Leukotriene biosynthesis inhibition

Phenanthrenes obtained from the Stemona species were evaluated on their leukotriene biosynthesis inhibition property using human neutrophile granulocytes in vivo. Stemanthrenes A 162 and D 165 display inhibitory activity in a dose-dependent manner, with IC50 values of 8.5 and 4.8 pM. Stemanthrenes B 163 and C 164 possess 100% inhibition against leukotriene biosynthesis at 25 pM. The phenanthrenes might be responsible for the anti-inflammatory and antiasthmatic principles of the Stemona species [154]. Denbinobin, a phenanthraquinone from Dendrobium moniliforme, shows in vitro anti-inflammatory activity. It inhibits the formation of tumor necrosis factor and prostaglandin E2 induced by lipopolysac-charide in RAW 264.7 and N9 cells at a dose of 1 pM [100]. 

Most of the drugs such as epinephrine and albuterol used to treat asthma attacks are bronchodilators—substances that expand the bronchial passages Newer drugs are designed to either inhibit the enzyme 5 lipoxygenase which acts on arachidomc acid m the first stage of leukotriene biosynthesis or to block leukotriene receptors... 

Kiuchi F, Iwakami S, Shibuya M, Hanaoka F, Sankawa U. (1992). Inhibition of prostaglandin and leukotriene biosynthesis by gingerols and diarylheptanoids. Chem Pharm Bull (Tol o). 40(2) 387-91. Kobayashi M, Shqji N, Ohizumi Y. (1987). Gingerol, a novel cardiotonic agent, activates the Ca2+-pumping ATPase in skeletal and cardiac sarcoplasmic reticulum. Biochim Biophys Acta. 903(1) 96-102. 

Hanaoka, and U. Sankawa. Inhibition of prostaglandin and leukotriene biosynthesis by gingerols and diaryl-heptanoids. Chem Pharm Bull 1992 40(2) 387-391. 

Boswellinic acids Leukotrienes appear to play a special role as inflammation mediators in the pathogenesis of PBC they also correlate closely with the increase in cholestasis-indicating enzymes. Boswellinic acids are selective non-redox inhibitors of 5-lipoxygen-ase and therefore inhibit leukotriene biosynthesis. So far, they have not been used in PBC treatment. Based on existing pharmacological data, their application should now be considered. 

Inhibition of prostaglandin, thromboxane and leukotriene biosynthesis. 15. Ill Integrated control of trematode diseases. 12. 53 Interethnic factors affecting drug response. 25. 1 Interferon and interferon inducers. 10, 101... 

FLAP inhibitors are a novel class of compounds that inhibit cellular leukotriene biosynthesis without acting directly on 5-LO. Instead, they bind to the 18-kDa membrane FLAP, thus preventing the activation of 5-LO. 

A tetrahydropyran that inhibits leukotriene biosynthesis Asymmetric synthesis of2-methyl-tetrahydropyran-4-one by kinetic resolution Part VI - Asymmetric Desymmetrisation of a Diels-Alder Adduct Ifetroban sodium a thromboxane receptor antagonist A laboratory synthesis starting with a Diels-Alder reaction Desymmetrisation of a symmetrical anhydride with a chiral Grignard reagent Laboratory and process routes compared Part VII - Asymmetric Synthesis of A Bicyclic 3-Lactone Lactacystin a naturalproteasome inhibitor... 

Fluocinolone is a low- to medium-potency topical corticosteroid with antiinflammatory, antipruritic, and vasoconstrictive properties, thought to act by induction of phospholipase A2 inhibitory proteins (lipocortins). Lipo-cortins appear to control biosynthesis of potent mediators of inflammation (prostaglandins, leukotrienes) by inhibiting... 

The mechanism of action of boswellic acids from crude extracts of Boswellia serrata has been established [59] and it was reported recently that they inhibit the increased urinary excretion of LTE4 in astrocytoma patients in vivo and block leukotriene biosynthesis ex vivo [60]. 

Brady HR, Serhan CN Adhesion promotes transcellular leukotriene biosynthesis during neutrophil-glomerular endothelial cell interactions Inhibition by antibodies against CD18 and L-selectin. Biochem Biophys Res Commun 1992 186 1307-1314. 

Ramesha, C.S. and Pickett, W.C. (1986). Platelet activating factor and leukotriene biosynthesis is inhibited in polymorphonuclear leukocytes depleted of arachidonic acid. J. Biol Chem., 261, 7592-7595... 

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