Fulton R J, Uhr J W, Vitetta E S
J Immunol. 1986 Apr 15;136(8):3103-9.
The cytotoxicity of A chain immunotoxins containing IgG or Fab fragments specific for the surface immunoglobulin of the Daudi cell line was assessed in the presence of B chain immunotoxins (IgG or Fab) or lysosomotropic amines, or both. The concentration required for 50% inhibition of protein synthesis (IC50) in Daudi cells was 1.3 X 10(-8) M for IgG-A and 5 X 10(-8) M for Fab-A. The toxicity of both A chain immunotoxins was enhanced twofold by ammonium chloride. In the presence of A chain immunotoxins and ammonium chloride, a maximum of 99 and 90% reduction of clonal precursors was obtained with IgG and Fab-A chain immunotoxins respectively. Immunotoxins containing ricin B chain and IgG or Fab fragments specific for the antibody portion of A chain immunotoxins were used as secondary "piggyback" immunotoxins to treat cells that were pretreated with A chain immunotoxins. Both B chain immunotoxins were nontoxic at 1 X 10(-6) M. When added to target cells pretreated with specific A chain immunotoxins, the IC50 of the A chain immunotoxins was decreased up to 16-fold in the absence of ammonium chloride. In contrast to the results obtained with A chain immunotoxins alone, ammonium chloride significantly increased the toxicity of the complete piggyback system, resulting in the killing of 99.999% or five logs of target cells in the clonal assay. This decreased the IC50 of A chain immunotoxins up to 116-fold when compared with A chain immunotoxin alone. This enhanced toxicity was independent of the valency of either immunotoxin.
在存在B链免疫毒素(IgG或Fab)或溶酶体促渗胺或两者的情况下,评估了含有针对Daudi细胞系表面免疫球蛋白的IgG或Fab片段的A链免疫毒素的细胞毒性。对于IgG-A,Daudi细胞中50%抑制蛋白质合成所需的浓度(IC50)为1.3×10⁻⁸M,对于Fab-A为5×10⁻⁸M。氯化铵使两种A链免疫毒素的毒性增强了两倍。在存在A链免疫毒素和氯化铵的情况下,IgG和Fab-A链免疫毒素分别使克隆前体细胞最多减少99%和90%。含有蓖麻毒素B链和针对A链免疫毒素抗体部分的IgG或Fab片段的免疫毒素被用作二级“搭载”免疫毒素,以处理预先用A链免疫毒素处理过的细胞。两种B链免疫毒素在1×10⁻⁶M时均无毒。当添加到用特异性A链免疫毒素预处理的靶细胞中时,在不存在氯化铵的情况下,A链免疫毒素的IC50降低了多达16倍。与单独使用A链免疫毒素获得的结果相反,氯化铵显著增加了完整搭载系统的毒性,在克隆试验中导致99.999%或五个对数的靶细胞死亡。与单独的A链免疫毒素相比,这使A链免疫毒素的IC50降低了多达116倍。这种增强的毒性与任何一种免疫毒素的价态无关。