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Octacosanol

Common Name(s): Cluytyl alcohol, Montanyl alcohol, N-octacosanol, Octacosyl alcohol

Clinical Overview

Use

Octacosanol, which has been studied mainly as a constituent of policosanol (see Policosanol monograph), may have a role to play in the management of dyslipidemia and may achieve antiplatelet effects similar to those of aspirin. Although octacosanol has been protective in rats with induced parkinsonism, clinical studies in humans have not documented these effects. Clinical trials are lacking to support claims of enhanced athletic performance due to supplemental octacosanol.

Dosing

Limited clinical trials have been conducted with octacosanol. In one pharmacokinetic study, octacosanol 30 mg daily for 4 weeks did not result in measurable serum concentration changes, whereas octacosanol 50 mg was detected in the serum within 8 hours.

Contraindications

Contraindications have not been identified.

Pregnancy/Lactation

Information regarding safety and efficacy in pregnancy and lactation is lacking.

Interactions

None well documented.

Adverse Reactions

Limited clinical trials have been conducted with octacosanol; however, one surveillance study found long-term tolerability with policosanol supplementation.

Toxicology

No data.

Source

Octacosanol is derived primarily from wheat germ oil, as well as from krill, perilla, tomato, and grape seed oils, and from sugarcane and rice bran waxes.1, 2, 3, 4, 5 The production of sugarcane wax and the further refinement of octacosanol are difficult and expensive processes,6 but more efficient methods of octacosanol synthesis have been described.7, 8

History

Early work on the potential uses of octacosanol in the form of wheat germ oil is attributed to Thomas K. Cureton (1901-1992), professor and pioneer in exercise physiology, who conducted studies among more than 1,000 schoolboys in the 1950s and among US Navy trainees in the 1960s.9, 10 The potential of octacosanol to enhance exercise performance was further investigated in the latter part of the 20th century, with equivocal findings; with attention then directed to the role of octacosanol in treating cardiovascular disease.10, 11

Chemistry

Octacosanol is a 28-carbon, straight-chain aliphatic primary fatty alcohol.1 It belongs to a group of long chain alcohols extracted from plant waxes, collectively called policosanol. Analytical methods for the identification of octacosanol have been developed, allowing for quantification in plasma samples in animal and human studies.10, 12

Uses and Pharmacology

CNS disease

Animal data

In limited studies, octacosanol was protective in rats with induced parkinsonism, as measured histologically.13, 14

Clinical data

One small study reported that octacosanol (15 mg daily as wheat germ oil) improved subjectively rated scores in 3 of 10 patients.15 In the 1980s, small studies of octacosanol in patients with amyotrophic lateral sclerosis did not show a clinical significance compared with placebo, and further clinical trials have not been conducted.16, 17

Cholesterol/Dyslipidemia

Animal data

In studies of the effects of octacosanol on endurance in rodents, observed changes in serum lipid levels led investigators to consider octacosanol as a potential agent in dyslipidemia.1, 10 Octacosanol prevented increased perirenal adipose tissue in one experiment, and in another, it acted on the esterification of fatty acid into triacylglycerol in rats fed a high-fat diet.1, 10 Reductions in plasma triacylglycerol,18 but not of low-density lipoprotein (LDL) cholesterol, have been demonstrated in other experiments in mice.19 In vitro studies have suggested that both policosanol and a synthetic analogue of octacosanol (octacosadienol) can down-regulate 3-hydroxy-3-methyl-glutaryl-CoA reductase.20, 21

Clinical data

A study of healthy adults found a decrease in fecal cholesterol end products with octacosanol 50 mg supplementation, but no impact on serum lipid indices was observed.22

Most studies have used policosanol rather than octacosanol and have reported some positive effects (lowered LDL and elevated high-density lipoprotein).1, 10, 22

Exercise/Athletic performance

Animal data

Studies conducted in the 1990s found that octacosanol distributes mainly to adipose tissue when administered orally in rats, and that it is potentially stored in the liver and muscle tissues.23, 24 Absorption of octacosanol was reportedly low, with excretion mainly via feces. Metabolites of the alcohol were found in urine.23

A 2003 study reported on the ergogenic properties of octacosanol in exercise-trained rats, including glycogen-sparing and enhanced oxygen-carrying capacity in muscle tissue.25

Clinical data

Aside from studies in the 1950s and 1960s, clinical trials are lacking to support claims of enhanced athletic performance due to supplemental octacosanol.1, 10, 26

Platelet aggregation

Animal data

Studies in rodents have shown antiaggregatory effects of policosanol.1, 10

Clinical data

Most studies use policosanol rather than octacosanol, reporting some effects similar to those achieved with aspirin.1, 10, 22

Other uses

The effects of octacosanol on endothelial cells,27 as well as antioxidant activity,28 have been studied. The antiangiogenic action of octacosanol has also been studied.29

A mix of long-chain fatty acids, including octacosanol, has been studied in rats for its gastroprotective effects, which are attributed to anti-inflammatory action.1, 30 Anti-inflammatory and antinociceptive effects have also been reported in an induced-pain study in mice.31

Dosing

In one pharmacokinetic study, octacosanol 30 mg daily for 4 weeks did not result in measurable serum concentration changes, whereas octacosanol 50 mg was detected in the serum within 8 hours.22

A dosage of policosanol 20 mg/day has been compared with aspirin 100 mg/day in studies investigating the prevention of platelet aggregation.1, 10, 22

Pregnancy / Lactation

Information regarding safety and efficacy in pregnancy and lactation is lacking.

