Tocotrienols – What Are They?
When you think of vitamin E, the first thing that comes to mind is the lipid-soluble nutrient that’s a great antioxidant and performs wonders for your skin.
In fact, before the mid-1960s, any mention of vitamin E simply meant tocopherol and specifically alpha-tocopherol. However tocopherol is only half of what vitamin E is.
Read on and discover what may be vitamin E’s better half… Tocotrienol and more specifically Annatto Tocotrienol.
“The health benefits realized by annatto tocotrienol go beyond that of any
other nutrient I know. It’s the one supplement I would want with me if I
were stranded on a desert island! This is a change for me as after 35 years
in this industry, my top desert island supplements have switched between
magnesium and fish oil and now it stands firmly as annatto tocotrienol alone.”
— JONATHAN LIZOTTE, DESIGNS FOR HEALTH FOUNDER AND BOARD CHAIRMAN.
TOCOTRIENOLS, WHAT ARE THEY?
To many people, vitamin E is associated with tocopherols, specifically alpha-tocopherol and rightly so because it was the first form of Vitamin E to be discovered and extensively studied.
So, what are tocotrienols and how did they come about? Often referred to as the lesser-known form of natural vitamin E, tocotrienols account for about 1% of the vitamin E research.
In 1959, the term “tocotrienol” was first coined by Bunyan J. and others in a 1961 study. Research has established that tocotrienols and tocopherols are sister compounds of vitamin E, but they exhibit certain molecular differences and consequently functional differences.
Vitamin E is a molecular compound composed of two isoforms, tocotrienols and tocopherols. Each of these isoforms is further divided into four isomers denoted by the Greek alphabet letters alpha (α), beta (β), gamma (γ), delta (δ), bringing the total to eight members of the vitamin E family.
An analogy from Dr. Tan adopted from American River Nutrition, Inc, helps us to understand the structural and functional differences between tocotrienols and tocopherols.
He describes tocopherols as policemen, who patrol and maintain order within a township, ensuring its people are safe from radical elements. Thanks to their bigger heads and bigger tails, they move slowly and cover a smaller area. And tocotrienols as state troopers, that crisscross county boundaries to ensure their citizens are safe from radicals statewide. Because they must cover a large area, they move extremely fast thanks to their smaller heads and tails. In terms of their antioxidant effectiveness, tocotrienols are 50 times more superior than tocopherols.
The molecular structure of tocotrienols can get very complicated but their most important elements are the chromanol ring that makes them potent free radical scavengers and their farnesyl tail that has a cholesterol-lowering ability.
Apart from slowing down the process of cholesterol formation the superiority of tocotrienols over tocopherols extends to other areas such as helping reduce the risks associated with metabolic syndrome, bone injuries, diabetes, skin health and cancer as will be discussed in the sections that follow.
WHERE CAN TOCOTRIENOLS BE FOUND?
If tocotrienols are that superior, where can they be sourced from? Well, the truth is that tocotrienols are naturally found in sources such as palm, wheat germ oils, rice bran, barley, and annatto. Most of these sources come with a natural mixture of both tocotrienols and tocopherols.
Before proceeding any further, it is important to point out that the presence of tocopherols interferes with the functioning of tocotrienols. Therefore, the best tocotrienols sources are those with the least to zero amounts of tocopherols. In scientific terms, a source is tocopherol-free when its measurable quantity of alpha-tocopherol is below 0.1%.
Going back to some of our sources mentioned above, the tocotrienol-to-tocopherol ratio is as follows, rice (50:50) and palm (75:25). Therefore, palm and rice bran will give you 25 -50% of tocopherols, mostly alpha-tocopherols. On the flipside, annatto is tocopherol-free. At worst, its ratio would be 99.5:0.5, thus making it the best source of pure, naturally-derived tocotrienols.
Annatto doesn’t require any synthetic curation and contains two of the best forms of tocotrienols, gamma and delta-tocotrienols. Therefore, with the interference of alpha-tocopherol chemically absent, annatto tocotrienols guarantee you the best outcomes in enhancing cellular health and lowering cholesterol levels.
