38 VITAMIN RETAILER WWW.VITAMINRETAILER.COM � JULY 2012

SupplementScience

By Gene Bruno, MS, MHSBenfotiamineBenfotiamineBenfotiamineBenfotiamine is a lipid-soluble form

of thiamine (vitamin B1) oftenconsidered to be the most effec-

tive of the allithiamine group of natural-ly occurring, thiamine-derived com-pounds, found in trace quantities inroasted crushed garlic and other veg-etables from the Allium genus (such asonions, shallots and leeks). It isabsorbed much better than water-solu-ble thiamine salts: maximum plasmalevels of thiamine are about five timeshigher after benfotiamine, the bioavail-ability is at maximum about 3.6 times ashigh as that of thiamine hydrochlorideand better than other lipophilic thi-amine derivates.1

Before further exploring the researchand benefits of benfotiamine, it isimportant to understand the basics ofthiamine since benfotiamine also per-forms the same functions.

A Review of ThiamineThiamine was one of the first organiccompounds to be recognized as a vita-min. In its coenzyme form, thiamine isrequired for a small number of veryimportant enzymes that play criticalroles in the production of energy fromfood, including the production of ATP.2

It is also required for the synthesis ofthe nucleic acids, DNA and RNA.3,4 Adeficiency of thiamine may lead to the

classic deficiency disease “beriberi,”characterized by:5

• Peripheral neuropathy• Muscle pain and tenderness• Rapid heart rate• Enlargement of the heart• Edema (severe swelling due to

water retention)• Congestive heart failure

Causes of Thiamine DeficiencyWhile thiamine deficiency is not commonin the U.S., there are situations in which adeficiency may result from an increasedrequirement or excessive loss of thisnutrient, as well as consumption of anti-thiamine factors. Situations in whichthere is an increased need for thiamineinclude strenuous physical exertion,fever, pregnancy, breast-feeding, adoles-cent growth and HIV-infection (with orwithout AIDS).6 Excessive thiamine lossmay be caused by chronic alcoholabuse/alcoholism7, the use of diuretics8,9

and hemodialysis.10 Anti-thiamin factors,including thiaminases which inactivatethiamin, can also promote a loss of thisvitamin. Consuming large amounts of teaand coffee (including decaffeinated), aswell as habitually eating certain rawfreshwater fish, raw shellfish and fernsare at higher risk of thiamin deficiencybecause these foods contain thiaminasenormally inactivated by heat in cooking.11

Benfotiamine for DiabetesBenfotiamine has particularly valuablebenefits to offer for individuals with dia-betes due to its unusual property ofinhibiting three major pathways of dia-betes-induced vascular damage andneuropathy, and also having value intreating diabetic retinopathy and kidneydamage. The three pathways includethe hexosamine pathway, the advancedglycation end product (AGE) formationpathway and the diacylglycerol (DAG)-protein kinase C (PKC) pathway.12 AGEsare particularly nasty, so inhibition oftheir formation is especially desirable.

Advanced Glycation End Product(AGE)AGEs are formed from glycosylated pro-teins, which in turn are formed when glu-cose has attached itself to protein. Forexample, glucose can attach itself to theprotein in red blood cells’ hemoglobinand form glycosylated hemoglobin, alsocalled hemoglobin A1C, HbA1C, or justA1C for short. If this process continues toexcess, one eventually ends up withAGEs, which become permanent fixturesin cells. AGE impregnated cells are veryreactive and react with one another, andother proteins. In the case of blood capil-laries, they can result in the walls of thecapillaries thickening, eventually causingthe vessels to be blocked off.13

JULY 2012 � WWW.VITAMINRETAILER.COM VITAMIN RETAILER 39

Essentially, AGE reactions create chemicalhandcuffs, which gum up proteins, deac-tivate enzymes, trigger unhealthy bio-chemical signaling in cells and damagesDNA, which contributes to the agingprocess. In a study on diabetic subjects,600 mg of benfotiamine was supple-mented for 28 days. Blood was drawnbefore and after treatment. The resultswere a significant reduction of intracellu-lar glycoxidation and AGE formation.14

Neuropathy Neuropathy is a collection of disorders thatoccurs when nerves of the peripheral nerv-ous system are damaged. This is common-ly referred to as peripheral neuropathy(PN). PN usually causes pain and numb-ness in the hands and feet. It can resultfrom traumatic injuries, infections, metabol-ic disorders and exposure to toxins.

