Inhibition of Na^+,K^+-ATPase in Housefly (Musca domestica L.) by Terpinen-4-ol and Its Ester Derivatives  

作　　者：GUO Zhi-bo MA Zhi-qing FENG Jun-tao ZHANG Xing 

机构地区：[1]Research ＆ Development Center of Biorational Pesticide, Northwest A＆F University/Technology and Engineering Center of Biopesticide, Shaanxi Province, Yangling 712100, P.R. China [2]College of Traditional Chinese Medicines, China Pharmaceutical University, Nanjing 210009, P.R.China

出　　处：《Agricultural Sciences in China》2009年第12期1492-1497,共6页中国农业科学（英文版）

基　　金：supported by the National Natural Science Foundation of China (30600404)

摘　　要：To reveal the insecticidal mechanism of terpinen-4-ol, the activity of Na＋,K＋-ATPase in insects tested were determined in vivo and in vitro. The results showed that terpinen-4-ol and its ester derivatives had strong contact activity to housefly and the contact toxicities of its derivatives except Z3 were all superior or equivalent to terpinen-4-ol. All the 7 compounds had strong inhibition towards activity of Na＋,K＋-ATPase. With poisoning symptom exacerbating, the inhibition rates were gradually increased. In vitro, the IC50 of terpinen-4-ol, Z1, Z2, Z4, Z5, and Z6 was 155.89, 197.98, 96.02, 121.36, 124.85, and 153.74 μg mL% respectively. There was well correlation between the LDs0 of terpinen-4-ol derivatives to housefly and the IC50 of terpinen-4-ol derivatives to Na＋,K＋-ATPase in housefly. In conclusion, Na＋,K＋-ATPase was likely the target of terpinen-4-ol against insects.To reveal the insecticidal mechanism of terpinen-4-ol, the activity of Na＋,K＋-ATPase in insects tested were determined in vivo and in vitro. The results showed that terpinen-4-ol and its ester derivatives had strong contact activity to housefly and the contact toxicities of its derivatives except Z3 were all superior or equivalent to terpinen-4-ol. All the 7 compounds had strong inhibition towards activity of Na＋,K＋-ATPase. With poisoning symptom exacerbating, the inhibition rates were gradually increased. In vitro, the IC50 of terpinen-4-ol, Z1, Z2, Z4, Z5, and Z6 was 155.89, 197.98, 96.02, 121.36, 124.85, and 153.74 μg mL% respectively. There was well correlation between the LDs0 of terpinen-4-ol derivatives to housefly and the IC50 of terpinen-4-ol derivatives to Na＋,K＋-ATPase in housefly. In conclusion, Na＋,K＋-ATPase was likely the target of terpinen-4-ol against insects.

关 键 词：TERPINEN-4-OL terpinen-4-ol ester derivatives Na＋ K＋-ATPase Musca domestica L. 

分 类 号：S511.01[农业科学—作物学] TQ463[化学工程—制药化工]