甾体-多肽缀合激素的合成及免疫抑制活性

THE SYNTHESIS AND IMMUNOSUPPRESSIVE EFFECTS OF STEROIDPEPTIDE LINKERS

尿毒素三肽ＵＴＰＡ，ＵＴＰＢ和ＵＴＰＣ分别与氢化可的松缀合，得到４种缀合激素。与尿毒素三肽或氢化可的松相比，缀合激素可延长不同种属小鼠异位移植（Ｈｅｔｅｒｏｔｏｐｉｃｔｒａｎｓｐｌａｔａｔｉｏｎ）心肌的存活时间；与氢化可的松和尿毒素三肽的机械混合物相比，低浓度下缀合激素可增强对淋巴细胞增殖的抑制作用。表明缀合激素有一定的免疫抑制作用。

Hydrocortisone was coupled with urotoxin tripeptide UTPA, UTPB and UTPC respectively yielding 4 linkers. Their bioactivities such as prolongation of heterotopic transplanted cardiac tissue survival, inhibitory effects on phagocytosis of mouse peritoneal macrophages and the influence on Con A induced proliferation of spleen lymphocytes of mouse were observed. Compared with UTPA, UTPB, UTPC or hydrocortisone the linkers were more potent immunosuppressants. The results suggest that the linker of steroidpeptide may simulate the permissive action.