DNA-Binding and Topoisomerase-I-Suppressing Activities of Novel Vanadium Compound Van-7

Vanadium compounds were studied during recent years to be considered as a representative of a new class of nonplatinum metal anticancer agents in combination to its low toxicity. Here, we found a vanadium compound Van-7 as an inhibitor of Topo I other than Topo II using topoisomerase-mediated superc...

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Main Authors: Xiao-mei Mo, Zhan-fang Chen, Xin Qi, Yan-tuan Li, Jing Li
Format: Article
Language:English
Published: Wiley 2012-01-01
Series:Bioinorganic Chemistry and Applications
Online Access:http://dx.doi.org/10.1155/2012/756374
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author Xiao-mei Mo
Zhan-fang Chen
Xin Qi
Yan-tuan Li
Jing Li
author_facet Xiao-mei Mo
Zhan-fang Chen
Xin Qi
Yan-tuan Li
Jing Li
author_sort Xiao-mei Mo
collection DOAJ
description Vanadium compounds were studied during recent years to be considered as a representative of a new class of nonplatinum metal anticancer agents in combination to its low toxicity. Here, we found a vanadium compound Van-7 as an inhibitor of Topo I other than Topo II using topoisomerase-mediated supercoiled DNA relaxation assay. Agarose gel electrophoresis and comet assay showed that Van-7 treatment did not produce cleavable complexes like HCPT, thereby suggesting that Topo I inhibition occurred upstream of the relegation step. Further studies revealed that Van-7 inhibited Topo I DNA binding involved in its intercalating DNA. Van-7 did not affect the catalytic activity of DNase I even up to100 μM. Van-7 significantly suppressed the growth of cancer cell lines with IC50 at nanomolar concentrations and arrested cell cycle of A549 cells at G2/M phase. All these results indicate that Van-7 is a potential selective Topo I inhibitor with anticancer activities as a kind of Topo I suppressor, not Topo I poison.
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spelling doaj-art-bfad09c1e49b40f0b1d30d9b6a47e9232025-08-20T03:22:39ZengWileyBioinorganic Chemistry and Applications1565-36331687-479X2012-01-01201210.1155/2012/756374756374DNA-Binding and Topoisomerase-I-Suppressing Activities of Novel Vanadium Compound Van-7Xiao-mei Mo0Zhan-fang Chen1Xin Qi2Yan-tuan Li3Jing Li4Key Laboratory of Marine Drugs, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, 5 Yu-Shan Road, Qingdao 266003, ChinaThe Department of Pharmacy, Qingdao Women and Children Hospital, 127 Liao-Yang West Road, Qingdao 266034, ChinaKey Laboratory of Marine Drugs, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, 5 Yu-Shan Road, Qingdao 266003, ChinaKey Laboratory of Marine Drugs, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, 5 Yu-Shan Road, Qingdao 266003, ChinaKey Laboratory of Marine Drugs, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, 5 Yu-Shan Road, Qingdao 266003, ChinaVanadium compounds were studied during recent years to be considered as a representative of a new class of nonplatinum metal anticancer agents in combination to its low toxicity. Here, we found a vanadium compound Van-7 as an inhibitor of Topo I other than Topo II using topoisomerase-mediated supercoiled DNA relaxation assay. Agarose gel electrophoresis and comet assay showed that Van-7 treatment did not produce cleavable complexes like HCPT, thereby suggesting that Topo I inhibition occurred upstream of the relegation step. Further studies revealed that Van-7 inhibited Topo I DNA binding involved in its intercalating DNA. Van-7 did not affect the catalytic activity of DNase I even up to100 μM. Van-7 significantly suppressed the growth of cancer cell lines with IC50 at nanomolar concentrations and arrested cell cycle of A549 cells at G2/M phase. All these results indicate that Van-7 is a potential selective Topo I inhibitor with anticancer activities as a kind of Topo I suppressor, not Topo I poison.http://dx.doi.org/10.1155/2012/756374
spellingShingle Xiao-mei Mo
Zhan-fang Chen
Xin Qi
Yan-tuan Li
Jing Li
DNA-Binding and Topoisomerase-I-Suppressing Activities of Novel Vanadium Compound Van-7
Bioinorganic Chemistry and Applications
title DNA-Binding and Topoisomerase-I-Suppressing Activities of Novel Vanadium Compound Van-7
title_full DNA-Binding and Topoisomerase-I-Suppressing Activities of Novel Vanadium Compound Van-7
title_fullStr DNA-Binding and Topoisomerase-I-Suppressing Activities of Novel Vanadium Compound Van-7
title_full_unstemmed DNA-Binding and Topoisomerase-I-Suppressing Activities of Novel Vanadium Compound Van-7
title_short DNA-Binding and Topoisomerase-I-Suppressing Activities of Novel Vanadium Compound Van-7
title_sort dna binding and topoisomerase i suppressing activities of novel vanadium compound van 7
url http://dx.doi.org/10.1155/2012/756374
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