Today, tocotrienols are available mainly through supplements and are almost synonymous with Dr. Barrie Tan, a Malaysian professor, researcher, and scientist whose extensive research has dubbed him the Vitamin E expert. Dr. Tan’s discovery in 2002 of the annatto plant’s properties is revolutionary.
Dr. Tan’s interest in carotenoids (naturally-occurring pigments-red, orange, and yellow- synthesised by algae, plants, and photosynthetic bacteria) led him to the Amazon rainforest where he stumbled on annatto.
Similar to the Southeast Asian rambutan fruit plant, annatto has about 20 to 30 seeds per pod and they're intensely red hence the name lipstick plant. When he touched the annatto fruit, it intensely stained his hand with a maroon colour.
As opposed to the inherent instability of carotenes, annatto is stable and its colour sticks much longer. While he didn’t expect it to be a tocotrienol he immediately suspected that it must contain a powerful antioxidant. Following further research, he found to his amazement that annatto not only contained tocotrienol (delta-tocotrienol) but had no traces of tocopherol thus making it one of the purest sources.
Dr. Tan has conducted lots of clinical trials for the past 20 years and published research work that has systematically shown that delta tocotrienols are effective in fighting chronic conditions amongst them cancer, osteopenia, and NAFLD fatty liver. The key benefits of annatto tocotrienols are manifested in their potency in combating inflammation and oxidative stress.
We at Youth and Earth have used this invaluable research and have our own supplement Tocotrienols EAnnato Delta Gold. Our Tocotrienols come from the annatto bean too and contain 90% Delta-Tocotrienol and 10% Gamma-Tocotrienol.
HOW DO TOCOTRIENOLS WORK
Simply put, tocotrienols can degrade HMG-CoA reductase, which is a key enzyme that determines how cholesterol is formed. Metabolic pathways form cholesterol in animal cells as well as humans. A factor of this pathway is the sterol regulatory element-binding proteins (SREBPs) which function like “on and off “switches that control cholesterol and fatty acid biosynthesis.
Tocotrienols, specifically gamma and delta-tocotrienols, are effective both in degrading HMG-CoA reductase and blocking the gene expression of SREBPs. This double whammy slows down lipid storage and prevents cholesterol biosynthesis. For diabetic and obese patients, this leads to a positive health outcome.
Tocotrienol Absorption and Bioavailability
Tocotrienols are fat-soluble, which means they must be consumed together with dietary fats. In the first phase also called the lipid phase, the tocotrienols are dissolved in lipids. Thereafter, the lipid droplet mixture is absorbed by the cells of our intestines. Here the lipids are transported through the gut, to the bloodstream and finally the liver.
At the liver, the remnants of these structures are degraded and repackaged into lipoprotein “fat shuttles” and dispersed to peripheral tissues. Research has shown that tocotrienols split faster from the lipoprotein shuttles and get deposited in organs such as the lungs, spleen, kidneys, brain, and heart.
Tocotrienols get absorbed fast into the tissues hence their lower levels in the blood. This impacts positively on their bioavailability compared to tocopherols that remain attached to the lipoproteins throughout circulation to and fro the liver. Studies on the rapid uptake of tocotrienols reveal that within 2-5 hours of taking tocotrienols with a meal, their levels in the blood peak.
IMPORTANCE OF TOCOTRIENOLS WITHOUT TOCOPHEROL
Tocopherols not only fail in lowering cholesterol levels but worse still interfere with the working of tocotrienols, if co-administered. According to studies this negative interference happens in several ways some of which include:
- Lowering the antioxidant capacity of tocotrienols
- Blocking the absorption of tocotrienols
- Limiting the storage of tocotrienols in the adipose tissue
- Blocking the anticarcinogenic potency of tocotrienols
- Causing a breakdown of tocotrienols
- Lowering the cholesterol and triglyceride activity of tocotrienols
Therefore, when supplementing with tocotrienols such as annatto tocotrienol, you may want to avoid co-administering with tocopherols, especially alpha-tocopherol.
