The effects of phosphodiesterase type 4 inhibitors on tumour necrosis factor-α and leukotriene B4 in a novel human whole blood assay

British Journal of Pharmacology

Volumn 126, Issue 4, 1999, Pages 979-988

  Brideau, Christine ^a   Van Staden, Carlo ^a   Styhler, Angela ^a   Rodger, Ian W ^a   Chan, Chi Chung ^a  

^a MERCK FROSST CENTRE FOR THERAPEUTIC RESEARCH   (Canada)

Author keywords

Leukotriene B4; Phosphodiesterase; Tumour necrosis factor ; Whole blood

Indexed keywords

3 [6 [7 CYANO 5 (3 FURYL) 2 NAPHTHOXYMETHYL] 2 PYRIDYL] 3 HYDROXY 6,8 DIOXABICYCLO[3.2.1]OCTANE; CALCIMYCIN; FORMYLMETHIONYLLEUCYLPHENYLALANINE; INDOMETACIN; LEUKOTRIENE B4; LIPOPOLYSACCHARIDE; PHOSPHODIESTERASE IV INHIBITOR; PICLAMILAST; PROSTAGLANDIN E2; TUMOR NECROSIS FACTOR ALPHA;

ANTIINFLAMMATORY ACTIVITY; ARTICLE; BLOOD LEVEL; CONTROLLED STUDY; DRUG POTENCY; HUMAN; PRIORITY JOURNAL; STEREOCHEMISTRY;

EID: 0032934381     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0702387     Document Type: Article

References (61)

