Ju D W, Zheng Q Y, Wang H B, Fang J
Department of Pharmacology, School of Pharmacy, Second Military Medical University, Shanghai.
Yao Xue Xue Bao. 1994;29(2):90-4.
Leflunomide (LFM, HWA 486) is an isoxazol derivative with antiphogistic and novel immunomodulating properties. It has been shown to be very effective in preventing and curing arthritis. In this report we found that platelet-activating factor (PAF) at 0.1-10 micrograms.ml-1 significantly stimulated DNA synthesis in cultured rabbit synovial cells. While LFM and its metabolite A771726 elicited inhibitory effects on this action of PAF. These two agents were also shown to markedly inhibit A23187 induced PAF production from rat peritoneal macrophages. The inhibition was dose and time-dependent. The inhibitory effects of LFM and A771726 on DNA synthesis in synovial cells and PAF production from macrophages may play an important role in the antiinflammatory effects of LFM.
来氟米特（LFM，HWA 486）是一种具有抗炎和新型免疫调节特性的异恶唑衍生物。已证明它在预防和治疗关节炎方面非常有效。在本报告中，我们发现0.1 - 10微克/毫升的血小板活化因子（PAF）能显著刺激培养的兔滑膜细胞中的DNA合成。而LFM及其代谢产物A771726对PAF的这一作用产生抑制效果。这两种药物还被证明能显著抑制A23187诱导的大鼠腹腔巨噬细胞PAF生成。这种抑制呈剂量和时间依赖性。LFM和A771726对滑膜细胞DNA合成以及巨噬细胞PAF生成的抑制作用可能在LFM的抗炎作用中起重要作用。
