A novel 11β-HSD1 inhibitor improves diabesity and osteoblast differentiation

Journal of Molecular Endocrinology

Volumn 52, Issue 2, 2014, Pages 191-202

  Park, Ji Seon ^a   Bae, Su Jung ^a,b   Choi, Sik Won ^a   Son, You Hwa ^a   Park, Sung Bum ^a,c   Rhee, Sang Dal ^a   Kim, Hee Youn ^a   Jung, Won Hoon ^a   Kang, Seung Kyu ^a   Ahn, Jin Hee ^a   Kim, Seong Hwan ^a   Kim, Ki Young ^a,d  

^a Korea Research Institute of Chemical Technology   (South Korea)

^b Ewha Womans University   (South Korea)

^c Chungnam National University   (South Korea)

^d University of Science and Technology (UST)   (South Korea)

Author keywords

Adipose tissue; Diabetes II; Obesity; Osteoporosis

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE 1 INHIBITOR; BONE MORPHOGENETIC PROTEIN 2; CHOLESTEROL; CORTISONE; FATTY ACID; GLUCOSE; HIGH DENSITY LIPOPROTEIN CHOLESTEROL; IMMUNOGLOBULIN ENHANCER BINDING PROTEIN; KR 67500; LOW DENSITY LIPOPROTEIN CHOLESTEROL; OSTEOCLAST DIFFERENTIATION FACTOR; OXIDOREDUCTASE INHIBITOR; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

ADIPOCYTE; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIDIABETIC ACTIVITY; ARTICLE; CELL DIFFERENTIATION; CHOLESTEROL BLOOD LEVEL; CONTROLLED STUDY; DRUG EFFECT; ENZYME ACTIVITY; FATTY ACID BLOOD LEVEL; GLUCOSE BLOOD LEVEL; GLUCOSE TOLERANCE; IC 50; IN VITRO STUDY; INSULIN SENSITIVITY; INSULIN TOLERANCE TEST; LYMPHOCYTE TRANSFORMATION; MALE; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; OBESITY; ORAL GLUCOSE TOLERANCE TEST; OSTEOBLAST; OSTEOCLASTOGENESIS; OSTEOPOROSIS; PRIORITY JOURNAL; PROTEIN EXPRESSION; REAL TIME POLYMERASE CHAIN REACTION; TREATMENT DURATION; TRIACYLGLYCEROL BLOOD LEVEL;

ADIPOSE TISSUE; DIABETES II; OBESITY; OSTEOPOROSIS;

11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1; 3T3-L1 CELLS; ADIPOGENESIS; ANIMALS; BONE MARROW CELLS; CELL DIFFERENTIATION; DIABETES MELLITUS, EXPERIMENTAL; DIET; ENZYME INHIBITORS; GLUCOSE TOLERANCE TEST; INSULIN RESISTANCE; MACROPHAGES; MALE; MICE; MICE, INBRED C57BL; OBESITY; OSTEOBLASTS; OSTEOCLASTS; REAL-TIME POLYMERASE CHAIN REACTION;

EID: 84897855781     PISSN: 09525041     EISSN: 14796813     Source Type: Journal    
DOI: 10.1530/JME-13-0177     Document Type: Article

References (39)

