VITAMIN B9, FOLATE & FOLIC ACID
Written by Slawomir Gromadzki, MPH
Vitamin B9, commonly known as folate or folic acid, is a water-soluble vitamin used in just about every process in the body and is absolutely essential throughout every stage of life.
FORMS OF VITAMIN B9
– Folate, naturally found in various foods.
– Folic acid (known also as pteroylmonoglutamic acid) is a synthetic form of vitamin B9 and it is commonly used to fortify food and as a nutritional supplement in multivitamins, including prenatal formulas. Unfortunately, in people who can’t properly metabolise this synthetic form of vitamin B9, it becomes unusable by the body and starts accumulating and preventing the absorption of natural folate from food sources, leading to folate deficiency and associated with its health problems. It also increases the risk of certain forms of cancer.
– L-methylfolate: Like folic acid, l-methylfolate is also found in supplements but it is a biologically active form of vitamin B9 and therefore safe. Unlike folic acid, it doesn’t require an enzyme for its conversion. This fact, therefore, eliminates the same risk which is associated with taking folic acid. L-methylfolate appears to be particularly beneficial for those with MTHFR mutation, as they can’t metabolise folic acid.
– Folacin is just another name used interchangeably for folic acid and folate.
BIOAVAILABILITY OF NATURAL FOLATE VS SYNTHETIC FOLIC ACID
Interestingly, some studies have demonstrated that absorption of folic acid is actually slightly higher than the absorption of folate from food sources. According to a study published in the American Journal of Clinical Nutrition, the natural folate found in various types of food is about 78 per cent as bioavailable as folic acid. Unfortunately, the problem is there are many people who are not able to metabolise it properly.
DO WE NEED SUPPLEMENTS WITH FOLIC ACID?
Unless you are pregnant there’s no need to supplement folic acid if you consume foods high in natural folate. In case supplementation is required try using only vitamin B9 in the form of L-methylfolate and not folic acid.
FOOD SOURCES OF NATURAL FOLATE
Folate is found in a variety of vegetables, fruits, pulses (legumes) and seeds. The highest and best source of folate are leafy greens such as especially raw spinach.
Other good sources include black-eyed peas, seaweed, sunflower seeds, leeks, turnip greens, mustard greens, collard greens, cauliflower, beets, beans, lentils, and sweet peppers.
Beef and chicken liver is also high in folate but I wouldn’t recommend it as it greatly increases the risk of cancer and other serious health problems.
AMOUNT OF FOLATE (IN MCG) PER ½ CUP
Spinach (raw) 130
Black-eyed peas 110
Asparagus 90
Brussels sprouts 80
Avocado 60
Broccoli 50
Romaine Lettuce 50
FOLATE DEFICIENCY SYMPTOMS
Fatigue and tiredness, anaemia (usually combined with B12 deficiency), painful mouth sores, poor memory and focus, low mood, depression, insomnia, dark skin spots, etc.
Increased risk of birth defects is also linked to the deficiency of folate (and vitamin B12).
HEALTHY LEVELS PREVENT CANCER BUT EXCESS FOLIC ACID MAY INCREASE THE RISK
According to various studies, maintaining adequate levels of folate through consuming foods high in it or by supplementing with folic acid reduces the risk of colorectal, oesophageal, breast, ovarian and pancreatic cancers.
However, it was also found that excess folic acid (synthetic form of vitamin B9) intake from supplements and fortified foods may actually increase the risk of prostate and colorectal cancer.
Folate protects our cells from becoming abnormal cancer cells by preventing DNA mutations. However, folate also stimulates proliferation (multiplication of cells), because it is necessary for the synthesis of certain DNA nucleotides. It means that in case of someone who already has a cancer growing, folate will probably encourage cancer to grow bigger. Because of this risk part of the chemotherapy program used in the attempt to kill cancer involves anti-folate drugs. Unfortunately, it doesn’t seem to be a wise solution because although these drugs may slightly slow down the growth of the existing tumour, yet at the same time by blocking folate they also encourage further DNA mutations, leading to metastasis from the tumour and an increased risk of new cancers.
