ArticleThe Biochemical journal2004
Comparative analysis of topoisomerase IB inhibition and DNA intercalation by flavonoids and similar compounds: structural determinates of activity.
Article in The Biochemical journal, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 139 citations in OpenAlex.
- Flavonoids as Dual Topoisomerase I and II Inhibitors: Mechanistic Insights and Emerging Anticancer Strategies.Chemistry & biodiversity · 2026Review
- Interaction of flavonoids with DNA: implications in cancer treatment.Molecular biology reports · 2026Review
- Synthesis and biological evaluation of pyrano and furano fused ring isoflavene derivatives.RSC advances · 2025Article
- The effects of hesperidin on valproic acid-induced reduction in hippocampal neurogenesis through the antioxidant and apoptotic pathways in adult rats.Scientific reports · 2024Article
- Radioprotective Effect of Resveratrol, Crocin, and Their Combination on Cytogenetic Alterations in Human Lymphocytes.Journal of biomedical physics & engineering · 2024Article
- DNA topoisomerase inhibition with the HIF inhibitor acriflavine promotes transcription of lncRNAs in endothelial cells.Molecular therapy. Nucleic acids · 2022Article
- Topoisomerase poisoning by the flavonoid nevadensin triggers DNA damage and apoptosis in human colon carcinoma HT29 cells.Archives of toxicology · 2021Article
- Apigenin and Hesperidin Downregulate DNA Repair Genes in MCF-7 Breast Cancer Cells and Augment Doxorubicin Toxicity.Molecules (Basel, Switzerland) · 2020Article
- Apigenin and hesperidin augment the toxic effect of doxorubicin against HepG2 cells.BMC pharmacology & toxicology · 2019Article
- Cytogenotoxic effects ofSaudi journal of biological sciences · 2019Article
- Ageing, Cellular Senescence and Neurodegenerative Disease.International journal of molecular sciences · 2018Review
- Metal-Catalyzed Photooxidation of Flavones in Aqueous Media.European journal of inorganic chemistry · 2018Article
- Natural Compounds as Anticancer Agents Targeting DNA Topoisomerases.Current genomics · 2017Review
- Ginkgo biloba leaf extract induces DNA damage by inhibiting topoisomerase II activity in human hepatic cells.Scientific reports · 2015Article
- Gold(III) macrocycles: nucleotide-specific unconventional catalytic inhibitors of human topoisomerase I.Journal of the American Chemical Society · 2014Article
- Article
- Iron chelators with topoisomerase-inhibitory activity and their anticancer applications.Antioxidants & redox signaling · 2013Review
- Article
- Protective effects of propolis and related polyphenolic/flavonoid compounds against toxicity induced by irinotecan.Medical oncology (Northwood, London, England) · 2010Article
- Anthocyanin Interactions with DNA: Intercalation, Topoisomerase I Inhibition and Oxidative Reactions.Journal of food biochemistry · 2008Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
Flavonoids and other polyphenolic compounds have been shown to inhibit human topoisomerase IB (topo I) through both inhibition of relaxation activity and through stabilization of the cleavable complex (poisoning). Some flavonoids have also been shown to intercalate DNA, and an association of topoisomerase inhibition with intercalation has been noted. We surveyed 34 polyphenolic compounds, primarily flavonoid glycones and aglycones, for their ability to inhibit topo I and to intercalate DNA using an in vitro gel electrophoresis method. We show that the most potent topo I poisons are the flavones and flavonols, and that these generally, but not always, are found to be DNA intercalators. There was no clear correlation, however, of topo-I-poisoning activity with the degree of DNA unwinding. Surprisingly, both DNA intercalation and topo I poisoning were shown to occur with some flavone glycones, including the C-glycosylflavone orientin. Inhibition of relaxation activity by flavonoids was found to be difficult to quantify and was most likely to be due to non-specific inhibition through flavonoid aggregation. As part of a structure-activity analysis, we also investigated the acid-base chemistry of flavonoids and determined that many flavonoids show acid-base activity with a pK(a) in the physiological pH region. For this reason, subtle pH changes can have significant effects on solution activity of flavonoids and their concomitant biological activity. In addition, these effects may be complicated by pH-dependent aggregation and oxidative degradation. Finally, we develop a simple model for the intercalation of flavonoids into DNA and discuss possible consequences of intercalation and topoisomerase inhibition on a number of cellular processes.
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