N-Acetyl-Carnosine Eye Drops

Recently Russian biochemists have been researching an analogue of the di-peptide carnosine called n-acetylcarnosine or NAC which they claim to be efficacious in the treatment of cataract.

N-acetylcarnosine was used in a clinical trial with 96 patients aged 60 and above. All the patients had senile cataract in various stages of maturity. The duration of the disease in these patients ranged between 2 and 21 years. The patients instilled 1 or 2 drops into each eye 3 - 4 times a day, for a range of 3 to 6 months. The results indicated a pronounced effect on primary senile cataract with all patients experiencing an improvement. Of the more mature senile cataract patients (long term cataract) about 80% exhibited improvements. There were no reported side effects in any patients.

Another Russian study using 49 volunteers of average age of 65 was designed to document and quantify the changes in lens clarity over a 6 to 24 month period. All patients suffered from senile cataract of a minimal to advanced opacification. The patients received either the NAC eye-drops or a placebo at a dose of 2-drops twice daily. The patients were then evaluated at 2 and 6-month periods. 6-months - 88.9% of all eyes treated with NAC had an improvement of glare sensitivity. 41.5% of all eyes treated with NAC had a significant improvement of the transmissivity of the lens. Importantly 90% of the eyes treated showed an improvement in visual acuity. The study also showed that at 24-months the NAC treated group maintained the improvement with the continued use of NAC eye-drops. No significant side effects were noted in the 2-year period.

Mechanism of action

Cataract develops when anti-oxidant defence is exhausted and when glycation leads to the cross-linking of crystalline lens proteins resulting in opacification. But, carnosine competes on the molecule for the glycating agent and protects cellular structures against aldehydes. Therefore, carnosine can slow and help to prevent proteins from becoming cross-linked (and in this case from becoming cataract).

When carnosine is delivered in high doses, it can reverse protein-aldehyde cross-linking (this reaction is normally very difficult to reverse). Under these circumstances, carnosine has been shown to have a “rejuvenating” effect on cultured cells.

Regular use of 1% NAC eye-drops, delivers high-dose carnosine through the aqueous humor to the crystalline lens to a level capable of reversing lens cross-linking and elimination of cataract. NAC (n-acetylcarnosine) eye drops do not suffer the same problem as L-carnosine eyedrops which fail to penetrate the cornea / conjunctiva and degrade easily. Once inside the eye’s aqueous humor the NAC provides bioavailable carnosine by transforming into L-carnosine (a process that occurs within 15 to 30 minutes). L-carnosine is an excellent anti-oxidant and is particularly effective against potent free-radicals. It is thought that the super anti-oxidant role of L-carnosine (within the aqueous humor) is a major factor, in the reversal of cataract.

NAC eye-drops appear to act as a universal anti-oxidant, both in the lipid phase of the cellular lens membranes, and in the aqueous environment.

References:

Boldyrev AA, Dupin AM, Bunin Aya, Babizhayev MA, Severin SE “The antioxidative properties of carnosine, a natural histidine containing di-peptide.” Biochem. Inrern., 1987, 15/6, 1105-1113.

Babizhayev MA et al “N-Acetylcarnosine, a natural histidine-containing di-peptide, as a potent ophthalmic drug in treatment of human cataracts.” Peptides (USA) 2001, 22(6): 979-994.

Babizhayev MA, Yermakova VN, Deyev Al, Seguin M-C “Imidazole-containing peptiomimetic NACA as a potent drug for the medicinal treatment of age-related cataract in humans.” J. Anti-Aging Medicine 2000, 2, 43-62.

Babizhayev MA, Yermakova VN, Semiletov yu A, Deyev Al “The natural histidine-containing di-peptide N-acetylcarnosine as an antioxidant for ophthalmic use.” Biochemistry (Moscow), 2000, 65, 588-598.

Babizhayev MA, Yermakova VN, Sakina NL, Evstigneeva RP, Rozhkova EA, Zheltukhina GA “N-Acetycarnosine is a prodrug of L-carnosine in ophthalmic application as antioxidant.” Clin. Chim. Acta., 1996, 254, 1-21.Babizhayev MA, Bozzo Costa E “Composizioni farmaceutiche contenenti N-acetilcarnosina per il trattamento della cataratta.” A61K gruppo 37/00 cap 20122 MI 15.10.1993. Italian patent.

