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Original Research

Early effects of roflumilast on insulin sensitivity in adults with prediabetes and overweight/obesity involve age-associated fat mass loss – results of an exploratory study

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Pages 743-759 | Published online: 27 May 2019

References

References

  • Dandona P Ghanim H Chaudhuri A Incretins: beyond type 2 diabetes Diabetes Obes Metab 2018 20 7349 59 67 29364583
  • FLAT-SUGAR Trial Investigators Glucose variability in A 26-week randomized comparison of mealtime treatment with rapid-acting insulin versus GLP-1 agonist in participants with type 2 diabetes at high cardiovascular risk Diabetes Care 2016 39 6 973 981 27208320
  • McNelis JC Olefsky JM Macrophages, immunity, and metabolic disease Immunity 2014 41 1 36 48 25035952
  • Houstis N Rosen ED Lander ES Reactive oxygen species have a causal role in multiple forms of insulin resistance Nature 2006 440 7086 944 948 16612386
  • Wong E Tanamas SK Wolfe R The role of obesity duration on the association between obesity and risk of physical disability Obesity 2015 23 2 443 447 25451850
  • Adams KF Schatzkin A Harris TB Overweight, obesity, and mortality in a large prospective cohort of persons 50 to 71 years old N Engl J Med 2006 355 8 763 778 16926275
  • Burkewitz K Zhang Y Mair WB AMPK at the nexus of energetics and aging Cell Metab 2014 20 1 10 25 24726383
  • Mottillo EP Desjardins EM Crane JD Lack of adipocyte AMPK exacerbates insulin resistance and hepatic steatosis through brown and beige adipose tissue function Cell Metab 2016 24 1 118 129 27411013
  • Mancini SJ White AD Bijland S Activation of AMP-activated protein kinase rapidly suppresses multiple pro-inflammatory pathways in adipocytes including IL-1 receptor-associated kinase-4 phosphorylation Mol Cell Endocrinol 2017 440 44 56 27840174
  • Meng W Liang X Chen H Rheb inhibits beiging of white adipose tissue via PDE4D5-dependent downregulation of the cAMP-PKA signaling pathway Diabetes 2017 66 5 1198 1213 28242620
  • Park SJ Ahmad F Philp A Resveratrol ameliorates aging-related metabolic phenotypes by inhibiting cAMP phosphodiesterases Cell 2012 148 3 421 433 22304913
  • Wang P Zhang RY Song J Loss of AMP-activated protein kinase-α2 impairs the insulin-sensitizing effect of calorie restriction in skeletal muscle Diabetes 2012 61 5 1051 1061 22396207
  • Sylow L Møller LLV Kleinert M Rac1 and AMPK account for the majority of muscle glucose uptake stimulated by ex vivo contraction but not in vivo exercise Diabetes 2017 66 6 1548 1559 28389470
  • Xu XJ Gauthier MS Hess DT Insulin sensitive and resistant obesity in humans: AMPK activity, oxidative stress, and depot-specific changes in gene expression in adipose tissue J Lipid Res 2012 53 4 792 801 22323564
  • Xu XJ Apovian C Hess D Carmine B Saha A Ruderman N Improved insulin sensitivity 3 months after RYGB surgery is associated with increased subcutaneous adipose tissue AMPK activity and decreased oxidative stress Diabetes 2015 64 9 3155 3159 26001396
  • Rogliani P Calzetta L Cazzola M Matera MG Drug safety evaluation of roflumilast for the treatment of COPD: a meta-analysis Expert Opin Drug Saf 2016 15 8 1133 1146 27279341
  • Keating GM Apremilast: a review in psoriasis and psoriatic arthritis Drugs 2017 77 4 459 472 28213862
  • Fabbri LM Calverley PMA Izquierdo-Alonso JL Roflumilast in moderate-to-severe chronic obstructive pulmonary disease treated with longacting bronchodilators: two randomised clinical trials Lancet 2009 374 9691 695 703 19716961
  • Tannheimer SL Wright CD Salmon M Combination of roflumilast with a beta-2 adrenergic receptor agonist inhibits proinflammatory and profibrotic mediator release from human lung fibroblasts Respir Res 2012 13 1 28 22452977
  • Jensterle M Kocjan T Janez A Phosphodiesterase 4 inhibition as a potential new therapeutic target in obese women with polycystic ovary syndrome J Clin Endocrinol Metab 2014 99 8 E1476 E1481 24823465
  • Jensterle M Salamun V Kocjan T Vrtacnik Bokal E Janez A Short term monotherapy with GLP-1 receptor agonist liraglutide or PDE 4 inhibitor roflumilast is superior to metformin in weight loss in obese PCOS women: a pilot randomized study J Ovarian Res 2015 8 1 32 26032655
