WO2002062329A1

WO2002062329A1 - Therapeutical and nutritional compositions containing pyruvic acid amd glutamine, having antioxidizing activity and capable of controlling overweight

Info

Publication number: WO2002062329A1
Application number: PCT/EP2002/000640
Authority: WO
Inventors: Elvira Pistolesi
Original assignee: Hunza Di Pistolesi Elvira E C. Sas
Priority date: 2001-02-02
Filing date: 2002-01-23
Publication date: 2002-08-15
Also published as: ITMI20010204A1

Abstract

Therapeutical and/or nutritional compositions, containing: A) pyruvic acid as such or salified with: I) minerals; II) basic amino acids; III) proteins or peptides containing basic amino acids; IV) nitrogen bases; and B) glutamine (and/or proteins and/or peptides containing it as such or salified).

Description

THERAPEUTICAL AND NUTRITIONAL COMPOSITIONS CONTAINING PYRUVIC ACID AND GLUTAMINE, HAVING ANTIOXIDIZING ACTIVITY AND CAPABLE OF CONTROLLING OVERWEIGHT

The present invention relates to therapeutical and nutritional compositions having antioxidizing activity and capable of controlling overweight, containing a mixture of two components.

More particularly, the present invention relates to compositions 5 consisting of:

1) pyruvic acid or salts thereof, and

2) glutamine (and/or proteins, and/or peptides containing them).

Said compositions are an effective, well-tolerated nutritional 10 supplement for increasing with surprising synergism the antioxidants defenses of the body, and for keeping under control overweight as well as any unbalances in the body fat mass (in excess) to lean mass ratio deriving from high caloric input of foods. All these beneficial results are always by far higher than the sum of the results obtainable by the separated 15 administration of the same active nutrients.

The present invention therefore relates to pharmaceutical and/or dietetic compositions as well as to functional foodstuffs capable of preventing both excessive increase in the peroxidative processes and overweight, as it happens in aging and in many related pathologies (such as

20 atherosclerosis, diabetes, hypertension, lipid dysmetabolies, tumors, etc.).

The compositions of the invention comprise two active principles represented by: A) pyruvic acid or salts thereof with:

I) minerals such as Ca, Mg, K, Na, Zn, Cr, Va, and the like; II) basic and/or neutral amino acids capable of inducing an anorectic effect, such as arginine, histidine, asparagine, trypthophan, phenylalanine, tyrosine, leucine, and the like;

III) proteins or peptides containing said basic and/or neutral amino acids;

IV) nitrogen bases such as choline and derivatives, ethanolamine and derivatives, mono and diinethylethanolamine and derivatives, poly amines, and the like; and B) glutamine (and/or proteins and/or peptides containing it as such or salified with lactic acid, pyruvic acid or other organic acids such as: fumaric, malic, oxalacetic, aspartic, citric, isocitric, acetic, propionic, butyric acids and the like.

In addition to the two above cited active principles, the compositions of the present invention can futher contain other compounds conventionally used, such as:

I) fibers and polysaccharides (such as inulins, pectins, celluloses, chitosans, maltodextrins, starches and flours, and the like);

II) vitamins and mineral salts, single or in mixture thereof; III) vegetable extracts both crude and as fractions enriched in their content in bioflavones, terpenes, tannins, polycosanols, and the like. Examples of said vegetable extracts are: vegetable extracts having diuretic, fat metabolism stimulating and intestinal improving activities (for example extracts from artichoke, milk thistle

(Silybum marianum), Curcuma longa, Pierroriza kurroa, etc.) and/or vegetable extracts having lymphokinetic and detoxifying activity (such as melilot (Melilotus officinalis), dandelion (Taraxacum officinale), citrus essential oils, and the like); and/or vegetable extracts capable of activating fat lipolysis (such as coffee, tea, green tea, oolong tea, wax extracts of citrus, rice, sugar cane, and the like); and/or - vegetable extracts capable of improving blood rheology, microcircle flow rate and NO release (such as Ginkgo biloba, Ginseng, and the like).

Pyruvic acid is present in amounts ranging from 0.1 to 2000 mg, preferably from 4 to 400 mg, per kg body weight of the treated subject.

Glutamine (and/or proteins and/or peptides containing it) is present in amounts ranging from 0.1 to 500 mg, preferably from 10 to 100 mg, per kg body weight of the treated subject.

Some examples of compositions of the invention are reported in the following.

Example 1 : a) calcium pyruvate 180 g b) glutamine 70 g

Example 2: a) calcium pyruvate 250 g b) wheat flour oligopeptides containing 29% glutamine 50 g

Example 3 : a) pyruvic acid 50 g b) wheat flour oligopeptides containing 29% glutamine 200 g Example 4: a) calcium pyruvate 90 g b) glutamine 133 g c) inulin 777 g Example 5: a) pyruvic acid 90 g b) wheat flour oligopeptides containing

29% glutamine 360 g c) oat fiber 500 g

Example 6: a) pyruvic acid or salts thereof 90 g b) wheat flour oligopeptides containing

29% glutamine 360 g c) Betaine-chitosan 400 g

Example 7: water-dispersible powder consisting of: a) pyruvic acid 150 g b) L-glutamine and/or peptides containing it

(in glutamine) 360 g c) an amino acids mixture consisting of:

L-trypthophan (30 g), L-phenylalanine (150 g) and L-arginine (150 g) d) a vegetable extracts mixture consisting of: green tea (300 g), artichoke (50 g), melilot (15 g), caffeine extracted from tea and or coffee (30 g), Ginkgo biloba (20 g), polycosanols extracted from sugar cane (3 g), lemon essential oils (5 g) and black pepper extracts containing 1-piperoylpiperidine (1 g) e) a mixture of vitamins and mineral salts consisting of: vitamin E (10 g), lipoic acid (8.5 g), vitamin F,

(linoleic acid and linolenic acid and/ or highly polyunsaturated derivatives thereof, 320 g), vitamin B6 (1 g), folates (200 mg) and vitamin B12 (2 mg). The various compositions described in the above examples can be used for the preparation of both functional foodstuffs (bread, pasta, crackers, biscuits or other bakery products; dressings, margarines, mayonnaise, sauces, beverages, fruit juices, soft drinks and the like; creams, chocolate, milk, cheese, yogurt, etc.) and galenic preparations consisting of vials, hard- or soft- gelatin capsules, tablets, sachets, effervescent tablets, chewing gums, syrups, etc.

