Huang Jun, Ma Li-Qun, Yang Yongle, Wen Nana, Zhou Wan, Cai Congli, Liu Qing-Hua, Shen Jinhua
Institute for Medical Biology and Hubei Provincial Key Laboratory for Protection and Application of Special Plants in Wuling Area of China, College of Life Sciences, South-Central University for Nationalities, Wuhan 430074, China.
Wuhan Youzhiyou Biopharmaceutical Co., Ltd., 666 Gaoxin Rd., Biolake, Wuhan 430075, China.
Evid Based Complement Alternat Med. 2017;2017:9870414. doi: 10.1155/2017/9870414. Epub 2017 Nov 12.
L. belongs to the Asteraceae family, which is indigenous to China. It has valuable pharmacological properties, such as antimalarial, anti-inflammatory, and anticancer properties. However, whether it possesses antiasthma properties is unknown. In the current study, chloroform extract of L. (CEAA) was prepared, and we found that CEAA completely eliminated acetylcholine (ACh) or high K-elicited (80 mM) contractions of mouse tracheal rings (TRs). Patch-clamp technique and ion channel blockers were employed to explore the underlying mechanisms of the relaxant effect of CEAA. In whole-cell current recording, CEAA almost fully abolished voltage-dependent Ca channel (VDCC) currents and markedly enhanced large conductance Ca-activated K (BK) channel currents on airway smooth muscle cells (ASMCs). In single channel current recording, CEAA increased the opening probability but had no effect on the single channel conductance of BK channels. However, under paxilline-preincubated (a selective BK channel blocker) conditions, CEAA only slightly increased BK channel currents. These results indicate that CEAA may contain active components with potent antiasthma activity. The abolished VDCCs by CEAA may mainly contribute to the underlying mechanism through which it acts as an effective antiasthmatic compound, but the enhanced BK currents might play a less important role in the antiasthmatic effects.
L.属于菊科,原产于中国。它具有宝贵的药理特性,如抗疟疾、抗炎和抗癌特性。然而,它是否具有抗哮喘特性尚不清楚。在当前的研究中,制备了L.的氯仿提取物(CEAA),我们发现CEAA完全消除了乙酰胆碱(ACh)或高钾(80 mM)引起的小鼠气管环(TRs)收缩。采用膜片钳技术和离子通道阻滞剂来探究CEAA舒张作用的潜在机制。在全细胞电流记录中,CEAA几乎完全消除了气道平滑肌细胞(ASMCs)上的电压依赖性钙通道(VDCC)电流,并显著增强了大电导钙激活钾(BK)通道电流。在单通道电流记录中,CEAA增加了BK通道的开放概率,但对其单通道电导没有影响。然而,在预先用paxilline(一种选择性BK通道阻滞剂)孵育的条件下,CEAA仅略微增加了BK通道电流。这些结果表明,CEAA可能含有具有强大抗哮喘活性的活性成分。CEAA对VDCCs的消除可能是其作为一种有效抗哮喘化合物发挥作用的主要潜在机制,但增强的BK电流在抗哮喘作用中可能起的作用较小。