Acaricidal activity of strophanthidin derivatives against Psoroptes cuniculi and their inhibitory effect on Na+-K+-ATPase

文献类型： 外文期刊

第一作者： Shang, Xiao-Fei

作者： Shang, Xiao-Fei;Miao, Xiao-Lou;Dai, Li-Xia;Wang, Yu;Li, Bing;Pan, Hu;Zhang, Ji-Yu

作者机构：

关键词： Strophanthidin derivatives; Acaricidal activity; Synthesis; Na+-K+-ATPase

期刊名称：VETERINARY PARASITOLOGY （ 影响因子：2.738； 五年影响因子：2.951 ）

ISSN： 0304-4017

年卷期： 2021 年 296 卷

页码：

收录情况： SCI

摘要： In our previous studies, we found that as the active gradients of Adonis coerulea, cardenolides and cardiac glycosides presented toxicity against mites by inhibiting Na+-K+-ATPase. In this paper, after evaluating the acaricidal activity of the commercial cardiac aglycones/glycosides, serials of novel strophanthidin derivatives were designed and synthesized with an efficient and simple route under mild conditions, and their toxicity against mites, the cytotoxicity and inhibitory effect on Na+-K+-ATP enzyme in PC12 cells were investigated. Results showed among of all compounds, including 9 commercial agent and 32 synthesized strophanthidin derivatives, QXG-1 presented the strongest toxicity against mites with the LC(50 )value of 320.0 mu g/mL. C-19 group of strophanthidin substituted with glycinemethylester would increase the toxicity against mites, and the hydroxyl group at C-5 play the vital role in terms of the toxicity. At the given concentration, QXG-1 displayed the safety against PC12 (10.0 mu g/mL) in vitro and mice (3.2 mg/kg) in acute toxicity test, and strong inhibitory effect on Na+-K+-ATPase. It could be used as a promising acaricidal agent. This study lays the foundation to develop of QXG-1 as a relatively safe and alternative acaricidal agent.

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