WO2004035059A1

WO2004035059A1 - Composition for the regulation of the human immune system and the prevention and treatment of diseases thereof

Info

Publication number: WO2004035059A1
Application number: PCT/CA2003/001451
Authority: WO
Inventors: Alan Fergusson; John Charles Davidson
Original assignee: Alan Fergusson; John Charles Davidson
Priority date: 2002-10-16
Filing date: 2003-09-24
Publication date: 2004-04-29
Also published as: AU2003271442A1; CA2407429A1; CA2407429C

Abstract

A new composition of natural products consisting of phytosterols, anti-oxidants, and complexes that include, but are not restricted to, hydrolysates of fatty acids, amino acids, peptides, proline rich polypeptides and digestive enzymes, formulated to boost or modulate the Human Immune System; to prevent or treat immune system diseases; to inhibit or reduce cancer cell growth in breast, colon and prostate cancer cases; to maintain CD4 Lymphocyte counts in HIV patients; and to treat enlarged prostate problems. In the preferred form, the invention comprises: phytosterols, antioxidants, together with hydrolysates of fatty acids derived from fish synergistically incorporated on plant protein carriers, amino acids, short chain peptides, proline rich polypeptides and digestive enzymes, and a micro-cellulose filler.

Description

TITLE:

COMPOSITION FOR THE REGULATION OF THE HUMAN IMMUNE SYSTEM AND THE PREVENTION AND TREATMENT OF DISEASES THEREOF.

FIELD OF THE INVENTION:

This invention relates to the field of the Human Immune System and to the prevention and treatment of diseases thereof.

DISCRETION:

This invention is a new composition of natural products formulated to regulate the Human Immune System and to prevent and treat diseases thereof. The formulation is novel and unique because it combines phytosterols with anti-oxidants and fatty acid complexes.

The inherent ingenuity of the invention is the discovery of the range of the amount of beta-sitosterol that is the most effective to achieve the goal of regulating the Human Immune System and the prevention treatment of diseases thereof. As a result, this new composition need only be taken once a day to maintain general health.

The further uniqueness of the invention is the discovery that combining phytosterols with anti-oxidants and fatty acid complexes produces a synergism whereby the cumulative total effect of the composition was greater than the sum of the individual effects of the respective components. As a result, this new composition optimizes the immune system to deal with viral and bacterial infections, while also protecting the body from degeneration due to free radical damage.

Additionally, the invention is original and novel because it not only assists in preventing possible causes of cancer, but, it inhibits or reduces cancer cell growth in breast, colon and prostate cancer cases, and facilitates the removal of the dead tissue arising from the death of the said tumors.

The utility of said invention is further demonstrated and confirmed by the fact that it accomplishes its goals with none of the physical or psychological side effects of traditional treatments such as radiation, chemotherapy and surgery.

The basis of the present invention is the use of a combination of phytosterols, anti-oxidants and fatty acid complexes for the following purposes:

1. To boost or modulate the Human Immune System;

2. To prevent or treat diseases of the Human Immune System, for example:

- Common cold and flu

- Viral and bacterial infections

- Allergies

- Rheumatoid Arthritis

- Lupus

- Chronic Fatigue Syndrome;

3. To inhibit or reduce cancer cell growth in breast, colon and prostate cancer cases;

4. To maintain CD4 Lymphocyte counts in HIV patients;

5. To treat enlarged prostate problems; and,

6. As an anti-inflammatory agent. Although preferred compositions to achieve these ends are listed below, they are by no means to be interpreted as limiting the broad scope of the present invention as various other combinations of phytosterols, anti-oxidants and fatty acid complexes may achieve the same beneficial results.

The preferred composition of the present application consists of 400mg capsules containing 300mg of phytosterols (a minimum of which is 117mg of beta-sitosterol), 50mg essential fatty acid complexes, 20mg broad spectrum antioxidants, and 30mg micro-cellulose filler. In another preferred form, the composition comprises from 29% to75% beta-sitosterol, 10% to 50% essential fatty acid complexes and from 5% to 50% antioxidants.

A further innovative feature of the invention is the discovery that the essential fatty acid complexes together are not only themselves a immune system modulator, but also optimize the body's absorption of beta-sitosterol and antioxidants.

This invention is a composition of natural products that is designed to stimulate the body to marshal its own natural defenses against allergies and other immune related disorders, breast, colon and prostate cancer, and AIDS, as opposed to alleviating or preventing these disorders with chemical or synthetic products. Many of the traditional treatments have severe side effects, which in the case of prostate cancer can include impotence and incontinence, and in the case of chemotherapy, severe depression of the immune system. Traditional treatments also only treat the tumors, i.e. the symptoms, and not the underlying cause, and in the case of chemotherapy, leave dead tissue to be removed from the body.

