New isoflavonoids as inhibitors of porcine 5-lipoxygenase.
The inhibitory activity of new isoflavonoids on 5-lipoxygenase of porcine leukocytes was investigated. Isoflavans (I) proved to be stronger inhibitors than isoflavones (II). The isoflavans containing ortho-hydroxy groups in ring A showed the lowest Ki values (0.8-50 microM). In comparison, isoflavans with meta-dihydroxy groups exhibited Ki values higher than 150 microM. The effect of commercial antioxidants was tested also on porcine 5-lipoxygenase. Butylated hydroxyanisole (Ki: 25 microM) and butylated hydroxytoluene (Ki: 55 microM) revealed moderate inhibitory activity, whereas L-ascorbic acid, L-ascorbyl palmitate, dl-alpha-tocopherol and n-propyl gallate showed weak inhibitory activities (Ki: 100-260 microM).
Voss
C
C
Institute of Physiological Chemistry, University Bonn, Germany.
Sepulveda-Boza
S
S
Zilliken
F W
FW
D000818:Animals; D000975:Antioxidants / Q000494:pharmacology*; D001094:Arachidonate 5-Lipoxygenase / Q000378:metabolism; D002839:Chromans / Q000494:pharmacology*; D007700:Kinetics; D007962:Leukocytes / Q000187:drug effects / Q000201:enzymology; D016859:Lipoxygenase Inhibitors / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013552:Swine
D000975:Antioxidants; D002839:Chromans; D016859:Lipoxygenase Inhibitors; D001094:Arachidonate 5-Lipoxygenase