MSN8C: A Promising Candidate for Antitumor Applications as a Novel Catalytic Inhibitor of Topoisomerase II.

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.

• Authors: Jie-Bin Ou, Wei-Hao Huang, Xing-Zi Liu, Guo-Yao Dai, Lu Wang, Zhi-Shu Huang, Shi-Liang Huang
• Journal: Molecules (Basel, Switzerland) (Molecules) Vol. 28 Issue 14 (Jul 24 2023) ISSN: 1420-3049 [Electronic] Switzerland
• PMID: 37513470 (Publication Type: Journal Article)

Chemical References

• DNA Topoisomerases, Type II
• Topoisomerase II Inhibitors
• Etoposide
• Antineoplastic Agents

Topics

• Humans
• DNA Topoisomerases, Type II (metabolism)
• Topoisomerase II Inhibitors (pharmacology)
• Etoposide (pharmacology)
• Cell Line, Tumor
• HL-60 Cells
• Antineoplastic Agents (pharmacology)