1. Autophagy Anti-infection Metabolic Enzyme/Protease Apoptosis
  2. Autophagy 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.

For research use only. We do not sell to patients.

CAS No. : 481-49-2

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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Cepharanthine:

Top Publications Citing Use of Products

    Cepharanthine purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Jan 22;23(1):103.  [Abstract]

    Cepharanthine (CPE) (2–5 μM) dose-dependently inhibited the proliferation of 143B cells.

    Cepharanthine purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Jan 22;23(1):103.  [Abstract]

    Cepharanthine (CPE) (2–5 μM) enhanced its inhibitory effects on arginine uptake in 143B cells with increasing concentration.

    Cepharanthine purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Jan 22;23(1):103.  [Abstract]

    Cepharanthine (CPE) (2–5 μM; 48 h) pretreatment significantly downregulated CD206 expression and upregulated CD86 expression in THP1-derived macrophages in a dose-dependent manner.

    Cepharanthine purchased from MedChemExpress. Usage Cited in: Virol J. 2025 Jun 4;22(1):181.  [Abstract]

    Cepharanthine (CPE) (0.33-3 nM; 24 h) dose-dependently suppressed protein levels of the viral PB2 in A549 cells.

    Cepharanthine purchased from MedChemExpress. Usage Cited in: Virol J. 2025 Jun 4;22(1):181.  [Abstract]

    Cepharanthine (CPE) (0.33-3 nM; 24 h) significantly reduced the expression of the IAV M2 protein in MDCK cells.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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)

