Gamma Tocotrienol Inhibits Cholesterol Synthesis

Byron's Comments:

Documentation of gamma tocotrienol as the specific tocotrienol that inhibits cholesterol synthesis.

Study Title:

Hypocholesterolemic activity of synthetic and natural tocotrienols.

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  t 2;35(20):3595-606.
Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492.

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