GB2289406A - Vitamin, betacarotene and zinc composition for sperm health - Google Patents
Vitamin, betacarotene and zinc composition for sperm health Download PDFInfo
- Publication number
- GB2289406A GB2289406A GB9407524A GB9407524A GB2289406A GB 2289406 A GB2289406 A GB 2289406A GB 9407524 A GB9407524 A GB 9407524A GB 9407524 A GB9407524 A GB 9407524A GB 2289406 A GB2289406 A GB 2289406A
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- GB
- United Kingdom
- Prior art keywords
- sperm
- vitamin
- zinc
- betacarotene
- formulation
- 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.)
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-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
- A61K33/30—Zinc; Compounds thereof
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A formulation for sperm health comprises vitamin E, vitamin C, zinc and betacarotene. The components together act in synergy to exert numerous beneficial effects on sperm motility, maturation, flexibility of sperm tails and reduced sperm clumping. The formulation can be used as a food supplement or can be administered to male subjects in tablet form. The preferred formulation contains 250mg of vitamin C, 15mg of betacarotene, 100mg of vitamin E and 10mg of zinc gluconate in conjunction with binding and flavouring agents.
Description
COMPOSITION FOR SPERM HEALTH
This invention relates to a composition which may suitably be taken as a food supplement, and to its use for improving sperm health.
Over the last 50 years, the average sperm count has virtually halved from 113 million sperm per ml to 66 million per ml (Carlsen E. et al. (1992) BMJ 305: 609-612).
Semen volume has dropped from an average of 3.4ml to 2.75m1; sperm motility has decreased and the percentage of sperm with abnormal architecture has increased.
It is estimated that as many as 10% of sperm can be abnormal without loss of fertility. It is now considered usual, however, to find up to 40% of sperm in the ejaculate with architectural abnormalities. It takes an average of 74 days for the production of a mature sperm from its primitive germ cell, and then a further 20 days for the sperm to traverse the epididymis, during which time they gain their motility. After this, sperm are in the vas deferens for at least another six days before ejaculation. During this 100 day time period, each sperm can undergo irreparable damage.
Most men have 20% to 40% obviously abnormal sperm when semen is examined in the laboratory. Many more have genetic abnormalities that remain undetected. It is estimated that 40% of all sperm damage is due to the harmful effects of free radicals.
Oxidative damage to DNA can result in the wrong nucleotide bases being inserted when the DNA sequence is read. If this occurs in a dividing germ cell destined to produce a sperm, a mutation results which may cause subfertility, birth defects, genetic diseases or childhood cancers in resultant offspring.
It is known that certain vitamins and minerals, if administered individually to male subjects, improve sperm quality and quantity.
For example, the use of vitamin C has been shown to play a role in protecting sperm. Vitamin C is actively secreted into semen and is present at concentrations eight times higher than those found in the blood. It has been shown that if between 250mg and 1000mg vitamin C is given to males, sperm quality is significantly improved as vitamin C, by acting as an anti-oxidant, decreases sperm agglutination and decreases free radical attack.
In one study, 35 infertile men were given 500mg of vitamin C every twelve hours (i.e. twice a day) for one month. After only one week, the average percentage of sperm clumped together had dropped from 37% to 14%. After two weeks, sperm agglutination had dropped to 13% and at four weeks was down to 11%. A significant improvement in the overall quality of the men's sperm was observed, including the percentage of normal sperm present, sperm viability and sperm motility.
Research also shows that vitamin C protects the genetic material (DNA) of sperm against the oxidising reactions of free radicals. This reduces the risk of siring offspring with an inherited genetic disease.
The UK recommended reference nutrient intake of vitamin C is currently 40mg/day, based on the amount needed to protect against vitamin C deficiency disease (scurvy) and to maintain healthy tissues.
It has also been shown that vitamin E, when administered per se, improves sperm quality. Unlike vitamin
C, it is fat-soluble, which means it can penetrate cell membranes and body fats to protect them against oxidising free radical attacks.
The reference nutrient intake for vitamin E is 10mg/day. This is based on providing enough vitamin E to prevent oxidation of polyunsaturated fats in our diet.
However, fifty per cent of British men obtain less than 9.3mg per day.
Zinc is also known to have a role in sperm health, as it is essential for spermatogenesis. Zinc deficiency is known to cause low sperm count, low testosterone levels and male infertility. It also reduces male libido, and is associated with impotence.
Zinc plays a major role in sensitivity of tissues to sex hormones and zinc deficiency in men results in delayed puberty. Eighteen to twenty year old males who are zinc deficient remain prepubertal.
