Liao C H, Ko F N, Kuo Y H, Teng C M
Pharmacological Institute, College of Medicine, National Taiwan University, Taipei.
Can J Physiol Pharmacol. 1996 Oct;74(10):1111-6. doi: 10.1139/cjpp-74-10-1111.
A semisynthetic chemical compound, demethyldiisoeugenol, concentration dependently inhibited platelet aggregation and ATP release stimulated by thrombin (0.1 U/mL), platelet-activating factor (2 ng/mL), arachidonic acid (100 microM), collagen (10 micrograms/mL), and U46619 (1 microM) in rabbit washed platelets. The IC50 values of demethyldiisoeugenol on the inhibition of platelet aggregation induced by these five agonists were 157.3 +/- 22.3, 156.2 +/- 12.9, 53.6 +/- 4.7, 54.5 +/- 3.9, and 87.7 +/- 3.2 microM, respectively. Demethyldiisoeugenol also inhibited thromboxane B2 formation induced by thrombin, platelet-activating factor, arachidonic acid, and collagen, and prostaglandin D2 formation was induced by arachidonic acid. The rising intracellular Ca2+ concentration stimulated by these five platelet aggregation inducers was inhibited by demethyldiisoeugenol, while formation of inositol monophosphate was unaffected. Platelet cAMP and cGMP levels were unchanged by demethyldiisoeugenol. It is concluded that demethyldiisoeugenol may directly inhibit both intracellular calcium mobilization and cyclooxygenase activity in platelets.
半合成化合物去甲基二异丁香酚在兔洗涤血小板中,能浓度依赖性地抑制由凝血酶(0.1 U/mL)、血小板活化因子(2 ng/mL)、花生四烯酸(100 microM)、胶原(10微克/毫升)和U46619(1 microM)刺激引起的血小板聚集和ATP释放。去甲基二异丁香酚对这五种激动剂诱导的血小板聚集抑制作用的IC50值分别为157.3±22.3、156.2±12.9、53.6±4.7、54.5±3.9和87.7±3.2 microM。去甲基二异丁香酚还抑制由凝血酶、血小板活化因子、花生四烯酸和胶原诱导的血栓素B2形成,以及由花生四烯酸诱导的前列腺素D2形成。去甲基二异丁香酚抑制了这五种血小板聚集诱导剂刺激引起的细胞内Ca2+浓度升高,而肌醇单磷酸的形成未受影响。去甲基二异丁香酚对血小板cAMP和cGMP水平无影响。结论是,去甲基二异丁香酚可能直接抑制血小板内的钙动员和环氧化酶活性。