  • Wouters EF Bredenbröker D Teichmann P Effect of the phos-phodiesterase 4 inhibitor roflumilast on glucose metabolism in patients with treatment-naive, newly diagnosed type 2 diabetes mellitus J Clin Endocrinol Metab 2012 97 9 E1720 E1725 22723325
  • Azevedo MF Faucz FR Bimpaki E Clinical and molecular genetics of the phosphodiesterases (PDEs) Endocr Rev 2014 35 2 195 233 24311737
  • Engels P Fichtel K Lübbert H Expression and regulation of human and rat phosphodiesterase type IV isogenes FEBS Lett 1994 350 2–3 291 295 8070581
  • Kenk M Greene M Thackeray J In vivo selective binding of (R)-[11C]rolipram to phosphodiesterase-4 provides the basis for studying intracellular cAMP signaling in the myocardium and other peripheral tissues Nucl Med Biol 2007 34 1 71 77 17210463
  • Nakamura J Okamura N Kawakami Y Augmentation of lipolysis in adipocytes from fed rats, but not from starved rats, by inhibition of rolipram-sensitive phosphodiesterase 4 Arch Biochem Biophys 2004 425 1 106 114 15081899
  • Omar B Banke E Ekelund M Frederiksen S Degerman E Alterations in cyclic nucleotide phosphodiesterase activities in omental and subcutaneous adipose tissues in human obesity Nutr Diabetes 2011 1 8 e13 23449489
  • Enoksson S Degerman E Hagström-Toft E Large V Arner P Various phosphodiesterase subtypes mediate the in vivo antilipolytic effect of insulin on adipose tissue and skeletal muscle in man Diabetologia 1998 41 5 560 568 9628274
  • Waddleton D Wu W Feng Y Phosphodiesterase 3 and 4 comprise the major cAMP metabolizing enzymes responsible for insulin secretion in INS-1 (832/13) cells and rat islets Biochem Pharmacol 2008 76 7 884 893 18706893
  • Friedlander RS Moss CE Mace J Role of phosphodiesterase and adenylate cyclase isozymes in murine colonic glucagon-like peptide 1 secreting cells Br J Pharmacol 2011 163 2 261 271 21054345
  • Roflumilast medication information https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022522s000lbl.pdf Accessed February 10, 2017
  • First MB Spitzer RL Gibbon M Williams JBW Structured Clinical Interview for DSM-IV Axis 1Disorders Washington, DC, USA American Psychiatric Press, Inc 1996
  • Possner K Brown GK Stanley B The Columbia-suicide severity rating scale: internal validity and internal consistency findings from three multi-site studies with adolescents and adults Am J Psychiatry 2011 168 12 1266 1277 22193671
  • Mifflin MD St Jeor ST Hill LA Scott BJ Daugherty SA Koh YO A new predictive equation for resting energy expenditure in healthy individuals Am J Clin Nutr 1990 51 2 241 247 2305711
  • Institute of Medicine Dietary Reference Intakes: The Essential Guide to Nutrient Requirements Washington, DC The National Academies Press 2006
  • Defronzo RA Tobin JD Andres R Glucose clamp technique: a method for quantifying insulin secretion and resistance Am J Physiol 1979 237 3 E214 E223 382871
  • Muniyappa R Noureldin R Ouwerkerk R Myocardial fat accumulation is independent of measures of insulin sensitivity J Clin Endocrinol Metab 2015 100 8 3060 3068 26020762
  • Ouwerkerk R Pettigrew RI Gharib AM Liver metabolite concentrations measured with 1H MR spectroscopy Radiology 2012 265 2 565 575 22891360
  • Magkos F Fabbrini E Korenblat K Okunade AL Patterson BW Klein S Reproducibility of glucose, fatty acid and VLDL kinetics and multi-organ insulin sensitivity in obese subjects with non-alcoholic fatty liver disease Int J Obes 2011 35 9 1233 1240
  • Zornitzki T Blaychfeld-Magnazi M Knobler H Ulman M The effect of phlebotomy-induced hemolysis on insulin level determination Endocr Pract 2015 21 10 1093 1097 26121452
  • White WB Cooke GE Kowey PR Cardiovascular safety in patients receiving roflumilast for the treatment of COPD Chest 2013 144 3 758 765 23412642
  • Vollert S Kaessner N Heuser A The glucose-lowering effects of the PDE4 inhibitors roflumilast and roflumilast-N-oxide in db/db mice Diabetologia 2012 55 10 2779 2788 22790061
  • Ong WK Gribble FM Reimann F The role of the PDE4D cAMP phosphodiesterase in the regulation of glucagon-like peptide-1 release Br J Pharmacol 2009 157 4 633 644 19371330
