Effects of bosentan on cellular processes involved in pulmonary arterial hypertension: Do they explain the long-term benefit?

Annals of Medicine

Volumn 35, Issue 8, 2003, Pages 605-613

  Clozel, Martine ^a  

^a ACTELION PHARMACEUTICALS LTD   (Switzerland)

Author keywords

Bosentan; Endothelin; Endothelin receptors; Pulmonary hypertension

Indexed keywords

ACETYLCHOLINE; BOSENTAN; ENDOTHELIN 1; ENDOTHELIN A RECEPTOR; ENDOTHELIN B RECEPTOR;

ANTIINFLAMMATORY ACTIVITY; BINDING AFFINITY; DRUG ACTIVITY; DRUG EFFECT; DRUG EFFICACY; DRUG MECHANISM; DRUG RECEPTOR BINDING; HEART VENTRICLE REMODELING; HORMONE ACTION; HUMAN; INFLAMMATION; LONG TERM CARE; LUNG FIBROSIS; NONHUMAN; PATHOPHYSIOLOGY; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN EXPRESSION; PULMONARY HYPERTENSION; REVIEW; VASODILATATION;

ANIMALS; ANTIHYPERTENSIVE AGENTS; ENDOTHELIUM, VASCULAR; HUMANS; HYPERTENSION, PULMONARY; PULMONARY ARTERY; PULMONARY FIBROSIS; SULFONAMIDES;

EID: 0346888758     PISSN: 07853890     EISSN: None     Source Type: Journal    
DOI: 10.1080/07853890310017477     Document Type: Review

References (79)

