EP1355539A2 - Gesundheitsfördernde zusammensetzung von verbindungen - Google Patents

Gesundheitsfördernde zusammensetzung von verbindungen

Info

Publication number
EP1355539A2
EP1355539A2 EP01270255A EP01270255A EP1355539A2 EP 1355539 A2 EP1355539 A2 EP 1355539A2 EP 01270255 A EP01270255 A EP 01270255A EP 01270255 A EP01270255 A EP 01270255A EP 1355539 A2 EP1355539 A2 EP 1355539A2
Authority
EP
European Patent Office
Prior art keywords
meg
vitamin
mixture
compounds
preparation
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP01270255A
Other languages
English (en)
French (fr)
Inventor
Paul Clayton
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sanofi Aventis Deutschland GmbH
Original Assignee
Aventis Pharma Deutschland GmbH
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from EP00127644A external-priority patent/EP1214893A1/de
Priority claimed from DE10109798A external-priority patent/DE10109798A1/de
Application filed by Aventis Pharma Deutschland GmbH filed Critical Aventis Pharma Deutschland GmbH
Priority to EP01270255A priority Critical patent/EP1355539A2/de
Priority claimed from PCT/EP2001/014260 external-priority patent/WO2002047493A2/en
Publication of EP1355539A2 publication Critical patent/EP1355539A2/de
Withdrawn legal-status Critical Current

