Pro-inflammatory response and adverse drug reactions: Mechanisms of action of ximelagatran on chemokine and cytokine activation in a monocyte in vitro model

Toxicology in Vitro

Volumn 22, Issue 6, 2008, Pages 1588-1594

  Edling, Ylva ^a   Sivertsson, Louise ^a   Andersson, Tommy B ^a,b   Porsmyr Palmertz, Margareta ^a   Ingelman Sundberg, Magnus ^a  

^a KAROLINSKA INSTITUTE   (Sweden)

^b ASTRAZENECA R AND D   (Sweden)

Author keywords

IL 8; Inflammation; MAPK; MCP 1; VEGF; Ximelagatran

Indexed keywords

AZETIDINE DERIVATIVE; CHEMOKINE; CYTOKINE; HYDROXYMELAGATRAN; INTERLEUKIN 8; MELAGATRAN; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE 3; MITOGEN ACTIVATED PROTEIN KINASE KINASE 4; MONOCYTE CHEMOTACTIC PROTEIN 1; VASCULOTROPIN; XIMELAGATRAN;

ARTICLE; CELL VIABILITY; CYTOKINE RELEASE; DRUG MECHANISM; DRUG TOXICITY; HUMAN; HUMAN CELL; IN VITRO STUDY; INFLAMMATION; METABOLITE; MONOCYTE; PHOSPHORYLATION;

AMIDINES; ANTICOAGULANTS; AZETIDINES; BENZYLAMINES; CELL LINE; CELL SURVIVAL; CHEMOKINES; CYTOKINES; HUMANS; INTERLEUKIN-8; JNK MITOGEN-ACTIVATED PROTEIN KINASES; MITOGEN-ACTIVATED PROTEIN KINASE 1; MITOGEN-ACTIVATED PROTEIN KINASE 3; MODELS, BIOLOGICAL; MONOCYTES;

EID: 49149100461     PISSN: 08872333     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.tiv.2008.06.011     Document Type: Article

References (36)