Interactions

Case reports are lacking; however, because policosanol has the potential to inhibit platelet aggregation, the risk of hemorrhage exists. Concomitant anticoagulant therapy should be used cautiously.1

Adverse Reactions

Limited clinical trials have been conducted with octacosanol; however, a surveillance study of 2,252 elderly patients taking policosanol supplementation found long-term tolerability of the supplements.32

Toxicology

Research regarding the toxicity of octacosanol is limited; however, policosanol studies in rodents have reported no carcinogenicity or teratogenicity.33, 34, 35, 36

References

1. Taylor JC, Rapport L, Lockwood GB. Octacosanol in human health. Nutrition. 2003;19(2):192-19512591561
2. Gao W, Liu D, Su S. High-performance thin-layer chromatography for quantification of 1-octacosanol in Antarctic krill (Euphausia superba Dana) [published online ahead of print August 21, 2014]. J Chromatogr Sci. 2015;53(5):811-815.2514649810.1093/chromsci/bmu098
3. Giuffrè AM, Capocasale M. Policosanol in Tomato (Solanum lycopersicum L.) Seed Oil: the Effect of Cultivar [published online ahead of print April 20, 2015]. J Oleo Sci. 2015;64(6):625-631.2589111410.5650/jos.ess15002
4. Jung DM, Lee MJ, Yoon SH, Jung MY. A gas chromatography-tandem quadrupole mass spectrometric analysis of policosanols in commercial vegetable oils. J Food Sci. 2011;76(6):C891-C899.22417487
5. Adhikari P, Hwang KT, Park JN, Kim CK. Policosanol content and composition in perilla seeds. J Agric Food Chem. 2006;54(15):5359-5362.16848517
6. Ou S, Zhao J, Wang Y, Tian Y, Wang J. Preparation of octacosanol from filter mud produced after sugarcane juice clarification. LWT - Food Sci Technol. 2012;45(2):295-298.
7. Cravotto G, Calcio Gaudino E, Barge A, Binello A, Albertino A, Aghemo C. Synthesis of 1-octacosanol and GC-C-IRMS discrimination of samples from different origin. Nat Prod Res. 2010;24(5):428-439.20306365
8. Kunkuma VL, Kaki SS, Rao BVSK, Prasad RBN, Prabhavathi Devi BLA. A simple and facile method for the synthesis of 1-octacosanol. Eur J Lipid Sci Technol. 2013;115(8):921-927.
9. Cureton TK, Barry AJ. Improving the Physical Fitness of Youth: A Report of Research in the Sports-Fitness School of the University of Illinois. Monogr Soc Res Child Dev. 1964;29:1-221.14288623
10. Mitmesser S. Octacosanol and Wheat Germ Oil. In: Driskell J, ed. Sports Nutrition: Fats and Proteins. Boca Raton, FL: CRC Press; 2007:99-104.
11. Saint-John M, McNaughton L. Octacosanol ingestion and its effects on metabolic responses to submaximal cycle ergometry, reaction time and chest and grip strength. Int Clin Nutr Rev. 1986;6:81-87.
12. Gonzalez-Bravo L, Magraner-Hernandez J, Acosta-Gonzalez PC, Perez-Souto N. Analytical procedure for the determination of 1-octacosanol in plasma by solvent extraction and capillary gas chromatography. J Chromatogr B Biomed Appl. 1996;682(2):359-363.8844431
13. Wang T, Liu Y, Yang N, Ji C, Chan P, Zuo P. Anti-parkinsonian effects of octacosanol in 1-methyl-4-phenyl-1,2,3,6 tetrahydropyridine-treated mice. Neural Regen Res. 2012;7(14):1080-1087.25722698
14. Wang T, Liu YY, Wang X, Yang N, Zhu HB, Zuo PP. Protective effects of octacosanol on 6-hydroxydopamine-induced Parkinsonism in rats via regulation of ProNGF and NGF signaling. Acta Pharmacol Sin. 2010;31(7):765-774.20581854
15. Snider SR. Octacosanol in parkinsonism. Ann Neurol. 1984;16(6):723.6395790
16. Norris FH, Denys EH, Fallat RJ. Trial of octacosanol in amyotrophic lateral sclerosis. Neurology. 1986;36(9):1263-1264.3528918
17. Orrell RW, Lane RJ, Ross M. Antioxidant treatment for amyotrophic lateral sclerosis / motor neuron disease. Cochrane Database Syst Rev. 2007;(1):CD002829.17253482
