WO1999030724A1 - Polyphenolic composition, useful as food supplement, functional food or cosmetic composition - Google Patents

Abstract

The invention concerns a polyphenolic composition, characterised in that it contains simultaneously at least two of the following constituents: (i) grape juice concentrate titrated with 1 to 20 wt. % of polyphenols; (ii) wine extract titrated with 1 to 20 wt. % of polyphenols; (iii) water soluble olive extract titrated with 0.5 to 40 % of polyphenols.

Description

 Polyphenolic composition, useful as a dietary supplement, nutraceutical or cosmetic composition

The present invention relates to a polyphenolic composition capable of finding its application as a food supplement, as a nutraceutical, or even as a cosmetic composition which can be administered orally or topically.

It is clear today that a healthy diet is a source of health. The media regularly report on discoveries in the field of nutraceuticals, a food promoting good health, supported by various epidemiological surveys on the Cretan, Mediterranean and southern European diets.

It is frequently observed that populations who consume a particular product are less affected by cardiovascular diseases, the leading cause of death in industrialized countries.

In 1978, the results of a study by the World Health Organization (WHO) on the causes of death in 23 European countries were analyzed by an author (Genevois), who showed that myocardial infarction is a of the most common diseases affecting men between 55 and 64 years of age.

However, it appears that mortality rates vary widely between countries. Genevois divides the countries into three groups:

1) wine-growing countries,

2) the countries of Central Europe, 3) the countries of Northern Europe.

The first being that of the least affected countries, and the third that of the countries with very high rates of infarction. In 1979, Saint-Léger, Cochrane and Moore publish their results of a survey carried out in 18 developed countries on the factors associated with cardiac mortality. (The Lancet - May 12, 1979, pages 1010-1020).

Mortality rates are confronted with various variables such as population density, medical density, individual gross income, smoking, eating behavior, etc.

The only indisputable correlation which emerges from this survey concerns, in a negative way the mortality rate by myocardial infarction and the usual consumption of micronutrients, between the flavonoids brought by vegetables, cereals, but also unrefined oils.

France and Italy, at the top of the list of consumers of wine, rich in flavonoids, register mortalities three to five times lower than those of Scotland and Ireland.

Saint-Léger, Cochrane and Moore deduce that the protective power of wine comes from constituents other than alcohol.

In 1982, supported by scientific evidence, Masquelier developed a new theory according to which procyanidins exert their effects on two levels, namely in the circulating blood and in the arterial wall.

- In the blood, wine accelerates the purification of cholesterol. This is the cholesterol-lowering power, described in 1961. The polyphenols in wine also act as cofactors and factor for saving vitamin C. In the arterial wall, these same procyanidins exert a double tissue action. On the one hand, they stabilize the collagen fibers which serve to support the various tunics of the vessel, this reinforcement of collagen is explained by the establishment of bridges between the polypeptide chains. On the other hand, an inhibition of the HD enzyme allows them to avoid an exaggerated production of histamine which would have the consequence of increasing the permeability of the arterial wall. Then the intermediate results of the Monica study fully confirm the low prevalence of cardiovascular risk in populations on a Mediterranean diet.

On the balance sheet, it emerges from these studies, that several nutrients have a role in the delay of emergence of pathology in the south of Europe:

vegetables and fruits through fibers and flavonoids, the unsaturated lipids of certain oils, especially olive oils, - wine.

The consumption of foods providing these nutrients is in sharp decline which justifies a supplementation.

The subject of the present invention is a polyphenolic composition, characterized in that it simultaneously contains at least two of the following constituents:

i) grape juice concentrate titrated from 1 to 20% by weight of polyphenols; ii) wine extract titrated from 1 to 20% by weight of polyphenols; iii) water-soluble olive extract titrated from 0.1 to 40% in polyphenols.

According to another characteristic of the invention, the composition is characterized in that the grape juice concentrate is rich in flavonoids and anthocyanins, and preferably contains from 1 to 20% by weight of flavonoids.

According to another characteristic, the composition according to the invention is characterized in that the wine extract is rich in flavonoids, anthocyanins and procyanidinols, and preferably contains from 1 to 20% by weight of flavonoids.

According to another characteristic of the invention, the composition according to the invention is characterized in that the water-soluble olive extract is rich in oleuropein, tyrosol and caffeic acid, and preferably contains from 0.1 to 40% in weight of tyrosol, oleuropein and caffeic acid. According to an advantageous variant of the present invention, the composition simultaneously contains the three constituents i), ii) and iii) and, in particular, corresponds to the following composition:

i) 3 to 20% by weight of grape juice concentrate, ii) 0.5 to 40% by weight of wine extract, iii) 0.01 to 5% by weight of water-soluble olive extract.