Links

Definitions

  • the invention refers to several compositions of compounds which are useful as food additives or part of pharmaceutical mixtures for improving health problems caused by several diseases.
  • 1st line Anti-oxidant enzymes are made in the body and contain an atom of selenium, zinc, manganese, copper or iron. Small amounts of these metals are vital to our health.
  • 2nd line Anti-oxidant micro-nutrients are obtained from our diet. These include Vitamins A, C and E, and the S vitamins. Co-enzyme 010, flavancids and carotenaids are important vitamin-5ke compounds which have anti-oxidant properties. 3rd line Anti-oxidant compounds are farmed in the body, and are made up from elements in the diet. These include meiatonin, glutathione, oestrogen, lipoic acid, Q10 and others.
  • Anti-oxidants in fruits and vegetables are more likely to survive the cooking process (although you will destroy them eventually if you cook your fruit and vegetables to a pulp, so lightly cooked is best). Anti-oxidants in fruits and vegetables are generally well absorbed - though some people absorb them better than others.
  • Liver and kidney are among the best sources of trace metals and of some vitamins like A, K, E.and Co-enzyme Q10.
  • offal meats are becoming more unpopular for human consumption, and in many affluent cultures are predominantly used for pet food.
  • the meat we eat is mostly skeletal muscle, which is not as good a source of many micro-nutrients.
  • Depleted soils produce crops low in specific minerals. This is particularly important in the case of selenium, and is the main cause of the selenium depletion which occurs throughout much of Northern Europe, mainland China, parts of Africa and elsewhere. If you live in an area where the soil is depleted, or you eat foods imported from regions with depleted soils, or you eat a lot of processed foods, your anti-oxidant enzyme defences are probably sub-optimal. The combination of impaired anti-oxidant defences and increased exposure to free radicals is a recipe for premature aging and illness.
  • Anti-oxidants work best to prevent disease when given together, rather than as monotherapies.
  • Our foods contain complex mixtures of anti-oxidants, and, before the arrival of the supplement industry, we obtained all our anti-oxidants from food.
  • many supplements contain beta carotene, but there are over 600 carotenoids in fruits and vegetables, so why supplement with just one?
  • beta carotene is the main carotenoid in most diets, our bodies also contain, and probably need, alpha carotene (from carrots or pumpkins), lutein (green leaf vegetables, especially kale and broccoli), lycopene (tomatoes), cryptoxanthin (oranges), zeaxanthin (red pepper and spinach) and others.
  • Beta carotene - 10-15 mg/day - mixed, natural source carotenoids are best - always combine with Vitamin C. This dose puts you in the top few per cent of the population, a group which appears to be at reduced risk of oral and colon cancers, coronary artery disease and cataracts. Larger doses are generally safe: 500 patients with skin conditions took 180-300 mg beta carotene/day for 10 years, without adverse effects (63) . However, smokers and others at risk of lung cancer must be cautious with beta carotene.
  • beta carotene 6 mg lycopene and 6 mg lutein per day. is a reasonable level, and beta carotene should always be taken with Vitamin C.
  • Vitamin E - 40OW (265 mg)/day - natural source is best. The American Physicians Trial and other data suggest this is an optimal dose for coronary disease. It should be natural E: the natural form contains only one isomer, D-alpha, whereas synthetic E contains eight. Why natural Vitamin E ? Because whereas D-alpha inhibits the proliferation of smooth muscle cells in blood vessel walls (a highly desirable and-coronary effect), some of the other isomers in synthetic E block this property, and could therefore be cardiotoxic. Very high doses of E are probably not generally useful and may be potentially harmful if used without other anti-oxidants. They may also inhibit the absorption of beta carotene and Vitamin K.
  • the current theory of coronary artery disease centres an the oxidization of LDL (low-density lipoprotein) cholesterol particles in the blood.
  • LDL low-density lipoprotein
  • the resulting lipid and cholesterol oxidation products attack the artery walls, increase the risk of clotting and raise blood pressure - all of which increases the risk of heart attacks.
  • Vitamin E has been shown to reduce the risk of heart attacks by half or more in three recent trials, and to reduce the progression of atheroma (furring of the arteries) in ways which are now well understood. So should we all be taking Vitamin E ?
  • Vitamin E can accelerate the oxidation of LDL cholesterol unless there is enough Vitamin C (or flavonoids) around to protect the Vitamin E itself from being oxidized.
  • Vitamin C also helps to maintain the lining of the arteries and reduces levels of clotting factors in the blood. It used to be thought that Vitamin C could increase levels of the 'good' HIDL (high-density lipoprotein) cholesterol, but this now looks unlikely. All this means that Vitamin E should really be taken with Vitamin C, Co-enzyme G10 (which appears to be a critical antioxidant in LIDL), and the metal trace elements manganese, zinc and copper which are necessary for the anti-oxidant enzymes to function properly - because all these anti-oxidant defence systems work together.
  • flavonoids come into their own: these anti-oxidants are able to get into the arterial walls, and slow or stop the progression of atheroma there (see Chapter 6, Flavonoids & isoflavones).
  • Beta carotene may be important too: it does not protect circulating LIDL from oxidation, but it prevents cells in the blood vessels' walls from further oxidizing the LDL that is already there.
  • the evidence that anti-oxidants reduce the risk of coronary artery disease is overwhelming. Conversely, some eminent scientists now say that a poor anti-oxidant status is a better predictor of the risk of heart attacks than high cholesterol levels, blood pressure or any other of the known risk factors.
  • Oxidative damage also contributes to the late stage complications of diabetes, where the incidence of coronary artery disease, cataract, nephropathy (damage to the kidneys) and neuropathy (nerve damage) scar.
  • the increased oxidative stress in these patients means they have more oxidized lipids in their blood and abnormally low levels of anti-oxidants.
