目的:采取化学修饰的方法以提高布鲁氏菌侵染抑制肽稳定性。方法:先通过多肽固相合成法(solid-phase peptide synthesis, SPPS)对布鲁氏菌侵染抑制肽OP11进行合成,然后氧化OP11得到环OP11后直接使用“一锅法”对环OP11分别进行2分支和4分支树状修饰,并通过HPLC以及核磁实验进行结果验证。结果:成功合成2分支和4分支树状环OP11肽。结论:“一锅法”可以有效解决水溶性差、侧链含有二硫键的难溶肽通过Click反应合成树状肽的问题。
Objective: To improve the stability of Brucella infection inhibitory peptides by chemical modification. Methods: Firstly, the brucella infection inhibitory peptide OP11 was synthesized by solid-phase peptide synthesis ( SPPS ), and then OP11 was oxidized to obtain cyclic OP11. After that, the cyclic OP11 was directly modified by ‘one-pot method’ with two branches and four branches, respectively, and the results were verified by HPLC and NMR experiments. Results: Two-branched and four-branched cyclic OP11 peptides were successfully synthesized. Conclusion: The “one-pot method” can effectively solve the problem of synthesis of dendritic peptides by Click reaction of insoluble peptides containing disulfide bonds with poor water solubility.
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