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Purity: =99.83%
| Targets |
Nuciferine targets multiple receptors in the central nervous system, primarily serotonin (5-HT) and dopamine receptors. It acts as an antagonist at 5-HT2A (IC50=478 nM), 5-HT2B (IC50=1 μM), and 5-HT2C (IC50=131 nM) receptors. It is an inverse agonist at the 5-HT7 receptor (IC50=150 nM). Nuciferine also acts as a partial agonist at the dopamine D2 receptor (EC50=64 nM, Emax=67% of dopamine) and D5 receptor (EC50=2.6 μM), and at the 5-HT6 receptor (EC50=700 nM). It is an agonist at the 5-HT1A receptor (EC50=3.2 μM) and D4 receptor (EC50=2 μM). This multi-target profile is similar to that of atypical antipsychotics like clozapine.
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| ln Vitro |
Similar to aripiprazole (Emax=50% of dopamine), nuciferine is a partial agonist at the DD2 receptor with action (Emax=67% of dopamine). Nuciferine is as effective as clozapine (Nuciferine KB=62 nM; Clozapine KB=20 nM) at blocking Gi activation of dopamine inducers, which is consistent with its partial agonist action, according to Schild regression analysis [1]. Nuciferine, a naturally occurring substance, effectively inhibits the movement of insects. Schistosoma adenalis's basal motility and 5-HT-induced motility can both be successfully inhibited by nuciferine. Nuciferine inhibits Schistosoma at 0.62±0.22 μM and Sm.5HTRL at 0.24±0.04 μM, respectively [2].
In vitro, Nuciferine has demonstrated various biological activities. It acts as a partial agonist at the D2 dopamine receptor, with an Emax of 67% of dopamine, similar to aripiprazole (Emax=50%). Schild regression analysis has shown that Nuciferine is as effective as clozapine (Nuciferine KB=62 nM; Clozapine KB=20 nM) at blocking Gi activation of dopamine inducers. Nuciferine inhibits the growth of MDA-MB-231 and MCF-7 human breast cancer cells by inducing apoptosis and inhibiting proliferation through cell cycle arrest. It is also effective at inhibiting both basal and 5-HT-evoked motility of adult schistosomes. In hyperuricemic models, Nuciferine decreases serum urate levels and inhibits IL-1β secretion. |
| ln Vivo |
In dental animal models related to the effects of antipsychotic drugs, nuciferine expands the apical response and prestimulatory effects of 5-HT2A agonists, replaces the precise stimulation of clozapine, enhances amphetamine-induced locomotor activity, and inhibits phencyclidine Piperidine (PCP)-induced locomotor activity and relieves PCP-induced prepulse inhibition but does not induce catalepsy. In the presence of 1 or 3 mg/kg Nuciferine, cumulative PCP dosages resulted in equivalent replacement to PCP alone. In clozapine-trained animals, a dose-dependent substitution of 1.25 mg/kg Clozapine was observed with 10 mg/kg Nuciferine (80.63% drug lever response), with an ED50 value of 5.42 mg/kg (95% CI 3.09-9.48 mg )/kg), whereas the lower doses tested (0.1 mg/kg-3 mg/kg) failed to produce discriminative cues for clozapine. In addition to eliciting a high number of responses to clozapine suitable levers, 10 mg/kg Nuciferine generated considerable gradient suppression (p<0.001) compared to vehicle control points [1].
In vivo, Nuciferine has been shown to decrease serum urate levels and improve kidney function in potassium oxonate-induced hyperuricemic mice. It also inhibits systemic and renal interleukin-1β (IL-1β) secretion in these mice. Nuciferine has been investigated for its anti-hyperlipidemic effects, although detailed in vivo efficacy data are limited. The compound has been cited in various scientific publications, including studies on its metabolic and anti-inflammatory effects. Further in vivo studies are needed to fully characterize its efficacy in animal models of neurological disorders, cancer, and metabolic diseases. |
| Enzyme Assay |
For affinity determination in non-cellular receptor binding assays, Nuciferine is typically subjected to primary radioligand binding assays. The compound is tested at a single 10 μM concentration to displace 50% of the radioligand at a given receptor target. The assay is performed in a suitable buffer using a radioligand at or near its Kd value. The reaction mixture is incubated for a specified time at room temperature or 37°C, and bound radioligand is separated from free radioligand by filtration or centrifugation. The radioactivity is measured using a scintillation counter, and the percentage of displacement is calculated to determine binding affinity. IC50 and Ki values are derived from competition binding curves using multiple concentrations of Nuciferine.
