The oleic acid esterification of policosanol increases its bioavailability and hypocholesterolemic action in rats

D. Haim; A. Valenzuela; M. C. Brañes; M. Fuenzalida; L. A. Videla

doi:10.3989/gya.010612

Authors

D. Haim Molecular and Clinical Pharmacology Program, Institute of Biomedical Sciences, Faculty of Medicine, University of Chile - Faculty of Medicine, University of the Andes
A. Valenzuela Laboratory of Lipids and Antioxidants, Institute of Nutrition and Food Technology, University of Chile - Faculty of Medicine, University of the Andes
M. C. Brañes Naturalis S.A.
M. Fuenzalida Naturalis S.A.
L. A. Videla Molecular and Clinical Pharmacology Program, Institute of Biomedical Sciences, Faculty of Medicine, University of Chile

DOI:

https://doi.org/10.3989/gya.010612

Keywords:

Bioavailability, Cholesterol lowering effect, Octacosanol, Policosanol, Policosanol absorption, Rats, Triacontanol

Abstract

Policosanol comprises a mixture of long-chain aliphatic alcohols from sugarcane wax. More than 50 studies indicate that policosanol decreases serum cholesterol, while others failed to reproduce this effect. The objective of this investigation was to assess the bioavailability of esterified policosanol and non-esterified policosanol (NEP), in relation to their hypocholesterolemic effects. Sprague Dawley rats were given a daily oral dose of 100 mg/kg of NEP, 117 mg kg^–1 of butyric acid esterified policosanol (BAEP), or 164 mg kg^–1 of oleic acid esterified policosanol (OAEP). Policosanol absorption was evaluated in plasma between 0 and 3 hours after ingestion. To assess changes in total cholesterol, LDL-cholesterol, HDLcholesterol and triacylglycerols in plasma and liver 3-hydroxy- 3-methylglutaryl coenzyme A reductase (HMG- CoA red) phosphorylation, the rats were supplemented with nonesterified or esterified policosanol for 5 weeks. The results indicate that policosanol absorption was significantly greater in OAEP-treated rats than in those subjected to NEP or BAEP administration. OAEP significantly reduced plasma total and LDL-cholesterol in rats, in addition to a 5.6-fold increase (P < 0.05) in the hepatic content of phosphorylated HMG-CoA red over the control values. In conclusion, esterification of policosanol with oleic acid enhances policosanol bioavailability, and significantly improves the serum lipid profile in normocholesterolemic rats in association with the inactivation of HMG-CoA red controlling cholesterogenesis.

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