Remogliflozin Etabonate Improves Fatty Liver Disease in Diet-Induced Obese Male Mice

Journal of Clinical and Experimental Hepatology

Volumn 5, Issue 3, 2015, Pages 190-198

  Nakano, Shigeru ^a   Katsuno, Kenji ^a   Isaji, Masayuki ^a   Nagasawa, Tatsuya ^a   Buehrer, Benjamin ^b   Walker, Susan ^c   Wilkison, William O ^d   Cheatham, Bentley ^e  

^a KISSEI PHARMACEUTICAL CO LTD   (Japan)

^b NATIONAL INSTITUTES OF HEALTH   (United States)

^c Apex Biostatistics   (United States)

^d Islet Sciences Inc   (United States)

^e RTP Laboratories   (United States)

Author keywords

Hepatic steatosis; NAFLD; NASH; Obesity; SGLT2

Indexed keywords

ALANINE AMINOTRANSFERASE; ASPARTATE AMINOTRANSFERASE; CANAGLIFLOZIN; DAPAGLIFLOZIN; MESSENGER RNA; MONOCYTE CHEMOTACTIC PROTEIN 1; REMOGLIFLOZIN ETABONATE; THIOBARBITURIC ACID REACTIVE SUBSTANCE; TRIACYLGLYCEROL; TUMOR NECROSIS FACTOR ALPHA;

ALANINE AMINOTRANSFERASE BLOOD LEVEL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIOXIDANT ACTIVITY; ARTICLE; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; C57BL 6 MOUSE; COHORT ANALYSIS; CONTROLLED STUDY; DIET INDUCED OBESITY; DRUG BLOOD LEVEL; DRUG DETERMINATION; DRUG EFFICACY; DRUG TISSUE LEVEL; FATTY LIVER; LIPID DIET; LIVER HOMOGENATE; LIVER WEIGHT; MALE; MOUSE; NONALCOHOLIC FATTY LIVER; NONHUMAN; ORAC ASSAY; OXIDATIVE STRESS; PRIORITY JOURNAL; RNA ANALYSIS; TRIACYLGLYCEROL BLOOD LEVEL;

EID: 84946474255     PISSN: 09736883     EISSN: 22133453     Source Type: Journal    
DOI: 10.1016/j.jceh.2015.02.005     Document Type: Article

References (43)

