光活化多炔类化合物对蚊幼虫的毒力  

Phototoxicity of synthetic polyacetylenes against mosquito larvae (Culex quinquefasciatus)

作　　者：万树青[1] 徐汉虹[1] 赵善欢[1] 尚稚珍[2] 刘准[2] 

机构地区：[1]华南农业大学昆虫毒理研究室,广州510642 [2]南开大学元素所有机化学国家重点实验室,天津300071

出　　处：《昆虫学报》2000年第3期264-270,共7页Acta Entomologica Sinica

基　　金：国家自然科学基金项目!(39870 437);南开大学元素有机化学所国家重点实验室资助课题

摘　　要：采用自制的光活化实验装置 ,测定了 11个合成的多炔类化合物对致倦库蚊Culexquinque fasciatus 4龄幼虫的光活化毒力 ,发现部分化合物在近紫外光照射条件下 ,能明显地提高光活化毒杀效应 ,测得化合物 5(1 苯基 4 (3,4 亚甲基二氧 )苯基 丁二炔 )光照与未光照处理LC50 分别是0 35μg/mL和 8 89μg/mL。实验中发现蚊虫先接触药后 ,再进行光照处理 ,才能较好地发挥毒效 ,而且毒杀效应与光照时间呈正相关。模拟田间试验表明 ,太阳光能显著提高化合物 5毒杀蚊幼虫的药效。利用抗氧化剂进行猝灭作用试验 ,间接地证明化合物 5的光活毒杀机理是与过氧化作用有关。分析结构与活性关系 ,发现二苯基 丁二炔衍生物比二烷基取代丁二炔活性高 ,苯基上不同取代基也影响光活毒杀效果 ,它们的活性顺序是 :亚甲基二氧基 >甲氧基 >邻硝基 >间硝基>Eleven new synthetic polyacetylenes were screened for their biological activity to the 4th instar larvae of the mosquito Culex quinquefasciatus . The toxicities of some compounds to the tested insects were found to be enhanced greatly by irradiation with near\|UV. Compound 5 (1\|phenyl\|4\|(3,4\|methylenedioxy)\|phenyl\|diacetylene) is an effective photosensitizer,of which LC 50 +UV\|A (in the presence of UV\|A) and LC 50 -UV\|A(in the absence of UV\|A) to the larvae were 0 35 μg/mL and 8 89 μg/mL respectively.The ratio of photoactivity [(LC 50 -UV\|A)/(LC 50 +UV\|A)] was 25 65. The results in simulated field experiment showed the phototoxicity of compound 5 also was enhanced greatly to the tested larvae by sunlight. The mortality of presence and absence of sunlight were 81 63 and 11 40 percent respectively. The result of preliminary experiment by adding different kinds of antioxidants showed the compound 5 belongs to the type of yielding superoxygen radical in organism and it differs from α terthienyl (α T) in the mechanism of photodynamic action. The analysis of structure\|bioactivity shows that diacetylene of biphenyl\|containing derivatives has higher activity in photoxicity than diacetylene of bialkyl substitute. Different substitutes on phenyl also affect its effect,the order in activity is methylene dioxy>methoxy>o\|nitro>m\|nitro>methyl ester.

关 键 词：多炔类化合物 致倦库蚊 光活毒杀作用 构效关系 

分 类 号：R184.31[医药卫生—流行病学]