Arai Masayoshi
Graduate School of Pharmaceutical Sciences, Osaka University.
Yakugaku Zasshi. 2016;136(4):669-76. doi: 10.1248/yakushi.15-00281.
With the development of cell biology and microbiology, it has become easy to culture many types of animal cells and microbes, and they are frequently used for phenotypic screening to explore medicinal seeds. On the other hand, it is recognized that cells and pathogenic microbes present in pathologic sites and infected regions of the human body display unique properties different from those under general culture conditions. We isolated several bioactive compounds from marine medicinal resources using constructed bioassay-guided separation focusing on the unique changes in the characteristics of cells and pathogenic microbes (Mycobacterium spp.) in the human body under disease conditions. In addition, we also carried out identification studies of target molecules of the bioactive compounds by methods utilizing the gene expression profile, transformants of cells or microbes, synthetic probe molecules of the isolated compounds, etc., since bioactive compounds isolated from the phenotypic screening system often target new molecules. This review presents our phenotypic screening systems, isolation of bioactive compounds from marine medicinal resources, and target identification of bioactive compounds.
随着细胞生物学和微生物学的发展，培养多种类型的动物细胞和微生物变得容易，并且它们经常用于表型筛选以探索药用植物。另一方面，人们认识到存在于人体病理部位和感染区域的细胞和致病微生物表现出与一般培养条件下不同的独特特性。我们利用构建的生物活性导向分离方法，从海洋药用资源中分离出几种生物活性化合物，该方法聚焦于疾病状态下人体细胞和致病微生物（分枝杆菌属）特性的独特变化。此外，由于从表型筛选系统中分离出的生物活性化合物通常靶向新分子，我们还通过利用基因表达谱、细胞或微生物转化体、分离化合物的合成探针分子等方法，对生物活性化合物的靶分子进行了鉴定研究。本综述介绍了我们的表型筛选系统、从海洋药用资源中分离生物活性化合物以及生物活性化合物的靶标鉴定。
