2,  Immo Serbian 1
Affiliations

Affiliations

  • 1 Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D- 06120, Halle (Saale), Germany.
  • 2 Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D- 06120, Halle (Saale), Germany. Electronic address: rene.csuk@chemie.uni-halle.de.
PMID: 31158743 DOI: 10.1016/j.ejmech.2019.05.059
Abstract

Unexpected inhibitory effects against eeAChE could be found for a newly synthesized class of caffeic acid phenethyl ester (CAPE) derivatives. Thus, phenethyl-(E)-3-(3,5-dimethoxy-4-phenethoxyphenyl)-acrylate (Ki = 1.97 ± 0.38 μM, Ki´ = 2.44 ± 0.07 μM) and 4-(2-(((E)-3-(3,4-bis(benzyloxy)phenyl)acryloyl)oxy)ethyl)-1,2-phenylene (2E,2'E)-bis(3-(3,4-bis(benzyloxy)phenyl)acrylate) (Ki = 0.72 ± 0.31 μM, Ki´ = 1.80 ± 0.21 μM) showed very good inhibition of eeAChE, while being non cytotoxic for malignant human Cancer cells and non-malignant mouse fibroblasts. Also, they are weak inhibitors for BChE (from equine serum).

Keywords

Acetylcholinesterase; Butyrylcholinesterase; Caffeic acid phenethyl ester; Cinnamic acid phenethyl esters; Inhibitors.

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