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新的氟喹诺酮衍生物A-56 619和A-56 620能够抑制由ConA和单克隆抗体OKT3所诱导的人外周血单核细胞的增殖.实验采用单核细胞、ConA分别加或不加A-56 619和A-56 620;单核细胞、单克隆抗体OKT3加或不加A-56 619或A-56 620,然后将各培养盘在37℃培养24小时,在培养终点之前,加入3.7×10~4Bq的〔~3H〕胸腺嘧啶.培养细胞用自动细胞收获器收获;〔~3H〕胸腺嘧啶掺入量用液体闪烁计数仪计算.结果表明A-56 619和A-56 620对由有丝分裂原ConA、OKT3单克隆抗体所诱导的细胞增殖有抑制作用,即使加大有丝分裂原的浓度或延长细胞孵化时间也不能逆转这种抑制效果.但从培养液中去除药物则能解除细胞DNA的抑制,表明这两种药物的抑制是可逆的.两药不抑制细胞蛋白质合成(通过〔~3H〕
The new fluoroquinolone derivatives A-56 619 and A-56 620 were able to inhibit the proliferation of human peripheral blood mononuclear cells induced by ConA and the monoclonal antibody OKT 3. The mononuclear cells were treated with ConA with or without A- 56 619 and A-56 620; monocytes, monoclonal antibodies OKT3 with or without A-56 619 or A-56 620, and then each plate was incubated at 37 ° C for 24 hours. Prior to the end of the culture, 3.7 × [~ 3H] thymidine with 10 ~ 4Bq. The cultured cells were harvested with an automatic cell harvester; the amount of [~ 3H] thymidine incorporation was calculated using a liquid scintillation counter. The results showed that A-56 619 and A- Inhibition of cell proliferation induced by the original ConA and OKT3 monoclonal antibodies did not reverse the inhibitory effect even if the mitogen concentration was increased or the cell incubation time was prolonged However, removal of the drug from the culture solution could relieve cellular DNA inhibition , Suggesting that the inhibition of these two drugs is reversible. Both drugs do not inhibit cellular protein synthesis (via [-3H]