Several studies indicate that increased atherogenecity of LDL during diabetes is associated with a preponderance of small dense (sd)-LDL subpopulation, that is more prone to oxidative modification than large buoyant (lb)-LDL. In this study, we describe the hypoglycemic, hypolipidemic and antioxidant properties of dietary tocotrienols (Tocomin) and Lovastatin supplementation in diabetic-hyperlipidemic rats. Diabetes in rats was induced by streptozotocin (6.0 mg/100 g body wt) and they were treated with 7.0 mg Tocomin or 2.0 mg Lovastatin for 23 weeks. At the end of the study, diabetic control rats had a significant increase in plasma glucose and blood HbA1, plasma TG, TC, VLDL-C, LDL-C, HDL-C, HDL2-C, HDL3-C and non-HDL-C. Tocomin and Lovastatin mediated a substantial decline in glucose and HbA1 to near normal levels, Our ex vivo results demonstrate that even in normal animals, relative to lb-LDL, the in vivo oxidizability of sd-LDL, measured as base line diene conjugation (BDC) was higher by 2.90-fold, which was further increased to 3.3-fold due to diabetes. Similarly, in comparison to a lag phase value of 53 min for lb-LDL in normal rats, sd-LDL lag phase was reduced to only 15.0 min, which was further shortened to 9.6 min in diabetic rats, indicating a substantially enhanced Cu++-catalyzed sd- LDL oxidizability. In conclusion, although multiple therapeutic benefits of Tocomin and Lovastatin are comparable, considering the host of side effects exhibited by Lovastatin, daily intake of dietary tocotrienols will be useful in the prevention and treatment of diabetes, diabetes linked hyperlipidemia with and without CHD and atherosclerosis.