Wagner G, Bunk E
Pharmazie. 1979 Oct;34(10):640-5.
In view of their potential activity as antigen-specific immunosuppressive agents, the authors produced conjugates by treating the tri- and tetracyclic compounds 1-8 (with isothiocyanate structure) with human serum albumin (HSA) and bovine gamma globulin (BGG). In certain cases the conjugates of BGG were obtained only under conditions leading to protein degeneration. The corresponding products were devoid of antigen-specific immunosuppressive activity and must be considered to be merely repository forms of the respective low-molecular compounds. In contrast, the conjugates of HSA could be obtained under conditions under which no protein denaturation was detectable. These conjugates may be used for the planned investigation. After reaction of the isothiocyanates with the proteins, time dependent changes were observed in the ultraviolet spectra of some conjugates, the possible causes of which are discussed.
鉴于它们作为抗原特异性免疫抑制剂的潜在活性,作者通过用人血清白蛋白(HSA)和牛γ球蛋白(BGG)处理具有异硫氰酸酯结构的三环和四环化合物1-8来制备缀合物。在某些情况下,仅在导致蛋白质变性的条件下才能获得BGG的缀合物。相应的产物缺乏抗原特异性免疫抑制活性,必须仅被视为各自低分子化合物的储存形式。相比之下,HSA的缀合物可以在未检测到蛋白质变性的条件下获得。这些缀合物可用于计划的研究。异硫氰酸酯与蛋白质反应后,观察到一些缀合物的紫外光谱随时间的变化,并讨论了其可能的原因。