1. Bryant NJ, Govers R & James DE 2002 Regulated transport of the glucose transporter GLUT4. Nature Reviews. Molecular Cell Biology 3 267-277. (doi:10.1038/nrm782)
2. Bujalska IJ, Gathercole LL, Tomlinson JW, Darimont C, Ermolieff J, Fanjul AN, Rejto PA & Stewart PM 2008 A novel selective 11b-hydroxysteroid dehydrogenase type 1 inhibitor prevents human adipogenesis. Journal of Endocrinology 197 297-307. (doi:10.1677/JOE-08-0050)
3. Canalis E, Mazziotti G, Giustina A & Bilezikian JP 2007 Glucocorticoid-induced osteoporosis: pathophysiology and therapy. Osteoporosis International 18 1319-1328.(doi:10.1007/s00198-007-0394-0)
4. Cho YS, Kim CH & Cheon HG 2009 Cell-based assay for screening 11b-hydroxysteroid dehydrogenase 1 inhibitors. Analytical Biochemistry 392 110-116. (doi:10.1016/j.ab.2009.04.038)
5. Choi SW, Moon SH, Yang HJ, Kwon DY, Son YJ, Yu R, Kim YS, Kim SI, Chsae EJ, Park SJ et al. 2013 Antiresorptive activity of bacillus-fermented antler extracts: inhibition of osteoclast differentiation. Evidence-Based Complementary and Alternative Medicine: eCAM 2013 748687.
6. Cooper MS, Walker EA, Bland R, Fraser WD, Hewison M & Stewart PM 2000 Expression and functional consequences of 11b-hydroxysteroid dehydrogenase activity in human bone. Bone 27 375-381. (doi:10.1016/S8756-3282(00)00344-6)
7. Cooper MS, Rabbitt EH, Goddard PE, Bartlett WA, Hewison M & Stewart PM 2002 Osteoblastic 11b-hydroxysteroid dehydrogenase type 1 activity increases with age and glucocorticoid exposure. Journal of Bone and Mineral Research 17 979-986. (doi:10.1359/jbmr.2002.17.6.979)
8. Dalle Carbonare L, Arlot ME, Chavassieux PM, Roux JP, Portero NR & Meunier PJ 2001 Comparison of trabecular bone microarchitecture and remodeling in glucocorticoid-induced and postmenopausal osteoporosis. Journal of Bone and Mineral Research 16 97-103. (doi:10.1359/ jbmr.2001.16.1.97)
9. Eijken M, Hewison M, Cooper MS, de Jong FH, Chiba H, Stewart PM, Uitterlinden AG, Pols HA & van Leeuwen JP 2005 11b-Hydroxysteroid dehydrogenase expression and glucocorticoid synthesis are directed by a molecular switch during osteoblast differentiation. Molecular Endocrinology 19 621-631. (doi:10.1210/me.2004-0212)
10. Hauner H, Schmid P & Pfeiffer EF 1987 Glucocorticoids and insulin promote the differentiation of human adipocyte precursor cells into fat cells. Journal of Clinical Endocrinology and Metabolism 64 832-835. (doi:10.1210/jcem-64-4-832)
11. Hofbauer LC, Gori F, Riggs BL, Lacey DL, Dunstan CR, Spelsberg TC & Khosla S 1999 Stimulation of osteoprotegerin ligand and inhibition of osteoprotegerin production by glucocorticoids in human osteoblastic lineage cells: potential paracrine mechanisms of glucocorticoid-induced osteoporosis. Endocrinology 140 4382-4389.
12. Hotamisligil GS, Johnson RS, Distel RJ, Ellis R, Papaioannou VE & Spiegelman BM 1996 Uncoupling of obesity from insulin resistance through a targeted mutation in aP2, the adipocyte fatty acid binding protein. Science 274 1377-1379. (doi:10.1126/science.274.5291.1377)
13. Ishikawa T, Kamiyama M, Tani-Ishii N, Suzuki H, Ichikawa Y, Hamaguchi Y, Momiyama N and Shimada H 2001 Inhibition ofosteoclast differentiation and bone resorption by cathepsin K antisense oligonucleotides. Molecular Carcinogenesis 32 84-91. (doi:10.1002/mc.1067)
