polymorphonuclear leukocytes

CJ-13,610 is an orally active and nonredox-type inhibitor of 5-lipoxygenase (5-LOX). CJ-13,610 inhibits the biosynthesis of leukotriene B4 and regulates the expression of IL-6 mRNA in macrophages.

Traxanox is an orally available diuretic.Traxanox enhances phagocytosis of yeast granules by mouse peritoneal macrophages or rat peritoneal polymorphonuclear leukocytes in vitro.Restorative effect of Traxanox on inhibition of antibody production in BALB/c mice.

Traxanox TFA is an orally available diuretic. Traxanox TFA enhances phagocytosis of yeast granules by mouse peritoneal macrophages or rat peritoneal polymorphonuclear leukocytes in vitro. Traxanox TFA restores inhibition of antibody production in BALB c mice. Traxanox TFA is also effective in restoring antibody production in BALB c mice. Traxanox TFA has been shown to enhance phagocytosis in BALB c mice.

L-Leucyl-L-Leucine methyl ester hydrochloride (Leu-Leu-ome hydrochloride) is a dipeptide condensation product of L-leucine methyl ester produced by human monocytes or polymorphonuclear leukocytes. L-Leucyl-L-Leucine methyl ester hydrochloride selectively eliminates lymphocytes with cytotoxic potential and also induces lysosomal stress.

Gordonoside J, a compound isolated from the stem of Chrysanthemum officinale, inhibits LPS-induced nitric oxide production in rat polymorphonuclear leukocytes (PMNS).

(+)-Guaiacin, isolated from the bark of Machilus wangchiana Chun, demonstrates potent in vitro inhibition of β-glucuronidase release in rat polymorphonuclear leukocytes (PMNs) induced by platelet-activating factor (PAF).

LY 178002 is an effective inhibitor of 5-lipoxygenase (5-LPO), phospholipase A2 (IC50: 0.6 μM for 5-lipoxygenase). LY 178002 also inhibits cellular production of LTB4 by human polymorphonuclear leukocytes and displays relatively weak inhibition on cycloox

HZ52 is a potent, reversible 5-lipoxygenase (5-LO) inhibitor that blocks leukotriene (LTs) synthesis with an IC50 of 0.7 μM in intact human polymorphonuclear leukocytes [1].

LY255283 is a specific antagonit of leukotriene B4 (LTB4) receptor. It inhibits the production of LTB(4) in human peripheral blood polymorphonuclear leukocytes (PMNL) and in monocytes activated by calcium ionophore A23187.

L 651142 is a weak inhibitor of the platelet-activating factor receptor. It is also binding to polymorphonuclear leukocytes.

Gea 3162 is a potent inhibitor of ADP-induced platelet aggregation in platelet rich plasma (PRP). GEA 3162 stimulates cGMP production in granulocytes, platelets, and polymorphonuclear leukocytes.

Traxanox sodium is an orally available diuretic. Traxanox sodium enhances phagocytosis of yeast granules by mouse peritoneal macrophages or rat peritoneal polymorphonuclear leukocytes in vitro. Traxanox sodium restores inhibition of antibody production in BALB c mice. Traxanox sodium is also effective in restoring antibody production in BALB c mice. Traxanox sodium has been shown to enhance phagocytosis in BALB c mice.

PMX-205 is a cyclic hexapeptide that acts as a potent antagonist of C5a receptor (C5aR; IC50= 31 nM).1It is orally active and blocks inflammatory signaling and symptoms in animal models of colitis and allergic asthma.2,3PMX-205 is also brain penetrant and reduces neuroinflammation and neurodegeneration in an animal model of Alzheimer's disease.4 1.March, D.R., Proctor, L.M., Stoermer, M.J., et al.Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activityMol. Pharmacol.65(4)868-879(2004) 2.Jain, U., Woodruff, T.M., and Stadnyk, A.W.The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10Br. J. Pharmacol.168(2)488-501(2013) 3.Staab, E.B., Sanderson, S.D., Wells, S.M., et al.Treatment with the C5a receptor/CD88 antagonist PMX205 reduces inflammation in a murine model of allergic asthmaInt. Immunopharmacol.21(2)293-300(2014) 4.Fonseca, M.I., Ager, R.R., Chu, S.-H., et al.Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's diseaseJ. Immunol.183(2)1375-1383(2009)

