School of Pharmacy, Lanzhou University, 222 South Tianshui Road, Lanzhou, 730000, P. R. China.
Key Laboratory of New Animal Drug Project, Gansu Province, Key Laboratory of Veterinary Pharmaceutical Development of Ministry of Agriculture, Lanzhou Institute of Husbandry and Pharmaceutical Sciences, Chinese Academy of Agricultural Sciences, 335 Jiangouyan, Lanzhou, 730050, P. R. China.
Sci Rep. 2018 Jan 25;8(1):1609. doi: 10.1038/s41598-018-19964-0.
As important secondary plant metabolites, naphthoquinones exhibit a wide range of biological activities. However, their potential as sustainable alternatives to synthetic acaricides has not been studied. This study for the first time investigates the acaricidal activity of naphthoquinones against Psoroptes cuniculi in vitro. Furthermore, the in vivo activity, the skin irritation effects, the cytotoxicity and the inhibitory activities against mite acetylcholinesterase (AChE) and glutathione S-transferase (GST) of the two compounds that displayed the best insecticidal activity in vitro were evaluated. Among fourteen naphthoquinones and their analogs, juglone and plumbagin were observed to possess the strongest acaricidal activities against P. cuniculi with LC values of 20.53 ppm and 17.96 ppm, respectively, at 24 h. After three treatments, these two chemicals completely cured naturally infested rabbits in vivo within 15 days, and no skin irritation was found in any of the treated rabbits. Compared to plumbagin, juglone presented no or weak cytotoxicity against HL-7702 cells. Moreover, these two chemicals significantly inhibited AChE and GST activity. These results indicate that juglone has promising toxicity against P. cuniculi, is safe for both humans and animals at certain doses, and could be used as a potential alternative bio-acaricide for controlling the development of psoroptic mange in agricultural applications.
作为重要的次生植物代谢物,萘醌类化合物表现出广泛的生物活性。然而,它们作为可持续替代合成杀螨剂的潜力尚未得到研究。本研究首次调查了萘醌类化合物对兔耳痒螨(Psoroptes cuniculi)的体外杀螨活性。此外,还评估了两种在体外表现出最佳杀虫活性的化合物在体内的活性、皮肤刺激性、细胞毒性以及对螨乙酰胆碱酯酶(AChE)和谷胱甘肽 S-转移酶(GST)的抑制活性。在 14 种萘醌及其类似物中,胡桃醌和铅丹表现出对兔耳痒螨最强的杀螨活性,在 24 小时时 LC 值分别为 20.53 ppm 和 17.96 ppm。经过三次处理,这两种化学物质在 15 天内完全治愈了体内自然感染的兔子,并且在任何处理过的兔子中都没有发现皮肤刺激。与铅丹相比,胡桃醌对 HL-7702 细胞没有或仅有较弱的细胞毒性。此外,这两种化学物质还显著抑制了 AChE 和 GST 的活性。这些结果表明,胡桃醌对兔耳痒螨具有有前景的毒性,在一定剂量下对人和动物都是安全的,可作为农业应用中控制痒螨病发展的潜在替代生物杀螨剂。