14. Kersten JR, Toller WG, Gross ER, Pagel PS & Warltier DC 2000 Diabetes abolishes ischemic preconditioning: role of glucose, insulin, and osmolality. American Journal of Physiology. Heart and Circulatory Physiology 278 H1218-H1224.
15. Kim HJ & Kim SH 2010 Tanshinone IIA enhances BMP-2-stimulated commitment of C2C12 cells into osteoblasts via p38 activation. Amino Acids 39 1217-1226. (doi:10.1007/s00726-010-0557-8)
16. Kim K, Lee SH, Ha Kim J, Choi Y & Kim N 2008 NFATc1 induces osteoclast fusion via up-regulation of Atp6v0d2 and the dendritic cell-specific transmembrane protein (DC-STAMP). Molecular Endocrinology 22 176-185. (doi:10.1210/me.2007-0237)
17. Kim SH, Bok JH, Lee JH, Kim IH, Kwon SW, Lee GB, Kang SK, Park JS, Jung WH, Kim HY et al. 2012 Synthesis and biological evaluation of cyclic sulfamide derivatives as 11b-hydroxysteroid dehydrogenase 1 inhibitors. ACS Medicinal Chemistry Letters 3 88-93. (doi:10.1021/ ml200226x)
18. Klein RG, Arnaud SB, Gallagher JC, Deluca HF & Riggs BL 1977 Intestinal calcium absorption in exogenous hypercortisonism. Role of 25-hydroxyvitamin D and corticosteroid dose. Journal of Clinical Investigation 60 253-259. (doi:10.1172/JCI108762)
19. Kotelevtsev Y, Holmes MC, Burchell A, Houston PM, Schmoll D, Jamieson P, Best R, Brown R, Edwards CR, Seckl JR et al. 1997 11b-hydroxysteroid dehydrogenase type 1 knockout mice show attenuated glucocorticoid-inducible responses and resist hyperglycemia on obesity or stress. PNAS 94 14924-14929. (doi:10.1073/pnas.94.26.14924)
20. Li G, Peng H, Corsi K, Usas A, Olshanski A & Huard J 2005 Differential effect of BMP4 on NIH/3T3 and C2C12 cells: implications for endochondral bone formation. Journal of Bone and Mineral Research 20 1611-1623. (doi:10.1359/JBMR.050513)
21. Masuzaki H, Paterson J, Shinyama H, Morton NM, Mullins JJ, Seckl JR & Flier JS 2001 A transgenic model of visceral obesity and the metabolic syndrome. Science 294 2166-2170. (doi:10.1126/ science.1066285)
22. Morton NM, Holmes MC, Fievet C, Staels B, Tailleux A, Mullins JJ & Seckl JR 2001 Improved lipid and lipoprotein profile, hepatic insulin sensitivity, and glucose tolerance in 11b-hydroxysteroid dehydrogenase type 1 null mice. Journal of Biological Chemistry 276 41293-41300. (doi:10.1074/ jbc.M103676200)
23. Morton NM, Paterson JM, Masuzaki H, Holmes MC, Staels B, Fievet C, Walker BR, Flier JS, Mullins JJ & Seckl JR 2004 Novel adipose tissue-mediated resistance to diet-induced visceral obesity in 11b-hydroxysteroid dehydrogenase type 1-deficient mice. Diabetes 53 931-938. (doi:10.2337/diabetes.53.4.931)
24. Park SY, Choi GH, Choi HI, Ryu J, Jung CY & Lee W 2005 Calorie restriction improves whole-body glucose disposal and insulin resistance in association with the increased adipocyte-specific GLUT4 expression in Otsuka Long-Evans Tokushima fatty rats. Archives of Biochemistry and Biophysics 436 276-284. (doi:10.1016/j.abb.2005.01.010)
25. Park JS, Rhee SD, Kang NS, Jung WH, Kim HY, Kim JH, Kang SK, Cheon HG, Ahn JH & 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). Biochemical Pharmacology 81 1028-1035. (doi:10.1016/j.bcp.2011.01.020)
26. Park JS, Rhee SD, Jung WH, Kang NS, Kim HY, Kang SK, Ahn JH & Kim KY 2012 Anti-diabetic and anti-adipogenic effects of a novel selective 11b-hydroxysteroid dehydrogenase type 1 inhibitor in the diet-induced obese mice. European Journal of Pharmacology 691 19-27. (doi:10.1016/ j.ejphar.2012.06.024)
