芦丁拮抗血小板活化因子与受体结合的作用

Inhibition of rutin on binding of platelet activating factor and receptor

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、4 nm ol/L [3H]PAF与血小板受体的特异性结合,其IC50 分别为7.3、8.7、17.2 mm ol/L ;芦丁可明显抑制PAF介导的血小板黏附,IC50 为1.5 1mm ol/L;芦丁浓度为6 8.2～5 4 6 μm ol/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。

Objective To observe the platelet activating factor (PAF)-receptor binding antagonistic effect of rutin. Methods The specific binding of [ 3H] 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-2 fluorescent technique. Results The specific binding inhibition of rutin was found to be concentration-dependent, the IC 50 of rutin in the concentrations of [ 3H] PAF 1, 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 IC 50 being 1.51 mmol/L. PMNs inner free calcium concentration increment induced by PAF was inhibited by rutin in the concentration of 68.2—546 μmol/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.