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EFFECTS OF LEFLUNOMIDE AND ITS ACTIVE METABOLITE ON THE PRODUCTION AND mRNA EXPRESSION OF TNF-α IN PERITONEAL MACROPHAGES AND SYNOVIAL CELLS WITH ADJUVANT ARTHRITIS IN RATS
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 10
- DOI:
- 10.3321/j.issn:0513-4870.2002.10.004
- Key Word:
- 来氟米特;活性代谢物;TNF-α;mRNA表达;佐剂性关节炎大鼠
Abstract： 目的观察免疫抑制剂来氟米特(leflunomide,LEF)及其活性代谢产物A771726(A77)对佐剂性关节炎(AA)模型大鼠TNF-α分泌活性及mRNA表达的影响.方法 TNF-α活性及mRNA表达用ELISA法和RT-PCR方法.结果 AA大鼠腹腔巨噬细胞(PMφ)呈高度活化状态,TNF-α分泌水平明显升高.LEF明显抑制LPS诱导的大鼠PMφ TNF-α释放且呈剂量依赖关系.体外用A77后TNF-α mRNA表达量降低.结论 LEF和A77对AA模型大鼠TNF-α分泌活性及mRNA表达有抑制作用,此可能为其抗炎和免疫抑制作用的机制之一.
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