HOW DO TOCOTRIENOLS FIGHT CANCER?
However, in cancerous conditions, the cycle doesn’t go past the cell proliferation stage. Consequently, in this situation, cells continue to multiply, thereby increasing the likelihood of cancerous mutations.
According to studies, tocotrienols can help return the cells to their natural cycle through their antioxidant and anti-inflammatory potencies. Here are some of the mechanisms through which tocotrienols work.
Induction of apoptosis is triggered when one or several living organism cells are infected with a virus which leads to cell death. Delta and Gamma-tocotrienols may have cancer-fighting properties, which inhibit the cancer-promoting protein NF-KAPPA B, causing cancer cells to die.
Targeting cell cycle checkpoints
Cell cycle checkpoints function as safeguard mechanisms that ensure cells complete cell cycle phases correctly. Using the de novo pathway, gamma-tocotrienol has been shown to induce ceramide synthesis, thereby reducing tumor growth and metastasis. Gamma-tocotrienol reduces cyclooxygenase-2 expression in gastric cancer. Cyclooxygenase-2 promotes the migration and invasion of gastric cancer cells.
The formation of new blood vessels or angiogenesis involves cell migration, growth, and differentiation. However, cancer cells can hijack this crucial process. Delta and gamma tocotrienols inhibit the Raf/MEK/ERK pathway, which is involved in angiogenesis, by suppressing its upstream signaling. This inhibition has also been shown to block proliferation in human hepatocellular carcinoma cells.
Inhibition of Breast Cancer Cell proliferation
In a 1995 study, a tocotrienol-rich fraction (TRF) of palm oil was found to inhibit breast cancer cell growth. In the same study, TRF was also shown to be effective in reducing plating efficiency. This means it successfully reduced the ability of cells to form colonies.
Reduces Cardiotoxicity of Epirubicin
In this case, tocotrienols were shown to help reduce the toxic side effects of Epirubicin (EPI), one of the mainline treatments for hepatocellular carcinoma. In a study, tocotrienols were seen to reduce the risk of EPI-induced inflammation and oxidative stress as well enhancing antitumor activity. Even though test subjects have not been carried out on humans as yet, they showed promise. .
WHY TAKE TOCOTRIENOLS?
Intake of tocotrienols, especially annatto tocotrienols is beneficial to the body in several ways. Apart from the anticancer properties discussed above, research has also established the following additional benefits of tocotrienols.
Here is a brief rundown on the effects tocotrienols have on overall body health.
Supports Cardiovascular Health
Cardiovascular health touches on both the health of the heart and that of blood vessels. Tocotrienols can help address the risk factors associated with cardiovascular conditions. Here are some of the ways they help to achieve this.
According to research, tocotrienols, especially the gamma and delta isomers, were found to be effective in lowering the levels of bad (LDL) cholesterol. It achieves this by inhibiting the enzymatic activity of HMG-CoA reductase.
However, it is important to note that human trials are still ongoing to determine the appropriate dosage. In an investigatory human study, it was shown that 250 mg of annatto tocotrienol helped in reducing LDL cholesterol by 18% and overall cholesterol by 15%.
Helps Fight Inflammation
Tocotrienols have been found to boost the immune system’s ability to fight off inflammation. By inhibiting the nuclear factor kappa B (NF-*B) signalling pathways, they contribute to reducing inflammation.
Tocotrienols are also effective in reducing biomarkers of inflammation such as high-sensitivity C-reactive protein (hsCRP). In several studies, supplementing with tocotrienol has been shown to reduce hsCRP by up to 40% in hypercholesterolemic patients.
Together, tocotrienols such as annatto tocotrienol and Vitamin B3 also boost the body's natural antioxidant capacity.
According to the Blood Pressure Association, 1 in 3 UK adults has blood pressure. With over £2.1 billion every year being spent by the NHS in treating this condition, any development towards finding a solution for hypertension is highly appreciated.