1. Arias-Negrete, S., Keller, K. & Chadee, K. (1995). Proinflammatory cytokines regulate cyclooxygenase-2 mRNA expression in human macrophages. Biochem. Biophys. Res. Commun., 208, 582-589.
2. Banner, K.H., Moriggi, E., Da Ros, B., Schioppacassi, G., Semeraro, C. & Page, C.P. (1996). The effect of selective phosphodiesterase 3 and 4 isoenzyme inhibitors and established anti-asthma drugs on inflammatory cell activation. Br. J. Pharmacol., 119, 1255-1261.
3. Batten, P., Yacoub, M.H. & Rose, M.L. (1996). Effect of human cytokines (IFN-gamma, TNF-alpha, IL-1 beta, IL-4) on porcine endothelial cells: induction of MHC and adhesion molecules and functional significance of these changes. Immunology, 87, 127-133.
4. Beutler, B. & Cerami, A. (1989). The biology of cachectin/TNF-a primary mediator of the host response. Annu. Rev. Immunol., 7, 625-655.
5. Borgeat, P. & Samuelsson, B. (1979). Arachidonic acid metabolism in polymorphonuclear leukocytes: effects of ionophore A23187. Proc. Natl. Acad. Sci. U.S.A., 76, 2148-2152.
6. Brain, S., Camp, R., Dowd, P., Black, A.K. & Greaves, M. (1984). The release of leukotriene B4-like material in biologically active amounts from the lesional skin of patients with psoriasis. J. Invest. Dermatol., 83, 70-73.
7. Brideau, C., Kargman, S., Liu, S., Dallob, A., Ehrich, E., Rodger, I.W. & Chan, C.C. (1996). A human whole blood assay for clinical evaluation of biochemical efficacy of cyclooxygenase inhibitors. Inflamm. Res., 45, 68-74.
8. Christensen, S.B., Guider, A., Forster, C.J., Gleason, J.G., Bender, P.E., Karpinski, J.M., Dewolf Jr W.E., Barnette, M.S., Underwood, D.C., Griswold, D.E., Cieslinski, L.B., Burman, M., Bochnowicz, S., Osborn, R.R., Manning, C.D., Grous, M., Hillegas, L.M., Bartus, J.O., Ryan, M.D., Eggleston, D.S., Haltiwanger, R.C. & Torphy, T.J. (1998). 1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma. J. Med. Chem., 41, 821-835.
9. Coleman, R.A., Smith, W.L. & Narumiya, S. (1994). International Union of Pharmacology classification of prostanoid receptors: properties, distribution, and structure of the receptors and their subtypes. Pharmacol. Re., 46, 205-229.
10. Cortijo, J., Villagrasa, V., Navarette, C., Zanz, C., Berto, L., Michel, A., Bonnet, P.A. & Morcillo, E.J. (1996). Effects of SCA40 on human isolated bronchus and human polymorphonuclear leukocytes: comparison with rolipram, SFK94120 and levcromakalim. Br. J. Pharmacol., 119, 99-106.
11. Davidson, E.M., Rae, S.A. & Smith, M.J. (1983). Leukotriene B4, a mediator of inflammation present in synovial fluid in rheumatoid arthritis. Ann. Rheum. Dis., 42, 677-679.
12. Dinarello, C.A., Cannon, J.G., Wolff, S.M., Bernheim, H.A., Beutler, B., Cerami, A., Figari, I.S., Palladino, Jr M.A. & O'Connor, J.V. (1986). Tumor necrosis factor (cachectin) is an endogenous pyrogen and induces production of interleukin 1. J. Exp. Med., 163, 1433-1450.
13. Doerfler, M.E., Danner, R.L., Shelhamer, J.H., & Parrillo, J.E. (1989). Bacterial lipopolysaccharides prime human neutrophils for enhanced production of leukotriene B4. J. Clin. Invest., 83, 970-977.
14. Eigler, A., Greten, T.F., Sinha, B., Haslberger, C., Sullivan, G.W. & Endres, S. (1997). Endogenous adenosine curtails lipopolysaccharide-stimulated tumour necrosis factor synthesis. Scand. J. Immunol., 45, 132-139.
15. Eigler, A., Sinha, B., Hartmann, G. & Endres, S. (1997). Taming TNF: strategies to restrain this proinflammatory cytokine. Immunology Today, 8, 487-492.
