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.
出处
《药学学报》
CAS
CSCD
北大核心
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)
