Lipoxygenases (LOs) are non-heme iron-containing dioxygenases that catalyze the oxidation of polyunsaturated fatty acids to generate unsaturated fatty acid hydroperoxides.1 The immediate products of 15-LO fatty acid oxidation act as mediators in inflammation, thrombosis, and cancer.2 CBDD is a cannabidiol derivative that potently and selectively inhibits 15-LO with an IC50 value of 0.28 µM.3 It does not inhibit 5-LO effectively (IC50 >200 µM).3
1
Hope, W.C., Welton, A.F., Fiedler-Nagy, C., et al. In vitro inhibition of the biosynthesis of slow reacting substance of anaphylaxis (SRS-A) and lipoxygenase activity by quercetin. Biochem Pharmacol32367-371(1983).
2
Argentieri, D.C., Ritchie, D.M., Ferro, M.P., et al. Tepoxalin: A dual cyclooxygenase/5-lipoxygenase inhibitor of arachidonic acid metabolism with potent anti-inflammatory activity and a favorable gastrointestinal profile. J Pharmacol Exp Ther2711399-1408(1994).
3
Takeda, S., Usami, N., Yamamoto, I., et al. Cannabidiol-2',6'-dimethyl ether, a cannabidiol derivative, is a highly potent and selective 15-lipoxygenase inhibitor. Drug Metab Dispos(2009).
Hope, W.C., Welton, A.F., Fiedler-Nagy, C., et al. In vitro inhibition of the biosynthesis of slow reacting substance of anaphylaxis (SRS-A) and lipoxygenase activity by quercetin. Biochem Pharmacol32367-371(1983).
Argentieri, D.C., Ritchie, D.M., Ferro, M.P., et al. Tepoxalin: A dual cyclooxygenase/5-lipoxygenase inhibitor of arachidonic acid metabolism with potent anti-inflammatory activity and a favorable gastrointestinal profile. J Pharmacol Exp Ther2711399-1408(1994).
Takeda, S., Usami, N., Yamamoto, I., et al. Cannabidiol-2',6'-dimethyl ether, a cannabidiol derivative, is a highly potent and selective 15-lipoxygenase inhibitor. Drug Metab Dispos(2009).
Cannabidiol dimethyl ether is available in the following screening
library: