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来自人乳转铁蛋白的四肽(赖—精—门冬—丝氨酸,K RDS)能抑制ADP诱导的犬血小板聚集反应(IC_(50):350μmol/L)和花生四烯酸诱导的血栓烷B_2的产生(IC_(50):175μmol/L),同时,KRDS能抑制凝血酶诱导的血小板表面α—颗粒膜蛋白(GMP-140)的表达(IC_(50):350μmol/L及5—羟色胺的释放(IC_(50):525μmol/L)。另外,KRDS能抑制犬股动脉实验血栓的形成,制备血栓模型4h后,离体血栓的重量为对照组的50%,以~(125)Ⅰ—SZ-51(抗GMP-140的单抗)为示踪剂,离体血栓与血液的放射活性比值仅为对照组的16%。结果提示:四肽KRDS不仅能抑制犬血小板的聚集和释放功能,对体内血栓的形成也有明显的抑制作用,为一生理性抗血栓寡肽。
Tetrapeptide derived from human milk transferrin (R-MS-KRDS) inhibited ADP-induced platelet aggregation (IC50: 350 μmol / L) and arachidonic acid-induced thromboxane (IC50: 175μmol / L). Meanwhile, KRDS inhibited the expression of GMP-140 induced by thrombin (IC50: 350μmol / L) and serotonin (IC 50: 525μmol / L) .In addition, KRDS could inhibit the formation of experimental thrombus in canine femoral artery. After 4h of thrombosis model, the weight of isolated thrombus was 50% -SZ-51 (anti-GMP-140 monoclonal antibody) was used as tracer, and the ratio of isolated thrombus to blood radioactivity was only 16% of the control group.The results suggest that tetrapeptide KRDS can not only inhibit platelet aggregation and release Function, the formation of thrombus in vivo also had a significant inhibitory effect, a physiological antithrombotic oligopeptide.