N-Methylcytisine(NMC), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. Oral administration (1, 4 and 16 mg/kg) of NMC attenuated the DSS(dextran sulfate sodium)-induced clinical symptoms and pathological damage. In addition, NMC treatment significantly reduced myeloperoxidase activity and level of pro-inflammatory cytokines. NMC blocked the activation of NF-κB by inhibiting IκB and IKK phosphorylation[3]. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a high affinity (Kd = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia[4].
N-Methylcytisine/N-甲基金雀花碱 细胞实验
Cell Line
Concentration
Treated Time
Description
References
DPX2 cells
10 µM
24 hours
To evaluate the effect of N-Methylcytisine on PXR activation. Results showed that N-Methylcytisine significantly activated PXR, with luciferase activity increasing ∼10-fold.
Drug Metab Dispos. 2010 Dec;38(12):2226-31
SMMC-7721 cells
4 mg/mL
24 hours
To evaluate the inhibitory effect of N-Methylcytisine on the proliferation of SMMC-7721 cells. The results showed that N-Methylcytisine significantly inhibited the proliferation of SMMC-7721 cells.
Sci Rep. 2018 Jan 12;8(1):624
HepaRG cells
10 µM
48 hours
To evaluate the effect of N-Methylcytisine on CYP3A4 expression. Results showed that N-Methylcytisine significantly induced CYP3A4 mRNA expression, and this induction was suppressed by the PXR antagonist sulforaphane.
Drug Metab Dispos. 2010 Dec;38(12):2226-31
N-Methylcytisine/N-甲基金雀花碱 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
ICR mice
DSS-induced colitis model
Oral
1, 4, 16 mg/kg
Once daily for 7 days
To evaluate the protective effect of NMC on DSS-induced colitis and its possible mechanisms. Results demonstrated that NMC significantly attenuated DSS-induced clinical symptoms and pathological damage, reduced myeloperoxidase activity and pro-inflammatory cytokine levels, and blocked NF-κB activation by inhibiting IκB and IKK phosphorylation.
Molecules. 2018 Feb 25;23(3):510
DBA/1 mice
Collagen-induced arthritis (CIA) model
Oral
100.0 mg/kg
Once daily for 30 days
To evaluate the anti-inflammatory effects of N-Methylcytisine in CIA mice, results showed that different batches of CRM extracts significantly suppressed the levels of pro-inflammatory cytokines such as TNF-α, IL-1β, IL-6, and IL-17.
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