除虫菊酯和拟除虫菊酯的毒理作用和药效

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	除虫菊酯和拟除虫菊酯的毒理作用和药效
	刘子超
学位类型	硕士
导师	梁醒财
	2007-06
学位授予单位	中国科学院研究生院
学位授予地点	北京
学位专业	动物学
关键词	除虫菊酯拟除虫菊酯增效醚迷迭香突触体 Atp酶
其他摘要	除虫菊酯是新型植物源农药，由于其具有杀虫谱广，杀虫活性高，对哺乳动物毒性低等优点而被广泛地应用于室内卫生昆虫防治。拟除虫菊酯是人工合成的除虫菊酯的结构类似物。由于人们在使用过程中不可避免地会接触除虫菊酯类药物，对其进行毒理学研究显得尤为重要。本论文以雄性Sprague-Dawley大鼠为材料，研究了除虫菊酯、氯氰菊酯、增效醚（PBO）和迷迭香对大鼠大脑突触体ATP酶活性的影响。采用Percoll梯度离心法分离出大脑突触体，通过测定ATP酶催化ATP产生的无机磷量测定ATP酶的活性。结果：总ATP酶和Mg2+-ATP酶在10 μM除虫菊酯作用下的活性分别为80.3％和45.9％，当除虫菊酯浓度上升到100 μM时，活性分别下降到5.4％和6.2％；总ATP酶在100 μM氯氰菊酯作用下活性为80.7％，氯氰菊酯浓度上升到1000 μM时，活性下降到2.3％；在3000 μM PBO作用下，总ATP酶活性为79.9％，相同浓度的迷迭香能使总ATP酶活性下降到66.8％；当有3倍浓度PBO存在时，10 μM除虫菊酯降低总ATP酶活性至37.8％，100 μM氯氰菊酯降低总ATP酶活性到28.5％；有3倍浓度迷迭香存在时，10 μM除虫菊酯降低总ATP酶活性到72.9％，100 μM氯氰菊酯降低总ATP酶活性至43.0％。结论：除虫菊酯和氯氰菊酯在适当浓度下都能显著抑制总ATP酶和Mg2+-ATP酶的活性。除虫菊酯的抑制作用比氯氰菊酯显著，除虫菊酯类药物对Mg2+-ATP酶活性抑制比对总ATP酶活性的抑制显著。增效剂PBO能有效增强除虫菊酯和氯氰菊酯对突触体ATP酶活性的抑制作用。在极高浓度下，PBO单独也能部分抑制ATP酶的活性。迷迭香本身只在极高浓度下才对ATP酶起部分抑制作用，但是能轻微增强除虫菊酯和氯氰菊酯的抑制活性，这可能与其延迟除虫菊酯和氯氰菊酯被氧化有关。本研究结果表明，除虫菊酯只在浓度 > 1 μM时才会对ATP酶起显著的抑制作用(p < 0.05)，但是前人研究表明除虫菊酯在0.01 μM下即能有效改变昆虫钠离子通道动力学，可见，除虫菊酯类药物在0.01－1 μM浓度下既能有效杀灭害虫，又对人畜安全，这一结论可用于指导除虫菊酯类药物的使用。此外，本研究还测定了云菊5％除虫菊酯乳油对东亚飞蝗四龄和五龄若虫的室内药效实验，结果表明除虫菊酯能有效杀灭东亚飞蝗，适用于东亚飞蝗防治。; Pyrethrins, which are widely used in households, are natural insecticides, originated from plants, with broad spectrum, high insecticidal potencies, and low mammalian toxicities. Pyrethroids are synthesized analogs of pyrethrins. Because of the inevitably exposure to pyrethrins and their analogs while using these pesticides, studies on their toxicology are of great importance. In this study, the effect of pyrethrins, cypermethrin, piperonyl butoxide (PBO) and rosemary on the ATPase activities of Sprague-Dawley rat cerebral synaptosome, which was isolated by Percoll gradient method was tested. ATPase activities were analyzed by determining the amount of inorganic phosphate. The results showed that the activities of total ATPase and Mg2+-ATPase were 80.3% and 45.9% in 10 μM pyrethrins and decreased to 5.4% and 6.2% respectively with the concentration rising to 100 μM. The total ATPase activities were 80.7% and 2.3% in 100 μM and 1000 μM cypermethrin respectively. And 3000 μM PBO and rosemary made a decrease of total ATPase activities to 79.9% and 66.8% respectively. In the presence of tripled concentration of PBO, 10 μM of pyrethrins caused the total ATPase activity down to 37.8% and 100 μM of cypermethrin caused that down to 28.5%. In the presence of tripled concentration of rosemary, 10 μM of pyrethrins caused the total ATPase activity down 72.9% and 100 μM of cypermethrin caused that down to 43.0%. The following conclusions are made: pyrethrins and cypermethrin in proper concentration can markedly inhibit both total ATPase and Mg2+-ATPase activities. Synergist PBO can potentiate the inhibiting effect of both pyrethrins and cypermethrin on the activities of synaptosomal ATPase. And at concentration high enough, PBO alone can also inhibit synaptosomal ATPase activity to some extent. Rosemary can inhibit synaptosomal ATPase acticity in part only at very high concentration. And it also potentiates the inhibiting effect of both pyrethrins and cypermethrin on the activities of synaptosomal ATPase slightly. This phenomenon may result from the degradation delay of pyrethrins and their analogs at the presence of rosemary. The present study also suggested that pyrethrins inhibit ATPase activities dramatically (p < 0.05) only at concentration of > 1 μM. However, previous study showed that 0.01 μM pyrethroid can change the kinetics of voltage-sensitive sodium channels effectively. This means that 0.01 - 1 μM of pyrethroids can not only control pests effectively but also be secure to human. This conclusion can guide the usage of pyrethrins and their analogs. Besides, we studied the laboratory toxicity of Yunju pyrethrins emulsifable concentrate (5%) to the 4th and the 5th instars of Locusta migratoria. The results indicates that pyrethrins are suitable to control locusts.
语种	中文
文献类型	学位论文
条目标识符	http://ir.kiz.ac.cn/handle/152453/11018
专题	其他
作者单位	中国科学院昆明动物研究所
推荐引用方式 GB/T 7714	刘子超. 除虫菊酯和拟除虫菊酯的毒理作用和药效[D]. 北京. 中国科学院研究生院,2007.

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