摘要
Ａｒｇ－Ａｒｇ二肽的胍基可以为ＮＯ合成酶利用，产生ＮＯ样舒血管效应．Ａｒｇ－Ａｒｇ的羧端用－ＣＨ＿３封闭，活性降低．Ａｒｇ－Ａｒｇ的两个α－氨基用丙二酰基或丁二酰基封闭，活性进一步降低，为了观察Ａｒｇ－Ａｒｇ的氨端用氨基酸封闭可能造成的影响，本文合成了Ｌｅｕ－Ａｒｇ－Ａｒｇ和Ｓｅｒ－Ｌｅｕ－Ａｒｇ－Ａｒｇ两种寡肽，测定了它们的抗血小板聚集作用和血管舒张作用．结果表明，Ａｒｇ－Ａｒｇ的氨端用氨基酸或寡肽封闭，对舒血管作用无反面影响。合成的两种寡肽还可以有效地抑制ＡＤＰ诱导的血小板聚集．实验表明，设计抗血栓寡肽时，羧端引入Ａｒｇ－Ａｒｇ二肽可能会有益处．
The guanidines of Arg-Arg dipeptide would be tised by NO synthetase to exhibit vasorelaxing effect.The C-terminal was blockaded with a methyl group and its bioactivity was decreased.The N-terminal was blockaded with dimalonyl or succinyl and its bioactivity was further decreased.To observe the possible effects of blockade of the N-terminal of Arg-Arg with amino acid or oligopeptide, Leu-Arg-Arg and Ser-Leu-Arg-Arg were prepared by the solution method,their vasorelaxing effect and inhibiting effect on ADP-induced platelet aggregation were observed.The results indicated there was no difference between them and Arg-Arg dipeptide for vasorelaxing potency and their antiplatelet aggregating effect was also significant.
出处
《中国药物化学杂志》
CAS
CSCD
1995年第2期91-95,共5页
Chinese Journal of Medicinal Chemistry
基金
国家自然科学基金
关键词
肽
含Arg-Arg寡肽
合成
药理学
Arg-Arg contained oligopeptide,Antiplatelet aggregation,Vasorelaxation
