Dosing profile profoundly influences nicotinic acid's ability to improve metabolic control in rats

Journal of Lipid Research

Volumn 56, Issue 9, 2015, Pages 1679-1690

  Kroon, Tobias ^a,b   Kjellstedt, Ann ^a   Thalén, Pia ^a   Gabrielsson, Johan ^b   Oakes, Nicholas D ^a  

^a ASTRAZENECA R AND D   (Sweden)

^b SWEDISH UNIVERSITY OF AGRICULTURAL SCIENCES   (Sweden)

Author keywords

Adipose tissue; Diabetes; Drug therapy hypolipidemic drugs; GPR109A; Insulin; Lipolysis and fatty acid metabolism; Niacin; Tachyphylaxis

Indexed keywords

FATTY ACID; NICOTINIC ACID; SODIUM CHLORIDE; GLUCOSE; INSULIN; MESSENGER RNA; TRIACYLGLYCEROL;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTINUOUS INFUSION; CONTROLLED STUDY; DRUG ACTIVITY; DRUG EXPOSURE; DRUG INTERMITTENT THERAPY; DRUG TOLERANCE; FATTY ACID BLOOD LEVEL; GLUCOSE CLAMP TECHNIQUE; GLUCOSE INFUSION; INSULIN RESISTANCE; INSULIN SENSITIVITY; LEAN BODY WEIGHT; METABOLIC REGULATION; MINIPUMP; NONHUMAN; OBESITY; PRIORITY JOURNAL; RAT; TREATMENT DURATION; ADIPOSE TISSUE; ANIMAL; BIOSYNTHESIS; DOSE RESPONSE; DRUG EFFECTS; GENETICS; LIPID METABOLISM; LIPOLYSIS; METABOLISM;

ADIPOSE TISSUE; ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; FATTY ACIDS, NONESTERIFIED; GLUCOSE; INSULIN; INSULIN RESISTANCE; LIPID METABOLISM; LIPOLYSIS; NIACIN; OBESITY; RATS; RNA, MESSENGER; TRIGLYCERIDES;

EID: 84940989761     PISSN: 00222275     EISSN: 15397262     Source Type: Journal    
DOI: 10.1194/jlr.M058149     Document Type: Article

References (47)

