Lee Do-Seop, Kim Tae-Ho, Jung Yi-Sook
College of Pharmacy and ‡College of Pharmacy, Research Institute of Pharmaceutical Sciences and Technology, Ajou University , Suwon 443-749, Republic of Korea.
J Agric Food Chem. 2014 Jul 23;62(29):7131-9. doi: 10.1021/jf4041518. Epub 2014 Jul 9.
Allyl isothiocyanate (AITC) is one of the major components of mustard. The present study for the first time attempted to evaluate the effect of AITC on platelet aggregation. In the in vitro study using platelet-rich plasma (PRP) from rats and humans, AITC at concentrations of 100 and 300 μM significantly inhibited platelet aggregation induced by collagen, thrombin, ADP, and arachidonic acid. AITC also attenuated thromboxane A2 production and ATP release in rat and human PRP. AITC elicited inhibitory effects on cellular Ca(2+) increase and platelet shape change in rat PRP. AITC further showed inhibitory effects on the phosphorylation of PKCδ, p38, ERK, and Akt in rat PRP. In the rat ex vivo study, 1 and 3 mg/kg (po) of AITC showed significant inhibitory effect on platelet aggregation. Furthermore, AITC showed a protective effect in thromboembolism attack model in mouse. These results suggest that AITC has remarkable antiplatelet effects and maybe a therapeutic potential for the prevention of aberrant platelet activation-related disorders.
异硫氰酸烯丙酯(AITC)是芥末的主要成分之一。本研究首次尝试评估AITC对血小板聚集的影响。在使用大鼠和人类富血小板血浆(PRP)的体外研究中,100和300μM浓度的AITC显著抑制了由胶原蛋白、凝血酶、ADP和花生四烯酸诱导的血小板聚集。AITC还减弱了大鼠和人类PRP中血栓素A2的产生和ATP的释放。AITC对大鼠PRP中细胞Ca(2+)增加和血小板形状变化产生抑制作用。AITC对大鼠PRP中PKCδ、p38、ERK和Akt的磷酸化也有抑制作用。在大鼠离体研究中,1和3mg/kg(口服)的AITC对血小板聚集有显著抑制作用。此外,AITC在小鼠血栓栓塞攻击模型中显示出保护作用。这些结果表明,AITC具有显著的抗血小板作用,可能对预防异常血小板激活相关疾病具有治疗潜力。