Farkas R, Sláma K
Institute of Experimental Endocrinology, Slovak Academy of Sciences, Bratislava, Slovak Republic.
Insect Biochem Mol Biol. 1999 Nov;29(11):1015-27. doi: 10.1016/s0965-1748(99)00077-6.
Two bisacylhydrazine insecticides with ecdysone-mimetic action, RH-5849 and RH-5992, have been subjected to several bioassay procedures that are prerequisites for ecdysone action in Drosophila larvae: (a) induction of early ecdysone-specific puffs on the polytene chromosomes of the larval salivary glands; (b) secretion of glycoprotein glue into the lumen of the salivary glands; (c) evagination of imaginal discs of adult wings and legs; and (d) partial rescue of wild-type phenotypic expression in ecdysone-deficient mutants (ecdysoneless1 (ecd1) and suppressor of forkedts67g (su(f)ts67g). In all these bioassays on Drosophila larvae, the two purely synthetic hydrazines exhibited similar dose-response relationships as did the natural steroid hormone, 20-hydroxyecdysone. In assays involving induction of early chromosomal puffs (74EF, 75B) or regression of the preexisting puffs (25AC, 68C), the dosages required for induction of standard ED-50 effects were one order of magnitude larger for the hydrazines in comparison with 20-hydroxyecdysone. In the assays related to glycoprotein glue secretion, evagination of imaginal discs, or rescue of phenotypic expression in ecdysone-deficient mutants, 20-hydroxyecdysone was two orders of magnitude more active than RH-5849 and RH-5992. We conclude that, in spite of these quantitative differences, the two hydrazine compounds studied are able to duplicate in Drosophila larvae the complex of qualitative biological effects that are a prerequisite for ecdysteroid hormones. The hormonomimetic stimulus of RH-compounds has been given at very low, intracellular, chromosomal level.
两种具有蜕皮激素模拟作用的双酰肼类杀虫剂,RH - 5849和RH - 5992,已经接受了几种生物测定程序的检测,这些程序是果蝇幼虫蜕皮激素作用的先决条件:(a)在幼虫唾液腺的多线染色体上诱导早期蜕皮激素特异性胀泡;(b)向唾液腺管腔分泌糖蛋白胶;(c)成虫翅膀和腿部的成虫盘外翻;以及(d)在蜕皮激素缺陷型突变体(无蜕皮激素1(ecd1)和叉状抑制因子ts67g(su(f)ts67g))中部分恢复野生型表型表达。在所有这些针对果蝇幼虫的生物测定中,这两种纯合成肼类化合物与天然甾体激素20 - 羟基蜕皮激素表现出相似的剂量 - 反应关系。在涉及诱导早期染色体胀泡(74EF、75B)或使预先存在的胀泡(25AC、68C)消退的测定中,与20 - 羟基蜕皮激素相比,诱导标准ED - 50效应所需的肼类化合物剂量大一个数量级。在与糖蛋白胶分泌、成虫盘外翻或蜕皮激素缺陷型突变体表型表达恢复相关的测定中,20 - 羟基蜕皮激素的活性比RH - 5849和RH - 5992高两个数量级。我们得出结论,尽管存在这些数量差异,但所研究的这两种肼类化合物能够在果蝇幼虫中复制蜕皮甾体激素所必需的复杂定性生物学效应。RH化合物的激素模拟刺激作用是在非常低的细胞内染色体水平上产生的。