1. Anand R.J., Paust H.J., Altenpohl K., and Mukhopadhyay A.K. Regulation of vascular endothelial growth factor production by Leydig cells in vitro: the role of protein kinase A and mitogen-activated protein kinase cascade. Biol. Reprod. 68 (2003) 1663-1673
2. Andersson S., Hofmann Y., Nordling A., Li X.Q., Nivelius S., Andersson T.B., Ingelman-Sundberg M., and Johansson I. Characterization and partial purification of the rat and human enzyme systems active in the reduction of N-hydroxymelagatran and benzamidoxime. Drug Metab. Dispos. 33 (2005) 570-578
3. Bredberg E., Andersson T.B., Frison L., Thuresson A., Johansson S., Eriksson-Lepkowska M., Larsson M., and Eriksson U.G. Ximelagatran, an oral direct thrombin inhibitor, has a low potential for cytochrome P450-mediated drug-drug interactions. Clin. Pharmacokinet. 42 (2003) 765-777
4. Cheng J.J., Wung B.S., Chao Y.J., and Wang D.L. Sequential activation of protein kinase C (PKC)-alpha and PKC-epsilon contributes to sustained Raf/ERK1/2 activation in endothelial cells under mechanical strain. J. Biol. Chem. 276 (2001) 31368-31375
5. Chou S.F., Chang S.W., and Chuang J.L. Mitomycin C upregulates IL-8 and MCP-1 chemokine expression via mitogen-activated protein kinases in corneal fibroblasts. Invest. Ophthalmol. Vis. Sci. 48 (2007) 2009-2016
6. Clauss M., Gerlach M., Gerlach H., Brett J., Wang F., Familletti P.C., Pan Y.C., Olander J.V., Connolly D.T., and Stern D. Vascular permeability factor: a tumor-derived polypeptide that induces endothelial cell and monocyte procoagulant activity, and promotes monocyte migration. J. Exp. Med. 172 (1990) 1535-1545
7. Clement B., and Lopian K. Characterization of in vitro biotransformation of new, orally active, direct thrombin inhibitor ximelagatran, an amidoxime and ester prodrug. Drug Metab. Dispos. 31 (2003) 645-651
8. Crooks S.W., and Stockley R.A. Leukotriene B4. Int. J. Biochem. Cell Biol. 30 (1998) 173-178
9. Eriksson B.I., Agnelli G., Cohen A.T., Dahl O.E., Mouret P., Rosencher N., Eskilson C., Nylander I., Frison L., and Ogren M. Direct thrombin inhibitor melagatran followed by oral ximelagatran in comparison with enoxaparin for prevention of venous thromboembolism after total hip or knee replacement. Thromb. Haemost. 89 (2003) 288-296
10. Eriksson U.G., Bredberg U., Hoffmann K.J., Thuresson A., Gabrielsson M., Ericsson H., Ahnoff M., Gislen K., Fager G., and Gustafsson D. Absorption, distribution, metabolism, and excretion of ximelagatran, an oral direct thrombin inhibitor, in rats, dogs, and humans. Drug Metab. Dispos. 31 (2003) 294-305
11. Francis C.W., Davidson B.L., Berkowitz S.D., Lotke P.A., Ginsberg J.S., Lieberman J.R., Webster A.K., Whipple J.P., Peters G.R., and Colwell Jr. C.W. Ximelagatran versus warfarin for the prevention of venous thromboembolism after total knee arthroplasty. A randomized, double-blind trial. Ann. Intern. Med. 137 (2002) 648-655
12. Gustafsson D., Nystrom J., Carlsson S., Bredberg U., Eriksson U., Gyzander E., Elg M., Antonsson T., Hoffmann K., Ungell A., Sorensen H., Nagard S., Abrahamsson A., and Bylund R. The direct thrombin inhibitor melagatran and its oral prodrug H 376/95: intestinal absorption properties, biochemical and pharmacodynamic effects. Thromb. Res. 101 (2001) 171-181
13. Hoffmann E., Dittrich-Breiholz O., Holtmann H., and Kracht M. Multiple control of interleukin-8 gene expression. J. Leukoc. Biol. 72 (2002) 847-855
14. Jaeschke H., and Hasegawa T. Role of neutrophils in acute inflammatory liver injury. Liver Int. 26 (2006) 912-919
15. Jaeschke H., and Smith C.W. Mechanisms of neutrophil-induced parenchymal cell injury. J. Leukoc. Biol. 61 (1997) 647-653
16. Kenne K., Skanberg I., Glinghammar B., Berson A., Pessayre D., Flinois J.P., Beaune P., Edebert I., Pohl C.D., Carlsson S., and Andersson T.B. Prediction of drug-induced liver injury in humans by using in vitro methods: The case of ximelagatran. Toxicol. In Vitro 22 (2008) 730-746
