Shang Xiao-Fei, Dai Li-Xia, Liu Ying-Qian, Zhao Zhong-Min, Li Jun-Cai, Yang Guan-Zhou, Yang Cheng-Jie
School of Pharmacy, Lanzhou University, Lanzhou 730000, PR China; Key Laboratory of Veterinary Pharmaceutical Development of Ministry of Agriculture, Key Laboratory of New Animal Drug Project, Gansu Province, Lanzhou Institute of Husbandry and Pharmaceutical Sciences, Chinese Academy of Agricultural Sciences, Lanzhou 730050, PR China.
Key Laboratory of Veterinary Pharmaceutical Development of Ministry of Agriculture, Key Laboratory of New Animal Drug Project, Gansu Province, Lanzhou Institute of Husbandry and Pharmaceutical Sciences, Chinese Academy of Agricultural Sciences, Lanzhou 730050, PR China.
Vet Parasitol. 2019 Mar;267:54-59. doi: 10.1016/j.vetpar.2019.01.013. Epub 2019 Feb 12.
Plant essential oils and its chemical compositions are commonly applied in medicinal and other industries due to their broad advanced pharmacological activities. In the present study, we systematically evaluated the acaricidal activities of twelve compounds of essential oils against Psoroptes cuniculi in vitro and in vivo. In addition, to support the clinic uses, their toxicities against immortalized human keratinocytes (HaCaT) and human liver cells (HL-7702) and skin irritation were studied for evaluating the liver and skin safety. The possible mechanism of action of certain chemical were investigated by determining the inhibitory activities against cytochrome P450 (P450) acetylcholinesterase (AChE) and glutathione-S-transferase (GST). Among all tested compounds, eugenol exhibited the best acaricidal activity with LC value of 56.61 μg/ml in vitro. Meanwhile, after the treatment of eugenol for five times within 10 days, the P. cuniculi were eliminated in the naturally infested rabbits, no skin irritation was found in rabbits treated by eugenol. Moreover, eugenol presented no or weak cytotoxicity against HaCaT cells and HL-7702 cells with IC values of greater than 100 μg/ml. Furthermore, the moderate inhibitory activities of eugenol against mites P450 and AChE were demonstrated. Above results indicated that eugenol presented the promising acaricidal activity against P. cuniculi in vitro and in vivo, is safe for both humans and animals at the given doses. This work lays the foundation for the development of eugenol as an environmentally friendly acaricide agent.
植物精油及其化学成分因其广泛的先进药理活性而常用于医药和其他行业。在本研究中，我们系统地评估了12种精油化合物对兔痒螨的体内外杀螨活性。此外，为支持临床应用，研究了它们对永生化人角质形成细胞（HaCaT）和人肝细胞（HL-7702）的毒性以及皮肤刺激性，以评估肝脏和皮肤安全性。通过测定对细胞色素P450（P450）、乙酰胆碱酯酶（AChE）和谷胱甘肽 - S - 转移酶（GST）的抑制活性，研究了某些化学物质可能的作用机制。在所有测试化合物中，丁香酚表现出最佳的杀螨活性，体外LC值为56.61μg/ml。同时，在10天内用丁香酚处理5次后，自然感染的兔子体内的兔痒螨被清除，用丁香酚处理的兔子未发现皮肤刺激。此外，丁香酚对HaCaT细胞和HL-7702细胞无细胞毒性或细胞毒性较弱，IC值大于100μg/ml。此外，丁香酚对螨的P450和AChE具有中等抑制活性。上述结果表明，丁香酚在体内外对兔痒螨均具有良好的杀螨活性，在给定剂量下对人和动物均安全。这项工作为丁香酚作为一种环境友好型杀螨剂的开发奠定了基础。