  • Their Vitamin C levels are often so low that some late stage diabetics are close to suffering from scurvy911. High dose anti-oxidants are clearly indicated.
  • Cataract and age-related macular degeneration are the two leading causes of blindness in the developed countries.
  • cataract surgery is the single largest item in the Medicare budget, costing some $ 3.2 billion per annum.
  • the risk of cataract is increased by oxidative stresses such as increased exposure to UV, which oxidises the normally transparent proteins in the lens of the eye, and possibly smoking.
  • the risk is reduced by anti-oxidants such as Vitamins C and E, alpha-lipoic acid, turmeric and possibly beta carotene.
  • Macular degeneration is the other major cause of deteriorating sight.
  • anti-oxidants such as E, C and beta carotene are protective. This is probably not the most effective combination of anti-oxidants, however.
  • the main anti-oxidants in the retina are the carotenoids lutein and zeaxanthin.
  • the optimal strategy to preserve sight, even if it has started to fail, is almost certainly a combination of lutein and zeaxanthin, together with Vitamin C, riboflavin, lycopene, selenium and a turmeric supplement to boost the anti-oxidant enzyme glutathione peroxidase; and the flavonoids in bilberry, a herb traditionally used to treat visual complaints.
  • Parkinsonism toxic tetrahydroquinolones are found in the affected areas of the brain. These compounds are mitochondrial toxins and they cause a decrease in glutathione, an increase in free radical formation, and an increase in nerve membrane damage and death. If a horse is unlucky enough to eat yellow star thistles, which contain compounds called sesquiterpene lactones, the same sort of things happen - and the horse develops a condition rather like Parkinsonism.
  • nitrous oxide (NO) radicals may be involved, so turmeric, together with beta carotene, or the even more effective carotenoid lycopene, is also worth incorporating in the program.
  • Vitamin E to this multi-component regimen.
  • Vitamin E alone is not very helpful in treating this condition, but chronic Vitamin E depletion is linked to a form of brain damage in animals rather like the damage found in Parkinsonism. In humans who cannot absorb Vitamin E, the risk of Parkinsonism also rises.
  • TD tardive dyskinesia
  • Vitamin E is an important antioxidant in the brain, but at least six months of high-dose supplementation are needed to pump up the levels to where they are needed . By that time, much of the nerve damage caused by the anti-psychotic drugs may have already occurred - so it might be better to co-prescribe anti-oxidants from the start.
  • LOPs Lipid Oxidation Products
  • a high magnesium intake is linked to improved lung function, and some clinicians have found magnesium aerosols useful in relaxing the airways of their asthmatic patients.
  • Low anti-oxidant consumption is a risk factor for developing arthritis (54) .
  • Some anti-oxidants such as beta carotene reduce symptoms in animal models of arthritis.
  • Other anti-oxidants such as those found in ginger, reduce joint swelling and pain in clinical trials, but these flavonoid compounds have specific anti-inflammatory properties. (See also Chapter 10, Amino sugars)
  • Tumour necrosis factor alpha is important in inflammatory conditions such as asthma, Crohn's disease and arthritis, and anti-TNF antibodies have been used with some success in clinical trials of arthritis. The success, however, was tempered; patients who made antibodies to the anti-TNF antibodies developed allergy-type responses.
  • the nutritional approach may offer a more durable solution.
  • the spice turmeric contains curcumin, a powerful inhibitor of TNF-alpha.
  • curcumin a powerful inhibitor of TNF-alpha.
  • a combination of turmeric and ginger which blocks the key inflammatory enzymes, has powerful anti- arthritic properties; when combined with high dose (ie 8-10 g a day) fish or hemp oil, plus 1200 mg per day of Vitamin E and 1-2 g of Vitamin C.
  • Free radicals are involved in the destruction of tissue that leads to ulcers of the skin and digestive tract.
  • Smoking which decreases our anti-oxidant defences, is a risk factor-, conversely anti-oxidants can treat these conditions and, if used prophylactically, may prevent them.
  • the flavonoids may be particularly useful here.
  • the flavonoids are one of the most important groups of compounds derived from plants, Over 20,000 have now been identified since the early days when they were all lumped together as Vitamin P by the great Hungarian biochemist Szent Gyorgyi in 1936 (who also discovered Vitamin C). Following Szent Gyorgyi's discovery, pharmaceutical companies brought out a range of medicines containing Vitamin P but, by the '60s, most had disappeared. As a natural compound, P could not be patented and because nobody knew exactly what P was, how best to measure it, or even whether P was a single compound or a group, the drug companies found it difficult to produce a reliable product.
  • flavonoids have been identified and divided into approximately 12 sub-types, many of which have profound anti-oxidant activity.
  • flavanoid which quenches free radicals in the lining of arteries occurs in very high concentrations in hawthorn and yarrow, two plants which have long been used to treat cardiovascular disease.
  • flavonoids are extremely potent anti-oxidants and anti-flammatory agents. Different flavonoids work in different tissues of the body; some can enter the brain, for instance, whereas others appear to concentrate in the lining of blood vessels. This means that different flavonoids can be used to target different tissues. For example, a flavonoid which is taken up by the lining of capillaries might be expected to be good for capillary function - and the ginkgo flavonoids, widely used to improve blood flow to the brain, hands and feet, do just this.
  • flavonoids neutralize free radicals, including the highly dangerous hydroxyl radical.
  • One group is particularly good at quenching the radicals which cause liver damage (these are the flavonoids found in milk thistle).
  • Phytate - can act as an anti-oxidant
  • the second anti-cancer ingredient is phytate, generally regarded as another anti-nutrient because it binds iron. But in certain conditions this is a good thing, as excess (free) iron in the body is a potent source of free radicals, and a potential carcinogen. When phytate binds iron, it is effectively acting as an antioxidant. This helps to explain why phytate is a powerful inhibitor of colon cancer, where free iron is one of the key causative factors. (I don't recommend phytate for everyone, however. Iron deficiency anaemia is still widespread, particularly among women of child-bearing age, and too much phytate could worsen an existing anaemia.)
