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目的甲基丁香酚是细辛挥发油的主要成分之一,对甲基丁香酚镇痛抗炎效果进行评价,探索其镇痛作用机制。方法本研究以醋酸刺激痛、福尔马林刺激痛、热刺激痛实验和二甲苯致小鼠耳肿胀实验评价甲基丁香酚的镇痛、抗炎作用,并以受体阻断实验、一氧化氮(NO)检测实验探讨其镇痛作用机制。结果 (1)甲基丁香酚(6,3,1.5 mg·kg~(-1)),在醋酸刺激痛实验中,显著抑制小鼠扭体次数,抑制率分别为56.58%,51.25%,40.93%;在福尔马林刺激痛实验中,缩短Ⅱ相舔足、咬足时间,抑制率分别为56.62%,47.03%,33.98%;在热刺激痛实验中明显延长小鼠热痛潜伏期,在2 h镇痛作用达高峰,痛阈提高率分别为57.32%,42.14%,26.29%。(2)甲基丁香酚(6,3,1.5 mg·kg~(-1))明显抑制二甲苯所致小鼠耳肿胀,抑制率分别为76.43%,57.23%,35.00%。(3)受体阻断实验显示甲基丁香酚(6 mg·kg~(-1))镇痛作用可被GABA_A受体阻断剂荷包牡丹碱(3 mg·kg~(-1))阻断,不能被阿片受体阻断剂纳洛酮(3 mg·kg~(-1))阻断。NO检测实验显示甲基丁香酚(6 mg·kg~(-1))可抑制醋酸致痛小鼠血清NO水平。结论本研究表明细辛挥发油成分甲基丁香酚有明显镇痛抗炎作用,其镇痛作用机制与激动GABAA受体,抑制NO水平相关。
Objective Methyl eugenol is one of the main components of the volatile oil of Asarum, analgesic and anti-inflammatory effects of methyl eugenol to evaluate its analgesic mechanism. Methods In this study, analgesic and anti-inflammatory effects of methyl eugenol were evaluated by acetic acid stimulation pain, formalin stimulation pain, heat stimulation pain test and xylene-induced mouse ear swelling test. Nitric oxide (NO) test to explore its analgesic mechanism. Results (1) Methyl eugenol (6, 3, 1.5 mg · kg -1) significantly inhibited the number of writhing in mice stimulated by acetic acid with the inhibitory rates of 56.58%, 51.25% and 40.93 %. In the formalin stimulation test, the phase Ⅱ licking and bite time were shortened, and the inhibition rates were 56.62%, 47.03% and 33.98%, respectively. In the heat stimulation test, The analgesic effect peaked at 2 hours, and the improvement rates of pain threshold were 57.32%, 42.14% and 26.29% respectively. (2) Methyl eugenol (6,3,1.5 mg · kg -1) significantly inhibited ear swelling in mice induced by xylene, the inhibitory rates were 76.43%, 57.23% and 35.00%, respectively. (3) Blockade experiments showed that the analgesic effect of methyl eugenol (6 mg · kg -1) was inhibited by GABA_A receptor blocker bicuculline (3 mg · kg -1) Can not be blocked by naloxone, an opioid receptor blocker (3 mg · kg -1). NO test results showed that methyl eugenol (6 mg · kg -1) could inhibit the serum NO level of acetic acid induced pain in mice. Conclusions This study shows that methyl eugenol, a component of Volatile Oil, has significant analgesic and anti-inflammatory effects. The mechanism of analgesic action is related to the activation of GABAA receptor and the inhibition of NO level.