1. Sanyal A.J. NASH: a global health problem. Hepatol Res 2011, 41:670-674.
2. Trappoliere M., Tuccillo C., Federico A., et al. The treatment of NAFLD. Eur Rev Med Pharmacol Sci 2005, 9:299-304.
3. Medina J., Fernandez-Salazar L.I., Garcia-Buey L., Moreno-Otero R. Approach to the pathogenesis and treatment of nonalcoholic steatohepatitis. Diabetes Care 2004, 27:2057-2066.
4. Mudaliar S., Henry R.R., Sanyal A.J., et al. Efficacy and safety of the farnesoid X receptor agonist obeticholic acid in patients with type 2 diabetes and nonalcoholic fatty liver disease. Gastroenterology 2013, 145:574-582. e571.
5. Brookheart R.T., Michel C.I., Schaffer J.E. As a matter of fat. Cell Metab 2009, 10:9-12.
6. Deng X.Q., Chen L.L., Li N.X. The expression of SIRT1 in nonalcoholic fatty liver disease induced by high-fat diet in rats. Liver Int 2007, 27:708-715.
7. Hou X., Xu S., Maitland-Toolan K.A., et al. SIRT1 regulates hepatocyte lipid metabolism through activating AMP-activated protein kinase. J Biol Chem 2008, 283:20015-20026.
8. Kohjima M., Higuchi N., Kato M., et al. SREBP-1c, regulated by the insulin and AMPK signaling pathways, plays a role in nonalcoholic fatty liver disease. Int J Mol Med 2008, 21:507-511.
9. Straub B.K., Stoeffel P., Heid H., Zimbelmann R., Schirmacher P. Differential pattern of lipid droplet-associated proteins and de novo perilipin expression in hepatocyte steatogenesis. Hepatology 2008, 47:1936-1946.
10. Bell M., Wang H., Chen H., et al. Consequences of lipid droplet coat protein downregulation in liver cells: abnormal lipid droplet metabolism and induction of insulin resistance. Diabetes 2008, 57:2037-2045.
11. Ahmed M.H., Byrne C.D. Modulation of sterol regulatory element binding proteins (SREBPs) as potential treatments for non-alcoholic fatty liver disease (NAFLD). Drug Discov Today 2007, 12:740-747.
12. Nagai Y., Yonemitsu S., Erion D.M., et al. The role of peroxisome proliferator-activated receptor gamma coactivator-1 beta in the pathogenesis of fructose-induced insulin resistance. Cell Metab 2009, 9:252-264.
13. Videla L.A., Rodrigo R., Araya J., Poniachik J. Insulin resistance and oxidative stress interdependency in non-alcoholic fatty liver disease. Trends Mol Med 2006, 12:555-558.
14. Darimont C., Avanti O., Zbinden I., et al. Liver X receptor preferentially activates de novo lipogenesis in human preadipocytes. Biochimie 2006, 88:309-318.
15. Borradaile N.M., Han X., Harp J.D., Gale S.E., Ory D.S., Schaffer J.E. Disruption of endoplasmic reticulum structure and integrity in lipotoxic cell death. J Lipid Res 2006, 47:2726-2737.
16. Hotamisligil G.S. Role of endoplasmic reticulum stress and c-Jun NH2-terminal kinase pathways in inflammation and origin of obesity and diabetes. Diabetes 2005, 54(suppl 2):S73-S78.
17. Hotamisligil G.S. Inflammation and endoplasmic reticulum stress in obesity and diabetes. Int J Obes (Lond) 2008, 32(suppl 7):S52-S54.
18. Ozcan U., Cao Q., Yilmaz E., et al. Endoplasmic reticulum stress links obesity, insulin action, and type 2 diabetes. Science 2004, 306:457-461.
19. Brzozowska M.M., Ostapowicz G., Weltman M.D. An association between non-alcoholic fatty liver disease and polycystic ovarian syndrome. J Gastroenterol Hepatol 2009, 24:243-247.
20. Chao E.C., Henry R.R. SGLT2 inhibition - a novel strategy for diabetes treatment. Nat Rev Drug Discov 2010, 9:551-559.
21. Fujimori Y., Katsuno K., Nakashima I., Ishikawa-Takemura Y., Fujikura H., Isaji M. Remogliflozin etabonate, in a novel category of selective low-affinity sodium glucose cotransporter (SGLT2) inhibitors, exhibits antidiabetic efficacy in rodent models. J Pharmacol Exp Ther 2008, 327:268-276.
22. Dobbins R.L., O'Connor-Semmes R., Kapur A., et al. Remogliflozin etabonate, a selective inhibitor of the sodium-dependent transporter 2 reduces serum glucose in type 2 diabetes mellitus patients. Diabetes Obes Metab 2012, 14:15-22.
23. Mudaliar S., Armstrong D.A., Mavian A.A., et al. Remogliflozin etabonate, a selective inhibitor of the sodium-glucose transporter 2, improves serum glucose profiles in type 1 diabetes. Diabetes Care 2012, 35:2198-2200.
