In vitro chemopreventive potential of fucophlorethols from the brown alga Fucus vesiculosus L. by anti-oxidant activity and inhibition of selected cytochrome P450 enzymes.
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 IC(50) values for scavenging of 1,1-diphenyl-2 picrylhydrazyl radicals (DPPH) in the range of 10.0-14.4 microg/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 IC(50) values in the range of 17.9-33 microg/ml, and aromatase (Cyp19) activity with IC(50) values in the range of 1.2-5.6 microg/ml.
Parys
Sabine
S
Institute for Pharmaceutical Biology, University of Bonn, Nussallee 6, D-53115 Bonn, Germany.
Kehraus
Stefan
S
Krick
Anja
A
Glombitza
Karl-Werner
KW
Carmeli
Shmuel
S
Klimo
Karin
K
Gerhäuser
Clarissa
C
König
Gabriele M
GM
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use; D000975:Antioxidants / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D047072:Aromatase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D001713:Biphenyl Compounds / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D045744:Cell Line, Tumor; D065607:Cytochrome P-450 Enzyme Inhibitors; D044645:Fucus / Q000737:chemistry*; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy; D010647:Phenyl Ethers / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D010696:Phloroglucinol / Q000031:analogs & derivatives / Q000494:pharmacology* / Q000627:therapeutic use; D010851:Picrates; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D013730:Terphenyl Compounds / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use
D000972:Antineoplastic Agents, Phytogenic; D000975:Antioxidants; D047072:Aromatase Inhibitors; D001713:Biphenyl Compounds; D065607:Cytochrome P-450 Enzyme Inhibitors; D010647:Phenyl Ethers; D010851:Picrates; D010936:Plant Extracts; D013730:Terphenyl Compounds; C551321:fucotriphlorethol A; C551322:trifucodiphlorethol A; C551323:trifucotriphlorethol A; C004931:1,1-diphenyl-2-picrylhydrazyl; D010696:Phloroglucinol