  • phytosterols - protect against carcinogenic bile acids Third up are the phytosterols, the plant equivalents of cholesterol. They are poorly absorbed and remain in the gut, where they are thought to protect against the harmful effects of certain (secondary) bile acids. These bile acids are formed from cholesterol and have mutagenic and carcinogenic properties. This may be why some phytosterols are capable of reducing the incidence of colon cancer by as much as 50 per cent.
  • saponins anti-oxidants which protect against free radical damage.
  • Lab tests have shown that saponins prevent mutations that can lead to cancer.
  • Isaflavones block oestrogen, a hormone linked to an increased risk of breast and other hormone-dependent cancers. They act rather like Tamoxifen, a drug widely used to treat and prevent breast cancer.
  • Prostate cancer like breast cancer, is usually hormone-dependent. But whereas breast cancer is encouraged by oestrogen, prostate cancer is often driven by testosterone. Isoflavones which block testosterone reduce the tendency for prostate cancers to grow.
  • flavonoids bind to dangerous free iron and copper in the body, thereby stopping free radical formation. Many are capable of locking up free oxygen and preventing the oxidation of ascorbic acid, thereby protecting Vitamin C in fruit, fruit juices, and in the body.
  • One flavonoid, quercitin, found in onions and apples may be one of the most cardio-protective substances yet discovered.
  • the Zutphen Elderly Study measured the flavonoid content of the diet of their subjects and discovered that the number of cardiac deaths in the group eating the most flavonoids was a quarter of the death rate in the group which ate the least flavonoids. And quercitin accounted for two-thirds of the total flavonoid intake.
  • quercitin a powerful anti-oxidant and anti-inflammatory agent is cardio-protective.
  • quercitin is absorbed from the gut, because little is found in the bloodstream. Recent work shows that quercitin and related compounds are absorbed and concentrated elsewhere in the body.
  • Tannins for example, which consist of long chains of flavanoids linked together, protect against stroke in hypertensive animals. Tannins are found in, e.g. tea, wine, quince and persimmons.
  • the purple pigment in beets consists of flavonoids which, when eaten, are absorbed from the gut and excreted in the urine - a colorful fact you can check for yourself. Combine beets with rhubarb or spinach at the same meal to get the most spectacular results.
  • Procyanidins are an extremely promising group of flavonoids. They are well absorbed from the gut, and are already used (in the form of pycnogenol and grapeseed extracts) to treat arthritic conditions, because of their ability to quench free radicals and stop the breakdown of synovial (lubricating) fluid inside inflamed joints.
  • flavonoids also target blood vessels and, once there, protect the connective tissue in the artery walls by exerting a powerful anti-oxidant, anti-inflammatory and anti-permeability effect. They also block enzymes which have a destructive effect on the connective tissues.
  • These protective actions mean the high procyanidin content of black grapes (and red wine) is probably one of the main factors underlying the so-called French paradox. The French eat a high fat diet, yet are relatively immune from heart disease. There are probably several factors involved, including the widespread use of olive oil, but there is evidence that consumption of two to four glasses of red wine a day reduces the risk of a heart attack by an astonishing 40 per cent.
  • the procyanidins' ability to bind to and protect the fibres in the vessel walls (like collagen and elastin) from oxidative or enzyme attack helps to reduce the amount of damage to the walls. If there is already damage, the two flavonoids seem to stop the site becoming inflamed and slow the furring of the arteries.
  • Procyanidins are best used preventatively, but even after a heart attack they can help. Their phenomenal ability to scavenge free radicals means that a procyanidin product will reduce your risk of developing a life-threatening arrhythmia after the attack.
  • Procyanidins are being incorporated into the latest cosmetics. They form a Protective shield around the collagen fibres which give skin its firmness and texture, and Protect them against the enzymes which break down these fibres, and against free radical damage too. It's early days, but Procyanidin's anti-allergic, anti-inflammatory and anti-oxidant Properties could constitute a major cosmetic break-through, especially when combined with other anti-aging nutrients such as the amino sugars.
  • Procyanidins target the bacteria which cause dental decay.
  • the flavonoids seem to stop the bugs sticking to the teeth and to dental plaque. Some dental scientists are looking at these flavonoids as a way Of slowing down tooth decay.
  • the anti- inflammatory effects may also help to control or minimize gingivitis (gum disease) which is responsible for more tooth loss than dental decay.
  • Free radicals damage DNA. Many flavonoids are potent anti-oxidants which mop up large numbers of free radicals, and reduce the amount of DNA 'hits'. Free radicals also damage cell membranes. This damage might also lead to tumor formation, so once again anti-oxidants, like flavonoids, should help. Not surprisingly, a great deal of nutritional research is concentrating on just this area.
  • Some of the most active and best researched compounds include: quercitin - onions ellagic acid - walnuts, pecan nuts caffeic acid - coffee beans chlorogenic acid - tomatoes epigallocatechingallate - tea camosic acid - rosemary genistein - soy.
  • Protease inhibitors (lectins) which block genes which promote cancer.
  • protease inhibitors also block the action of a number of genes which cause cancer. Most protease inhibitors are destroyed by cooking, but there is evidence that enough survive to confer a significant protective effect.
  • Genistein King of the isoflavones, and subject of well over 300 research papers to date, is genistein. Genistein has little effect on normal cells - but it is a powerful inhibitor of nearly every cancer cell type examined so far.
