Yuan Ruqiang, Gao Mingjing, Xu Hu, Liang Qing, Qian Lei, Wang Yali, Zhang Houli, Qiang Erjiao, Yun Weijing
Advanced Institute for Medical Sciences, Dalian Medical University, Dalian, 116044, China.
Department of Pharmacy, Dalian Port Hospital, Dalian, 116001, China.
BMC Cardiovasc Disord. 2025 Jan 6;25(1):7. doi: 10.1186/s12872-024-04461-2.
The dried root of Inula helenium L., known as Inulae Radix in Mongolian medicine, is a widely used heat-clearing plant drug within the Asteraceae family. Alantolactone (ATL), a compound derived from Inulae Radix, is a sesquiterpene lactone with a range of biological activities. However, there is a lack of studies investigating its effectiveness in the treatment of hypertension. The aim of this study is to explore the regulatory effect of alantolactone on blood pressure and its underlying mechanism.
Network pharmacology analysis suggested that ATL had a potential therapeutic effect on hypertension induced by angiotensin II (Ang II). Subsequently, the results of animal experiments demonstrated that ATL could suppress the increase in blood pressure caused by Ang II. Vascular ring experiments indicated that ATL could inhibit the vascular contractions induced by Ang II, Phenylephrine, and Ca⁺. Further experiments demonstrated that ATL could inhibit the calcium influx induced by Ang II and increase the expression of pMLC2. Molecular docking experiments showed that ATL had a high binding affinity with L-type Voltage-gated Calcium Channels (VGCC), and vascular ring experiments indicated that ATL could significantly inhibit the vascular contractions caused by the agonists of L-type VGCC. In addition, we also observed that ATL had an ameliorative effect on the vascular remodeling induced by Ang II.
ATL exerted an antihypertensive effect by inhibiting the activation of L-type VGCC and reducing calcium influx.
土木香干燥根在蒙药中称为土木香，是菊科中广泛使用的清热植物药。土木香内酯（ATL）是一种从土木香中提取的化合物，是一种具有多种生物活性的倍半萜内酯。然而，目前缺乏关于其治疗高血压有效性的研究。本研究旨在探讨土木香内酯对血压的调节作用及其潜在机制。
网络药理学分析表明，ATL对血管紧张素II（Ang II）诱导的高血压具有潜在治疗作用。随后，动物实验结果表明，ATL可抑制Ang II引起的血压升高。血管环实验表明，ATL可抑制Ang II、去氧肾上腺素和Ca⁺诱导的血管收缩。进一步实验表明，ATL可抑制Ang II诱导的钙内流并增加pMLC2的表达。分子对接实验表明，ATL与L型电压门控钙通道（VGCC）具有高结合亲和力，血管环实验表明，ATL可显著抑制L型VGCC激动剂引起的血管收缩。此外，我们还观察到ATL对Ang II诱导的血管重塑具有改善作用。
ATL通过抑制L型VGCC的激活和减少钙内流发挥降压作用。
