Datelliptium (chloride hydrochloride)

Datelliptium is an anticancer agent and a derivative of ellipticine (Item No. 18742).¹ It intercalates into DNA and inhibits topoisomerase II in a concentration-dependent manner. Datelliptium also inhibits mitochondrial complex IV, also known as cytochrome c oxidase (IC₅₀ = 70 µM for the potato enzyme).² It inhibits the growth of L1210 leukemia cells (IC₅₀ = 0.076 µM) but is also cytotoxic to primary human hepatocytes (IC₅₀ = 4 µM).^1,3 Datelliptium reduces glycogen synthesis, albumin synthesis, total protein synthesis, gluconeogenesis, triglyceride secretion, and ureogenesis in isolated rat hepatocytes (IC₅₀s = 14.3, 15.4, 3, 28.8, 2.3, and 96.4 µM, respectively).³ It increases survival in several murine models of cancer.¹

WARNING This product is not for human or veterinary use.

1. Auclair, C., Pierre, A., Voisin, E., et al. Physicochemical and pharmacological properties of the antitumor ellipticine derivative 2-(diethylamino-2-ethyl)9-hydroxy ellipticinium-chloride, HCl. Cancer Res. 47(23), 6254-6561 (1987).

2. Dupont, J., Dodin, G., and Schwaller, M.-A. Interactions between ellipticine derivatives and the mitochondrial respiratory chain. Plant Sci. 54(2), 109-115 (1988).

3. Donato, M.T., Goethals, F., Gómez-Lechón, M.J., et al. Toxicity of the antitumoral drug datelliptium in hepatic cells: Use of models in vitro for the prediction of toxicity in vivo. Toxicol. in Vitro 6(4), 295-302 (1992).