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[摘要]
目的观察芦丁对血小板活化因子(PAF)与受体结合的拮抗作用.方法以放射配基结合试验观察[3H]PAF与家兔血小板受体特异性结合的作用;体外以分光光度法测定PAF介导血小板黏附的强度;以Fura-2荧光分光光度法测定PAF介导的兔多形核白细胞(PMNs)内钙离子浓度的升高.结果芦丁可浓度依赖地抑制1、2、4nmol/L[3H]PAF与血小板受体的特异性结合,其IC50分别为7.3、8.7、17.2mmol/L;芦丁可明显抑制PAF介导的血小板黏附,IC50为1.51mmol/L;芦丁浓度为68.2~546μmol/L时可浓度依赖地抑制PAF介导的PMNs内游离钙浓度的升高.结论芦丁具有抗PAF作用,为一种新的PAF受体拮抗剂.
[Key word]
[Abstract]
Objective To observe the platelet activating factor(PAF)一receptor binding antagonistic effect of rutin.Methods The specific binding of[3HI PAF to rabbit platelet receptor was investigated by radio ligand binding assay(RLBA).Platelet adhesion induced by PAF was measured with spectrophotometry in vitro.Rabbit polymorphonucleocytes(PMNs)inner free calcium concentration increment of rabbit induced by PAF was assayed by Fura一2 fluorescent technique.Results The specific binding inhibition of rutin was found to be concentration—dependent,the IC Eo of rutin in the concentrations of[3H]PAF1,2,4 nmol/L was 7.3,8.7,and 17.2 mmol/L,respectively.The PAF—induced reactions of rabbit platelet adhesion were inhibited by rutin in IC50 being 1.51 mmol/L.PMNs inner free calcium concentration increment induced by PAF was inhibited by rutin in the concentration of 68.2—546gmol/L in a concentration—dependent manner.Conclusion The specific receptor binding of PAF can be antagonized by rutin which is a new receptor antagonist to PAF.
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[基金项目]
国家自然科学基金(39670884);北京市自然科学基金(7013034)