摘要
目的研究精氨酸-甘氨酸-天门冬氨酸(RGD)肽衍生物——ω-氨基辛酸-甘氨酸-天门冬氨酸-色氨酸(AoG-DW)抗血小板聚集的活性及特异性。方法采用比浊法测定AoGDW肽抑制人血小板聚集的活性,体外细胞脱黏附试验及MTT法检测AoGDW对人脐带静脉内皮细胞(HUVEC)的脱黏附作用。结果AoGDW和RGDS抑制人血小板聚集的IC50分别为(4.71±2.51)μmol/L和(61.82±8.08)μmol/L,AoGDW使HUVEC产生脱黏附的IC50为(16.50±0.68)mmol/L。结论AoGDW具有高活性的抗血小板聚集作用,并保留了其特异性,有可能避免或减少毒副作用的发生。对于抗血小板药物的临床应用将具有重要的现实意义。
bjective To explore the activity and specificity of ω-aminooctanoic acid-glycine-aspartic acid-tryptophan（ AoGDW） in inhibiting platelet aggregation. Methods Determine the activity of AoGDW in inhibiting human platelet aggregation by turbidimetry. Test for the detachment of AoGDW to human umbilical venous endothehal cell（HUVEC） by cell detachment test in vitro and MTT method. Results The IC50 of AoGDW and RGDS（ arginine-glycine-aspartic acid-tryptophan-serine） in inhibiting the aggregation of human platelet were （4. 71 ±2. 51 ） μmol/L and （ 61.82 ±8.08 ） μmol/L respectively. The IC50 of AoGDW causing detachment to HUVEC was （ 16. 50 ± 0. 68 ） mmol/L. Conclusion Rational design may enhance inhibitory potency of AoGDW peptide while retaining its specificity toward antiplatelet aggression, which may be an important consideration for the successful development of drugs as anti- thrombotic drugs.
出处
《中国生物制品学杂志》
CAS
CSCD
2007年第6期432-434,438,共4页
Chinese Journal of Biologicals
