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MoonDragon's Health & Wellness
Nutrition Basics


Vitamin B-1 Derivative

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  • Benfotiamine Description
  • Benfotiamine Supplements & Products



    Benfotiamine is also known as S-benzoylthiamine O-monophosphate, is a synthetic S-acyl derivative or Thiamine, Vitamin B-1.

    It has been licensed for use in Germany since 1993 under the trade name Milgamma (combinations with pyridoxine or cyanocobalamin are also sold under this name). It is prescribed there for treating sciatica and other painful nerve conditions. It is marketed as a medicine and/or dietary supplement, depending on the respective regulatory agency.



    Benfotiamine is primarily marketed as an antioxidant dietary supplement. In a clinical study with six patients, benfotiamine lowered AGE (advanced glycation end products) by 40 percent.

    Benfotiamine may be useful for the treatment of diabetic retinopathy, neuropathy, and nephropathy. However, most of the effects attributed to benfotiamine are extrapolated from in vitro and animal studies. Unfortunately apparent evidences from human studies are scarce and especially endpoint studies are missing. Therefore additional clinical studies are mandatory to explore the therapeutic potential of benfotiamine in both diabetic and non-diabetic pathological conditions.

    It is thought that treatment with benfotiamine leads to increased intracellular thiamine diphosphate levels, a cofactor of transketolase. This enzyme directs advanced glycation and lipoxidation end products (AGE's, ALE's) substrates to the pentose phosphate pathway, thus reducing tissue AGEs.


    In human nutrition and biology, advanced glycation end products, known as AGEs are substances that can be a factor in the development or worsening of many degenerative diseases, such as diabetes, atherosclerosis, chronic renal failure, and Alzheimer's disease. These harmful compounds can affect nearly every type of cell and molecule in the body and are thought to be one factor in aging and in some age-related chronic diseases. They are also believed to play a causative role in the blood-vessel complications of diabetes mellitus. AGEs are seen as speeding up oxidative damage to cells and in altering their normal behavior.

    AGEs are formed both outside and inside the body. Specifically, they stem from glycation reaction, which refers to the addition of a carbohydrate to a protein without the involvement of an enzyme. Glucose can bind with proteins in a process called glycation, making cells stiffer, less pliable and more subject to damage and premature aging. Outside the body, AGEs can be formed by heating (for example, cooking). Intermediate products in the formation of an AGE are known as Amadori, Schiff base, and Maillard products, named after the researchers who first described them.

  • Smoking: Smoking is known to elevate the level of AGEs. AGEs are formed when tobacco leaves are dried in the presence of sugars. During inhalation, these AGEs are absorbed in the lungs. Both serum AGEs and AGEs in skin (measured with skin autofluorescence) are higher in smokers, compared to non-smokers.

  • barbequed foods are high in AGEs

  • Foods: Dietary AGEs (dAGEs) can be present in some foods (particularly meat, also butter and some vegetable products), and can form in food during cooking, particularly in dry cooking such as frying, roasting and baking, far less so in boiling, stewing, steaming and microwaving. In addition some foods promote glycation within the body. The total state of oxidative and peroxidative stress on the healthy body, with the AGE-related damage to it, is proportional to the dietary intake of exogenous (preformed) AGEs and the consumption of sugars with a propensity towards glycation such as fructose and galactose.

  • Diabetes: In diabetes, in cells unable to reduce glucose intake (e.g., endothelial cells), hyperglycemia results in higher intracellular glucose levels. Higher intracellular glucose levels result in increased levels of NADH and FADH, increasing the proton gradient beyond a particular threshold at which the complex III prevents further increase by stopping the electron transport chain. This results in mitochondrial production of reactive oxygen species, activating PARP1 by damaging DNA. PARP1, in turn, induces ADP-ribosylation of GAPDH, a protein involved in glucose metabolism, leading to its inactivation and an accumulation of metabolites earlier in the metabolism pathway. These metabolites activate multiple pathogenic mechanisms, one of which includes increased production of AGEs. Examples of AGEs are carboxymethyllysine (CML), carboxyethyllysine (CEL), and argpyrimidine, which is the most common.


    AGEs affect nearly every type of cell and molecule in the body and are thought to be one factor in aging and some age-related chronic diseases. They are also believed to play a causative role in the vascular complications of diabetes mellitus. Under certain pathologic conditions, such as oxidative stress due to hyperglycemia in patients with diabetes, and hyperlipidemia, AGE formation can be increased beyond normal levels. AGEs are now known to play a role as proinflammatory mediators in gestational diabetes as well. The animal and human evidence is that significant amounts of dAGEs are absorbed, and that dAGEs contribute to the body's burden of AGE, and are associated with diseases such as atherosclerosis and kidney disease.

    In Other Diseases: The formation and accumulation of advanced glycation endproducts (AGEs) has been implicated in the progression of age-related diseases. AGEs have been implicated in Alzheimer's Disease, cardiovascular disease, and stroke. The mechanism by which AGEs induce damage is through a process called cross-linking that causes intracellular damage and apoptosis. They form photosensitizers in the crystalline lens, which has implications for cataract development. Reduced muscle function is also associated with AGEs.

    Pathology: AGEs have a range of pathological effects, such as:
    • Increased vascular permeability.
    • Increased arterial stiffness.
    • Inhibition of vascular dilation by interfering with nitric oxide.
    • Oxidizing LDL.
    • Binding cells - including macrophage, endothelial, and mesangial - to induce the secretion of a variety of cytokines.
    • Enhanced oxidative stress.


