Trailović Saša M, Marjanović Djordje S, Nedeljković Trailović Jelena, Robertson Alan P, Martin Richard J
Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Belgrade, Belgrade, Serbia,
Parasitol Res. 2015 Aug;114(8):3059-68. doi: 10.1007/s00436-015-4508-x. Epub 2015 May 7.
Essential plant oils (or their active principles) are safe to use and a potentially attractive alternative to current antiparasitic drugs. In the present study, we tested the effects of carvacrol on the isolated tissues of Ascaris suum and investigated potential interactions with other antiparasitic drugs. We used somatic muscle flaps for contraction assays, as well as for electrophysiological investigations. Carvacrol 300 μM highly significantly inhibited contractions caused by 1, 3, 10, 30, and 100 μM of ACh (p = 0.0023, p = 0.0002, p = 0.0002, p < 0.0001, and p < 0.0001). The control EC50 for acetylcholine was 8.87 μM (log EC50 = 0.95 ± 0.26), while R max was 2.53 ± 0.24 g. The EC50 of acetylcholine in the presence of 300 μM of carvacrol was 27.71 μM (log EC50 = 1.44 ± 0.28) and the R max decreased to 1.63 ± 0.32 g. Furthermore, carvacrol highly significant potentiates inhibitory effect of GABA and piperazine on the contractions induced by ACh. However, carvacrol (100 and 300 μM), did not produce any changes in the membrane potential or conductance of the A. suum muscle cell. While, 300 μM of carvacrol showed a significant inhibitory effect on ACh-induced depolarization response. The mean control depolarization was 13.58 ± 0.66 mV and decreased in presence of carvacrol to 4.50 ± 1.02 mV (p < 0.0001). Mean control Δg was 0.168 ± 0.017 μS, while in the presence of 300 μM of carvacrol, Δg significantly decreased to 0.060 ± 0.018 ΔS (p = 0.0017). The inhibitory effect on contractions may be the explanation of the antinematodal potential of carvacrol. Moreover, inhibition of depolarizations caused by ACh and reduction of conductance changes directly points to an interaction with the nAChR in A. suum.
植物精油（或其活性成分）使用安全，是当前抗寄生虫药物潜在的有吸引力的替代品。在本研究中，我们测试了香芹酚对猪蛔虫离体组织的作用，并研究了其与其他抗寄生虫药物的潜在相互作用。我们使用体肌瓣进行收缩试验以及电生理研究。300μM香芹酚对由1、3、10、30和100μM乙酰胆碱引起的收缩具有高度显著的抑制作用（p = 0.0023、p = 0.0002、p = 0.0002、p <0.0001和p <0.0001）。乙酰胆碱的对照EC50为8.87μM（log EC50 = 0.95±0.26），而R max为2.53±0.24 g。在存在300μM香芹酚的情况下，乙酰胆碱的EC50为27.71μM（log EC50 = 1.44±0.28），R max降至1.63±0.32 g。此外，香芹酚高度显著地增强了γ-氨基丁酸和哌嗪对乙酰胆碱诱导的收缩的抑制作用。然而，香芹酚（100和300μM）对猪蛔虫肌细胞膜电位或电导率没有产生任何变化。同时，300μM香芹酚对乙酰胆碱诱导的去极化反应显示出显著的抑制作用。对照平均去极化值为13.58±0.66 mV，在存在香芹酚的情况下降至4.50±1.02 mV（p <0.0001）。对照平均Δg为0.168±0.017μS，而在存在300μM香芹酚的情况下，Δg显著降至0.060±0.018ΔS（p = 0.0017）。对收缩的抑制作用可能解释了香芹酚的抗线虫潜力。此外，对乙酰胆碱引起的去极化的抑制以及电导率变化的降低直接表明其与猪蛔虫中的烟碱型乙酰胆碱受体相互作用。
