Pallardy M, Alberici G F, Dessaux J J, Bohuon C
Int J Immunopharmacol. 1987;9(2):151-6. doi: 10.1016/0192-0561(87)90089-0.
In order to elucidate the immune-mediated hemolytic disease induced in man by elliptinium acetate, a quaternary ammonium compound with antineoplastic activity, polyclonal antibodies directed against this hapten were raised in rabbits. The coupling step between drug and carrier was performed according to a putative human in vivo hapten conjugation mechanism. Structure-activity relationships of the resulting IgG were compared with the epitope site recognized by human anti-elliptinium IgM by using a panel of twelve elliptinium acetate analogues. Although both antibodies were directed principally against the quaternary ammonium ion, a poor correlation between the cross-reactivity indices was obtained. In fact, it appeared that both antibodies recognized specifically the ammonium group plus different regions of the molecule: the indole ring for human antibodies, the N-alkyl group and its vicinity for rabbit ones. The specificity of the obtained rabbit polyclonal antisera is discussed, with regard to the conjugation mechanism of the drug occurring in man.
为了阐明由具有抗肿瘤活性的季铵化合物醋酸椭圆玫瑰树碱在人体内诱发的免疫介导溶血性疾病，针对这种半抗原的多克隆抗体在兔体内产生。药物与载体之间的偶联步骤是根据假定的人体内半抗原结合机制进行的。通过使用一组十二种醋酸椭圆玫瑰树碱类似物，将所得IgG的构效关系与人抗醋酸椭圆玫瑰树碱IgM识别的表位位点进行比较。尽管两种抗体主要针对季铵离子，但交叉反应指数之间的相关性较差。事实上，似乎两种抗体都特异性识别铵基团加上分子的不同区域：人抗体识别吲哚环，兔抗体识别N-烷基及其附近区域。就人体内发生的药物结合机制而言，对所获得的兔多克隆抗血清的特异性进行了讨论。
