KDT501, a derivative from hops, normalizes glucose metabolism and body weight in rodent models of diabetes

PLoS ONE

Volumn 9, Issue 1, 2014, Pages

  Konda, Veera R ^a   Desai, Anuradha ^a   Darland, Gary ^a   Grayson, Neile ^a   Bland, Jeffrey S ^a  

^a KinDex Therapeutics   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIDIABETIC AGENT; CHOLESTEROL; GLUCOSE; HEMOGLOBIN A1C; INSULIN; KDT 501; LIPID; METFORMIN; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR; PIOGLITAZONE; ROSIGLITAZONE; TELMISARTAN; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

ADIPOCYTE; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIDIABETIC ACTIVITY; ANTIINFLAMMATORY ACTIVITY; ARTICLE; BODY COMPOSITION; BODY FAT; BODY WEIGHT; CHOLESTEROL BLOOD LEVEL; DIABETES MELLITUS; DRUG SCREENING; GENE EXPRESSION PROFILING; GLUCOSE BLOOD LEVEL; GLUCOSE METABOLISM; HEMOGLOBIN BLOOD LEVEL; HOPS; HUMAN; HUMAN CELL; INSULIN SENSITIVITY; LIPOGENESIS; MACROPHAGE; MALE; MONOCYTE; MOUSE; NONHUMAN; OBESITY; PLEIOTROPY; RAT; RODENT; WEIGHT GAIN; ZUCKER DIABETIC FATTY RAT;

ADIPOCYTES; ANIMALS; BLOOD GLUCOSE; BODY WEIGHT; CELLS, CULTURED; DIABETES MELLITUS, EXPERIMENTAL; DIABETES MELLITUS, TYPE 2; GLUCOSE; HEMOGLOBIN A, GLYCOSYLATED; HUMANS; HUMULUS; HYPOGLYCEMIC AGENTS; INSULIN; INSULIN RESISTANCE; MACROPHAGES; MALE; METFORMIN; MICE; MICE, INBRED C57BL; MICE, OBESE; MONOCYTES; PPAR GAMMA; RATS; RATS, ZUCKER; THIAZOLIDINEDIONES; TRIGLYCERIDES;

EID: 84900399238     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0087848     Document Type: Article

References (37)

