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[12-亚氨基取代的8-氮杂-D-高戈那和曲美宗的免疫药理特性]

[Immunopharmacologic properties of 12-iminosubstituted 8-aza-D-homogonan and trimezon].

作者信息

Liubin G S, Konoplia N A, Guliakevich O V, Kuz'mitskiĭ B B

机构信息

Department of Biological Tests, Academy of Sciences of Belarus, Minsk, Belarus.

出版信息

Eksp Klin Farmakol. 2000 Jul-Aug;63(4):45-7.

Abstract

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.

摘要

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。

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