16. Essayan, D.M., Kagey-Sobotka, A., Lichtenstein, L.M. & Huang, S.K. (1997). Differential regulation of human antigen-specific Th1 and Th2 lymphocyte responses by isozyme selective cyclic nucleotide phosphodiesterase inhibitors. J. Pharmacol. Exp. Ther., 282, 505-512.
17. Foey, A.D., Parry, S.L., Williams, L.M., Feldmann, M., Foxwell, B.M. & Brennan, F.M. (1998). Regulation of monocyte IL-10 synthesis by endogenous IL-1 and TNF-alpha: role of the p38 and p42/44 mitogen-activated protein kinases. J. Immunol., 160, 920-928.
18. Fonteh, A.N., Winkler, J.D., Torphy, T.J., Heravi, J., Uundem, B.J. & Chilton, F.H. (1993). Influence of isoproterenol and phosphodiesterase inhibitors on platelet-activating factor biosynthesis in the human neutrophil. J. Immunol., 151, 339-350.
19. Ford-Hutchinson, A.W. (1990). Leukotriene B4 in inflammation. Crit. Rev. Immunol., 10, 1-12.
20. Gordon, J.R. & Galli, S.J. (1991). Release of both preformed and newly synthesized tumor necrosis factor alpha(TNF-alpha)/ cachectin by mouse mast cells stimulated via the Fc epsilon RI. A mechanism for the sustained action of mast cell-derived TNF-alpha during IgE-dependent biological responses. J. Exp. Med., 174, 103-107.
21. Grabbe, J., Czarnetzki, B.M., Rosenbach, T. & Mardin, M. (1984). Identification of chemotactic lipoxygenase products of arachidonate metabolism in psoriatic skin. J. Invest. Dermatol., 82, 477-479.
22. Hamel, P., Riendeau, D., Brideau, C., Chan, C.C., Desmarais, S., Delorme, D., Dube, D., Ducharme, Y., Ethier, D., Grimm, E., Falgueyret, J.P., Guay, J., Jones, T.R., Kwong, E., McAuliffe, M., McFarlane, C.S., Piechuta, H., Roumi, M., Tagari, P., Young, R.N. & Girard, Y. (1997). Substituted (pyridylmethoxy) naphthalenes as potent and orally active 5-lipoxygenase inhibitors; synthesis, biological profile, and pharmacokinetics of L-739,010. J. Med. Chem., 40, 2866-2875.
23. Han, J., Thompson, P. & Beutler, B. (1990). Dexamethasone and pentoxifylline inhibit endotoxin-induced cachectin/tumor necrosis factor synthesis at separate points in the signaling pathway. J. Exp. Med., 172, 391-394.
24. Hartman, D.A., Ochalski, S.J & Carlson, R.P. (1993). The effects of anti-inflammatory and antiallergic drugs on the release of IL-1 beta and TNF-alpha in the human whole blood assay. Agents Actions, 39, C70-C72.
25. Hartman, D.A., Ochalski, S.J. & Carlson, R.P. (1995). The effects of antiinflammatory and antiallergic drugs on cytokine release after stimulation of human whole blood by lipopolysaccharide and zymosan A. Inflamm. Res., 44, 269-274.
26. Hughes, B., Howat, D., Lisle, H., Holbrook, M., James, T., Gozzard, N., Blease, K., Hughes, P., Kingaby, R., Warrellow, G., Alexander, R., Head, J., Boyd, E., Eaton, M., Perry, M., Wales, M., Smith, B., Owens, R., Catterall, C., Lumb, S., Russell, A., Allen, R., Merriman, M., Bloxham, D. & Higgs, G. (1996). The inhibition of antigen-induced eosinophilia and bronchoconstriction by CDP840, a novel stereo-selective inhibitor of phosphodiesterase type 4. Br. J. Pharmacol., 118, 1183-1191.
27. Jia, S.F. & Kleinerman, E.S. (1991). Antitumor activity of TNF-alpha, IL-1, and IFN-gamma against three human osteosarcoma cell lines. Lymph. Cyto. Res., 10, 281-284.
28. Kaminuma, O., Mori, A., Suko, M., Nishizaki, Y., Kikkawa, H., Ikezawa, K. & Okudaira, H. (1996). A novel phosphodiesterase inhibitor, T-440: possible management of eosinophilic inflammation by down-regulation of interleukin-5 production. Int. Arch. Allergy Immunol., 111, 16-18.
29. Krakauer, T. & Oppenheim, J.J. (1993). II-1 and tumor necrosis factor-alpha each up-regulate both the expression of IFN-gamma receptors and enhance IFN-gamma-induced HLA-DR expression on human monocytes and a human monocytic cell line (THP-1). J. Immunol., 150, 1205-1211.