1. Morita, S., Y. Shimajiri, S. Sakagashira, M. Furuta, and T. Sanke. 2012. Effect of exposure to non-esterified fatty acid on progressive deterioration of insulin secretion in patients with type 2 diabetes: a long-term follow-up study. Diabet. Med. 29: 980-985.
2. Krauss, R. M. 2004. Lipids and lipoproteins in patients with type 2 diabetes. Diabetes Care. 27: 1496-1504.
3. Eckel, R. H., S. M. Grundy, and P. Z. Zimmet. 2005. The metabolic syndrome. Lancet. 365: 1415-1428.
4. Kraegen, E. W., and G. J. Cooney. 2008. Free fatty acids and skeletal muscle insulin resistance. Curr. Opin. Lipidol. 19: 235-241.
5. Girousse, A., G. Tavernier, C. Valle, C. Moro, N. Mejhert, A. L. Dinel, M. Houssier, B. Roussel, A. Besse-Patin, M. Combes, et al. 2013. Partial inhibition of adipose tissue lipolysis improves glucose metabolism and insulin sensitivity without alteration of fat mass. PLoS Biol. 11: e1001485.
6. Claus, T. H., D. B. Lowe, Y. Liang, A. I. Salhanick, C. K. Lubeski, L. Yang, L. Lemoine, J. Zhu, and K. B. Clairmont. 2005. Specific inhibition of hormone-sensitive lipase improves lipid profile while reducing plasma glucose. J. Pharmacol. Exp. Ther. 315: 1396-1402.
7. Dhalla, A. K., M. Y. Wong, P. J. Voshol, L. Belardinelli, and G. M. Reaven. 2007. A1 adenosine receptor partial agonist lowers plasma FFA and improves insulin resistance induced by high-fat diet in rodents. Am. J. Physiol. Endocrinol. Metab. 292: E1358-E1363.
8. Ge, H., X. Li, J. Weiszmann, P. Wang, H. Baribault, J. Chen, H. Tian, and Y. Li. 2008. Activation of G protein-coupled receptor 43 in adipocytes leads to inhibition of lipolysis and suppression of plasma free fatty acids. Endocrinology. 149: 4519-4526.
9. Sakurai, T., R. Davenport, S. Stafford, J. Grosse, K. Ogawa, J. Cameron, L. Parton, A. Sykes, S. Mack, S. Bousba, et al. 2014. Identification of a novel GPR81-selective agonist that suppresses lipolysis in mice without cutaneous flushing. Eur. J. Pharmacol. 727: 1-7.
10. Offermanns, S. 2014. Free fatty acid (FFA) and hydroxy carboxylic acid (HCA) receptors. Annu. Rev. Pharmacol. Toxicol. 54: 407-434.
11. Altschul, R., A. Hoffer, and J. D. Stephen. 1955. Influence of nicotinic acid on serum cholesterol in man. Arch. Biochem. Biophys. 54: 558-559.
12. Parsons, W. B., Jr, R. W. Achor, K. G. Berge, B. F. Mckenzie, and N. W. Barker. 1956. Changes in concentration of blood lipids following prolonged administration of large doses of nicotinic acid to persons with hypercholesterolemia: preliminary observations. Proc. Staff Meet. Mayo Clin. 31: 377-390.
13. Parsons, W. B., Jr, and J. H. Flinn. 1959. Reduction of serum cholesterol levels and beta-lipoprotein cholesterol levels by nicotinic acid. Am. Med. Assoc. Arch. Intern. Med. 103: 783-790.
14. Carlson, L. A., and L. Oro. 1962. The effect of nicotinic acid on the plasma free fatty acid; demonstration of a metabolic type of sympathicolysis. Acta Med. Scand. 172: 641-645.
15. Carlson, L. A. 1963. Studies on the effect of nicotinic acid on catecholamine stimulated lipolysis in adipose tissue in vitro. Acta Med. Scand. 173: 719-722.
16. Phan, B. A. P., L. Muñoz, P. Shadzi, D. Isquith, M. Triller, B. G. Brown, and X. Zhao. 2013. Effects of niacin on glucose levels, coronary stenosis progression, and clinical events in subjects with normal baseline glucose levels (<100 mg/dl): a combined analysis of the Familial Atherosclerosis Treatment Study (FATS), HDL-Atherosclerosis Treatment Study (HATS), Armed Forces Regression Study (AFREGS), and Carotid Plaque Composition by MRI during lipid-lowering (CPC) study. Am. J. Cardiol. 111: 352-355.
17. Guyton, J. R., S. Fazio, A. J. Adewale, E. Jensen, J. E. Tomassini, A. Shah, and A. M. Tershakovec. 2012. Effect of extended-release niacin on new-onset diabetes among hyperlipidemic patients treated with ezetimibe/simvastatin in a randomized controlled trial. Diabetes Care. 35: 857-860.
