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Neferine NF-κB inhibitor

Cat.No.S5144

Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. It induces apoptosis in renal cancer cells. This compound prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. It strongly inhibits NF-κB activation. It possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.
Neferine NF-κB inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 624.77

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Chemical Information, Storage & Stability

Molecular Weight 624.77 Formula

C38H44N2O6

 Storage (From the date of receipt)
CAS No. 2292-16-2 Download SDF Storage of Stock Solutions

Synonyms (R)-1,2-Dimethoxyaporphine Smiles CN1CCC2=CC(=C(C=C2C1CC3=CC=C(C=C3)OC)OC4=C(C=CC(=C4)CC5C6=CC(=C(C=C6CCN5C)OC)OC)O)OC

Solubility

In vitro
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DMSO : 100 mg/mL (160.05 mM)
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Mechanism of Action

Targets/IC50/Ki
NF-κB [4]
In vitro

Neferine induces reactive oxygen species mediated caspase-dependent apoptosis in liver and lung cancer cells, reverses the multidrug resistance in human breast cancer cells (MCF-7/ADM), human hepatocarcinoma (HepG2/ADR) and human gastric carcinoma cells (SGC7901/VCR). This compound enhances the cytotoxic potential of cisplatin in A549 cells and augments cisplatin inducecd Sub-G1 accumulation. It inhibits the migration and invasion of human lung cancer cells and lowers the antioxidant enzyme activities. This chemical sensitizes the lung cancer cells to cisplatin and induces apoptosis through G1 cell cycle arrest, upstream ROS production, depletion of cellular antioxidant pool, reduction of mitochondrial membrane potential (ΔΨm) with increased expression of Bax, Bad, Bak, down regulates the expression of Bcl2, release of cytochrome c, cleaved caspase-9, cleaved caspase-3 and PARP[1].
In vivo

Neferine has an antifibrosis effect on CCl4-induced hepatic fibrosis in mice, possibly partly due to the decreased expression of TGF-β1 in the liver[2]. The plasma concentration-time curves of this compound (10, 20 and 50 mg/kg, i.g.) shows double absorption peaks with the first peak at 10 min and the second peak at 1 h. The tβ1/2 are 15.6 h, 22.9 h and 35.5 h, for each of these doses, respectively. This compound distributes rapidly into different organ systems, with the highest concentrations found in the liver, followed by the lung, kidney and heart at doses of 10 or 20 mg/kg. At 50 mg/kg dose, concentrations of the kidney and lung are higher than those of others. Moreover, this compound is mainly metabolized in the liver and converted partially by CYP2D6 to liensinine, isoliensinine, desmethyl-liensinine and desmethyl-isoliensinine[3].
References

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