Wing K D
Research Labs, Rohm and Haas Co., Spring House, PA 19477.
Science. 1988 Jul 22;241(4864):467-9. doi: 10.1126/science.3393913.
The steroid molting hormone 20-hydroxyecdysone is the physiological inducer of molting and metamorphosis in insects. In ecdysone-sensitive Drosophila Kc cells, the insecticide RH 5849 (1,2-dibenzoyl-1-tert-butylhydrazine) mimics the action of 20-hydroxyecdysone by causing the formation of processes, an inhibition of cell proliferation, and induction of acetylcholinesterase. RH 5849 also competes with [3H]ponasterone A for high-affinity ecdysone receptor sites from Kc cell extracts. Resistant cell populations selected by growth in the continued presence of either RH 5849 or 20-hydroxyecdysone are insensitive to both compounds and exhibit a decreased titer of measurable ecdysone receptors. Although it is less potent than 20-hydroxyecdysone in both whole-cell and cell-free receptor assays, RH 5849 is the first nonsteroidal ecdysone agonist.
类固醇蜕皮激素20-羟基蜕皮酮是昆虫蜕皮和变态的生理诱导剂。在对蜕皮激素敏感的果蝇Kc细胞中，杀虫剂RH 5849（1,2-二苯甲酰基-1-叔丁基肼）通过引起突起形成、抑制细胞增殖和诱导乙酰胆碱酯酶来模拟20-羟基蜕皮酮的作用。RH 5849还能与[3H]蜕皮甾酮A竞争Kc细胞提取物中的高亲和力蜕皮激素受体位点。通过在持续存在RH 5849或20-羟基蜕皮酮的情况下生长而选择的抗性细胞群体对这两种化合物均不敏感，且可测量的蜕皮激素受体滴度降低。尽管在全细胞和无细胞受体测定中，RH 5849的效力均低于20-羟基蜕皮酮，但它是第一种非甾体类蜕皮激素激动剂。
