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Cepharanthine

SKU: orb1224981

Description

Cepharanthine is a biscoclaurine alkaloid inhibiting tumor necrosis factor (TNF)-α-mediated NFκB stimulation, plasma membrane lipid peroxidation and platelet aggregation and suppressing cytokine production.

Images & Validation

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Cepharanthine

Key Properties

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CAS Number481-49-2
MW606.73
Purity>98% (HPLC)
FormulaC37H38N2O6
SMILESCOC1=CC2=C3C=C1OC4=C(OCO5)C5=CC6=C4[C@@](CC7=CC=C(OC(C(OC)=C8)=CC=C8C[C@@]3([H])N(C)CC2)C=C7)([H])N(C)CC6
TargetOthers
SolubilityDMSO: 100 mg/mL (164.82 mM)

Bioactivity

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In Vivo
Animal model: MDA-MB-231 cell xenografts in mice. 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. 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. 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. 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%.
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In Vitro
Apoptosis Analysis 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. 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 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 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.
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Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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O-Methylcepharanoline | NSC 623442

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Cepharanthine (orb1224981)

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