5-Lipoxygenase inhibitors phenols

Yet another indole-based lipoxygenase inhibitor has shown activity in models of inflammatory bowel disease. The starting benzylaniline (23-3) can speculatively be obtained by alkylation on the phenol oxygen in (23-2) with 2-bromomethyl-quinoline (23-1). The customary diazotisation reduction sequence then affords the... 

A lipoxygenase activity has been detected in freshly prepared olive oils (Georgalaki el al. 1998). Taking into consideration the higher stabilities of cloudy oil, it can be postulated that the polar phenolic compounds present act not only as primary antioxidants, but also as inhibitors of oxidising enzymes. 

Caffeic Acid Phenethyl Ester (CAPE). CAPE, a phenolic compound with antioxidant properties, is an active ingredient derived from honeybee propolis (52). CAPE has antiviral, anti-inflammatory and antiproliferative properties. The compound differentially suppresses the growth of numerous human cancer cells and also inhibits tumor promoter-mediated processes in transformed cells (53,54). In transformed cells, CAPE induces apoptosis and inhibits the expression of the malignant phenotype (55,56). In addition, CAPE treatment attenuates the formation of azoxymethane-induced aberrant crypts and the activities of ornithine decarboxylase (ODC), tyrosin protein kinase, and lipoxygenase activity (57). Although the molecular basis for these multiple chemopreventive effects of CAPE is not clear, recent studies have demonstrated that CAPE is a potent and specific inhibitor of the transcription factor NF-kB (58). CAPE inhibited the activity and expression of COX-2 in the carrageenan air pouch model of inflammation as well as in TPA-treated human oral epithelial cells (59). CAPE was able to reduce neointimal formation by inhibiting NF-kB activation in a model of endothelial injury of rat carotid artery (60). 

Odabasoglu F, Aslan A, Cakir A et al (2004) Comparison of antioxidant activity and phenolic content of three lichen species. Phytother Res 18 938-941 Ogmundsdottir HM, Zoega GM, Gissurarson SR et al (1998) Anti-proliferative effects of lichen-derived inhibitors of 5-lipoxygenase on malignant cell-lines and mitogen-stimulated lymphocytes. J Pharm Pharmacol 50 107-115... 

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