Anticholinesterase activity of 3-formylchromone derivatives


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Abstract

The aim of the study. To evaluate the anticholinesterase activity of 3-formylchromine derivatives in experimental Alzheimer's disease in rats. Material and methods. The work was performed on male Wistar rats that were modeled for Alzheimer's disease by injecting the fragment AB1-42 into the CA1 part of the hippocampus. The test-compounds and the reference drug (ipidacrine, 1 mg / kg, per os) were administered for 60 days. Further, the preservation of the memorable trace in the Morris water maze test and the acetylcholinesterase activity by photometric method in the hippocampus were evaluated. Results. In the course of the work, it was found that among the eighteen studied substances the most pronounced anticholinesterase effect provided by 3-[(E)-3-(3,5-ditret-butyl-4-hydroxy-phenyl)-3-oxo-prop-1-enyl]-6-methoxy-chromene-4-one, the use of which at a dose of 40 mg/kg (oral), reduced the activity of hippocampus acetylcholinesterase by 50.5% (p<0.05) and contributed to the preservation of spatial memory in rats equally with the reference drug. Conclusion. The study demonstrated that the use of 3-formylchromone derivatives and to a greater extent 3-[(E)-3-(3,5-ditret-butyl- 4-hydroxy-phenyl)-3-oxo-prop-1-enyl]-6-methoxy-chromene-4-one contributed to the preservation of a memorable trace in animals with experimentally modeled Alzheimer's disease, which may be associated with the anticholinesterase effect of these compounds.

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About the authors

D. I Pozdnyakov

Pyatigorsk medical and pharmaceutical institute

Email: pozdniackow.dmitry@yandex.ru
Ph.D. (Pharm.), Associate Professor of Department of Pharmacology with Clinical Pharmacology Course, Head of Living System Laboratory Pyatigorsk, Russia

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