The new European recommended daily intake of zinc is 15mg per day, but 50% of British men obtain less than 10.9mg zinc per day.
However, with the present falling sperm count and the increase in the number of abnormal sperm, there is a need to find a way to promote sperm health more effectively.
We have now made the unexpected finding that a formulation comprising a combination of active ingredients acts synergistically, and is very beneficial to sperm health.
According to the present invention there is provided a formulation for sperm health comprising vitamin
E, vitamin C, zinc and betacarotene. Such a formulation could be suitably taken as a food supplement.
Preferably, the formulation comprises 50-200mg of vitamin E, 150-1000mg vitamin C, 5-20mg zinc and 7.5-20mg betacarotene.
Most preferably, the formulation comprises about 100mg vitamin E, 250mg vitamin C, lOmg zinc and 15 mg betacarotene.
Desirably, the formulation further comprises at least one binder and/or at least one flavour agent. The formulation could then be suitably taken by male subjects in tablet form as a food supplement. Examples of suitable binders are microcrystallic cellulose and magnesium stearate, and examples of suitable flavour agents are stearic acid and silica.
The present invention also provides the abovedescribed formulation or a pharmaceutical preparation thereof for use in medicine.
Although the formulation is preferably for use as a food supplement, it is also envisaged that the formulation could be administered to male subjects specifically for medical purposes for the improvement of sperm health and maintenance of sperm count levels.
By using this particular combination of antioxidants, it has been found that there is a significant synergistic effect.
In accordance with the present invention, it has been found that by using vitamin C and vitamin E together in a single formulation, the vitamin C regenerates vitamin E from its oxidised form into its reduced one, after the vitamin E has mopped up a superoxide free radical. Further, by combining betacarotene and zinc with vitamin C, their respective antioxidant effects free up more vitamin C to regenerate and protect vitamin E, thus keeping more of a substance called non-specific sperm agglutinin (NSSA) in its reduced form. NSSA is a seminal protein that binds to sperm and plays an important role in sperm clumping.
Vitamin E is a component of the non-specific sperm agglutinin. NSSA is made up of a protein, a sugar, vitamin
E and several sulphur-containing groups.
NSSA exists in either an oxidised or a reduced form. When in the reduced form, it binds to sperm heads through its sulfhydryl groups, and prevents sperm clumping together. This increases sperm motility.
When NSSA exists in its oxidised form, it cannot bind to sperm, and sperm therefore stick to each other. This causes them to clump together and become immobile, and if 20% or more sperm are affected, this leads to infertility.
It has been discovered that the use of a combination of active ingredients can prevent oxidation and keep the NSSA in a reduced form, which will improve sperm quality by decreasing clumping, and also such a formulation will mop up free radicals and decrease oxidation levels.
High levels of superoxide radicals in semen are linked with subfertility. Vitamin E will mop up these superoxide radicals and improve fertility. Also, vitamin E plays an important role in preventing sperm clumping and promoting motility. Vitamin E, as a fat-soluble antioxidant, also has an additional, beneficial effect on sperm motility as it improves sperm cell wall flexibility.
One of the benefits of the formulation of the present invention is that NSSA and vitamin E itself are maintained in a non-oxidised form by vitamin C. By acting as an antioxidant, vitamin C keeps the agglutinin in its reduced form so that it can bind to sperm and regenerates vitamin E.
It has also been found that betacarotene can be used effectively to assist vitamins E, C and zinc as an antioxidant to improve sperm health. As betacarotene is a water-soluble vitamin, it may protect sperm in semen from free radical attack in a similar way to vitamin C.
Further, it is believed that betacarotene may have a beneficial effect on sperm in its own right.
Vitamin A is thought to be important in sperm maturation whilst the sperm travels through the epididymis and beyond. Sperm vitamin A may also be important for the egg upon fertilisation.
Betacarotene is converted into vitamin A when body levels are low. Thus, the betacarotene acts both as a powerful antioxidant and, when necessary, is converted into vitamin A to assist sperm maturation.
Zinc is also an antioxidant and has likewise been found to act in synergy with vitamins C, E and betacarotene.
Increases in extracellular zinc cause corresponding increases in spermatozoal zinc, which inhibit sperm oxygen consumption by slowing sperm down within the male tract and conserving their energy. It now seems that zinc is involved in maintaining sperm in a transitory quiescent state until they enter the female reproductive tract.
In the female tract, zinc levels are low and zinc is rapidly removed from sperm, causing a sudden spurt of motility. Thus, zinc both acts as an antioxidant in synergy with vitamins C, E and betacarotene, and preserves sperm energy until it is required.
