Nurtjahja-Tjendraputra Effie, Ammit Alaina J, Roufogalis Basil D, Tran Van H, Duke Colin C
Herbal Medicines Research and Education Center, Faculty of Pharmacy, University of Sydney, NSW 2006, Australia.
Thromb Res. 2003;111(4-5):259-65. doi: 10.1016/j.thromres.2003.09.009.
Based on recent studies, pungent constituents of ginger (Zingiber officinale) and related substances represent a potential new class of anti-platelet agents. The ability of 20 pungent constituents of ginger and related substances to inhibit arachidonic acid (AA) induced platelet activation in human whole blood was studied.
Anti-platelet activity of the compounds was measured in vitro by the Chrono Log whole blood platelet aggregometer. Molecular hydrophobicity (log P) was measured by reversed-phase high-performance liquid chromatography. COX-1 (ovine) inhibitory effect of [8]-paradol and analogues 1 and 5 was carried out using a COX-1 inhibitor assay kit.
[8]-Gingerol, [8]-shogaol, [8]-paradol and gingerol analogues (1 and 5) exhibited anti-platelet activities with IC(50) values ranging from 3 to 7 microM, whilst under similar conditions the IC(50) value for aspirin was 20+/-11 microM. The COX-1 inhibitory activity of [8]-paradol (IC(50)=4+/-1 microM) was more potent than the gingerol analogues (1 and 5) (IC(50) approximately 20 microM).
The above findings show that gingerol compounds and their derivatives are more potent anti-platelet agents than aspirin under the conditions described in this study. [8]-Paradol, a natural constituent of ginger, was found to be the most potent COX-1 inhibitor and anti platelet aggregation agent. The mechanism underlying AA-induced platelet aggregation inhibition may be related to attenuation of COX-1/Tx synthase enzymatic activity. Lastly, important features of phenolic compounds for inhibition of AA-induced platelet aggregation and COX-1 activity were revealed in this study.
基于最近的研究，生姜（姜科植物）的辛辣成分及相关物质代表了一类潜在的新型抗血小板药物。研究了20种生姜辛辣成分及相关物质对花生四烯酸（AA）诱导的人全血血小板活化的抑制能力。
通过Chrono Log全血血小板聚集仪在体外测量化合物的抗血小板活性。通过反相高效液相色谱法测量分子疏水性（log P）。使用COX - 1抑制剂检测试剂盒对[8]-姜辣二醇及其类似物1和5进行COX - 1（绵羊）抑制作用检测。
[8]-姜酚、[8]-姜烯酚、[8]-姜辣二醇及姜酚类似物（1和5）表现出抗血小板活性，IC50值范围为3至7微摩尔，而在类似条件下阿司匹林的IC50值为20±11微摩尔。[8]-姜辣二醇的COX - 1抑制活性（IC50 = 4±1微摩尔）比姜酚类似物（1和5）（IC50约为20微摩尔）更强。
上述研究结果表明，在本研究所述条件下，姜酚化合物及其衍生物是比阿司匹林更有效的抗血小板药物。发现生姜的天然成分[8]-姜辣二醇是最有效的COX - 1抑制剂和抗血小板聚集剂。AA诱导的血小板聚集抑制的潜在机制可能与COX - 1/Tx合酶酶活性的减弱有关。最后，本研究揭示了酚类化合物抑制AA诱导的血小板聚集和COX - 1活性的重要特征。
