Jin Weiyue, Xue Yurun, Xue Yucong, Liang Yingran, Zhang Yixin, Zhang Jianping, Chu Xi, Wang Hongfang, Guan Shengjiang
School of Basic Medicine, Hebei University of Chinese Medicine, Shijiazhuang, Hebei, China.
Gen Physiol Biophys. 2020 Sep;39(5):491-498. doi: 10.4149/gpb_2020025.
The main active components of saffron are crocin, crocetin, picrocrocin, and safranal. There are many studies on their cardioprotective effects, but their cardiotoxicities have not been reported. The human ether-a-go-go-related gene (hERG) K+ channels are of considerable pharmaceutical interest as the target responsible for acquired long QT syndromes. The aim of this study is to explore the effects of crocin, crocetin, picrocrocin, and safranal on the K+ channels encoded by hERG. The interaction of these components with the rapid delayed rectification of K+ currents (IKr) were studied using the perforated patch recording technique. Crocin and picrocrocin had no significant effects on IKr, but crocetin and safranal inhibited hERG K+ currents in a concentration-dependent manner, with IC50 values of 36.35 μM and 37.86 μM, respectively. The maximum inhibitory effects were 37.74 ± 4.14% and 33.74 ± 4.81%, respectively, and the effects were reversible upon washout. The results demonstrate that crocetin and safranal significantly inhibit hERG K+ current, but crocin and picrocrocin do not. This suggests that crocetin and safranal may increase the risk of cardiac arrhythmias by inhibiting IKr.
藏红花的主要活性成分是藏花素、藏红花酸、苦藏花素和藏红花醛。关于它们的心脏保护作用有很多研究，但尚未见其心脏毒性的报道。人类醚 - 去极化相关基因（hERG）钾通道作为获得性长QT综合征的致病靶点，具有相当大的药学研究价值。本研究旨在探讨藏花素、藏红花酸、苦藏花素和藏红花醛对hERG编码的钾通道的影响。采用穿孔膜片钳记录技术研究了这些成分与快速延迟整流钾电流（IKr）的相互作用。藏花素和苦藏花素对IKr无显著影响，但藏红花酸和藏红花醛以浓度依赖性方式抑制hERG钾电流，IC50值分别为36.35 μM和37.86 μM。最大抑制作用分别为37.74±4.14%和33.74±4.81%，洗脱后作用可逆。结果表明，藏红花酸和藏红花醛显著抑制hERG钾电流，而藏花素和苦藏花素则无此作用。这表明藏红花酸和藏红花醛可能通过抑制IKr增加心律失常的风险。