I think in case of cancer patients the best way to maintain normal folate levels is by consuming raw vegetable juices from leafy greens such as spinach with the addition of carrots and beets (or taking supplements such as super greens powders) as they are known to have powerful anti-cancer properties.
OVERDOSING FOLIC ACID
Possible excess folic acid side effects may include difficulty sleeping, increased risk of epileptic seizures, changes in mood and in sex drive, or increased risk of cancer.
EXCESS FOLIC ACID MASKS VITAMIN B12 DEFICIENCY
Vitamin B12 deficiency is a common problem today especially among elderly people because after 60 we usually stop producing intrinsic factor required for proper metabolism and absorption of vitamin B12. Unfortunately, excess folic acid intake from supplements and fortified foods makes the problem even worse because it masks vitamin B12 deficiency. It means that too high levels of folic acid in the body make impossible to detect B12 deficiency. Untreated chronic deficiency of this very important vitamin leads to serious nerve damage and neurological changes with symptoms similar to those of multiple sclerosis, including even paralysis.
In addition, taking folic acid supplements without high dosages of vitamin B12 in the form of sublingual methylcobalamin makes B12 deficiency even worse. In one study, consumption of folic acid in excess of 400 micrograms per day among older adults resulted in a significantly faster rate of cognitive decline! Another study found a higher prevalence of both anaemia and cognitive impairment in association with high folic acid intake in older adults with a low vitamin B12 status.
MTHFR MUTATION RISK
Folic acid (pteroylmonoglutamic acid) – is a synthetic and inactive form and therefore in human body requires MTHFR enzyme for its conversion to bioactive form. In people who are deficient in MTHFR enzyme, folic acid can’t be converted and properly metabolise. As a result, it becomes unusable by the body and starts accumulating and preventing the absorption of natural folate from food sources, leading to folate deficiency and associated with its health problems. Research suggests that it may also increase the risk of certain forms of cancer. In this case supplemental L-methylfolate – a biologically active form should be used by people who can’t metabolise folic acid due to MTHFR mutation.
There are sources, however, that claim the above is not true: “You might have read or heard that folic acid is not safe if you have one or two copies of the MTHFR C677T variant. This is not true. Even if you have one or two copies of the MTHFR C677T variant, your body can safely and effectively process the different types of folate, including folic acid.” (>)
The synthetic form of vitamin B9 known as folic acid requires an enzyme (made by MTHFR gene) which is to convert it in the body into a usable form. Unfortunately, some of us may be either deficient in that enzyme or it may be very inefficient in the conversion process. As a result, the unmetabolized folic acid builds up and accumulates in the plasma and tissues increasing the risk of prostate and colorectal cancer.
In addition, the unusable for people with MTHFR mutations folic acid plugs the receptor sites in cells not allowing the usable folate to attach itself to the receptor and be used. In this way, the body cells are deprived of folate leading to folate deficiency and associated with it very serious health problems.
MTHFR is a gene that provides the body with instructions for making an enzyme called methylenetetrahydrofolate reductase which is required in our body to convert folic acid (the synthetic form of vitamin B9) into the usable form. Since individuals with MTHFR mutations are unable to properly convert folic acid they actually experience worsened symptoms from taking supplements containing folic acid.
The form of folate that can enter the main folate metabolic cycle is tetrahydrofolate (THF). Unlike natural folate, which is metabolized to THF in the mucus of the small intestine, folic acid must first be reduced in the liver and then be converted to THF form, which process requires enzyme dihydrofolate reductase. Unfortunately, the low activity of this enzyme in the liver, combined with a high intake of folic acid from supplements and fortified foods, may result in accumulation of unnatural levels of unmetabolized folic acid.
