Inhibitory effect of (-), (+) clausenamide on acetylcholinesterase in vitro

W. Z. Duan, J. T. Zhang

Research output: Contribution to journalArticlepeer-review

Abstract

To study the effects of (-), (+) clausenamide on acetyleholinesterase (ACHE). AChE activities were determined by colorimetric method of Ellman. The results showed that (-), (+) clausenamide inhibited AChE activity in hippocampus and frontal cortex of mouse brain. The IC50(95% confidence limit) value of (-)clausenamide was 0.31 (0.27-0.36) mmol · L-1 in frontal cortex and 0.33 (0.28-0.39) mmol · L-1 in hippocampus; the value of (+) clausenamide was 0.71 (0.53-0.94) mmol · L-1 in frontal cortex and 0.77 (0.55-1.07) mmol · L-4 in hippocampus. The inhibition of (-), (+) clausenamide on AChE activity of erythrocyte membrane was of linear mixed type and in a reversible manner. The inhibition constant K1 values of (-) clausenamide and (+) clausenamide were 0.26 mmol · L-1 and 0.72 mmol · L-1 K(i) values of (-) clausenamide and (+) clausenamide were 1. 205 mmol · L-1 and 1. 856 mmol · L-1 respectively. These results suggest that clausenamide is a new reversible AChE inhibitor, and the inhibitory effect on AChE of (-) clausenamide is more potent than that of (+) clausenamide.

Original languageEnglish (US)
Pages (from-to)16-19
Number of pages4
JournalChinese Journal of Pharmacology and Toxicology
Volume12
Issue number1
StatePublished - Jan 1 1998
Externally publishedYes

Keywords

  • Chirality
  • Cholinesterase inhibitors
  • Clausenamide

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology

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