HIS-388, a novel orally active and long-acting 11β-hydroxysteroid dehydrogenase type 1 inhibitor, ameliorates insulin sensitivity and glucose intolerance in diet-induced obesity and nongenetic type 2 diabetic murine models

Journal of Pharmacology and Experimental Therapeutics

Volumn 351, Issue 1, 2014, Pages 181-189

  Okazaki, Seiji ^a   Takahashi, Takehiro ^a   Iwamura, Tomokatsu ^a   Nakaki, Junko ^a   Sekiya, Yumiko ^a   Yagi, Mai ^a   Kumagai, Hiroki ^a   Sato, Mikiya ^a   Sakami, Satoshi ^a   Nitta, Aiko ^a   Kawai, Koji ^a   Kainoh, Mie ^a  

^a TORAY INDUSTRIES INC   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE 1; 544 [(3 ADAMANTAN 1YL) 6,7,8,9 TETRAHYDRO 5H [1,2,4]TRIAZOLO[4,3 A]AZEPINE]; ANTIDIABETIC AGENT; CARBENOXOLONE; ENZYME INHIBITOR; GLUCOSE; HYDROCORTISONE; INSULIN; INSULIN SENSITIZING AGENT; PIOGLITAZONE; STREPTOZOCIN; UNCLASSIFIED DRUG; [N (5 HYDROXYADAMANTAN 2YL) 3 (PYRIDIN 2 YL) ISOXAZOLE 4 CARBOXAMIDE]; 2,4 THIAZOLIDINEDIONE DERIVATIVE; 3-(1-ADAMANTYL)-6,7,8,9-TETRAHYDRO-5H-(1,2,4)TRIAZOLO(4,3-A)AZEPINE; ADAMANTANE; AZEPINE DERIVATIVE; ISOXAZOLE DERIVATIVE; N-(5-HYDROXYADAMANTAN-2-YL)-3-(PYRIDIN-2-YL)ISOXAZOLE-4-CARBOXAMIDE; TRIAZOLE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; BODY WEIGHT; CONTROLLED STUDY; DIET INDUCED OBESITY; DISEASE ASSOCIATION; DRUG STRUCTURE; ENZYME ACTIVITY; ENZYME ASSAY; GLUCOSE BLOOD LEVEL; GLUCOSE INTOLERANCE; GLUCOSE METABOLISM; HYDROCORTISONE BLOOD LEVEL; HYPERCORTISOLISM; HYPERINSULINEMIA; IN VIVO STUDY; INSULIN BLOOD LEVEL; INSULIN RESISTANCE; INSULIN SENSITIVITY; LIPID DIET; LOW DRUG DOSE; MALE; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; OBESITY; SINGLE DRUG DOSE; ANALOGS AND DERIVATIVES; ANIMAL; ANTAGONISTS AND INHIBITORS; C57BL MOUSE; COMPARATIVE STUDY; DIABETES MELLITUS, EXPERIMENTAL; DRUG EFFECTS; ENZYMOLOGY; FEMALE; HUMAN; LIVER MICROSOME; METABOLISM; ORAL DRUG ADMINISTRATION;

11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1; ADAMANTANE; ADMINISTRATION, ORAL; ANIMALS; AZEPINES; CARBENOXOLONE; DIABETES MELLITUS, EXPERIMENTAL; ENZYME INHIBITORS; FEMALE; GLUCOSE INTOLERANCE; HUMANS; HYPOGLYCEMIC AGENTS; INSULIN RESISTANCE; ISOXAZOLES; MALE; MICE; MICE, INBRED C57BL; MICROSOMES, LIVER; OBESITY; THIAZOLIDINEDIONES; TRIAZOLES;

EID: 84907176114     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.114.216556     Document Type: Article

References (34)

