【摘要】 目的:分析聚乙二醇修饰对天花粉蛋白抗生育活性和引起过敏反应的影响。方法:妊娠11-12d小鼠静脉给药,48h后解剖,计算引产率;豚鼠药物致敏5次,末次致敏14d、21d攻击,观察0．5h内过敏反应情况;大鼠皮内接种抗血清,24h后抗原加染料攻击,观察染料渗出情况。结果:与天花粉蛋白相比,聚乙二醇化天花粉蛋白在较低浓度(0．5mg/kg)就可达到引产目的(引产率>85％),且引起豚鼠和大鼠过敏反应的程度较低。结论:聚乙二醇化修饰能提高天花粉蛋白的体内活性,降低其免疫原性,在临床中有广阔的应用前景。更多还原

【Abstract】 Objective: To analyse the abortifacient activity and anaphylaxis induced by PEGylated Trichosanthin. Methods: Mid-gestation mice were administrated by intravenous injection sacrificed 48 h later and then induced labor rate was caculated; guinea pigs were sensitized 5 times with antigens 14 d and 21 d after the last sensitizing injection, respectively, the guinea pigs were challenged by an intravenous injection into the hind limb peripheral vein with the same antigen to evoke systemic anaphylaxis, signs were observed for 30 min immediately after injection; rats were intradermal injected antiserum in back, antigens were intravenous injected through tail vein with Evens blue, then the seepage of the dye was observed. Results: After PEGylation, in vivo abortifacient activity increased in the same dosage, but the degree of passive cutaneous anaphylaxis in rats and systemic anaphylaxis reaction in guinea pigs induced greatly reduced. Conclusion: As a new drug, PEGylated Trichosanthin with a higher in vivo activity can become a better therapeutic agent in future.更多还原