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SupplementScience

BenfotiamineBenfotiamineBenfotiamine By Gene Bruno, MS, MHS

enfotiamine is a -soluble form classic deficiency disease “beriberi,” for Diabetes of ( B1) often characterized by:5 Benfotiamine has particularly valuable Bconsidered to be the most effec- • benefits to offer for individuals with dia- tive of the group of natural- • Muscle pain and tenderness betes due to its unusual property of ly occurring, thiamine-derived com- • Rapid heart rate inhibiting three major pathways of dia- pounds, found in trace quantities in • Enlargement of the heart betes-induced vascular damage and roasted crushed and other veg- • Edema (severe swelling due to neuropathy, and also having value in etables from the Allium genus (such as water retention) treating diabetic retinopathy and kidney onions, shallots and leeks). It is • Congestive heart failure damage. The three pathways include absorbed much better than water-solu- the hexosamine pathway, the advanced ble thiamine salts: maximum plasma Causes of glycation end product (AGE) formation levels of thiamine are about five times While thiamine deficiency is not common pathway and the diacylglycerol (DAG)- higher after benfotiamine, the bioavail- in the U.S., there are situations in which a protein kinase C (PKC) pathway.12 AGEs ability is at maximum about 3.6 times as deficiency may result from an increased are particularly nasty, so inhibition of high as that of thiamine hydrochloride requirement or excessive loss of this their formation is especially desirable. and better than other lipophilic thi- nutrient, as well as consumption of anti- amine derivates.1 thiamine factors. Situations in which Advanced Glycation End Product Before further exploring the research there is an increased need for thiamine (AGE) and benefits of benfotiamine, it is include strenuous physical exertion, AGEs are formed from glycosylated pro- important to understand the basics of fever, pregnancy, breast-feeding, adoles- teins, which in turn are formed when glu- thiamine since benfotiamine also per- cent growth and HIV-infection (with or cose has attached itself to protein. For forms the same functions. without AIDS).6 Excessive thiamine loss example, glucose can attach itself to the may be caused by chronic alcohol protein in red blood cells’ hemoglobin A Review of Thiamine abuse/alcoholism7, the use of diuretics8,9 and form glycosylated hemoglobin, also Thiamine was one of the first organic and hemodialysis.10 Anti-thiamin factors, called hemoglobin A1C, HbA1C, or just compounds to be recognized as a vita- including thiaminases which inactivate A1C for short. If this process continues to min. In its coenzyme form, thiamine is thiamin, can also promote a loss of this excess, one eventually ends up with required for a small number of very vitamin. Consuming large amounts of teaAGEs, which become permanent fixtures important enzymes that play critical and coffee (including decaffeinated), as in cells. AGE impregnated cells are very roles in the production of energy from well as habitually eating certain raw reactive and react with one another, and food, including the production of ATP.2 freshwater fish, raw shellfish and ferns other proteins. In the case of blood capil- It is also required for the synthesis of are at higher risk of thiamin deficiency laries, they can result in the walls of the the nucleic acids, DNA and RNA.3,4 A because these foods contain thiaminase capillaries thickening, eventually causing deficiency of thiamine may lead to the normally inactivated by heat in cooking.11 the vessels to be blocked off.13 38 VITAMIN RETAILER WWW.VITAMINRETAILER.COM JULY 2012 “Benfotiamin is a particularly Essentially, AGE reactions create chemical rats, and completely prevented increas- handcuffs, which gum up proteins, deac- well-absorbed form of vitamin B1. es in AGE and PKU activity. This sug- tivate enzymes, trigger unhealthy bio- Double-blind research in gests that benfotiamine may help pre- chemical signaling in cells and damages diabetics demonstrated that oral vent or delay the progression of DNA, which contributes to the aging doses of 400 mg daily resulted in microvascular changes in patients with process. In a study on diabetic subjects, a statistically significant diabetic retinopathy. 