Ellipticine hydrochloride (NSC-71795 (hydrochloride)) is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.

Ellipticine是一种强效的抗肿瘤剂，其作用机制多样。Ellipticine的抗肿瘤、诱变和细胞毒性活性被认为是通过插入DNA和抑制DNA拓扑异构酶II活性来实现的。另一种作用模式是通过其与细胞色素P450（CYP）和过氧化酶的氧化作用介导的形成共价DNA加合物[1]。Ellipticine还能作为生物转化酶的抑制剂或诱导剂，从而调节自身的代谢，导致其遗传毒性和药理学效应。用Ellipticine处理细胞会抑制细胞生长和增殖，这一效应与两种共价的Ellipticine衍生的DNA加合物的形成有关[2]。

Ellipticine处理在多个健康器官(肝脏、肾脏、肺、脾脏、乳腺、心脏和大脑)以及乳腺腺癌的DNA中导致ellipticine衍生的DNA加成产物生成。这些腺癌中ellipticine衍生的DNA加成产物的水平几乎是正常健康乳腺组织的2倍。在用ellipticine处理的大鼠肝脏中诱导表达的细胞色素b5蛋白质表明，细胞色素b5可能调节CYP介导的ellipticine生物活化和解毒[3]。

The cytotoxicity of ellipticine is determined by MTT test. Ellipticine is dissolved in DMSO (1 mM) and diluted in culture medium to final concentrations of 0, 0.1, 1, 5 or 10 μM. Cells in exponential growth are seeded at 1×104 per well in a 96-well microplate. After incubation the MTT solution is added, the microplates are incubated for 4 hours and cells lysed in 50% N,N-dimethylformamide containing 20% of sodium dodecyl sulfate (SDS), pH 4.5. The absorbance at 570 nm is measured. The mean absorbance of medium controls is subtracted as a background. The viability of control cells is taken as 100% and the values of treated cells are calculated as a percentage of control. The IC50 values are calculated using linear regression of the dose-log response curves[2] .