蜂毒肽片段的合成及活性研究

Study on Synthesis and Activity of Peptide Fragment of Anti-rheumatic Arthritis

为了保留蜂毒肽抗类风湿关节炎活性,降低溶血性和致敏性,设计合成蜂毒肽的片段,观察它对兔免疫性关节炎的治疗作用。采用多肽合成法合成蜂毒肽结构中亲水性片段,经高效液相色谱及质谱分析,确定合成多肽片段的氨基酸组成。建立家兔卵蛋白性关节炎模型,进行溶血性试验、致敏性试验以及动物模型治疗实验。结果:蜂毒肽片段溶血率<5%,致敏率<8%,动物模型治疗有效率可达到70%。实验证明蜂毒肽片段的合成可有效地保留蜂毒肽抗类风湿关节炎活性,减低蜂毒肽的强溶血活性及致敏活性。

In order to keep the anti-rheumatic arthritis activity and reduce the hemolysis hypersuscepti-bility of melittin, a deletion peptide of melittin was synthesized. Its anti-inflammation effect was observed. A hydrophile peptide fragment of melittin was synthesized by standard solid-phase method. The product was analyzed by HPLC and MS. Its hemolysis and hypersusceptibility were tested. The rabbits＇ model of immune arthritis was established and cured. The hemolysis rate of Peptide is less than 5%. The hypersusceptibility of its rate is less than 8%. The hydrophile peptide fragment of melittin may keep anti-rheumatic arthritis activity and reduce its hemolysis and hypersusceptibility.