S26948, a new specific peroxisome proliferator activated receptor gamma modulator improved in vivo hepatic insulin sensitivity in 48 h lipid infused rats

European Journal of Pharmacology

Volumn 608, Issue 1-3, 2009, Pages 104-111

  Sohn, Kyung Ah Kim ^a   Cruciani Guglielmacci, Céline ^a   Kassis, Nadim ^a   Clément, Laurence ^a   Ouali, Fetta ^a   Caüzac, Michèle ^b   Lebègue, Nicolas ^c   Berthelot, Pascal ^c   Caignard, Daniel Henri ^d   Pégorier, Jean Paul ^b   Renard, Pierre ^d   Dacquet, Catherine ^d   Ktorza, Alain ^d   Magnan, Christophe ^a  

^a UNIVERSITÉ PARIS DESCARTES   (France)

^b INSERM   (France)

^c UNIV LILLE   (France)

^d INSTITUT DE RECHERCHES INTERNATIONALES SERVIER   (France)

Author keywords

Fatty acid; Glucose hepatic production; Glucose homeostasis; Liver; SPPARM agonist

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; FATTY ACID; GLUCOSE; INSULIN; INTRALIPID; LIPID; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA AGONIST; ROSIGLITAZONE; S 26948; SODIUM CHLORIDE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CELL ISOLATION; CONTROLLED STUDY; DRUG EFFECT; DRUG MECHANISM; FATTY ACID BLOOD LEVEL; GENE EXPRESSION; GLUCOSE METABOLISM; GLUCOSE TOLERANCE TEST; GLUCOSE UTILIZATION; HORMONE ACTION; HYPERINSULINEMIA; IN VIVO STUDY; INCUBATION TIME; INFUSION; INSULIN RELEASE; INSULIN RESISTANCE; INSULIN SENSITIVITY; JUGULAR VEIN; LIVER CELL; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; SENSITIVITY ANALYSIS;

EID: 63149140668     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2009.02.033     Document Type: Article

References (45)