Fortunately, there is an excellent solution to the problem in the form of avoiding folic acid, consuming foods high in natural folate and supplementing with l-methylfolate or fermented folic acid, as both are processed by the body more like folate. The strength of L-methylfolate in supplements is usually lower than that of folic acid as it is more difficult to pack into capsules, so if your require higher dosages you try to find supplements with a fermented folic acid, which is bio-transformed into a more bioavailable form by friendly yeasts.
Please keep in mind that apart from supplements folic acid is also found in processed cereals, commercial flour, or grain-based processed foods.
RECOMMENDED DAILY INTAKE AND DOSAGES
The upper limit of folic acid from supplements and fortified foods is 1,000 micrograms per day.
An average adult person needs about 400 micrograms of folate. Pregnant or breastfeeding women need 600 and 500 mcg, respectively. Try to get this amount from mentioned above natural sources but if you are unable to do it you need supplements.
With regards to supplementation, a better option than folic acid is L-methylfolate because it is a biologically active form of vitamin B9 and unlike folic acid, it doesn’t require enzyme for its conversion which eliminates the risk of harmful accumulation of unmetabolized folic acid and its consequences.
HOW TO FIND PROPER SUPPLEMENT?
Read the labels and make sure ingredient list specifies the right form. Beware of supplements that list only “folate”, “methylfolate”, or “5-MTHF” without specifying the exact form. The ingredient list must include L-methylfolate (5-methyltetrahydrofolate) (5-MTHF in short), 6(S)-methylfolate, metafolin, or quatrefolic ((6S)-5-Methylfolate, glucosamine salt) as these are biologically active forms of vitamin B9.
Don’t buy supplements that contain vitamin B9 in the form of folic acid as well as D-methylfolate and 6(R)-methylfolate because both are regarded as biologically inactive and should be avoided.
When you find right supplements also compare the strength and check how much L-methylfolate per capsule they have. Generally, they contain 400 mcg to 5000 mcg per tablet/capsule. Make sure you’re also getting a high enough dose of 5-MTHF folate to meet your needs.
I wouldn’t recommend high doses of even methylfolate to anyone who already suffers from cancer.
The most commonly found 5-MTHF supplements use calcium salt while newer form called quatrefolic uses glucosamine salts claiming better solubility in water and enhanced bioavailability. In reality, however, it looks that although it is absorbed faster yet at the same time the lower percentage is actually absorbed compared to calcium salt-based methylfolates.
POSSIBLE METHYLFOLATE SIDE EFFECTS
In those who have MTHFR mutations (especially the C677T MTHFR mutation) methylfolate is critical to take – and folic acid is critical to avoid. Unfortunately, the problem is that methylfolate can sometimes cause more harm than good if not started at the right time and with smaller dosages increased gradually. It is believed the side effects are linked to methylation, pre-existing inflammation, overall nutrient status and other genetic mutations. Some people just don’t do well with methylfolate and if this is your case it is better to not force it. You can consume leafy greens instead or stop taking the supplement for a week or so and start again by taking small doses and increase gradually.
Possible side effects may include rash, irritability, headaches, insomnia, anxiety, sore muscles, joint pain, acne, palpitations, nausea, runny nose, migraines, neurological sensations, etc. Read more >
EXAMPLES OF GOOD SUPPLEMENTS
Let me give you a few examples of good folate supplements:
– Solgar – Folate 800 mcg (as Metafolin®) Tablets
– Swanson – Ultra Folate 5-Methyltetrahydrofolic Acid 400 mcg (as Quatrefolic® [6S]-5-methyltetrahydrofolic acid equivalent to 800 mcg of [6S]-5-methyltetrahydrofolic acid, glucosamine salt)
– LifeExtension – High Potency Optimized Folate (L-Methylfolate), 5000 mcg: Folate [as (6S)-5-Methyltetrahydrofolic acid, calcium salt] 5000 mcg
– Cytoplan – Methylfolate: 400 mcg of Methylfolate per capsule
– NOW – Methylfolate [1.000 mcg (6S)-5-MTHF] [from Quatrefolic (6S)-5-MTHF Glucosamine Salt]: 1.667 mcg
TAKE L-METHYLFOLATE WITH SUBLINGUAL METHYLCOBALAMIN FORM OF B12
Since methylfolate works very closely with vitamin B12 for methylation and for the production of energy and healthy red blood cells, take L-methylfolate with sublingual methylcobalamin form of vitamin B12 which is much more effective than cyanocobalamin B12. Remember that methylcobalamin must be sublingual (designed to dissolve under the tongue). It is important because swallowed methylcobalamin will be lost in the digestive process.
