背景:当归是一种多年生草本植物,属于伞形科。传统上用于治疗发烧,上呼吸道感染,出血和高血压。然而,尽管其广泛的药理潜力,关于其抗高血压药理特性的文献报道很少。
目的:在研究中,研究了A.decursiva根的粗提物的抗高血压活性,并探讨了其分子基础。
方法:A.用乙醇提取decursiva根,硅胶正相色谱和反相高效液相色谱分离。使用L-NAME诱导的高血压小鼠模型来检测体内高血压活性。胸主动脉环收缩活动和电生理记录用于评估体外抗高血压活性,并揭示了抗高血压目标,在HEK293T细胞中瞬时表达。
结果:ADED在L-NAME诱导的高血压模型和去氧肾上腺素诱导的血管收缩中表现出显著的抗高血压作用。进一步的筛选显示,去甲基亚黑草素是A.decursiva的抗高血压作用的重要组成部分。电压门控钙通道CaV1.2可能是A.decursiva抗高血压作用的靶标。
结论:该研究表明,在临床前研究中,decursiva和去甲基亚瑟罗素可能是有效的抗高血压药物。看来,A.decursiva和去甲基木素通过抑制CaV1.2通道发挥抗高血压作用,这有助于血管舒张作用。本研究提供了实验证据,证明A.decursiva是民间传说中高血压的有效治疗方法。去甲基木素可能是抗高血压药物开发的主要分子。
BACKGROUND: Angelica decursiva is a perennial herb that belongs to the Umbelliferae family. It is traditionally used to treat fever, upper respiratory tract infections, bleeding and hypertension. However, despite its extensive pharmacological potential, literature reports on its antihypertensive pharmacological properties are scarce.
OBJECTIVE: In the study, crude extract from A. decursiva roots was examined for its antihypertensive activity and its molecular basis was explored.
METHODS: A. decursiva roots were extracted with ethanol, and isolated with silica gel normal-phase chromatography and reverse-phase high performance liquid chromatography. L-NAME-induced hypertensive mouse model was used to detect in vivo hypertensive activity. Thoracic aorta ring contraction activity and electrophysiology recordings were employed to evaluate in vitro antihypertensive activity and revealed an antihypertensive target, which was transiently expressed in HEK293T cells.
RESULTS: Angelica decursiva ethanol decoction (ADED) exhibited significant antihypertensive effects in L-NAME-induced hypertension models and phenylephrine-induced vasoconstriction. Further screening revealed that demethylsuberosin is an essential component accounting for the antihypertension effects of A. decursiva. Voltage-gated calcium channel CaV1.2 is the likely target of A. decursiva for its antihypertension effects.
CONCLUSIONS: The study suggests that A. decursiva and demethylsuberosin may be effective antihypertensive agents in preclinical studies. It appears that A. decursiva and demethylsuberosin exert antihypertensive effects by inhibiting the CaV1.2 channel, which contributes to the vasodilatory effect. The present study provides experimental evidence that A. decursiva is an effective remedy for hypertension in folklore. Demethylsuberosin could be a lead molecule for antihypertension drug development.