  • Soy protects against heart disease as well.
  • CAD coronary artery disease
  • Diet is the key. A diet rich in animal fats and low in anti-oxidants and fish oil is a fast route to a heart attack, as is smoking. And so is high blood cholesterol.
  • the large bowel which is where the majority of gastrointestinal cancers occur, is full of four to five hundred different species of bacteria, known in medical language as 'flora'. Some of these can cause serious illness, while others are associated with positive health.
  • lactobacilli There are at least two types of health-promoting bacteria, the lactobacilli and the bifidobacteria. Some of these are found in live yogurt, and various scientists and nutritionists have used yogurt to try to change the flora of the lower bowel. However, the bacteria have a limited shelf-life, even when freeze-dried, and many of them are unable to survive the acid conditions in the stomach. Even if the bacteria do arrive in the colon, they have to compete with the dense population of hostile bacteria that are already there.
  • pre-biotics cannot be digested and they pass into the colon intact. Once there, they act as a growth enhancer for the health-promoting lactobacilli and bifidobacteria.
  • the 'good' bacteria multiply, they secrete enzymes which break down pre-bictics into acids such as acetic and butyric acid. These inhibit the growth of disease-causing bacteria.
  • the 'good' bacteria also secrete antibiotic substances which restrain the 'unhealthy' bugs, including most of those responsible for food poisoning.
  • Pre-biotics reduce the disease-causing bacteria in the gut, and the amount of cancer-causing compounds they produce which could well have a protective effect. Finally, as the bifids grow they bind free iron, thereby reducing levels of free radicals in the colon. This must be another cancer-preventing property.
  • B depletion is surprisingly common in the developed countries, and low B levels are a major risk factor for coronary artery disease. So pre-biotics, by increasing the good bacteria in the gut and B vitamin levels, will be cardioprotective by lowering homocysteine, and simultaneously raising HDL levels.
  • Short chain pre-biotics ie FOS
  • bifidogenesis bifidobacteria
  • bifidogenesis bifidobacteria
  • the combination of bifidogenesis and bile acid binding is also likely to be cancer protective, especially if FOS is combined with longer chain pre-biotics.
  • the edible fats and oils are basically similar compounds. Oils, however, melt at lower temperatures than fats, and at room temperature oils are liquid and fats are solid. Fatty acids (fats and oils) are a rich source of calories, which can either be 'burned' to produce energy, or stored as fat for lean times ahead. They are also incorporated into cell membranes and other tissues, where they have an important structural role.
  • fatty acids are metabolised into compounds called eicasanoids.
  • Fats and oils produce quite different eicosanoids: broadly speaking, fats form eicosanoids which increase inflammation, and oils produce eicosanoids which reduce inflammation.
  • PUFAs poly- unsaturated tatty acids
  • Essential PUFAs There are two families of essential pc iy-unsatu rated fatty acids, Omega 6 and Omega 3, both of which are oils. These oils are vital for the functioning of every cell in our bodies, and yet our bodies cannot make them. We have to obtain them from our diet, and in that sense they are similar to vitamins. Once the oils have been absorbed from our food, our enzymes make all the other Omega 3 and 6 PUFAs our cells and systems need.
  • PUFAs are a powerful force for good health but, as with other powerful agents, they should not be taken indiscdminately.
  • the ratio of the various PUFAs in the diet is important, and the fact that in most mammals' cells the level of Omega 6 (from vegetable sources) is three to tour times higher than the Omega 3 content (from fish sources), gives us a painter as to what we should aim for.
  • PUFAs poly-unsatu rated tatty acids
  • LOPs lipid oxidation products
  • Vitamin E 400 lU/day
  • Mixed flavonoids 100-500 mg
  • Co-enzyme Q 10 is particularly recommended. Apart from its other benefits (see Chapter 9, Co-enzyme Q I0), it is very good at preventing the increase in free radicals otherwise caused by fish oil supplements.
  • Co-enzyme Q10 is often referred to as Vitamin Q, but although it is vital to life, and occurs in trace amounts in certain foods such as sardines, Q10 is not technically a vitamin because we can produce small amounts of it sacred in the liver.
  • GAGs and PGs Macro-molecules built up from amino sugars, called GAGs and PGs, together with the proteins called collagen and elastin, make up the framework for all our tissues.
  • GAGs and collagen make up tendons, ligaments, heart valves, skin and finger-nails. Combined with another protein, elastin, they make cartilage in joints and the discs in the spine.
  • the rate of cell growth may outstrip the rate of glucosamine and GAG (glycosaminoglycan) production.
  • GAG glycosaminoglycan
  • the inflammation itself may inhibit the making of GAGs, and increase the rate at which they are broken down.
  • the amino sugar compounds in the skin are constantly being broken down and replaced. As much as one fifth of the glucose in the blood is destined for connective tissue formation. But if the glucosamine-producing enzymes slow down,, as they do with age, they cannot keep pace with the deterioration caused by exposure to ultra-violet light (UV), cigarette smoke, pollution and other sources of free radicals.
  • UV ultra-violet light
  • the connective tissue that gives the skin strength, elasticity and firmness deteriorates, with all-too-obvious results.
  • procyanidin flavonoids e.g. bilberry or grapeseed
  • bilberry or grapeseed the procyanidin flavonoids
  • Methyl groups like vitamins, are essential in our diet. Foods that contain significant levels of the methyl groups are, in descending order, sugar beet, sugar cane, prawns, shrimps and eggs. To give an idea of the importance of methyl groups, the nervous system, the immune system, the heart and blood vessels, the kidneys and the liver all depend on methyl groups to function normally.