1. Auwerx J. PPARgamma, the ultimate thrifty gene. Diabetologia 42 (1999) 1033-1049
2. Berg A.H., Combs T.P., Du X., Brownlee M., and Scherer P.E. The adipocyte-secreted protein Acrp30 enhances hepatic insulin action. Nat. Med. 7 (2001) 947-953
3. Bhatia V., and Viswanathan P. Insulin resistance and PPAR insulin sensitizers. Curr. Opin. Investig. Drugs 7 (2006) 891-897
4. Blanc-Delmas E., Lebegue N., Wallez V., Leclerc V., Yous S., Carato P., Farce A., Bennejean C., Renard P., Caignard D.H., Audinot-Bouchez V., Chomarat P., Boutin J., Hennuyer N., Louche K., Carmona M.C., Staels B., Penicaud L., Casteilla L., Lonchampt M., Dacquet C., Chavatte P., Berthelot P., and Lesieur D. Novel 1,3-dicarbonyl compounds having 2(3H)-benzazolonic heterocycles as PPARgamma agonists. Bioorg. Med. Chem. 14 (2006) 7377-7391
5. Carmona M.C., Louche K., Lefebvre B., Pilon A., Hennuyer N., Audinot-Bouchez V., Fievet C., Torpier G., Formstecher P., Renard P., Lefebvre P., Dacquet C., Staels B., Casteilla L., and Penicaud L. S26948: a new specific peroxisome proliferator activated receptor gamma modulator with potent antidiabetes and antiatherogenic effects. Diabetes 56 (2007) 2797-2808
6. Chao L., Marcus-Samuels B., Mason M.M., Moitra J., Vinson C., Arioglu E., Gavrilova O., and Reitman M.L. Adipose tissue is required for the antidiabetic, but not for the hypolipidemic, effect of thiazolidinediones. J. Clin. Invest. 106 (2000) 1221-1228
7. Chen S., Lam T., Park E., Burdett E., Wang P., Wiesenthal S., Lam L., Tchipashvili V., Fantus I., and Giacca A. Oleate-induced decrease in hepatocyte insulin binding is mediated by PKC-delta. Biochem. Biophys. Res. Commun. 346 (2006) 931-937
8. Chirgwin J.M., Przybyla A.E., MacDonald R.J., and Rutter W.J. Isolation of biologically active ribonucleic acid from sources enriched in ribonuclease. Biochemistry 18 (1979) 5294-5299
9. Clement L., Kim-Sohn K.A., Magnan C., Kassis N., Adnot P., Kergoat M., Assimacopoulos-Jeannet F., Penicaud L., Hsu F., Turk J., and Ktorza A. Pancreatic beta-cell alpha2A adrenoceptor and phospholipid changes in hyperlipidemic rats. Lipids 37 (2002) 501-506
10. Edvardsson U., Ljungberg A., and Oscarsson J. Insulin and oleic acid increase PPARgamma2 expression in cultured mouse hepatocytes. Biochem. Biophys. Res. Commun. 340 (2006) 111-117
11. Ferre P., Pegorier J.P., Williamson D.H., and Girard J. Interactions in vivo between oxidation of non-esterified fatty acids and gluconeogenesis in the newborn rat. Biochem. J. 182 (1979) 593-598
12. Fryer L., Parbu-Patel A., and Carling D. The anti-diabetic drugs rosiglitazone and metformin stimulate AMP-activated protein kinase through distinct signaling pathways. J. Biol. Chem. 277 (2002) 25226-25232
13. Fujimura T., Sakuma H., Ohkubo-Suzuki A., Aramori I., and Mutoh S. Unique properties of coactivator recruitment caused by differential binding of FK614, an anti-diabetic agent, to peroxisome proliferator-activated receptor gamma. Biol. Pharm. Bull. 29 (2006) 423-429
14. Hevener A.L., Reichart D., Janez A., and Olefsky J. Thiazolidinedione treatment prevents free fatty acid-induced insulin resistance in male wistar rats. Diabetes 50 (2001) 2316-2322
15. Krzyzanowska K., Mittermayer F., Krugluger W., Roden M., Schernthaner G., and Wolzt M. Adiponectin concentrations increase during acute FFA elevation in humans treated with rosiglitazone. Horm. Metab. Res. 39 (2007) 769-772
16. Lara-Castro C., Fu Y., Chung B.H., and Garvey W.T. Adiponectin and the metabolic syndrome: mechanisms mediating risk for metabolic and cardiovascular disease. Curr. Opin. Lipidol. 18 (2007) 263-270
17. Liu Y.Q., and Uyeda K. A mechanism for fatty acid inhibition of glucose utilization in liver. Role of xylulose 5-P. J. Biol. Chem. 271 (1996) 8824-8830
18. Luconi M., Forti G., and Baldi E. Genomic and nongenomic effects of estrogens: molecular mechanisms of action and clinical implications for male reproduction. J. Steroid Biochem. Mol. Biol. 80 (2002) 369-381
19. Magnan C., Collins S., Berthault M., Kassis N., Vincent M., Gilbert M., Pénicaud L., Ktorza A., and Assimacopoulos-Jeannet F. Lipid infusion lowers sympathetic nervous activity and leads to increased β-cell responsiveness to glucose. J. Clin. Invest. 103 (1999) 413-419
20. Mannaerts G.P., Debeer L.J., Thomas J., and De Schepper P.J. Mitochondrial and peroxisomal fatty acid oxidation in liver homogenates and isolated hepatocytes from control and clofibrate-treated rats. J. Biol. Chem. 254 (1979) 4585-4595
21. McGarry J.D., and Foster D.W. The regulation of ketogenesis from octanoic acid. The role of the tricarboxylic acid cycle and fatty acid synthesis. J. Biol. Chem. 246 (1971) 1149-1159
22. Mudaliar S., and Henry R.R. New oral therapies for type 2 diabetes mellitus: the glitazones or insulin sensitizers. Annu. Rev. Med. 52 (2001) 239-257
23. Murano K., Inoue Y., Emoto M., Kaku K., and Kaneko T. CS-045, a new oral antidiabetic agent, stimulates fructose-2,6-bisphosphate production in rat hepatocytes. Eur. J. Pharmacol. 254 (1994) 257-262
