Elkhatali Samya, Maayah Zaid H, El-Sherbeni Ahmed A, Elshenawy Osama H, Abdelhamid Ghada, Shoieb Sherif M, El-Kadi Ayman O S
Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta, Canada.
J Cardiovasc Pharmacol. 2017 Jul;70(1):16-24. doi: 10.1097/FJC.0000000000000494.
Recent data demonstrated the role of CYP1B1 in cardiovascular disease. It was, therefore, necessary to examine whether the inhibition of CYP1B1 and hence inhibiting the formation of its metabolites, using 2,4,3',5'-tetramethoxystilbene (TMS), would have a cardioprotective effect against angiotensin II (Ang II)-induced cardiac hypertrophy. For this purpose, male Sprague Dawley rats were treated with Ang II with or without TMS (300 μg/kg every third day i.p.). Thereafter, cardiac hypertrophy and the formation of mid-chain HETEs and arachidonic acid were assessed. In vitro, RL-14 cells were treated with Ang II (10 μM) in the presence and absence of TMS (0.5 μM). Then, reactive oxygen species, mitogen-activated protein kinase phosphorylation levels, and nuclear factor-kappa B-binding activity were determined. Our results demonstrated that TMS protects against Ang II-induced cardiac hypertrophy as indicated by the improvement in cardiac functions shown by the echocardiography as well as by reversing the increase in heart weight to tibial length ratio caused by Ang II. In addition, the cardioprotective effect of TMS was associated with a significant decrease in cardiac mid-chain HETEs levels. Mechanistically, TMS inhibited reactive oxygen species formation, the phosphorylation of ERK1/2, p38 mitogen-activated protein kinase, and the binding of p65 NF-κB.
近期数据表明CYP1B1在心血管疾病中发挥的作用。因此,有必要研究使用2,4,3',5'-四甲氧基茋(TMS)抑制CYP1B1从而抑制其代谢产物的形成,是否会对血管紧张素II(Ang II)诱导的心脏肥大产生心脏保护作用。为此,将雄性Sprague Dawley大鼠用Ang II处理,同时或不同时给予TMS(每三天腹腔注射300μg/kg)。此后,评估心脏肥大以及中链HETEs和花生四烯酸的形成。在体外,在存在和不存在TMS(0.5μM)的情况下,用Ang II(10μM)处理RL-14细胞。然后,测定活性氧、丝裂原活化蛋白激酶磷酸化水平和核因子-κB结合活性。我们的结果表明,TMS可预防Ang II诱导的心脏肥大,这通过超声心动图显示的心脏功能改善以及逆转Ang II引起的心脏重量与胫骨长度比值增加来表明。此外,TMS的心脏保护作用与心脏中链HETEs水平的显著降低有关。从机制上讲,TMS抑制活性氧的形成、ERK1/2、p38丝裂原活化蛋白激酶的磷酸化以及p65 NF-κB的结合。