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目的:观察人参皂苷20(S)-Rg3和20(R)-Rg3的的大鼠体内抗凝血活性和体外ADP诱导的血小板聚集活性的差异,初步探究其抗凝作用机制。方法:将大鼠随机分为5组[对照组、20(S)-Rg3和20(R)-Rg3低、高剂量组],每组3只。给药组分别以5 mg·kg-1和20 mg·kg-1剂量尾静脉给药,眼眶取血后,测定血浆的APTT、PT和TT值;取大鼠全血,以ADP为诱导剂,体外测定Rg3对血小板聚集的抑制率。结果:在20 mg·kg-1的剂量下,20(R)-Rg3对APTT有显著的延长作用(P<0.05),对PT有显著的缩短作用(P<0.05),而S构型则对上述指标无显著的影响。1 mg·m L-1的20(R)-Rg3显著抑制ADP诱导的血小板聚集(P<0.05),而20(S)-Rg3则显著促进ADP诱导的血小板聚集(P<0.01)。结论:人参皂苷Rg3的两个手性异构体在抗凝血和抗血小板聚集作用上有差异。20(R)-Rg3构型相对于S构型更具有抗凝作用,通过延长APTT和抗血小板聚集两种机制体现出来。
OBJECTIVE: To observe the difference between the anticoagulant activity of ginsenoside 20 (S) -Rg3 and 20 (R) -Rg3 in rats and the ADP-induced platelet aggregation activity in vitro, and to explore the anticoagulant mechanism. Methods: The rats were randomly divided into 5 groups [control group, 20 (S) -Rg3 and 20 (R) -Rg3 low and high dose groups], 3 in each group. The rats in the treatment group were administered with 5 mg · kg-1 and 20 mg · kg-1 doses of tail vein respectively, and the orbital blood was collected to measure the plasma APTT, PT and TT values. Whole blood was taken from rats and ADP was used as an inducer , In vitro determination of Rg3 inhibition of platelet aggregation. Results: 20 (R) -Rg3 significantly prolonged the APTT (P <0.05) and shortened the PT (P <0.05) at the dose of 20 mg · kg-1, while the S configuration No significant impact on the above indicators. 20 (R) -Rg3 at 1 mg · mL-1 significantly inhibited ADP-induced platelet aggregation (P <0.05), while 20 (S) -Rg3 significantly promoted ADP-induced platelet aggregation (P <0.01). CONCLUSION: The two chiral isomers of ginsenoside Rg3 differ in their anti-coagulation and anti-platelet aggregation effects. The 20 (R) -Rg3 configuration is more anticoagulant than the S configuration and is manifested by two mechanisms: prolonged APTT and anti-platelet aggregation.