One of the suspected causes of cancer is free radical damage on cellular components such as DNA or the cell membranes. Free radicals are the natural by- products of many processes within and among cells. They are also created by exposure to various environmental factors such as tobacco smoke and radiation. Once formed these highly reactive radicals can start a chain of reactions that can result in damage to cell walls, certain cell structures, and the genetic material within the cells such as DNA,

In the preferred form this composition contains one of the world's most advanced anti-oxidant complexes, Enzogenol™, produced by Enzo Nutraceuticals through a patented process that creates an aqueous extract from Pinus Radiata (pine bark), which is a superior source of proanthocyanidins and flavonoids. This technically advanced anti- oxidant complex provides an excellent source of free radical scavengers.

In addition to scavenging free radicals, the Enzogenol™ in this composition can stimulate phagocytosis, an immune system response in which cells ingest and eliminate harmful micro-organisms and foreign heavy metals, and hence facilitates the removal of the by-products of cell death.

Research has shown that the Human Immune System can be stimulated by beta- sitosterol. This composition contains this remarkable phytonutrient which has been shown to be effective in inhibiting cancer cell growth and accelerating cancer cell death in breast, prostate and colon cancer. It can also reduce metastases to lymph nodes.

Research at the University of New York at Buffalo by Awad, Downey and Fink has shown that beta-sitosterol can inhibit breast cancer cell growth by 66% after 3 days and 80% after 5 days. It can also increase the rate of cell death by 600% (Int. J. Mol. Med 2000 May 5(5)). Research by the same group has also shown that beta-sitosterol can inhibit prostate cancer cell growth by 24% and increase cell death by 400% (Nutr Cancer 1998; 32 (1)). Similar research on colon cancer cells showed a reduction in cell growth of 55% (Anti Cancer Res. 1998 Mar- Apr 18 (2a)). The exact mechanism behind the inhibition of cancer cell growth and the increase in apoptosis is not yet fully understood, but may be related to the increase in T-cell proliferation produced by beta-sitosterol (Int. Jnl. Immuno Pharmacol 1996 vol 18 Bouic et al). Beta-sitosterol has been shown to maintain CD4 lymphocyte count in AIDS patients( AIDS Bulletin Summer 97).

The benefits of the antioxidants together with the beta-sitosterol to scavenge free radicals and to kill and remove tumors can only be realized if the human body actually absorbs both the anti-oxidant complex and the beta-sitosterol. The role of the essential fatty acid complex is to ensure that the anti-oxidant complex and the beta-sitosterol are absorbed. The essential fatty acid complex itself is a proprietary blend of functional proteins harvested from cold sea fish by a special process, together with essential fatty acids, amino acids, proline rich peptides and short chain poly-peptides. This complex also happens to be an immune system modulator, and consequently also supports the body's attack on cancer by promoting and supporting the T-cell proliferation initiated by the beta-sitosterol.

The combined effects of the antioxidant complex, the beta-sitosterol and the essential fatty acid complex on breast, colon and prostate cancers are to reduce the risk of the formation of new cancers through the more effective scavenging of free radicals, to inhibit the growth and increase the rate of cell death of the tumors, and to assist the body in disposing of dead tumor cells.

This formulation has been used to treat a 68 year old male with a PSA of 17. Over a six month period his PSA, (the normal measure of prostate cancer which would normally increase over time), dropped to 11.8, a reduction of over 30%, with no side effects.

The combined immune modulating properties of beta-sitosterol, antioxidant complex, and the essential fatty acid complex also make this formulation an excellent anti-allergen with no side effects which is also new and unique in the field of anti- allergens. This formulation has been used to treat several adults with ages ranging between 22 and 52 with excellent results occurring in the space of five to six days, again with none of the side effects normally associated with anti-allergens.

Early trials of this unique formulation have also shown the capacity to alleviate such immune related disorders as rheumatoid arthritis, again with none of the adverse side effects normally associated with the remedies traditionally used in this area.

In addition, the effectiveness of beta-sitosterol in mamtaining the CD4 lymphocyte count in AIDS patients can be increased by the addition of the antioxidant and essential fatty acid complexes in this formulation, again providing an important new application for this new and unique formulation.

Normally capsules are taken once a day, one hour before and at least 2 hours after food, with water or fruit juice ( NOT milk or any other fat containing liquid).

The term " phytosterols" is to be construed to include, but not to be restricted to, beta-sitosterol, stigmasterol, campesterol, brassicasterol together with their associated glucosides.

The term "antioxidant complex" is to be construed to include, but not to be restricted to, a broad range of proanthocyanidins, flavonoids and polyphenols.

