Inhibition of leukotriene synthesis, pharmacokinetics, and tolerability of a novel dietary fatty acid formulation in healthy adult subjects

Clinical Therapeutics

Volumn 25, Issue 3, 2003, Pages 948-971

  Surette, Marc E ^a,b,c   Koumenis, Iphigenia L ^a   Edens, Michelle B ^a   Tramposch, Kenneth M ^a   Chilton, Floyd H ^a,b  

^a Pilot Therapeutics Inc   (United States)

^b WAKE FOREST SCHOOL OF MEDICINE   (United States)

^c NONE   (United States)

Author keywords

5 lipoxygenase; Allergy; Arachidonic acid; Diet; Leukotriene

Indexed keywords

ALANINE AMINOTRANSFERASE; ARACHIDONIC ACID; FATTY ACID; GAMMA LINOLENIC ACID; ICOSAPENTAENOIC ACID; LEUKOTRIENE; OLIVE OIL; PLACEBO; PLT 3514; POLYUNSATURATED FATTY ACID;

ADULT; ANOREXIA; ARTICLE; BIOSYNTHESIS; CLINICAL ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DIET SUPPLEMENTATION; DOUBLE BLIND PROCEDURE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG TOLERABILITY; EMULSION; ERUCTATION; FAT INTAKE; FATTY ACID BLOOD LEVEL; FEMALE; HEADACHE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; INFLAMMATORY CELL; LABORATORY TEST; MALE; MAXIMUM TOLERATED DOSE; NAUSEA; NORMAL HUMAN; RANDOMIZED CONTROLLED TRIAL; ULTRAVIOLET RADIATION;

EID: 0037361911     PISSN: 01492918     EISSN: 1879114X     Source Type: Journal    
DOI: 10.1016/S0149-2918(03)80116-9     Document Type: Article

References (35)