18. Xu Z, Fitz E, Riediger N, Moghadasian MH. Dietary octacosanol reduces plasma triacylglycerol levels but not atherogenesis in apolipoprotein E-knockout mice. Nutr Res. 2007;27(4):212-217.
19. Dullens SP, Mensink RP, Bragt MC, Kies AK, Plat J. Effects of emulsified policosanols with different chain lengths on cholesterol metabolism in heterozygous LDL receptor-deficient mice. J Lipid Res. 2008;49(4):790-796.18162663
20. Oliaro-Bosso S, Calcio Gaudino E, Mantegna S, et al. Regulation of HMGCoA reductase activity by policosanol and octacosadienol, a new synthetic analogue of octacosanol. Lipids. 2009;44(10):907-916.19763655
21. Singh DK, Li L, Porter TD. Policosanol inhibits cholesterol synthesis in hepatoma cells by activation of AMP-kinase. J Pharmacol Exp Ther. 2006;318(3):1020-1026.16714400
22. Keller S, Gimmler F, Jahreis G. Octacosanol administration to humans decreases neutral sterol and bile acid concentration in feces. Lipids. 2008;43(2):109-115.18004604
23. Kabir Y, Kimura S. Biodistribution and metabolism of orally administered octacosanol in rats. Ann Nutr Metab. 1993;37(1):33-38.8470870
24. Kabir Y, Kimura S. Tissue distribution of (8-14C)-octacosanol in liver and muscle of rats after serial administration. Ann Nutr Metab. 1995;39(5):279-284.8585696
25. Kim H, Park S, Han DS, Park T. Octacosanol supplementation increases running endurance time and improves biochemical parameters after exhaustion in trained rats. J Med Food. 2003;6(4):345-351.14977443
26. Jones AM, Haramizu S, Ranchordas M, Burke L, Stear S, Castell LM. A-Z of nutritional supplements: Dietary supplements, sports nutrition foods and ergogenic aids for health and performance-Part 27. Br J Sports Med. 2011;45(15):1246-1248.22076991
27. Liu YW, Zuo PY, Zha XN, et al. Octacosanol enhances the proliferation and migration of human umbilical vein endothelial cells via activation of the PI3K/Akt and MAPK/Erk pathways [published online ahead of print February 1, 2015]. Lipids. 2015;50(3):241-251.2563806310.1007/s11745-015-3991-2
28. Ohta Y, Ohashi K, Matsura T, Tokunaga K, Kitagawa A, Yamada K. Octacosanol attenuates disrupted hepatic reactive oxygen species metabolism associated with acute liver injury progression in rats intoxicated with carbon tetrachloride. J Clin Biochem Nutr. 2008;42(2):118-125.18385828
29. Thippeswamy G, Sheela ML, Salimath BP. Octacosanol isolated from Tinospora cordifolia downregulates VEGF gene expression by inhibiting nuclear translocation of NF-B and its DNA binding activity. Eur J Pharmacol. 2008;588(2-3):141-150.18513715
30. Molina V, Ravelo Y, Zamora Z, Mas R. Effects of D-002 on non-steroidal anti-inflammatory drugs-induced gastric ulcer in rats. Int J Pharm Sci Rev Res. 2015;30(1):253-257.
31. de Oliveira AM, Conserva LM, de Souza Ferro JN, de Almeida Brito F, Lyra Lemos RP, Barreto E. Antinociceptive and anti-inflammatory effects of octacosanol from the leaves of Sabicea grisea var. grisea in mice. Int J Mol Sci. 2012;13(2):1598-1611.22408410
32. Fernández S, Más R, Gamez R, et al. A pharmacological surveillance study of the tolerability of policosanol in the elderly population. Am J Geriatr Pharmacother. 2004;2(4):219-229.15903280
33. Rodríguez MD, García H. Evaluation of peri- and post-natal toxicity of Policosanol in rats. Teratog Carcinog Mutagen. 1998;18(1):1-7.9586765
34. Rodríguez MD, García H. Teratogenic and reproductive studies of policosanol in the rat and rabbit. Teratog Carcinog Mutagen. 1994;14(3):107-113.7940402
35. Alemán CL, Puig MN, Elías EC, et al. Carcinogenicity of policosanol in mice: an 18-month study. Food Chem Toxicol. 1995;33(7):573-578.7628793
36. Alemán CL, Más Ferreiro R, Noa Puig M, Rodeiro Guerra I, Hernández Ortega C, Capote A. Carcinogenicity of policosanol in Sprague Dawley rats: a 24-month study. Teratog Carcinog Mutagen. 1994;14(5):239-249.7855743

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