Skip to main content

Niacin: Vitamin and Antidyslipidemic Drug

  • Chapter
  • First Online:
Water Soluble Vitamins

Part of the book series: Subcellular Biochemistry ((SCBI,volume 56))

Abstract

Niacin is defined collectively as nicotinamide and nicotinic acid, both of which fulfill the vitamin functions of niacin carried out by the bioactive forms NAD(P). In the last few decades numerous new enzymes that consume NAD(P) as substrates have been identified. The functions of these enzymes are emerging as exciting paradigm shifts, even though they are in early stages of discovery. The recent identification of the nicotinic acid receptor has allowed distinction of the drug-like roles of nicotinic acid from its vitamin functions, specifically in modulating blood lipid levels and undesirable side effects such as skin vasodilation and the more rare hepatic toxicities. This information has led to a new strategy for drug delivery for niacin, which, if successful, could have a major impact on human health through decreasing risk for cardiovascular disease. Understanding the many other effects of niacin has much broader potential for disease intervention and treatment in numerous diseases including cancer.

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 179.00
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 229.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book
USD 249.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

References

  • Aktories K, Jakobs KH, Schultz G (1980) Nicotinic acid inhibits adipocyte adenylate cyclase in a hormone – like manner. FEBS Lett 115:11–14

    Article  PubMed  CAS  Google Scholar 

  • Chinetti-Gbaguidi G, Rigamonti E, Helin L, Mutka AL, Lepore M, Fruchart JC, Clavey V, Ikonen E, Lestavel S, Staels B (2005) Peroxisome proliferator-activated receptor alpha controls cellular cholesterol trafficking in macrophages. J Lipid Res 46:2717–2725

    Article  PubMed  CAS  Google Scholar 

  • Elvehjem CA, Madden RJ, Strong FM, Woolley DW (1938) The isolation and identification of the anti-black tongue factor. J Biol Chem 123:137–149

    CAS  Google Scholar 

  • Fruchart JC, Duriez P, Staels B (1999) Peroxisome proliferator-activated receptor-alpha activators regulate genes governing lipoprotein metabolism, vascular inflammation and atherosclerosis. Curr Opin Lipidol 10:245–257

    Article  PubMed  CAS  Google Scholar 

  • Fu CS, Swendseid ME, Jacob RA, McKee RW (1989) Biochemical markers for assessment of niacin status in young men: levels of erythrocyte niacin coenzymes and plasma tryptophan. J Nutr 119:1949–1955

    PubMed  CAS  Google Scholar 

  • Haigis MC, Mostoslavsky R, Haigis KM, Fahie K, Christodoulou DC, Murphy AJ, Valenzuela DM, Yancopoulos GD, Karow M, Blander G, Wolberger C, Prolla TA, Weindruch R, Alt FW, Guarente L (2006) SIRT4 inhibits glutamate dehydrogenase and opposes the effects of calorie restriction in pancreatic beta cells. Cell 126:941–954

    Article  PubMed  CAS  Google Scholar 

  • Hassa PO, Haenni SS, Elser M, Hottiger MO (2006) Nuclear ADP-ribosylation reactions in mammalian cells: where are we today and where are we going? Microbiol Mol Biol Rev 70:789–829

    Article  PubMed  CAS  Google Scholar 

  • Kim H, Jacobson EL, Jacobson MK, Lacko AG (2004) Apoa-1 milano and regression of atherosclerosis. JAMA 291:1319

    Article  PubMed  CAS  Google Scholar 

  • Kontush A, Chantepie S, Chapman MJ (2003) Small, dense HDL particles exert potent protection of atherogenic LDL against oxidative stress. Arterioscler Thromb Vasc Biol 23:1881–1888

    Article  PubMed  CAS  Google Scholar 

  • LaRosa JH, LaRosa JC (2000) Enhancing drug compliance in lipid-lowering treatment. Arch Fam Med 9:1169–1175

    Article  PubMed  CAS  Google Scholar 

  • Lee Y, Yu X, Gonzales F, Mangelsdorf DJ, Wang MY, Richardson C, Witters LA, Unger RH (2002) PPAR alpha is necessary for the lipopenic action of hyperleptinemia on white adipose and liver tissue. Proc Natl Acad Sci USA 99:11848–11853

    Article  PubMed  CAS  Google Scholar 

  • Lundasen T, Liao W, Angelin B, Rudling M (2003) Leptin induces the hepatic high density lipoprotein receptor scavenger receptor B type I (SR-BI) but not cholesterol 7alpha-hydroxylase (cyp7a1) in leptin-deficient (ob/ob) mice. J Biol Chem 278:43224–43228