1. Abdul-Ghani MA, Tripathy D, and DeFronzo RA (2006) Contributions of beta-cell dysfunction and insulin resistance to the pathogenesis of impaired glucose tolerance and impaired fasting glucose. Diabetes Care 29:1130-1139.
2. Alberts P, Nilsson C, Selen G, Engblom LO, Edling NH, Norling S, Klingström G, Larsson C, Forsgren M, Ashkzari M, et al. (2003) Selective inhibition of 11 betahydroxysteroid dehydrogenase type 1 improves hepatic insulin sensitivity in hyperglycemic mice strains. Endocrinology 144:4755-4762.
3. Anagnostis P, Katsiki N, Adamidou F, Athyros VG, Karagiannis A, Kita M, and Mikhailidis DP (2013) 11beta-Hydroxysteroid dehydrogenase type 1 inhibitors: novel agents for the treatment of metabolic syndrome and obesity-related disorders? Metabolism 62:21-33.
4. Arner P (2003) The adipocyte in insulin resistance: key molecules and the impact of the thiazolidinediones. Trends Endocrinol Metab 14:137-145.
5. Bhat BG, Younis H, Herrera J, Palacio K, Pascual B, Hur G, Jessen B, Ogilvie KM, and Rejto PA (2008) Antisense inhibition of 11betahydroxysteroid dehydrogenase type 1 improves diabetes in a novel cortisone-induced diabetic KK mouse model. Biochem Biophys Res Commun 365:740-745.
6. Derosa G and Maffioli P (2012) Peroxisome proliferator-activated receptor-g (PPAR-g) agonists on glycemic control, lipid profile and cardiovascular risk. Curr Mol Pharmacol 5:272-281.
7. Evans RM, Barish GD, and Wang YX (2004) PPARs and the complex journey to obesity. Nat Med 10:355-361.
8. Friedman JE, Yun JS, Patel YM, McGrane MM, and Hanson RW (1993) Glucocorticoids regulate the induction of phosphoenolpyruvate carboxykinase (GTP) gene transcription during diabetes. J Biol Chem 268:12952-12957.
9. Gillies PS and Dunn CJ (2000) Pioglitazone. Drugs 60:333-343, discussion 344-345.
10. Goto A, Goto M, Noda M, and Tsugane S (2013) Incidence of type 2 diabetes in Japan: a systematic review and meta-analysis. PLoS ONE 8:e74699.
11. Harno E and White A (2010) Will treating diabetes with 11b-HSD1 inhibitors affect the HPA axis? Trends Endocrinol Metab 21:619-627.
12. Hermanowski-Vosatka A, Balkovec JM, Cheng K, Chen HY, Hernandez M, Koo GC, Le Grand CB, Li Z, Metzger JM, Mundt SS, et al. (2005) 11beta-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice. J Exp Med 202:517-527.
13. Kahn SE, Hull RL, and Utzschneider KM (2006) Mechanisms linking obesity to insulin resistance and type 2 diabetes. Nature 444:840-846.
14. Kotelevtsev Y, Holmes MC, Burchell A, Houston PM, Schmoll D, Jamieson P, Best R, Brown R, Edwards CR, and Seckl JR, et al. (1997) 11beta-Hydroxysteroid dehydrogenase type 1 knockout mice show attenuated glucocorticoid-inducible responses and resist hyperglycemia on obesity or stress. Proc Natl Acad Sci USA 94:14924-14929.
15. Kushiro M, Takahashi Y, and Ide T (2004) Species differences in the physiological activity of dietary lignan (sesamin and episesamin) in affecting hepatic fatty acid metabolism. Br J Nutr 91:377-386.
16. Lee HJ, Choi SS, Park MK, An YJ, Seo SY, Kim MC, Hong SH, Hwang TH, Kang DY, Garber AJ, et al. (2002) Fenofibrate lowers abdominal and skeletal adiposity and improves insulin sensitivity in OLETF rats. Biochem Biophys Res Commun 296: 293-299.
17. Lehmann JM, Moore LB, Smith-Oliver TA, Wilkison WO, Willson TM, and Kliewer SA (1995) An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem 270: 12953-12956.
18. Lindsay RS, Wake DJ, Nair S, Bunt J, Livingstone DE, Permana PA, Tataranni PA, and Walker BR (2003) Subcutaneous adipose 11 beta-hydroxysteroid dehydrogenase type 1 activity and messenger ribonucleic acid levels are associated with adiposity and insulinemia in Pima Indians and Caucasians. J Clin Endocrinol Metab 88:2738-2744.