17. Kindmark, A., Jawaid, A., Harbron, C.G., Barratt, B.J., Bengtsson, O.F., Andersson, T.B., Carlsson, S., Cederbrant, K.E., Gibson, N.J., Armstrong, M., Lagerstrom-Fermer, M.E., Dellsen, A., Brown, E.M., Thornton, M., Dukes, C., Jenkins, S.C., Firth, M.A., Harrod, G.O., Pinel, T.H., Billing-Clason, S.M., Cardon, L.R., March, R.E. (2007). Genome-wide pharmacogenetic investigation of a hepatic adverse event without clinical signs of immunopathology suggests an underlying immune pathogenesis. Pharmacogenomics J.
18. Lee W.M. Drug-induced hepatotoxicity. N Engl. J. Med. 349 (2003) 474-485
19. Lee W.M., Larrey D., Olsson R., Lewis J.H., Keisu M., Auclert L., and Sheth S. Hepatic findings in long-term clinical trials of ximelagatran. Drug Safety 28 (2005) 351-370
20. Livak K.J., and Schmittgen T.D. Analysis of relative gene expression data using real-time quantitative PCR and the 2(-Delta Delta C(T)) Method. Methods 25 (2001) 402-408
21. Lowry O.H., Rosebrough N.J., Farr A.L., and Randall R.J. Protein measurement with the folin phenol reagent. J. Biol. Chem. 193 (1951) 265-275
22. Matsukawa A., Hogaboam C.M., Lukacs N.W., Lincoln P.M., Strieter R.M., and Kunkel S.L. Endogenous monocyte chemoattractant protein-1 (MCP-1) protects mice in a model of acute septic peritonitis: cross-talk between MCP-1 and leukotriene B4. J. Immunol. 163 (1999) 6148-6154
23. Matsushima K., Morishita K., Yoshimura T., Lavu S., Kobayashi Y., Lew W., Appella E., Kung H.F., Leonard E.J., and Oppenheim J.J. Molecular cloning of a human monocyte-derived neutrophil chemotactic factor (MDNCF) and the induction of MDNCF mRNA by interleukin 1 and tumor necrosis factor. J. Exp. Med. 167 (1988) 1883-1893
24. Michael S.L., Pumford N.R., Mayeux P.R., Niesman M.R., and Hinson J.A. Pretreatment of mice with macrophage inactivators decreases acetaminophen hepatotoxicity and the formation of reactive oxygen and nitrogen species. Hepatology 30 (1999) 186-195
25. Milanini J., Vinals F., Pouyssegur J., and Pages G. p42/p44 MAP kinase module plays a key role in the transcriptional regulation of the vascular endothelial growth factor gene in fibroblasts. J. Biol. Chem. 273 (1998) 18165-18172
26. Mukaida N., Harada A., and Matsushima K. Interleukin-8 (IL-8) and monocyte chemotactic and activating factor (MCAF/MCP-1), chemokines essentially involved in inflammatory and immune reactions. Cytokine Growth Factor Rev. 9 (1998) 9-23
27. Mukaida N., Okamoto S., Ishikawa Y., and Matsushima K. Molecular mechanism of interleukin-8 gene expression. J. Leukoc. Biol. 56 (1994) 554-558
28. Muriel P., and Escobar Y. Kupffer cells are responsible for liver cirrhosis induced by carbon tetrachloride. J. Appl. Toxicol. 23 (2003) 103-108
29. Navarro V.J., and Senior J.R. Drug-related hepatotoxicity. N Engl. J. Med. 354 (2006) 731-739
30. Ni C.W., Wang D.L., Lien S.C., Cheng J.J., Chao Y.J., and Hsieh H.J. Activation of PKC-epsilon and ERK1/2 participates in shear-induced endothelial MCP-1 expression that is repressed by nitric oxide. J. Cell Physiol. 195 (2003) 428-434
31. Ridley S.H., Sarsfield S.J., Lee J.C., Bigg H.F., Cawston T.E., Taylor D.J., DeWitt D.L., and Saklatvala J. Actions of IL-1 are selectively controlled by p38 mitogen-activated protein kinase: regulation of prostaglandin H synthase-2, metalloproteinases, and IL-6 at different levels. J. Immunol. 158 (1997) 3165-3173
32. Simi A., Ingelman-Sundberg M., and Tindberg N. Neuroprotective agent chlomethiazole attenuates c-fos, c-jun, and AP-1 activation through inhibition of p38 MAP kinase. J. Cereb. Blood Flow Metab. 20 (2000) 1077-1088
33. Tang Y., Nakada M.T., Rafferty P., Laraio J., McCabe F.L., Millar H., Cunningham M., Snyder L.A., Bugelski P., and Yan L. Regulation of vascular endothelial growth factor expression by EMMPRIN via the PI3K-Akt signaling pathway. Mol. Cancer Res. 4 (2006) 371-377
34. Thornton A.J., Strieter R.M., Lindley I., Baggiolini M., and Kunkel S.L. Cytokine-induced gene expression of a neutrophil chemotactic factor/IL-8 in human hepatocytes. J. Immunol. 144 (1990) 2609-2613
35. Tilg H., and Diehl A.M. Cytokines in alcoholic and nonalcoholic steatohepatitis. N Engl. J. Med. 343 (2000) 1467-1476
36. Yoshimura T., and Ueda A. Moncyte chemoattractant protein-1. Human Cytokines II: Handbook for Basic and Clinical Research (1996), Oxford, UK