Flasch H, Heinz N, Petersen R
Arzneimittelforschung. 1977;27(3):649-53.
The affinities of some polar and non-polar digoxin and digitoxin metabolites to the related antibodies are largely dependent on the structure of their genin parts. Metabolites with unchanged genins show high cross reactivities towards their related antibodies when compared to the original immunogenic cardenolides. Towards the digoxin antibody the following cross reactivities were found: digoxin-16'-glucuronide 50%, digoxigenin 89.5%, and digoxigenin-3-glucuronide 85%. Values of the same order of magnitude were found with the corresponding digitoxin metabolites and the digitoxin antibody. In contrast, there is a marked decrease in cross reactivity caused by only minor changes in the genin part. With the digitoxin antibody the following cross reactivities are found: digoxin (i.e. 12-OH-digitoxin) 9.1%, 3-epi-digitoxigenin 5.6% and 3-epi-digitoxigenin-3-sulphate 1%. Bcause 12-hydroxylation has been reported to be one of several possible ways of digitoxin metabolisation in man, from a theoretical point of view erroneous results in the clinical digitoxin estimation by radioimmuno-assay are possible. In the case of all of the other metabolites the alterations in positive inotropic activity and cross reactivity run largely parallel.
一些极性和非极性地高辛及洋地黄毒苷代谢产物与相关抗体的亲和力在很大程度上取决于其苷元部分的结构。与原始免疫原性强心苷相比，苷元未改变的代谢产物对其相关抗体表现出高交叉反应性。对于地高辛抗体，发现了以下交叉反应性：地高辛 -16'-葡萄糖醛酸苷50%，地高辛配基89.5%，以及地高辛配基 -3-葡萄糖醛酸苷85%。在相应的洋地黄毒苷代谢产物和洋地黄毒苷抗体中也发现了相同数量级的值。相比之下，苷元部分仅发生微小变化就会导致交叉反应性显著降低。对于洋地黄毒苷抗体，发现了以下交叉反应性：地高辛（即12 - 羟基洋地黄毒苷）9.1%，3 - 表洋地黄毒苷配基5.6%，以及3 - 表洋地黄毒苷配基 -3-硫酸盐1%。由于据报道12 - 羟基化是人体中洋地黄毒苷几种可能的代谢方式之一，从理论角度来看，通过放射免疫测定法在临床洋地黄毒苷估计中可能会出现错误结果。在所有其他代谢产物的情况下，正性肌力活性的改变和交叉反应性在很大程度上是平行的。
