Sharma Priyanka, Thakur Sunil, Awasthi Pamita
Department of Chemistry, National Institute of Technology, Hamirpur, 177005, India.
Appl Biochem Biotechnol. 2015 May;176(1):125-39. doi: 10.1007/s12010-015-1562-x. Epub 2015 Apr 23.
Juvenile hormone is an important hormone which controls the developmental process in the lepidopteran insects, hence, referred as insect growth regulator. Juvenile hormone binding proteins are the carrier of juvenile hormone from the site of secretion to the site of action and play vital role in juvenile hormone action. We have designed four different juvenile hormone analogs incorporating sulfonamide and heterocyclic moieties using computer-aided tools. All analogs (T3-T6) gave comparative energy profile in comparison to in use insect growth regulators like fenoxycarb (T2) and pyriproxyfen (T1). Further, theses analogs have been screened on biological model Galleria mellonella (wax moth) for their mortality rate. All analogs were evaluated using three different concentrations (1000, 1500, and 2000 ppm) and five different exposure periods (2, 4, 6, 8, and 10 h). In vivo study showed that analog N-(1-isopropyl-2-oxo-2-morpholino-ethyl) toluene sulfonamide (T6) and N-(1-isopropyl-2-oxo-2-piperidino-ethyl) toluene sulfonamide (T4) exhibit the good larval mortality at lower concentration (1000 ppm) after 8 h exposure in comparison to pyriproxyfen (T1) and fenoxycarb (T2). The findings demonstrate the effectiveness and validity of the virtual screening approach (docking) and provide a starting point for the development of novel juvenile hormone analogs to counter G. mellonella.
保幼激素是一种重要的激素,它控制鳞翅目昆虫的发育过程,因此被称为昆虫生长调节剂。保幼激素结合蛋白是保幼激素从分泌部位到作用部位的载体,在保幼激素的作用中起着至关重要的作用。我们使用计算机辅助工具设计了四种不同的含有磺酰胺和杂环部分的保幼激素类似物。与正在使用的昆虫生长调节剂如苯氧威(T2)和吡丙醚(T1)相比,所有类似物(T3 - T6)都具有相当的能量分布。此外,这些类似物已在生物模型大蜡螟(蜡蛾)上进行了死亡率筛选。所有类似物均使用三种不同浓度(1000、1500和2000 ppm)和五个不同暴露时间(2、4、6、8和10小时)进行评估。体内研究表明,与吡丙醚(T1)和苯氧威(T2)相比,类似物N -(1 - 异丙基 - 2 - 氧代 - 2 - 吗啉代 - 乙基)甲苯磺酰胺(T6)和N -(1 - 异丙基 - 2 - 氧代 - 2 - 哌啶基 - 乙基)甲苯磺酰胺(T4)在8小时暴露后,在较低浓度(1000 ppm)下表现出良好的幼虫死亡率。这些发现证明了虚拟筛选方法(对接)的有效性和正确性,并为开发对抗大蜡螟的新型保幼激素类似物提供了一个起点。