5-HT2A receptor antagonists inhibit hepatic stellate cell activation and facilitate apoptosis

Liver International

Volumn 33, Issue 4, 2013, Pages 535-543

  Kim, Dong Chan ^a   Jun, Dae Won ^a   Kwon, Young Il ^a   Lee, Kang Nyeong ^a   Lee, Hang Lak ^a   Lee, Oh Young ^a   Yoon, Byung Chul ^a   Choi, Ho Soon ^a   Kim, Eun Kyung ^b  

^a Hanyang University College of Medicine   (South Korea)

^b Eulji University   (South Korea)

Author keywords

5 HT; 5 HT2A receptor; Fibrosis; Hepatic stellate cell; Sarpogrelate

Indexed keywords

ALPHA SMOOTH MUSCLE ACTIN; KETANSERIN; PROCOLLAGEN; PROCOLLAGEN TYPE 1; SARPOGRELATE; SMAD2 PROTEIN; SMAD3 PROTEIN; TRANSFORMING GROWTH FACTOR BETA; UNCLASSIFIED DRUG; ACTA2 PROTEIN, HUMAN; ACTIN; COLLAGEN TYPE 1; MADH2 PROTEIN, RAT; MADH3 PROTEIN, RAT; MESSENGER RNA; REACTIVE OXYGEN METABOLITE; RITANSERIN; SEROTONIN 2 ANTAGONIST; SEROTONIN 2A RECEPTOR; SMAD2 PROTEIN, HUMAN; SMAD3 PROTEIN, HUMAN; SUCCINIC ACID DERIVATIVE; THIOACETAMIDE;

ANIMAL EXPERIMENT; APOPTOSIS; ARTICLE; CELL ACTIVATION; CELL SURVIVAL; CELL VIABILITY; CONTROLLED STUDY; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; LIVER CIRRHOSIS; NONHUMAN; RAT; STELLATE CELL; WOUND HEALING; ANIMAL; CELL LINE; CHEMICALLY INDUCED; DOSE RESPONSE; DRUG EFFECTS; GENETICS; LIVER CIRRHOSIS, EXPERIMENTAL; METABOLISM; PATHOLOGY; SPRAGUE DAWLEY RAT; TIME; CHEMICALLY INDUCED DISORDER; DRUG EFFECT; EXPERIMENTAL LIVER CIRRHOSIS;

ACTINS; ANIMALS; APOPTOSIS; CELL LINE; CELL SURVIVAL; COLLAGEN TYPE I; DOSE-RESPONSE RELATIONSHIP, DRUG; HEPATIC STELLATE CELLS; HUMANS; KETANSERIN; LIVER CIRRHOSIS, EXPERIMENTAL; RATS; RATS, SPRAGUE-DAWLEY; REACTIVE OXYGEN SPECIES; RECEPTOR, SEROTONIN, 5-HT2A; RITANSERIN; RNA, MESSENGER; SEROTONIN 5-HT2 RECEPTOR ANTAGONISTS; SMAD2 PROTEIN; SMAD3 PROTEIN; SUCCINATES; THIOACETAMIDE; TIME FACTORS; TRANSFORMING GROWTH FACTOR BETA; WOUND HEALING;

EID: 84875054830     PISSN: 14783223     EISSN: 14783231     Source Type: Journal    
DOI: 10.1111/liv.12110     Document Type: Article

References (32)

