1. Anti-infection Metabolic Enzyme/Protease Apoptosis
  2. SARS-CoV Cytochrome P450 Apoptosis Parasite
  3. Cepharanthine

Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM. Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model. Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects.

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Cepharanthine Chemical Structure

Cepharanthine Chemical Structure

CAS No. : 481-49-2

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Description

Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM[1]. Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model[2][3]. Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects[4][5][6][7][8].

IC50 & Target[4]

CYP3A4

16.29 μM (IC50)

CYP2E1

25.62 μM (IC50)

CYP2C9

24.57 μM (IC50)

In Vitro

Cepharanthine (CEP) (2 μM, 48 h) inhibits cell viability and colony formation and induces apoptosis via the mitochondrial pathway in human TNBC cells[2].
Cepharanthine (2 μM, 48 h) Combinates with Epirubicin (HY-13624) impairs mitochondrial function and causes mitochondrial fission and apoptosis in MDA-MB-231 cells[2].
Cepharanthine (5 μM, 24 h) potently enhances the sensitivity of anticancer agents Doxorubicin (HY-15142A) and Vincristine (HY-N0488) and enhanced apoptosis induced by anticancer agents in K562 cells[3].
Cepharanthine (10-50 μM, 0.5-1 h) changes the distribution of Doxorubicin (HY-15142A) from cytoplasmic vesicles to nucleoplasm in K562 cells by inhibiting the acidification of cytoplasmic organellesin[3].
Cepharanthine (0-50 μM, 30 min) shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4,CYP2E1 and CYP2C9in vitro[4].
Cepharanthine(0-4 μM, 48 hours) blocks P. falciparum development in ring stage with IC50s of 3.059, 0.927, 2.276, and 1.803 μM for FCM29, W2, 3D7 and K1, respectively[5].

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

Apoptosis Analysis[2]

Cell Line: MDAMB-231 and BT549 cells
Concentration: 2 μM
Incubation Time: 48 h
Result: Cepharanthine alone minimally increased apoptosis (~5% to ~10%), whereas combinated with Epirubicin (HY-13624) markedly increased apoptosis (~50%).

Western Blot Analysis[2]

Cell Line: MDAMB-231 cells
Concentration: 2 μM
Incubation Time: 48 h
Result: Combinated with Epirubicin (HY-13624) markedly resulted in oxidation of the actin-remodeling protein cofilin, which promoted formation of an intramolecular disulfide bridge between Cys39, Cys80 and Ser3 dephosphorylation, leading to mitochondria translocation of cofilin.
Combinated with Epirubicin (HY-13624) induced mitochondrial fission in MDA-MB-231 cells.

Immunofluorescence[3]

Cell Line: K562 cells or MIA-PaCa-2 cells
Concentration: 10,20,25,50 μM
Incubation Time: 0.5 h or 1 h
Result: Made the intracellular localization of Doxorubicin (HY-15142A) in cytoplasmic vesicles shifted to the nucleoplasm.
Decreased red AO (weakly basic fluorescence probe) fluorescence by dose-dependent mannar in K562 cells.

Cell Viability Assay[5]

Cell Line: P. falciparum cultivated in type A+ human erythrocytes
Concentration: 2 μM
Incubation Time: 48 h
Result: Blocked P. falciparum development in ring stage with IC50s of 3.059, 0.927, 2.276, and 1.803 μM for FCM29, W2, 3D7 and K1, respectively.
In Vivo

Cepharanthine (12 mg/kg, i.p., once daily for 36 days) enhances the therapeutic efficacy of Epirubicin (HY-13624) in MDA-MB-231 cell xenografts[2].
Cepharanthine (10 mg/kg, i.p., single dose) prevents LPS-induced pulmonary vascular injury in rats by inhibiting leukocyte activation[6].
Cepharanthine (CE)(10 mg/kg, i.p., single dose) exerts anti-inflammatory effects via NF-kB inhibition in a LPS-induced rat model of systemic inflammation[7].
Cepharanthine (20-180 mg/kg, i.p.) results in a dose-dependent antinociceptive effect with an ED50 value of 24.5 mg/kg in mice pain models[8].

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

Animal Model: MDA-MB-231 cell xenografts in mice[1]
Dosage: 12 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 36 days
Result: Combinated with Epirubicin (HY-13624) greatly enhanced the therapeutic efficacy compared with administration of either drug alone.
Animal Model: LPS-induced pulmonary vascular injury in male Wistar rats[6]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Decreased LPS-induced pulmonary vascular injury.
Significantly inhibited the increases in plasma tumor necrosis factor-a (TNF-a) concentrations.
Animal Model: LPS-induced Wistar rat model of systemic inflammation[7]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Significantly inhibited the increase in LPS-induced IL-6, TNF-α and nitrate/nitrite levels.
Reduced interstitial edema and inflammatory cell compared with the control group.
Reduced pathologic abnormalities, such as vacuolization, dot necrosis, striped necrosis, and bridging necrosis appeared, and inflammatory cells compared with the control group.
group compared with the LPS group.
Animal Model: Mice pain models in Kunming (KM) strain male and female mice [8]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Resulted in a dose-dependent antinociceptive effect with an ED50 value of 24.5 mg/kg in mice pain models.
Significantly decreased the intestinal propulsion with maximal inhibition at 33.6%.
Clinical Trial
Molecular Weight

606.71

Formula

C37H38N2O6

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

[H][C@]12N(C)CCC(C1=C3)=CC(OC)=C3OC4=C5C(OCO5)=CC6=C4[C@](N(C)CC6)([H])CC(C=C7)=CC=C7OC8=C(OC)C=CC(C2)=C8

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (82.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6482 mL 8.2412 mL 16.4823 mL
5 mM 0.3296 mL 1.6482 mL 3.2965 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.12 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 6.02 mg/mL (9.92 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  15% Cremophor EL    85% Saline

    Solubility: 6.02 mg/mL (9.92 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.91%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6482 mL 8.2412 mL 16.4823 mL 41.2058 mL
5 mM 0.3296 mL 1.6482 mL 3.2965 mL 8.2412 mL
10 mM 0.1648 mL 0.8241 mL 1.6482 mL 4.1206 mL
15 mM 0.1099 mL 0.5494 mL 1.0988 mL 2.7471 mL
20 mM 0.0824 mL 0.4121 mL 0.8241 mL 2.0603 mL
25 mM 0.0659 mL 0.3296 mL 0.6593 mL 1.6482 mL
30 mM 0.0549 mL 0.2747 mL 0.5494 mL 1.3735 mL
40 mM 0.0412 mL 0.2060 mL 0.4121 mL 1.0301 mL
50 mM 0.0330 mL 0.1648 mL 0.3296 mL 0.8241 mL
60 mM 0.0275 mL 0.1374 mL 0.2747 mL 0.6868 mL
80 mM 0.0206 mL 0.1030 mL 0.2060 mL 0.5151 mL
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Cepharanthine
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