Sousa D G, Sousa S D G, Silva R E R, Silva-Alves K S, Ferreira-da-Silva F W, Kerntopf M R, Menezes I R A, Leal-Cardoso J H, Barbosa R
Laboratório de Fisiofarmacologia das Células Excitáveis, Universidade Regional do Cariri, Crato, CE, Brasil.
Laboratório de Eletrofisiologia, Instituto Superior de Ciências Biomédicas, Universidade Estadual do Ceará, Fortaleza, CE, Brasil.
Braz J Med Biol Res. 2015 Aug;48(8):697-702. doi: 10.1590/1414-431X20154710. Epub 2015 Jun 30.
Lippia alba is empirically used for infusions, teas, macerates, and hydroalcoholic extracts because of its antispasmodic, analgesic, sedative, and anxiolytic effects. Citral is a mixture of trans-geranial and cis-neral and is the main constituent of L. alba essential oil and possesses analgesic, anxiolytic, anticonvulsant, and sedative effects. The present study evaluated the effects of the essential oil of L. alba (EOLa) and citral on compound action potentials (CAPs) in Wistar rat sciatic nerves. Both drugs inhibited CAP in a concentration-dependent manner. The calculated half-maximal inhibitory concentrations (IC50) of peak-to-peak amplitude were 53.2 µg/mL and 35.00 µg/mL (or 230 µM) for EOLa and citral, respectively. Peak-to-peak amplitude of the CAP was significantly reduced by 30 µg/mL EOLa and 10 µg/mL citral. EOLa and citral (at 60 and 30 µg/mL, values close to their respective IC50 for CAP blockade) significantly increased chronaxy and rheobase. The conduction velocity of the first and second CAP components was statistically reduced to ∼86% of control with 10 µg/mL EOLa and ∼90% of control with 3 µg/mL citral. This study showed that EOLa inhibited nerve excitability and this effect can be explained by the presence of citral in its composition. Both EOLa and citral showed inhibitory actions at lower concentrations compared with other essential oils and constituents with local anesthetic activity. In conclusion, these data demonstrate that EOLa and citral are promising agents in the development of new drugs with local anesthetic activity.
由于具有解痉、镇痛、镇静和抗焦虑作用,白香蜂草在经验上被用于制作浸剂、茶、浸渍液和水醇提取物。柠檬醛是反式香叶醛和顺式橙花醛的混合物,是白香蜂草精油的主要成分,具有镇痛、抗焦虑、抗惊厥和镇静作用。本研究评估了白香蜂草精油(EOLa)和柠檬醛对Wistar大鼠坐骨神经复合动作电位(CAPs)的影响。两种药物均以浓度依赖性方式抑制CAP。EOLa和柠檬醛的峰峰值幅度计算得出的半数最大抑制浓度(IC50)分别为53.2 µg/mL和35.00 µg/mL(或230 µM)。30 µg/mL的EOLa和10 µg/mL的柠檬醛可使CAP的峰峰值幅度显著降低。EOLa和柠檬醛(分别为60和30 µg/mL,接近其各自阻断CAP的IC50值)显著增加时值和基强度。10 µg/mL的EOLa使第一和第二CAP成分的传导速度统计学上降至对照的约86%,3 µg/mL的柠檬醛使其降至对照的约90%。本研究表明,EOLa抑制神经兴奋性,这种作用可由其成分中存在柠檬醛来解释。与其他具有局部麻醉活性的精油和成分相比,EOLa和柠檬醛在较低浓度下均表现出抑制作用。总之,这些数据表明,EOLa和柠檬醛在开发具有局部麻醉活性的新药方面是有前景的药物。