Food Function Research Division, Korea Food Research Institute, Gyeonggido 463-746, Korea.
Biol Pharm Bull. 2010;33(8):1360-3. doi: 10.1248/bpb.33.1360.
Ligusticum wallichii is an herb widely used to treat vascular disorders in Asian countries, and tetramethylpyrazine (TMP) has been identified as one of its vasorelaxant active components. This study was performed to examine the endothelium-independent relaxation produced by the butanol-soluble fraction of L. wallichii extract (LwBt) and its possible mechanisms of action in isolated rat aortic rings. The effects were compared with those of TMP. LwBt produced vasorelaxation that increased gradually after 2-3 min of LwBt administration and reached a maximum within 30 min. LwBt-induced relaxation was significantly attenuated by pretreatment with 4-aminopyridine and apamin. Additionally, LwBt attenuated CaCl(2)-induced vasoconstriction in high-potassium depolarized medium. Thus, LwBt-induced vasorelaxation apparently involved inhibition of calcium influx, mediated by the opening of voltage-dependent and/or Ca(2+)-activated potassium channels. On the other hand, the effect of TMP was significantly attenuated by pretreatment with glibenclamide, and 4-aminopyridine had no effect. In conclusion, LwBt-induced endothelium-independent vasorelaxation was mediated by the opening of voltage-dependent potassium channels, while TMP-induced relaxation was mediated by the opening of ATP-dependent potassium channels. These effects of LwBt may be due to a substance other than TMP.
当归是一种在亚洲国家被广泛用于治疗血管疾病的草药,其中已鉴定出川芎嗪(TMP)是其血管舒张活性成分之一。本研究旨在检测当归提取物的丁醇可溶部分(LwBt)产生的非内皮依赖性血管舒张作用及其在分离的大鼠主动脉环中的可能作用机制,并将其与 TMP 的作用进行比较。LwBt 产生的血管舒张作用在给药后 2-3 分钟逐渐增加,并在 30 分钟内达到最大值。LwBt 诱导的松弛作用在前处理 4-氨基吡啶和阿帕米时明显减弱。此外,LwBt 还可减轻高钾去极化介质中 CaCl2 诱导的血管收缩。因此,LwBt 诱导的血管舒张显然涉及钙内流的抑制,这是通过开放电压依赖性和/或 Ca(2+)激活的钾通道介导的。另一方面,TMP 的作用在前处理格列本脲时明显减弱,而 4-氨基吡啶没有作用。总之,LwBt 诱导的非内皮依赖性血管舒张是通过开放电压依赖性钾通道介导的,而 TMP 诱导的松弛是通过开放 ATP 依赖性钾通道介导的。LwBt 的这些作用可能归因于 TMP 以外的物质。