    Cellular Effect
    Cell Line Type Value Description References
    A-431 ED50
    2.1 μg/mL
    Compound: 11
    Cytotoxicity against human A431 cells after 3 days by sulforhodamine B assay
    Cytotoxicity against human A431 cells after 3 days by sulforhodamine B assay
    [PMID: 8450319]
    A549 IC50
    5 μM
    Compound: 7
    Cytotoxicity against human A549 cells after 48 hrs by MTS assay
    Cytotoxicity against human A549 cells after 48 hrs by MTS assay
    [PMID: 23621840]
    A673 GI50
    4.5 μM
    Compound: Cepheranthine
    Antiproliferative activity against human A673 assessed as cell growth inhibition after 48 hrs by SRB assay
    Antiproliferative activity against human A673 assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 33226219]
    HCC1806 GI50
    7.2 μM
    Compound: Cepheranthine
    Antiproliferative activity against human HCC1806 assessed as cell growth inhibition after 48 hrs by SRB assay
    Antiproliferative activity against human HCC1806 assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 33226219]
    HCC1937 GI50
    6 μM
    Compound: Cepheranthine
    Antiproliferative activity against human HCC1937 assessed as cell growth inhibition after 48 hrs by SRB assay
    Antiproliferative activity against human HCC1937 assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 33226219]
    HCC70 GI50
    5.8 μM
    Compound: Cepheranthine
    Antiproliferative activity against human HCC70 assessed as cell growth inhibition after 48 hrs by SRB assay
    Antiproliferative activity against human HCC70 assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 33226219]
    HEK-293T CC50
    2.1 μM
    Compound: 3; cep
    Cytotoxicity against HEK293T cells assessed as reduction in cell viability by CellTiter-Glo assay
    Cytotoxicity against HEK293T cells assessed as reduction in cell viability by CellTiter-Glo assay
    [PMID: 37043739]
    HL-60 IC50
    9.2 μM
    Compound: 7
    Cytotoxicity against human HL60 cells after 48 hrs by MTS assay
    Cytotoxicity against human HL60 cells after 48 hrs by MTS assay
    [PMID: 23621840]
    HT-1080 ED50
    6.1 μg/mL
    Compound: 11
    Cytotoxicity against human HT1080 cells after 3 days by sulforhodamine B assay
    Cytotoxicity against human HT1080 cells after 3 days by sulforhodamine B assay
    [PMID: 8450319]
    HeLa IC50
    1.53 μM
    Compound: Cepharanthine
    Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
    Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
    [PMID: 29624387]
    KB ED50
    5.9 μg/mL
    Compound: 11
    Cytotoxicity against human KB cells after 3 days by sulforhodamine B assay
    Cytotoxicity against human KB cells after 3 days by sulforhodamine B assay
    [PMID: 8450319]
    KB ED50
    9700 nM
    Compound: 12
    Cytotoxicity against human KB cells after 72 hrs by SRB assay
    Cytotoxicity against human KB cells after 72 hrs by SRB assay
    [PMID: 9917283]
    KB-V1 ED50
    0.9 μg/mL
    Compound: 11
    Cytotoxicity against human KBV1 cells after 3 days by sulforhodamine B assay
    Cytotoxicity against human KBV1 cells after 3 days by sulforhodamine B assay
    [PMID: 8450319]
    LNCaP ED50
    5.6 μg/mL
    Compound: 11
    Cytotoxicity against human LNCAP cells after 3 days by sulforhodamine B assay
    Cytotoxicity against human LNCAP cells after 3 days by sulforhodamine B assay
    [PMID: 8450319]
    MCF7 IC50
    2.9 μM
    Compound: 7
    Cytotoxicity against human MCF7 cells after 48 hrs by MTS assay
    Cytotoxicity against human MCF7 cells after 48 hrs by MTS assay
    [PMID: 23621840]
    MDA-MB-231 GI50
    5.3 μM
    Compound: Cepheranthine
    Antiproliferative activity against human MDA-MB-231 assessed as cell growth inhibition after 48 hrs by SRB assay
    Antiproliferative activity against human MDA-MB-231 assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 33226219]
    MDA-MB-453 GI50
    5.5 μM
    Compound: Cepheranthine
    Antiproliferative activity against human MDA-MB-453 assessed as cell growth inhibition after 48 hrs by SRB assay
    Antiproliferative activity against human MDA-MB-453 assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 33226219]
    MOLT-4 CC50
    10 μg/mL
    Compound: CEP, Cepharanthine
    Cytotoxicity against human MOLT4 cells assessed as cell growth inhibition after 24 hrs by MTT assay
    Cytotoxicity against human MOLT4 cells assessed as cell growth inhibition after 24 hrs by MTT assay
    [PMID: 24704028]
    P388 ED50
    0.3 μg/mL
    Compound: 11
    Cytotoxicity against mouse P388 cells after 2 days by sulforhodamine B assay
    Cytotoxicity against mouse P388 cells after 2 days by sulforhodamine B assay
    [PMID: 8450319]
    SJRH30 GI50
    3.8 μM
    Compound: Cepheranthine
    Antiproliferative activity against human SJRH30 assessed as cell growth inhibition after 48 hrs by SRB assay
    Antiproliferative activity against human SJRH30 assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 33226219]
    SK-MEL-2 ED50
    14.5 μg/mL
    Compound: 11
    Cytotoxicity against human SK-MEL-2 cells after 3 days by sulforhodamine B assay
    Cytotoxicity against human SK-MEL-2 cells after 3 days by sulforhodamine B assay
    [PMID: 8450319]
    SMMC-7721 IC50
    9.9 μM
    Compound: 7
    Cytotoxicity against human SMMC7721 cells after 48 hrs by MTS assay
    Cytotoxicity against human SMMC7721 cells after 48 hrs by MTS assay
    [PMID: 23621840]
    SW480 IC50
    4.7 μM
    Compound: 7
    Cytotoxicity against human SW480 cells after 48 hrs by MTS assay
    Cytotoxicity against human SW480 cells after 48 hrs by MTS assay
    [PMID: 23621840]
    U-937 IC50
    > 50 μM
    Compound: 8, NSC 623442
    Cytotoxicity against human U937 cells after 24 hrs by alamar blue assay
    Cytotoxicity against human U937 cells after 24 hrs by alamar blue assay
    [PMID: 22766217]
    Vero CC50
    > 50 μM
    Compound: Cepharanthine
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    10.1101/2020.03.20.999730
    Vero IC50
    4.47 μM
    Compound: Cepharanthine
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    10.1101/2020.03.20.999730
    Vero C1008 EC50
    0.98 μM
    Compound: Cepharanthine
    Antiviral activity against SARS-Co-V-2 infected in Vero E6 cells assessed as reduction in viral replication
    Antiviral activity against SARS-Co-V-2 infected in Vero E6 cells assessed as reduction in viral replication
    [PMID: 37229831]
    ZR-75-1 ED50
    1.2 μg/mL
    Compound: 11
    Cytotoxicity against human ZR-75-1 cells after 3 days by sulforhodamine B assay
    Cytotoxicity against human ZR-75-1 cells after 3 days by sulforhodamine B assay
    [PMID: 8450319]
    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.

    • Molarity Calculator

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    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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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
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    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: 99.87%

    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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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Cat. No.:
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