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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...

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Autores principales: Ou, Jie-Bin, Huang, Wei-Hao, Liu, Xing-Zi, Dai, Guo-Yao, Wang, Lu, Huang, Zhi-Shu, Huang, Shi-Liang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
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.
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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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