Nuclear factor-κB (NF-κB) is a protein complexes which is a pivotal transcription factor. It involves in regulating the immune system by enhancing the transcription of proinflammatory cytokines in the generation of acute inflammatory responses[1]. QNZ is a potent and selective NF-κB inhibitor with IC50 value of 11 nM[2]. SK-HEP-1 cells were treated with 0.4 µM QNZ and the cell viability measured by MTT assay was significantly inhibited in a time dependent manner. The NF-κB p65 (Ser536), anti-apoptotic proteins (XIAP, MCL-1 and c-FLIP) level examined by western blotting assay also inhibited after 48 hours of treatment[3]. BALB/c mice with infection in the right hind paw were i.p. injected with 0.001 g/kg of QNZ and 0.1 g/kg glucantime for five consecutive days. The combined treatment could decrease the lesion sizes of the infected paws significantly compared with the control group and increase IL-1β production in the supernatant from the excised infected paws measured by ELISA[4].
作用机制
QNZ inhibited the activation of NF-κB through inhibiting the phosphorylation of the its subunit IκBα and block the nuclear translocation of NF-κB[5][6].
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