Nachman Ronald J, Coast Geoffrey M, Douat Céline, Fehrentz Jean Alain, Kaczmarek Krzyztoff, Zabrocki Janusz, Pryor Nan W, Martinez Jean
Areawide Pest Management Research, Southern Plains Agricultural Research Center, USDA, 2881 F/B Road, College Station, TX 77845, USA.
Peptides. 2003 Oct;24(10):1615-21. doi: 10.1016/j.peptides.2003.06.008.
The first reported examples of C-terminal aldehyde analogs of an insect neuropeptide are described. They are hexapeptide insect kinin analogs Boc-VFFPWG-H and Fmoc-RFFPWG-H. Activity observed for these modified analogs in an in vitro insect diuretic assay confirms that the C-terminal aldehyde group is tolerated by an insect kinin receptor. The two analogs demonstrate greatly enhanced activity over standard C-terminal amide insect kinins in a larval weight gain inhibition assay in the corn earworm Helicoverpa zea. Treatment with Boc-VFFPWG-H led to significant increases in larval mortality at doses of 500pm (45%) and 5nm (67%). Boc-VFFPWG-H represents a lead analog in the development of novel, environmentally friendly pest insect management agents based on the insect kinin class of neuropeptides.
本文描述了昆虫神经肽C端醛类似物的首个报道实例。它们是六肽昆虫激肽类似物Boc-VFFPWG-H和Fmoc-RFFPWG-H。在体外昆虫利尿试验中观察到这些修饰类似物的活性，证实昆虫激肽受体能够耐受C端醛基。在玉米穗虫Helicoverpa zea的幼虫体重增加抑制试验中，这两种类似物显示出比标准C端酰胺昆虫激肽大大增强的活性。用Boc-VFFPWG-H处理，在500pm（45%）和5nm（67%）剂量下导致幼虫死亡率显著增加。Boc-VFFPWG-H代表了基于昆虫激肽类神经肽开发新型、环境友好型害虫管理剂的先导类似物。
