Mechanism of inhibition of CYP1A1 and glutathione S-transferase activities in fish liver by quercetin, resveratrol, naringenin, hesperidin, and rutin.
Quercetin, resveratrol, naringenin, hesperidin, and rutin are phenolic compounds/flavonoids that may have roles in the reduction of cancer susceptibility. In this study, in vitro modulatory effects of them were studied on liver CYP1A1 associated 7-ethoxyresorufin-O-deethylase (EROD) activity and glutathione S-transferase (GST) activity of leaping mullet (Liza saliens). All of the phenolic compounds/flavonoids used exerted an inhibitory effect on both EROD and GST activities of fish. Quercetin, resveratrol, hesperidin, and rutin were found to inhibit EROD activity in a competitive manner; on the other hand, naringenin was found to inhibit EROD activity in a noncompetitive manner. Ki values of quercetin, resveratrol, naringenin, hesperidin, and rutin were calculated from Dixon plots as 0.12 μM, 0.67 μM, 2.63 μM, 18 μM and 0.1 mM, respectively. Resveratrol, quercetin, and hesperidin were found to inhibit GST activity in a competitive manner; on the other hand, rutin and naringenin were found to inhibit GST activity in a mixed-type manner. Ki values of resveratrol, quercetin, hesperidin, naringenin, and rutin were calculated from Dixon plots as 3.2 μM, 12.5 μM, 45 μM, 128 μM, and 150 μM, respectively. The results suggest that quercetin and resveratrol containing foods are effective in the prevention and treatment of cancer.
a Department of Biological Sciences , Middle East Technical University , Ankara , Turkey.
Emel
E
Arinç
Duygu
D
Yilmaz
Azra
A
Bozcaarmutlu
D000818:Animals; D016588:Anticarcinogenic Agents / Q000494:pharmacology; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology; D000975:Antioxidants / Q000494:pharmacology; D001667:Binding, Competitive; D019363:Cytochrome P-450 CYP1A1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D003600:Cytosol / Q000187:drug effects / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000494:pharmacology; D029941:Fish Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D005399:Fishes / Q000254:growth & development / Q000378:metabolism*; D005419:Flavonoids / Q000494:pharmacology*; D005982:Glutathione Transferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D007700:Kinetics; D008099:Liver / Q000187:drug effects* / Q000201:enzymology; D008522:Mediterranean Sea; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D013267:Stilbenes / Q000494:pharmacology*; D014421:Turkey
D016588:Anticarcinogenic Agents; D000972:Antineoplastic Agents, Phytogenic; D000975:Antioxidants; D004791:Enzyme Inhibitors; D029941:Fish Proteins; D005419:Flavonoids; D013267:Stilbenes; D019363:Cytochrome P-450 CYP1A1; D005982:Glutathione Transferase