600 mg of benfotiamine was supple- improvement in neuropathy score mented for 28 days. Blood was drawn Kidney Damage before and after treatment. The results in the treatment group Hemodialysis patients have an elevated were a significant reduction of intracellu- compared to placebo. The most level of damage to their genes in periph- lar glycoxidation and AGE formation.14 significant improvement reported eral blood lymphocytes (PBLs) and an was pain decrease in increased cancer incidence, possibly due Neuropathy to accumulation of toxins like AGEs. polyneuropathy (a type of Neuropathy is a collection of disorders that Since benfotiamine reduces AGE levels, peripheral neuropathy). Other occurs when nerves of the peripheral nerv- and since hemodialysis patients tend ous system are damaged. This is common- research has demonstrated toward vitamin B1 deficiency, researchers ly referred to as peripheral neuropathy statistically significant conducted two consecutive studies23 sup- (PN). PN usually causes pain and numb- effectiveness in reducing plementing hemodialysis patients with ness in the hands and feet. It can result pain with benfotiamine. In both studies, benfoti- from traumatic injuries, infections, metabol- amine significantly lowered gene damage daily doses ranging between ic disorders and exposure to toxins. of PBLs in hemodialysis patients, inde- In a double-blind, randomized, place- 150-320 mg benfotiamine.” pendent of changes in plasma AGE lev- bo-controlled pilot study, 40 subjects with — A Guide to Complementary els. Since the antioxidative activity diabetic PN were given 400 mg benfoti- Treatments for Diabetes by Gene increased in treated patients, this may be amine daily or placebo for three weeks. Bruno (2010, Square One Publishers) the mechanism by which benfotiamine Results showed a statistically significant thy. During weeks five through eight, the ameliorated the DNA damage. improvement in the neuropathy score in dose of benfotiamine was reduced to Chronic renal insufficiency is when the the benfotiamine group compared to 120 mg daily. The results were that ben- filtering capacity of the kidneys are slow- placebo, with the most significant fotiamine led to significant improvement ly and gradually destroyed, and the kid- improvement being a decrease in pain.15 in the entire range of symptoms of alco- neys no longer have enough kidney Other research has demonstrated statisti- holic neuropathy. For some reason the function to maintain a normal state of cally significant effectiveness in reducing benfotiamine-alone group had better health. Many patients with chronic renal nerve pain with daily doses ranging results than the benfotiamine with vita- insufficiency have decreased erythrocyte between 150-320 mg benfotiamine.16 mins B6 and B12 group.19 In a Russian transketolase activity, which is a sign of In addition, several studies have shown study, 14 chronic alcoholic men with neu- thiamin deficiency. In clinical research24, beneficial results when using benfoti- ropathy were given 450 mg benfotiamine 20 patients with end-stage renal disease amine in combination with other B vita- daily for two weeks, followed by 300 mg where supplemented with a single 100 mins in the treatment of diabetic neu- daily for four weeks. The results showed a mg dose of benfotiamine or 100 mg of ropathy.17 In one study18, 30 subjects regression of neuropathy symptoms.20 thiamin nitrate. The results were that received 400 mg benfotiamine and 2,000 patients receiving the benfotiamine mcg of daily for three weeks, Diabetic Retinopathy experienced higher concentrations of a followed by 150 mg benfotiamine and Diabetic retinopathy is the most com- thiamine coenzyme, as well as improved 750 mcg vitamin B12 daily for nine mon diabetic eye disease and a leading erythrocyte transketolase activity. The weeks, and another group of 15 subjects cause of blindness in American adults. It researchers concluded that benfotiamine received a B-complex vitamin supple- is caused by damage to the blood ves- may be of clinical benefit in patients with ment three months. The results were that sels of the retina. In a nine-month ani- end-stage renal disease. all patients treated with benfotiamine and mal study21, researchers administered vitamin B12 experienced significant relief benfotiamine to diabetic rodents to Conclusion in and dramatic determine the potential for retinal pro- Clearly, benfotiamine offers important improvement in vibration perception tection. The results were that benfoti- benefits for individuals with diabetes. thresholds, while subjects receiving a B- amine promoted normal AGE levels in Perhaps most significant is its ability to complex vitamin experienced only slight, the animals’ retina, as well as several reduce AGE formation. This reduction non-statistically significant improvement. key metabolic parameters within the may, in turn, reduce the risk for devel- An eight-week, randomized, multi-cen- animals’ cells. In addition, benfotiamine oping many of the complications associ- ter, placebo-controlled, double-blind inhibited AGE-associated retinal dam- ated with diabetes, including neuropa- study compared the effect of 320 mg age. In an animal and in-vitro study22, thy, nephropathy and retinopathy. benfotiamine alone to 320 mg benfoti- researchers found that that supplemen- For a full list of references, visit amine with viamins B6 and B12 or place- tation with benfotiamine prevented www.vitaminretailer.com and view the bo in 84 alcoholic patients with neuropa- experimental diabetic retinopathy in online edition. JULY 2012 WWW.VITAMINRETAILER.COM VITAMIN RETAILER 39