24. Kapur A., O'Connor-Semmes R., Hussey E.K., et al. First human dose-escalation study with remogliflozin etabonate, a selective inhibitor of the sodium-glucose transporter 2 (SGLT2), in healthy subjects and in subjects with type 2 diabetes mellitus. BMC Pharmacol Toxicol 2013, 14:26.
25. Sykes A.P., Gail L.K., Dobbins R., et al. Randomized efficacy and safety trial of once daily remogliflozin etabonate for the treatment of type 2 diabetes diabetes. Obes Metabolism 2015, 17:98-101.
26. Sykes A.P., O'Connor Semmes R.L., Dobbins R., et al. Randomized trial demonstrating efficacy and safety of twice daily remogliflozin etabonate for the treatment of type 2 diabetes. Diabetes Obes Metab 2015, 17:94-97.
27. Isaji M. SGLT2 inhibitors: molecular design and potential differences in effect. Kidney Int Suppl 2011, S14-S19.
28. Ghosh R.K., Ghosh S.M., Chawla S., Jasdanwala S.A. SGLT2 inhibitors: a new emerging therapeutic class in the treatment of type 2 diabetes mellitus. J Clin Pharmacol 2012, 52:457-463.
29. Isaji M. Sodium-glucose cotransporter inhibitors for diabetes. Curr Opin Investig Drugs 2007, 8:285-292.
30. Folch J., Lees M., Sloane Stanley G.H. A simple method for the isolation and purification of total lipides from animal tissues. J Biol Chem 1957, 226:497-509.
31. Nagasawa T., Inada Y., Nakano S., et al. Effects of bezafibrate, PPAR pan-agonist, and GW501516, PPARdelta agonist, on development of steatohepatitis in mice fed a methionine- and choline-deficient diet. Eur J Pharmacol 2006, 536:182-191.
32. Trogan E., Choudhury R.P., Dansky H.M., Rong J.X., Breslow J.L., Fisher E.A. Laser capture microdissection analysis of gene expression in macrophages from atherosclerotic lesions of apolipoprotein E-deficient mice. Proc Natl Acad Sci U S A 2002, 99:2234-2239.
33. Dandona P., Aljada A., Bandyopadhyay A. Inflammation: the link between insulin resistance, obesity and diabetes. Trends Immunol 2004, 25:4-7.
34. Kanda H., Tateya S., Tamori Y., et al. MCP-1 contributes to macrophage infiltration into adipose tissue, insulin resistance, and hepatic steatosis in obesity. J Clin Invest 2006, 116:1494-1505.
35. Huang D., Ou B., Prior R.L. The chemistry behind antioxidant capacity assays. J Agric Food Chem 2005, 53:1841-1856.
36. Hussey E.K., Kapur A., O'Connor-Semmes R., et al. Safety, pharmacokinetics and pharmacodynamics of remogliflozin etabonate, a novel SGLT2 inhibitor, and metformin when co-administered in subjects with type 2 diabetes mellitus. BMC Pharmacol Toxicol 2013, 14:25.
37. Fujimori Y., Katsuno K., Ojima K., et al. Sergliflozin etabonate, a selective SGLT2 inhibitor, improves glycemic control in streptozotocin-induced diabetic rats and Zucker fatty rats. Eur J Pharmacol 2009, 609:148-154.
38. Katsuno K., Fujimori Y., Ishikawa-Takemura Y., Isaji M. Long-term treatment with sergliflozin etabonate improves disturbed glucose metabolism in KK-A(y) mice. Eur J Pharmacol 2009, 618:98-104.
39. Katsuno K., Fujimori Y., Takemura Y., et al. Sergliflozin, a novel selective inhibitor of low-affinity sodium glucose cotransporter (SGLT2), validates the critical role of SGLT2 in renal glucose reabsorption and modulates plasma glucose level. J Pharmacol Exp Ther 2007, 320:323-330.
40. Tahara A., Kurosaki E., Yokono M., et al. Effects of SGLT2 selective inhibitor ipragliflozin on hyperglycemia, hyperlipidemia, hepatic steatosis, oxidative stress, inflammation, and obesity in type 2 diabetic mice. Eur J Pharmacol 2013, 715:246-255.
41. Tahara A., Kurosaki E., Yokono M., et al. Effects of sodium-glucose cotransporter 2 selective inhibitor ipragliflozin on hyperglycaemia, oxidative stress, inflammation and liver injury in streptozotocin-induced type 1 diabetic rats. J Pharm Pharmacol 2014, 66:975-987.
42. Lindor K.D. Farnesoid X receptor agonists for primary biliary cirrhosis. Curr Opin Gastroenterol 2011, 27:285-288.
43. Miura K., Yang L., van Rooijen N., Ohnishi H., Seki E. Hepatic recruitment of macrophages promotes nonalcoholic steatohepatitis through CCR2. Am J Physiol Gastrointest Liver Physiol 2012, 302:G1310-G1321.