  • a diet low in methyl groups damages all the above systems. Stress becomes more destructive, toxins become more toxic, carcinogens more carcinogenic. In fact, a lack of methyl groups in the diet is the only dietary deficiency known to be directly carcinogenic. If there are not enough methyl groups, DNA reproduction can go wrong, leading to the activation of ancogenes (cancer-causing genes). To appreciate why a deficiency of methyl groups in the diet is so dangerous, we need to understand a process called the methyl group cycle (see diagram an next page). It's also important to know that excessive levels of the amino acid homocysteine in the body are a major risk factor for heart disease and Alzheimer's (see Chapters 14, Heart disease and 17, A healthy brain).
  • Methyl groups are a simple combination of carbon and hydrogen atoms. You will see from the diagram that methyl groups from the diet combine with homacysteine in the body to form methionine. Methionine is then turned into S-adenosyl methionine (SAM).
  • SAM S-adenosyl methionine
  • SAM passes an the methyl groups in the body to produce many essential compounds. These include creatine and camitine (important in energy production), phospholipids, (essential molecules involved in-cell membrane and especially nerve health), RNA and DNA, the stress hormones epinephrine and nor-epinephrine, and the neurotransmitters involved in mood. Methyl groups are also essential to the basic functioning of the immune system.
  • the body cannot synthesize methyl groups, and therefore a constant dietary intake of methyl groups is essential to maintain the cycle, in order to keep levels of SAM up and levels of homocysteine down.
  • the principal dietary sources of methyl groups are, in descending order, the nutrients betaine,-chaiine and methionine; and to a lesser extent the Vitamins B6, B 12 and folic acid.
  • the vitamins are not the best donors; betaine is far more effective.
  • methyl groups are needed for the formation of stress hormones, for various defence mechanisms and for the synthesis of polyamines, RNA and DNA, all of which are needed for tissue repair.
  • betaine is very effective at lowering levels of homacysteine. Most humans, however, do not consume much betaine; and in this situation, the B vitamins become the next line of defence.
  • a strong B complex preparation reduces levels of homocysteine. This is why supplements of folic acid and Vitamins B6 and B12 are increasingly being used to reduce homocysteine levels, and the risk of homocysteine-related cardiovascular and neurological diseases.
  • mixtures of compounds as provided by the invention exhibits different favourable effects with respect to several important aspects of human health as mental decline, diabetes, arthritis, osteoporosis, asthma and age related eye disease in particular macular degeneration. These mixtures may be useful as food additives or as medicaments.
  • nutraceutical intervention is always filtered through the nutritional baseline of the subject or by other lifestyle factors such as smoking and activity levels or by genetic variations. One cannot change genetic variations. But in order to achieve optimal results the neutraceutical intervention should be combined with a reduction or cessation in smoking, a reduction in sodium intake and/or an increase in activity levels.
  • the invention refers to several mixtures of compounds comprising one or several of the following compounds but avoiding to contain all of them in one mixture:
  • the amount given as abovementioned to determine the quantity of each single compound within the master mixture defines the average content of this said compound. This content may vary within a upper or lower limit of up to 15% of this value caused for example by varations within the compound sources or methodlogical variatons from weighing or packaging Likewise in a preferred embodiment of the invention the amount of each single compound may fall within the upper and lower limits as defined by table 1 as far as limits have been provided by this table.
  • the invention refers to a Mixture of compounds comprising at least a) 800 meg (2664IU) of Vitamin A, 1000 mg of Vitamin C, 400IU of Vitamin E, 200 meg of Vitamin K, b) 10 mg of Beta carotene, 6 mg of Lutein, 5 mg of Lycopene, 100 meg of Zeaxant c) 7.5 mg of Vitamin B1 , 7.5 mg of Vitamin B2, 15 mg of Niacin, 15 mg of Pantothenic acid, 7.5 mg of Vitamin B6, 200 meg of Folic acid, 6.75 meg of Vitamin B12, d) 200 meg of Selenium (preferrably in the yeast form), 10 mg of Zinc, 120 meg of Chromium, 2 mg of Copper, 4 mg of Manganese, 100 meg of Iodine, 100 meg of Molybdenum, e) 200 meg of Biotin, 1000 mg of Betaine, 250 mg of Oligoproanthocyanidins (OPC), 150 mg of Polyphenol complex, 1000mg of alpha
  • the invention refers further to preparation of this mixture according to the immediately aforegoing section by first producing the said single compounds by chemical synthesis or isolating them from natural sources, therafter putting the single eompunds together in a suitable vessel in relative amounts as to end up with the specified amount for each compund, then mixing the compounds after having put them together as aforementioned, and adding additional substances for stabilisation and/or formulation of this mixture.
  • the invention refers also to use of this same mixture for preparation of a food additive with beneficial effects preventing, curing, or improving of symptoms of diabetes and to use of this same mixture for preparation of a medicament for preventing, improving, or curing of diabetes.
  • the invention refers to a mixture of compounds comprising at least a) 800 meg (26641U) of Vitamin A, 500 mg of Vitamin C, 200IU of Vitamin E, 200 meg of Vitamin K, b) 10 mg of Beta carotene, 6 mg of Lutein, 5 mg of Lycopene, 100 meg of Zeaxanthin, c) 7.5 mg of Vitamin B1 , 7.5 mg of Vitamin B2, 15 mg of Niacin, 15 mg of Pantothenic acid, 7.5 mg of Vitamin B6, 200 meg of Folic acid, 6.75 meg of Vitamin B12, d) 200 meg of Selenium (preferably in the yeast form), 10 mg of Zinc, 120 meg of Chromium, 2 mg of Copper, 4 mg of Manganese, 100 meg of Iodine, 100 meg of
  • Molybdenum 200 meg of Biotin, 5000 mg of Oligoproanthocyanidins (OPC), 150 mg of Polyphenol complex, 600 mg of Omega 3, 100 mg of Co-Q10 f) 1000 mg of Glucosamine and possibly additional substances for the purpose of stabilisation and formulation of the above mentioned compounds of this claim.
  • OPC Oligoproanthocyanidins
  • the invention refers further to reparation of this mixture according to the immediately aforegoing section by first producing the said single compounds by chemical synthesis or isolating them from natural sources, therafter putting the single eompunds together in a suitable vessel in relative amounts as to end up with the specified amount for each compund, then mixing the compounds after having put them together as aforementioned, and adding additional substances for stabilisation and/or formulation of this mixture.
