title: DNA-protective activities of hyperforin and aristoforin.
abstract: The aim of this study was to explain the molecular mechanisms of action of hyperforin, a phluoroglucinol derivative found in Hypericum perforatum L. and its more stable derivative aristoforin. DNA-topology assay revealed partial DNA-protective activities of hyperforin and aristoforin against Fe(2+)-induced DNA breaks. In order to assess molecular mechanisms underlying DNA-protective activity, the potential antioxidant activity of hyperforin and aristoforin was investigated using DPPH and OH scavenging assays, reducing power assay and Fe(2+)-chelating assay. We also studied interaction of hyperforin and aristoforin with DNA using established protocols for fluorescence titration. The ability of the studied compounds to relax topoisomerase I with electrophoretic techniques was investigated. The reduction in the fluorescence of hyperforin indicated an interaction between hyperforin and DNA with a binding constant of 0.2×10(8)M(-1). We suggest that a mechanism of hyperforin/aristoforin DNA-protective abilities is based on free radicals (mainly OH) scavenging activity.
authors: Department of Genetics, Faculty of Natural Sciences, Comenius University, Mlynská dolina, 842 15 Bratislava, Slovakia. Electronic address: sevcovicova@fns.uniba.sk.
authors: A
authors: A
authors: Ševčovičová
authors: Institute of Biology and Ecology, Faculty of Sciences, P.J. Šafárik University in Košice, Moyzesova 11, 040 01 Košice, Slovakia.
authors: M
authors: M
authors: Šemeláková
authors: Institute of Chemistry, Faculty of Sciences, P.J. Šafárik University in Košice, Moyzesova 11, 040 01 Košice, Slovakia.
authors: J
authors: J
authors: Plšíková
authors: Department of Genetics, Faculty of Natural Sciences, Comenius University, Mlynská dolina, 842 15 Bratislava, Slovakia.
authors: D
authors: D
authors: Loderer
authors: Department of Genetics, Faculty of Natural Sciences, Comenius University, Mlynská dolina, 842 15 Bratislava, Slovakia.
authors: P
authors: P
authors: Imreová
authors: Department of Genetics, Faculty of Natural Sciences, Comenius University, Mlynská dolina, 842 15 Bratislava, Slovakia.
authors: E
authors: E
authors: Gálová
authors: Institute of Chemistry, Faculty of Sciences, P.J. Šafárik University in Košice, Moyzesova 11, 040 01 Košice, Slovakia.
authors: M
authors: M
authors: Kožurková
authors: Department of Genetics, Faculty of Natural Sciences, Comenius University, Mlynská dolina, 842 15 Bratislava, Slovakia.
authors: E
authors: E
authors: Miadoková
authors: Institute of Biology and Ecology, Faculty of Sciences, P.J. Šafárik University in Košice, Moyzesova 11, 040 01 Košice, Slovakia.
authors: P
authors: P
authors: Fedoročko
mesh_terms: D000975:Antioxidants / Q000494:pharmacology; D004247:DNA / Q000187:drug effects*; D053960:DNA Breaks / Q000187:drug effects; D016166:Free Radical Scavengers / Q000494:pharmacology; D020902:Hypericum / Q000737:chemistry; D007501:Iron / Q000633:toxicity; D007502:Iron Chelating Agents / Q000494:pharmacology; D010696:Phloroglucinol / Q000031:analogs & derivatives* / Q000494:pharmacology; D013729:Terpenes / Q000494:pharmacology*; D059004:Topoisomerase I Inhibitors / Q000494:pharmacology
chemical_list: D000975:Antioxidants; C502222:Aristoforin; D016166:Free Radical Scavengers; D007502:Iron Chelating Agents; D013729:Terpenes; D059004:Topoisomerase I Inhibitors; D004247:DNA; D010696:Phloroglucinol; D007501:Iron; C001654:hyperforin
keywords: Aristoforin; DNA unwinding assay; DNA-topology assay; DPPH()/()OH scavenging activity; Hyperforin; Reducing power assay