Pharmacological and/or dietetic experimentation

The pharmacological and/or dietetic characteristics of the compositions of the present invention were assessed by means of two series of tests on rat and humans, respectively.

In a first series of tests on rats, the animals were given a hypercaloric, hypertriglyceridemizing and hypercholesterolemizing diet. After twenty days of treatment, the following parameters were evaluated: 1) lipoperoxides levels in plasma, liver, brain and heart;

2) body weight changes;

3) cholesterol plasma levels;

4) triglycerids plasma levels.

50 Male rats, each weighing 150-200 g, were used. The animals were subdivided into 5 groups of 10 animals each:

1^st group: control (C); 10 animals (control at time 0) received no treatment, 10 animals received for 20 days standard hypercaloric, hypertriglyceridemizing and hypercholesterolemizing diet consisting of:

20% casein; 3.5% mixture of oligoelements and mineral salts; 0.1% mixture of vitamins; 0.2%> choline ditartrate; 2% cellulose; 0.5% cholesterol; 0.25% sodium cholate; 58.44% saccharose; 10.0%> lard and 4.9% olive oil.

2^nd group: animals treated with glutamine (G); animals received for 20 days the same diet as the controls except that 3.0 g of glutamine replaced in part a similar amount of casein (casein used: 17%).

3^rd group: animals treated with pyruvic acid; animals received for 20 days the same diet as the controls except that 4.5 g of pyruvic acid replaced in part a similar amount of saccharose (saccharose used: 53.94%).

4^th group: animals treated with glutamine + pyruvic acid; animals received for 20 days the same diet as the controls except that 3.0 g of glutamine and 4.5 g of pyruvic acid replaced respectively similar amounts of casein (casein used: 17%) and saccharose (saccharose used: 53.94%).

The obtained results prove that the administration of the composition of the invention is capable of promoting, in rats subjected for 20 days to hypercaloric diet enriched in animal saturated fats and cholesterol, a surprising, synergistic effect in: 1) improving antioxidants defenses of plasma, liver, brain and heart;

2) reducing body overweight;

3) limiting excessive increase in plasma cholesterol and triglycerid levels, thereby promoting the accumulation of the lean body mass to the detriment of the fat body mass. Said beneficial, therapeutical effects obtainable by the administration of the compositions of the invention are always significantly higher than the sum of the beneficial effects obtainable by administering separately the single components of the various compositions. In a second series of tests in humans, the tested composition contained pyruvate (3.75 g/die) and glutamine (5 g/die) added with amino acids, vitamins, minerals and vegetable extracts in the same quali-quantitative composition as that reported in example 7. The dietetic supplement, administered for 30 days, gave surprising beneficial effects in: a) significantly reducing overweight; b) significantly improving the lean mass/fat mass ratio; c) significantly improving membrane fluidity of erythrocytes and lymphocytes; d) improving the antioxidant defenses of plasma lipoproteins. Said therapeutical improvements obtainable by the administration of the composition as reported in example 7 were always significantly higher than those obtained when administering separately the different components of the above mentioned compositions, i.e.: a) pyruvate; b) glutamine; c) the fraction containing all of the other components of the mixture without pyruvate and glutamine.

Claims

1. Therapeutical and/or nutritional compositions, containing:

A) pyruvic acid as such or salified with minerals, basic amino acids, proteins or peptides containing basic amino acids or nitrogen bases; and

B) glutamine (and/or proteins and/or peptides containing it as such or salified).

2. Compositions as claimed in claim 1, wherein minerals are selected from: Ca, Mg, K, Na, Zn, Cr, Va.

3. Compositions as claimed in claim 1 , wherein glutamine and/or proteins and/or peptides containing it are salified with lactic acid or other organic acids selected from the group consisting of pyruvic, furnaric, malic, oxalacetic, aspartic, citric, isocitric, acetic, propionic and butyric acids.

4. Compositions as claimed in claim 1, wherein pyruvic acid is present, as such or in salified form, in amounts ranging from 0.1 to 2000 mg, preferably from 4 to 400 mg, per kg body weight of the treated subject.

5. Compositions as claimed in claim 1, wherein glutamine is present in amounts ranging from 0.1 to 500 mg, preferably from 10 to 100 mg, per kg body weight of the treated subject.

6. Compositions as claimed in any one of the above claims, further containing fibers, polysaccharides, vitamins, mineral salts and vegetable extracts.

7. Compositions as claimed in claim 6, wherein fibers and polysaccharides are selected from the group consisting of inulins, pectins, celluloses, chitosans, maltodextrins, starches and flours.

8. Compositions as claimed in claim 6, wherein the vegetable extracts are selected from extracts of artichoke, milk thistle (Silybun marianum), Curcuma longa, Pierroriza kurroa, melilot (Melilotus officinalis), dandelion (Taraxacum officinale), tea, green tea, oolong tea, coffee, Ginkgo biloba, Ginseng, rice, sugar cane, citrus fruits.

9. Foodstuffs containing the compositions of claims 1 to 8.