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来自厄瓜多尔亚马逊地区野生基乔柯特桂(樟科)花萼的精油的抗血小板和抗血栓形成活性

Antiplatelet and antithrombotic activities of essential oil from wild Ocotea quixos (Lam.) Kosterm. (Lauraceae) calices from Amazonian Ecuador.

作者信息

Ballabeni Vigilio, Tognolini Massimiliano, Bertoni Simona, Bruni Renato, Guerrini Alessandra, Rueda Gabriela Moreno, Barocelli Elisabetta

机构信息

Dip. di Scienze Farmacologiche, Biologiche e Chimiche Applicate, Università di Parma, Viale G.P.Usberti 27/A, 43100 Parma, Italy.

出版信息

Pharmacol Res. 2007 Jan;55(1):23-30. doi: 10.1016/j.phrs.2006.09.009. Epub 2006 Sep 29.

Abstract

Ocotea quixos essential oil was shown to possess significant inhibitory activity of platelet aggregation and clot retraction in rodent plasma. This study is aimed at fully characterizing the antiplatelet activity of the whole essential oil and its main components trans-cinnamaldehyde and methyl cinnamate also in human plasma, at investigating the mechanism underlying such activity and at evaluating the potential antithrombotic activity of subacute treatment of mice with Ocotea essential oil. In vitro Ocotea essential oil and trans-cinnamaldehyde inhibited arachidonic acid-, U46619-, ADP-, phorbol12-myristate13-alcetate-, collagen-induced platelet aggregation and thrombin-induced clot retraction in human and rodent plasma; Ocotea oil and trans-cinnamaldehyde competitively antagonized contractions induced by thromboxane A2 receptor agonist U46619 in rat isolated aortic ring (K(B) = 18 and 3.2 microg ml(-1), respectively). In vivo Ocotea oil, orally administered in a subacute treatment (30-100 mg kg(-1) day(-1) for 5 days) to mice, prevented acute thrombosis induced by collagen-epinephrine intravenous injection. This antithrombotic activity was not accompanied by pro-haemorragic side effect, as detected by the inactivity in bleeding test, thus showing a favourable safety profile compared to the conventional antiplatelet agent, acetylsalicylic acid. Present findings indicate that Ocotea essential oil possesses potent and safe antithrombotic activity attributable to its antiplatelet and vasorelaxant effects. The main constituent trans-cinnamaldehyde seems to be the primary responsible for this activity through a putative mechanism involving the inhibition of thromboxane A2 receptors.

摘要

樟桂叶油在啮齿动物血浆中显示出显著的抑制血小板聚集和凝块退缩的活性。本研究旨在全面表征该全精油及其主要成分反式肉桂醛和肉桂酸甲酯在人血浆中的抗血小板活性,研究这种活性的潜在机制,并评估用樟桂叶油对小鼠进行亚急性治疗的潜在抗血栓形成活性。在体外,樟桂叶油和反式肉桂醛可抑制花生四烯酸、U46619、ADP、佛波酯12 -肉豆蔻酸13 -乙酯、胶原诱导的人及啮齿动物血浆中的血小板聚集和凝血酶诱导的凝块退缩;樟桂叶油和反式肉桂醛竞争性拮抗血栓素A2受体激动剂U46619在大鼠离体主动脉环中诱导的收缩(KB分别为18和3.2μg ml-1)。在体内,对小鼠进行亚急性治疗(30 - 100mg kg-1天-1,持续5天)口服樟桂叶油,可预防胶原 - 肾上腺素静脉注射诱导的急性血栓形成。通过出血试验未检测到活性,表明这种抗血栓形成活性未伴有促出血副作用,因此与传统抗血小板药物乙酰水杨酸相比,显示出良好的安全性。目前的研究结果表明,樟桂叶油具有强效且安全的抗血栓形成活性,这归因于其抗血小板和血管舒张作用。主要成分反式肉桂醛似乎是这种活性的主要原因,其可能机制涉及抑制血栓素A2受体。

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