Benzbromarone, an old uricosuric drug, inhibits human fatty acid binding protein 4 in vitro and lowers the blood glucose level in db/db mice

Acta Pharmacologica Sinica

Volumn 34, Issue 11, 2013, Pages 1397-1402

  Cai, Hai Yan ^a,b   Wang, Ting ^a   Zhao, Jian Chun ^c   Sun, Peng ^a   Yan, Gui Rui ^a   Ding, Hai Peng ^b   Li, Ying Xia ^c   Wang, He Yao ^a   Zhu, Wei Liang ^a   Chen, Kai Xian ^a  

^a SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

^b TONGJI UNIVERSITY   (China)

^c FUDAN UNIVERSITY   (China)

Author keywords

Adipocyte; Benzbromarone; Db db mouse; Diabetes; Fatty acid binding protein 4; Molecular docking; Uricosuric drug

Indexed keywords

BENZBROMARONE; FATTY ACID BINDING PROTEIN 4; FORSKOLIN;

ADIPOCYTE; ANIMAL EXPERIMENT; ANTIDIABETIC ACTIVITY; ARTICLE; CONTROLLED STUDY; DRUG PROTEIN BINDING; GLUCOSE BLOOD LEVEL; HUMAN; IN VITRO STUDY; IN VIVO STUDY; LIPOLYSIS; MALE; MOLECULAR DOCKING; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PROTEIN EXPRESSION; SITE DIRECTED MUTAGENESIS;

3T3-L1 CELLS; ANIMALS; BENZBROMARONE; BLOOD GLUCOSE; DIABETES MELLITUS, TYPE 2; DOSE-RESPONSE RELATIONSHIP, DRUG; FATTY ACID-BINDING PROTEINS; GLUCOSE TOLERANCE TEST; HUMANS; INHIBITORY CONCENTRATION 50; INSULIN RESISTANCE; MALE; MICE; MICE, INBRED C57BL; MOLECULAR DOCKING SIMULATION; MUTAGENESIS, SITE-DIRECTED; URICOSURIC AGENTS;

EID: 84887400598     PISSN: 16714083     EISSN: 17457254     Source Type: Journal    
DOI: 10.1038/aps.2013.97     Document Type: Article

References (26)

