麻叶千里光果实中的季铵苯并[c]菲啶生物碱（QBAs）对湖北钉螺的杀螺活性和生理毒性。
Molluscicidal activity and physiological toxicity of quaternary benzo[c]phenanthridine alkaloids (QBAs) from Macleaya cordata fruits on Oncomelania hupensis.
机构信息
Green Resources Transformation and Collaborative Innovation Center, and State Key Laboratory of Biocatalysis and Enzyme Engineering, School of Life Science, Hubei University, Wuhan, PR China.
The First Affiliated Hospital of Huanghuai University, Zhumadian, PR China.
出版信息
PLoS Negl Trop Dis. 2019 Oct 11;13(10):e0007740. doi: 10.1371/journal.pntd.0007740. eCollection 2019 Oct.
Schistosomiasis is a serious worldwide parasitic disease. One of the best ways to control schistosomiasis is to control the population of Oncomelania hupensis snails. We sought to identify a high-efficiency biogenic molluscicide against Oncomelania with low toxicity, to avoid chemical molluscicide contamination and toxicity in aquatic organisms. We extracted quaternary benzo[c]phenanthridine alkaloids (QBAs) from Macleaya cordata fruits. Molluscicidal activity of the QBAs against Oncomelania was determined using bioassay. Our results showed that the extracted QBAs had a strong molluscicidal effect. In treatment of O. hupensis with QBAs for 48 h and 72 h, the lethal concentration (LC50) was 2.89 mg/L and 1.29 mg/L, respectively. The molluscicidal activity of QBAs was close to that of niclosamide (ethanolamine salt), indicating that QBAs have potential development value as novel biogenic molluscicides. We also analyzed physiological toxicity mechanisms by examining the activity of several important detoxification enzymes. We measured the effect of the extracted QBAs on the activities of glutathione S-transferase (GST), carboxylesterase (CarE), acid phosphatase (ACP), and alkaline phosphatase (AKP) in the liver of O. hupensis. We found that the effects of QBAs on detoxification metabolism in O. hupensis were time and concentration dependent. The activities of GST, CarE, AKP, and ACP in the liver of snails increased significantly in the early stage of treatment (24 h), but decreased sharply in later stages (120 h), compared with these activities in controls. GST, CarE, AKP, and ACP activity in the liver of snails treated with LC50 QBAs for 120 h decreased by 62.3%, 78.1%, 59.2%, and 68.6%, respectively. Our results indicate that these enzymes were seriously inhibited by the extracted QBAs and the detoxification and metabolic functions of the liver gradually weakened, leading to poisoning, which could be the main cause of death in O. hupensis snails.
血吸虫病是一种严重的全球性寄生虫病。控制日本血吸虫病的最佳方法之一是控制钉螺的种群。我们试图寻找一种高效、低毒的生物源杀螺剂，以避免化学杀螺剂对水生生物的污染和毒性。我们从博落回果实中提取了季铵型苯并[c]菲啶生物碱（QBAs）。采用生物测定法测定 QBAs 对钉螺的杀螺活性。结果表明，提取的 QBAs 具有很强的杀螺活性。在 QBAs 处理钉螺 48 h 和 72 h 时，其致死浓度（LC50）分别为 2.89 mg/L 和 1.29 mg/L。QBAs 的杀螺活性与氯硝柳胺（乙醇胺盐）相近，表明 QBAs 具有作为新型生物源杀螺剂的潜在开发价值。我们还通过检测几种重要解毒酶的活性来分析生理毒性机制。我们测定了提取的 QBAs 对钉螺肝脏谷胱甘肽 S-转移酶（GST）、羧酸酯酶（CarE）、酸性磷酸酶（ACP）和碱性磷酸酶（AKP）活性的影响。结果发现，QBAs 对钉螺解毒代谢的影响具有时间和浓度依赖性。在处理早期（24 h），钉螺肝脏 GST、CarE、AKP 和 ACP 活性显著升高，但在后期（120 h）急剧下降，与对照组相比差异显著。用 LC50 QBAs 处理 120 h 的钉螺肝脏 GST、CarE、AKP 和 ACP 活性分别下降 62.3%、78.1%、59.2%和 68.6%。结果表明，这些酶被提取的 QBAs 严重抑制，肝脏的解毒和代谢功能逐渐减弱，导致中毒，这可能是钉螺死亡的主要原因。
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