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].
QNZ 细胞实验
Cell Line
Concentration
Treated Time
Description
References
macrophages
20 nM
to study the effect of QNZ on the NFκB signaling pathway in macrophages
Front Immunol. 2017 Sep 4;8:1063.
SW620 cells
10 nM
QNZ decreased the expression of CCL20 in SW620 cells
J Immunother Cancer. 2019 Aug 8;7(1):215.
DLD-1 cells
10 nM
QNZ decreased the expression of CCL20 in DLD-1 cells
J Immunother Cancer. 2019 Aug 8;7(1):215.
BM-LCs
10 μM
2 h
To detect the effect of IL-38 on CCR7 expression in BM-LCs. The results showed that QNZ pretreatment could inhibit the upregulation of CCR7 expression induced by IL-38.
Int J Biol Sci. 2024 May 27;20(8):3094-3112.
BMDCs
80 μg/mL
22 h
To verify whether QNZ affects BMDC maturation by inhibiting the NF-κB signaling pathway. The results showed that pretreatment with QNZ significantly inhibited KK2DP7-induced BMDC maturation.
Adv Sci (Weinh). 2023 May;10(15):e2300116.
BV2 microglial cells
10 µM
24 h
QNZ significantly suppressed the inhibitory effect of 2.5 µM EC on the expression of iNOS
Molecules. 2019 Sep 12;24(18):3317.
HaCaT cells
5 μM
QNZ alone significantly inhibited cell proliferation and induced apoptosis, and no additional effect on inhibiting cell proliferation or inducing apoptosis was observed when combined with BIX01294.
Cell Death Dis. 2023 Sep 22;14(9):627.
QNZ 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
DNFB-induced AD model
Transdermal administration
2 mg/kg
From day 6 until the end of modelling
QNZ alleviated DNFB-induced AD symptoms by inhibiting the NF-κB signaling pathway
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