鬼臼毒素类物质生物活性的研究  

Bioactivity of several podophyllotoxin analogues

作　　者：刘艳青[1] 张守刚[1] 程洁[1] 肖杭[1] 高蓉[1] 

机构地区：[1]南京医科大学应用毒理研究所神经毒理室,江苏南京210029

出　　处：《医学研究生学报》2006年第3期205-209,共5页Journal of Medical Postgraduates

基　　金：国家自然科学基金资助项目(批准号:30371169);江苏省普通高校自然科学研究计划基金资助项目(批准号:02KJA330001)

摘　　要：目的:研究脱氧鬼臼毒素、β-阿朴苦鬼臼、鬼臼毒素和4′-去甲鬼臼毒素共四种鬼臼毒素类似物对3龄初淡色库蚊幼虫和5龄初菜青虫的毒杀和抑制生长发育活性。方法:采用WHO生物测试法和小叶碟添加法分别测定四种类似物对淡色库蚊和菜青虫的毒杀和拒食活性。结果:①脱氧鬼臼毒素和β-阿朴苦鬼臼对淡色库蚊的毒杀作用较明显,致死中浓度(LC50)分别是0.001 48和0.001 68 g/L。②四种化合物对淡色库蚊的生长发育有明显的抑制作用,与对照组相比,加药组的化蛹率相对较低。③脱氧鬼臼毒素、β-阿朴苦鬼臼和鬼臼毒素对菜青虫有毒杀作用,96 h的LC50分别是0.045 4、0.078 2和0.159 7 g/L。4′-去甲鬼臼毒素对菜青虫的毒杀活性很弱。④四种化合物对菜青虫都有拒食活性,但前三种拒食活性较强,其拒食中浓度(AFC50)分别是0.016 1、0.018 7、0.039 4和0.273 9 g/L。⑤四种化合物对菜青虫都有不同程度的抑制其生长发育现象,但作用的程度和方式不同,脱氧鬼臼毒素组的试虫全部死于5龄期,β-阿朴苦鬼臼毒素和鬼臼毒素的高浓度组不能化蛹,死于幼虫期,而4′-去甲鬼臼毒素组的试虫则表现出畸蛹等现象。结论:四种鬼臼毒素类似物对淡色库蚊和菜青虫毒杀和抑制生长发育活性之间的差异可能与结构上的差异有关。Objective： The bioactivity of four podophyllotoxin analogues were tested against 3rd instar larvae of Culex pipiens pallens and 5 h instar larvae of Pieris rapae L. Methods ： WHO bioassay and leafdipping method. Results： ①Deoxypodophyllotoxin and β-apopicropodophyllotoxin exhibited toxicity against Culex pipiens pallens, and their LC50 were 0.001 48 and 0. 001 68 g/L , respectively. ②All the four podophyllotoxin analogues displayed inhibitory effect on the growth and development against Culex pipiens pallens, their pupation rates were delayed comparing with control. ③Deoxypodophyllotoxin, β-apopicropodophyllotoxin and Podophyllotoxin exhibited toxicity against Pieris rapae L, the LC50 96 h after treatment were 0.045 4,0.078 2 and 0. 159 7 g/L , respectively. ④All the four podophyllotoxin analogues showed antifeedant activity against Pieris rapae L, their AFC50 were 0. 016 1,0. 018 7,0. 039 4 and 0.273 9 g/L, respectively.⑤All four podophyllotoxin analogues displayed inhibitory effect on the growth and development against Pieris rapae L, but the extent of each compound were very different. Conclusion： Based on the data obtained in this investigation, it is possible that the dissimilarity in the structure of the analogues leads to their different bioactivity.

关 键 词：鬼臼毒素类似物 淡色库蚊 菜青虫 植物源杀虫剂 

分 类 号：R979.1[医药卫生—药品] R318.08[医药卫生—药学]