Is N-acetylcarnosine the cure for cataract? Press Release Article The 3rd Annual Monte Carlo Anti-Aging Conference
By Robert Mason Ph.D. and Phil Micans PharmB.

Cataract is the leading cause of blindness and accounts for about 42% of all such cases worldwide, and this is in-spite of the availability of effective surgical treatment. Today we have the appalling situation where more than 17 million people around the world are blind because of cataract and 28,000 new cases are reported everyday. In developing countries, there is simply not a sufficient number of surgeons to perform cataract operations.
Cataract surgery is the most commonly performed surgical procedure in people over 65-years of age, and 43% of all visits to ophthalmologists by Medicare patients in the US are directly associated with cataract.
Meanwhile, approximately 25% of the population over 65, (and about 50% over 80) have a serious loss of vision due to cataract. Since this is the population that is most susceptible to lens opacification and as this section of the population is expected to increase dramatically, the numbers of individuals with cataract is set to explode!
For example, the World Health Organization anticipates that within the next 25-years, that 20% of the population will be 65 or older. Furthermore, the single largest growing section of the population are those over 85 and their actual numbers are expected to quadruple in about the same period. Such a rapidly burgeoning older population can only increase the numbers of individuals suffering from cataract.
Of course, there is also the economic impact. Currently 1.35 million cataract operations are performed annually in the United States alone and Medicare estimates the annual cost at $3.5 billion! There's no doubt about it, cataract is a major disease.
It is also becoming apparent that it will not be possible to eliminate the overall problems (including blindness), caused by cataract with the current procedures. With so many people presenting the afflictions of maturity onset cataract, it appears not to be possible to train in-time, the necessary numbers of surgeons required. In-fact, as-it-stands, it looks likely that the total number of people with serious eye-disorders because of cataract, will increase dramatically worldwide.

Surgical complications:
There is another aspect to the problem that is rarely discussed. While cataract surgery is generally recognised as being one of the safest operations, there is a significant complication rate. For example, in the United States 30% to 50% of all patients having cataract extraction, develop opacification of the posterior lens capsule within two years and require further lazer treatment.
Since the number of cataract operations is so large, even a small percentage of complications represents a significant number of people. Of the patients having cataract surgery, 0.8% have retinal detachments, 0.6% to 1.3% are hospitalized for corneal edema (or require corneal transplantation), and 0.1% present endophthalmitis.
Thus, aside from secondary cataract, about 2% of the 1.35 million (or approximately 27,000 individuals), just in the US each year, develop serious complications as a result of cataract surgery. It is therefore difficult to support the argument that cataract research is unimportant with statistics such as those cited above. The large and growing number of people blind with cataract and the significant complication rate, should be sufficient reason to increase cataract research.
The considerable discomfort experienced by patients as their vision diminishes, and the complete loss of accommodation resulting in the removal of the lens should also be recognised. Besides the possible complications, an artificial lens just does not have the overall optical qualities of a natural lens.
A medical solution is required that will maintain the transparency of the lens. Even if the development of cataract can be delayed by 10-years, the overall benefits would be highly significant.

The development of N-acetylcarnosine:
Russian researchers and scientists and over the last several-years have developed and tested a unique new form of the di-peptide, carnosine. This form of carnosine is known as n-acetylcarnosine and it appears to be the first major leap forward in the treatment and possible prevention of senile cataract.
Since having developed a proprietary method of producing extremely high purity N-acetylcarnosine, (that has proven itself to be a suitable ophthalmic drug for the non-surgical treatment of age-related cataracts), N-acetylcarnosine also displays high efficacy and physiological tolerance.
N-acetylcarnosine has a highly statistical and very significant clinical success rate for patients within 3-6 months of treatment. Not surprisingly, many worldwide patents, including its use for senile cataract, have already been issued. It is also interesting to note that N-acetylcarnosine eye-drops are patented for use in open-angle glaucoma, but as yet, the research for that disorder remains unpublished.

Human trials:
Carnosine eye-drops were used in a clinical trial to treat 96 patients aged 60 and above. All the patients had senile cataract in various degrees of maturity. The duration of the disease in these patients ranged between 2 and 21 years. Firstly, the researchers stopped the patients use of all other anti-cataract drugs. Then the patients instilled 1 or 2 drops into each eye 3 or 4 times a day, for a period of 3 to 6 months.
The level of eyesight improvement and the change of lens transparency was considered as an evaluation index. The results showed that there was a pronounced effect on primary senile cataract, the effective rate was 100% (i.e. all patients experienced an improvement). For the more mature senile cataract (i.e. those who had had the cataract the longest time, in some cases more than 20-years), the effective rate was still an extremely impressive 80%.
These are remarkable results considering that the best that could normally be expected would be a slight improvement, a halt to the progression and under normal (i.e. non-treated) circumstances, a continual worsening of the disease. Importantly, it was also noted that there were no side effects noted in any of the cases.
Another Russian study was designed to document and quantify the changes in lens clarity over a 6 to 24 month period for 49 volunteers. Their average age was 65 and all suffered from senile cataract of a minimal to advanced opacification. The patients received either a 1% solution of N-acetylcarnosine eye-drops or a placebo, (as 2-drops twice a day into each eye). The patients were then evaluated at 2 and 6 month periods. The tests consisted of ophthalmoscopy (glare test), stereocinematagraphic (slit-image) and retro-illumination (photography). A computerized digital analysis then displayed the light scattering and absorbing effects of the centers of each lens.
At 6-months, 88.9% of all eyes treated with N-acetylcarnosine had an improvement of glare sensitivity (lowest individual score was a 27% improvement, right the way up to a 100% improvement). 41.5% of all eyes treated with N-acetylcarnosine had a significant improvement of the transmissivity of the lens, but perhaps most importantly 90% of the eyes treated with N-acetylcarnosine showed an improvement in visual acuity. Meanwhile, in the placebo group there was little change in eye quality at 6-months and a gradual deterioration at 12 to 24 months.
Importantly, this study also showed that at 24-months the N-acetylcarnosine treated group, (who already had significant improvement to the quality of their eyesight), sustained these results with continued use of the N-acetylcarnosine eye-drops. Once again, no significant side effects were noted in any cases throughout the 2-year period.
Another interesting study also evaluated patients between the ages of 48 and 60, who had various degrees of eyesight impairment, but who did not have the symptoms of cataract. After a course of treatment ranging from 2 to 6 months the conclusion was, that the eye-drops alleviated eye-tiredness and continued to improve eyesight (i.e. there was more clear vision). The subjects reported that the treatment "brightened" and "relaxed" their eyes. This is an important indicator that the eye-drops have a value both for preventative purposes, as well as medical applications.
At this time, it is now believed that carnosine eye-drop treatment has been applied to over one thousand patients with senile cataract in China and Russia, (those countries are home to the principal researchers behind the work). Clear evidence is emerging that N-acetylcarnosine eye-drops are a safe, effective treatment and potential preventative against senile cataract.

