Laboratorio de Neurofarmacología de Productos Naturales, Dirección de Investigaciones en Neurociencias, Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz, Ciudad de México 14370, Mexico.
Laboratorio de Neurociencias, Instituto Nacional de Pediatría, Ciudad de México 04530, Mexico.
Molecules. 2020 Feb 5;25(3):675. doi: 10.3390/molecules25030675.
Cav. (Asteraceae) is an ancient medicinal plant commonly used to alleviate pain. Nevertheless, scientific studies validating this property are lacking in the literature. Animal models of pain were used to evaluate the antinociceptive and anti-inflammatory activities of essential oil (TLEO) and a bioactive metabolite. The chemical constitution and possible toxicity of the extract and the mechanism of action of β-caryophyllene were also explored. Temporal course curves and dose-response graphics were generated using TLEO (0.1-10 mg/kg or 3.16-31.62 mg/kg) and β-caryophyllene (3.16-10 mg/kg). Metamizole (80 mg/kg) and indomethacin (20 mg/kg) were used as reference drugs in the formalin assay and writhing test in rats and mice, respectively. The β-caryophyllene mechanism of action was explored in the presence of naloxone (1 mg/kg), flumazenil (10 mg/kg), WAY100635 (0.16 mg/kg), or nitro-l-arginine methyl ester (L-NAME) (20 mg/kg) in the formalin test in rats. GC/MS analysis demonstrated the presence of geranyl acetate (49.89%), geraniol (7.92%), and β-caryophyllene (6.27%). Significant and dose-dependent antinociceptive response was produced by TLEO and β-caryophyllene without the presence of gastric damage. In conclusion, β-caryophyllene was confirmed as a bioactive compound in the analgesic properties by involving the participation of receptors like opioids, benzodiazepines, and Serotonin 1A receptor (5-HT), as well as nitric oxide.
缬草（菊科）是一种古老的药用植物，常用于缓解疼痛。然而，文献中缺乏验证这种特性的科学研究。使用动物疼痛模型来评估精油（TLEO）和一种生物活性代谢物的镇痛和抗炎活性。还探索了提取物的化学组成和可能的毒性以及β-石竹烯的作用机制。使用 TLEO（0.1-10 mg/kg 或 3.16-31.62 mg/kg）和β-石竹烯（3.16-10 mg/kg）生成时间过程曲线和剂量-反应图。在大鼠和小鼠的福尔马林试验和扭体试验中，分别使用甲灭酸（80 mg/kg）和吲哚美辛（20 mg/kg）作为参考药物。在大鼠福尔马林试验中，在纳洛酮（1 mg/kg）、氟马西尼（10 mg/kg）、WAY100635（0.16 mg/kg）或硝基-L-精氨酸甲酯（L-NAME）（20 mg/kg）存在的情况下，探索了β-石竹烯的作用机制。GC/MS 分析表明存在乙酸香叶酯（49.89%）、香叶醇（7.92%）和β-石竹烯（6.27%）。TLEO 和 β-石竹烯产生了显著的、剂量依赖性的镇痛反应，而没有胃损伤的发生。综上所述，β-石竹烯被确认为具有镇痛作用的生物活性化合物，涉及到阿片受体、苯二氮䓬受体和 5-羟色胺 1A 受体（5-HT）以及一氧化氮等受体的参与。
