紫花地丁中抗甲型H1N1流感病毒的环肽  

A cyclotide against influenza A H1N1 virus from Viola yedoensis

作　　者：刘忞之 杨燕 张书香 唐亮 王惠敏 陈成娟 申竹芳 程克棣 孔建强 王伟[1] 

机构地区：[1]中国医学科学院、北京协和医学院药物研究所、天然药物活性物质与功能国家重点实验室,北京100050

出　　处：《药学学报》2014年第6期905-912,共8页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(30772677,81072562);国家“重大新药创制”科技重大专项资助项目(2012ZX09301002);中央高校基本科研业务费(2012N06)

摘　　要：本研究从紫花地丁全草中分离得到3个环肽。其中,varv peptide E和cycloviolacin Y5已报道,另一种新的环肽命名为cycloviolacin VY1。环肽经DTT还原、碘乙酰胺(IAA)烷基化,再分别利用赖氨酸内肽酶、胰蛋白酶和糜蛋白酶酶解,通过MS/MS质谱解析酶解肽段的碎片离子鉴定出其结构。稳定性分析再次证实其具有一般环肽的特性,能较好地耐受胰蛋白酶和糜蛋白酶酶解及耐热变性。体外活性评价结果表明其对甲型H1N1流感病毒具有较强的抑制作用,其半数抑制浓度(IC50)为(2.27±0.20)μg·mL-1。它是报道的第一个具有抑制甲型H1N1流感病毒的活性环肽。Three cyclotides were isolated from the whole plant of 1,7ola yedoensis in this study. The two, vary peptide E and cycloviolacin YS, were previously reported, and a novel cycloviolacin VY1 was characterized according to the interpretation of MS/MS fragmentation of peptides which were produced from the reduced and alkylated parent peptide with the digestion of Endo Lys-C, trypsin and chymotrypsin, separately. The stability of remarkable resistance to proteolytic degradation by trypsin and chymotrypsin, and that of thermal denaturation was confirmed again. Besides, the ICso value of cycloviolacin VY1 against influenza A H1N1 virus was （2.27 ± 0.20）μg·mL-1. It is the first cvclotide renorted with anti-influenza A H1N1 virus activity in vitro assay.

关 键 词：紫花地丁 环肽 热稳定性 酶解稳定性 抗甲型H1N1流感病毒活性 

分 类 号：R284[医药卫生—中药学]