Department of Pharmacology, Central Drug Research Institute (CSIR), 1. M.G. Marg, Lucknow - (U.P) - 226001 India.
Thromb Res. 2011 Feb;127(2):111-8. doi: 10.1016/j.thromres.2010.11.007. Epub 2010 Dec 8.
Extensive research on the mechanism of action and medicinal importance of curcumin obtained from turmeric (Curcuma longa) has unfolded its potential therapeutic value against many chronic ailments. Curcuma oil (C.oil), the highly lipophilic component from Curcuma longa has been documented for its neuroprotective efficacy against rat cerebral ischemia-reperfusion injury; however its effect on myocardial reperfusion injury remains unexplored. In the present study, effect of C.oil (500 mg/kg, po) was evaluated against myocardial ischemia-reperfusion induced injury in the rat model. C.oil failed to confer protection against cardiac injury, however significant reversal of ADP induced platelet aggregation (p<0.05) was evident in the same animals. Moreover, collagen and thrombin induced platelet aggregation (p<0.001) as well as tyrosine phosphorylation of various proteins in activated platelets was also suppressed. C.oil also offered significant protection against collagen-epinephrine induced thromboembolism in mice as well as augmented total time to occlusion against FeCl(3) induced arterial thrombosis in rats. C.oil however had no effect on coagulation parameters (TT, PT and aPTT) and exerted a mild effect on the bleeding time. Bioavailability of C.oil, as assessed by monitoring ar-turmerone, α,β-turmerone and curlone, was 13%, 11% and 7% respectively, indicating high systemic exposure. Moreover, longer mean residence time (MRT) of ar-turmerone (13.2h), α,β-turmerone (11.6h) and Curlone (14.0 h) and plasma elimination half lives in the range of 5.5 to 7.2h correlated with single 500 mg/kg dose regimen of C.oil. In the present study, C.oil thus seems to be an efficacious and safe anti-platelet agent which was protective against intravascular thrombosis.
从姜黄(Curcuma longa)中提取的姜黄素的作用机制和医学重要性的广泛研究已经揭示了其对许多慢性疾病的潜在治疗价值。姜黄油(C.oil)是姜黄的高亲脂性成分,已被证明具有对抗大鼠脑缺血再灌注损伤的神经保护作用;然而,其对心肌再灌注损伤的影响仍未得到探索。在本研究中,评估了 C.oil(500mg/kg,po)对大鼠心肌缺血再灌注损伤的作用。C.oil 未能提供对心脏损伤的保护,但在相同动物中明显逆转了 ADP 诱导的血小板聚集(p<0.05)。此外,胶原和凝血酶诱导的血小板聚集(p<0.001)以及激活血小板中各种蛋白质的酪氨酸磷酸化也被抑制。C.oil 还对胶原-肾上腺素诱导的小鼠血栓栓塞以及增加 FeCl3 诱导的大鼠动脉血栓形成的总闭塞时间提供了显著保护。然而,C.oil 对凝血参数(TT、PT 和 aPTT)没有影响,对出血时间只有轻微影响。通过监测 ar-姜黄素、α,β-姜黄素和 curlone 来评估 C.oil 的生物利用度,分别为 13%、11%和 7%,表明其具有高全身暴露。此外,ar-姜黄素(13.2h)、α,β-姜黄素(11.6h)和 curlone(14.0h)的平均驻留时间(MRT)较长,血浆消除半衰期在 5.5 到 7.2h 范围内,与 C.oil 单次 500mg/kg 剂量方案相关。在本研究中,C.oil 似乎是一种有效且安全的抗血小板药物,可预防血管内血栓形成。