1. Samuelsson B. Prostaglandins, thromboxanes, and leukotrienes: Formation and biological roles. Harvey Lect. 1979;75:1-40.
2. Murphy RC, Hammarstrom S, Samuelsson B. Leukotriene C: A slow-reacting substance from murine mastocytoma cells. Proc Natl Acad Sci U S A. 1979;76:4275-4279.
3. Smith MJ, Ford-Hutchinson AW, Bray MA. Leukotriene B: A potential mediator of inflammation. J Pharm Pharmacol. 1980;32:517-518.
4. Piper PJ, Samhoun MN, Tippins JR, et al. Slow-reacting substances and their formation by a lipoxygenase pathway. Agents Actions. 1980;10:541-547.
5. Goetzl EJ. Leukocyte recognition and metabolism of leukotrienes. Fed Proc. 1983;42:3128-3131.
6. Leff JA, Busse WW, Pearlman D, et al. Montelukast, a leukotriene-receptor antagonist, for the treatment of mild asthma and exercise-induced bronchoconstriction. N Engl J Med. 1998;339:147-152.
7. Kane GC, Pollice M, Kim CJ, et al. A controlled trial of the effect of the 5-lipoxygenase inhibitor, zileuton, on lung inflammation produced by segmental antigen challenge in human beings. J Allergy Clin Immunol. 1996;97:646-654.
8. Wenzel SE, Trudeau JB, Kaminsky DA, et al. Effect of 5-lipoxygenase inhibition on bronchoconstriction and airway inflammation in nocturnal asthma. Am J Respir Crit Care Med. 1995;152:897-905.
9. Barham JB, Edens MB, Fonteh AN, et al. Addition of eicosapentaenoic acid to gamma-linolenic acid-supplemented diets prevents serum arachidonic acid accumulation in humans. J Nutr. 2000;130:1925-1931.
10. Johnson MM, Swan DD, Surette ME, et al. Dietary supplementation with gamma-linolenic acid alters fatty acid content and eicosanoid production in healthy humans. J Nutr. 1997;127:1435-1444.
11. Pullman-Mooar S, Laposata M, Lem D, et al. Alteration of the cellular fatty acid profile and the production of eicosanoids in human monocytes by gamma-linolenic acid. Arthritis Rheum. 1990;33:1526-1533.
12. Ziboh VA, Fletcher MP. Dose-response effects of dietary gamma-linolenic acid-enriched oils on human polymorphonuclear-neutrophil biosynthesis of leukotriene B4. Am J Clin Nutr. 1992;55:39-45.
13. Chapkin RS, Miller CC, Somers SD, Erickson KL. Utilization of dihomo-gamma-linolenic acid (8,11,14-eicosatrienoic acid) by murine peritoneal macrophages. Biochim Biophys Acta. 1988;959:322-331.
14. Chapkin RS, Miller CC, Somers SD, Erickson KL. Ability of 15-hydroxyeicosatrienoic acid (15-OH-20:3) to modulate macrophage arachidonic acid metabolism. Biochem Biophys Res Commun. 1988;153:799-804.
15. Miller CC, Ziboh VA. Gammalinolenic acid-enriched diet alters cutaneous eicosanoids. Biochem Biophys Res Commun. 1988;154:967-974.
16. Chilton-Lopez T, Surette ME, Swan DD, et al. Metabolism of gammalinolenic acid in human neutrophils. J Immunol. 1996;156:2941-2947.
17. Surette ME, Winkler JD, Fonteh AN, Chilton FH. Relationship between arachidonate-phospholipid remodeling and apoptosis. Biochemistry. 1996;35:9187-9196.
18. Bligh EG, Dyer WJ. A rapid method of total lipid extraction and purification. Can J Biochem Physiol. 1959;37:911-917.
19. Surette ME, Odeimat A, Palmantier R, et al. Reverse-phase high-performance liquid chromatography analysis of arachidonic acid metabolites in plasma after stimulation of whole blood ex vivo. Anal Biochem. 1994;216:392-400.
20. Seyberth HW, Oelz O, Kennedy T, et al. Increased arachidonate in lipids after administration to man: Effects on prostaglandin biosynthesis. Clin Pharmacol Ther. 1975;18:521-529.
21. Surette ME, Krump E, Picard S, Borgeat P. Activation of leukotriene synthesis in human neutrophils by exogenous arachidonic acid: Inhibition by adenosine A(2a) receptor agonists and crucial role of autocrine activation by leukotriene B(4). Mol Pharmacol 1999;56:1055-1062.
22. 4 biosynthesis by endogenous adenosine in ligand-activated human neutrophils. J Exp Med. 1997;186:1401-1406.
23. 4 by human platelets. A potential cellular source of leukotriene C4. J Biol Chem. 1988;263:174-181.
24. Fiore S, Serhan CN. Formation of lipoxins and leukotrienes during receptor-mediated interactions of human platelets and recombinant human granulocyte/macrophage colony-stimulating factor-primed neutrophils. J Exp Med. 1990;172:1451-1457.
25. Gronert K, Clish CB, Romano M, Serhan CN. Transcellular regulation of eicosanoid biosynthesis. Methods Mol Biol. 1999;120:119-144.
26. Entressangles B, Sari H, Desnuelle P. On the positional specificity of pancreatic lipase. Biochim Biophys Acta. 1966;125:597-600.
27. Decker EA. The role of stereospecific saturated fatty acid positions on lipid nutrition. Nutr Rev. 1996;54:108-110.
28. Harris WS, Muzio F. Fish oil reduces postprandial triglyceride concentrations without accelerating lipid-emulsion removal rates. Am J Clin Nutr. 1993;58:68-74.
29. Roche HM, Gibney MJ. Long-chain n-3 polyunsaturated fatty acids and triacylglycerol metabolism in the postprandial state. Lipids. 1999;34(Suppl):S259-S265.
30. Harris WS. n-3 Fatty acids and serum lipoproteins: Human studies. Am J Clin Nutr. 1997;65(Suppl 5):S1645-S1654.
31. Hammond BG, Mayhew DA, Naylor MW, et al. Safety assessment of DHA-rich microalgae from Schizochytrium sp. Regul Toxicol Pharmacol. 2001;33:192-204.
32. Hempenius RA, Van Delft JM, Prinsen M, Lina BA. Preliminary safety assessment of an arachidonic acid-enriched oil derived from Mortierella alpina: Summary of toxicological data. Food Chem Toxicol. 1997;35:573-581.
33. Ritskes-Hoitinga J, Verschuren PM, Meijer GW, et al. The association of increasing dietary concentrations of fish oil with hepatotoxic effects and a higher degree of aorta atherosclerosis in the ad lib-fed rabbit. Food Chem Toxicol. 1998;36:663-672.
34. Eritsland J, Seljeflot I, Abdelnoor M, et al. Long-term effects of n-3 fatty acids on serum lipids and glycaemic control. Scand J Clin Lab Invest. 1994;54:273-280.
35. Schmidt EB, Møller JM, Svaneborg N, Dyerberg J. Safety aspects of fish oils. Experiences with an n-3 concentrate of re-esterified triglycerides (Pikasol®). Drug Invest. 1994;7:215-220.