Dráberová L, Dráber P, Benes L
Folia Biol (Praha). 1980;26(5):327-37.
We have examined the effect of six carbanilic acid derivatives (differing in the substitution of the aromatic ring, in the coupling chain or the basic moiety of the molecule) and trimecaine, i.e. agents with local anaesthetic action, on concanavalin A-induced blastic transformation of lymphocytes. We have found that these compounds differ in the ability to block blastic transformation and agglutination of lymphocytes when added to cell cultures at different concentrations simultaneously with Con A. At the minimal inhibitory concentrations, the derivatives exhibit a different degree of toxicity which, however, provides no explanation for the inhibitory effect of most of the compounds. The known effect of these compounds on the membranes together with observed inhibition of agglutination (a relatively early sign of activation), and their lower inhibitory activity, when added several hours after Con A, support the idea that they affect the early cell membrane-mediated processes during blastic transformation. In agreement with this finding is also the observed correlation between local anaesthetic activity and the ability of individual carbanilic acid derivatives to block the blastic transformation.
我们研究了六种邻氨基苯甲酸衍生物(它们在芳环取代、连接链或分子的碱性部分存在差异)以及三甲卡因(即具有局部麻醉作用的药剂)对伴刀豆球蛋白A诱导的淋巴细胞母细胞转化的影响。我们发现,当这些化合物与伴刀豆球蛋白A同时以不同浓度添加到细胞培养物中时,它们在阻断淋巴细胞母细胞转化和凝集的能力方面存在差异。在最小抑制浓度下,这些衍生物表现出不同程度的毒性,然而,这并不能解释大多数化合物的抑制作用。这些化合物对细胞膜的已知作用,以及观察到的凝集抑制(激活的一个相对早期迹象),还有它们在伴刀豆球蛋白A添加数小时后较低的抑制活性,都支持这样一种观点,即它们在母细胞转化过程中影响早期细胞膜介导的过程。局部麻醉活性与个别邻氨基苯甲酸衍生物阻断母细胞转化能力之间观察到的相关性也与这一发现相符。