Shatalin Iu V, Shubina V S, Fisiuk A S
Tsitologiia. 2010;52(3):242-7.
The effect of 6 synthetic Biginelli pyrimidines on production of reactive oxygen species by polymorphonuclear neutrophils was investigated. It has been shown by method of luminol-dependent chemiluminescence that test compounds in a concentrations of 10-100 microM stimulate production of reactive oxygen species. An increase in the reactive oxygen species production by stimulated neutrophils in the presence of 10 microM 1-(3, 4-dimetoxyphenyl)ethyl-4(alkyl/aryl) substituted Biginelli pyrimidines was 50-90 %. An increase in the priming effect of Biginelli pyrimidines on reactive oxygen species production by neutrophils was noted in the case of replacement of phuryl radical by phenyl and alkyl radicals at C(4) pyrimidine cycle and in the case of replacement benzyl radical at N(1) by 3, 4-dimetoxyphenyl radical. It has been revealed a high inhibitory effect of 1-(3, 4-dimetoxyphenylethyl)-4(alkyl/aryl) substituted Biginelli pyrimidine in concentration 0.01-0.10 microM. It has been found that high concentration of ethyl-1-[2-(3, 4-dimethoxyphenyl)ethyl]-6- methyl-4-phenyl-2-thioxo-1, 2, 3, 4-tetrahydropyrimidine -5-carboxylate (1 mM and more) is able to cause respiratory burst of neutrophils without additional stimulation.
研究了6种合成的Biginelli嘧啶对多形核中性粒细胞产生活性氧的影响。通过鲁米诺依赖的化学发光法表明,浓度为10 - 100微摩尔的受试化合物刺激活性氧的产生。在存在10微摩尔1-(3,4 - 二甲氧基苯基)乙基 - 4(烷基/芳基)取代的Biginelli嘧啶的情况下,受刺激的中性粒细胞产生的活性氧增加了50 - 90%。在嘧啶环的C(4)位用苯基和烷基取代呋喃基以及在N(1)位用3,4 - 二甲氧基苯基取代苄基的情况下,观察到Biginelli嘧啶对中性粒细胞产生活性氧的引发作用增强。已揭示浓度为0.01 - 0.10微摩尔的1-(3,4 - 二甲氧基苯乙基)-4(烷基/芳基)取代的Biginelli嘧啶具有高抑制作用。已发现高浓度的乙基 - 1 - [2-(3,4 - 二甲氧基苯基)乙基]-6 - 甲基 - 4 - 苯基 - 2 - 硫代 - 1,2,3,4 - 四氢嘧啶 - 5 - 羧酸盐(1毫摩尔及以上)能够在无额外刺激的情况下引起中性粒细胞的呼吸爆发。