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| N-Acetyl-Carnosine
(Can-C™) Eye Drops - The Cure For Cataract? |
Dr.
Robert Mason |
A
Doctor's Point of View
Robert
Mason PhD - International Guide to Anti-Aging Drugs
NOTE:
This articleis provided with the expressed permission of IAS and Dr.
Mark Babizhayev of Moscow and is under full copy write protection
of Dr. Robert Mason.
|
In
the East and particularly in Russia
over the last several years, they have been researching a special analogue
of the di-peptide carnosine. This particular form is known as N-acetylcarnosine
or NAC and it has been proven to be highly efficacious in the treatment
of cataract and may also present a case for the prevention of the same.
This article is about the case for NAC and the problems associated with
senile-cataract.
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) has 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 Rarely Discussed.. There
is another aspect to the problem that is rarely discussed. While cataract
surgery is generally recognized 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 laser treatment. |
|
Since
the number of cataract operations is so large, even a small percentage
of complications represent 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 recognized. 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
Develoment of N-acetylcarnosine (Can-C™) Eye Drops
N-acetylcarnosine
Eye Drop Information Page - Click Here
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Innovative
Vision Products (IVP)
is
a US based corporation, operating in Russia (utilizing Russian researchers
and scientists),  who
have over the last several-years developed and tested a unique new form
of carnosine. This form of carnosine is known as n-acetylcarnosine or
abbreviated to NAC.
NAC presents the first major leap forward in the treatment and possible
prevention of senile cataract. As a bio-engineering company, IVP has
developed a proprietary method of producing extremely high purity NAC,
which has proven to be a suitable ophthalmic drug for the non-surgical
treatment of age-related cataracts. Yet it also displays high efficacy
and physiological tolerance.
NAC has a highly statistical and very significant
clinical success rate for patients within 3-12 months of treatment.
Not surprisingly, IVP has been quick to ensure that its NAC has worldwide
patents, including its use for cataract. It is also interesting to note
that NAC eye-drops are patented for use in open-angle glaucoma, but
as yet, the research for that disorder remains unpublished. [Ed.- We
are keen to report on NAC's benefit for glaucoma as soon as it becomes
available, especially as this is an eye-disorder that is extremely difficult
to treat].
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 patient's 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 NAC 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 NAC 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 NAC had a significant improvement of
the transmissivity of the lens, but perhaps most importantly 90%
of the eyes treated with NAC 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 NAC treated group, (who
already had significant improvement to the quality of their eyesight),
sustained these results with continued use of the NAC
eye-drops. Once
again, no significant side effects were noted in
any cases throughout the 2-year period.
Another
interesting study 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 NAC eye-drops
are a safe, effective treatment and potential preventative against
cataract. N-acetylcarnosine
Eye Drop Information Page - Click Here |
NAC
Method of Action
 Cataract
is 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. But, carnosine is known to compete on the
molecule for the glycating agent and protect cellular structures against
aldehydes. Therefore, carnosine can slow and help to prevent proteins
from becoming cross-linked, (and in this case from becoming cataract).
NAC
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 NAC 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 an excellent anti-oxidant and is particularly effective against potent
free-radicals, especially 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. So, NAC may act as a "carrier" for L-carnosine
delivering it to where it is needed, [Ed.-see the next section of
this article for further comparisons of NAC to L-carnosine].
The powerful anti-oxidant abilities of carnosine within the eye, and
the prevention of cross-linking, helps to explain why NAC is effective
at preventing and slowing cataract, perhaps even halting it. But it
doesn't explain why NAC 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 defense is 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% NAC 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,
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.
NAC eye-drops reduce and protect the crystalline lens from oxidative
stress-induced, cross-linking damage.
NAC
compared to L-carnosine
We
may logically ask the question; why have NAC 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? Dr. Mark Babizhayev,
(Link to babizhayev interview) one of the principal Russian researchers
behind the clinical trials with NAC eye-drops gave us this reply to
that very same question. |
 "I
believe that the application of simple L-carnosine for the treatment
of human cataracts is misleading. This is because L-carnosine, by
itself, readily becomes a substrate for the activity of natural peptidases
(i.e. carnosinase) in the aqueous humour to the degree that there
is virtually no sign of L-carnosine in the aqueous humour within 15
minutes after instillation.
Furthermore,
I consider that L-carnosine, in the form of eye-drops, may be harmful
to the eyes because it gradually releases histamine, which, located
as it would be in the presence of the eye-lens, is a very toxic agent.
