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- Title
MSN8C: A Promising Candidate for Antitumor Applications as a Novel Catalytic Inhibitor of Topoisomerase II.
- Authors
Ou, Jie-Bin; Huang, Wei-Hao; Liu, Xing-Zi; Dai, Guo-Yao; Wang, Lu; Huang, Zhi-Shu; Huang, Shi-Liang
- Abstract
MSN8C, an analog of mansonone E, has been identified as a novel catalytic inhibitor of human DNA topoisomerase II that induces tumor regression and differs from VP-16(etoposide). Treatment with MSN8C showed significant antiproliferative activity against eleven human tumor cell lines in vitro. It was particularly effective against the HL-60/MX2 cell line, which is resistant to Topo II poisons. The resistance factor (RF) of MSN8C for Topo II in HL-60/MX2 versus HL-60 was 1.7, much lower than that of traditional Topo II poisons. Furthermore, in light of its potent antitumor efficacy and low toxicity, as demonstrated in the A549 tumor xenograft model, MSN8C has been identified as a promising candidate for antitumor applications.
- Subjects
DNA topoisomerase II; DNA topoisomerase I; DNA topoisomerase inhibitors; CELL lines; POISONS
- Publication
Molecules, 2023, Vol 28, Issue 14, p5598
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules28145598