da Silva-Alves Kerly Shamyra, Ferreira-da-Silva Francisco Walber, Coelho-de-Souza Andrelina Noronha, Albuquerque Aline Alice Cavalcante, do Vale Otoni Cardoso, Leal-Cardoso José Henrique
Laboratory of Electrophysiology, Superior Institute of Biomedical Sciences, State University of Ceará, Fortaleza, Ceará, Brazil.
Department of Clinical Medicine, Federal University of Ceará, Fortaleza, Ceará, Brazil.
Planta Med. 2015 Mar;81(4):292-7. doi: 10.1055/s-0034-1396309. Epub 2015 Feb 25.
Croton zehntneri is an aromatic plant native to Northeast Brazil and employed by local people to treat various diseases. The leaves of this plant have a rich content of essential oil. The essential oil of C. zehntneri samples, with anethole as the major constituent and anethole itself, have been reported to have several pharmacological activities such as antispasmodic, cardiovascular, and gastroprotective effects and inducing the blockade of neuromuscular transmission and antinociception. Since several works have demonstrated that essential oils and their constituents block cell excitability and in view of the multiple effects of C. zehntneri essential oil and anethole on biological tissues, we undertook this investigation aiming to characterize and compare the effects of this essential oil and its major constituent on nerve excitability. Sciatic nerves of Wistar rats were used. They were mounted in a moist chamber, and evoked compound action potentials were recorded. Nerves were exposed in vitro to the essential oil of C. zehntneri and anethole (0.1-1 mg/mL) up to 180 min, and alterations in excitability (rheobase and chronaxie) and conductibility (peak-to-peak amplitude and conduction velocity) parameters of the compound action potentials were evaluated. The essential oil of C. zehntneri and anethole blocked, in a concentration-dependent manner with similar pharmacological potencies (IC50: 0.32 ± 0.07 and 0.22 ± 0.11 mg/mL, respectively), rat sciatic nerve compound action potentials. Strength-duration curves for both agents were shifted upward and to the right compared to the control curve, and the rheobase and chronaxie were increased following essential oil and anethole exposure. The time courses of the essential oil of C. zehntneri and anethole effects on peak-to-peak amplitude of compound action potentials followed an exponential decay and reached a steady state. The essential oil of C. zehntneri and anethole caused a similar reduction in conduction velocities of the compound action potential waves investigated. In conclusion, we demonstrated here that the essential oil of C. zehntneri blocks neuronal excitability and that this effect, which can be predominantly attributable to its major constituent, anethole, is important since these agents have several pharmacological effects likely related to the alteration of excitability. This finding is relevant due to the use of essential oils in aromatherapy and the low acute toxicity of this agent, which exhibits other effects of potential therapeutic usefulness.
克罗顿·泽恩特纳里是一种原产于巴西东北部的芳香植物,当地居民用它来治疗各种疾病。这种植物的叶子富含精油。据报道,以茴香脑为主要成分的泽恩特纳里克罗顿精油及其主要成分茴香脑本身具有多种药理活性,如解痉、心血管和胃保护作用,以及诱导神经肌肉传递阻滞和抗伤害感受。由于多项研究表明精油及其成分会阻断细胞兴奋性,并且鉴于泽恩特纳里克罗顿精油和茴香脑对生物组织的多种作用,我们进行了这项研究,旨在表征和比较这种精油及其主要成分对神经兴奋性的影响。使用了Wistar大鼠的坐骨神经。将它们安装在潮湿的小室中,并记录诱发的复合动作电位。将神经在体外暴露于泽恩特纳里克罗顿精油和茴香脑(0.1 - 1毫克/毫升)长达180分钟,并评估复合动作电位的兴奋性(基强度和时值)和传导性(峰峰值幅度和传导速度)参数的变化。泽恩特纳里克罗顿精油和茴香脑以浓度依赖性方式阻断大鼠坐骨神经复合动作电位,且药理效力相似(IC50分别为0.32±0.07和0.22±0.11毫克/毫升)。与对照曲线相比,两种药物的强度 - 时间曲线均向上和向右移动,暴露于精油和茴香脑后基强度和时值增加。泽恩特纳里克罗顿精油和茴香脑对复合动作电位峰峰值幅度的作用时间过程呈指数衰减并达到稳定状态。泽恩特纳里克罗顿精油和茴香脑对所研究的复合动作电位波的传导速度产生了类似的降低作用。总之,我们在此证明泽恩特纳里克罗顿精油会阻断神经元兴奋性,并且这种作用主要可归因于其主要成分茴香脑,这一点很重要,因为这些药物具有多种可能与兴奋性改变相关的药理作用。由于精油在芳香疗法中的应用以及该药物的低急性毒性,且具有其他潜在治疗用途的作用,这一发现具有重要意义。