N-acetylcarnosine's method of action:
Cataract is primarily a glycosylation problem. This reaction occurs when proteins became cross-linked (and hence impaired). The result of this reaction leads to the discoloration of the eye-lens to yellow and brown, and hence the impairment of vision.
As carnosine is known to compete on the molecule for the glycating agent and protect cellular structures against aldehydes, carnosine can therefore slow and help to prevent proteins from becoming cross-linked, (and in this case from becoming cataract). N-acetylcarnosine has been shown to be highly resistant to carnosinase, (the natural enzyme that breaks down L-carnosine into histamine etc.). An experiment on rabbits showed that N-acetylcarnosine eye drops allow themselves to be broken down into L-carnosine once inside the eye's aqueous humor, (a process that occurs within 15 to 30 minutes after application of the eye-drops).
L-carnosine is a potent anti-oxidant and is particularly effective against "extreme" free-radicals, such as the Superoxide and the Hydroxyl. It is therefore presumed, that the anti-oxidant role of L-carnosine (within the aqueous humor), is a major factor in slowing and preventing the appearance of cataract.
However, when L-carnosine eye-drops were used there was no presence of L-carnosine in the aqueous humor, (even after 30-minutes). This may be because L-carnosine is broken down early into histamine etc., before it reaches the aqueous humor. N-acetylcarnosine may act as a "carrier" for L-carnosine delivering it to where it is needed. So the powerful anti-oxidant abilities of carnosine within the eye, and the prevention of cross-linking, helps to explain why N-acetylcarnosine is effective at preventing and slowing cataract, perhaps even halting it. But it doesn't explain why N-acetylcarnosine has been shown to reverse cataract. But we may already know the answer.
However, when L-carnosine eye-drops were used there was no presence of L-carnosine in the aqueous humor, (even after 30-minutes). This may be because L-carnosine is broken down early into histamine etc., before it reaches the aqueous humor. N-acetylcarnosine may act as a "carrier" for L-carnosine delivering it to where it is needed. So the powerful anti-oxidant abilities of carnosine within the eye, and the prevention of cross-linking, helps to explain why N-acetylcarnosine is effective at preventing and slowing cataract, perhaps even halting it. But it doesn't explain why N-acetylcarnosine has been shown to reverse cataract. But we may already know the answer.
For example, it is known that when carnosine is delivered in high doses, that 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. Cataract develops when anti-oxidant defenses are exhausted, leading to the cross-linking of the lens crystallins, (producing a clouded lens, and hence impaired eyesight). We can assume that the regular use of a 1% N-acetylcarnosine eye-drop (as used in the clinical trials), delivers "a high-dose of carnosine capable of reversing the lens cross-linking," and hence the reduction and eradication of cataract. So in conclusion, N-acetylcarnosine 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. N-acetylcarnosine eye-drops reduce and protect the crystalline lens from oxidative stress-induced, cross-linking damage.

N-acetylcarnosine compared to L-carnosine:
We may logically ask the question; why have N-acetylcarnosine eye-drops been shown to have this action upon cataract, and yet L-carnosine (which is its sister di-peptide) appears to have little benefit? Mark Babizhayev Ph.D., one of the principal Russian researchers behind the clinical trials with N-acetylcarnosine eye-drops gave us this reply to that very same question: "I believe that the application of L-carnosine for the treatment of human cataracts is misleading. This is because L-carnosine readily becomes a substrate for the activity of natural peptidases (i.e. carnosinase) in the aqueous humor. So much so, that there is no sign of L-carnosine in the aqueous humor within 15 minutes after instillation. Furthermore, I consider that L-carnosine eye-drops may even be harmful for eyes because it gradually releases histamine, which, located as it would be in the presence of the eye-lens is a very toxic agent. However, N-acetylcarnosine eye-drops are resistant to hydrolysis with natural carnosinase. Therefore, N-acetylcarnosine is the only currently known agent which reverses and prevents human cataracts." The scientists, Dr. Hipkiss and Dr. Kyriazis have concluded that some of the benefits of oral L-carnosine probably derive after carnosinase breaks down into histamine. However, it would appear that in the case of eye-drops, L-carnosine must be avoided.

Conclusion:
Cataract is a widespread age-related affliction and N-acetylcarnosine eye-drops appear to be a highly efficacious and safe treatment for cataract. As such, I suspect that this supplement is going to become one of the most important new discoveries, and will have a major impact on the way that cataract is controlled.