1. Rich S. Primary Pulmonary Hypertension: Executive Summary. World symposium on primary pulmonary hypertension, 1998 (Evian, France) Vol. 2002:1998.
2. Giaid A, Yanagisawa M, Langleben D, Michel RP, Levy R, Shennib H, et al. Expression of endothelin-1 in the lungs of patients with pulmonary hypertension. N Engl J Med 1993; 328:1732-9.
3. Gaine SP, Rubin LJ. Primary pulmonary hypertension. Lancet 1998;352:719-25.
4. Rubin LJ. Primary pulmonary hypertension. N Engl J Med 1997;336:111-7.
5. Rubens C, Ewert R, Halank M, Wensel R, Orzechowski H-D, Schultheiss H-P, et al. Big endothelin-1 and endothelin-1 plasma levels are correlated with the severity of primary pulmonary hypertension. Chest 2001;120:1562-9.
6. Galiè N, Grigioni F, Bacchi-Reggiani K, Ussia GP, Parlangeli R, Catanzariti P, et al. Relation of endothelin-1 to survival in patients with primary pulmonary hypertension. Eur J Clin Invest 1996;26:273.
7. Li H, Chen S-J, Chen Y-F, Cheng Q, Meng C, Durand J, et al. Enhanced endothelin-1 and endothelin receptor gene expression in chronic hypoxia. J Appl Physiol 1994;77:1451-9.
8. Shi-wen X, Denton CP, Dashwood MR, Holmes AM, BouGharios G, Pearson JD, et al. Fibroblast matrix gene expression and connective tissue remodeling: Role of endothelin-1. J Invest Dermatol 2001;116:417-25.
9. Sakai S, Miyauchi T, Kobayashi M, Yamaguchi I, Goto K, Sugishita Y. Inhibition of myocardial endothelin pathway improves long-term survival in heart failure. Nature 1996;384: 353-5.
10. Bauer M, Wilkens H, Langer F, Schneider SO, Lausberg H, Schafers HJ. Selective upregulation of endothelin B receptor gene expression in severe pulmonary hypertension. Circulation 2002;105:1034-6.
11. Clozel M, Breu V, Gray GA, Kalina B, Loffler B-M, Burri K, et al. Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. J Pharmacol Exper Therapeut 1994;270:228-35.
12. Iwasa S, Fan J, Shimokama T, Nagata M, Watanabe T. Increased immunoreactivity of endothelin-1 and endothelin B receptor in human atherosclerotic lesions. A possible role in atherogenesis. Atherosclerosis 1999;146(1)93-100.
13. Roux S, Loffler BM, Gray GA, Sprecher U, Clozel M, Clozel JP. The role of endothelin in experimental cerebral vasospasm. Neurosurgery 1995;37:78-86.
14. Kakoki M, Hirata Y, Hayakawa H, Tojo A, Nagata D, Suzuki E, et al. Effects of hypertension, diabetes mellitus, and hypercholesterolemia on endothelin type B receptor-mediated nitric oxide release from rat kidney. Circulation 1999;99:1242-8.
15. Abraham DJ, Vancheeswaran R, et al. Increased levels of endothelin-1 and differential endothelin type A dn B receptor expression in scleroderma-associated fibrotic lung disease. Am J Pathol 1997;151:831-41.
16. Dagassan PH, Breu V, Clozel M, Kunzli A, Vogt P, Turina M, et al. Up-regulation of endothelin-B receptors in atherosclerotic human coronary arteries. J Cardiovasc Pharmacol 1996;27: 147-53.
17. Sargent CA, Liu EC, Chao CC, Monshizadegan H, Webb ML, Grover GJ. Role of endothelin receptor subtype B (ET-B) in myocardial ischemia. Life Sci 1994;55:1833-44.
18. McLaughlin V, Sitbon O, Rubin LJ, Levy P, Barst R, Badesch D, et al. The Effect of First-Line Bosentan on Survival of Patients with Primary Pulmonary Hypertension. Am J Respir Crit Care Med 2003;167:A441.
19. Rossi GP, Seccia TM, Albertin G, Pessina AC. Measurement of endothelin: clinical and research use. Ann Clin Biochem 2000;37:608-26.
20. Jeffery TK, Morrell NW. Molecular and cellular basis of pulmonary vascular remodeling in pulmonary hypertension. Prog Cardiovasc Dis 2002;45:173-202.
21. Jeffery TK, Wanstall JC. Pulmonary vascular remodeling: a target for therapeutic intervention in pulmonary hypertension. Pharmacol Ther 2001;92:1-20.
22. Teder P, Noble PW. A cytokine reborn? Endothelin-1 in pulmonary inflammation and fibrosis. Am J Respir Cell Mol Biol 2000;23:7-10.