Studies show that supplementing with gamma-tocotrienol helps to enhance arterial function by lowering blood pressure. Even though the studies currently available are confined to animal models, tocotrienols have shown promising results in improving vascular endothelial function.
Improves Bone Health
People's ability to strengthen their bone tissue deteriorates as they age. When left unchecked, this may lead to osteoporosis. Thanks to the antioxidant and anti-inflammatory properties of tocotrienols, they have proved to be effective in preventing bone loss and in supporting bone remodelling processes.
In separate studies, tocotrienol supplements were shown to restore bone calcium levels and reduce proliferation in cells associated with the regulation of bone resorption.
Reduces Fat in the Livery (NAFLD)
Non-alcoholic fatty liver disease (NAFLD) results from excessive fat deposits in the liver. As the condition progresses, the liver becomes inflamed leading to cirrhosis. Through their ability to burn fat stores and relieve inflammation, tocotrienols have been confirmed to improve the health outcomes for NAFLD.
In both animal and human studies, incredible reductions were recorded in fasting blood glucose, circulating lipid levels, and inflammation levels after administering tocotrienol therapy.
Improves Risk Factors of Metabolic Disorders
Exercise and a healthy diet can help improve metabolism, but severe cases of metabolic disorders may require much more urgent attention. Tocotrienol suppresses adipogenesis - the development of fat-laden cells - by influencing fatty acid biosynthesis and lipid metabolism. In turn, this reduces fat mass and body weight.
Also, by suppressing oxidative stress and inflammation, tocotrienols can help prevent multiple systemic diabetes and obesity complications.
Upholds a Healthy Blood Sugar Level (Diabetes)
Uncontrolled changes in blood glucose levels can have a negative impact on your immune system. This is especially the case in diabetic patients. Through their anti-diabetic and anti-inflammatory properties, tocotrienols were found to have the ability to improve fasting blood glucose which is a key diabetes indicator. Specifically, delta-tocotrienol helps in normalising diabetes-associated blood glucose levels.
HOW DO TOCOTRIENOLS FIGHT AGEING?
Tocotrienols play a role in helping to defend ageing tissues. DNA damage is an underlying factor in most ageing processes. Through a randomised clinical trial, 160mg of tocotrienols was administered to middle-aged and older adults. Within just three months, there was a huge improvement in DNA damage.
As DNA damage is also a contributing factor to aging blood vessels, reducing its rate can reduce the risk of cardiovascular disease. To further affirm this statement, tocotrienols in the dosage of 100mg/day and 200mg /day were administered to patients. Significant reductions in arterial stiffness were observed.
With ageing comes not just DNA damage, but also immune senescence. When the immune system becomes dysfunctional, it interferes with the body's response to autoimmune disorders and excessive inflammation. Research studies suggest that supplementing with tocotrienol has the potential to lower the risk of preventable infections and reverse certain components of immune senescence.
The fact that tocotrienols also help reduce sun damage by combating oxidative stress, makes them vital ingredients in maintaining skin health. Studies show that the unsaturated farnesyl tail increases the absorption of tocotrienols in the skin tissue, thus helping in lowering the rate of oxidation and subsequent skin damage.
The fact that vitamin E is a valuable all-around nutrient is indisputable. But thanks to advanced research, we now know that the other branch of isomers known as tocotrienols is much more powerful.
Youth and Earth now have an annatto tocotrienol supplement, Tocotrienols EAnnato Delta Gold.
Now you too can experience the many advantages of Annatto tocotrienols because they are free of tocopherol. Whether it is in fighting free radicals, lowering the LDL cholesterol levels, fighting hypertension, or improving risk factors in metabolic disorders, Annatto tocotrienols play a crucial role.
If you are looking for a vitamin E supplement that has greater anti-inflammatory and free radical scavenging benefits, annatto tocotrienols could be what you need.
The content of this article is for informational purposes only.
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Do not ignore medical advice or delay seeking it because of something you’ve read on this site or any Youth & Earth product.