作 者：
万树青;徐汉虹;赵善欢;蒋志胜;尚稚珍;刘准
单 位：
华南农业大学;南开大学元素有机化学研究所
关键词：
多炔类化合物;美洲大蠊;触杀活性;Na+-K+-ATPase;Ca2+-Mg2+-ATPase
摘 要：
采用药膜法测定了人工合成的11个多炔类化合物对美洲大蠊Periplanetaamericana初孵若虫的触杀活性。结果表明,当化合物处理浓度为20μg/cm2时,致死率达70%以上的有:化合物2(1-叔丁基-4-羟甲基-丁二炔)、化合物9(1-苯甲基-4-甲基-丁二炔)和化合物10(O-炔丙基硫代磷酸二乙酯)。经毒力测定,化合物9和化合物10的LC50分别为3.91μg/cm2和1.50μg/cm2。化合物2、化合物7(1-苯基-4-邻硝基苯基-丁二炔)和化合物10对美洲大蠊乙酰胆碱酯酶(AChE)具有抑制活性,抑制率分别为12.00%、27.24%和62.22%。化合物2和化合物10对Na+-K+-ATPase具有抑制活性,抑制率分别为44.55%和31.44%;而化合物5(1-苯基-4-(3,4-亚甲基二氧)苯基-丁二炔)和化合物6(1-苯基-4-间硝基苯基-丁二炔)对该酶具有激活活性,激活率分别为24.98%和20.99%。化合物2、化合物4(1-苯基-4-对甲氧基苯基-丁二炔)和化合物7对Ca2+-Mg2+-ATPase具有抑制活性,抑制率分别为49.02%、38.53%和35.32%,其他化合物对该酶具有激活活性,其中激活活性最高的为化合物5,激活率达81.12%。
译 名：
Contact toxicity of polyacetylenes to Periplaneta americana and their effects on AChE and ATPase
作 者：
WAN Shu-Qing~1, XU Han-Hong~1, ZHAO Shan-Huan~1, JIANG Zhi-Sheng~2, SHANG Zhi-Zhen~2, LIU Zhun~2?(1. Key Laboratory of Pesticide, Chemical Biology of Educational Ministry, South China Agricultural University, Guangzhou 510642, China; 2. Institute of Element-Organic Chemistry, Nankai University, Tianjin 300071, China)
关键词：
Polyacetylenes; Periplaneta americana; contact toxicity; AChE; Na~+-K~+-ATPase; Ca~(2+)-Mg~(2+)-ATPase
摘 要：
The contact toxicity of 11 synthetic polyacetylenes was tested to newly-hatched Periplaneta americana larvae with the method of drug film. The results showed these compounds, 1-t-butyl-4-hydroxymethyl-diacetylene, 1-benzyl-4-methyl-diacetylene and di-ethyl-2-propargyl-thiophosphate caused high mortality of over 70% to the larvae at 20 μg/cm~2. The LC(50) of 1-benzyl-4-methyl-diacetylene and di-ethyl-2-propargyl-thiophosphate was 3.91 μg/cm~2 and 1.50 μg/cm~2, respectively. The effect on AChE of the insect indicated that 1-t-butyl-4-hydroxymethyl-diacetylene, 1-phenyl-4-o-nitrophenyl-diacetylene and di-ethyl-2-propargyl-thiophosphate inhibited its activity, and the inhibition rate was 12.00%, 27.24% and 62.22%, respectively. To ATPase, 1-t-butyl-4-hydroxymethyl-diacetylene and di-ethyl-2-propargyl-thiophosphate inhibited the activity of Na~+-K~+-ATPase, and the inhibition rate was 44.55% and 31.44%, respectively; but 1-phenyl-4-(3,4-methylenedioxy)-phenyl-diacetylene and 1-phenyl-4-m-nitrophenyl-diacetylene enhanced the activity of the enzyme, and the activation rate was 24.98% and 20.61%; 1-t-butyl-4-hydroxymethyl-diacetylene,1-phenyl-4-p-methoxyphenyl-diacetylene and 1-phenyl-4-o-nitrophenyl-diacetylene inhibited the activity of Ca~(2+)-Mg~(2+)-ATPase, and the inhibition rate was 49.02%, 38.53% and 35.32%, respectively; but other compounds enhanced activity of the enzyme, among them the highest activity was observed with 1-phenyl-4-(3,4-methylenedioxy)-phenyl-diacetylene, and the activation rate was 81.12%.