NAC eye-drops however
are resistant to hydrolysis with natural carnosinase. Therefore, our
patented NAC is the only currently known agent which reverses and
prevents
human cataracts." Mark
Babizhayev MA, PhD |
In
conjunction with Dr. Hipkiss and Dr. Kyriazis information,
we can conclude that while some of the benefits of oral L-carnosine
may derive after carnosinase breaks down into histamine that in the
form of eye-drops, simple L-carnosine must be avoided.
It is also interesting to note that a study by Dr. Boldyrev et al,
also concluded that even the oral use of NAC was far less likely to
be broken down by carnosinase than simple L-carnosine.
Dr.
Mark Babizhayev also makes it quite clear that "ordinary"
L-Carnosine will not be of much use in the treatment of senile-cataract.
This is because there are many synthesized "carnosines"
and their biological and medicinal activity strongly varies and depends
on the mode of their obtention. Ed.- see
Dr. Babizhayev Interview
N-acetylcarnosine
Eye Drop Information Page - Click Here |
The
Cataract Cure
By
Marios Kyriazis MD
 This
book highlights the Russian breakthrough for the treatment and prevention
of senile cataract using an eye-drop. It is the story of N-acetylcarnosine,
and Dr. Kyriazis book contains details of how it should be used to
achieve the best results, what to look out for and case studies. A
number of aging eye disorders are mentioned (i.e., glaucoma, macular
degeneration, dry eye syndrome) and how they can be eased. This is
the first book to attempt to bring to the fore the various international
breakthroughs for the alleviation degenerative eye disease.
Click
here to order book
|
| For
example, if carnosine is extracted from meat muscle substances, the
biological and anti-oxidant activity is very low. This is presumably
due to the contamination of the "pure" carnosine substance
by heavy metal salts and proteins and other related impurities. It is
very difficult to purify carnosine chromatographically, as the compound
chelates divalent metal ions very heavily and the biological and anti-oxidant
activities can not be regenerated during the purification procedures.
In
conclusion there were many forms of carnosine, which were
abandoned, in the Russian studies because of their lack of anti-cataract
and anti-oxidant ability in the human eye,. However, Innovative
Vision Products (IVP), in conjunction with their Japanese partner
and manufacturer, have developed a synthesized pure NAC which has
biological activity and has been well controlled and proven in human
lens studies. This is the formula that has been used in the clinical
trials.
IVP holds the proprietary knowledge to the correct and efficient production
of high-purity NAC. If the label doesn't state it is formulated
by Innovative Vision Products (IVP), then the source of the raw material
is NOT the one that the clinical trials were conducted with. "Unknown"
sources of carnosine eye-drops should be avoided, as the material
could be ineffective, and possibly even dangerous to the human eye.
"Cataract
is a widespread age-related affliction and NAC 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." -
Mark
Babizhayev MA, PhD |
Back
References:
1. 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.
2. 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.
3. 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.
4. 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.
5. 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.
6. 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.
7. 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.
8. 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.
9. Babizhayev MA, "Antioxidant activity of L-carnosine, a natural
histidine-containing di-peptide in crystalline lens." Biochem.
Biophys. Acta., 1989, 1004, 363-371.
10. Babizhayev MA, Deyev Al "Lens opacity induced by lipid peroxidation
products as a model of cataract associated with retinal disease."
Biochim. Biophys. Acta., 1989, 1004, 124-133.
11. Babizhayev MA, Deyev Al "Free radical oxidation of lipid
and thiol groups in genesis of cataract." Biophysics (biofizika),
1986, 31, 119-125, Pergamon Journals Ltd.
12. Kantha S, Wada S, Tanaka H, Takeushi M, Watabe S, Ochi H (1966),
Biochem. Biophys. Res. Commun. 223, 278-292.
13. Babizhayev MA, Deyev Al, Linberg LF "Lipid peroxidation as
a possible cause of cataract." Mech. Ageing Dev. 1988, 44, 69-89.
14. Boldyrev AA, "Problems and perspectives in studying the biological
role of carnosine" International Center for Biotechnology, Department
of Biochemistry, Lomonosov, Moscow State University.
15. Hipkiss A, (1998) Int. J. Biochem. Mol. Biol., 30, 863-868.
16. Boldyrev AA, Dupin A, Bunin A, Babizhayev MA, Severin SE (1987),
Biochem. Int., 15, 1107-1113.
17. Wang AM, Ma C, Xie H, F Shen "Medical application of carnosine
" Department of Biochemistry and Neurobiology, Harbin Medical
University, China.
18. World Health Organisation, Ageing and Health, Website: http://www.who.int/ageing/scope.htm
DISCLAIMER: ALL INFORMATION IS EDUCATIONAL AND DOES NOT, AND SHOULD
NOT, REPLACE THE ADVICE OF YOUR PHYSICIAN.
Last Updated: Tuesday, July 20, 2004 |
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