19. Luo J, Quan J, Tsai J, Hobensack CK, Sullivan C, Hector R, and Reaven GM (1998) Nongenetic mouse models of non-insulin-dependent diabetes mellitus. Metabolism 47:663-668.
20. Masuzaki H, Paterson J, Shinyama H, Morton NM, Mullins JJ, Seckl JR, and Flier JS (2001) A transgenic model of visceral obesity and the metabolic syndrome. Science 294:2166-2170.
21. Masuzaki H, Yamamoto H, Kenyon CJ, Elmquist JK, Morton NM, Paterson JM, Shinyama H, Sharp MG, Fleming S, Mullins JJ, et al. (2003) Transgenic amplification of glucocorticoid action in adipose tissue causes high blood pressure in mice. J Clin Invest 112:83-90.
22. Moller DE (2001) New drug targets for type 2 diabetes and the metabolic syndrome. Nature 414:821-827.
23. Morton NM, Holmes MC, Fiévet C, Staels B, Tailleux A, Mullins JJ, and Seckl JR (2001) Improved lipid and lipoprotein profile, hepatic insulin sensitivity, and glucose tolerance in 11beta-hydroxysteroid dehydrogenase type 1 null mice. J Biol Chem 276:41293-41300.
24. Mu J, Petrov A, Eiermann GJ, Woods J, Zhou YP, Li Z, Zycband E, Feng Y, Zhu L, Roy RS, et al. (2009) Inhibition of DPP-4 with sitagliptin improves glycemic control and restores islet cell mass and function in a rodent model of type 2 diabetes. Eur J Pharmacol 623:148-154.
25. Okuno A, Tamemoto H, Tobe K, Ueki K, Mori Y, Iwamoto K, Umesono K, Akanuma Y, Fujiwara T, Horikoshi H, et al. (1998) Troglitazone increases the number of small adipocytes without the change of white adipose tissue mass in obese Zucker rats. J Clin Invest 101:1354-1361.
26. Park JS, Rhee SD, Kang NS, Jung WH, Kim HY, Kim JH, Kang SK, Cheon HG, Ahn JH, and Kim KY (2011) Anti-diabetic and anti-adipogenic effects of a novel selective 11b-hydroxysteroid dehydrogenase type 1 inhibitor, 2-(3-benzoyl)-4-hydroxy- 1,1-dioxo-2H-1,2-benzothiazine-2-yl-1-phenylethanone (KR-66344). Biochem Pharmacol 81:1028-1035.
27. Paterson JM, Morton NM, Fievet C, Kenyon CJ, Holmes MC, Staels B, Seckl JR, and Mullins JJ (2004) Metabolic syndrome without obesity: Hepatic overexpression of 11beta-hydroxysteroid dehydrogenase type 1 in transgenic mice. Proc Natl Acad Sci USA 101:7088-7093.
28. Pickavance LC, Brand CL, Wassermann K, and Wilding JP (2005) The dual PPARalpha/gamma agonist, ragaglitazar, improves insulin sensitivity and metabolic profile equally with pioglitazone in diabetic and dietary obese ZDF rats. Br J Pharmacol 144:308-316.
29. Ruderman NB, Carling D, Prentki M, and Cacicedo JM (2013) AMPK, insulin resistance, and the metabolic syndrome. J Clin Invest 123:2764-2772.
30. Sundbom M, Kaiser C, Björkstrand E, Castro VM, Larsson C, Selén G, Nyhem CS, and James SR (2008) Inhibition of 11betaHSD1 with the S-phenylethylaminothiazolone BVT116429 increases adiponectin concentrations and improves glucose homeostasis in diabetic KKAy mice. BMC Pharmacol 8:3.
31. Wamil M, Battle JH, Turban S, Kipari T, Seguret D, de Sousa Peixoto R, Nelson YB, Nowakowska D, Ferenbach D, Ramage L, et al. (2011) Novel fat depot-specific mechanisms underlie resistance to visceral obesity and inflammation in 11 b-hydroxysteroid dehydrogenase type 1-deficient mice. Diabetes 60:1158-1167.
32. Wang SJ, Birtles S, de Schoolmeester J, Swales J, Moody G, Hislop D, O'Dowd J, Smith DM, Turnbull AV, and Arch JR (2006) Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 reduces food intake and weight gain but maintains energy expenditure in diet-induced obese mice. Diabetologia 49:1333-1337.
33. Whiting DR, Guariguata L, Weil C, and Shaw J (2011) IDF diabetes atlas: global estimates of the prevalence of diabetes for 2011 and 2030. Diabetes Res Clin Pract 94:311-321.
34. Yang T and Soodvilai S (2008) Renal and vascular mechanisms of thiazolidinedioneinduced fluid retention. PPAR Res 2008:943614.