Babizhayev MA, Bozzo Costa E “Pharmaceutical compositions containing N-Acetylcarnosine for the treatment of cataract.” European Patent PCT/EP 94/03340 10.10.1994 Ref. SCB 238 PCT.

Babizhayev MA, Seguin M-C, Gueyene J, Evstigneeva RP, Ageyeva EA, Zheltukhina GA “L-carnosine and carcinine act as natural antioxidants with hydroxyl-radical-scavenging and lipid peroxidase activities.” Biochem J. 304, 509-516.

Babizhayev MA, “Antioxidant activity of L-carnosine, a natural histidine-containing di-peptide in crystalline lens.” Biochem. Biophys. Acta., 1989, 1004, 363-371.

Methylcobalamin (Vitamin B12)

Vitamin B12 deficiencies have been mainly related to blood deficiency diseases, such as macrocytos and pernicious aneamia. Vitamin B12 deficiencies are followed by neurological and psychological disorders, such as disturbed sense of co-ordination, loss of memory, abnormal reflexes, weakness, loss of muscle strength, exhaustion, confusion, low self-confidence, incontinence, impaired vision, frequent need to pass water, psychological deviances.

Deficiencies can be caused by low intestinal B12 uptake (intestinal disorders), low intrinsic factor (a substance essential for its transport to the blood) in the stomach, deficiency of hydrochloric acid in the gastric juices (increasing with old age), regular use of laxatives or medicines like Losec (for treatment of peptic ulcer), low uptake in the central nervous system (CNS) or excessive B12 degradation. Lack of calcium in the food can also reduce the uptake and so can heavy metals.

The transport of vitamin B12 to the brain can be disturbed or interrupted by heavy metals such as inorganic mercury, which affects the blood-brain barrier by causing leakage and hampering the active transport of nutrients. Non-anaemic vitamin B12 deficiencies also play a role in diseases like Multiple Sclerosis, Fibromyalgia, Diabetes and Chronic Fatigue Syndrome. Schizophrenia, a psychotic condition, has been successfully treated with B12 injections in combination with other supplements. There also seems to be a connection between B12 deficiencies and cardiovascular diseases. Methylcobalamin acts as a cofactor for methionine synthase in the conversion of homocysteine to methionine, thus lowering blood levels of homocysteine.  Methylcobalamin acts as a methyl donor and participates in the synthesis of SAM-e (S-adenosylmethionine), a nutrient that has powerful mood elevating properties.

Vitamin B12 comes in many different forms – methylcobalamin, cyanocobalamin, hydroxocobalamin, being the most common. They are freely transformed into each other in the body however, vitamin B12 in the brain and CNS is only present as methylcobalamin. Supplemented Vitamin B12 in its active form, methylcobalamin, gives a much better result than other forms which have to be transformed into methylcobalamin. It is possible that the process of transformation itself is inefficient in many patients.

The uptake from oral methylcobalamin B12 supplementation is usually very low, approx. 1 %. Vitamin B12 is therefore often given intramuscularly. Subbuccal lozenges which is directly absorbed into the blood stream avoiding the need of injections are also available and preferred. Sublingual drops which are placed under the tounge, transdermal creams and nasal sprays are also available however due to its short half life in solution it needs to be used within 14 days of preparation.

Other benefits of methylcobalamin:
Regulate homocysteine

Protect against nerve damage, assist in nerve regeneration and diabetic neuropathy

Increase energy levels

Improve sleep

Reduce stress

Enhance growth and repair of all cells

Aid in metabolism of carbohydrates and fats

Improve protein synthesis

Improve immune function

Increase mental alertness

Special Note: Vitamin B-12 is not recommended in people who have mercury toxicity because it is a “methylator”. A methylator is a chemical that attaches a “methyl” chemical group onto another chemical. Methylation is an important process in the body however in the case of attaching a methyl group (CH-3) onto mercury, elemental mercury becomes methyl mercury (MeHg). MeHg is about 100 times more damaging to the nervous system than elemental mercury. MeHg has an affinity for the nervous system, so it will be attracted to the place where it can do the most damage. Therefore Vit B12 should be avoided in these patients and this may help explain why some patients actually get worse on Vit 12 supplements. If this is the case you should have your mercury levels tested. Vit B12 can be used once mercury has been removed from your system.

