6,7,4'-Trihydroxyisoflavan: a potent and selective inhibitor of 5-lipoxygenase in human and porcine peripheral blood leukocytes.
The effect of 6,7,4'-trihydroxyisoflavan on human platelet 12-lipoxygenase and human and porcine PMNL 5-lipoxygenase activities has been studied. 6,7,4'-Trihydroxyisoflavan was found to inhibit 5-lipoxygenase more strongly than 12-lipoxygenase; its concentration for 50% inhibition (IC50) was 1.6 microM for human and porcine 5-lipoxygenase and 22 microM for human platelet 12-lipoxygenase. Inhibition of microsomal cyclooxygenase from ram seminal vesicles is exhibited at much higher concentrations of 6,7,4'-trihydroxyisoflavan (IC50 = 200 microM).
D000818:Animals; D001091:Arachidonate Lipoxygenases; D001095:Arachidonic Acids / Q000097:blood / Q000138:chemical synthesis; D001578:Benzopyrans / Q000494:pharmacology*; D001792:Blood Platelets / Q000201:enzymology*; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D006801:Humans; D007529:Isoflavones; D008084:Lipoxygenase / Q000097:blood* / Q000302:isolation & purification; D016859:Lipoxygenase Inhibitors; D008297:Male; D008861:Microsomes / Q000201:enzymology; D009504:Neutrophils / Q000201:enzymology*; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism; D012669:Seminal Vesicles / Q000201:enzymology; D012756:Sheep; D013552:Swine
D001095:Arachidonic Acids; D001578:Benzopyrans; D007529:Isoflavones; D016859:Lipoxygenase Inhibitors; C044274:6,7,4'-trihydroxyisoflavan; D001091:Arachidonate Lipoxygenases; D008084:Lipoxygenase; D011451:Prostaglandin-Endoperoxide Synthases