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MSN8C: A Promising Candidate for Antitumor Applications as a Novel Catalytic Inhibitor of Topoisomerase II
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...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10383749/ https://www.ncbi.nlm.nih.gov/pubmed/37513470 http://dx.doi.org/10.3390/molecules28145598 |
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author | Ou, Jie-Bin Huang, Wei-Hao Liu, Xing-Zi Dai, Guo-Yao Wang, Lu Huang, Zhi-Shu Huang, Shi-Liang |
author_facet | Ou, Jie-Bin Huang, Wei-Hao Liu, Xing-Zi Dai, Guo-Yao Wang, Lu Huang, Zhi-Shu Huang, Shi-Liang |
author_sort | Ou, Jie-Bin |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-10383749 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-103837492023-07-30 MSN8C: A Promising Candidate for Antitumor Applications as a Novel Catalytic Inhibitor of Topoisomerase II Ou, Jie-Bin Huang, Wei-Hao Liu, Xing-Zi Dai, Guo-Yao Wang, Lu Huang, Zhi-Shu Huang, Shi-Liang Molecules Article 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. MDPI 2023-07-24 /pmc/articles/PMC10383749/ /pubmed/37513470 http://dx.doi.org/10.3390/molecules28145598 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Ou, Jie-Bin Huang, Wei-Hao Liu, Xing-Zi Dai, Guo-Yao Wang, Lu Huang, Zhi-Shu Huang, Shi-Liang MSN8C: A Promising Candidate for Antitumor Applications as a Novel Catalytic Inhibitor of Topoisomerase II |
title | MSN8C: A Promising Candidate for Antitumor Applications as a Novel Catalytic Inhibitor of Topoisomerase II |
title_full | MSN8C: A Promising Candidate for Antitumor Applications as a Novel Catalytic Inhibitor of Topoisomerase II |
title_fullStr | MSN8C: A Promising Candidate for Antitumor Applications as a Novel Catalytic Inhibitor of Topoisomerase II |
title_full_unstemmed | MSN8C: A Promising Candidate for Antitumor Applications as a Novel Catalytic Inhibitor of Topoisomerase II |
title_short | MSN8C: A Promising Candidate for Antitumor Applications as a Novel Catalytic Inhibitor of Topoisomerase II |
title_sort | msn8c: a promising candidate for antitumor applications as a novel catalytic inhibitor of topoisomerase ii |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10383749/ https://www.ncbi.nlm.nih.gov/pubmed/37513470 http://dx.doi.org/10.3390/molecules28145598 |
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