Octacosanol
Common Name(s): Cluytyl alcohol, Montanyl alcohol, N-octacosanol, Octacosyl alcohol
Medically reviewed by Drugs.com. Last updated on Sep 21, 2023.
Clinical Overview
Use
Octacosanol, which has been studied mainly as a constituent of policosanol (see Policosanol monograph), may play a role in the management of dyslipidemia and may achieve antiplatelet effects similar to those of aspirin. Although octacosanol has shown protective effects in rats with induced parkinsonism, clinical studies in humans have not documented these effects. Clinical trial data are lacking to support claims of enhanced athletic performance due to supplemental octacosanol intake. Quality clinical trial data are lacking to support use for any indication.
Dosing
Limited clinical trials using octacosanol have been conducted; data are lacking to provide dosing recommendations.
Contraindications
Contraindications have not been identified.
Pregnancy/Lactation
Avoid use. 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, tomatoes, grape seed oil, sugarcane, and rice bran waxes.Adhikari 2006, Gao 2015, Giuffrè 2015, Jung 2011, Taylor 2003 The production of sugarcane wax and the further refinement of octacosanol are difficult and expensive processes,Ou 2012 but more efficient methods of octacosanol synthesis have been described.Cravotto 2010, Kunkuma 2013
History
Early work on the potential uses of octacosanol in the form of wheat germ oil is attributed to Thomas K. Cureton (1901-1992), a 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.Cureton 1964, Mitmesser 2007 The potential of octacosanol to enhance exercise performance was further investigated in the latter part of the 20th century, with equivocal findings. Attention was then directed to the role of octacosanol in treating various cardiovascular diseases.Mitmesser 2007, Saint-John 1986
Chemistry
Octacosanol is a major constituent of policosanol, a mixture of long-chain aliphatic alcohols.Kaushik 2017 Octacosanol is a 28-carbon, straight-chain aliphatic primary fatty alcohol.Taylor 2003 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.Gonzalez-Bravo 1996, Mitmesser 2007
Uses and Pharmacology
Antiangiogenic activity
In vivo data
Octacosanol isolated from Tinospora cordifolia downregulates VEGF gene expression by inhibiting nuclear translocation of nuclear factor kappa B and its DNA binding activity, which suggests octacosanol may play a role in antiangiogenic activity.Thippeswamy 2008
Anti-inflammatory/Antinociceptive effects
Animal data
Anti-inflammatory and antinociceptive effects of octacosanol from the leaves of Sabicea grisea have been reported in a study in mice with acetic acid–induced pain.de Oliveira 2012
Antioxidant effects
Animal data
Octacosanol attenuates disrupted hepatic reactive oxygen species metabolism associated with acute liver injury progression in rats intoxicated with carbon tetrachloride.Ohta 2008 Octacosanol fights against cellular stress by increasing glutathione (GSH) levels and thus scavenging oxygen reactive species.Kaushik 2017 Increased GSH also contributes to stress tolerance.Kaushik 2017
Atherosclerosis
In vitro and experimental data
Octacosanol has demonstrated enhanced proliferation and migration of human umbilical vein endothelial cells via activation of the PI3K/Akt and MAPK/Erk pathways.Liu 2015
Cholesterol/Dyslipidemia
Animal data
In studies evaluating the effects of octacosanol on endurance in rodents, observed changes in serum lipid levels led investigators to consider octacosanol as a potential agent for dyslipidemia.Mitmesser 2007, Taylor 2003 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.Mitmesser 2007, Taylor 2003 Reductions in plasma triacylglycerolXu 2007 but not in low-density lipoprotein (LDL) cholesterol have been demonstrated in other experiments in mice.Dullens 2008 In vitro studies have suggested that both policosanol and a synthetic analogue of octacosanol (octacosadienol) can downregulate 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase.Oliaro-Bosso 2009, Singh 2006 In a study evaluating the effects of octacosanol or policosanol on high-fat diet–induced obesity, mice receiving a high-fat diet and treated with octacosanol or policosanol showed no significant reduction in plasma levels of triglycerides, total cholesterol, and free fatty acids compared with those in the high-fat diet alone group.Sharma 2019
Clinical data
A study of healthy adults showed a decrease in fecal cholesterol end products with octacosanol 50 mg supplementation, but no impact on serum lipid indices was observed.Keller 2008 In a study in males engaged in a weight-loss and taekwondo training program, those taking octacosanol 40 mg daily for 6 days experienced significant benefits in lipid status and markers of oxidative stress compared with those in the placebo group.Lee 2019
CNS effects
Animal data
In limited studies, octacosanol was protective in rats with induced parkinsonism, as measured histologically.Wang 2010, Wang 2012 In mice, octacosanol did not alter normal sleep and did alleviate stress and restore stress-affected sleep.Kaushik 2017
Clinical data
One small study reported that octacosanol (15 mg daily of wheat germ oil taken for 6 weeks) improved subjectively rated scores in 3 of 10 patients with Parkinson disease who were asked to rate themselves weekly based on activities of daily living and mood, endurance, and parkinsonism symptoms.Snider 1984
In the 1980s, small studies of octacosanol in patients with amyotrophic lateral sclerosis did not show clinically important improvement compared with placebo.Norris 1986, Orrell 2007
Exercise/Athletic performance
Studies conducted in the 1990s found that octacosanol distributes mainly to adipose tissue when administered orally in rats, and is potentially stored in the liver and muscle tissues.Kabir 1993, Kabir 1995 Absorption of octacosanol was reportedly low, with excretion mainly via feces. However, metabolites from the alcohol moiety of octacosanol were found in the urine.Kabir 1993
Animal data
There is very little in vivo or in vitro evidence regarding the effect of octacosanol on stimulating lipolysis.Kim 2016
One study reported the ergogenic properties of octacosanol in exercise-trained rats, including glycogen-sparing and enhanced oxygen-carrying capacity in muscle tissue.Kim 2003
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.Jones 2011, Mitmesser 2007, Taylor 2003 Sufficient evidence regarding the efficacy of octacosanol on endurance performance in humans is lacking, although it may have an ergogenic effect.Kim 2016
Metabolic effects
Animal data
In mice, octacosanol and policosanol prevented high-fat diet–induced obesity and metabolic disorders by activating brown adipose tissue and improving hepatic lipid metabolism.Sharma 2019
Dosing
Limited clinical trials using octacosanol have been conducted; data are lacking to provide dosing recommendations.
In one pharmacokinetic study, octacosanol 30 mg daily for 4 weeks did not result in measurable serum concentration changes, whereas serum concentrations were detectable when octacosanol 50 mg was administered.Keller 2008
Pregnancy / Lactation
Avoid use. 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.Taylor 2003
Adverse Reactions
Limited clinical trials have been conducted with octacosanol; however, a surveillance study of 2,252 elderly patients taking policosanol supplementation showed long-term tolerability.Fernández 2004 Policosanol is safe for humans because it is well tolerated and not associated with any adverse effects, even at single oral doses of 1,000 mg.Weerawatanakorn 2019
Toxicology
Research regarding the toxicity of octacosanol is limited; however, policosanol studies in rodents have reported no carcinogenicity or teratogenicity.Alemán 1994, Alemán 1995, Rodríguez 1994, Rodríguez 1998
References
Disclaimer
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