Georgieva T G, Jankulova E D, Ralchev K H, Dunkov B C
Department of Genetics, Faculty of Biology, Sofia University, St. Kliment Ohridski, Bulgaria.
Arch Insect Biochem Physiol. 1995;29(1):25-34. doi: 10.1002/arch.940290104.
Drosophila diaphorase-1 (DIA-1) is an enzyme similar to mammalian DT-diaphorase and is inhibited in vitro by dicoumarol. However, a ten-fold increase in DIA-1 activity was observed when third instar Drosophila virilis larvae were fed on a diet containing 0.1 M dicoumarol for 48 h. This induction was shown to be dose dependent and immunoprecipitation experiments with DIA-1 anti-serum demonstrated an increase in the DIA-1 protein level in dicoumarol-treated larvae. The induction of DIA1 by dicoumarol was found to be blocked by actinomycin D, which suggests a transcriptional mechanism of regulation. The opposite effect of dicoumarol on DIA-1 in vitro vs. in vivo suggests that a metabolic conversion takes place after the ingestion of this compound by D. virilis larvae.
果蝇黄递酶-1(DIA-1)是一种类似于哺乳动物DT-黄递酶的酶,在体外被双香豆素抑制。然而,当用含有0.1M双香豆素的饲料喂养三龄果蝇幼虫48小时后,观察到DIA-1活性增加了10倍。这种诱导作用呈剂量依赖性,用DIA-1抗血清进行的免疫沉淀实验表明,在双香豆素处理的幼虫中DIA-1蛋白水平增加。发现双香豆素对DIA1的诱导作用被放线菌素D阻断,这表明存在转录调控机制。双香豆素在体外和体内对DIA-1的相反作用表明,果蝇幼虫摄入这种化合物后发生了代谢转化。