23. Teerlink JR, Carteaux JP, Sprecher U, Loffler BM, Clozel M, Clozel JP. Role of endogenous endothelin in normal hemodynamic status of anesthetized dogs. Am J Physiol 1995;268: H432-40.
24. Weber C, Schmitt R, Birnboeck H, Hopfgartner G, van Marle SP, Peeters PAM, et al. Pharmacokinetics and pharmacodynamics of the endothelin-receptor antagonist bosentan in healthy human subjects. Clin Pharmacol Ther 1996;60:124-37.
25. Chen SJ, Chen YF, Meng QC, Durand J, Dicarlo VS, Oparil S. Endothelin-receptor antagonist bosentan prevents and reverses hypoxic pulmonary hypertension in rats. J Appl Physiol 1995;79:2122-31.
26. Holm P, Liska J, Clozel M, Franco-Cereceda A. The endothelin antagonist bosentan: hemodynamic effects during normoxia and hypoxic pulmonary hypertension in pigs. J Thorac Cardiovasc Surg 1996;112:890-7.
27. Pearl JM, Wellmann SA, McNamara JL, Lombardi JP, Wagner CJ, Raake JL, et al. Bosentan prevents hypoxiareoxygenation-induced pulmonary hypertension and improves pulmonary function. Ann Thorac Surg 1999;68:1714-21.
28. Carteaux JP, Roux S, Siaghy M, Schjoth B, Dolofon P, Bechamps Y, et al. Acute pulmonary hypertension after cardiopulmonary bypass in pig: the role of endogenous endothelin. Eur J Cardiothorac Surg 1999;15:346-52.
29. Weitzberg E, Hemsen A, Rudehill A, Modin A, Wanecek M, Lundberg JM. Bosentan-improved cardiopulmonary vascular performance and increased plasma levels of endothelin-1 in porcine endotoxin shock. Br J Pharmacol 1996;118:617-26.
30. Hess P, Clozel M, Clozel J-P. Telemetry monitoring of pulmonary arterial pressure in freely moving rats. J Appl Physiol 1996;81:1027-32.
31. Hill NS, Warburton RR, Pietras L, Klinger JR. Nonspecific endothelin-receptor antagonist blunts monocrotaline-induced pulmonary hypertension in rats. J Appl Physiol 1997;83:1209-15.
32. Rondelet B, Kerbaul F, Motte S, van Beneden R, Remmelink M, Brimioulle S, et al. Bosentan for the prevention of overcirculation-induced experimental pulmonary arterial hypertension. Circulation 2003;107:1329-35.
33. Rossi GP, Seccia TM, Nussdorfer GG. Reciprocal regulation of endothelin-1 and nitric oxide: relevance in the physiology and pathology of the cardiovascular system. Int Rev Cytol 2001;209:241-72.
34. Richard V, Hogie M, Clozel M, Loffler BM, Thuillez C. In vivo evidence of an endothelin-induced vasopressor tone after inhibition of nitric oxide synthesis in rats. Circulation 1995;91: 771-5.
35. Tyler RC, Muramatsu M, Abman SH, Stelzner TJ, Rodman DM, Bloch KD, et al. Variable expression of endothelial NO synthase in three forms of rat pulmonary hypertension. Am J Physiol 1999;276:L297-303.
36. Giaid A, Saleh D. Reduced expression of endothelial nitric oxide synthase in the lungs of patients with pulmonary hypertension. N Engl J Med 1995;333:214-21.
37. Rossi GP, Colonna S, Pavan E, Albertin G, Della Rocca F, Gerosa G, et al. Endothelin-1 and its mRNA in the wall layers of human arteries ex vivo. Circulation 1999;99:1147-55.
38. Dumont AS, Lovren F, McNeill JH, Sutherland GR, Triggle CR, Anderson TJ, et al. Augmentation of endothelial function by endothelin antagonism in human saphenous vein conduits. J Neurosurg 2001;94:281-6.
39. Verma S, Lovren F, Dumont AS, Mather KJ, Maitland A, Kieser TM, et al. Endothelin receptor blockade improves endothelial function in human internal mammary arteries. Cardiovasc Res 2001;49:146-51.
40. Suwaidi JA, Hamasaki S, Higano ST, Nishimura RA, Holmes Jr DR, Lerman A. Long-term follow-up of patients with mild coronary artery disease and endothelial dysfunction. Circulation 2000;101:948-54.
41. Perticone F, Ceravolo R, Pujia A, Ventura G, Lacopino S, Scozzafava A, et al. Prognostic significance of endothelial dysfunction in hypertensive patients. Circulation 2001;104: 191-6.
