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MSN8C：一种新型拓扑异构酶 II 催化抑制剂，有望用于抗肿瘤应用。

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

机构信息

Department of Pharmacy, Sun Yat-sen Memorial Hospital, Sun Yat-sen University, Guangzhou 510120, China.

School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.

出版信息

Molecules. 2023 Jul 24;28(14):5598. doi: 10.3390/molecules28145598.

DOI:10.3390/molecules28145598
PMID:37513470
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10383749/
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.

摘要

MSN8C，曼森酮 E 的类似物，已被鉴定为一种新型的人源拓扑异构酶 II 的催化抑制剂，可诱导肿瘤消退，与 VP-16（依托泊苷）不同。MSN8C 处理对体外的 11 个人类肿瘤细胞系表现出显著的抗增殖活性。它对 HL-60/MX2 细胞系特别有效，该细胞系对拓扑异构酶 II 毒物有抗性。MSN8C 对 HL-60/MX2 中的拓扑异构酶 II 的抗性因子（RF）为 1.7，远低于传统的拓扑异构酶 II 毒物。此外，鉴于其在 A549 肿瘤异种移植模型中表现出的强大的抗肿瘤功效和低毒性，MSN8C 已被鉴定为抗肿瘤应用的有前途的候选药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d53/10383749/f1fc0f556f5c/molecules-28-05598-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d53/10383749/df0103c57bb5/molecules-28-05598-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d53/10383749/9dcff52716b4/molecules-28-05598-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d53/10383749/13d4e898b112/molecules-28-05598-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d53/10383749/f1fc0f556f5c/molecules-28-05598-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d53/10383749/df0103c57bb5/molecules-28-05598-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d53/10383749/9dcff52716b4/molecules-28-05598-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d53/10383749/13d4e898b112/molecules-28-05598-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d53/10383749/f1fc0f556f5c/molecules-28-05598-g004.jpg

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