Glutathione, Reduced (GSH)

Glutathione (GSH) is classified as a ‘tripeptide’, which means it is composed of three amino acids. The human body produces glutathione from the amino acids Cysteine, Glutamic Acid and Glycine, and it is the key antioxidant compound required for vital functioning of all cells.

Glutathione is a powerful antioxidant essential for alleviating oxidative stress and protecting individual cells and tissues from free radicals. It is also known to enhance healthy growth and activity of immune cells needed for disease resistance and immune protection. In addition it enables the body to rid itself of unwanted toxins and heavy metals, detoxifying the liver, the body’s most concentrated source of glutathione; and protecting the body from today’s environmental pollutants, natural and synthetic toxins, genetically engineered processed foods and toxic waste.

Low levels of glutathione have been implicated in many autoimmune disorders and neurodegenerative diseases such as Parkinson’s, Autism, HIV, MS Rheumatoid Arthritis etc.
Raising the amount of glutathione in the blood, it will help bind the heavy metals and remove them from the body and also help brain and immune development for children with autism. Increasing glutathione levels and effectively improving detoxification of the liver has been found to increase language and awareness for these children.

Glutathione has also been used to help treat Aging, Autism, Cancer, Chemotherapy recovery, Chronic Fatigue Syndrome, for Detoxification, Drug addiction, Emphysema, Fibromyalgia, Glaucoma, Hepatitis, Hypoglycemia, Kydney disease, Liver disease, Liver cancer, Mercury poisoning,Parkinson’s disease, Respiratory problems such as cystic and pulmonary fibrosis, Smoking, Tuberculosis, to name a few.

How to administer GSH 

GSH is a very powerful antioxidant and therefore oxidizes rapidly in the presence of water. Therefore formulations such as nasal sprays should be avoided. Injections should be administered soon after being prepared and creams containing any water should also be avoided. Our laboratory produces a water free oily lotion which contains liposomes to aid transdermal absorption.This lotion bypasses the stomach and liver and thus provides glutathione into the blood stream and throughout the body.

Slow release capsules which minimize the destruction of GSH in the stomach aids absorption and is one of the best ways to concentrate glutathione in the liver for detoxification reactions. If you intend to use it for an overall systemic effect then the lotion, suppositories or nebules would be the preferred option.

Subbuccal lozenges and suppositories, which bypass the stomach and liver, increase levels in the blood to help boost energy levels. As a substantial amount of the lozenges may be swollowed and thus encounter the stomach and liver, therefore the suppositories would be the preferred option.

GSH administered by nebuliser is the best method for increasing GSH levels in the lungs for the treatment of pulmonary conditions. It is also one of the best ways for an overall systemic affect as it is readily absorbed into the blood stream nearly as rapidly as a injection. The dry nebulizer capsule contents are dissolved into 4ml of sterile or boiled water prior to being administered by a nebulizer. Once the capsule contents are dissolved the resulting solution is buffered and isotonic with a pH of about 6 which eliminates the irritation causes by acidic GSH. A 125mg capsule should be nebulized twice daily for maximum benefits.

Human Growth Hormone

Growth Hormone or human growth hormone, also known as hGH or somatotropin, is secreted by the pituitary gland into your blood stream where it stays for only a short time before it is metabolized by the liver into somatomedin-C (insulin like growth factor, IGF-1), which stays in the blood a lot longer and is actually the driving force behind all the remarkable properties of hGH. The highest levels are found in the blood during the first 3 to 4 hours hours of sleep at night.

The production of hGH peaks during adolescence, reaching around 1.5mg/day, and then gradually drops off after the age of 20 to 25 where it averages around 0.35mg/day and continues to decline by approximately 14% each decade for the rest of your life. By the time you are 60 to 70 years of age you only produce about 15% of the amount produced at your peak. The decline in hGH with age is directly associated with many symptoms of aging including wrinkles, grey hair, hair loss, decreased energy, decreased sexual function, loss of muscle mass, increase in body fat, depression, cardiovascular disease, osteoporosis, and overall lower life expectancy.

