Stojković Maja, Marjanović Djordje S, Medić Dragana, Charvet Claude L, Trailović Saša M
Department of Pharmacology, Clinical Pharmacology and Toxicology, Faculty of Medicine, University of Belgrade, 11000 Belgrade, Serbia.
Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Belgrade, 11000 Belgrade, Serbia.
Pharmaceuticals (Basel). 2025 Aug 20;18(8):1232. doi: 10.3390/ph18081232.
The active ingredients of essential plant oils appear as potentially effective antinematodal drugs or substances that can potentiate the action of already-existing anthelmintics. So far, we have verified that, aside from the direct effect on the neuromuscular system of nematodes, some of them can potentiate the effects of drugs that are agonists or antagonists of nematode cholinergic receptors. In this study, the antinematodal effects of geraniol and carvacrol were compared, as well as their interaction in the experimental model , on the contractile properties of neuromuscular preparations and on the ACR-16 nicotinic acetylcholine receptor (nAChR) of expressed in Xenopus leavis oocytes. The combination of geraniol and carvacrol showed a synergistic nematocidal effect in the tests on , reducing the value of individual LC by almost 10-times. This combination also exerted a synergistic inhibitory effect on the contractions of , significantly increased the EC of ACh and reduced the maximal contractile effect. The synergistic interaction of these two monoterpenes on Asu-ACR-16 nAChR expressed in Xenopus oocytes resulted in a significant decrease in the maximum current, while the ACh EC value remained unchanged. Our findings provide a better understanding of the mode of action of monoterpene plant compounds. The possible antiparasitic application of active ingredients of essential plant oils that exhibit a synergistic anthelmintic effect represents an important basis for the development of new drugs and new therapeutic procedures.
植物精油的活性成分似乎是潜在有效的抗线虫药物或可增强现有驱虫药作用的物质。到目前为止,我们已经证实,除了对线虫神经肌肉系统有直接作用外,其中一些还能增强作为线虫胆碱能受体激动剂或拮抗剂的药物的作用。在本研究中,比较了香叶醇和香芹酚的抗线虫作用,以及它们在实验模型中对神经肌肉制剂收缩特性和非洲爪蟾卵母细胞中表达的ACR - 16烟碱型乙酰胆碱受体(nAChR)的相互作用。香叶醇和香芹酚的组合在对[具体对象未明确]的测试中显示出协同杀线虫作用,使个体LC值降低了近10倍。这种组合对[具体对象未明确]的收缩也产生了协同抑制作用,显著增加了乙酰胆碱的EC值并降低了最大收缩效应。这两种单萜在非洲爪蟾卵母细胞中表达的Asu - ACR - 16 nAChR上的协同相互作用导致最大电流显著降低,而乙酰胆碱EC值保持不变。我们的研究结果有助于更好地理解单萜类植物化合物的作用模式。具有协同驱虫作用的植物精油活性成分的可能抗寄生虫应用是开发新药和新治疗方法的重要基础。