Srivastava K C, Malhotra N
Department of Environmental Medicine, ISH, Odense C, Denmark.
Prostaglandins Leukot Essent Fatty Acids. 1991 Jan;42(1):73-81. doi: 10.1016/0952-3278(91)90070-l.
In continuation of our studies with the oil of cloves--a common kitchen spice and a crude drug for home medicine--we have isolated yet another active component identified as acetyl eugenol (AE); the earlier reported active component being eugenol. The isolated material (IM) was found to be a potent platelet inhibitor; IM abolished arachidonate (AA)-induced aggregation at ca. 12 microM, a concentration needed to abolish the second phase of adrenaline-induced aggregation. Chemically synthesized acetyl eugenol showed similar effects on AA- and adrenaline-induced aggregation. A dose-dependent inhibition of collagen-induced aggregation was also observed. AE did not inhibit either calcium ionophore A23187- or thrombin-induced aggregation. Studies on aggregation and ATP release were done using whole blood (WB). AA-induced aggregation in WB was abolished at 3 micrograms/ml (14.6 microM) which persisted even after doubling the concentration of AA. ATP release was inhibited. Inhibition of aggregation appeared to be mediated by a combination of two effects: reduced formation of thromboxane and increased generation of 12-lipoxygenase product (12-HPETE). These effects were observed by exposing washed platelets to (14C)AA or by stimulating AA-labelled platelets with ionophore A23187. Acetyl eugenol inhibited (14C)TxB2 formation in AA-labelled platelets on stimulation with thrombin. AE showed no effect on the incorporation of AA into platelet phospholipids.
在我们对丁香油——一种常见的厨房香料和家用药物的研究中,我们又分离出了另一种活性成分,鉴定为乙酰丁香酚(AE);先前报道的活性成分是丁香酚。分离出的物质(IM)被发现是一种有效的血小板抑制剂;IM在约12微摩尔浓度时可消除花生四烯酸(AA)诱导的聚集,这一浓度也是消除肾上腺素诱导聚集第二阶段所需的浓度。化学合成的乙酰丁香酚对AA和肾上腺素诱导的聚集表现出类似的作用。还观察到对胶原诱导聚集的剂量依赖性抑制。AE对钙离子载体A23187或凝血酶诱导的聚集均无抑制作用。使用全血(WB)进行了聚集和ATP释放的研究。WB中AA诱导的聚集在3微克/毫升(14.6微摩尔)时被消除,即使将AA浓度加倍,这种抑制作用仍持续存在。ATP释放受到抑制。聚集的抑制似乎是由两种作用共同介导的:血栓素形成减少和12 - 脂氧合酶产物(12 - HPETE)生成增加。通过将洗涤后的血小板暴露于(14C)AA或用离子载体A23187刺激AA标记的血小板观察到了这些作用。乙酰丁香酚在凝血酶刺激下抑制AA标记血小板中(14C)TxB2的形成。AE对AA掺入血小板磷脂没有影响。