Zinc also protects sperm DNA (chromatin) from degradation and has a significant effect on the secondary structure (2D-shape) of human sperm protamines - proteins that condense 85% of sperm DNA into an insoluble, stable, nucleoprotein complex.
This is thought to be physiologically significant considering the high levels of zinc found in human sperm.
Sperm chromatin must be condensed for successful fertilisation.
This is another example of how zinc and antioxidant vitamins act synergistically to improve sperm health.
When a sperm meets an egg, it releases enzymes from a sac at the sperm head which digest the outer egg coating and allow sperm penetration. Sometimes, these enzymes are discharged early and spontaneously, which effectively renders a sperm no longer capable of fertilisation. Zinc has been shown to significantly reduce the number of sperm undergoing the acrosome reaction probably by altering membrane permeability to potassium.
This effect is reversible, so when zinc concentrations are reduced in the female tract, the acrosome reaction can again occur. This mechanism reduces the change of a spontaneous acrosome reaction occurring before the sperm reaches the egg and fertilisation can take place.
Thus, it will be realised that, although the individual components of the formulation of the present invention would be expected to show some positive effect on sperm health by acting as individual antioxidants, the components together act in synergy to exert numerous other beneficial effects on: sperm motility (Vitamin E, zinc), DNA integrity (Vitamin C, zinc), chromatin condensed structure (zinc), sperm maturation (betacarotene), inhibition of the acrosome reaction (zinc), preservation of sperm energy stores (zinc), reducing sperm clumping (vitamin C and vitamin E) and improved flexibility of sperm tails (vitamin
E), leading to improved motile efficiency.
In addition, vitamin C is essential for the regeneration of vitamin E once it has exerted its antioxidant effect. The vitamin E radical is inactivated, and the active vitamin reformed, by reaction with vitamin C in accordance with the following reaction:
ut-Tocopherol Semidehydro
ascorbate
Ascorbate ot-Tocopheroxyl radical
The synergistic effects of these ingredients on sperm health - especially in regard to NSSA function and the mopping up of free superoxide radicals - may help to reverse the observed downturn in sperm health.
In order to illustrate the present invention, the following example is given of a formulation in accordance with the present invention.
ExamDle
Vitamin C 250mg Active
Betacarotene 15mg Active
Vitamin E 100mg Active
Zinc Gluconate lOmg Active
Microcrystallic Cellulose 180mg Binder
Magnesium Stearate Binder
Stearic Acid Flavour Agent
Silica Flavour Agent
Claims (10)
- CLAIMS: 1. A formulation for sperm health comprising vitamin E, vitamin C, zinc and betacarotene.
- 2. A formulation according to claim 1, which comprises 50-200mg vitamin E, 150-1000mg vitamin C, 5-20mg zinc and 7.5-20mg betacarotene.
- 3. A formulation according to claim 2, which comprises 100mg vitamin E, 250mg vitamin C, lOmg zinc and 15mg betacarotene.
- 4. A formulation according to claim 1, 2 or 3, which further comprises at least one binder and/or at least one flavour agent.
- 5. A formulation according to claim 4, wherein the binder is microcrystallic cellulose and/or magnesium stearate.
- 6. A formulation according to claim 4, wherein the flavour agent is stearic acid and/or silica.
- 7. The use of a formulation according to any of claims 1 to 6 as a food supplement.
- 8. The use according to claim 7, wherein the food supplement is in tablet form.
- 9. A formulation according to any of claims 1 to 6 or a pharmaceutical preparation thereof for use in medicine.
