Bisantrene, recognized for its potent antitumor properties, achieves its cytotoxic effects through DNA intercalation. It specifically interacts with eukaryotic type II topoisomerases and is also identified as a substrate for MDR1[1][2][3][4]. Bisantrene enhances DNase I cleavage at oligopurine-oligopyrimidine sequences and marginally diminishes the cleavage at alternating purine-pyrimidine sequences[1]. Bisantrene acts as an inhibitor of [3H]uridine integration into RNA and [3H]thymidine integration into DNA[2].
Bisantrene/比生群 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Yeast DNA topoisomerase II (from S. cerevisiae)
1.596 ± 0.096 µM
30 min
To evaluate the inhibitory effect of Bisantrene on yeast DNA topoisomerase II, results showed it was more effective against the yeast enzyme than the human counterpart.
Sci Rep. 2025 Mar 18;15(1):9311
Bisantrene/比生群 动物研究
Animal study
Bisantrene's efficacy spans a dosage range from 1.56 to 150 mg/kg, varying according to the treatment's frequency, administration method, and schedule, as well as the tumor model utilized. Pre-treatment with Bisantrene at doses of 25, 50, and 100 mg/kg, administered intraperitoneally once, in conjunction with macrophages, demonstrates an antitumor effect in mice injected with P815 tumor cells[3]. Administered intravenously in a single dose ranging from 10 to 150 mg/kg, Bisantrene causes leukopenia in Neo mice in a dose-dependent manner. Both B cells and macrophages are susceptible to the toxic effects of Bisantrene[4].
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