1. Kim DY, Camilleri M. Serotonin: A mediator of the brain-gut connection. Am J Gastroenterol 2000; 95: 2698-709.
2. Tamir H, Payette RF, Huang YL, Liu KP, Gershon MD. Human serotonectin: A blood glycoprotein that binds serotonin and is associated with platelets and white blood cells. J Cell Sci 1985; 73: 187-206.
3. Hoyer D, Clarke DE, Fozard JR, et al. International union of pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol Rev 1994; 46: 157-203.
4. Foxx-Orenstein AE, Kuemmerle JF, Grider JR. Distinct 5-HT receptors mediate the peristaltic reflex induced by mucosal stimuli in human and guinea pig intestine. Gastroenterology 1996; 111: 1281-90.
5. Lesurtel M, Graf R, Aleil B, et al. Platelet-derived serotonin mediates liver regeneration. Science 2006; 312: 104-7.
6. Nagao Y, Akahoshi T, Kamori M, et al. Liver regeneration is promoted by increasing serotonin content in rat liver with secondary biliary cirrhosis. Hepatol Res 2011; 41: 784-94.
7. Tian Y, Graf R, El-Badry AM, et al. Activation of serotonin receptor-2B rescues small-for-size liver graft failure in mice. Hepatology 2011; 53: 253-62.
8. Nocito A, Dahm F, Jochum W, et al. Serotonin mediates oxidative stress and mitochondrial toxicity in a murine model of nonalcoholic steatohepatitis. Gastroenterology 2007; 133: 608-18.
9. Ruddell RG, Oakley F, Hussain Z, et al. A role for serotonin (5-HT) in hepatic stellate cell function and liver fibrosis. Am J Pathol 2006; 169: 861-76.
10. Kasho M, Sakai M, Sasahara T, et al. Serotonin enhances the production of type IV collagen by human mesangial cells. Kidney Int 1998; 54: 1083-92.
11. Hahn A, Heusinger-Ribeiro J, Lanz T, Zenkel S, Goppelt-Struebe M. Induction of connective tissue growth factor by activation of heptahelical receptors. modulation by Rho proteins and the actin cytoskeleton. J Biol Chem 2000; 275: 37429-35.
12. 2A receptor induces TGF-beta1 expression in mesangial cells via ERK: proliferative and fibrotic signals. Am J Physiol 1999; 276: F922-30.
13. Beaudry P, Hadengue A, Callebert J, et al. Blood and plasma 5-hydroxytryptamine levels in patients with cirrhosis. Hepatology 1994; 20: 800-3.
14. Dees C, Akhmetshina A, Zerr P, et al. Platelet-derived serotonin links vascular disease and tissue fibrosis. J Exp Med 2011; 208: 961-72.
15. Xu L, Hui AY, Albanis E, et al. Human hepatic stellate cell lines, LX-1 and LX-2: New tools for analysis of hepatic fibrosis. Gut 2005; 54: 142-51.
16. Wang XM, Yu DM, McCaughan GW, Gorrell MD. Fibroblast activation protein increases apoptosis, cell adhesion, and migration by the LX-2 human stellate cell line. Hepatology 2005; 42: 935-45.
17. Bedossa P, Poynard T. An algorithm for the grading of activity in chronic hepatitis C. The METAVIR cooperative study group. Hepatology 1996; 24: 289-93.
18. Hempfling C, Neuhuber WL, Worl J. Serotonin-immunoreactive neurons and mast cells in the mouse esophagus suggest involvement of serotonin in both motility control and neuroimmune interactions. Neurogastroenterol Motil 2012; 24: e67-78.
19. Reikvam AG, Hustad S, Reikvam H, et al. The effects of selective serotonin reuptake inhibitors on platelet function in whole blood and platelet concentrates. Platelets 2012; 23: 299-308.
20. Nichols DE, Nichols CD. Serotonin receptors. Chem Rev 2008; 108: 1614-41.
21. Tanaka N, Goto R, Ito R, et al. [2-(O-Phenylalkyl)phenoxy]alkylamines III: Synthesis and selective serotonin-2 receptor binding (2). Chem Pharm Bull(Tokyo) 2000; 48: 1729-39.
22. Lesurtel M, Soll C, Humar B, Clavien PA. Serotonin: A double-edged sword for the liver? Surgeon 2012; 10: 107-13.
23. 2B receptor in chronic liver disease. Nat Med 2011; 17: 1668-73.
24. Breard M, Grillon C. Serotonin binds to purified neuronal nitric oxide synthase: a possible explanation for ROS production induced by 5HT in the presence of nNOS. Free Radic Res 2009; 43: 206-13.
25. Lesurtel M, Clavien PA. Serotonin: A key molecule in acute and chronic liver injury! Clin Res Hepatol Gastroenterol 2012; 36: 319-322.
26. Li T, Weng SG, Leng XS, et al. Effects of 5-hydroxytryptamine and its antagonists on hepatic stellate cells. Hepatobiliary Pancreat Dis Int 2006; 5: 96-100.
27. Sanganalmath SK, Babick AP, Barta J, et al. Antiplatelet therapy attenuates subcellular remodelling in congestive heart failure. J Cell Mol Med 2008; 12: 1728-38.
28. Doggrell SA. Sarpogrelate: cardiovascular and renal clinical potential. Expert Opin Investig Drugs 2004; 13: 865-74.
29. Saini HK, Takeda N, Goyal RK, et al. Therapeutic potentials of sarpogrelate in cardiovascular disease. Cardiovasc Drug Rev 2004; 22: 27-54.
30. Kodama A, Komori K, Hattori K, et al. Sarpogrelate hydrochloride reduced intimal hyperplasia in experimental rabbit vein graft. J Vasc Surg 2009; 49: 1272-81.
31. Shinohara Y, Nishimaru K, Sawada T, et al. Sarpogrelate-Aspirin Comparative Clinical Study for Efficacy and Safety in Secondary Prevention of Cerebral Infarction (S-ACCESS): A randomized, double-blind, aspirin controlledtrial. Stroke 2008; 39: 1827-33.
32. Hara H, Osakabe M, Kitajima A, Tamao Y, Kikumoto R. MCI-9042, a new antiplatelet agent is a selective S2-serotonergic receptor antagonist. Thromb Haemost 1991; 65: 415-20.