Boina Dhana Raj, Bloomquist Jeffrey R
Neurotoxicology Laboratory, Department of Entomology, Virginia Polytechnic Institute and State University, Blacksburg, VA 24061, USA.
Arch Insect Biochem Physiol. 2009 Mar;70(3):151-61. doi: 10.1002/arch.20287.
In this study, four blockers of anion transporters (ATs) belonging to four different classes of organic acids, including DIDS (4, 4'-diisothiocyanatostilbene-2, 2'- disulfonic acid; a stilbene disulfonic acid), NPPB [(5-nitro-2-(3-phenylpropylamino) benzoic acid; an anthranilic acid)], 9-AC (anthracene-9-carboxylic acid; an aromatic carboxylic acid), and IAA-94 (indanyloxy acetic acid; an indanyloxy alkanoic acid), were tested for their toxicity against the European corn borer (ECB), Ostrinia nubilalis. All the AT blockers inhibited the growth of larvae, increased the developmental time, and decreased survival compared to controls, when second-instar ECB larvae were fed for seven days on treated diet. In general, DIDS and NPPB were the most active compounds, with the rank order of activity being DIDS>NPPB>IAA-94>9-AC. All the AT blockers decreased the midgut alkalinity in fifth-instar larvae when fed for 3 h on treated diet. Effective concentrations required for 50% decrease in midgut alkalinity (EC(50)) ranged between 29.1 and 41.2 ppm and the rank order of activity was NPPB>DIDS>IAA-94>9-AC. Similarly, all the tested AT blockers inhibited (36)Cl(-) uptake from the midgut lumen in fifth-instar larvae when fed for 3 h on treated diet. Concentrations required for 50% inhibition of (36)Cl(-) uptake (IC(50)) ranged between 7.4 and 11.0 ppm and the rank order of activity was DIDS>NPPB>9-AC >IAA-94. Modest to highly strong positive correlations observed among growth, midgut alkalinity, and midgut Cl(-) ion transport in AT blocker-fed larvae suggested that these effects are causally related to each other. Finally, AT blockers have the potential to become good candidates for development of insecticides with a unique mode of action.
在本研究中,测试了四种属于不同类别的有机酸的阴离子转运体(AT)阻滞剂对欧洲玉米螟(ECB),即玉米螟(Ostrinia nubilalis)的毒性。这四种阻滞剂包括二硫代二苯乙烯二磺酸(DIDS,4,4'-二异硫氰基芪-2,2'-二磺酸;一种芪二磺酸)、5-硝基-2-(3-苯丙基氨基)苯甲酸(NPPB;一种邻氨基苯甲酸)、蒽-9-羧酸(9-AC;一种芳香羧酸)和茚氧基乙酸(IAA-94;一种茚氧基链烷酸)。当用经处理的饲料喂养二龄ECB幼虫7天时,与对照相比,所有的AT阻滞剂均抑制了幼虫的生长,延长了发育时间,并降低了存活率。总体而言,DIDS和NPPB是最具活性的化合物,活性顺序为DIDS > NPPB > IAA-94 > 9-AC。当用经处理的饲料喂养五龄幼虫3小时后,所有的AT阻滞剂均降低了中肠碱度。使中肠碱度降低50%所需的有效浓度(EC50)在29.1至41.2 ppm之间,活性顺序为NPPB > DIDS > IAA-94 > 9-AC。同样,当用经处理的饲料喂养五龄幼虫3小时后,所有测试的AT阻滞剂均抑制了中肠腔对(36)Cl(-)的摄取。抑制(36)Cl(-)摄取50%所需的浓度(IC50)在7.4至11.0 ppm之间,活性顺序为DIDS > NPPB > 9-AC > IAA-94。在喂食AT阻滞剂的幼虫中,生长、中肠碱度和中肠Cl(-)离子转运之间观察到适度至高度强烈的正相关,这表明这些效应彼此之间存在因果关系。最后,AT阻滞剂有可能成为开发具有独特作用方式的杀虫剂的良好候选物。