Freundt K J, Römer K G, Kamal A M
J Appl Toxicol. 1981 Aug;1(4):215-9. doi: 10.1002/jat.2550010406.
The dithiocarbamates (DTCs) disulfiram, thiram, diethyldithiocarbamate and dimethyldithiocarbamate on the equimolar base inhibited to the same extent both the lipid peroxidation (LPO) induced by ascorbic acid (non-enzymatic) and that stimulated by an NADPH-regenerating system with CCl4 admixture (enzymatic). Lipid peroxidation measurements were made in terms of malondialdehyde (MDA) formation in rat liver microsomes, or in the 9000 X g supernatant. The inhibitory action of tetramethylthiuram monosulphide was considerably weaker. Carbon disulphide (CS2) inhibited the enzymatic and non-enzymatic stimulated microsomal LPO by 4 orders less than the DTCs. In parallel with the inhibition of MDA formation, oxidative destruction of microsomal cytochrome P-450 was delayed with increasing concentrations of the DTCs. A well-correlated, non-linear, semi-logarithmic relation was found for the concentration-activity relationship for all DTCs and CS2. As the DTCs inhibited LPO both in heat-denatured and freshly prepared microsomes, it can be deduced that the DTCs intervene in a non-enzymatic oxidation phase of the LPO. The DTC inhibitory action is attributed to a radical-trap mechanism since LPO that has already been initiated was inhibited with the DTCs. However, more inhibitor is required to trap the radicals the later the DTC administration takes place.
二硫代氨基甲酸盐(DTCs)中的双硫仑、福美双、二乙基二硫代氨基甲酸盐和二甲基二硫代氨基甲酸盐在等摩尔基础上对等抑制了由抗坏血酸诱导的脂质过氧化(LPO)(非酶促)以及由含四氯化碳混合物的NADPH再生系统刺激的脂质过氧化(酶促)。脂质过氧化的测量是根据大鼠肝微粒体或9000×g上清液中丙二醛(MDA)的形成来进行的。一硫化四甲基秋兰姆的抑制作用要弱得多。二硫化碳(CS2)抑制酶促和非酶促刺激的微粒体LPO的程度比DTCs低4个数量级。随着DTCs浓度的增加,与MDA形成的抑制同时发生的是微粒体细胞色素P - 450的氧化破坏延迟。发现所有DTCs和CS2的浓度 - 活性关系呈良好相关的非线性半对数关系。由于DTCs在热变性微粒体和新鲜制备的微粒体中均抑制LPO,因此可以推断DTCs干预了LPO的非酶促氧化阶段。DTC的抑制作用归因于自由基捕获机制,因为已经启动的LPO被DTCs抑制。然而,DTC给药越晚,捕获自由基所需的抑制剂就越多。