  • Meier JJ Gethmann A Götze O Glucagon-like peptide 1 abolishes the postprandial rise in triglyceride concentrations and lowers levels of non-esterified fatty acids in humans Diabetologia 2006 49 3 452 458 16447057
  • Hermansen K Bækdal TA Düring M Liraglutide suppresses postprandial triglyceride and apolipoprotein B48 elevations after a fat-rich meal in patients with type 2 diabetes: a randomized, double-blind, placebo-controlled, cross-over trial Diabetes Obes Metab 2013 15 11 1040 1048 23683069
  • Bachmann OP Dahl DB Brechtel K Effects of intravenous and dietary lipid challenge on intramyocellular lipid content and the relation with insulin sensitivity in humans Diabetes 2001 50 11 2579 2584 11679437
  • Lara-Castro C Newcomer BR Rowell J Effects of short-term very low-calorie diet on intramyocellular lipid and insulin sensitivity in nondiabetic and type 2 diabetic subjects Metabolism 2008 57 1 1 8 18078853
  • Möllmann J Kahles F Lebherz C The PDE4 inhibitor roflumilast reduces weight gain by increasing energy expenditure and leads to improved glucose metabolism Diabetes Obes Metab 2017 19 4 496 508 27917591
  • Chai W Dong Z Wang N Glucagon-like peptide 1 recruits microvasculature and increases glucose use in muscle via a nitric oxide-dependent mechanism Diabetes 2012 61 4 888 896 22357961
  • Ohnuki Y Umeki D Mototani Y Role of phosphodiesterase 4 expression in the Epac1 signaling-dependent skeletal muscle hyper-trophic action of clenbuterol Physiol Rep 2016 4 10 e12791 27207782
  • Hodson DJ Mitchell RK Bellomo EA Lipotoxicity disrupts incretin-regulated human β cell connectivity J. Clin. Invest 2013 123 10 4182 4194 24018562
  • Pérez-Torres S Miró X Palacios JM Cortés R Puigdoménech P Mengod G Phosphodiesterase type 4 isozymes expression in human brain examined by in situ hybridization histochemistry and [3H]rolipram binding autoradiography. Comparison with monkey and rat brain J Chem Neuroanat 2000 20 3–4 349 374 11207431
  • Lönnqvist F Nyberg B Wahrenberg H Arner P Catecholamine-induced lipolysis in adipose tissue of the elderly J Clin Invest 1990 85 5 1614 1621 2159025
  • Camell CD Sander J Spadaro O Inflammasome-driven catechol-amine catabolism in macrophages blunts lipolysis during ageing Nature 2017 27 7674 119 123
  • Franceschi C Garagnani P Parini P Giuliani C Santoro A Inflammaging: a new immune–metabolic viewpoint for age-related diseases Nat Rev Endocrinol 2018 14 10 576 590 30046148
  • Brechtel K Dahl DB Machann J Fast elevation of the intra-myocellular lipid content in the presence of circulating free fatty acids and hyperinsulinemia: a dynamic 1H-MRS study Magn Reson Med 2001 45 2 179 183 11180422
  • Byrne MM Gliem K Wank U Glucagon-like peptide 1 improves the ability of the beta-cell to sense and respond to glucose in subjects with impaired glucose tolerance Diabetes 1998 47 8 1259 1265 9703326
  • Santilli F Simeone PG Guagnano MT Effects of liraglutide on weight loss, fat distribution, and β-cell function in obese subjects with pre-diabetes or early type 2 diabetes Diabetes Care 2017 40 11 1556 1564 28912305
  • Sanz MJ Cortijo J Taha MA Roflumilast inhibits leukocyteendothelial cell interactions, expression of adhesion molecules and microvascular permeability Br J Pharmacol 2007 152 4 481 492 17704822
  • Chou HH Hsu LA Wu S Teng MS Sun YC Ko YL Leptin-to-Adiponectin ratio is related to low grade inflammation and insulin resistance independent of obesity in non-diabetic Taiwanese: a cross-sectional cohort study Acta Cardiol Sin 2014 30 3 204 214 27122790
  • Frühbeck G Catalán V Rodríguez A Normalization of adiponectin concentrations by leptin replacement in ob/ob mice is accompanied by reductions in systemic oxidative stress and inflammation Sci Rep 2017 7 1 2752 28584304
  • Barreiro E Puig-Vilanova E Salazar-Degracia A Pascual-Guardia S Casadevall C Gea J The phosphodiesterase-4 inhibitor roflumilast reverts proteolysis in skeletal muscle cells of patients with COPD cachexia J Appl Physiol 2018 125 2 287 303 29648516
  • Ruscica M Ferri N Macchi C Corsini A Sirtori CR Lipid lowering drugs and inflammatory changes: an impact on cardiovascular outcomes? Ann Med 2018 32 1 1 24
  • Burkewitz K Zhang Y Mair WB AMPK at the nexus of energetics and aging Cell Metab 2014 20 1 10 25 24726383