软刀素肽的固相合成
Solid-phase synthesis of urumin
作者:莫金秋;刘泰容;苏春丽;廖洪利;胡宏岗;
Author:
收稿日期: 年卷(期)页码:2018,33(04):-356-358
期刊名称:华西药学杂志
Journal Name:WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字:软刀素肽;H1型病毒;固相合成;高效液相色谱法;高分辨质谱;多肽;王树脂;1-羟基苯并三唑/N,N-二异丙基碳二亚胺
Key words:
基金项目:四川省教育厅科研基金重点项目(18ZA0149)
中文摘要
目的制备抗H1型病毒的软刀素肽。方法采用9-芴甲氧羰基(Fmoc)固相合成法,选用Wang树脂为载体,以HOBt/DIC为缩合试剂依次偶联氨基酸后,将多肽从树脂上切割下来,得到的粗品采用制备HPLC进行纯化。结果制得纯度>98.2%的多肽产物,用HPLC归一化法测定的含量为26.3%,所得产物通过HRMS分析,确定为软刀素肽。结论所用方法可行性高、操作简便,收率较高,目标化合物可用于抗H1型病毒的后续药物研究。
参考文献
[1]Garten RJ,Dais CT,Russell CA,et al.Antigenic and genetic characteristics of swine-origin 2009(H1N1)influenza viruses circulating in humans[J].Science,2009,325:197-201.
[2]Vineeth KTP,Asha R,Shyla G,et al.Identification and characterization of novel host defense peptides from the skin secretion of the fungoid frog,Hydrophylax bahuvistara[J].Chem Bio Drug Des,2017.doi:10.1111/cbdd.12937.[Epub ahead of print].
[3]Tripathi S,Tecle T,Verma A,et al.APD2:The updated antimicrobial peptide database and its application in peptide design[J].J General Virology,2013,94:40-49.
[4]David J,Holthausen,Song HL,et al.An amphibian host defense peptide is virucidal for human H1 hemagglutinin-bearing influenza viruses[J].Immunity,2017,46(4):587-595.
[5]Fiore AE,Fry A,Shay D,et al.Antiviral agents forthe treatment and chemoprophylaxis of influenza-recommendations of the advisory committee on immunization practices(ACIP)[J].MMWR Recomm Rep,2011,60(1):1-24.
[6]Hurt AC,Ho HT,Barr I.Resistance to anti-influenza drugs:Adamantanes and neuraminidase inhibitors[J].Expert Rev Anti Infect Ther,2006,4:795-805.
【关闭】