Low hGH has also been related to elevated cholesterol, elevated apolipoprotein, thin skin, lack of collagen, decreased nail and hair growth, poor thermo-regulation, dehydration, emotional instability, poor memory, reduced energy, hypoglycemia, insulin resistance, abnormal metabolic rates, to name a few. Low levels of hGH cause aging because it is responsible for growth and regeneration of every cell in our bodies.

There is now ample evidence which demonstrates that by replacing hGH levels we can dramatically reverse all of these symptoms. The more closely the scientific evidence is examined the clearer it becomes that everything we associate with aging may be due in part to the decline of hGH in our bodies.

Many of the beneficial effects of supplementing hGH are listed below:

1. Improves lean muscle/body fat ratio – this not only improves strength and vitality in aging people but also for those with muscle wasting disorders such as stroke and recuperation from surgery or long hospitalization.
2. Positive effects on the heart – it improves cardiac impairment, blood pressure and HDL levels while reducing cholesterol, LDL and triglycerides.
3. Osteoporosis – it reverses osteoporosis with a 30 to 40% increase in bone formation in only 12 weeks. It also stimulates cartilage formation which may play a roll in degenerative arthritis.
4. Improved Wellbeing – Most patients report across the board that they suffer less aches and pains, increased strength, better energy levels, hair growth, reduction in wrinkles, increased sexual function, and a general sense of wellbeing.
5. Brain Function – it improves memory, alertness, motivation, and very importantly it restores slow wave sleep paterns.
6. Improves Immune Function – it restores thymus gland function, stimulates the production of antibodies, T and B macrophages, natural killer cells and reduces the risk of certain cancers.

hGH is considered a very safe hormone to administer when it is administered in regular physiological doses which mimic the bodies own natural secretions and should only be used in cases where current levels are shown to be deficient or suboptimal. Therefore it is only used for growth hormone deficiency syndrome and should be monitored by an experienced physician. Deficiencies start to occur when levels IGF-1 levels fall below 33nmol/L in men and 24nmol/L in women. The aim of therapy is to supply the shortfall and bring the level back into the optimal physiological range which is 39 to 46nmol/L in men and 29 to 40nmol/L in women.

Many traditional medical doctors with no experience in hGH supplementation consider hGH therapy unorthodox and usually criticize the idea out of fear of the unknown, however those in the know are well aware of its benefits and restorative properties and its relative safety when used correctly.

Some side effects have been reported, usually when taking larger pharmacological doses. These include water retention in hands and feet, carpet tunnel syndrome, tingling in fingers and nose, hormone imbalances and enlargement of the hands and feet. These side effects are reversible when doses are reduced. 

It is important to monitor your hGH levels to ensure the dose you are taking provides you with a normal physiological level There are several ways to determine hGH levels however most have many drawbacks. A common way is to measure IGF-1 in serum however this is considered unreliable in thyroid disorders, poorly controlled diabetes, liver disease and malnutrition. Research also indicates about 25% of patients on hGH actually experience a decline in IGF-1 levels. Therefore one of the best ways to determine growth hormone levels is a 24hour urine analysis. By closely monitoring your levels you can ensure your dose is appropriate thus maximizing its benefits while minimizing any potential side effects of potentially escalating levels.

Growth Hormone replacement has its drawbacks as it has to be administered as a daily subcutaneous injection. This is the only way hGH will work as nasal sprays, tablets and creams often advertised on the internet are not bioavailable and therefore ineffective. It is also expensive, even though the price has halved in the last few years now costing between $285 to $570 a month depending on the dose being used. The price is expected to continue to decline with pharmaceutical patents running out and more competition.

There are many natural products, proteins, amino acids, herbs, etc on the market reported to increase the bodies own production of growth hormone. We have had experience with many of them and found  them to produce only slight increases in hGH levels which were not significant enough for any  therapeutic effects. None of these products have proven to come even close in comparison to taking the real authentic hormone itself.