In a double-blind, randomized, place-bo-controlled pilot study, 40 subjects withdiabetic PN were given 400 mg benfoti-amine daily or placebo for three weeks.Results showed a statistically significantimprovement in the neuropathy score inthe benfotiamine group compared toplacebo, with the most significantimprovement being a decrease in pain.15

Other research has demonstrated statisti-cally significant effectiveness in reducingnerve pain with daily doses rangingbetween 150-320 mg benfotiamine.16

In addition, several studies have shownbeneficial results when using benfoti-amine in combination with other B vita-mins in the treatment of diabetic neu-ropathy.17 In one study18, 30 subjectsreceived 400 mg benfotiamine and 2,000mcg of vitamin B12 daily for three weeks,followed by 150 mg benfotiamine and750 mcg vitamin B12 daily for nineweeks, and another group of 15 subjectsreceived a B-complex vitamin supple-ment three months. The results were thatall patients treated with benfotiamine andvitamin B12 experienced significant reliefin neuropathic pain and dramaticimprovement in vibration perceptionthresholds, while subjects receiving a B-complex vitamin experienced only slight,non-statistically significant improvement.

An eight-week, randomized, multi-cen-ter, placebo-controlled, double-blindstudy compared the effect of 320 mgbenfotiamine alone to 320 mg benfoti-amine with viamins B6 and B12 or place-bo in 84 alcoholic patients with neuropa-

thy. During weeks five through eight, thedose of benfotiamine was reduced to120 mg daily. The results were that ben-fotiamine led to significant improvementin the entire range of symptoms of alco-holic neuropathy. For some reason thebenfotiamine-alone group had betterresults than the benfotiamine with vita-mins B6 and B12 group.19 In a Russianstudy, 14 chronic alcoholic men with neu-ropathy were given 450 mg benfotiaminedaily for two weeks, followed by 300 mgdaily for four weeks. The results showed aregression of neuropathy symptoms.20

Diabetic RetinopathyDiabetic retinopathy is the most com-mon diabetic eye disease and a leadingcause of blindness in American adults. Itis caused by damage to the blood ves-sels of the retina. In a nine-month ani-mal study21, researchers administeredbenfotiamine to diabetic rodents todetermine the potential for retinal pro-tection. The results were that benfoti-amine promoted normal AGE levels inthe animals’ retina, as well as severalkey metabolic parameters within theanimals’ cells. In addition, benfotiamineinhibited AGE-associated retinal dam-age. In an animal and in-vitro study22,researchers found that that supplemen-tation with benfotiamine preventedexperimental diabetic retinopathy in

rats, and completely prevented increas-es in AGE and PKU activity. This sug-gests that benfotiamine may help pre-vent or delay the progression ofmicrovascular changes in patients withdiabetic retinopathy.

Kidney DamageHemodialysis patients have an elevatedlevel of damage to their genes in periph-eral blood lymphocytes (PBLs) and anincreased cancer incidence, possibly dueto accumulation of toxins like AGEs.Since benfotiamine reduces AGE levels,and since hemodialysis patients tendtoward vitamin B1 deficiency, researchersconducted two consecutive studies23 sup-plementing hemodialysis patients withbenfotiamine. In both studies, benfoti-amine significantly lowered gene damageof PBLs in hemodialysis patients, inde-pendent of changes in plasma AGE lev-els. Since the antioxidative activityincreased in treated patients, this may bethe mechanism by which benfotiamineameliorated the DNA damage.

Chronic renal insufficiency is when thefiltering capacity of the kidneys are slow-ly and gradually destroyed, and the kid-neys no longer have enough kidneyfunction to maintain a normal state ofhealth. Many patients with chronic renalinsufficiency have decreased erythrocytetransketolase activity, which is a sign ofthiamin deficiency. In clinical research24,20 patients with end-stage renal diseasewhere supplemented with a single 100mg dose of benfotiamine or 100 mg ofthiamin nitrate. The results were thatpatients receiving the benfotiamineexperienced higher concentrations of athiamine coenzyme, as well as improvederythrocyte transketolase activity. Theresearchers concluded that benfotiaminemay be of clinical benefit in patients withend-stage renal disease.

ConclusionClearly, benfotiamine offers importantbenefits for individuals with diabetes.Perhaps most significant is its ability toreduce AGE formation. This reductionmay, in turn, reduce the risk for devel-oping many of the complications associ-ated with diabetes, including neuropa-thy, nephropathy and retinopathy.

For a full list of references, visitwww.vitaminretailer.com and view theonline edition.

“Benfotiamin is a particularly

well-absorbed form of vitamin B1.

Double-blind research in

diabetics demonstrated that oral

doses of 400 mg daily resulted in

a statistically significant

improvement in neuropathy score

in the treatment group

compared to placebo. The most

significant improvement reported

was pain decrease in

polyneuropathy (a type of

peripheral neuropathy). Other

research has demonstrated

statistically significant

effectiveness in reducing

diabetic neuropathy pain with

daily doses ranging between

150-320 mg benfotiamine.”

— A Guide to ComplementaryTreatments for Diabetes by GeneBruno (2010, Square One Publishers)