摘要
目的合成能够诱导T淋巴细胞白血病Jurkat细胞凋亡的花椒属环八肽Zanriorb A1。方法通过9-芴甲氧羰基(Fmoc)固相合成法,以2-氯三苯基氯树脂(CTC)为载体,Fmoc-Gly-OH为起始原料,N,N-二异丙基乙胺(DIEA)/6-氯苯并三氮唑-1,1,3,3-四甲基脲六氟磷酸酯(HCTU)为缩合体系,在液相经1-羟基苯并三氮唑(HOBt)/苯并三唑-1-基氧三吡咯烷基六氟磷酸(PyBOP)/DIEA实现环合,所得化合物通过RP-HPLC、MS等光谱表征。结果通过本法顺利得到纯度>98%的花椒属环八肽Zanriorb A1,总收率为48%。结论该合成方法具有可行性,操作简单,总收率高,目标化合物可用于抗Jurkat细胞的药物研究。
Objective To synthesize the Zanriorb A1 of zanthoxylum cyclic octapeptide which can induce the apoptosis of Jurkat cells. Methods The Fmoc solid-phase polypeptide synthesis （SPPS ） was used with 2-chlorotrityl chloride resin as a solid support,Fmoc-Gly-OH as the starting material,and DIEA/HCTU as a condensation system.The cyclization was achieved in the liquid phase by HOBt/PyBOP/DIEA,and the target peptide was confirmed by RP-HPLC and MS.Results The Zanriorb A1 of zanthoxylum cyclic octapeptide was synthesized with the final purity of over 98% and the overall yield of 48%.Conclusion The synthetic method was feasible,simple and practical with high yield,and the desired target peptide could be used for drug screening of anti-Jurkat cells.
出处
《成都医学院学报》
CAS
2017年第1期40-43,48,共5页
Journal of Chengdu Medical College
基金
四川省高校科研创新团队项目资助(No:13TD0028)
