Cepharanthine

Cepharanthine is a biscoclaurine alkaloid extracted from S. cepharantha that is cationic and amphipathic and has been reported to decrease the fluidity of biological membranes.¹ It exhibits antiparasitic, antimalarial, antiviral, anti-inflammatory, antimetastatic, and anticancer activities in various cell and animal models.^1,2,3 Cepharanthine can decrease LPS-stimulated expression of TNF-α, IL-6, and IL-1β in macrophages and prevent the activation of NF-κB, ERK, JNK, and p38 MAPK.⁴ It has also been shown to inhibit cell and tumor growth, inducing G₁ phase cell cycle arrest and apoptosis, and decreasing expression of STAT3, Bcl-xL, c-Myc, and cyclin D1 in osteosarcoma models.⁵

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1. Matsuda, K., Hattori, S., Komizu, Y., et al. Cepharanthine inhibited HIV-1 cell-cell transmission and cell-free infection via modification of cell membrane fluidity. Bioorg. Med. Chem. Lett. 24(9), 2115-2117 (2014).

2. Desgrouas, C., Chapus, C., Desplans, J., et al. In vitro antiplasmodial activity of cepharanthine. Malar. J. 13:327, (2014).

3. Rogosnitzky, M., and Danks, R. Therapeutic potential of the biscoclaurine alkaloid, cepharanthine, for a range of clinical conditions. Pharmacol. Rep. 63(2), 337-347 (2011).

4. Huang, H., Hu, G., Wang, C., et al. Cepharanthine, an alkaloid from Stephania cepharantha Hayata, inhibits the inflammatory response in the RAW264.7 cell and mouse models. Inflammation 37(1), 235-246 (2014).

5. Chen, Z., Huang, C., Yang, Y.l., et al. Inhibition of the STAT3 signaling pathway is involved in the antitumor activity of cepharanthine in SaOS2 cells. Acta Pharmacol. Sin. 33(1), 101-108 (2012).