Clinical Applications
METHYLATION ENZYME ACTIVATORS is manufactured in a Federal Drug Registered and State Board Pharmacy cGMP laboratory
METHYLATION ENZYME ACTIVATORS is a comprehensive formula featuring significant amounts of five nutrients that support optimal methylation and help maintain healthy homocysteine
levels in the blood.
• Support Healthy Homocysteine Levels
• Support Healthy Methylation of Estrogen, Dopamine, Epinephrine, Heavy Metals,
Environmental Toxins
• Repletion of Nutrients Potentially Depleted by Use of Oral Contraceptives
Folic Acid (as folic acid) in the amount of 2000 mcgs is five times the content of many non-prescription supplements on the market. A number of studies have found no benefit of methyltetrahydrofolate (MTHF) supplementation over regular folate for lowering plasma homocysteine.1,2,3 Although lower doses of folic acid are usually efficacious, “many individuals with cardiovascular disease and kidney disease are refractory to these lower levels and require significantly higher levels of folic acid supplementation.”4 Nearly all large intervention trials that combined folic acid with other vitamins used at least 2 mg of folic acid per day. 4 Larger doses of folate increase nitric oxide production by the endothelium.5 Besides cardiovascular support, folic acid has important roles in detoxification, nervous system function, breast tissue health, and prenatal development.
Trimethylglycine (as anhydrous betaine), found in several tissues in humans, acts as an alternative methyl donor in homocysteine metabolism. Betaine is synergistic with folic acid and also supports healthy fasting plasma homocysteine. Betaine may also be a preventive agent against the activation of NF-kappaB induced during inflammation and aging.6
Vitamin B12 (as methylcobalamin) is another methyl donor. Cyanocobalamin, the form of B12 present in many supplements, has to be converted in the liver to methylcobalamin. The important enzyme, methyltetrahydrofolate reductase that converts folic acid to a form of methyltetrahydrofolate is vitamin B12 dependent demonstrating the synergism of this formula. Addition of B12 to a folate regimen lowered homocysteine an extra 7%. 7
Vitamin B6 (as pyridoxal 5’ phosphate), the coenzyme form of vitamin B6 is the primary bioactive form. It is a coenzyme in approximately 100 enzymatic reactions.8 The Framingham Study population showed an inverse association between homocysteine and vitamin B6 (as well as B12 and folate).9
Vitamin B2 (as riboflavin 5’phosphate) is the principal coenzyme form of riboflavin used in many oxidative reactions. Folate and riboflavin interact to lower plasma homocysteine, possibly by maximizing the catalytic activity of MTHFR. The effect may be unrelated to MTHFR genotype.10
References
1. Lamers Y, Prinz-Langenohl R, Moser R, Pietrzik K. Supplementation with [6S]-5-methyltetrahydrofolate or folic acid equally reduces
plasma total homocysteine concentrations in healthy women. Am J Clin Nutr. 2004 Mar;79(3):473-8.[ PMID: 14985224 ]
2. Pentieva K, et. al. The short-term bioavailabilities of [6S]-5-methyltetrahydrofolate and folic acid are equivalent in men: J Nutr,
2004 Mar;134(3):580-5 [PMID:14988450]
3. Venn BJ,Comparison of the effect of low-dose supplementation with L-5-methyltetrahydrofolate or folic acid on plasma homocysteine:
a randomized placebo-controlled study. Am J Clin Nutr. 2003 Mar;77(3):658-62 [PMID:12600857]
4. Guilliams, T.G. Homocysteine- A risk factor for vascular diseases: guidelines for the clinical practice. Jour Amer Nutra Assoc.
Vol 7(1) Winter, 2004
5. Hanneke W. Wilmink; Erik S. G. Stroes; Willem D. Erkelens; Arteriosclerosis, Thrombosis, and Vascular Biology. 2000;20:185
6. Go EK, Jung KJ, Kim JY, Yu BP, Chung HYBetaine Suppresses Proinflammatory Signaling During Aging: The Involvement
of Nuclear Factor-{kappa}B via Nuclear Factor-Inducing Kinase/I{kappa}B Kinase and Mitogen-Activated Protein Kinases. J
Gerontol A Biol Sci Med Sci. 2005 Oct;60(10):1252-1264 [PMID: 16282556]
7. Venn BK,Green TJ, Moser R, McKenzie JE, Skeaff CM, MannJ Increases in blood folate indices are similar in women of
childbearing age supplemented with [6S]-5-methyltetrahydrofolate and folic acid. J Nutr 2002 Nov;132(11):3353-5.
8.Strain JJ, Dowey L, Ward M, Pentieva K, McNulty H. B-vitamins, homocysteine metabolism and CVD. Proc Nutr Soc. 2004
Nov;63(4):597-603. [PMID: 15831132]
9. Selhub, J. 2006. The many facets of hyperhomocysteinemia: studies from the framingham cohorts. Journal of Nutrition. 136(6
Suppl):1726S-1730S.
10. Moat, SJ. et al. Effect of riboflavin status on the homocysteine-lowering effect of folate in relations to the MTHFR (C6775)
genotype.
