Effect of biginelli pyrimidines on production of reactive oxygen species by polymorphonuclear leukocytes |
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Authors: | Yu V Shatalin V S Shubina A S Fisyuk |
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Institution: | 1.Pushchino State University,Pushchino, Moscow oblast,Russia;2.Institute of Theoretical and Experimental Biophysics,Russian Academy of Sciences,Pushchino, Moscow oblast,Russia;3.Dostoevsky Omsk State University,Omsk,Russia |
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Abstract: | The action of six synthetic Biginelli pyrimidines on the production of reactive oxygen species (ROS) by polymorphonuclear
leukocytes has been studied. It has been shown using the method of luminoldependent chemiluminescence that, at concentrations
of 10–100 μM, these compounds stimulate the production of ROS by neutrophils stimulated by phorbol-12-myristate-13-acetate
(PMA). The ROS production by PMA-stimulated neutrophils in the presence of 10 μM 1-(3,4-dimethoxyphenylethyl)-4-(alkyl/aryl)
substituted Biginelli pyrimidines increased by 50–90%. The priming action of Biginelli pyrimidines on the ROS production by
neutrophils has been shown to increase when the furyl radical was replaced by phenyl and isopropyl radicals by the C(4) pyrimidine cycle and replacement of the benzyl substitute at N(1) by 3,4-phenylethyl. At a concentration
of 0.01–0.1 μM, 1-(3,4-dimethoxyphenylethyl)-4-(alkyl/aryl) substituted Biginelli pyrimidines had a high inhibitory activity.
It has been found that 1-(2-3,4-dimethoxyphenyl]-ethyl)-4-phenyl-5-carbethoxy-6-methyl-3,4-dihydro-2(1H)-pyrimidinethion
at high concentrations (1 mM and more) is able to induce a respiratory burst of neutrophils without additional stimulation. |
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