Goto M, Chiba K, Hashida R, Shirota H
Eisai Research Laboratories, Eisai Co., Ltd., Ibaraki, Japan.
Agents Actions Suppl. 1991;32:225-9. doi: 10.1007/978-3-0348-7405-2_30.
E5090 is an orally active inhibitor of IL-1 generation, being converted in vivo into the pharmacologically active deacetylated form (DA-E5090). In vitro effects of DA-E5090 on the generation of IL-1 by human monocytes stimulated with LPS were examined. DA-E5090 inhibited both IL-1 alpha and IL-1 beta generation by human monocytes stimulated with 1 microgram/ml of LPS in a dose dependent-manner (1-10 microM), as determined by LAF assay and ELISA. Northern blotting analysis indicated that DA-E5090 inhibits transcription of IL-1 alpha and IL-1 beta m-RNAs.
E5090是一种口服活性白细胞介素-1生成抑制剂，在体内可转化为具有药理活性的脱乙酰化形式（DA-E5090）。研究了DA-E5090对脂多糖刺激的人单核细胞生成白细胞介素-1的体外作用。通过LAF分析和酶联免疫吸附测定法测定，DA-E5090以剂量依赖性方式（1-10微摩尔）抑制1微克/毫升脂多糖刺激的人单核细胞生成白细胞介素-1α和白细胞介素-1β。Northern印迹分析表明，DA-E5090抑制白细胞介素-1α和白细胞介素-1β信使核糖核酸的转录。
