由一株放线菌产生的抑制VCAM-1表达的活性物质研究

Studies on an active compound preventing VCAM-1 expression from one strain of actinomycetes

以VCAM-1为靶位点,使用含有荧光素酶报告基因的转染细胞株筛选模型从微生物的代谢产物中高通量筛选能够抑制VCAM-1表达的生物活性物质,以期找到能够治疗诸如类风湿性关节炎等免疫性疾病的新型药物。在筛选过程中使用有机溶媒萃取、ODS反相柱层析、HPLC制备等方法,从一株放线菌来源的发酵液中分离到了一个对测活用细胞株的荧光素酶报告基因的表达有较强抑制作用的化合物,其IC50为10.8μmol/L,经理化性质及NMR分析确定该化合物与文献报道的glucopiericidin A同质。

Focused on the VCAM-1 as the research target, we used a stable transfected cell line carrying the luciferase report gene in high throughput system to screen bioactive compound that prevent the expression of VCAM-1 for searching new drugs of treating immunological diseases such as rheumatoid arthritisr from the metabolites of microorganisms. In the course of screening, one active compound was isolated from the mycelium of actinomycetes by solvent extraction, ODS column chromatography and HPLC purification etc. This compound showed moderate strength inhibitory activity against the luciferase report gene expression of the assay cell line and the IC50 is 10.8μmol/L. The structure of this compound was elucidated to be identical with glucopiericidin A by means of physico-chemical properties and NMR analysis.