Shah B H, Nawaz Z, Pertani S A, Roomi A, Mahmood H, Saeed S A, Gilani A H
Department of Physiology and Pharmacology, The Aga Khan University, Karachi, Pakistan.
Biochem Pharmacol. 1999 Oct 1;58(7):1167-72. doi: 10.1016/s0006-2952(99)00206-3.
Curcumin, a dietary spice from turmeric, is known to be anti-inflammatory, anticarcinogenic, and antithrombotic. Here, we studied the mechanism of the antiplatelet action of curcumin. We show that curcumin inhibited platelet aggregation mediated by the platelet agonists epinephrine (200 microM), ADP (4 microM), platelet-activating factor (PAF; 800 nM), collagen (20 microg/mL), and arachidonic acid (AA: 0.75 mM). Curcumin preferentially inhibited PAF- and AA-induced aggregation (IC50; 25-20 microM), whereas much higher concentrations of curcumin were required to inhibit aggregation induced by other platelet agonists. Pretreatment of platelets with curcumin resulted in inhibition of platelet aggregation induced by calcium ionophore A-23187 (IC50; 100 microM), but curcumin up to 250 microM had no inhibitory effect on aggregation induced by the protein kinase C (PKC) activator phorbol myrsitate acetate (1 microM). Curcumin (100 microM) inhibited the A-23187-induced mobilization of intracellular Ca2+ as determined by using fura-2 acetoxymethyl ester. Curcumin also inhibited the formation of thromboxane A2 (TXA2) by platelets (IC50; 70 microM). These results suggest that the curcumin-mediated preferential inhibition of PAF- and AA-induced platelet aggregation involves inhibitory effects on TXA2 synthesis and Ca2+ signaling, but without the involvement of PKC.
姜黄素是一种来自姜黄的食用香料,已知具有抗炎、抗癌和抗血栓形成的作用。在此,我们研究了姜黄素抗血小板作用的机制。我们发现姜黄素可抑制由血小板激动剂肾上腺素(200微摩尔/升)、二磷酸腺苷(4微摩尔/升)、血小板活化因子(PAF;800纳摩尔/升)、胶原蛋白(20微克/毫升)和花生四烯酸(AA:0.75毫摩尔/升)介导的血小板聚集。姜黄素优先抑制PAF和AA诱导的聚集(半数抑制浓度;25 - 20微摩尔/升),而抑制其他血小板激动剂诱导的聚集则需要更高浓度的姜黄素。用姜黄素预处理血小板可抑制钙离子载体A - 23187诱导的血小板聚集(半数抑制浓度;100微摩尔/升),但高达250微摩尔/升的姜黄素对蛋白激酶C(PKC)激活剂佛波酯(1微摩尔/升)诱导的聚集没有抑制作用。通过使用乙酰氧基甲基酯形式的fura - 2测定发现,姜黄素(100微摩尔/升)可抑制A - 23187诱导的细胞内钙离子动员。姜黄素还可抑制血小板血栓素A2(TXA2)的形成(半数抑制浓度;70微摩尔/升)。这些结果表明,姜黄素介导的对PAF和AA诱导的血小板聚集的优先抑制作用涉及对TXA2合成和钙离子信号传导的抑制作用,但不涉及PKC。