  • the invention refers also to use of this same mixture as food additive with beneficial effects on preventing, curing, or improving of symptoms of osteo-arthritis as well as to use of this mixture for preparation of a medicament for preventing, improving, or curing of osteo-arthritis.
  • the invention refers to a mixture of compounds comprising at least a) 800 meg (2664IU) of Vitamin A, 500 mg of Vitamin C, 20 meg of Vitamin D, 200 meg of Vitamin K, b) 10 mg of Beta carotene, 6 mg of Lutein, 5 mg of Lycopene, 100 meg of Zeaxanthin, c) 7.5 mg of Vitamin B1 , 7.5 mg of Vitamin B2, 15 mg of Niacin, 15 mg of Pantothenic acid, 7.5 mg of Vitamin B6, 200 meg of Folic acid, 6.75 meg of Vitamin B12, d) 200 meg of Selenium (preferably in the yeast form), 10 mg of Zinc, 100 mg of Calcium, 50 mg of Magnesium, 120 meg of Chromium, 2 mg of Copper, 4 mg of Manganese, 100 meg of Iodine, 100 meg of Molybdenum, e) 200 meg of Biotin, 250 mg of Oligoproanthocyanidins (OPC), 150 mg of Polyphenol complex,
  • the invention refers further to preparation of a mixture according to the immediately foregoing section by first producing the said single compounds by chemical synthesis or isolating them from natural sources, thereafter putting the single compounds together in a suitable vessel in relative amounts as to end up with the specified amount for each compound, then mixing the compounds after having put them together as aforementioned, and adding additional substances for stabilization and/or formulation of this mixture.
  • the invention refers also to use of this same mixture for preparation of a food additive with beneficial effects for preventing, curing, or improving of symptoms of osteoporosis as well as of use of this same mixture for preparation of a medicament for preventing, improving, or curing of osteoporosis.
  • the invention refers to a mixture of compounds comprising at least a) 800 meg (26641 U) of Vitamin A, 1000 mg of Vitamin C, 15 meg of Vitamin D, 400IU of Vitamin E, 200 meg of Vitamin K, b) 10 mg of Beta carotene, 6 mg of Lutein, 5 mg of Lycopene, 100 meg of Zeaxanthin, c) 7.5 mg of Vitamin B1 , 7.5 mg of Vitamin B2, 15 mg of Niacin, 15 mg of Pantothenic acid, 7.5 mg of Vitamin B6, 200 meg of Folic acid, 6.75 meg of Vitamin B12, d) 200 meg of Selenium (preferably in the yeast form), 10 mg of Zinc, 100 mg of Calcium, 50 mg of Magnesium, 120 meg of Chromium, 2 mg of Copper, 4 mg of Manganese, 100 meg of Iodine, 100 meg of Molybdenum, e) 200 meg of Biotin, 1000 mg of Betaine, 250 mg of Oligoproanthocyanidin
  • the invention refers further to preparation of a mixture according to the immediately foregoing section by first producing the said single compounds by chemical synthesis or isolating them from natural sources, thereafter putting the single compounds together in a suitable vessel in relative amounts as to end up with the specified amount for each compound, then mixing the compounds after having put them together as aforementioned, and adding additional substances for stabilization and/or formulation of this mixture.
  • the invention refers also to use of the same mixture for preparation of a food additive with beneficial effects on preventing, curing, or improving of symptoms of asthma as well as of use of the same mixture for preparation of a medicament for preventing, improving, or curing of asthma.
  • the invention refers to a mixture of compounds comprising at least a) 800 meg (2664IU) of Vitamin A, 500 mg of Vitamin C, 200IU of Vitamin E, 200 meg of Vitamin K, b) 10 mg of Beta carotene, 6 mg of Lutein, 5 mg of Lycopene, 100 meg of Zeaxanthin, c) 7.5 mg of Vitamin B1 , 7.5 mg of Vitamin B2, 15 mg of Niacin, 15 mg of Pantothenic acid, 7.5 mg of Vitamin B6, 200 meg of Folic acid, 6.75 meg of Vitamin B12, d) 200 meg of Selenium (preferrably the yeast form), 10 mg of Zinc, 120 meg of Chromium, 2 mg of Copper, 4 mg of Manganese, 100 meg of Iodine, 100 meg of Molybdenum, e) 200 meg of Biotin, 1000 mg of Betaine, 250 mg of Oligoproanthocyanidins (OPC), 150 mg of Polyphenol complex, 40 mg of Isof
  • the invention refers further to preparation of a mixture according to the immediately foregoing section by first producing the said single compounds by chemical synthesis or isolating them from natural sources, thereafter putting the single compounds together in a suitable vessel in relative amounts as to end up with the specified amount for each compound, then mixing the compounds after having put them together as aforementioned, and adding additional substances for stabilization and/or formulation of this mixture.
  • the invention refers also to use of the same mixture of for preparation of a food additive with beneficial effects on preventing, curing, or improving of symptoms of mental decline as well as use of the same mixture for preparation of a medicament for preventing, improving, or curing of mental decline.
  • the invention refers to a mixture of compounds comprising at least a) 800 meg (2664IU) of Vitamin A, 500 mg of Vitamin C, 265 mg (400IU) of Vitamin E, 50 meg of Vitamin K, b) 10 mg of Beta carotene, 6 mg of Lutein, 5 mg of Lycopene, 100 meg of Zeaxanthin, c) 7.5 mg of Vitamin B1 , 7.5 mg of Vitamin B2, 15 mg of Niacin, 15 mg of Pantothenic acid, 7.5 mg of Vitamin B6, 200 meg of Folic acid, 6.75 meg of Vitamin B12, d) 150 meg of Selenium, 10 mg of Zinc, 120 meg of Chromium, 2 mg of Copper, 4 mg of Manganese, 100 meg of Iodine, 100 meg of Molybdenum, e) 200 meg of Biotin, 500 - 1000 mg of Betaine, 100 mg of Oligoproanthocyanidins
  • the invention refers further to preparation of a mixture according to the immediately foregoing section by first producing the said single compounds by chemical synthesis or isolating them from natural sources, thereafter putting the single compounds together in a suitable vessel in relative amounts as to end up with the specified amount for each compound, then mixing the compounds after having put them together as aforementioned, and adding additional substances for stabilization and/or formulation of this mixture.
  • the invention refers also to use of the same mixture for preparation of a food additive with beneficial effects on preventing, curing, or improving of symptoms of age related eye disease as well of use of this mixture for preparation of a medicament for preventing, improving, or curing of age related eye disease.