    Article  PubMed  CAS  Google Scholar 

  • Morgan JM, Capuzzi DM, Baksh RI, Intenzo C, Carey CM, Reese D, Walker K (2003) Effects of extended-release niacin on lipoprotein subclass distribution. Am J Cardiol 91:1432–1436

    Article  PubMed  CAS  Google Scholar 

  • Myers MG Jr (2004) Leptin receptor signaling and the regulation of mammalian physiology. Recent Prog Horm Res 59:287–304

    Article  PubMed  CAS  Google Scholar 

  • Nissen SE, Tsunoda T, Tuzcu EM, Schoenhagen P, Cooper CJ, Yasin M, Eaton GM, Lauer MA, Sheldon WS, Grines CL, Halpern S, Crowe T, Blankenship JC, Kerensky R (2003) Effect of recombinant apoA-I milano on coronary atherosclerosis in patients with acute coronary syndromes: a randomized controlled trial. JAMA 290:2292–2300

    Article  PubMed  CAS  Google Scholar 

  • Offermanns S (2006) The nicotinic acid receptor GPR109A (HM74A or PUMA-G) as a new therapeutic target. Trends Pharmacol Sci 27:384–390

    Article  PubMed  CAS  Google Scholar 

  • Sasaki J, Yamamoto K, Ageta M (2002) Effects of fenofibrate on high-density lipoprotein particle size in patients with hyperlipidemia: a randomized, double-blind, placebo-controlled, multicenter, crossover study. Clin Ther 24:1614–1626

    Article  PubMed  CAS  Google Scholar 

  • Soga T, Kamohara M, Takasaki J, Matsumoto S, Saito T, Ohishi T, Hiyama H, Matsuo A, Matsushime H, Furuichi K (2003) Molecular identification of nicotinic acid receptor. Biochem Biophys Res Commun 303:364–369

    Article  PubMed  CAS  Google Scholar 

  • Syvanne M, Nieminen MS, Frick MH, Kauma H, Majahalme S, Virtanen V, Kesaniemi YA, Pasternack A, Ehnholm C, Taskinen MR (1998) Associations between lipoproteins and the progression of coronary and vein-graft atherosclerosis in a controlled trial with gemfibrozil in men with low baseline levels of HDL cholesterol. Circulation 98:1993–1999

    PubMed  CAS  Google Scholar 

  • Tunaru S, Kero J, Schaub A, Wufka C, Blaukat A, Pfeffer K, Offermanns S (2003) PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect. Nat Med 9:352–355

    Article  PubMed  CAS  Google Scholar 

  • Wise A, Foord SM, Fraser NJ, Barnes AA, Elshourbagy N, Eilert M, Ignar DM, Murdock PR, Steplewski K, Green A, Brown AJ, Dowell SJ, Szekeres PG, Hassall DG, Marshall FH, Wilson S, Pike NB (2003) Molecular identification of high and low affinity receptors for nicotinic acid. J Biol Chem 278:9869–9874

    Article  PubMed  CAS  Google Scholar 

  • Yoshikawa M, Sakuma N, Hibino T, Sato T, Fujinami T (1997) HDL3 exerts more powerful anti-oxidative, protective effects against copper-catalyzed LDL oxidation than HDL2. Clin Biochem 30:221–225

    Article  PubMed  CAS  Google Scholar 

  • Yu S, Yarnell JW, Sweetnam P, Bolton CH (2003) High density lipoprotein subfractions and the risk of coronary heart disease: 9-years follow-up in the caerphilly study. Atherosclerosis 166:331–338

    Article  PubMed  CAS  Google Scholar 

  • Ziegler M (2000) New functions of a long-known molecule. Emerging roles of NAD in cellular signaling. Eur J Biochem 267:1550–1564

    Article  PubMed  CAS  Google Scholar 

Download references

Acknowledgments

The research described herein was supported in part by the National Institutes of Health and Niadyne, Inc. ELJ and MKJ are principles in Niadyne, Inc. and conflict of interest management is conducted by the University of Arizona Board of Regents.

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Elaine L. Jacobson .

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 2012 Springer Science+Business Media B.V.

About this chapter

Cite this chapter

Jacobson, E.L., Kim, H., Kim, M., Jacobson, M. (2012). Niacin: Vitamin and Antidyslipidemic Drug. In: Stanger, O. (eds) Water Soluble Vitamins. Subcellular Biochemistry, vol 56. Springer, Dordrecht. https://doi.org/10.1007/978-94-007-2199-9_3

Download citation

Publish with us

Policies and ethics