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川芎嗪作为一种偏头痛防治化合物的作用及机制。

Effect and mechanism of senkyunolide I as an anti-migraine compound from Ligusticum chuanxiong.

机构信息

Engineering Research Center of Modern Preparation Technology of Traditional Chinese Medicine, Ministry of Education, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, China.

出版信息

J Pharm Pharmacol. 2011 Feb;63(2):261-6. doi: 10.1111/j.2042-7158.2010.01191.x.

Abstract

OBJECTIVE

To evaluate the analgesic and anti-migraine activities of senkyunolide I from Ligusticum chuanxiong.

METHODS

Mice were orally administered various doses of senkyunolide I, and their pain levels were assessed in a hot-plate test and by application of acetic acid. The levels of 5-hydroxytryptamine (5-HT), 5-hydroxytryptophan (5-HTP), 5-hydroxyindoleacetic acid (5-HIAA), norepinephrine (NE) and dopamine (DA) in plasma and brain were assessed, and the monoamine turnover rates (5-HT/5-HTP, 5-HIAA/5-HT and NE/DA) were also calculated.

RESULTS

Mice given senkyunolide I at 16 and 32 mg/kg had significantly elevated pain thresholds in the hot-plate test, and a dose of 32 mg/kg also reduced the number of abdominal writhing responses caused by acetic acid. Significant improvements were observed in the neurotransmitter levels of the drug-treated rats compared with the saline-administered controls. Compared to the rats with nitroglycerin-induced migraines, the levels of nitric oxide in the plasma and whole brain of rats given senkyunolide I were lower.

CONCLUSIONS

The present study suggests that senkyunolide I may be an active component of L. chuanxiong, traditionally used to treat migraine. The mechanism of pain relief in migraine model rats may be through adjusting the levels of monoamine neurotransmitters and their turnover rates, as well as decreasing nitric oxide levels in the blood and brain. Therefore, senkyunolide I may be developed as a potential treatment for migraine pain.

摘要

目的

评价川芎嗪酮 I 的镇痛和抗偏头痛活性。

方法

小鼠口服给予不同剂量的川芎嗪酮 I,通过热板试验和醋酸应用评估其疼痛水平。评估血浆和脑中 5-羟色胺(5-HT)、5-羟色氨酸(5-HTP)、5-羟吲哚乙酸(5-HIAA)、去甲肾上腺素(NE)和多巴胺(DA)的水平,并计算单胺转化率(5-HT/5-HTP、5-HIAA/5-HT 和 NE/DA)。

结果

给予 16 和 32 mg/kg 川芎嗪酮 I 的小鼠在热板试验中疼痛阈值显著升高,32 mg/kg 剂量还减少了醋酸引起的腹部扭曲反应次数。与生理盐水对照组相比,药物治疗大鼠的神经递质水平有显著改善。与硝酸甘油诱导偏头痛的大鼠相比,给予川芎嗪酮 I 的大鼠血浆和全脑的一氧化氮水平较低。

结论

本研究表明,川芎嗪酮 I 可能是川芎的一种活性成分,传统上用于治疗偏头痛。偏头痛模型大鼠的镇痛机制可能是通过调节单胺神经递质及其周转率的水平,以及降低血液和大脑中的一氧化氮水平。因此,川芎嗪酮 I 可能被开发为治疗偏头痛疼痛的潜在药物。

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