Garside C S, Nachman R J, Tobe S S
Department of Zoology, University of Toronto, M5S 3G5, Toronto, On, Canada.
Insect Biochem Mol Biol. 2000 Aug-Sep;30(8-9):703-10. doi: 10.1016/s0965-1748(00)00041-2.
Studies on the catabolism of allatostatins (ASTs) provided the rationale for the design of a series of Dip-allatostatin-derived pseudopeptide mimetic analogues. In vitro, the Dip-ASTs and pseudopeptides show varying degrees of resistance to catabolism and all show significant inhibition of juvenile hormone (JH) biosynthesis. This study was undertaken to determine whether potent Dip-ASTs and/or their pseudopeptide mimetic counterparts caused 'allatostatic' effects in vivo following injection into mated female Diploptera punctata. Animals injected with aqueous solvent or Dip-AST 7(1-7) N-terminal fragment, which excludes the active core region of the ASTs, were used as controls. An in vitro radiochemical assay revealed that injection of Dip-AST 5, 7 or pseudopeptide analogues 397-2 or AST(b)φ2 significantly inhibited the biosynthesis of JH (P<0.05). The results also indicate that basal oocyte growth was significantly inhibited by injection of these same compounds, with the exception of Dip-AST 7 (P<0.05). Analogues 396-1 and 419 did not significantly inhibit rates of JH biosynthesis but did significantly inhibit the growth of basal oocytes. Analyses of feeding, excretion and food absorption/utilization patterns of these same animals suggested that these compounds are not toxic to the insect; rather they directly inhibit the biosynthesis of JH by the corpora allata, and reduce the rate of growth of basal oocytes. Disruption of critical reproductive and/or developmental processes by pseudopeptide analogues of the ASTs could provide novel and selective strategies for future insect pest management.
对抑咽侧体素(ASTs)分解代谢的研究为设计一系列源自双翅目抑咽侧体素的拟肽模拟类似物提供了理论依据。在体外,双翅目抑咽侧体素和拟肽对分解代谢表现出不同程度的抗性,并且均显著抑制保幼激素(JH)的生物合成。本研究旨在确定强效双翅目抑咽侧体素和/或其拟肽模拟类似物在注射到已交配的雌性点刻条胸蜚蠊体内后是否会产生“抑咽侧体素效应”。注射水性溶剂或双翅目抑咽侧体素7(1-7)N端片段(该片段不包括抑咽侧体素的活性核心区域)的动物用作对照。一项体外放射化学分析表明,注射双翅目抑咽侧体素5、7或拟肽类似物397-2或AST(b)φ2可显著抑制JH的生物合成(P<0.05)。结果还表明,除双翅目抑咽侧体素7外,注射这些相同的化合物可显著抑制基础卵母细胞的生长(P<0.05)。类似物396-1和419没有显著抑制JH生物合成速率,但确实显著抑制了基础卵母细胞的生长。对这些相同动物的摄食、排泄和食物吸收/利用模式的分析表明,这些化合物对昆虫无毒;相反,它们直接抑制咽侧体对JH的生物合成,并降低基础卵母细胞的生长速率。ASTs的拟肽类似物对关键生殖和/或发育过程的破坏可为未来害虫管理提供新的选择性策略。