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Epirubicin is an inhibitor of DNA topoisomerase (TOPII) [1].
Epirubicin belongs to the Anthracylines chemical class, it is a sort of DNA topoisomerase poison. It can inhibit the religation step of DNA topology, resulting in stabilization of the 5’ phosphotyrosyl-DNA complex (cleavage complex). These lesions are cytotoxic and lead to activation of the DNA damage response and potentially apoptosis. Because of this, it is usually used in cancer therapy. Unfortunately, it also has genotoxic side effects, including the formation of leukemogenic chromosome translocations [1].
Epirubicin is one of the chemotherapeutic agents used for the treatment of Osteosarcoma. It exhibits growth inhibition of tumors by inducing apoptosis. Conversely, it reduces apoptosis in OS cells by activating NF-κB. It is reported that epirubicin combined with cerulenin can enhance the anti-tumor activity in vitro and in vivo [2].
References:[1] Ian G. Cowell, Caroline A. Austin. Mechanism of Generation of Therapy Related Leukemia in Response to Anti-Topoisomerase II Agents. International Journal of Environmental Research and Public Health. 2012 (9): 2075-2091.[2] Z.L. LIU, G. WANG, Y. SHU, P.A. ZOU, Y. ZHOU and Q.S. YIN. Enhanced antitumor activity of epirubicin combined with cerulenin in osteosarcoma. Molecular Medicine Reports. 2012 (5): 326-330.
Cell lines
Human-liver derived hepatoma G2 cells (Hep G2 cells)
Reaction Conditions
0 ~ 12 μg/ml epirubicin HCl for 24, 48 or 72 h incubation
Applications
Epirubicin HCl produced a concentration- and time-dependent cytotoxicity to Hep G2 cells. The mechanism of cytotoxicity of epirubicin HCl (IC50 value of 1.6 μg/ml within 24 h) appeared to involve a production of free radical species since activities of free radical scavenging enzymes (SOD, catalase, Se-dependent GPx) were increased.
Animal models
Nude mice xenografted with human breast carcinoma cell line R-27
Dosage form
3.5 or 7 mg/kg
Administered intravenously every 4 d for 3 times
Epirubicin treatment alone suppressed tumor growth in a dose-dependent manner. At a dose of 3.5 mg/kg, epirubicin alone suppressed tumor mass of human breast tumor xenograft R-27 by 74.4 %.
Note
The technical data provided above is for reference only.
References:
1. Ozkan A, Fişkin K. Epirubicin HCl toxicity in human-liver derived hepatoma G2 cells. Polish Journal of Pharmacology, 2004, 56(4): 435-444.
2. Asanuma F, Yamada Y, Kawamura E, et al. Antitumor activity of paclitaxel and epirubicin in human breast carcinoma, R-27. Folia Microbiologica (Praha), 1998, 43(5): 473-474.
