Journal archive > 2012 > N 1 January-February

ISOMERIC DERIVATIVES OF LUPININE AND EPILUPININE – ORGANOPHOSPHORUS
INHIBITORS OF CHOLINESTERASES

N. E. Basova, B. N. Kormilitsyn, A. Yu. Perchenok, E. V. Rozengart, V. S. Saakov, A. A. Suvorov

Sechenov Institute of Evolutionary Physiology and Biochemistry,
Russian Academy of Science, St. Petersburg;

The isomeric-structure analysis data of anticholinesterase action of organophosphorous inhibitors with similar structure help in the search of specific effectors and detection of differences in reactivity of various animals’ enzymes. This study compared the data of efficacy in respect of 4 mammal and 5 arthropoda cholineste­rase preparations for 26 quinolizidine inhibitors, which molecules contain both the isomeric unbranched and branched alkoxyl radicals in the phosphoryl group, and the epimeric lupinine and epilupinine derivatives in the leaving group. The changes in the alkoxyl radical structure of inhibitor molecules act on their efficacy only with respect to the mammal enzymes («group» inhibitor specificity). The differences between lupinine and epilupinine derivatives were revealed. Highly specific inhibitors of different enzymes were detected among the tested compounds.

Key words: lupinine, epilupinine, cholinesterase, organophosphorous inhibitors, structure-activity relationship.

The original article in Russian is available for download in PDF format.

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