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The present study was aimed to explore the antihyperlipidemic and anti-inflammatory effect of acyclic isoprenoid on high fat diet fed rats. Hypercholesterolemia was induced by the diet comprising of the normal rat chow 84.3%, lard 5%, yolk powder 10%, cholesterol 0.2% and 0.5% bile salt were fed to the rats for the period of 8 weeks. The results showed that abnormally elevated levels of plasma lipid profiles. Three different doses of acyclic isoprenoid (20, 40 and 80 mg/kg b.w/day) were administered orally to hypercholesterolemia suffering rats for the period of 30 days. Among these three doses of acyclic isoprenoid, the dose 80 mg/kg b.w. was significantly decreased the plasma lipid profiles when compared to other two doses. The effect produced by acyclic isoprenoid (80 mg/kg b.w) was comparable to that of simvastatin. Therefore, 80 mg/kg b.w was fixed as a effective dose and used for further analyses. Acyclic isoprenoid administration reinstated the elevated levels of cardiac and inflammatory markers in both blood and serum of hypercholesterolemic rats. In addition, acyclic isoprenoid administration decreased activity of 3-hydroxy 3-methyl-glutaryl-CoA reductase and increased the activity of lecithin cholesterol acyl transferase. These findings suggest that the administration of acyclic isoprenoid was potentially ameliorated the cardiac marker enzymes and inflammatory markers in addition to its antihypercholesterolemic effect.