27. Paterson JM, Morton NM, Fievet C, Kenyon CJ, Holmes MC, Staels B, Seckl JR & Mullins JJ 2004 Metabolic syndrome without obesity: hepatic overexpression of 11b-hydroxysteroid dehydrogenase type 1 in transgenic mice. PNAS 101 7088-7093. (doi:10.1073/pnas. 0305524101)
28. Rosen ED & MacDougald OA 2006 Adipocyte differentiation from the inside out. Nature Reviews. Molecular Cell Biology 7 885-896. (doi:10.1038/nrm2066)
29. Rosenstock J, Banarer S, Fonseca VA, Inzucchi SE, Sun W, Yao W, Hollis G, Flores R, Levy R, Williams WV et al. 2010 The 11-b-hydroxysteroid dehydrogenase type 1 inhibitor INCB13739 improves hyperglycemia in patients with type 2 diabetes inadequately controlled by metformin monotherapy. Diabetes Care 33 1516-1522. (doi:10.2337/dc09-2315)
30. Sato T, Man ZW, Toide K & Asahi Y 1997 Plasma membrane content of insulinregulated glucose transporter in skeletal muscle of the male Otsuka Long-Evans Tokushima fatty rat, a model of non-insulin-dependent diabetes mellitus. FEBS Letters 407 329-332. (doi:10.1016/ S0014-5793(97)00369-4)
31. Stewart PM & Krozowski ZS 1999 11b-Hydroxysteroid dehydrogenase. Vitamins and Hormones 57 249-324.
32. Tachibe M, Kato R, Sugano S, Kishida T & Ebihara K 2009 Hydroxypropy-lated tapioca starch retards the development of insulin resistance in KKAy mice, a type 2 diabetes model, fed a high-fat diet. Journal of Food Science 74 H232-H236. (doi:10.1111/j.1750-3841.2009.01276.x)
33. Takayanagi H, Kim S, Koga T, Nishina H, Isshiki M, Yoshida H, Saiura A, Isobe M, Yokochi T, Inoue J et al. 2002 Induction and activation of the transcription factor NFATc1 (NFAT2) integrate RANKL signaling for terminal differentiation of osteoclasts. Developmental Cell 3 889-901. (doi:10.1016/S1534-5807(02)00369-6)
34. Tomlinson JJ, Boudreau A, Wu D, Atlas E & Haché RJ 2006 Modulation of early human preadipocyte differentiation by glucocorticoids. Endocrinology 147 5284-5293. (doi:10.1210/en.2006-0267)
35. Wang M 2005 The role of glucocorticoid action in the pathophysiology of the metabolic syndrome. Nutrition and Metabolism 2 3. (doi:10.1186/ 1743-7075-2-3)
36. Wang ZQ, Ovitt C, Grigoriadis AE, Möhle-Steinlein U, Rüther U & Wagner EF 1992 Bone and haematopoietic defects in mice lacking c-fos. Nature 360 741-745. (doi:10.1038/360741a0)
37. Wing RR, Blair EH, Bononi P, Marcus MD, Watanabe R & Bergman RN 1994 Caloric restriction per se is a significant factor in improvements in glycemic control and insulin sensitivity during weight loss in obese NIDDM patients. Diabetes Care 17 30-36. (doi:10.2337/ diacare.17.1.30)
38. Wu Z, Bucher NL & Farmer SR 1996 Induction of peroxisome proliferator-activated receptor gamma during the conversion of 3T3 fibroblasts into adipocytes is mediated by C/EBPb, C/EBPd, and glucocorticoids. Molecular and Cellular Biology 16 4128-4136.
39. Yamaguchi A, Ishizuya T, Kintou N, Wada Y, Katagiri T, Wozney JM, Rosen V & Yoshiki S 1996 Effects of BMP-2, BMP-4, and BMP-6 on osteoblastic differentiation of bone marrow-derived stromal cell lines, ST2 and MC3T3-G2/PA6. Biochemical and Biophysical Research Communications 220 366-371. (doi:10.1006/bbrc.1996.0411)