- 10. The use of a formulation according to any of claims 1 to 6 or a pharmaceutical preparation thereof in the manufacture of a medicament for administration to male subjects for the improvement of sperm health and maintenance of sperm count levels.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB9407524A GB2289406A (en) | 1994-04-15 | 1994-04-15 | Vitamin, betacarotene and zinc composition for sperm health |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB9407524A GB2289406A (en) | 1994-04-15 | 1994-04-15 | Vitamin, betacarotene and zinc composition for sperm health |
Publications (2)
Publication Number | Publication Date |
---|---|
GB9407524D0 GB9407524D0 (en) | 1994-06-08 |
GB2289406A true GB2289406A (en) | 1995-11-22 |
Family
ID=10753612
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
GB9407524A Withdrawn GB2289406A (en) | 1994-04-15 | 1994-04-15 | Vitamin, betacarotene and zinc composition for sperm health |
Country Status (1)
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GB (1) | GB2289406A (en) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6410602B1 (en) * | 1997-12-09 | 2002-06-25 | Astacarotene Ab | Method of increasing the production and improving the quality of semen |
GB2379876A (en) * | 2001-08-03 | 2003-03-26 | Mars Uk Ltd | Foodstuff containing vitamin E, vitamin C and a carotenoid |
FR2884691A1 (en) * | 2005-04-21 | 2006-10-27 | Formquest Ltd | Oral composition, useful to prepare food complement to aid fertility and to prevent abortion and embryonic malformations, comprises mixture of antioxidizing agents and mixture of energizing elements |
Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB916659A (en) * | 1958-11-12 | 1963-01-23 | Michael Alexandre Colin | Improvements in or relating to compositions for oral, parental or rectal administration |
WO1992021368A1 (en) * | 1991-06-06 | 1992-12-10 | Life Sciences' Technologies, Inc. | Composition and method for disease treatment |
EP0564804A1 (en) * | 1992-04-10 | 1993-10-13 | Clintec Nutrition Company | Improved high protein liquid nutrition for patients with elevated wound healing requirements |
EP0596717A1 (en) * | 1992-11-05 | 1994-05-11 | Chandra Consultants | Nutritional supplement for the elderly |
WO1994013265A1 (en) * | 1992-12-11 | 1994-06-23 | Smith Milton G | A free radical quenching liposomal composition |
WO1994014458A1 (en) * | 1992-12-23 | 1994-07-07 | Abbott Laboratories | Medical foods for the nutritional support of infant/toddler metabolic diseases |
WO1995000130A1 (en) * | 1993-06-28 | 1995-01-05 | The Howard Foundation | Use of hydrophilic carotenoids for the manufacture of a medicament for the treatment of diseases having an oxygenation mechanism |
-
1994
- 1994-04-15 GB GB9407524A patent/GB2289406A/en not_active Withdrawn
Patent Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB916659A (en) * | 1958-11-12 | 1963-01-23 | Michael Alexandre Colin | Improvements in or relating to compositions for oral, parental or rectal administration |
WO1992021368A1 (en) * | 1991-06-06 | 1992-12-10 | Life Sciences' Technologies, Inc. | Composition and method for disease treatment |
EP0564804A1 (en) * | 1992-04-10 | 1993-10-13 | Clintec Nutrition Company | Improved high protein liquid nutrition for patients with elevated wound healing requirements |
EP0596717A1 (en) * | 1992-11-05 | 1994-05-11 | Chandra Consultants | Nutritional supplement for the elderly |
WO1994013265A1 (en) * | 1992-12-11 | 1994-06-23 | Smith Milton G | A free radical quenching liposomal composition |
WO1994014458A1 (en) * | 1992-12-23 | 1994-07-07 | Abbott Laboratories | Medical foods for the nutritional support of infant/toddler metabolic diseases |
WO1995000130A1 (en) * | 1993-06-28 | 1995-01-05 | The Howard Foundation | Use of hydrophilic carotenoids for the manufacture of a medicament for the treatment of diseases having an oxygenation mechanism |
Non-Patent Citations (3)
Title |
---|
CAS PLUS ONLINE Abstract Acc. No. 1994:491769 & CZ 278105 B 23.06.93 * |
CAS PLUS ONLINE Abstract Acc. No. 1994:686683 & CZ 278116 B 23.06.93 * |
CH 657967A 15.10.86 & WPI Abstract Acc. No. 86-298776/46 * |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6410602B1 (en) * | 1997-12-09 | 2002-06-25 | Astacarotene Ab | Method of increasing the production and improving the quality of semen |
GB2379876A (en) * | 2001-08-03 | 2003-03-26 | Mars Uk Ltd | Foodstuff containing vitamin E, vitamin C and a carotenoid |
AU783103B2 (en) * | 2001-08-03 | 2005-09-22 | Mars, Incorporated | Lara for use in reduction of DNA damage |
FR2884691A1 (en) * | 2005-04-21 | 2006-10-27 | Formquest Ltd | Oral composition, useful to prepare food complement to aid fertility and to prevent abortion and embryonic malformations, comprises mixture of antioxidizing agents and mixture of energizing elements |
Also Published As
Publication number | Publication date |
---|---|
GB9407524D0 (en) | 1994-06-08 |
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Legal Events
Date | Code | Title | Description |
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732E | Amendments to the register in respect of changes of name or changes affecting rights (sect. 32/1977) | ||
WAP | Application withdrawn, taken to be withdrawn or refused ** after publication under section 16(1) |