As a variant, the composition according to the invention may also contain at least one additional constituent chosen from vitamins, in particular, natural vitamin E, trace elements, hydrolysates of soybean, sunflower and olive oil, lycopenes, flavoring minerals, colors, antioxidants and food additives.

The compositions according to the invention can be used in general as a food supplement, they can in particular enter into the culinary preparation composition by playing the role of flavoring agents, colorings, antioxidants, or any other function of food additives.

The method of manufacturing traditional virgin olive oil will be recalled below.

After washing, the ripe fruits are subjected to moderate pressure at a temperature below 80 ° C. The emulsion is collected, then the mixture is separated by centrifugation in two phases, aqueous and lipid where persistent emulsion phenomena persist.

The microcomponents of the olive are distributed between these two phases according to their solubility (partition coefficient).

Unrefined virgin oil is, in particular, relatively rich in micronutrients such as phytosterols, fat-soluble vitamins (E, etc.), polyphenols (caffeic acid, tyrosol, syringic, etc.) and their precursor, namely oleuropein. .

These compounds also exist in similar ratios in the aqueous phase which can therefore be used for the preparation of the compounds according to the invention as active extracts. The analytical study of phenolic compounds highlights:

The similarity of these polyphenolic and iridoid compounds both in the aqueous phase and in the lipid phase.

the identity of the compounds present in the aqueous phase and in the lipid phase, for example caffeic acid, tyrosol, oleuropόine,

that these compounds participate in whole or in part in the effect observed at the cardiovascular level in populations consuming unrefined olive oil,

the use of an active ingredient from the aqueous phase in nutraceutical-type preparations intended to supplement essential trace elements in the Mediterranean diet, in healthy individuals, receiving only industrial standardized food.

We will quickly recall how the grape juice concentrate and wine extract can be obtained.

These extracts are generally obtained by evaporation under reduced pressure, under an inert atmosphere, of the corresponding juices and liquids. By way of example, the "flash trigger" methods can be used, but other methods are also applicable.

The dehydration of these juices and liquids can be total (dry extract containing less than 8.1% of water incorporating an agent such as maltodextrin, starch, silica) or partial (fluid extract containing less than 0.5% w / w ethanol).

The grape juice concentrate thus obtained is rich in flavonoids and anthocyanins: 1 to 20% expressed in flavonoids.

The wine extract thus obtained is rich in flavonoids, anthocyanins, procyanidinols: 1 to 20% expressed in flavonoids. Assessment of the activity of the components and of the association:

• Atheromatous plaque is formed by the deposition of lipid substances on the vascular endothelium, then by oxidation of these substances by cells of the white line (Polynuclear neutrophils);

• The prophylactic and curative activity of a substance or a combination of substances can be evaluated in vitro by simple tests mimicking the pathological phenomenon: the decrease in the adhesion of white lineage cells to endothelial cells corresponding to a response favorable.

In particular,

• Decrease in the adhesion of PMN to the surface of endothelial cells in culture,

• Inhibition of gene expression of adhesion factors (VCAM, ICAM) by endothelial cells.

Experimental part :

Human endothelial cells from umbilical cords are cultured on the well plates under appropriate conditions. The culture is carried out to confluence. The compounds to be studied or their association are introduced into the culture 30 to 60 min before the triggering of a pharmacological reaction causing the adhesion of lymphocytes (interieukin 1: iL1; xanthine -xanthine oxidase: XXO).

Results

Absence of cytotoxic activity: None of the components evaluated or their combination (50/50 w / w) has cytotoxic activity at 100 μg / ml

Grape juice concentrate 023323n Wine extract 023324r

Water-soluble olive extract 023328μ Inhibition of the adhesion of lymphocytes to endothelial cells triggered by iL1: the adhesion measured by flow cytometry is reduced as follows by the associations:

The strong potentiation found, at these concentrations, by the concentrated association of grape juice / water-soluble olive extract, is manifest at much lower concentrations of water-soluble olive extracts. For example :

A higher inhibition, for the "grape-olive" associations is demonstrated when the adhesion reaction is triggered by stimulation of the radical type such as xanthine-xanthine oxidase.

Expression of adhesion molecules: the expression of adhesion molecules is triggered by contact of the cells with iL1 in 4 hours.

The grape juice concentrate and the wine extract alone has moderate activity.