18. Grundy, S. M., G. L. Vega, M. E. McGovern, B. R. Tulloch, D. M. Kendall, D. Fitz-Patrick, O. P. Ganda, R. S. Rosenson, J. B. Buse, D. D. Robertson, et al. 2002. Efficacy, safety, and tolerability of once-daily niacin for the treatment of dyslipidemia associated with type 2 diabetes: results of the assessment of diabetes control and evaluation of the efficacy of Niaspan trial. Arch. Intern. Med. 162: 1568-1576.
19. Elam, M. B., D. B. Hunninghake, K. B. Davis, R. Garg, C. Johnson, D. Egan, J. B. Kostis, D. S. Sheps, and E. A. Brinton. 2000. Effect of niacin on lipid and lipoprotein levels and glycemic control in patients with diabetes and peripheral arterial disease: the ADMIT study: a randomized trial. J. Am. Med. Assoc. 284: 1263-1270.
20. Oh, Y. T., K. S. Oh, Y. M. Choi, A. Jokiaho, C. Donovan, S. Choi, I. Kang, and J. H. Youn. 2011. Continuous 24-h nicotinic acid infusion in rats causes FFA rebound and insulin resistance by altering gene expression and basal lipolysis in adipose tissue. Am. J. Physiol. Endocrinol. Metab. 300: E1012-E1021.
21. Vaag, A. A., and H. Beck-Nielsen. 1992. Effects of prolonged Acipimox treatment on glucose and lipid metabolism and on in vivo insulin sensitivity in patients with non-insulin dependent diabetes mellitus. Acta Endocrinol. (Copenh.). 127: 344-350.
22. Worm, D., J. E. Henriksen, A. Vaag, P. Thye-Ronn, A. Melander, and H. Beck-Nielsen. 1994. Pronounced blood glucose-lowering effect of the antilipolytic drug acipimox in noninsulin-dependent diabetes mellitus patients during a 3-day intensified treatment period. J. Clin. Endocrinol. Metab. 78: 717-721.
23. Carlson, L. A., L. Oro, and J. Ostman. 1968. Effect of a single dose of nicotinic acid on plasma lipids in patients with hyperlipoproteinemia. Acta Med. Scand. 183: 457-465.
24. Miettinen, T. A., M. R. Taskinen, R. Pelkonen, and E. A. Nikkila. 1969. Glucose tolerance and plasma insulin in man during acute and chronic administration of nicotinic acid. Acta Med. Scand. 186: 247-253.
25. Poynten, A. M., S. Khee Gan, A. D. Kriketos, A. O'Sullivan, J. J. Kelly, B. A. Ellis, D. J. Chisholm, and L. V. Campbell. 2003. Nicotinic acid-induced insulin resistance is related to increased circulating fatty acids and fat oxidation but not muscle lipid content. Metabolism. 52: 699-704.
26. Ahlström, C., T. Kroon, L. A. Peletier, and J. Gabrielsson. 2013. Feedback modeling of non-esterified fatty acids in obese Zucker rats after nicotinic acid infusions. J. Pharmacokinet. Pharmacodyn. 40: 623-638.
27. Oakes, N. D., P. Thalen, T. Hultstrand, S. Jacinto, G. Camejo, B. Wallin, and B. Ljung. 2005. Tesaglitazar, a dual PPAR{alpha}/{gamma} agonist, ameliorates glucose and lipid intolerance in obese Zucker rats. Am. J. Physiol. Regul. Integr. Comp. Physiol. 289: R938-R946.
28. Wallenius, K., A. Kjellstedt, P. Thalen, L. Lofgren, and N. D. Oakes. 2013. The PPARα/γ agonist, tesaglitazar, improves insulin mediated switching of tissue glucose and free fatty acid utilization in vivo in the obese Zucker rat. PPAR Res. 2013: 305347.
29. Gabrielsson, J., and A. R. Green. 2009. Quantitative pharmacology or pharmacokinetic pharmacodynamic integration should be a vital component in integrative pharmacology. J. Pharmacol. Exp. Ther. 331: 767-774.
30. Li, G., Q. Zhou, Y. Yu, L. Chen, Y. Shi, J. Luo, J. Benovic, J. Lu, and N. Zhou. 2012. Identification and characterization of distinct C-terminal domains of the human hydroxycarboxylic acid receptor-2 that are essential for receptor export, constitutive activity, desensitization, and internalization. Mol. Pharmacol. 82: 1150-1161.
31. Oakes, N. D., A. Kjellstedt, P. Thalén, B. Ljung, and N. Turner. 2013. Roles of fatty acid oversupply and impaired oxidation in lipid accumulation in tissues of obese rats. J. Lipids. 2013: 420754.
32. Li, H. M., M. Zhang, S. T. Xu, D. Z. Li, L. Y. Zhu, S. W. Peng, G. Q. Chen, P. M. Martin, V. Ganapathy, and C. J. Wei. 2011. Nicotinic acid inhibits glucose-stimulated insulin secretion via the G protein-coupled receptor PUMA-G in murine islet β cells. Pancreas. 40: 615-621.