Landscapes

  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EP01270255A 2000-12-16 2001-12-05 Gesundheitsfördernde zusammensetzung von verbindungen Withdrawn EP1355539A2 (de)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP01270255A EP1355539A2 (de) 2000-12-16 2001-12-05 Gesundheitsfördernde zusammensetzung von verbindungen

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
EP00127644 2000-12-16
EP00127644A EP1214893A1 (de) 2000-12-16 2000-12-16 Zusammensetzungen zur Verbesserung der Gesundheit
DE10109798 2001-03-01
DE10109798A DE10109798A1 (de) 2001-03-01 2001-03-01 Gesundheitsfördernde Zusammensetzung von Verbindungen
EP01270255A EP1355539A2 (de) 2000-12-16 2001-12-05 Gesundheitsfördernde zusammensetzung von verbindungen
PCT/EP2001/014260 WO2002047493A2 (en) 2000-12-16 2001-12-05 Health promoting compositions

Publications (1)

Publication Number Publication Date
EP1355539A2 true EP1355539A2 (de) 2003-10-29

Family

ID=28794616

Family Applications (1)

Application Number Title Priority Date Filing Date
EP01270255A Withdrawn EP1355539A2 (de) 2000-12-16 2001-12-05 Gesundheitsfördernde zusammensetzung von verbindungen

Country Status (1)

Country Link
EP (1) EP1355539A2 (de)

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO0247493A3 *

Similar Documents

Publication Publication Date Title
US20020146463A1 (en) Health promoting compositions
EP1214893A1 (de) Zusammensetzungen zur Verbesserung der Gesundheit
Mann Diet and risk of coronary heart disease and type 2 diabetes
KR20190007412A (ko) 식이 및 운동 후 체중 감량 및 심대사 건강을 향상시키는 방법 및 조성물
Wichansawakun et al. Antioxidant diets and functional foods promote healthy aging and longevity through diverse mechanisms of action
DE10109798A1 (de) Gesundheitsfördernde Zusammensetzung von Verbindungen
Awuchi et al. Natural nutraceuticals, especially functional foods, their ma-jor bioactive components, formulation, and health benefits for disease prevention-An overview
AU2005247160A1 (en) Functional foods comprising flavonoids and tocotrienols and methods thereof
Reavley The new encyclopedia of vitamins, minerals, supplements, & herbs: How they are best used to promote health and well being
JP2008161077A (ja) 血液流動性改善作用をもたらす機能性食品
Sharma et al. Bioavailability of nutrients and safety measurements
Bartlett et al. Possible contraindications and adverse reactions associated with the use of ocular nutritional supplements
EP1355539A2 (de) Gesundheitsfördernde zusammensetzung von verbindungen
Tomada et al. Science‐based anti‐ageing nutritional recommendations
Clayton Health defence
Prakash et al. EXPLORING ROLE OF DIETARY FIBRES, NUTRACEUTICALS AND FUNCTIONAL FOODS IN CARDIOVASCULAR DISORDERS.
Pol et al. Approaches for Treating Ulcer with Functional Foods
Iriti et al. Phytochemical diversity behind health-promoting effects of traditional Mediterranean foods
Tewfik et al. Nutraceuticals, functional foods and botanical dietary supplements; promote wellbeing and underpin public health
Tralongo et al. Cancer, heart diseases and common risk factors: Diet and physical activity
Chace Turning Off Breast Cancer: A Personalized Approach to Nutrition and Detoxification in Prevention and Healing
Murray The Magic of Food: Live Longer and Healthier--and Lose Weight--with the Synergetic Diet
Barrita et al. Antioxidants and natural compounds in Mexican foods
Dinelli et al. Physiologically bioactive compounds of functional foods, herbs, and dietary supplements
Wahlqvist et al. Vitamins and vitamin like compounds

Legal Events

Date Code Title Description
PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

17P Request for examination filed

Effective date: 20030716

AK Designated contracting states

Kind code of ref document: A2

Designated state(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR

AX Request for extension of the european patent

Extension state: AL LT LV MK RO SI

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: THE APPLICATION HAS BEEN WITHDRAWN

18W Application withdrawn

Effective date: 20040813