This invention relates to a novel farnesylated dibenzodiazepinone, named ECO-04601, its pharmaceutically acceptable salts and derivatives, and to methods for obtaining such compounds. One method of obtaining the ECO-04601 compound is by cultivation of a novel strain of
Micromonospora
sp., 046-ECO11; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to
Micromonospora
sp. strain 046-ECO11, to the use of and its pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of cancer cell growth, bacterial cell growth, mammalian lipoxygenase, and to pharmaceutical compositions comprising ECO-04601 or a pharmaceutically acceptable salt or derivative thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of ECO-04601.
本发明涉及一种新型的法尼酰化二苯并二氮平酮,名为
ECO-04601,其药学上可接受的盐和衍
生物,以及获得这种化合物的方法。获得
ECO-04601化合物的一种方法是通过培养一种新的微单孢菌株Micromonosporasp.,046-
ECO11;另一种方法涉及在转化的宿主细胞中表达
生物合成途径
基因。本发明还涉及Micromonosporasp.株系046-
ECO11的使用及其药学上可接受的盐和衍
生物作为药物,特别是它们作为抑制癌细胞生长、细菌细胞生长、哺乳动物脂氧合酶的药物的使用,以及包含
ECO-04601或其药学上可接受的盐或衍
生物的药物组合物。最后,本发明涉及新的多核苷酸序列及其编码的蛋白质,这些蛋白质参与
ECO-04601的
生物合成。