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环孢菌素A免疫抗原的制备

吴琼英, 戴晓雁, 黄文才, 刘一超, 范昕建, 陈米娜, 冯萍   

  1. 1.四川大学化工学院, 成都, 610065;
    2.四川大学药学院, 成都, 610041;
    3.四川大学附属第一医院传染病教研室,成都, 610041
  • 收稿日期:2002-01-02 修回日期:2002-05-18 出版日期:2002-09-15 发布日期:2002-09-15

Preparation of Cyclosporine A Immunogen

Wu Qiongying, Dai Xiaoyan, Huang Wencai, Liu Yichao, Fan Xinjian, Chen Mina, Feng Ping   

  1. 1.School of Chemical Engineering, Sichuan University, Chengdu 610065;
    2.West China School of Pharmacy, Sichuan University, Chengdu 610041;
    3.Department of Infection, West China Hospital, Sichuan University, Chengdu 610041
  • Received:2002-01-02 Revised:2002-05-18 Online:2002-09-15 Published:2002-09-15

摘要: 环孢菌素A(CsA)与光敏交联剂4-苯甲酰苯甲酸(BBa)溶于丙酮, 在紫外光照下, 通过光化学反应在CsA残基侧链上引入活泼的羧基. 纯化后的CsA-BBa共轭物在水溶性碳二亚胺偶联剂的作用下与聚-L-赖氨酸载体发生偶联, 获得免疫抗原. 该方法更完整的保留了CsA的特征结构. 选用具有更大氨基密度和较低免疫原性的聚-L-赖氨酸作载体, 所得偶联效率更高, 平均分子量为40000PL载体上偶联13.1-17.4CsA分子.

关键词: 环孢菌素A, 免疫抗原, 4苯甲酰苯甲酸, 聚L赖氨酸

Abstract: Cyclosporin A reacted with 4-benzoylbenzoic acid under ultraviolet radiation to give the conjugate of CsABBa. Then, the conjugate was linked to poly-L-lysine with the action of l-ethyl-3-(3-dimethylamino propyl)-carbodiimide hydrochloride to generate CsA immunogen. There were 13.1-17.4 molecules of CsA on each molecule of PL whose average molecular weight was 40 000. The coupling efficiency was fairly high and the constitution of CsA was maintained well.

Key words: Cyclosporin A, Cyclosporin A, Immunogen, Immunogen, 4-Benzoylbenzoic acid, 4-Benzoylbenzoic acid, Polylysine, Polylysine

Supporting: *This project was supported by the fund of Sichuan Key Science and Technology (97012152501).