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

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. Los Policosanoles están formados por una mezcla de alcoholes alifáticos de cadena larga y se obtienen de las ceras de la ca a de azúcar. Más de cincuenta estudios indican que los policosanoles reducen el colesterol sérico, mientras que otros no logran reproducir este efecto. El objetivo de esta investigación fue evaluar la biodisponibilidad de policosanoles esterificados y no esterificados (NEP), en relación con sus efectos hipocolesterolémicos. Para ello, a ratas Sprague Dawley se les administró una dosis oral diaria de 100 mg kg–1 de NEP, 117 mg kg–1 de policosanoles esterificados con ácido butírico (BAEP), ó 164 mg kg–1 de policosanoles esterificados con ácido oleico (OAEP). La absorción de los policosanoles se evaluó en el plasma entre 0 y 3 horas después de la ingestión. Para evaluar los cambios en el colesterol total, colesterol-LDL, colesterol-HDL y triglicéridos en el plasma y en la fosforilación de la hígado 3-hidroxi-3-metilglutaril coenzima A reductasa (HMG-CoA red), la ingesta de las ratas fue suplementada con policosano