1. Hotamisligil GS, Shargill NS, Spiegelman BM (1993) Adipose expression of tumor necrosis factor-alpha: direct role in obesity-linked insulin resistance. Science 259: 87-91. (Pubitemid 23036092)
2. Siriwardhana N, Kalupahana NS, Cekanova M, Lemieux M, Greer B, et al. (2013) Modulation of adipose tissue inflammation by bioactive food compounds. J Nutr Biochem 24: 613-623.
3. Weisberg SP, McCann D, Desai M, Rosenbaum M, Leibel RL, et al. (2003) Obesity is associated with macrophage accumulation in adipose tissue. J Clin Invest 112: 1796-1808. (Pubitemid 38063703)
4. Ferrante AW Jr (2007) Obesity-induced inflammation: a metabolic dialogue in the language of inflammation. J Intern Med 262: 408-414.
5. Lumeng CN, DelProposto JB, Westcott DJ, Saltiel AR (2008) Phenotypic switching of adipose tissue macrophages with obesity is generated by spatiotemporal differences in macrophage subtypes. Diabetes 57: 3239-3246.
6. Odegaard JI, Ricardo-Gonzalez RR, Goforth MH, Morel CR, Subramanian V, et al. (2007) Macrophage-specific PPARgamma controls alternative activation and improves insulin resistance. Nature 447: 1116-1120. (Pubitemid 47014427)
7. Brun RP, Spiegelman BM (1997) PPAR gamma and the molecular control of adipogenesis. J Endocrinol 155: 217-218. (Pubitemid 27475813)
8. Peraza MA, Burdick AD, Marin HE, Gonzalez FJ, Peters JM (2006) The toxicology of ligands for peroxisome proliferator-activated receptors (PPAR). Toxicol Sci 90: 269-295.
9. Nesto RW, Bell D, Bonow RO, Fonseca V, Grundy SM, et al. (2003) Thiazolidinedione use, fluid retention, and congestive heart failure: a consensus statement from the American Heart Association and American Diabetes Association. October 7, 2003. Circulation 108: 2941-2948. (Pubitemid 37517824)
10. Berger JP, Petro AE, Macnaul KL, Kelly LJ, Zhang BB, et al. (2003) Distinct properties and advantages of a novel peroxisome proliferator-activated protein [gamma] selective modulator. Mol Endocrinol 17: 662-676. (Pubitemid 36403578)
11. Acton JJ 3rd, Black RM, Jones AB, Moller DE, Colwell L, et al. (2005) Benzoyl 2-methyl indoles as selective PPARgamma modulators. Bioorg Med Chem Lett 15: 357-362. (Pubitemid 39647150)
12. Chang CH, McNamara LA, Wu MS, Muise ES, Tan Y, et al. (2008) A novel selective peroxisome proliferator-activator receptor-gamma modulator-SPPAR- gammaM5 improves insulin sensitivity with diminished adverse cardiovascular effects. Eur J Pharmacol 584: 192-201.
13. Motani A, Wang Z, Weiszmann J, McGee LR, Lee G, et al. (2009) INT131: a selective modulator of PPAR gamma. J Mol Biol 386: 1301-1311.
14. Acton JJ 3rd, Akiyama TE, Chang CH, Colwell L, Debenham S, et al. (2009) Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoro- methoxy)-1H-indol-1 -yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus with a reduced potential to increase plasma and extracellular fluid volume. J Med Chem 52: 3846-3854.
15. Guasch L, Sala E, Castell-Auvi A, Cedo L, Liedl KR, et al. (2012) Identification of PPARgamma Partial Agonists of Natural Origin (I): Development of a Virtual Screening Procedure and In Vitro Validation. PLoS One 7: e50816.
16. Castrillo A, Mojena M, Hortelano S, Bosca L (2001) Peroxisome proliferator-activated receptor-gamma-independent inhibition of macrophage activation by the non-thiazolidinedione agonist L-796,449. Comparison with the effects of 15-deoxy-delta(12,14)-prostaglandin J(2). J Biol Chem 276: 34082-34088.
17. Bassaganya-Riera J, Guri AJ, Lu P, Climent M, Carbo A, et al. (2011) Abscisic acid regulates inflammation via ligand-binding domain-independent activation of peroxisome proliferator-activated receptor gamma. J Biol Chem 286: 2504-2516.
18. Guri AJ, Hontecillas R, Si H, Liu D, Bassaganya-Riera J (2007) Dietary abscisic acid ameliorates glucose tolerance and obesity-related inflammation in db/db mice fed high-fat diets. Clin Nutr 26: 107-116. (Pubitemid 46179115)
19. Desai A, Konda VR, Darland G, Austin M, Prabhu KS, et al. (2009) META060 inhibits multiple kinases in the NF-kappaB pathway and suppresses LPS-mediated inflammation in vitro and ex vivo. Inflamm Res 58: 229-234.
