alexa Flavonoids: potent inhibitors of arachidonate 5-lipoxygenase.


Journal of Nutritional Disorders & Therapy

Author(s): Yoshimoto T, Furukawa M, Yamamoto S, Horie T, WatanabeKohno S

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Abstract Various flavonoids were found to be relatively selective inhibitors of arachidonate 5-lipoxygenase which initiates the biosynthesis of leukotrienes with the activity of slow reacting substance of anaphylaxis. Cirsiliol (3',4',5-trihydroxy-6,7-dimethoxyflavone) was most potent, and the enzyme partially purified from rat basophilic leukemia cells was inhibited by 97\% at a concentration of 10 microM (IC50, about 0.1 microM). 12-Lipoxygenases from bovine platelets and porcine leukocytes were also inhibited but at higher concentrations (IC50, about 1 microM), and fatty acid cyclooxygenase purified from bovine vesicular gland was scarcely affected. The compound at 10 microM suppressed by 99\% the immunological release of slow reacting substance of anaphylaxis from passively sensitized guinea pig lung (IC50, about 0.4 microM).
This article was published in Biochem Biophys Res Commun and referenced in Journal of Nutritional Disorders & Therapy

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