30. 4 synthesis in whole blood ex vivo. Br. J. Pharmacol., 117, 1639-1644.
31. Larsen, J.S. & Jackson, S.K. (1996). Antileukotriene therapy for asthma. Am. J. Health. Syst. Pharm., 53, 2821-2830.
32. Mackay, F., Loetscher, H., Stueber, D., Gehr, G. & Lesslauer, W. (1993). Tumor necrosis factor alpha (TNF-alpha)-induced cell adhesion to human endothelial cells in under dominant control of one TNF receptor type, TNF-R55. J. Exp. Med., 177. 1277-1286.
33. Manning, C.D., McLaughlin, M.M., Livi, G.P., Cieslinski, L.B., Torphy, T.J. & Barnette, M.S. (1996). Prolonged beta adrenoceptor stimulation up-regulates cAMP phosphodiesterase activity in human monocytes by increasing mRNA and protein for phosphodiesterase 4A and 4B. J. Pharmacol. Exp. Ther., 276, 810-818.
34. 2 inhibits lipopolysaccharide-induced tumour necrosis factor-α generation. Br. J. Pharmacol., 122, 149-157.
35. Mohri, M., Spriggs, D.R. & Kuge, D. (1990). Effects of lipopolysaccharide on phospholipase A2 activity and tumor necrosis factor expression in HL-60 cells. J. Immunol., 144, 2678-2682.
36. Nakane, A., Numata, A. & Minagawa, T. (1992). Endogenous tumor necrosis factor, interleukin-6, and gamma interferon levels during Listeria monocytogenes infection in mice. Infect. Immun., 60, 523-528.
37. Nielson, C.P., Vestal, R.E., Sturm, R.J. & Heaslip, R. (1990). Effects of selective phosphodiesterase inhibitors on the polymorphonuclear leukocyte respiratory burst. J. Allergy Clin. Immunol., 86, 801-808.
38. Ollivier, V., Parry, G.C.N., Cobb, R.R., De Prost, D. & Mackman, N. (1996). Elevated cyclic AMP inhibits NF-kappaB-mediated transcription in human monocytic cells and endothelial cells. J. Biol. Chem., 271, 20828-20835.
39. Oshima, M., Dinchuk, J.E., Kargman, S.L., Oshima, H., Hancock, B., Kwong, E., Trzaskos, J.M., Evans, J.F. & Taketo, M.M. (1996). Suppression of intestinal polyposis in Apc delta716 knockout mice by inhibition of cyclooxygenase 2 (COX-2). Cell, 87, 803-809.
40. Patrignani, P., Panara, M.R., Greco, A., Fusco, O., Natoli, C., Iacobelli, S., Cipollone, F., Ganci, A., Creminon, C., Maclouf, J. & Patrono, C. (1994). Biochemical and pharmacological characterization of the cyclooxygenase activity of human whole blood prostaglandin endoperoxide synthases. J. Pharmacol. Exp. Ther., 271, 1705-1712.
41. Schade, F.U. & Schudt, C. (1993). The specific type III and IV phosphodiesterase inhibitor zardaverine suppresses formation of tumor necrosis factor by macrophages. Eur. J. Pharmacol., 230, 9-14.
42. Scheurich, P., Thoma, B., Ucer, U. & Pfizenmaier, K. (1987). Immunoregulatory activity of recombinant human tumor necrosis factor (TNF)-alpha: induction of TNF receptors on human T cells and TNF-alpha-mediated enhancement of T cell responses. J. Immunol., 138, 1786-1790.
43. Schudt, C., Tenor, H. & Hatzelmann, A. (1995). PDE isoenzymes as targets for anti-asthma drugs. Eur. Respir. J., 8, 1179-1183.
44. Schudt, C., Winder, S., Forderkunz, S., Hatzelmann, A. & Ullrich, V. (1991). Influence of selective phosphodiesterase inhibitors on human neutrophil functions and levels of cAMP and Cai. Naunyn Schmiedebergs Arch. Pharmacol., 344, 682-690.
45. Schutze, S., Wiegmann, K., Machleidt, T. & Kronke, M. (1995). TNF-induced activation of NF-kappa B. Immunobiology, 193, 193-203.
46. Seldon, P.M., Barnes, P.J., Meja, K. & Giembycz, M.A. (1995). Suppression of lipopolysaccharide-induced tumor necrosis factor-alpha generation from human peripheral blood monocytes by inhibitors of phosphodiesterase 4: interaction with stimulants of adenylyl cyclase. Mol. Pharmacol., 48, 747-757.