KEY HEALTH BENEFITS OF FOLATE
FOETUS DEVELOPMENT
Getting enough folate is very important before and during pregnancy (especially three months before conception and during the first trimester of pregnancy). Vitamin B9 is very important during the preconception and pregnancy as it increases the chances of conceiving and is required for proper foetus development. For this reason public health authorities recommend that, all women of childbearing age should consume 400 micrograms of folic acid (or even better L-methylfolate) daily to prevent neural tube birth defects and other malformations in the developing babies.
REQUIRED FOR HEALTHY BRAIN, MOOD AND NERVOUS SYSTEM FUNCTION
Folate prevents cognitive decline and dementia including Alzheimer’s disease. It is particularly important for maintaining healthy nervous system and brain function supporting strong memory, good mood, and focus.
Folic Acid is important to nourish the brain and promote a healthy nervous system function. A recent study found that patients suffering from dementia had low levels of folate. Another study found that participants who were taking a daily dose of 400 mcg Folic Acid cut their risk of memory loss in half. Folic Acid is also involved in the synthesis of Serotonin – regarded as the most powerful natural antidepressant good mood hormone.
CARDIOVASCULAR HEALTH
Vitamin B9 also contributes to the maintenance of healthy heart function, normal blood pressure, blood cholesterol and glucose levels. Scientific research has already demonstrated strong evidence that Folic acid when paired with Vitamin B12 can effectively keep blood homocysteine levels under control. Homocysteine is a type of amino acid that can contribute to the formation of blood clots and cause arteries to narrow and harden. A recent study found that taking a 0.4 mg of Folic Acid supplement for 12 weeks could reduce bad cholesterol levels. A large study also showed that supplementation with Folic acid could promote normal blood pressure.
HEALTHY METABOLISM, BODY WEIGHT AND ENERGY LEVELS
Folic acid is required for normal blood formation, including formation of red blood cells which carry oxygen around the body energising every cell including brain cells. Its deficiency, therefore, is the frequent cause of fatigue and anaemia in both children and adults.
The most common complaint today is fatigue which is often caused by Folic Acid deficiency. Fortunately, it can be easily reversed by supplementation of this Vitamin. Folic Acid helps us to feel better as it is involved in the production of oxygen-carrying red blood cells. It also contributes to the control of body weight and maintenance of energy levels by converting carbohydrates into glucose, which is the preferred source of energy.
HELPS INCREASE GLUTATHIONE LEVELS
Folic acid (Vitamin B9) contributes to normal amino acid (protein) synthesis, including the production of glutathione (the ‘king’ of all antioxidants) which reduces oxidative damage caused by free radicals, reduces the risk of cancer, heart attacks, strokes and fatigue, slows down the ageing process and make our immune system much stronger.
IMPORTANT FOR NORMAL PIGMENTATION OF THE SKIN
Folic acid deficiency may lead to hyperpigmentation of the skin, contributing to dark spots, also known as liver or age spots.
OTHER BENEFITS
Folate may also help support strong bones (by reducing homocysteine which increases risk of osteoporosis).
Studies show that low levels of folate may be associated with the development of restless legs syndrome, especially during pregnancy.
