非核糖体七肽lipovelutibols A的固相合成  

Solid-Phase Synthesis of Nonribosomal Heptapeptide Lipovelutibols A

作　　者：廖秀飞 莫金秋 刘泰容 唐铭 廖洪利[1] LIAO Xiufei;MO Jinqiu;LIU Tairong;TANG Ming;LIAO Hongli(School of Pharmacy,Chengdu Medical College,Chengdu 610500,China;Medical College of Tarim University,Alar 843300,China)

机构地区：[1]成都医学院药学院,四川成都610500 [2]塔里木大学医学院,新疆阿拉尔843300

出　　处：《化学与生物工程》2022年第1期17-20,共4页Chemistry & Bioengineering

基　　金：四川省科技厅重点研发项目(2019YFS0097)。

摘　　要：以Wang-Leu-NHFmoc树脂为载体、Fmoc-Ile-OH为起始原料、N,N-二异丙基碳二亚胺(DIC)/2-肟氰乙酸乙酯(Oxyme)为缩合体系,通过Fmoc固相合成法,合成了N端接有辛酰基的脂肪七肽,使用NaBH_(4)将C端羧基还原成醇,所得粗品经制备型RP-HPLC纯化,得纯度大于98%的非核糖体脂肪七肽lipovelutibols A,总收率40.0%。该方法操作简便,产物纯度及收率均很高,适用于同类型非核糖体多肽的化学合成。Using Wang-Leu-NHFmoc resin as a carrier,Fmoc-Ile-OH as a starting material,N,N-diisopropylcarbon diimine(DIC)/ethyl cyanoglyoxylate-2-oxime(Oxyme)as a condensation system,we synthesized lipoheptapeptide with octanoyl group at N-terminal and leucinol at C-terminal through Fmoc solid-phase synthesis method,and purified the crude product by preparative RP-HPLC.The purity of the obtained nonribosomal heptapeptide lipovelutibols A is over 98%,and the total yield is 40.0%.This method has the characteristics of easy operation,high purity,and high yield,which is suitable for the chemical synthesis of the same type of nonribosomal peptides.

关 键 词：lipovelutibols A 非核糖体多肽 抗肿瘤 固相合成 

分 类 号：R914.5[医药卫生—药物化学]