摘要
目的固相合成鳖甲抗肝纤维化活性多肽,为开发抗肝纤维化多肽药物提供结构明确的受试品。方法采用固相合成法,以Fmoc保护氨基酸和W ang树脂为原料,经1-氧-3-双二甲胺羧基苯骈三氮唑四氟化硼盐、N-甲基吗啡啉缩合,以20%哌啶的N,N-二甲基甲酰胺溶液进行脱保护,用三氟乙酸切割试剂将多肽粗品从W ang树脂上切割下来。结果经反相高效液相色谱分析纯化,可得纯度>98%的目的肽,经质谱鉴定其相对分子质量与理论值一致。结论该合成方法条件温和、副反应少,操作简便,纯化效率高,可用于大规模合成目的肽。
Objective To study the solid-phase synthesis of the active anti-hepatic fibrosis peptides of Carapax Trionycis,and provide the theoretical basis for developing the medicines against hepatic fibrosis. Methods Solid-phase synthesis was carried out with resin Wang as a carrier,Fmoc as an amino acids protector.After condensed with the mix reagents of TBTV/NMM,deprotected with 20% priperdine,the crude produts of synthetic peptide were cut down from the wang resin by the cleared reagents TFA/TLS/H2O. Results The purity of the target peptides was over 98% by RP-HPLC analysis,the molecular weight of which was identical with the theoretical value by mass-spectrum identification. Conclusion This synthesis method is mild,safety,efficient and easy to operate,which can be applied to the large scale synthesis of objective peptides.
出处
《医药导报》
CAS
2011年第5期561-562,共2页
Herald of Medicine
关键词
鳖甲
多肽
固相合成
Carapax Trionycis
Peptides
Solid-phase synthesis