The term"essential fatty acid complex" is to be construed to include, but not restricted to, hydrolysates of fatty acids derived from fish and synergistically incorporated on plant protein carriers, together with amino acids, essential fatty acids, peptides, proline rich poly peptides, and various digestive enzymes. REFERENCES

International Journal of Immuno Pharmacology 1996 Vol 18 Bouic et al.

Beta-sitosterol and beta-sitosterol glucoside, stimulate human peripheral blood lymphocyte proliferation; implications for their use as an immunomodulatory vitamin combination.

International Journal Molecular Medicine 2000 Vol 5 Awad et al.

Inhibition of growth, and stimulation of apoptosis, by beta-sitosterol treatment of human breast cancer cells.

Anti Cancer Research 1998 Vol 18 (la) Awad, Holtz et al.

Beta-sitosterol inhibits growth of HT-29 human colon cancer cells.

Nutrition and Cancer 1998 Vol 32 (1) von Holtz, Fink et al.

Beta-sitosterol induces apoptosis in LNCaP human prostate cancer cells.

AIDS Bulletin 1997 Vol 6 Bouic.

Immodulation in HIV/AIDS: The Tygerberg/Stellenbosch University Experience.

South African Journal of Science, 1997 Vol 93 Pegel.

The Importance of Sitosterol and Sitosterolin in human and animal nutrition.

British Journal of Urology 1997 Vol 80 Klippel et al.

A multi centric, placebo controlled, double blind clinical trial of beta- sitosterol for the treatment of benign prostatic hyperplasia.

The Lancet 1995 Vol 345 Berges et al.

Randomized placebo controlled double blind clinical trial of beta- sitosterol in patients with benign prostatic hyperplasia.

The Arthritis Trust of America Summer 98 Bouic.

Sterols/Sterolins the natural, none toxic immuno-modulators and their role in the control of rheumatoid arthritis.

Nutrition Reviews 1992 Vol 50 NO. 7 Block.

The data support a role for antioxidants in reducing cancer risks. Methods in Enzymology 1990 Vol 186 Bors, Heller et al.

Flavanoids as anti-oxidants: determination of radical scavenging efficiencies.

The Lancet 1996 Vol 344 Cerruti. Oxi-radicals and cancer.

Biochemical Pharmacology 1990 Vol 39 No. 11 DeWhalley, Rankin et al.

Flavanoids inhibit the oxidative modification of low density lipoproteins by macrophages.

The Lancet 1994 Vol 344 Grishan.

Oxidants and free radicals in inflammatory bowel disease.

Phytochemistry 1987 Vol 26 No. 9 Husain, Cillard et al. Hydroxyl radical scavenging activity of flavanoids.

The Lancet 1994 Vol 344, Jenner.

Oxidative damage in neuerodagenerative disease.

Free Radicals in Diagnostic Medicine, D. Armstrong, Plenum Press New York. Free radical scavenging and antioxidant activity of plant flavanoids.

New Zealand Journal of Science 1973 Vol 16 Markam and Porter. Extractives of pinus radiata bark- phenolic components.

New Zealand Journal of Science 1974 Vol 17 Porter.

Extractives of pinus radiata bark-procyanidin constituents.

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The relative antioxidant activities of plant derived polyphenolic flavanoids.

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Free Radical Biology in Medicine 1990 Vol 9 Yuting, Rongliang et al. Flavanoids as super oxide scavengers and antioxidants.

Claims

CLAIMSThe embodiments of the invention in which an exclusive property or privilege is claimed are defined as follows:

1. A composition for the regulation of the human immune system and the prevention and treatment of diseases thereof which contains phytosterols, an anti-oxidant complex, and a fatty acid complex that includes, but is not restricted to, hydrolysates of fatty acids derived from fish and synergistically incorporated on plant protein carriers, amino acids, peptides, proline rich polypeptides and digestive enzymes.

2. A composition as defined in claim 1 containing phytosterols and their associated glucosides, Enzogenol™ and Biolysate™.

3. A composition as defined in claims 1 and 2 in which the proportion of each constituent may vary from 1% to 95% of the total composition.

4. A composition as defined in claims 1,2 and 3 in which the composition of the Enzogenol™ may be subsequently modified.

5. A composition as defined in claims 1,2,3 and 4 in which the composition of the Biolysate™ may be subsequently modified.

6. A composition as defined in claims 1,2,3,4 and 5 in which the proportion of the beta-sitosterol is between 5% and 95% of the total content of phytosterols.

7. A composition as defined in 1,2,3,4,5, and 6 in which another or other antioxidants are substituted for the Enzogenol™.

8. A composition as defined in claims 1,2,3,4,5,6, and 7 in which another or other fatty acid complexes, amino acids, peptides, proline rich polypeptides or digestive enzymes are substituted for the Biolysate™.