1. Neuronal Signaling Apoptosis Immunology/Inflammation NF-κB MAPK/ERK Pathway
  2. Cholinesterase (ChE) Apoptosis Bcl-2 Family Caspase Interleukin Related TNF Receptor Toll-like Receptor (TLR) MyD88 NF-κB p38 MAPK
  3. Chuanbeinone

Chuanbeinone (22-Epidelavinone) is an orally active alkaloid found in Fritillaria pallidiflora. Chuanbeinone shows cytotoxicity against mutiple cancer cells and can induces apoptosis and S phase arrest. Chuanbeinone downregulates Bcl-2, upregulates Bax, and activates caspase-3. Chuanbeinone exerts anti-inflammatory and antitussive effects by reducing pro-inflammatory cytokine (IL-1β, IL-6 and TNF-α) production and mRNA expression, and inhibiting TRIF-, MyD88-, NF-κB-, and MAPK-dependent signaling pathways. Chuanbeinone inhibits AChE and BChE with IC50 values of 7.7 and 0.7 μM. Chuanbeinone can be used for the researches of lung carcinoma, cough, inflammatory diseases.

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Chuanbeinone

Chuanbeinone Chemical Structure

CAS No. : 103530-47-8

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Description

Chuanbeinone (22-Epidelavinone) is an orally active alkaloid found in Fritillaria pallidiflora. Chuanbeinone shows cytotoxicity against mutiple cancer cells and can induces apoptosis and S phase arrest. Chuanbeinone downregulates Bcl-2, upregulates Bax, and activates caspase-3. Chuanbeinone exerts anti-inflammatory and antitussive effects by reducing pro-inflammatory cytokine (IL-1β, IL-6 and TNF-α) production and mRNA expression, and inhibiting TRIF-, MyD88-, NF-κB-, and MAPK-dependent signaling pathways. Chuanbeinone inhibits AChE and BChE with IC50 values of 7.7 and 0.7 μM. Chuanbeinone can be used for the researches of lung carcinoma, cough, inflammatory diseases[1][2][3][4].

IC50 & Target[1]

BChE

0.7 μM (IC50)

AChE

7.7 μM (IC50)

Bax

 

Bcl-2

 

Caspase 3

 

IL-1β

 

IL-6

 

In Vitro

Chuanbeinone inhibits the growth of LLC, A2780, HepG2, and A549 cells with IC50 values of 10.51 μg/mL, 18.16 μg/mL, 37.97 μg/mL, and 43.74 μg/mL, respectively[1].
Chuanbeinone (5-15 μg/mL; 48 h) induces dose-dependent apoptosis in LLC cells, with apoptotic rates of 12.8% to 64.8%[1].
Chuanbeinone (10 μg/mL; 24-72 h) induces time-dependent S phase arrest and decreases the cells in the G0/G1 phase[1].
Chuanbeinone (5-15 μg/mL; 48 h) downregulates Bcl-2, upregulates Bax, and activates caspase-3 in LLC cells[1].
Chuanbeinone (20-100 μM; 24 h) reduces RAW 264.7 cell viability[2].
Chuanbeinone (5-20 μM; 24 h, co-treated with 0.2 μg/mL LPS) exerts anti-inflammatory effects on LPS (HY-D1056)-induced RAW 264.7 cells by reducing pro-inflammatory cytokine production and mRNA expression, and inhibiting TRIF-, MyD88-, NF-κB-, and MAPK-dependent signaling pathways[2].
Chuanbeinone inhibits AChE with an IC50 of 7.7 ± 0.001 μM and BChE with an IC50 of 0.7 ± 0.001 μM, and exhibits 70.7 ± 3.3% enzyme inhibition at 100
μM[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: LLC
Concentration: 10 μg/mL
Incubation Time: 24, 48, 72 h
Result: Caused time-dependent accumulation of LLC cells in the S phase, accompanied by a decrease in G0/G1 phase cells.
Increased the sub-G1 population (apoptotic DNA fragmentation) over time.

Western Blot Analysis[1]

Cell Line: LLC
Concentration: 5, 10, 15 μg/mL
Incubation Time: 48 h
Result: Reduced expression of antiapoptotic Bcl-2 and increased expression of proapoptotic Bax (elevating the Bax/Bcl-2 ratio).
Increased levels of cleaved caspase-3 in a dose-dependent manner.

ELISA Assay[2]

Cell Line: RAW 264.7 cells
Concentration: 5, 10, 20 μg/mL
Incubation Time: 24 h co-treated with 0.2 μg/mL LPS
Result: Reduced NO, IL-1β, IL-6 and TNF-α production and mRNA expression.

Western Blot Analysis[2]

Cell Line: RAW 264.7 cells
Concentration: 5, 10, 20 μg/mL
Incubation Time: 24 h co-treated with 0.2 μg/mL LPS
Result: Reduced TRIF, MyD88, NF-κB, and MAPK levels.
In Vivo

Chuanbeinone (10-40 mg/kg; p.o.; daily; 10 days) exhibits significant antitumor activity in LLC-bearing C57BL/6J and S180-bearing ICR mice, inducing tumor growth inhibition, apoptosis, and angiogenesis inhibition[1].
Chuanbeinone (1.5-3.0 mg/kg; p.o.; single dose) exhibits dose-dependent antitussive effects in ammonia-induced cough in Mus musculus, with 3.0 mg/kg producing a 60.49% inhibition of cough frequency[4].
Chuanbeinone (3.0 mg/kg; p.o.; single dose) does not exhibit significant expectorant activity in the tracheal phenol red secretion model in mice[4].
Chuanbeinone (1.5-3.0 mg/kg; p.o.; single dose) exhibits anti-inflammatory effects at 3.0 mg/kg in xylene-induced ear edema in Mus musculus[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: LLC-bearing C57BL/6J and S180-bearing ICR mice (male, 18-22 g)[1]
Dosage: 10, 20, 40 mg/kg
Administration: P.o.; daily; 10 days
Result: Achieved 40.97% and 39.15% tumor growth inhibition rate.
Increased TUNEL-positive apoptotic cell number in tumor tissues.
Reduced microvessel density via decreased CD31 expression.
Increased cleaved caspase-3 expression in tumor tissues compared to the control group.
Animal Model: Kunming mice (either sex, 18-22 g)[4]
Dosage: 1.5, 3.0 mg/kg
Administration: P.o.; single dose
Result: Increased cough latent period to 58.20 ± 10.64 s at 3.0 mg/kg.
Reduced cough frequency to 24.30 ± 4.84 (60.49% inhibition) at 3.0 mg/kg.
Reduced cough frequency to 30.16 ± 5.29 (52.68% inhibition) at 1.5 mg/kg.
Molecular Weight

413.64

Formula

C27H43NO2

CAS No.
SMILES

C[C@@]12[C@]3([H])[C@](CC([C@@]1([H])C[C@H](CC2)O)=O)([H])[C@@]4([H])[C@@]([C@@]5([H])[C@@]([C@H]([C@]6([H])N(C[C@H](CC6)C)C5)C)([H])CC4)([H])C3

Structure Classification
Initial Source
Shipping

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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