Inhibition of 15-lipoxygenase

Sumner H, Umit S, Knight DW, Hoult JRS. Chrysanthemum parthenium (L.) Bernh. Inhibition of 5-lipoxygenase and cyclooxygenase in leukocytes by feverfew Involvement of sesquiterpene lactones and other components. Biochem Pharmacol 1992 43 2313-2320. 

Israel E, Rubin P, Kemp JP et al. The effect of inhibition of 5-lipoxygenase by zi-leuton in mild-to-moderate asthma. Ann Intern Med 1993 119 1059-1066. 

Muller, K. and K. Ziereis. 1994. The antipsoriatic Mahonia aquifolium and its active consitutents. I. Pro- and antioxidant properties and inhibition of 5-lipoxygenase. Planta Med. 60 421-424. 

Fig. (14). Dose-dependent inhibition of 5-lipoxygenase by artonin E (7, ), morusin (3, o), and cirsiliol (51,...

Whatever the mechanism of action for the inhibition of 5-lipoxygenase by flavonoids, it appears to be distinct from the antioxidant properties of these compounds. The results comparing antioxidant activity with leukotriene inhibitory activity clearly demonstrate this distinction. The profound effects of metabolic transformation on the anti-inflammation activity of dietary flavonoids such as quercetin must also be considered in relation to in vitro studies, and further highlights the need to use actual metabolic forms of flavonoids rather than the free aglycone or glycosides occurring in the diet. 

Devaraj, S., and Jialal, I. (1999) Alpha-tocopherol decreases interleukin-1 beta release from activated human monocytes by inhibition of 5-lipoxygenase. Arterioscler Thromb Vase Biol 19, 1125-33. 

The effects of berbamine, oxyacanthine, and berberine on 5-lipoxygenase lipid peroxidation in phospholipid liposomes induced by 2,2 -azo-(bis-2-amidinopropane)(AAPH), deoxyribose degradation, and their reactivities against the free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH) were studied. None of the alkaloids showed any appreciable effects in the inhibition of 5-lipoxygenase. Reactivity against DPPH increased in the following order berberine < oxyacanthine < berbamine. Pro-oxidant effects of the alkaloids were excluded, since deoxyribose degradation was not influenced as determined by the release of malondialdehyde [200],... 

AEA hydrolysis by FAAH in vitro is not affected by calcium (Hillard et al. 1995 Maurelli et al. 1995). Interestingly, however, lipoxygenase products appear to inhibit FAAH activity such that inhibition of 5-lipoxygenase enhances AEA hydrolysis in mast cells (Maccarrone et al. 2000c) and neuroblastoma cells (Mac-... 

McAlexander MA, Myers AC, Undem BJ (1999) Adaptation of guinea-pig vagal airway afferent neurones to mechanical stimulation. J Physiol 521(Part 1) 239 7 McAlexander MA, Myers AC, Undem BJ (1998) Inhibition of 5-lipoxygenase diminishes neu-rally evoked tachykinergic contraction of guinea pig isolated airway, J Pharmacol Exp Ther 285(2) 602-7... 

Kim, J.H., N.E. Hubbard, V. Ziboh, K.L. Erickson. Attenuation of Breast Tumor Cell Growth by Conjugated Linoleic Acid via Inhibition of 5-lipoxygenase Activating Protein, Qipip j O ippl s Act 1736 244—250 (2005). 

Lobaria linita Tenuiorin Depsides APP Inhibition of 5-lipoxygenase activity Ingolfsdottir and Gudmundsdottir (2002)... 

Ingolfsdottir K, Bren W, Huneck S et al (1994) In-vitro inhibition of 5-lipoxygenase by protolichesterinic acid from Cetraria islandica. Phytomedicine 1 187-191 Ingolfsdottir K, Gissurarson SR, Muller-Jakic B et al (1996) Inhibitory effects of the lichen metabolite lobaric acid on arachidonate metabolism in-vitro. Phytomedicine 2 243-246... 

How can one inhibit leukotriene biosynthesis From what we have seen above, there are several possible ways (Fig. 4.20). Inhibition of 5-lipoxygenase activity is the most obvious one, and it has been extensively explored. In this line, the design of drugs that interact with the iron present at the active site of 5-lipoxygenase has been particularly fruitful. To this group of compounds... 

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