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In vitro chemopreventive potential of fucophlorethols from the brown alga Fucus vesiculosus L. by anti-oxidant activity and inhibition of selected cytochrome P450 enzymes
Authors:Sabine Parys  Stefan Kehraus  Anja Krick  Karl-Werner Glombitza  Shmuel Carmeli  Karin Klimo  Clarissa Gerhäuser  Gabriele M. König
Affiliation:1. Institute for Pharmaceutical Biology, University of Bonn, Nussallee 6, D-53115 Bonn, Germany;2. School of Chemistry, Tel Aviv University, Ramat Aviv, Tel Aviv, Israel;3. Division of Epigenomics and Cancer Risk Factors, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 280, D-69120 Heidelberg, Germany
Abstract:Within a project focusing on the chemopreventive potential of algal phenols, two phloroglucinol derivatives, belonging to the class of fucophlorethols, and the known fucotriphlorethol A were obtained from the ethanolic extract of the brown alga Fucus vesiculosus L. The compounds trifucodiphlorethol A and trifucotriphlorethol A are composed of six and seven units of phloroglucinol, respectively.The compounds were examined for their cancer chemopreventive potential, in comparison with the monomer phloroglucinol. Trifucodiphlorethol A, trifucotriphlorethol A as well as fucotriphlorethol A were identified as strong radical scavengers, with IC50 values for scavenging of 1,1-diphenyl-2 picrylhydrazyl radicals (DPPH) in the range of 10.0–14.4 μg/ml. All three compounds potently scavenged peroxyl radicals in the oxygen radical absorbance capacity (ORAC) assay. In addition, the compounds were shown to inhibit cytochrome P450 1A activity with IC50 values in the range of 17.9–33 μg/ml, and aromatase (Cyp19) activity with IC50 values in the range of 1.2–5.6 μg/ml.
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