Background:

Aclacinomycin A is a dual inhibitor of topoisomerase I and II [1]. Aclacinomycin A is an anticancer drug which can reduce the tumor with minimal damage to normal cells. Aclacinomycin A shows potency against a wide variety of solid tumours and haematological malignancies. In A549, HepG2 and MCF-7 cells, Aclacinomycin A shows cytotoxic activity with IC50 values of 0.27μM, 0.32μM and 0.62μM, respectively. Aclacinomycin A induces cell apoptosis in these cells and the effects change to be necrosis when the incubation time is prolonged. Aclacinomycin A is demonstrated to increase the activity of both caspase-3 and caspase-8, thus inducing the activation of PARP. Apart from that, as an inhibitor of opoisomerases, Aclacinomycin A is found to induce DNA damage in V79 and irs-2 cells. Aclacinomycin A is used to treat acute leukaemias, lymphomas and other solid tumors through its inhibition of topo II [1, 2].

参考文献:
[1] Hajji N, Mateos S, Pastor N, Domínguez I, Cortés F.  Induction of genotoxic and cytotoxic damage by aclarubicin, a dual topoisomerase inhibitor. Mutat Res. 2005 May 2;583(1):26-35.[2] Rogalska A, Szwed M, Jó wiak Z. Aclarubicin-induced apoptosis and necrosis in cells derived from human solid tumours. Mutat Res. 2010 Jul 19;700(1-2):1-10.