Study Title:

Gamma Tocotrienol Inhibits Cholesterol Synthesis

Study Abstract

Tocotrienols are farnesylated benzopyran natural products that exhibit hypocholesterolemic activity in vitro and in vivo. The mechanism of their hypolipidemic action involves posttranscriptional suppression of HMG-CoA reductase by a process distinct from other known inhibitors of cholesterol biosynthesis. An efficient synthetic route to tocotrienols and their isolation from palm oil distillate using an improved procedure is presented. gamma-Tocotrienol exhibits a 30-fold greater activity toward cholesterol biosynthesis inhibition compared to alpha-tocotrienol in HepG2 cells in vitro. The synthetic (racemic) and natural (chiral) tocotrienols exhibit nearly identical cholesterol biosynthesis inhibition and HMG-CoA reductase suppression properties as demonstrated in vitro and in vivo.

Study Information

Pearce BC, Parker RA, Deason ME, Qureshi AA, Wright JJ.
Hypocholesterolemic activity of synthetic and natural tocotrienols.
J Med Chem.
1992 October
Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492.

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