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[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].

[1]Hijikata A, et al. Evaluating cepharanthine analogues as natural drugs against SARS-CoV-2. FEBS Open Bio. 2022;12(1):285-294|[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.|[3]Ikeda R, et.al. Cepharanthine potently enhances the sensitivity of anticancer agents in K562 cells. Cancer Sci. 2005 Jun;96(6):372-6. |[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. |[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. |[6]Desgrouas C, et.al. In vitro antiplasmodial activity of cepharanthine. Malar J. 2014 Aug 22;13:327. |[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. |[8]Wei XY, et,al. Antinociceptive activities and mechanism of action of Cepharanthine. Biochem Biophys Res Commun. 2022 Jul 23;614:219-224.