    AGEs are the subject of ongoing research. There are three therapeutic approaches: preventing the formation of AGEs, breaking crosslinks after they are formed and preventing their negative effects. Compounds that have been found to inhibit AGE formation in the laboratory include Vitamin C, benfotiamine, pyridoxamine, alpha-lipoic acid, taurine, pimagedine, aspirin, carnosine, metformin, pioglitazone, and pentoxifylline. Studies in rats and mice have found that natural phenols such as resveratrol and curcumin can prevent the negative effects of the AGEs. Compounds that are thought to break some existing AGE crosslinks include Alagebrium (and related ALT-462, ALT-486, and ALT-946) and N-phenacyl thiazolium bromide.

    There is, however, no agent known that can break down the most common AGE, glucosepane, which appears 10 to 1,000 times more common in human tissue than any other cross-linking AGE. Some chemicals, on the other hand, like aminoguanidine, might limit the formation of AGEs by reacting with 3-deoxyglucosone.


  • Benfotiamine Supplement Products


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    Benfotiamine protects agains diabetic neuropathy or retinopathy. This fat-soluble form of Vitamin B-1 lasts longer in the body and is less toxic than the water-soluble form. It blocks absorption of excess glucose into cells. Dose is 150 to 600 mg daily or as recommended by a health care provider. Do not use if you are pregnant or breastfeeding.


    HerbsPro: Benfotiamine, Nature's Life, 60 VCaps
    HerbsPro: Benfotiamine With Vitamin B-1, Country Life, 60 VCaps
    Supports cell glucose metabolism and provides strong nerve support. More bioavailable than standard B-1. Gluten free dietary supplement.
    HerbsPro: Coenzyme B-Complex Advanced, With Benfotiamine, PQQ & NADH, Country Life, 60 VCaps
    A gluten free dietary supplement that supports increased energy production and support sugar metabolism. With Benfotiamine, PQQ and NADH.
    HerbsPro: Coenzyme B-Complex Advanced, With Benfotiamine, PQQ & NADH, Country Life, 120 VCaps
    A gluten free dietary supplement that supports increased energy production and support sugar metabolism. With Benfotiamine, PQQ and NADH.
    HerbsPro: Benfotiamine With Thiamin, Life Extension, 100 mg, 120 Caps
    HerbsPro: Benfotiamine With Thiamin, Life Extension, 100 mg, 120 Caps
    HerbsPro: Benfotiamine, Source Naturals, 150 mg, 60 Tabs
    HerbsPro: Best Benfotiamine Plus Alpha Lipoic Acid, Doctors Best, 150 mg / 300 mg, 60 VCaps
    HerbsPro: Benfotiamine Thiamine B-1, Futurebiotics, 150 mg, 120 Caps
    HerbsPro: Best Benfotiamine, Doctors Best, 150 mg, 120 VCaps
    HerbsPro: Benfotiamine, Source Naturals, 150 mg, 120 Tabs
    HerbsPro: Best Benfotiamine, Doctors Best, 150 mg, 360 VCaps
    HerbsPro: Mega Benfotiamine, Life Extension, 250 mg, 120 VCaps
    HerbsPro: Best Benfotiamine, Doctors Best, 300 mg, 60 VCaps


    LEF: Benfotiamine with Thiamine, Life Extension, 100 mg, 120 VCaps
    Benfotiamine, a fat-soluble form of vitamin B-1 (thiamine), supports healthy blood sugar metabolism and helps protect the bodys tissues against advanced glycation end products and oxidative stress.
    LEF: Mega Benfotiamine, Life Extension, 250 mg, 120 VCaps


    Kalyx: Benfotiamine, Future Biotics, 150 mg, 120 VCaps: HF


    Amazon: Benfotiamine Supplement Products

    Amazon: Benfotiamine Multi-B Formula, Benfotiamine, 150 mg, 120 Caps
    Benfotiamine Multi-B Formula is designed to dramatically boost AGE-fighting thiamine pyrophosphate (TPP) and cell-shielding activity of the enzyme transketolase in your body. Benfotiamine is enhanced in this formula with the help of other B vitamins, including vitamin B-2, vitamin B-6, folic acid, vitamin B-12 and vitamin B-5.

    Amazon: Benfotiamine, Vitacost, 150 mg, 120 Caps
    Benfotiamine is derived from thiamine (vitamin B1), part of the family commonly known as B-vitamins. It is well understood that thiamine plays a vital role in nerve function, energy dynamics and the digestive process. Thiamine is well researched for its important role in the metabolism of sugars. As people age, the conversion of sugars in the body can lead to age-associated glycation end products (AGEs), which are created inside the body through normal metabolism and aging. This process involves the adherence of sugars to proteins reducing the proper function of those proteins and the accumulation of these undesireable AGEs. Benfotiamine plays a role in blocking the age-associated glycation end products (AGEs).* Benfotiamine is an amphiphilic S-acyl thiamine derivative that is virtually fat soluble. It is very well absorbed in the body, but does not appear to cross the blood-brain barrier. Supports the digestion of food and carbohydrates. Supports desirable by-products related to sugar metabolism. Slows the formation of age-associated glycation end products, which can be caused by aging. Helps to maintain healthy endothelial function. Necessary for healthy heart function.

  • Nutrition Basics: Benfotiamine Supplement Information

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