环氧化酶-2特异性抑制剂筛选模型的研究

Research of Screening Model by COX-2 Selective Inhibitors

佛波酯诱导静息NIH 3T3细胞建立炎症模型,以GAPDH为内标,地塞米松为阳性药物,运用半定量RT-PCR技术,初步建立环氧化酶-2(COX-2)基因转录调控药物筛选模型。RIA法测定Rofecoxib对COX-1酶的作用,并与其对COX-2酶的抑制作用相比较,得到IC50(COX-2)/IC50(COX-1)为0.003,完善在蛋白质水平上筛选COX-2特异性抑制剂的模型。

To set an inflammation model by inducing quiescent NIH 3T3 celll with phorbol ester, After the inhibition of Dexemethasone,COX-2 mRNA was determined by RT-PCR,normalized to GAPDH expression.So a primary COX-2 gene transcripdon regulatory drugs screening model has been set. The inhibition of Rofecoxib on COX-1 enzyme was determined by RIA. Compared with the inhibition of Rofecoxib on COX-2 enzyme, the value of IC50 (COX-2)/IC50 (COX-1)is 0.003. The model of screening COX-2 protein selective inhibiting drugs was perfected by this way.