42. Tuder RM, Chacon M, Alger L, Wang J, Taraseviciene-Stewart L, Kasahara Y, et al. Expression of angiogenesis-related molecules in plexiform lesions in severe pulmonary hypertension: evidence for a process of disordered angiogenesis. J Pathol 2001;195:367-74.
43. Tuder RM, Voelkel NF. Angiogenesis and pulmonary hypertension: a unique process in a unique disease. Antioxid Redox Signal 2002;4:833-43.
44. Cruz A, Parnot C, Ribatti D, Corvol P, Gasc JM. Endothelin-1, a regulator of angiogenesis in the chick chorioallantoic membrane. J Vasc Res 2001;38:536-45.
45. Ito H, Hirata Y, Hiroe M, Tsujino M, Adachi S, Takamoto T, et al. Endothelin-1 induces hypertrophy with enhanced expression of muscle-specific genes in cultured neonatal rat cardiomyocytes. Circ Res 1991;69:209-15.
46. Yang Z, Krasnici N, Luscher TG. Endothelin-1 potentiates human smooth muscle cell growth to PDGF. Effects of ETA and ETB receptor blockade. Circulation 1999;100:5-8.
47. Porter KE, Olojugba DH, Masood I, Pemberton M, Bell PRF, London NJM. Endothelin-B receptors mediate intimal hyperplasia in an organ culture of human saphenous vein. J Vasc Surg 1998;28:695-701.
48. Jasmin JF, Lucas M, Cernacek P, Dupuis J. Effectiveness of a nonselective ET(A/B) and a selective ET(A) antagonist in rats with monocrotaline-induced pulmonary hypertension. Circulation 2001;103:314-8.
49. Rossi GP, Cavallin M, Belloni AS, Mazzocchi G, Nussdorfer GG, Pessina AC, et al. Aortic smooth muscle cell phenotypic modulation and fibrillar collagen deposition in angiotensin II-dependent hypertension. Cardiovasc Res 2002;55:178-89.
50. Katwa LC, Guarda E, Weber KT. Endothelin receptors in cultured adult rat cardiac fibroblasts. Cardiovasc Res 1993;27: 2125-9.
51. Cambrey AD, Harrison NK, Dawes KE, Southcott AM, Black CM, du Bois RM, et al. Increased levels of endothelin-1 in bronchoalveolar lavage fluid from patients with systemic sclerosis contribute to fibroblast mitogenic activity in vitro. Am J Respir Cell Mol Biol 1994;11:439-45.
52. Hocher G, Schwarz A, Pagan KA, Thone-Reineke C, El-Hag K, Kusserow H, et al. Pulmonary fibrosis and chronic lung inflammation in ET-1 transgenic mice. Am J Respir Cell Mol Biol 2000;23:19-26.
53. Mutsaers SE, Foster ML, Chambers RC, Laurent GJ, McAnulty RJ. Increased endothelin-1 and its localization during the development of bleomycin-induced pulmonary fibrosis in rats. Am J Respir Cell Mol Biol 1998;18:611-9.
54. Mulder P, Richard V, et al. Role of endogenous endothelin in chronic heart failure: Effect of a long-term treatment with an endothelin antagonist on survival, hemodynamic and cardiac remodeling. Circulation 1997;96:1976-82.
55. Seccia TM, Belloni AS, Kreutz R, Paul M, Nussdorfer GG, Pessina AC, et al. Cardiac fibrosis occurs early and involves endothelin and AT-1 receptors in hypertension due to endogenous angiotensin II. J Am Coll Cardiol 2003;41:666-73.
56. Park SH, Saleh D, Giaid A, Michel RP. Increased endothelin-1 in bleomycin-induced pulmonary fibrosis and the effect of an endothelin receptor antagonist. Am J Respir Crit Care Med 1997;156:600-8.
57. B receptors. Br J Pharmacol 1995;115:227-36.
58. Helset E, Lindal S, Olsen R, Myklebust R, Jorgensen L. Endothelin-1 causes sequential trapping of platelets and neutrophils in pulmonary microcirculation in rats. Am J Physiol 1996;271:L538-46.
59. Browatzki M, Schmidt J, Kubler W, Kranzhofer R. Endothelin-1 induces interleukin-6 release via activation of the transcription factor NF-kappa B in human vascular smooth muscle cells. Basic Res Cardiol 2000;95:98-105.
60. Wilson SH, Simari RD, Lerman A. The effect of endothelin-1 on nuclear factor kappa B in macrophages. Biochem Biophys Res Commun 2001;286:968-72.
61. Filep JG. Endogenous endothelin modulates blood pressure, plasma volume, and albumin escape after systemic nitric oxide blockade. Hypertension 1997;30:22-8.