SOURCES
– https://www.drmcdougall.com/misc/2005nl/oct/051000folic.htm
– https://draxe.com/folic-acid-foods/
– https://draxe.com/mthfr-mutation/
– Amymyersmd.com MTHFR Mutation
– Bulletproof, Dr. Ben Lynch: MTHFR Gene, Beating Disease, and Folic Acid
– Worlds Healthiest Foods, Folate
Folic Acid Supplements are a Health Hazard
Stop Folic Acid Pills Now
Limit Your Intake of Fortified Flour Products (in the USA)
By Dr John McDougall
Don’t Lower Your Homocysteine Levels with Supplements
Taking supplements with as little as 0.8 mg/day of folic acid has been shown to increase your risk of dying of heart disease and cancer, according to the results of the first large randomized treatment trial to carefully examine this issue.1 The Norwegian Vitamin Trial (NORVIT) of 3,749 patients, who were followed for 3.5 years was designed to show the benefits of taking supplements—but the results were contrary to expectations. Folic acid supplementation was found to lower homocysteine levels by 28%., but to increase relative risks of heart attack, stroke, and death by 20%, along with a more than a 30% increase in cancer. Those with the highest baseline homocysteine levels (13 umol/L or greater) suffered the most harm from taking supplements of folic acid.
Folic Acid Supplements Overload the Body
Consuming more than 0.2 mg of folic acid daily floods the bloodstream with this vitamin, overloading the metabolic capacities of the body, causing imbalances that increase the risk of heart disease and cancer.2 Folic acid is a synthetic version of the natural vitamin, folate, found in plant foods. Folate from food is essential for good health. Folic acid sold in capsules is a medication at best and a toxin at worst. When given in doses of 0.8 mg it will lower homocysteine by about 30% (3 to 4 umol/L).3 Higher doses than 0.8 mg have no greater benefit for lowering blood levels of homocysteine.
Folic Acid Mandated for U.S. Cereal Products
January 1998 was the mandatory deadline for the fortification of grain products with folic acid in the United States. Folic acid was added to flours used to make bread, rolls, and crackers. Another hefty source of this supplement comes from enriched (vitamin-added) “ready-to-eat cereals.”
Since 1998, folic acid intake has increased significantly in every segment of the U.S. population with the average additional intake of 0.22 mg/day.3,4 Remember, as little is .2 mg causes overloads and imbalances with an increased risk of illness. A significant segment of the USA population is now consuming over 1 mg/day of folic acid daily—an amount found by the NORVIT study to increase the risk of heart disease and cancer.
Doctors Harm Patients with Supplements
Cardiologists are fond of recommending vitamin pills to treat elevated homocysteine in hopes of preventing further heart disease in their patients. One of the most commonly prescribed preparations is called Foltx – a combination of 2.5 mg (2,500 mcg) of folic Acid, 25 mg of vitamin B6, and 2 mg of vitamin B12. A recent study showed a similar preparation reduced the homocysteine levels of patients with a history of stroke by 2 units (umol/L), but found no difference in risk of future strokes, heart attacks, or death compared to a control group.5
Another recent study showing folic acid actually causes the heart arteries to close should cause doctors to mend their prescribing practices. After six months of supplementation in 636 heart patients with stents (stents are wire-mesh supports placed in the coronary arteries during angioplasty), the Folate After Coronary Intervention Trial found those patients taking folic acid had significantly more narrowing of the arteries, more artery closure (restenosis), and more major adverse cardiac events compared to those taking placebo—the exact opposite of what investigators had expected to find.6,7 As expected, the homocysteine blood levels were reduced by the above treatment. The authors recommended that the routine administration of folate treatment not be advocated at the present time.
Even with all this condemning evidence, you can easily find experts (many working with vitamin companies) trying to convince the unaware buyer that high-dose folic acid supplementation—as much as 5 mg/day—will be good for their heart and blood vessels.8
Appropriate Response to Homocysteine in Your Blood
The main motivation behind fortification of flours and taking supplemental vitamins has been to reduce the occurrence of serious birth defects, especially the occurrence of neural tube defects (NTDs). The effort seems to be working a little—since the onset of fortification there has been a 19% decrease in the incidence of NTDs. Unfortunately, these same widespread recommendations to take folic acid may be causing more heart disease and cancer. So, what to do?
