DNA-protective activities of hyperforin and aristoforin

  • Toxicol In Vitro. 2015 Apr;29(3):631-7. doi: 10.1016/j.tiv.2015.01.016.
A Ševčovičová  1 ,  M Šemeláková  2 ,  J Plšíková  3 ,  D Loderer  4 ,  P Imreová  4 ,  E Gálová  4 ,  M Kožurková  3 ,  E Miadoková  4 ,  P Fedoročko  2
Affiliations
  • 1. Department of Genetics, Faculty of Natural Sciences, Comenius University, Mlynská dolina, 842 15 Bratislava, Slovakia. Electronic address: [email protected].
  • 2. Institute of Biology and Ecology, Faculty of Sciences, P.J. Šafárik University in Košice, Moyzesova 11, 040 01 Košice, Slovakia.
  • 3. Institute of Chemistry, Faculty of Sciences, P.J. Šafárik University in Košice, Moyzesova 11, 040 01 Košice, Slovakia.
  • 4. Department of Genetics, Faculty of Natural Sciences, Comenius University, Mlynská dolina, 842 15 Bratislava, Slovakia.
PMID: 25678043 DOI: 10.1016/j.tiv.2015.01.016
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.

Keywords
Aristoforin; DNA unwinding assay; DNA-topology assay; DPPH()/()OH scavenging activity; Hyperforin; Reducing power assay.
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