33. Dobbins, R. L., M. W. Chester, M. B. Daniels, J. D. McGarry, and D. T. Stein. 1998. Circulating fatty acids are essential for efficient glucose-stimulated insulin secretion after prolonged fasting in humans. Diabetes. 47: 1613-1618.
34. Oakes, N. D., G. J. Cooney, S. Camilleri, D. J. Chisholm, and E. W. Kraegen. 1997. Mechanisms of liver and muscle insulin resistance induced by chronic high-fat feeding. Diabetes. 46: 1768-1774.
35. Ruderman, N. B., C. J. Toews, and E. Shafrir. 1969. Role of free fatty acids in glucose homeostasis. Arch. Intern. Med. 123: 299-313.
36. Digby, J. E., F. Martinez, A. Jefferson, N. Ruparelia, J. Chai, M. Wamil, D. R. Greaves, and R. P. Choudhury. 2012. Anti-inflammatory effects of nicotinic acid in human monocytes are mediated by GPR109A dependent mechanisms. Arterioscler. Thromb. Vasc. Biol. 32: 669-676.
37. Hara, N., K. Yamada, T. Shibata, H. Osago, T. Hashimoto, and M. Tsuchiya. 2007. Elevation of cellular NAD levels by nicotinic acid and involvement of nicotinic acid phosphoribosyltransferase in human cells. J. Biol. Chem. 282: 24574-24582.
38. Wang, W., A. Basinger, R. A. Neese, M. Christiansen, and M. K. Hellerstein. 2000. Effects of nicotinic acid on fatty acid kinetics, fuel selection, and pathways of glucose production in women. Am. J. Physiol. Endocrinol. Metab. 279: E50-E59.
39. Daniele, G., R. Eldor, A. Merovci, G. D. Clarke, J. Xiong, D. Tripathy, A. Taranova, M. Abdul-Ghani, and R. A. DeFronzo. 2014. Chronic reduction of plasma free fatty acid improves mitochondrial function and whole-body insulin sensitivity in obese and type 2 diabetic individuals. Diabetes. 63: 2812-2820.
40. McCulloch, D. K., S. E. Kahn, M. W. Schwartz, D. J. Koerker, and J. P. Palmer. 1991. Effect of nicotinic acid-induced insulin resistance on pancreatic B cell function in normal and streptozocin-treated baboons. J. Clin. Invest. 87: 1395-1401.
41. Heemskerk, M. M., S. A. van den Berg, A. C. Pronk, J. B. van Klinken, M. R. Boon, L. M. Havekes, P. C. Rensen, K. W. van Dijk, and V. van Harmelen. 2014. Long-term niacin treatment induces insulin resistance and adrenergic responsiveness in adipocytes by adaptive downregulation of phosphodiesterase 3B. Am. J. Physiol. Endocrinol. Metab. 306: E808-E813.
42. Vega, G. L., N. B. Cater, S. Meguro, and S. M. Grundy. 2005. Influence of extended-release nicotinic acid on nonesterified fatty acid flux in the metabolic syndrome with atherogenic dyslipidemia. Am. J. Cardiol. 95: 1309-1313.
43. Quabbe, H. J., A. S. Luyckx, M. L'age, and C. Schwarz. 1983. Growth hormone, cortisol, and glucagon concentrations during plasma free fatty acid depression: different effects of nicotinic acid and an adenosine derivative (BM 11.189). J. Clin. Endocrinol. Metab. 57: 410-414.
44. Usman, M. H., A. Qamar, R. Gadi, S. Lilly, H. Goel, J. Hampson, M. L. Mucksavage, G. A. Nathanson, D. J. Rader, and R. L. Dunbar. 2012. Extended-release niacin acutely suppresses postprandial triglyceridemia. Am. J. Med. 125: 1026-1035.
45. Rajanna, V., K. B. Campbell, J. Leimberger, B. D. Mohanty, and J. R. Guyton. 2012. Elevation of fasting morning glucose relative to hemoglobin A1c in normoglycemic patients treated with niacin and with statins. J. Clin. Lipidol. 6: 168-173.
46. Lauring, B., A. K. Taggart, J. R. Tata, R. Dunbar, L. Caro, K. Cheng, J. Chin, S. L. Colletti, J. Cote, S. Khalilieh, et al. 2012. Niacin lipid efficacy is independent of both the niacin receptor GPR109A and free fatty acid suppression. Sci. Transl. Med. 4: 148ra115.
47. Kesisoglou, F., S. Rossenu, C. Farrell, M. Van Den Heuvel, M. Prohn, S. Fitzpatrick, P. J. De Kam, and R. Vargo. 2014. Development of in vitro-in vivo correlation for extended-release niacin after administration of hypromellose-based matrix formulations to healthy volunteers. J. Pharm. Sci. 103: 3713-3723.