• Tocotrienols exert their cholesterol lowering effect through the suppression of HMG-CoA reductase, a rate-limiting enzyme in cholesterol bio-synthesis.
• Alpha tocotrienols suppresses hepatic HMG-CoA reductase activity that results in the lowering of LDL cholesterol levels.
• Combination of gamma-tocotrienols and alpha-tocopherol is found as a potential hypolipemic agent in hyperlipemic humans at atherogenic risk.
• Tocotrienols inhibit cholesterogenesis by suppressing HMG-CoA reductase.
• A 4 weeks supplementation of Tocotrienols 200 mg/day resulted in a significant (p.< 0.05) drop of 15-22% of serum total cholesterol and 10-20% of LDL cholesterol, while the level of HDL fraction remained unchanged.
• Total cholesterol declined significantly with tocotrienols compared to alpha-tocopherol in patients with mild hypercholesterolemia.
• Combination of citrus flavonoids and tocotrienols were found to lower serum cholesterol levels in hypercholesterolemic patients.

Tocotrienols reduce macrophages cholesterol accumulation. Cholesterol synthesis inhibition induced by α-tocotrienols is not limited to liver, as previously reported, it is also effective in decreasing cholesterol stores in macrophages.