School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, China.
Guangdong Pharmaceutical University, Guangzhou 510006, China.
Molecules. 2020 Feb 17;25(4):885. doi: 10.3390/molecules25040885.
is a plant with a native range in China used in herbal medicine for treating angina pectoris. In this study, we investigated the vasodilatory effects of isodillapiolglycol (IDG), which is one of the main ingredients isolated from ethyl acetate extract, in Sprague-Dawley rat aortic rings, and measured intracellular Ca ([Ca]) using a molecular fluo-3/AM probe. The results show that IDG dose-dependently relaxed endothelium-intact or -denuded aortic rings pre-contracted with noradrenaline (NE) or potassium chloride (KCl), and inhibited CaCl-induced contraction in high K depolarized aortic rings. Tetraethyl ammonium chloride (a Ca-activated K channel blocker) or verapamil (an L-type Ca channel blocker) significantly reduced the relaxation of IDG in aortic rings pre-contracted with NE. In vascular smooth muscle cells, IDG inhibited the increase in [Ca] stimulated by KCl in Krebs solution; likewise, IDG also attenuated the increase in [Ca] induced by NE or subsequent supplementation of CaCl. These findings demonstrate that IDG relaxes aortic rings in an endothelium-independent manner by reducing [Ca], likely through inhibition of the receptor-gated Ca channel and the voltage-dependent Ca channel, and through opening of the Ca-activated K channel.
是一种原产于中国的植物,在草药学中用于治疗心绞痛。在这项研究中,我们研究了异紫堇醇苷(IDG)的血管舒张作用,IDG 是从乙酸乙酯提取物中分离得到的主要成分之一,我们使用分子荧光-3/AM 探针测量了 Sprague-Dawley 大鼠主动脉环中的细胞内 Ca([Ca])。结果表明,IDG 浓度依赖性地松弛了去内皮或内皮完整的由去甲肾上腺素(NE)或氯化钾(KCl)预收缩的主动脉环,并抑制了在高 K 去极化的主动脉环中由 CaCl2 诱导的收缩。四乙铵氯化物(一种 Ca 激活的 K 通道阻滞剂)或维拉帕米(一种 L 型 Ca 通道阻滞剂)显著减少了 IDG 在 NE 预收缩的主动脉环中的松弛作用。在血管平滑肌细胞中,IDG 抑制了 Krebs 溶液中由 KCl 刺激引起的 [Ca]增加;同样,IDG 也减弱了由 NE 或随后补充 CaCl2 引起的 [Ca]增加。这些发现表明,IDG 通过减少 [Ca]以非内皮依赖性方式松弛主动脉环,可能通过抑制受体门控 Ca 通道和电压依赖性 Ca 通道,以及通过打开 Ca 激活的 K 通道来实现。