Resolvin E2 (RvE2) is a member of the specialized pro-resolving mediator (SPM) family of bioactive lipids.1It is produced from eicosapentaenoic acidviaan 18-HEPE intermediate, which is formed by aspirin-acetylated COX-2-mediated oxidation of EPA, by 5-lipoxygenase (5-LO) in human polymorphonuclear (PMN) neutrophils.2,3RvE2 (20 ng/animal) inhibits increases in inflammatory exudate neutrophil infiltration in a mouse model of peritonitis induced by zymosan A .3Hepatic RvE2 levels are increased in mice fed normal chow, as well as in a mouse model of high-fat diet-induced non-alcoholic fatty liver disease (NAFLD), by dietary supplementation with EPA.4Plasma levels of RvE2 are increased by dietary supplementation with fish oil containing ω-3 polyunsaturated fatty acids (PUFAs) in patients with peripheral artery disease or chronic kidney disease.1,5,6 1.Chiang, N., and Serhan, C.N.Specialized pro-resolving mediator network: An update on production and actionsEssays Biochem.64(3)443-462(2020) 2.Tjonahen, E., Oh, S.F., Siegelman, J., et al.Resolvin E2: Identification and anti-inflammatory actions: Pivotal role of human 5-lipoxygenase in resolvin E series biosynthesisChemistry & Biology131193-1202(2006) 3.Sungwhan, F.O., Pillai, P.S., Recchiuti, A., et al.Pro-resolving actions and stereoselective biosynthesis of 18S E-series resolvins in human leukocytes and murine inflammationJ. Clin. Invest.121(2)569-581(2011) 4.Echeverría, F., Valenzuela, R., Espinosa, A., et al.Reduction of high-fat diet-induced liver proinflammatory state by eicosapentaenoic acid plus hydroxytyrosol supplementation: Involvement of resolvins RvE1/2 and RvD1/2J. Nutr. Biochem.6335-43(2019) 5.Ramirez, J.L., Gasper, W.J., Khetani, S.A., et al.Fish oil increases specialized pro-resolving lipid mediators in PAD (the OMEGA-PAD II trial)J. Surg. Res.238164-174(2019) 6.Barden, A.E., Shinde, S., Burke, V., et al.The effect of n-3 fatty acids and coenzyme Q10 supplementation on neutrophil leukotrienes, mediators of inflammation resolution and myeloperoxidase in chronic kidney diseaseProstaglandins Other Lipid Mediat.1361-8(2018)

Leukotriene B5 (LTB5) is a metabolite of eicosapentaenoic acid formed via the 5-lipoxygenase (5-LO) pathway, possessing diverse biological activities, including the ability to increase contraction of bullfrog lung strips ex vivo in a concentration-dependent manner.

H-Leu-Leu-OMe . HBr is a dipeptide condensation product of L-leucine methyl ester generated by human monocytes or polymorphonuclear leukocytes. H-Leu-Leu-OMe . HBr induces endolysosomal pathway stress and selectively eliminates lymphocytes with cytotoxic potential.

1,2,3-Trieicosapentaenoyl-rac-glycerol (EPA-TG) is a glycerol ester of eicosapentaenoic acid , which is an ω-3 fatty acid. An EPA-TG emulsion, administered i.v., lowers leukotriene B4 production by 40% in polymorphonuclear leukocytes from rabbits and reduces platelet aggregation. It suppresses natural killer cell activity both in vitro and in vivo, in human lymphocytes and murine spleens, respectively, with the in vivo effects lasting up to seven days.

Lipoxin B4 is a metabolite of arachidonic acid that inhibits leukocyte infiltration and mucus secretion in the nasal mucosa of the upper respiratory tract, exhibiting mucosal protective effects. It is commonly used in studies of allergic inflammation in the upper and lower respiratory tracts.

5(S),12(S)-DiHETE is a natural bioactive lipid derived from arachidonic acid . It is synthesized by glycogen-induced rabbit peritoneal polymorphonuclear leukocytes (PMNLs) incubated with AA. 5(S),12(S)-DiHETE can be produced by successive oxygenation of AA by 5-lipoxygenase (5-LO) in platelets and 12-LO in leukocytes. It can also be synthesized from 12(S)-HETE by 5-LO, in the presence of 5-LO activating protein (FLAP), activated with calcium ionophore. 5(S),12(S)-DiHETE is an epimer of leukotriene B4 that is weakly chemotactic for PMNL.

13(S)-HODE is the lipoxygenase metabolite of linoleic acid. 13(S)-HODE modulates the platelet-activating factor, leukotriene B4, and formyl-Met-Leu-Phe-induced calcium influx in human polymorphonuclear leukocytes. The mechanism by which 13(S)-HODE elicits its inhibitory effect is still unclear. The use of biotinylated 15(S)-HETE as a probe for detecting binding proteins and/or receptors that specifically bind 15(S)-HETE provides a basis for similar use of 13(S)-HODE-biotin.

Defensin HNP-3 is a peptide secreted by human polymorphonuclear leukocytes (PMNs) that has antimicrobial properties. It induces lysis of mammalian cells when used at a concentration of 25 μg/mL. It also inhibits growth of E. faecalis (ED50 = 100 nM) and clinical isolates of P. aeruginosa (MIC90 = 4 μM). HNP-3 binds to recombinant HIV-1 envelope glycoprotein (gp120) and human CD4 (Kds = 52.8 and 34.9 nM, respectively). It also binds to recombinant, immobilized human surfactant protein D (SP-D; Kd = 55.7 nM) and inhibits focus formation in Madin-Darby canine kidney (MDCK) cells infected with influenza A virus (IAV).

Lipoxin B4 (LXB4) methyl ester is a lipid-soluble prodrug form of the transcellular metabolite LXB4, which is a positional isomer of LXA4 produced by the metabolism of 15-HETE or 15-HpETE by human leukocytes. At 100 nM, LXB4 inhibits polymorphonuclear leukocyte (PMN) migration stimulated by leukotriene B4 and inhibits LTB4-induced adhesion of PMNs with an IC50 of 0.3 nM.

1. Praeruptorin C and E can relax swine coronary artery and decrease contractility in guinea-pig left atria, these effects are similar in many respects to those displayed by drugs that have calcium entry blocking activity. 2. Praeruptorin D and E can prot

Aseanostatin P5 inhibits myeloperoxidase (MPO) release from human polymorphonuclear leukocytes.