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目的 建立用于筛选人ＩＬ－６受体拮抗剂的Ｍ１细胞模型，并在该细胞模型上筛选具有人ＩＬ－６受体拮抗活性的化合物。方法 用反转录ＰＣＲ，检测Ｍ１细胞系上ＩＬ－６Ｒα／ｇｐ１３０ ｍＲＮＡ的表达情况，然后应用ＭＴＴ比色法检测在体外液体培养中，Ｍ１细胞对ｒｈＩＬ－６的反应性和多种小分子化合物对ｒｈＩＬ－６的拮抗活性。 结果 Ｍ１细胞有高丰度的ＩＬ－６Ｒα／ｇｐ１３０ ｍＲＮＡ表达；并对ｒｈＩＬ－６具有较为灵敏的反应性；经对１１３个化合物的筛选，发现两个化合物能部分地拮抗人ＩＬ－６受体的生物学活性。 结论 以Ｍ１细胞作为筛选人ＩＬ－６受体拮抗剂的细胞模型，筛选出具有一定人ＩＬ－６受体拮抗活性的两个化合物。
OBJECTIVE: To establish an M1 cell model for screening human IL-6 receptor antagonists and screen the cell model for compounds that have human IL-6 receptor antagonistic activity. Methods The expression of IL-6Rα / gp130 mRNA in M1 cell line was detected by reverse transcription-polymerase chain reaction (RT-PCR). Then the responsiveness of M1 cells to rhIL-6 and the activity of various small molecule compounds Antagonistic activity against rhIL-6. Results M1 cells had high abundance of IL-6Rα / gp130 mRNA expression and had more sensitive reactivity to rhIL-6. After screening 113 compounds, it was found that both compounds could partially antagonize human IL-6 receptor Biological activity. Conclusion M1 cells were selected as the cell model for screening human IL-6 receptor antagonist and two compounds with certain human IL-6 receptor antagonistic activity were screened out.