Effects of naturally-occurring flavonoids and biflavonoids on epidermal cyclooxygenase and lipoxygenase from guinea-pigs.
Although there have been numerous topical applications of plant extracts having flavonoids known as anti-inflammatory compounds, only a few studies were reported concerning effects of flavonoids on epidermal cyclooxygenase/lipoxygenase. In this investigation, effects of naturally occurring flavonoids on epidermal cyclooxygenase/lipoxygenase were studied using five selected derivatives: flavanone, apigenin (flavone), quercetin (flavonol), amentoflavone and ginkgetin (biflavone) because eicosanoids generated in the epidermis are believed to be involved in various biological activities of the skin. Microsomal and cytosolic fractions were obtained from guinea-pig epidermal homogenate by centrifugation and used as a source for cyclooxygenase and lipoxygenase. It was found that quercetin inhibited both cyclooxygenase and lipoxygenase, being more potent against lipoxygenase, while flavanone and apigenin did not show any inhibition. Amentoflavone, one of the biflavones tested, showed potent and selective inhibitory activity on cyclooxygenase (IC50 = 3 microM) which was comparable to indomethacin (IC50 = 1 microM). In contrast, structurally similar ginkgetin possessed weak inhibitory activity on cyclooxygenase. The in vivo effects of these flavonoids on the normal and diseased skin remain to be studied.
Kim
H P
HP
College of Pharmacy, Kangweon Nat'l. Univ., Chuncheon, Korea.
Mani
I
I
Iversen
L
L
Ziboh
V A
VA
D000818:Animals; D016861:Cyclooxygenase Inhibitors / Q000494:pharmacology; D003600:Cytosol / Q000201:enzymology; D015777:Eicosanoids / Q000378:metabolism; D004817:Epidermis / Q000187:drug effects*; D005419:Flavonoids / Q000494:pharmacology*; D006168:Guinea Pigs; D006893:Hydroxyeicosatetraenoic Acids / Q000378:metabolism; D007213:Indomethacin / Q000494:pharmacology; D008084:Lipoxygenase / Q000378:metabolism*; D016859:Lipoxygenase Inhibitors / Q000494:pharmacology; D008297:Male; D008861:Microsomes / Q000201:enzymology; D015394:Molecular Structure; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism*
D016861:Cyclooxygenase Inhibitors; D015777:Eicosanoids; D005419:Flavonoids; D006893:Hydroxyeicosatetraenoic Acids; D016859:Lipoxygenase Inhibitors; D008084:Lipoxygenase; D011451:Prostaglandin-Endoperoxide Synthases; D007213:Indomethacin