An anthracycline antitumor antibiotic
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].
参考文献:
[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 experiment: | Hep G2 cells (500 cells/well, monolayer) are plated in a 96-well plate. The next day the cells are treated with Epirubicin in the medium. At the end of the incubation periods, 15% volume of MTT dye solution is added. After 1 hr of incubation at 37°C, an equal volume of solubilization/stop solution (dimethylsul-foxide) is added to each well for an additional 1 hr incubation. The absorbance of the reaction solution at 570 nm is recorded. |
参考文献: [1]. Cersosimo RJ, et al. Epirubicin: a review of the pharmacology, clinical activity, and adverse effects of an adriamycin analogue. J Clin Oncol. 1986 Mar;4(3):425-39. | |
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