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| Cell Assay |
For in vitro cell-based studies, Nuciferine is dissolved in DMSO and diluted in cell culture medium to the desired concentrations. Human breast cancer cell lines such as MDA-MB-231 and MCF-7 are cultured in appropriate media and treated with Nuciferine for 24-72 hours. Cell proliferation is assessed using MTT or CellTiter-Glo assays. Apoptosis is evaluated by flow cytometry using Annexin V/PI staining or by detecting caspase activity. Cell cycle analysis is performed by propidium iodide staining followed by flow cytometry. The effect of Nuciferine on signaling pathways can be examined by Western blot analysis of proteins involved in apoptosis and cell cycle regulation, such as Bcl-2, Bax, p21, and cyclin D1.
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| Animal Protocol |
In vivo animal studies with Nuciferine have been conducted in mouse models. For the potassium oxonate-induced hyperuricemic mouse model, mice are treated with potassium oxonate to induce hyperuricemia, followed by administration of Nuciferine. Nuciferine is typically administered orally or intraperitoneally at various doses. Blood samples are collected to measure serum urate levels. Kidney function is assessed by measuring serum creatinine and blood urea nitrogen (BUN). Inflammatory markers such as IL-1β are measured in serum and kidney tissues by ELISA. The effect of Nuciferine on renal pathology is evaluated by histopathological examination of kidney sections.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Nuciferine have not been extensively characterized in the available literature. As a natural alkaloid with a molecular weight of 295.38 g/mol, Nuciferine is expected to have moderate oral bioavailability. It is commonly used as a reference standard in analytical research, indicating that it is stable and can be detected and quantified by HPLC, GC, and MS methods. Detailed PK parameters such as half-life, Cmax, AUC, and protein binding have not been reported and require further investigation. The compound is typically stored under recommended conditions as specified in the Certificate of Analysis.
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| Toxicity/Toxicokinetics |
Toxicological data for Nuciferine are limited, as it is primarily used as a research standard and not as a therapeutic agent. The compound is typically handled with standard laboratory safety precautions. Nuciferine's multi-target receptor profile suggests potential for central nervous system effects, but comprehensive toxicology studies have not been reported. The compound has been studied for its anti-hyperlipidemic and anti-inflammatory effects, which may indicate a favorable safety profile, but formal toxicity assessments in animal models are needed.
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| References |
[1]. Farrell MS, et al. In Vitro and In Vivo Characterization of the Alkaloid Nuciferine. PLoS One. 2016 Mar 10;11(3):e0150602.
[2]. Chan JD, et al. Pharmacological profiling an abundantly expressed schistosome serotonergic GPCR identifies nuciferine as a potent antagonist. Int J Parasitol Drugs Drug Resist. 2016 Dec;6(3):364-370 |
| Additional Infomation |
According to reports, jujubes, Qinghai clams, and other organisms with available data contain lotus leaf alkaloids.
Nuciferine is a natural product alkaloid that serves as a valuable research tool for studying serotonin and dopamine receptor pharmacology. Its multi-target profile resembles that of atypical antipsychotics, making it a useful reference compound in neuropharmacology research. Nuciferine is commonly used as an analytical standard in qualitative, quantitative, and methodological research experiments in HPLC, GC, and MS. It has also been investigated for its anti-cancer, anti-inflammatory, and anti-hyperlipidemic properties, although it is not an FDA-approved drug. Nuciferine continues to be an active area of research for its potential therapeutic applications. |
| Molecular Formula |
C19H21NO2
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|---|---|
| Molecular Weight |
295.3755
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| Exact Mass |
295.157
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| CAS # |
475-83-2
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| PubChem CID |
10146
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
430.7±45.0 °C at 760 mmHg
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| Melting Point |
165.5°C
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| Flash Point |
151.9±17.3 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.597
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| LogP |
4.12
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
401
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O(C([H])([H])[H])C1=C(C([H])=C2C([H])([H])C([H])([H])N(C([H])([H])[H])[C@]3([H])C([H])([H])C4=C([H])C([H])=C([H])C([H])=C4C1=C32)OC([H])([H])[H]
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| InChi Key |
ORJVQPIHKOARKV-OAHLLOKOSA-N
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| InChi Code |
InChI=1S/C19H21NO2/c1-20-9-8-13-11-16(21-2)19(22-3)18-14-7-5-4-6-12(14)10-15(20)17(13)18/h4-7,11,15H,8-10H2,1-3H3/t15-/m1/s1
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| Chemical Name |
(6aR)-1,2-dimethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~5 mg/mL (~16.93 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.11 mg/mL (3.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.1 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.11 mg/mL (3.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.1 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3855 mL | 16.9273 mL | 33.8547 mL | |
| 5 mM | 0.6771 mL | 3.3855 mL | 6.7709 mL | |
| 10 mM | 0.3385 mL | 1.6927 mL | 3.3855 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04148677 | Unknown status | Dietary Supplement: Protoves M1® | Bladder Cancer LUTS Pain |
Cardarelli Hospital | 2019-12-01 |
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