Nachman Ronald J, Fehrentz Jean-Alain, Martinez Jean, Kaczmarek Krzyztof, Zabrocki Janusz, Coast Geoffrey M
Areawide Pest Management Research Unit, Southern Plains Agricultural Research Center, U.S. Department of Agriculture, College Station, TX 77845, USA.
Peptides. 2007 Jan;28(1):146-52. doi: 10.1016/j.peptides.2006.09.017. Epub 2006 Nov 28.
The insect kinins are present in a wide variety of insects and function as potent diuretic peptides in flies. A C-terminal aldehyde insect kinin analog, Fmoc-RFFPWG-H (R-LK-CHO), demonstrates stimulation of Malpighian tubule fluid secretion in crickets, but shows inhibition of both in vitro and in vivo diuresis in the housefly. R-LK-CHO reduced the total amount of urine voided over 3 h from flies injected with 1 microL of distilled water by almost 50%. The analog not only inhibits stimulation of housefly fluid secretion by the native kinin Musdo-K, but also by thapsigargin, a SERCA inhibitor, and by ionomycin, a calcium ionophore. The activity of R-LK-CHO is selective, however, as related C-terminal aldehyde analogs do not demonstrate an inhibitory response on housefly fluid secretion. The selective inhibitory activity of R-LK-CHO on housefly tubules represents an important lead in the development of environmentally friendly insect management agents based on the insect kinins.
昆虫激肽存在于多种昆虫中，在果蝇中作为有效的利尿肽发挥作用。一种C末端醛类昆虫激肽类似物Fmoc-RFFPWG-H（R-LK-CHO），在蟋蟀中可刺激马氏管液体分泌，但在家蝇中却显示出对体外和体内利尿的抑制作用。R-LK-CHO使注射1微升蒸馏水的家蝇在3小时内排出的尿液总量减少了近50%。该类似物不仅抑制天然激肽Musdo-K对家蝇液体分泌的刺激，还抑制毒胡萝卜素（一种SERCA抑制剂）和离子霉素（一种钙离子载体）对家蝇液体分泌的刺激。然而，R-LK-CHO的活性具有选择性，因为相关的C末端醛类类似物对家蝇液体分泌并未表现出抑制反应。R-LK-CHO对家蝇肾小管的选择性抑制活性是基于昆虫激肽开发环境友好型昆虫管理剂的重要线索。