All that money and effort now spent on supplementation with the hope of reducing birth defects, heart disease, and cancer should be directed towards educational programs to teach people to eat more legumes, vegetables, and fruits—the plentiful and safe sources of folic acid. (The name folic comes from the word foliage, which refers to plants.) When packaged in the plant, folic acid is never harmful and always beneficial. Further efforts should be made towards making sure all people have ready access to plant-foods.
Because of the overwhelming evidence that the vitamin supplements people are buying are a serious health hazard, I propose these products be labeled with bold warnings like: “Taking Vitamin E can raise your risk of dying,” Vitamin A (retinol) can damage your bones and cause birth defects,” and “Folic acid causes heart disease.” All supplement packages should also tell people that vitamins and other nutrients are best obtained from healthy vegetable foods. For more information on the hazards of supplementation, please read from my newsletter archives the following:
August 2003: Plants, not Pills, for Vitamins and Minerals:http://www.nealhendrickson.com/mcdougall/030800puvitaminsandminerals.htm
November 2004: Vitamins Do Not Prevent Cancer and May Increase Likelihood of Death: How Supplements Can Make You Sicker
http://www.nealhendrickson.com/mcdougall/2004nl/041100pufavorite5.htm
July 2005: Neither Aspirin Nor Vitamin E Will Save Women
https://www.drmcdougall.com/misc/2005nl/july/050700fav5.htm
February 2004: Treating Homocysteine with Vitamins Fails
http://www.nealhendrickson.com/mcdougall/040200pufavorite5.htm
References:
1) Bonaa KH. NORVIT: Randomized trial of homocysteine-lowering with B-vitamins for secondary prevention of cardiovascular disease after acute myocardial infarction. Program and Abstracts from the European Society of Cardiology Congress 2005; September 3-7, 2005; Stockholm, Sweden. Hot Line II.
2) Quinlivan EP, Gregory JF 3rd. Effect of food fortification on folic acid intake in the United States. Am J Clin Nutr. 2003 Jan;77(1):221-5.
3) Homocysteine Lowering Trailists Collaboration. Dose-dependent effects of folic acid on blood concentrations of homocysteine: a meta-analysis of the randomized trials. Am J Clin Nutr. 2005 Oct;82(4):806-812.
4) Choumenkovitch SF, Selhub J, Wilson PW, Rader JI, Rosenberg IH, Jacques PF. Folic acid intake from fortification in United States exceeds predictions. J Nutr. 2002 Sep;132(9):2792-8.
5) Toole JF . Lowering homocysteine in patients with ischemic stroke to prevent recurrent stroke, myocardial infarction, and death: the Vitamin Intervention for Stroke Prevention (VISP) randomized controlled trial. JAMA. 2004 Feb 4;291(5):565-75.
6) Lange H. Folate After Coronary Intervention Trial” (FACIT). http://www.accitalia.it/congress_centre/meeting_int/detail.asp?acr_trial=FACIT
Lange H. The folate after coronary intervention trial (FACIT). Scientific presentation at the 52nd Annual Scientific Sessions of the American College of Cardiology, Chicago, March 30th, 2003.
7) Schnyder G, Roffi M, Flammer Y, et al. Effects of homocysteine-lowering therapy on restenosis after percutaneous coronary intervention for narrowings in small coronary arteries. Am J Cardiol 2003; 91:1265-1269.
8) LifeExtension: http://www.lef.org/magazine/mag2005/mar2005_report_folic_01.htm?source=Google&
SOURCE OF THE ABOVE ARTICLE: https://www.drmcdougall.com/misc/2005nl/oct/051000folic.htm