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Cepharanthine

MCE China：Cepharanthine

Brand：MedChemExpress (MCE)

Cat. No.HY-N6972

CAS：481-49-2

Purity：99.91%

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

Shipping：Room temperature in continental US; may vary elsewhere.

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. 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.

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].

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].

IC50 & Target：CYP3A4 16.29 μM (IC50) CYP2E1 25.62 μM (IC50) CYP2C9 24.57 μM (IC50)

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References：

[1]. Hijikata A, et al. Evaluating cepharanthine analogues as natural drugs against SARS-CoV-2. FEBS Open Bio. 2022;12(1):285-294  [Content Brief]

[2]. Shen LW, et.al. Cepharanthine sensitizes human triple negative breast cancer cells to chemotherapeutic agent epirubicin via inducing cofilin oxidation-mediated mitochondrial fission and apoptosis. Acta Pharmacol Sin. 2022 Jan;43(1):177-193.  [Content Brief]

[3]. Ikeda R, et.al. Cepharanthine potently enhances the sensitivity of anticancer agents in K562 cells. Cancer Sci. 2005 Jun;96(6):372-6.  [Content Brief]

[4]. Zhang X, et.al. In vitro inhibitory effects of cepharanthine on human liver cytochrome P450 enzymes. Pharm Biol. 2020 Dec;58(1):247-252.  [Content Brief]

[5]. Hua P, et.al. Cepharanthine induces apoptosis through reactive oxygen species and mitochondrial dysfunction in human non-small-cell lung cancer cells. Biochem Biophys Res Commun. 2015 May 1;460(2):136-42.  [Content Brief]

[6]. Desgrouas C, et.al. In vitro antiplasmodial activity of cepharanthine. Malar J. 2014 Aug 22;13:327.  [Content Brief]

[7]. Murakami K, et.al. The prevention of lipopolysaccharide-induced pulmonary vascular injury by pretreatment with cepharanthine in rats. Am J Respir Crit Care Med. 2000 Jan;161(1):57-63.  [Content Brief]

[8]. Wei XY, et,al. Antinociceptive activities and mechanism of action of Cepharanthine. Biochem Biophys Res Commun. 2022 Jul 23;614:219-224.  [Content Brief]