24. Olefsky J.M. Treatment of insulin resistance with peroxisome proliferator-activated receptor gamma agonists. J. Clin. Invest. 106 (2000) 467-472
25. Pegorier J.P., Duee P.H., Herbin C., Laulan P.Y., Blade C., Peret J., and Girard J. Fatty acid metabolism in hepatocytes isolated from rats adapted to high-fat diets containing long- or medium-chain triacylglycerols. Biochem. J. 249 (1988) 801-806
26. Puigserver P., and Spiegelman B.M. Peroxisome proliferator-activated receptor-gamma coactivator 1 alpha (PGC-1 alpha): transcriptional coactivator and metabolic regulator. Endocr. Rev. 24 (2003) 78-90
27. Puigserver P., Rhee J., Donovan J., Walkey C.J., Yoon J.C., Oriente F., Kitamura Y., Altomonte J., Dong H., Accili D., and Spiegelman B.M. Insulin-regulated hepatic gluconeogenesis through FOXO1-PGC-1alpha interaction. Nature 423 (2003) 550-555
28. Racette S.B., Davis A.O., McGill J.B., and Klein S. Thiazolidinediones enhance insulin-mediated suppression of fatty acid flux in type 2 diabetes mellitus. Metabolism 51 (2002) 169-174
29. Rhee J., Inoue Y., Yoon J.C., Puigserver P., Fan M., Gonzalez F.J., and Spiegelman B.M. Regulation of hepatic fasting response by PPARgamma coactivator-1alpha (PGC-1): requirement for hepatocyte nuclear factor 4alpha in gluconeogenesis. Proc. Natl. Acad. Sci. U. S. A. 100 (2003) 4012-4017
30. Saha A.K., Avilucea P.R., Ye J.M., Assifi M.M., Kraegen E.W., and Ruderman N.B. Pioglitazone treatment activates AMP-activated protein kinase in rat liver and adipose tissue in vivo. Biochem. Biophys. Res. Commun. 314 (2004) 580-585
31. Scheen A.J. Thiazolidinediones and liver toxicity. Diabetes Metab. 27 (2001) 305-313
32. Shi Q., Canada E.J., Xu Y., Warshawsky A.M., Etgen G.J., Broderick C.L., Clutinger C.K., Irwin L.A., Laurila M.E., Montrose-Rafizadeh C., Oldham B.A., Wang M., Winneroski L.L., Xie C., York J.S., Yumibe N.P., Zink R.W., and Mantlo N. Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists. Bioorg. Med. Chem. Lett. (2007)
33. Tolman K.G. Thiazolidinedione hepatotoxicity: a class effect?. Int. J. Clin. Pract., Suppl. (2000) 29-34
34. Tolman K.G., and Chandramouli J. Hepatotoxicity of the thiazolidinediones. Clin. Liver Dis. 7 (2003) 369-379 vi
35. Tonstad S., Retterstol K., Ose L., Ohman K.P., Lindberg M.B., and Svensson M. The dual peroxisome proliferator-activated receptor alpha/gamma agonist tesaglitazar further improves the lipid profile in dyslipidemic subjects treated with atorvastatin. Metabolism 56 (2007) 1285-1292
36. Uchino H., Kim T., Lam T., Yoshii H., Klement P., Williams W., Kawamori R., and Giacca A. FK-614, a selective peroxisome proliferator-activated receptor gamma agonist, improves peripheral glucose utilization while decreasing hepatic insulin extraction in alloxan-induced diabetic dogs. Metabolism 54 (2005) 1250-1258
37. Van Schaftingen E., and Hers H.G. Inhibition of fructose-1,6-bisphosphatase by fructose 2,6-biphosphate. Proc. Natl. Acad. Sci. U. S. A. 78 (1981) 2861-2863
38. Vasudevan A.R., and Balasubramanyam A. Thiazolidinediones: a review of their mechanisms of insulin sensitization, therapeutic potential, clinical efficacy, and tolerability. Diabetes Technol. Ther. 6 (2004) 850-863
39. Vidal-Puig A., Jimenez-Linan M., Lowell B.B., Hamann A., Hu E., Spiegelman B., Flier J.S., and Moller D.E. Regulation of PPAR gamma gene expression by nutrition and obesity in rodents. J. Clin. Invest. 97 (1996) 2553-2561
40. Watkins S.M., Reifsnyder P.R., Pan H.J., German J.B., and Leiter E.H. Lipid metabolome-wide effects of the PPARgamma agonist rosiglitazone. J. Lipid Res. 43 (2002) 1809-1817
41. Yamamoto T., Shimano H., Nakagawa Y., Ide T., Yahagi N., Matsuzaka T., Nakakuki M., Takahashi A., Suzuki H., Sone H., Toyoshima H., Sato R., and Yamada N. SREBP-1 interacts with HNF-4alpha and interferes with PGC-1 recruitment to suppress hepatic gluconeogenic genes. J. Biol. Chem. (2004) Jan 13 [Electronic publication ahead of print]
42. Yamauchi T., Kamon J., Waki H., Terauchi Y., Kubota N., Hara K., Mori Y., Ide T., Murakami K., Tsuboyama-Kasaoka N., Ezaki O., Akanuma Y., Gavrilova O., Vinson C., Reitman M.L., Kagechika H., Shudo K., Yoda M., Nakano Y., Tobe K., Nagai R., Kimura S., Tomita M., Froguel P., and Kadowaki T. The fat-derived hormone adiponectin reverses insulin resistance associated with both lipoatrophy and obesity. Nat. Med. 7 (2001) 941-946
43. Yoon J.C., Puigserver P., Chen G., Donovan J., Wu Z., Rhee J., Adelmant G., Stafford J., Kahn C.R., Granner D.K., Newgard C.B., and Spiegelman B.M. Control of hepatic gluconeogenesis through the transcriptional coactivator PGC-1. Nature 413 (2001) 131-138
44. Yu J.G., Javorschi S., Hevener A.L., Kruszynska Y.T., Norman R.A., Sinha M., and Olefsky J.M. The effect of thiazolidinediones on plasma adiponectin levels in normal, obese, and type 2 diabetic subjects. Diabetes 51 (2002) 2968-2974
45. Zierath J.R., Ryder J.W., Doebber T., Woods J., Wu M., Ventre J., Li Z., McCrary C., Berger J., Zhang B., and Moller D.E. Role of skeletal muscle in thiazolidinedione insulin sensitizer (PPARgamma agonist) action. Endocrinology 139 (1998) 5034-5041