The association of the three constituents in reports ranging from 1.1.1. at 10.1 1/10 (grape juice, wine, olives) all have activities superior to a simple addition of effect. In conclusion, we observe that:

> The grape juice concentrate, wine extract and water-soluble olive extracts are non-cytotoxic,> They have a moderate activity on the adhesion of lymphocytes to the endothelium,

> The potentiating activity of the ternary association is greater than that of the compounds taken individually when the adhesion reaction is triggered by IL1 and especially by the xanthine-xanthine-oxidase radical reactions.

> The activity of the ternary association is evident in the expression of the adhesion molecules, while each of the components is not very active.

Active ingredient n ° 1: Water-soluble olive extract

Titrated in polyphenols: 0.5 to 40%

This product is rich in polyphenols, oleuropein, tyrosol and caffeic acid

Active ingredient n ° 2: Grape juice concentrate

Titrated from 1 to 20% of polyphenols expressed in flavonoids This product is rich in flavonoids and anthocyanins

Active ingredient n ° 3: Wine concentrate

Titrated from 1 to 20% of polyphenols expressed as flavonoids

This product is rich in flavonoids, anthocyanins and oligo-procyanidinols.

Formulations:

Different dosage forms have been developed, solid and liquid such as powders, capsules, tablets, syrups, solutions for incorporation either in the manufacture or in the consumption of food preparations.

The formulations below illustrate the invention without limiting its scope: Example 1:

In weight

Grape juice concentrate 5 to 95% Wine concentrate 5 to 25%

Example 2:

Water-soluble olive extract 0.01 to 25% Grape juice concentrate 5 to 95% Wine concentrate 5 to 25%

Example 3:

Grape juice concentrate 5 to 95%

Wine concentrate: 5 to 25%

Stabilized by vitamins E, C and licopene

Example 4:

Water-soluble olive extract 0.01 to 25% Grape juice concentrate 5 to 95% Wine concentrate 5 to 25%

Stabilized with vitamins E and C and licopene

Example 5:

The following formulas in the form of a pure or diluted drinking solution have been found to be particularly interesting:

Example 6:

Soybean oil hydrolyzate combined with Example 5.

Example 7:

Sunflower oil hydrolyzate combined with Example 5.

Example 8:

Olive oil hydrolyzate combined with Example 5.

Example 9:

Soybean oil, sunflower oil hydrolyzate combined with Example 5.

Example 10:

Soybean and olive oil hydrolyzate combined with Example 5. Example 11:

Olive oil and sunflower hydrolyzate combined with Example 5.

Example 12:

Soybean, olive and sunflower oil hydrolyzate combined with Example 5.

Presentations:

The compositions according to the invention can be formulated for the following presentations:

Food ingredients intended for use in the manufacture or flavoring of dishes: powders, paraffin-based lipid solutions,

Active ingredients available in assimilable form: drink, capsules, bars, for a beneficial nutraceutical effect.

• * Cosmetic active ingredients for presentations intended to be ingested or applied to the skin, for a beneficial cutaneous effect.

Claims

1. Polyphenolic composition, useful as a dietary supplement and / or nutraceutical, characterized in that it simultaneously contains at least two of the following constituents: i) grape juice concentrate titrated from 1 to 20% by weight of polyphenols; ii) wine extract titrated from 1 to 20% by weight of polyphenols; iii) water-soluble olive extract titrated from 0.5 to 40% in polyphenols.

2. Composition according to claim 1, characterized in that the grape juice concentrate is rich in flavonoids and anthocyanins.

3. Composition according to claim 2, characterized in that the grape juice concentrate has a content of 1 to 20% by weight of flavonoids.

4. Composition according to one of claims 1 to 3, characterized in that the wine extract is rich in flavonoids, anthocyanins and procyanidinols.

5. Composition according to claim 4, characterized in that the wine extract has a content of 1 to 20% by weight of flavonoids.

6. Composition according to one of claims 1 to 5, characterized in that the water-soluble olive extract is rich in oleuropein, tyrosol and caffeic acid.

7. Composition according to one of claims 1 to 5, characterized in that the water-soluble olive extract has a content of 0.1 to 40% by weight of tyrosol, oleuropein and caffeic acid.

8. Composition according to one of claims 1 to 7, characterized in that the three constituents i), ii) and iii) are present simultaneously.

9. Composition according to claim 8, characterized in that it contains:

i) 3 to 20% by weight of grape juice concentrate, ii) 0.5 to 40% by weight of wine extract, iii) 0.01 to 5% by weight of water-soluble olive extract.

10. Composition according to one of the preceding claims, characterized in that it contains at least one additional constituent chosen from vitamins, in particular natural vitamin E, trace elements, hydrolysates of soybean oil, of sunflower and olive, lycopenes, flavoring minerals, colors, antioxidants, and food additives.