Home Neuronal Signaling 5-HT Receptor antagonist - Dopamine Receptor agonist Nuciferine For research use only.

Nuciferine

Synonyms: Sanjoinine E, (-)-Nuciferine, VLT 049

Nuciferine (Sanjoinine E, (-)-Nuciferine, VLT 049) is a major active aporphine alkaloid from the leaves of N. nucifera Gaertn and possesses anti-hyperlipidemia, anti-hypotensive, anti-arrhythmic, and insulin secretagogue activities. Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.

Nuciferine Chemical Structure

Nuciferine Chemical Structure

CAS No. 475-83-2

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Nuciferine Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

Biological Activity

Description Nuciferine (Sanjoinine E, (-)-Nuciferine, VLT 049) is a major active aporphine alkaloid from the leaves of N. nucifera Gaertn and possesses anti-hyperlipidemia, anti-hypotensive, anti-arrhythmic, and insulin secretagogue activities. Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
In vitro
In vitro Nuciferine inhibits the growth of MDA-MB-231 and MCF-7 human breast cancer cells by inducing apoptosis and inhibiting proliferation via cell cycle arrest. Nuciferine inhibits the receptor activator of nuclear factor kappa-B ligand- (RANKL-) induced osteoclast differentiation in mouse bone marrow macrophage cells and mature osteoclast-mediated bone resorption. It reduces the viability of SY5Y human neuroblastoma cells and CT26 murine colon cancer cells, inhibits nicotine-induced non-small-cell lung cancer progression[1].
Cell Research Cell lines MDA-MB-231 or MCF-7 cells
Concentrations 0, 20, 40, 60 μM
Incubation Time 24 hours
Method MDA-MB-231 or MCF-7 cells (5 × 103 cells/well) are cultured in serum-free media with the various concentrations of liensinine or nuciferine in the absence or presence of zVAD-fmk (10 μM) for 24 h. Bone marrow macrophages (5 × 104 cells/well) are cultured in serum-free medium with liensinine or nuciferine at the indicated concentrations for 5 days. Cell viability is measured with an MTT assay.
In Vivo
In vivo Nuciferine is found to decrease serum urate levels and improve kidney function, as well as inhibit system and renal interleukin-1β (IL-1β) secretion in potassium oxonate-induced hyperuricemic mice. Furthermore, nuciferine reverses expression alteration of renal urate transporter 1 (URAT1), glucose transporter 9 (GLUT9), ATP-binding cassette, subfamily G, membrane 2 (ABCG2), organic anion transporter 1 (OAT1), organic cation transporter 1 (OCT1), and organic cation/carnitine transporters 1/2 (OCTN1/2) in hyperuricemic mice. It also suppresses renal activation of TLR4/MyD88/NF-κB signaling and NOD-like receptor family, NLRP3 inflammasome to reduce serum and renal IL-1β levels in hyperuricemic mice with renal inflammation reduction[2].
Animal Research Animal Models Male Kun-Ming strain of mice
Dosages 10, 20 and 40 mg/kg
Administration by oral gavage

Chemical Information & Solubility

Molecular Weight 295.38 Formula

C19H21NO2
CAS No. 475-83-2 SDF Download Nuciferine SDF
Smiles CN1CCC2=CC(=C(C3=C2C1CC4=CC=CC=C43)OC)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 7 mg/mL ( (23.69 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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