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  • Besting Natural Molecules Still A Challenge

    November 2, 2016: by Bill Sardi

    Two-thousand years ago Roman soldiers wrapped their wounds in wine-soaked bandages and chewed garlic going into battle as an antibiotic.  From that point forward we can’t say modern pharmacology has advanced much beyond that point.

    The broad biological action of the molecules in grapes and garlic cloves activate key genes (mTOR, AMPK, NF Kappa B, Sirtuin1, Sirtuin3, Foxo1 and Nrf2) that perform beyond the limited capacity of any synthetically made molecule. [Resveratrol News Dec 15, 2015]

    Maybe synthetic molecules can be made that work better than natural ones but they will certainly be more expensive and problematic.

    Pharmacologists have had great difficulty making synthetic versions of the red wine molecule resveratrol or allicin, the primary active molecule in fresh-crushed garlic, that out-perform their natural counterparts.

    Efforts to produce a molecular analog (look-alike) of resveratrol were thwarted when it was found that liver metabolism of resveratrol knocks off the synthetically-added molecular tail and returns it to its natural form.  [Molecular Pharmacology 2013]

    Allicin, the primary active molecule in fresh-crushed garlic, is difficult to reproduce as a drug because it is a transient molecule that converts to other less active sulfur molecules over time.  The best that can be done is to deliver alliin-rich garlic powder that will then utilize an active enzyme (alliinase) to convert to allicin as the garlic clove is crushed.

    However, stomach acid degrades alliinase and negates the formation of allicin.  Garlic cloves must be crushed outside the acidic digestive tract, so as to mix alliinase with alliin, to produce allicin and then orally consumed.  However, the pungency of such a practice is not a desirable experience for most consumers.

    Resveratrol pills are a modern phenomenon, garlic cloves are not.

    So just how does garlic stack up against resveratrol?

    In an animal study researchers recently compared garlic and resveratrol next to metformin, an anti-diabetic drug.  The laboratory mice were chemically induced to develop diabetes.

    The results of that study remarkably reveals allicin/garlic is on par with or exceeds the biological action of the anti-diabetic medicine metformin and even bested resveratrol.

    Garlic/allicin-fed animals at less food (lower appetite), gained less weight, had higher insulin levels (evidence of renewed ability of the pancreas to secrete insulin), had lower blood sugar levels and far higher levels of an internally-produced antioxidant enzyme, catalase, than metformin.  Resveratrol was superior in controlling weight gain but not by much over garlic/allicin.

    Regeneration of the pancreas’ ability to secrete insulin is not something modern medicine talks about.  There are no medicine’s that do that effectively.

    Every other anti-diabetic medicine aside from metformin induces weight gain among diabetic subjects.

    A reason why these animal studies often do not translate to human studies is because the animals are on a controlled diet.  Humans can sneak into the refrigerator and grab snacks or choose to eat sugary or carbohydrate-rich foods (bread, rice, pasta, cereal), which converts to sugar in the body.  About 80% of the processed and prepared foods in today’s grocery stores have sugar added.

    Unfortunately, researchers did not examine whether the combination of resveratrol + garlic/allicin as a synergistic effect.

    Garlic/allicin and resveratrol are far superior to most anti-diabetic drugs, at least in the animal lab.

    An added note: most commercially available garlic pills advertise they yield or have potential to deliver allicin.  This is based on crude studies in lab dishes in water.  If crushed garlic is placed in vinegar to replicate the acidic environment in the digestive tract, almost not allicin is produced due to the destruction of the alliinase enzyme.

    A patented alkaline-buffered garlic capsule overcomes this problem and has been demonstrated to produce allicin in human subjects. []

    Sadly, most diabetologists are unaware of the potential health benefits from resveratrol and garlic/allicin for diabetics.  ©2016 Bill Sardi,

    Comparsion Of The Effect Of Allicin (Garlic), Resveratrol & Anti-Diabetic Drug (Metformin) In Experimentally-Induced Diabetes (Mice)
    Source: Frontiers in Pharmacology Oct 13, 2016




    Diabetic + Garlic

    Diabetic + Resveratrol

    Diabetic + Metformin

    Food Intake
    Beginning/End of study


    20 grams


    18 grams


    17 grams


    18 grams


    19 grams

    Body Weight
    Beginning/End of study;
    net gain/loss


    – –


    260/320 g
    +60 grams


    250/220 g
    -30 grams


    240/220 g
    -40 grams


    265/240 g
    -15 grams

    micromole concentration






    Blood Sugar






    Oxidation of Lipids (fats)
    TBARS) Thiobarbituric acid reactive substances






    Enzymatic antioxidant











    * Higher number insulin = better ability restore insulin secretion from the pancreas.

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