62. Guimaraes CL, Da-Silva S, Couture R, Rae GA. Mixed endothelin ET(A) and ET(B) antagonist bosentan inhibits oleic acid-induced lung plasma extravasation in mouse. J Cardiovasc Pharmacol 2000;36:S371-3.
63. Filep JG. Role for endogenous endothelin in the regulation of plasma volume and albumin escape during endotoxin shock in conscious rats. Br J Pharmacol 2000;129:975-83.
64. Filep JG, Fournier A, Foldes-Filep E. Effects of the ETA/ETB receptor antagonist, bosentan on endothelin-1-induced myocardial ischaemia and oedema in the rat. Br J Pharmacol 1995; 116:1745-50.
65. Finsnes F, Skjonsberg OH, Tonnessen T, Naess O, Lyberg T, Christensen G. Endothelin production and effects of endothelin antagonism during experimental airway inflammation. Am J Rispir Crit Care Med 1997;155:1404-12.
66. Finsnes F, Lyberg T, Christensen G, Skjonsberg OH. Effect of endothelin antagonism on the production of cytokines in eosinophilic airway inflammation. Am J Physiol Lung Cell Mol Physiol 2001;280:L659-65.
67. Verma S, Li S-H, Badiwala MV, Weisel RD, Fedak PWM, Li R-K, et al. Endothelin antagonism and interleukin-6 inhibition attenuate the proatherogenic effects of C-reactive protein. Circulation 2002;105:1890-6.
68. Loffler BM, Breu V, Clozel M. Effect of different endothelin receptor antagonists and of the novel non-peptide antagonist Ro 46-2005 on endothelin levels in rat plasma. FEBS Lett 1993;333:108-10.
69. Donckier J, Stoleru L, Hayashida W, Van Mechelen H, Selvais P, Galanti L, et al. Role of endogenous endothelin-1 in experimental renal hypertension in dogs. Circulation 1995;92:106-13.
70. Belloni AS, Rossi GP, Andreis PG, Neri G, Albertin G, Pessina AC, et al. Endothelin adrenocortical secretagogue effect is mediated by the B receptor in rats. Hypertension 1996;27: 1153-9.
71. Rossi GP, Ganzaroli C, Cesari M, Maresca A, Plebani M, Nussdorfer GG, et al. Endothelin receptor blockade lowers plasma aldosterone levels via different mechanisms in primary aldosteronism and high-to-normal renin hypertension. Cardiovasc Res 2003;57:277-83.
72. Rossi GP, Cavallin M, Nussdorfer GG, Pessina AC. The endothelin- aldosterone axis and cardiovascular diseases. J Cardiovasc Pharmacol 2001;38:S49-52.
73. Schmidt BM, Schmieder RE. Aldosterone-induced cardiac damage: Focus on blood pressure independent effects. Am J Hypertens 2003;16:80-6.
74. Cockcroft JR, Clarke JG, Webb DJ. The effect of intra-arterial endothelin on resting blood flow and sympathetically mediated vasoconstriction in the forearm of man. Br J Clin Pharmacol 1991;31:521-4.
75. Wong-Dusting HK, La M, Rand MJ. Endothelin-1 enhances vasoconstrictor responses to sympathetic nerve stimulation and noradrenaline in the rabbit ear artery. Clin Exp Pharmacol Physiol 1991;18:131-6.
76. Rossi GP, Sacchetto A, Rizzoni D, Bova S, Porteri E, Mazzocchi G, et al. Blockade of angiotensin II type 1 receptor and not of endothelin receptor prevents hypertension and cardiovascular disease in transgenic (mREN2)27 rats via adrenocortical steroid-independent mechanisms. Arterioscler Thromb Vasc Biol 2000;20:949-56.
77. Mulder P, Boujedaini H, Richard V, Derumeaux G, Henry JP, Renet S, et al. Selective endothelin-A versus combined endothelin-A/endothelin-B receptor blockade in rat chronic heart failure. Circulation 2000;102:491-3.
78. Sütsch G, Bertel O, Rickenbacher P, Clozel M, Yandle TG, Nicholls G, et al. Regulation of aldosterone secretion in patients with chronic congestive heart failure by endothelins. Am J Cardiol 2000;85:973-6.
79. Jakobsen J, Glaus L, Graf P, Degen P, Maurice NP, Bellet M, et al. Unmasking of the hypotensive effect of nifedipine in normotensives by addition of the angiotensin converting enzyme inhibitor benazepril. J Hypertens 1992;10:1045-51.