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The exact mechanism of action responsible for this activity has not been fully elucidated; however, several theories exist. One observation that appears to be agreed on by researchers is that policosanol does not inhibit the activity of HMG-CoA reductase, although it produces similar clinical results to HMG-CoA reductase inhibitors.

Some data indicate that policosanol inhibits cholesterol synthesis at an earlier point in the cholesterol biosynthetic pathway and increases LDL-cholesterol processing (Menendez et al 1994, 1996, 2000). Other evidence indicates that policosanol downregulates the cellular expression of HMG-CoA reductase by up to 50%, thereby suppressing biosynthesis of the enzyme (McCarty 2002). It has also been suggested that policosanol may stimulate the degradation of HMG-CoA reductase (Menendez et al 2001). Furthermore, animal studies suggest that LDL cataholism may be enhanced (Gouni-Berthold & Berthold 2002).

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