1. Spiegelman BM, Frank M, Green H. Molecular cloning of mRNA from 3T3 adipocytes. Regulation of mRNA content for glycerophosphate dehydrogenase and other differentiation-dependent proteins during adipocyte development. J Biol Chem 1983; 258: 10083-9.
2. Hunt CR, Ro JH, Dobson DE, Min HY, Spiegelman BM. Adipocyte P2 gene: developmental expression and homology of 5′-flanking sequences among fat cell-specific genes. Proc Natl Acad Sci U S A 1986; 83: 3786-90. (Pubitemid 16062370)
3. Hotamisligil GS, Johnson RS, Distel RJ, Ellis R, Papaioannou VE, Spiegelman BM. Uncoupling of obesity from insulin resistance through a targeted mutation in aP2, the adipocyte fatty acid binding protein. Science 1996; 274: 1377-9. (Pubitemid 26391462)
4. Uysal KT, Scheja L, Wiesbrock SM, Bonner-Weir S, Hotamisligil GS. Improved glucose and lipid metabolism in genetically obese mice lacking aP2. Endocrinology 2000; 141: 3388-96. (Pubitemid 32269028)
5. Tuncman G, Erbay E, Hom X, De Vivo I, Campos H, Rimm EB, et al. A genetic variant at the fatty acid-binding protein aP2 locus reduces the risk for hypertriglyceridemia, type 2 diabetes, and cardiovascular disease. Proc Natl Acad Sci U S A 2006; 103: 6970-5.
6. Makowski L, Boord JB, Maeda K, Babaev VR, Uysal KT, Morgan MA, et al. Lack of macrophage fatty-acid-binding protein aP2 protects mice deficient in apolipoprotein E against atherosclerosis. Nat Med 2001; 7: 699-705. (Pubitemid 32588026)
7. Furuhashi M, Tuncman G, Gorgun CZ, Makowski L, Atsumi G, Vaillancourt E, et al. Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2. Nature 2007; 447: 959-65. (Pubitemid 46975747)
8. Heel RC, Brogden RN, Speight TM, Avery GS. Benzbromarone: a review of its pharmacological properties and therapeutic use in gout and hyperuricaemia. Drugs 1977; 14: 349-66. (Pubitemid 8218330)
9. Cai HY, Yan GR, Zhang XD, Gorbenko O, Wang HY, Zhu WL. Discovery of highly selective inhibitors of human fatty acid binding protein 4 (FABP4) by virtual screening. Bioorg Med Chem Lett 2010; 20: 3675-9.
10. Zhang XD, Yan JW, Yan GR, Sun XY, Ji J, Li YM, et al. Pharmacological inhibition of diacylglycerol acyltransferase 1 reduces body weight gain, hyperlipidemia, and hepatic steatosis in db/db mice. Acta Pharmacol Sin 2010; 31: 1470-7.
11. Morris GM, Goodsell DS, Halliday RS, Huey R, Hart WE, Belew RK, et al. Automated docking using a Lamarckian genetic algorithm and an empirical binding free energy function. J Comput Chem 1998; 19: 1639-62. (Pubitemid 128590223)
12. Sulsky R, Magnin DR, Huang Y, Simpkins L, Taunk P, Patel M, et al. Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP). Bioorg Med Chem Lett 2007; 17: 3511-5. (Pubitemid 46824179)
13. Coe NR, Simpson MA, Bernlohr DA. Targeted disruption of the adipocyte lipid-binding protein (aP2 protein) gene impairs fat cell lipolysis and increases cellular fatty acid levels. J Lipid Res 1999; 40: 967-72. (Pubitemid 29220539)
14. Hertzel AV, Hellberg K, Reynolds JM, Kruse AC, Juhlmann BE, Smith AJ, et al. Identification and characterization of a small molecule inhibitor of Fatty Acid binding proteins. J Med Chem 2009; 52: 6024-31.
15. Lehmann F, Haile S, Axen E, Medina C, Uppenberg J, Svensson S, et al. Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target. Bioorg Med Chem Lett 2004; 14: 4445-8. (Pubitemid 39043964)
16. Ringom R, Axen E, Uppenberg J, Lundback T, Rondahl L, Barf T. Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1H)-ones: a novel class of selective human A-FABP inhibitors. Bioorg Med Chem Lett 2004; 14: 4449-52. (Pubitemid 39043965)
17. Barf T, Lehmann F, Hammer K, Haile S, Axen E, Medina C, et al. N-Benzyl-indolo carboxylic acids: Design and synthesis of potent and selective adipocyte fatty-acid binding protein (A-FABP) inhibitors. Bioorg Med Chem Lett 2009; 19: 1745-8.
18. LaLonde JM, Levenson MA, Roe JJ, Bernlohr DA, Banaszak LJ. Adipocyte lipid-binding protein complexed with arachidonic acid. Titration calorimetry and X-ray crystallographic studies. J Biol Chem 1994; 269: 25339-47.
19. Marr E, Tardie M, Carty M, Brown Phillips T, Wang IK, Soeller W, et al. Expression, purification, crystallization and structure of human adipocyte lipid-binding protein (aP2). Acta Crystallogr Sect F Struct Biol Cryst Commun 2006; 62: 1058-60. (Pubitemid 44684138)
20. Butler EG, Ichida T, Maruyama H, Schulte-Hermann R, Williams GM. Toxicological studies on a benzofurane derivative. II. Demonstration of peroxisome proliferation in rat liver. Toxicol Appl Pharmacol 1990; 106: 500-8.
21. Kunishima C, Inoue I, Oikawa T, Nakajima H, Komoda T, Katayama S. Activating effect of benzbromarone, a uricosuric drug, on peroxisome proliferator-activated receptors. PPAR Res 2007; 2007: 36092-8.
22. Montanari R, Saccoccia F, Scotti E, Crestani M, Godio C, Gilardi F, et al. Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. J Med Chem 2008; 51: 7768-76.
23. Festuccia WT, Laplante M, Berthiaume M, Gelinas Y, Deshaies Y. PPARgamma agonism increases rat adipose tissue lipolysis, expression of glyceride lipases, and the response of lipolysis to hormonal control. Diabetologia 2006; 49: 2427-36. (Pubitemid 44359105)
24. Carmona MC, Louche K, Nibbelink M, Prunet B, Bross A, Desbazeille M, et al. Fenofibrate prevents Rosiglitazone-induced body weight gain in ob/ob mice. Int J Obes (Lond) 2005; 29: 864-71. (Pubitemid 40897026)
25. WHO Drug Information: Benzbromarone and hepatitis. WHO Drug Information 2000; 14.
26. Lee MH, Graham GG, Williams KM, Day RO. A benefit-risk assessment of benzbromarone in the treatment of gout. Was its withdrawal from the market in the best interest of patients? Drug Saf 2008; 31; 643-65. (Pubitemid 352019563)