20. Desai A, Darland G, Bland JS, Tripp ML, Konda VR (2012) META060 attenuates TNF-alpha-activated inflammation, endothelial-monocyte interactions, and matrix metalloproteinase-9 expression, and inhibits NF-kappaB and AP-1 in THP-1 monocytes. Atherosclerosis 223: 130-136.
21. Konda VR, Desai A, Darland G, Bland JS, Tripp ML (2010) META060 inhibits osteoclastogenesis and matrix metalloproteinases in vitro and reduces bone and cartilage degradation in a mouse model of rheumatoid arthritis. Arthritis Rheum 62: 1683-1692.
22. Vroegrijk IO, van Diepen JA, van den Berg SA, Romijn JA, Havekes LM, et al. (2013) META060 protects against diet-induced obesity and insulin resistance in a high-fat-diet fed mouse. Nutrition 29: 276-283.
23. Yajima H, Ikeshima E, Shiraki M, Kanaya T, Fujiwara D, et al. (2004) Isohumulones, bitter acids derived from hops, activate both peroxisome proliferator-activated receptor alpha and gamma and reduce insulin resistance. J Biol Chem 279: 33456-33462. (Pubitemid 39062995)
24. Everard A, Geurts L, Van Roye M, Delzenne NM, Cani PD (2012) Tetrahydro iso-alpha acids from hops improve glucose homeostasis and reduce body weight gain and metabolic endotoxemia in high-fat diet-fed mice. PLoS One 7: e33858.
25. Urban J, Dahlberg CJ, Carroll BJ, Kaminsky W (2013) Absolute Configuration of Beer's Bitter Compounds. Angew Chem Int Ed Engl 52: 1553-1555.
26. Babish JG, Pacioretty LM, Bland JS, Minich DM, Hu J, et al. (2010) Antidiabetic screening of commercial botanical products in 3T3-L1 adipocytes and db/db mice. J Med Food 13: 535-547.
27. Benson SC, Pershadsingh HA, Ho CI, Chittiboyina A, Desai P, et al. (2004) Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARgamma-modulating activity. Hypertension 43: 993-1002. (Pubitemid 38579904)
28. Pang T, Benicky J, Wang J, Orecna M, Sanchez-Lemus E, et al. (2012) Telmisartan ameliorates lipopolysaccharide-induced innate immune response through peroxisome proliferator-activated receptor-gamma activation in human monocytes. J Hypertens 30: 87-96.
29. Hirai S, Takahashi N, Goto T, Lin S, Uemura T, et al. (2010) Functional food targeting the regulation of obesity-induced inflammatory responses and pathologies. Mediators Inflamm 2010: 367838.
30. Kanda H, Tateya S, Tamori Y, Kotani K, Hiasa K, et al. (2006) MCP-1 contributes to macrophage infiltration into adipose tissue, insulin resistance, and hepatic steatosis in obesity. J Clin Invest 116: 1494-1505.
31. Weisberg SP, Hunter D, Huber R, Lemieux J, Slaymaker S, et al. (2006) CCR2 modulates inflammatory and metabolic effects of high-fat feeding. J Clin Invest 116: 115-124. (Pubitemid 43121796)
32. Nio Y, Yamauchi T, Iwabu M, Okada-Iwabu M, Funata M, et al. (2012) Monocyte chemoattractant protein-1 (MCP-1) deficiency enhances alternatively activated M2 macrophages and ameliorates insulin resistance and fatty liver in lipoatrophic diabetic A-ZIP transgenic mice. Diabetologia 55: 3350-3358.
33. Goldfine AB, Fonseca V, Jablonski KA, Pyle L, Staten MA, et al. (2010) The effects of salsalate on glycemic control in patients with type 2 diabetes: a randomized trial. Ann Intern Med 152: 346-357.
34. Ohshima K, Mogi M, Jing F, Iwanami J, Tsukuda K, et al. (2012) Direct angiotensin II type 2 receptor stimulation ameliorates insulin resistance in type 2 diabetes mice with PPARgamma activation. PLoS One 7: e48387.
35. Olivares-Reyes JA, Arellano-Plancarte A, Castillo-Hernandez JR (2009) Angiotensin II and the development of insulin resistance: implications for diabetes. Mol Cell Endocrinol 302: 128-139.
36. de Gasparo M, Catt KJ, Inagami T, Wright JW, Unger T (2000) International union of pharmacology. XXIII. The angiotensin II receptors. Pharmacol Rev 52: 415-472.
37. Tan Y, Muise ES, Dai H, Raubertas R, Wong KK, et al. (2012) Novel transcriptome profiling analyses demonstrate that selective peroxisome proliferator-activated receptor gamma (PPARgamma) modulators display attenuated and selective gene regulatory activity in comparison with PPARgamma full agonists. Mol Pharmacol 82: 68-79.