Liubin G S, Konoplia N A, Guliakevich O V, Kuz'mitskiĭ B B
Department of Biological Tests, Academy of Sciences of Belarus, Minsk, Belarus.
Eksp Klin Farmakol. 2000 Jul-Aug;63(4):45-7.
The immunopharmacological properties of two new compounds with an 8-azasteroidal structure, representing the salts (hydrochloride and acetate) of 12-imino-substituted 8-aza-D-homogonan, were studied in comparison with the properties of the immunostimulant trimeson. Similar to trimeson, both new compounds produce a dose-dependent activation of the humoral chain of immunogenesis in the model of primary immune response to goat erythrocytes in CBA, C57BL/6, and C57W mice. The immunostimulant activity of the 8-aza-D-homogonan derivatives is inversely proportional to the antigen load (2 x 10(7)-2 x 10(9) goat erythrocytes per mice) and depends to a considerable extent of the genotype of experimental animals. A modification of the 8-aza-D-homogonan structure by substituting imino group for oxygen at position 12 of the 8-azasteroidal skeleton leads to a sharp increase in toxicity as compared to that of trimeson.
研究了两种具有8-氮杂甾体结构的新化合物（12-亚氨基取代的8-氮杂-D-高诺酮的盐类，即盐酸盐和醋酸盐）的免疫药理学特性，并与免疫刺激剂曲美松的特性进行了比较。与曲美松相似，在CBA、C57BL/6和C57W小鼠对山羊红细胞的初次免疫应答模型中，这两种新化合物均能产生剂量依赖性的免疫发生体液链激活。8-氮杂-D-高诺酮衍生物的免疫刺激活性与抗原负荷（每只小鼠2×10⁷-2×10⁹个山羊红细胞）成反比，且在很大程度上取决于实验动物的基因型。与曲美松相比，在8-氮杂甾体骨架的12位用氧取代亚氨基对8-氮杂-D-高诺酮结构进行修饰会导致毒性急剧增加。
