Degranulation inhibition

Degranulation inhibition. Hot water extract of the rhizome, in cell culture at a concentration of 0.1 mg/mL, was active vs compound 48/40-induced degranulation of mast cells. A mixture of Bupleurum falcatum, Pinellia ternata, Poria cocos, Scutellaria bai-... 

Blocks calcium influx across mast cell membrane Inhibits mast ceU degranulation Inhibits mast ceU degranulation... 

Peptides (beta-endorphin, methionine-enkephalin, beta-hpotro-pin, granuloc3de inhibiting proteins I and II, degranulation-inhibiting protein, adrenomedulhn)... 

Britigan BE, Hassett DJ, Rosen GM, Hamill DR, Cohen MS. Neutrophil degranulation inhibits potential hydroxyl-radical formation. Relative impact of myeloperoxidase and lactoferrin release on hydroxyl-radical production by iron-supplemented neutrophils assessed by spin-trapping techniques. Biochem J 1989 264 447 55. 

Treatment of ocular allergy is aimed at slowing or stopping these processes. Antihistamines block the histamine receptors and some prevent histamine production and/or inhibit mediator release from the mast cells.15 Mast cell stabilizers inhibit the degranulation of mast cells, preventing mediator release. Some topical agents have multiple mechanisms of action, combining antihistaminic, mast cell stabilization, and antiinflammatory properties (Tables 60-3 and 60-4).16... 

Dynorphin, a-neoendorphin and /1-endorphin each produced a dose-dependent (10 6 M to 10 4 M) release of histamine from rat peritoneal mast cells but not from rat mucosal mast cells which were isolated following collagenase digestion [128]. When administered intradermally to the forearms of human volunteers, dynorphin, /f-endorphin, Leu-enkephalin and morphiceptin each produced a wheal and flare reaction at nM concentrations. Mast cell degranulation was confirmed by electron microscopy of biopsy samples and by its inhibition by hyroxyzine pretreatment [129]. 

Recently, BN 52063 has been demonstrated to be effective against mastocytosis [304], a condition which was previously incurable. This suggests that PAF, as well as mast cell degranulation, may have a role in systemic mastocytosis. The injectable (pure) form of BN 52021 is much more powerful than BN 52063. Preliminary clinical investigations have shown a long and intense inhibition of ex vivo PAF-induced platelet aggregation. The injectable form is now under clinical trials in graft rejection, stroke, haemodialysis and shock. 

Damen, J.E. Ware, M.D., Kalesnikoff, J., Hughes, M.R. and Krystal, G., 2001, SHIP S C terminus is essential for ist hydrolysis of P1P3 and inhibition of mast cell-degranulation. 

Histamine inhibits neutrophil chemotaxis due to HR2 triggering, which is mimicked by impromidine (HR2 agonist), but not by betahistine (HRl agonist). In addition, histamine inhibits neutrophil activation, superoxide formation and degranulation via HR2 [40]. Downregulation of... 

Pfizer s tenidap (CP-66,248) (157), another enolic compound, was also more potent (500-fold) toward CO over 5-LO inhibition in human ISN (0.032 /iM and 18 /iM, respectively) [379-381]. Efficacy in rheumatoid arthritis clinical trials has been reported [380,382] in patients, serum levels of acute phase proteins and synovial fluid levels of IL-1 were reduced by tenidap, in contrast to the lack of this effect with NSAIDs. Besides CO/5-LO inhibition, a variety of in vitro activities have been reported, including a number of effects on monocyte functions and differentiation [379], inhibition of neutrophil degranulation [382], inhibition of the activation of neutrophil collagenase [383], inhibition of leukocyte-endothelial cell adhesion [384], and inhibition of LTB4-induced neutrophil chemotaxis [385]. Al-... 

Evidence of a reduction in the number of acid-soluble SH-groups by feverfew extract in neutrophils at concentrations similar to those inhibiting neutrophil behaviour has been described [45]. It was suggested that interference with SH-groups alters assembly of microtubules which are known to be involved in phagocytosis and degranulation of neutrophils. 

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