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Deigner HP, Wolf G, Ohlenmacher U, Reichling J: 1'-Hydroxyeugenol- and coniferyl alcohol derivatives as effective inhibitors of 5-lipoxygenase and Cu (2+)-mediated low density lipoprotein oxidation. Arzneimittelforschung. 1994 Aug;44(8):956-61.
Evidence for a dual mechanism.. 1'-Hydroxyeugenol- and epoxy-Z-coniferyl alcohol esters from Coreopsis species as well as synthetic derivatives of these natural compounds were examined as lipoxygenase inhibitors and as LDL (low density lipoprotein)-stabilizing agents. Most of the compounds displayed inhibitory activity on the formation of leukotrienes (LTB4 and LTC4) in a cellular (RBL-1 cells) assay as well as in a cell-free 5-lipoxygenase assay at concentrations of 4-24 mumol/l. No effect of selected compounds was observed on mammalian lipoxygenases with other specificity (12- and 15-lipoxygenase). The more lipophilic derivatives also effectively reduced Cu (2+)-mediated oxidation of LDL. The findings are discussed on the base of structure-activity relationships. |
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