Apitz-Castro R, Escalante J, Vargas R, Jain M K
Thromb Res. 1986 May 1;42(3):303-11. doi: 10.1016/0049-3848(86)90259-8.
Ajoene, the major antiplatelet compound derived from garlic, synergistically potentiates the antiaggregatory action of prostacyclin, forskolin, indomethacin and dypiridamole. For collagen-induced platelet aggregation in human PRP, the ID50 for ajoene is 95 +/- 5 microM. However, in the presence of the antiaggregatory drugs mentioned above, the ID50 for ajoene decreases more than what would be predicted on the basis of simple additive effects. Similarly, the ID50 for prostacyclin decreases from 1 nM to 0.15 nM in the presence of 80 microM ajoene. Isobolic curves for the various combinations of ajoene with prostacyclin or indomethacin exhibit departure from linearity, as predicted for a potentiated synergism between ajoene and these drugs. Dypiridamole, which in PRP has very little effect on the dose-response curve for ajoene, when assayed in whole blood decreases the ID50 for ajoene by a factor of four. These results demonstrate that the antithrombotic potential of ajoene is substantially increased in the presence of physiologically and pharmacologically active antiplatelet agents.
大蒜素是大蒜中的主要抗血小板化合物,它能协同增强前列环素、福斯高林、吲哚美辛和双嘧达莫的抗聚集作用。对于人富血小板血浆中胶原蛋白诱导的血小板聚集,大蒜素的半数抑制浓度(ID50)为95±5微摩尔。然而,在上述抗聚集药物存在的情况下,大蒜素的ID50下降幅度超过基于简单相加效应的预测值。同样,在80微摩尔大蒜素存在的情况下,前列环素的ID50从1纳摩尔降至0.15纳摩尔。大蒜素与前列环素或吲哚美辛的各种组合的等效应线显示出偏离线性,正如预测的大蒜素与这些药物之间的增效协同作用那样。双嘧达莫在富血小板血浆中对大蒜素的剂量反应曲线影响很小,但在全血中检测时,可使大蒜素的ID50降低四倍。这些结果表明,在生理和药理活性抗血小板药物存在的情况下,大蒜素的抗血栓形成潜力会显著增加。