固相合成法制备环肽Hymenistatin-1及其含statine的类似物  

Preparation of cyclopeptide Hymenistatin-1 and its four statine analogues by solid-phase peptide synthesis method

作　　者：李从岩[1] 徐琪[2] 颜炜群[1] 

机构地区：[1]吉林大学再生医学科学研究所,长春130021 [2]杭州中肽生化有限公司,杭州310018

出　　处：《中国抗生素杂志》2008年第11期678-681,共4页Chinese Journal of Antibiotics

摘　　要：目的研究固相合成法制备Hymenistatin-1[HS-1,序列为cyclo-(-Pro-Pro-Tyr-Val-Pro-Leu-Ile-Ile-)]及其statine类似物的工艺步骤和影响因素。方法采用Fmoc或Boc保护α-氨基,以HBTU/NMM为缩合剂进行直链肽接肽反应、以BOP/HOBt/DIEA为缩合剂进行环化固相合成HS-1及其类似物。用色谱仪和质谱仪对合成的环肽及其杂聚肽类似物进行纯化鉴定。结果多肽合成收率可达65%,经反相高效液相色谱(RP-HPLC)柱对合成的多肽进行纯化后纯度均达到90%以上,通过基质辅助激光解吸附电离飞行质谱仪(MALDI-MS)检测所合成的环肽及环肽类似物的分子质量与理论分子质量相符。结论成功合成出了较高纯度的目标多肽化合物。Objective Preparation of Hymenistatin-I [-HS-1, cyclo-（-Pro-Pro-Tyr-Val-Pro-Leu-Ile- Ile-）] and its four statine-analogues by solid-phase peptide synthesis method, and the synthesis process and influencing factors were investigated. Methods Using the Fmoc-or Boc- protected a-amino acids, HBTU/ NMM as coupling reagent （linear peptide synthesis） and BOP/HOBt/DIEA as eyclizing reagent, the cyclooetapeptide HS-1 and its analogues were synthesized. The target peptides were purified by RP-HPLC and identified by MALDI-MS. Results The purity of the five peptides exceeded 90% and the yields up to 65%. The molecular weights of the synthesized peptides were identified by mass spectrogram. Conclusion The target peptide compounds with higher purity were synthesized.

关 键 词：固相多肽合成 HS-1 Statine类似物 纯化 

分 类 号：R978.16[医药卫生—药品]