47. Sharon, P. & Stenson, W.F. (1984). Enhanced synthesis of leukotriene B4 by colonic mucosa in inflammatory bowel disease. Gastroenterology, 86, 453-460.
48. Souness, J.E., Griffin, M., Maslen, C., Ebsworth, K., Scott, L.C., Pollock, K., Palreyman, M.N. & Karlsson, J.A. (1996). Evidence that cyclic AMP phosphodiesterase inhibitors suppress TNF alpha generation from human monocytes by interacting with a 'low-affinity' phosphodiesterase 4 conformer. Br. J. Pharmacol., 118, 649-658.
49. Souness, J.E., Maslen, C., Webber, S., Foster, M., Raeburn, D., Palfreyman, M.N., Ashton, M.J. & Karlsson, J.A. (1995). Suppression of eosinophil function by RP 73401, a potent and selective inhibitor of cyclic AMP-specific phosphodiesterase: comparison with rolipram. Br. J. Pharmacol., 115, 39-46.
50. Surette, M.E., Palmantier, R., Gosselin, J & Borgeat, P. (1993). Lipopolysaccharides prime whole human blood and isolated neutrophils for the increased synthesis of 5-lipoxygenase products by enhancing arachidonic acid availability: Involvement of the CD14 antigen. J. Exp. Med., 178, 1347-1355.
51. Talpain, E., Armstrong, R.A., Coleman, R.A. & Vardey, C.J. (1995). Characterization of the PGE receptor subtype mediating inhibition of superoxide production in human neutrophils. Br. J. Pharmacol., 114, 1459-1465.
52. Torphy, T.J., Christensen, S.B., Barnette, M.S., Burman, M., Cieslinski, L.B. & DeWolf, W.E. (1997). Molecular basis for an improved therapeutic index of SB 207499, a second generation phosphodiesterase 4 inhibitor (Abstract). Eur. Respir. J., 10, 313s.
53. Torphy, T.J. & Undem, B.J. (1991). Phosphodiesterase inhibitors: new opportunities for the treatment of asthma. Thorax, 46, 512-523.
54. Torphy, T.J., Zhou, H.L. & Cieslinski, L.B. (1992). Stimulation of beta adrenoceptors in a human monocyte cell line (U937) up-regulates cyclic AMP-specific phosphodiesterase activity. J. Pharm. Exp. Ther., 263, 1195-1205.
55. Tracey, K.J., Beutler, B., Lowry, S.F., Merryweather, J., Wolpe, S., Milsark, I.W., Hariri, R.J., Fahey III T.J., Zentella, A., Albert, J.D., Shires, T., & Cerami A. (1986). Shock and tissue injury induced by recombinant human cachectin. Science, 234, 470-474.
56. Trefzer, U., Brockhaus, M., Lotscher, H., Parlow, F., Budnick, A., Grewe, M., Christop, H., Kapp, A., Schopf, E., Luger, T.A. & Krutmann J. (1993). The 55-kD tumor necrosis factor receptor on human keratinocytes is regulated by tumor necrosis factor-alpha and by ultraviolet B radiation. J. Clin. Invest., 92, 462-470.
57. Underwood, D.C., Kotzer, C.J., Bochnowicz, S., Osborn, R.R., Luttmann, M.A., Hay, D.W. & Torphy, T.J. (1994). Comparison of phosphodiesterase III, IV and dual III/IV inhibitors on bronchospasm and pulmonary eosinophil influx in guinea pigs. J. Pharmacol. Exp. Ther., 270, 250-259.
58. Valyi-Nagy, I., Jensen, P.J., Albelda, S.M. & Rodeck, U. (1992). Cytokine-induced expression of transforming growth factor-alpha and the epidermal growth factor receptor in neonatal skin explants. J. Invest. Dermatol., 99, 350-356.
59. Villagrasa, V., Navarete, C., Sanz, C., Berto, L., Perpina, M., Cortijo, J. & Morcillo, E.J. (1996). Inhibition of phosphodiesterase IV and intracellular calcium levels in human polymorphonuclear leukocytes. Methods Find. Exp. Clin. Pharmacol., 18, 239-245.
60. Warren, J.S., Ward, P.A. & Johnson, K.J. (1988). Tumor necrosis factor: a plurifunctional mediator of acute inflammation. Mod. Pathol., 1, 242-247.
61. Wilhelm, R.S. & Fatheree, P.R. (1994). WO patent 22852.