FR2786096A1 - Compositions for the prevention and treatment of cellulitis contain plant extracts comprising a sulfur heteroside - Google Patents

Abstract

Compositions containing an extract of a plant containing a sulfur heteroside in a cosmetic or pharmaceutical base, are new.

Description

The present invention relates to cosmetic compositions or

  pharmaceuticals for the prevention and treatment of aesthetic and / or pathophysiological disorders, better known in common parlance under the name of cellulite and using, as active ingredient, products of natural origin. The clinical entity called cellulite is primarily seen as a consequence of polyendocrine changes. The pathogenesis seems to be linked to a hyperpolymerization of the mucopolysaccharides and to fluid retention, leading to hyperviscosity of the fundamental substance then to a microvascular deficit and to alterations in capillary permeability. This state leads to a decrease in exchanges between cells, fibers and vessels, and gradually leads to a fibrinoid modification of the connective fibers, to capillary compression with circulatory slowing, and finally to an overload of adipocytes with triglycerides. This situation leads to the formation of micro- and then subcutaneous macronodules which give the skin

  a padded appearance in "orange peel".

  Many products are available on the market, but these products have no proven activity. One explanation for the failures encountered could be that the treatments available are concerned with and are limited, in most cases, to the physiology of the adipocyte, and then possibly to

  improving blood circulation.

  The present invention is based on an original approach according to which it is essential to take into account and treat the rigidity of the conjunctival framework. It is then possible to restore the functionality of the microcirculation, then downstream of the cascade of events, to contribute to

activation of lipolysis.

  A solution is proposed by the use of plant extracts containing sulfur heterosides (such as glucosinolates) allowing an inhibition of lysyloxydase and thus of the formation of bridges between collagen fibrils, bridges which are at the origin of the stiffening of the environment and imprisonment

  enlarged fat cells.

  Collagen fibers are normally stabilized by the formation of covalent bonds on lysine and OH-lysine residues. Oxidative deamination of lysyl and OH-lysyl residues by lysyl oxidase precedes the formation of these bridges. The inhibition of lysyloxidase, by reducing the formation of covalent bonds, makes it possible to reduce the rigidity of the fibers

  collagen and helps facilitate tissue exchange.

  The present invention therefore more particularly relates to a cosmetic or pharmaceutical composition for the prevention and topical treatment of cellulite, comprising, as active principle, an effective amount of a plant extract containing sulfur heterosides, in a base

  cosmetic or pharmaceutical for topical application.

  The present invention also relates to a method for the prevention and topical treatment of cellulite, which consists in applying to the skin an effective amount of a plant extract containing heterosides

sulfur.

  The plant extract used in the present invention is chosen in particular from plants containing glucosinolates such as: * in the Tropaeolaceae family: Tropaeolum majus (Capucine) * in the Pentadiplandraceae family: Pentadiplandra brazzeana * in the Cruciferous family: Brassica barrelieri, Capsella bursa-pastoris, Diplotaxis catholica, Erysimum allionii, Raphanus sativus, Sinapis arvensis; a in the Moringaceae family: Moringa oleifera; * in the Phytolaccaceae family: Phytolacca americana;

  * in the Resedaceae family: Reseda phyteum.

  The compositions according to the invention may advantageously contain an agent promoting microcirculation. As agents of this type, mention may be made of

  extracts of Gingko biloba, ruscus, sweet clover, red vine, viburnum.

  The compositions according to the invention may also advantageously contain an agent for activating lipolysis. As agents of this type, mention may be made of extracts of ground ivy (Glechoma), of Angelica root, of Paullinia extract, of Mate or also of xanthic bases such as

  caffeine, theobromine and theophylline.

  The cosmetic or pharmaceutical compositions according to the invention may also optionally contain all the known substances having beneficial properties on the integuments and particularly for their cosmetic or pharmaceutical activity in the care of skin of all kinds, in particular those manifesting a tendency to overloads. greasy and cellulite formation. They may contain antiseptics, comedolytics, antiseborrheics, perfumes,

1o preservatives and dyes.

  The cosmetic or pharmaceutical compositions according to the invention can be in any topical form used in pharmacy or in cosmetology: cream or gel in jars or in tubes, milk, lotion in glass or plastic bottle, in ampoules, microinjections or in dosing bottles,

  impregnated compresses, plasters, patch tests, patches.

  For each particular form, appropriate excipients are used.

  These excipients must have all the qualities usually required. By way of examples, there may be mentioned: propylene glycol, glycerin, cetyl alcohol, polyols, phospholipids put in liposomes or not, vegetable, animal, mineral oils, wetting agents, thickeners,

  commonly used stabilizers and emulsifiers.

  The different cosmetic or medicinal forms mentioned above

  above are obtained according to the methods used in this field.

  Process for obtaining and content of cilucosinates Among the plants mentioned, it is possible to retain very particularly the aerial parts of Nasturtium to obtain an extract which can be used in the formulation of the products. Any process involving glucosinolates can be used, for example: the aerial parts of Capucine are ground and then extracted with ten times their weight of solvent (such as 60% ethanol). The extraction is carried out under reflux, with stirring for at least one hour. After cooling, the crushed nasturtium is separated from the ethanolic solution by wringing. The latter is concentrated under reduced pressure at 60 C until a

  solution containing, at most, 1000 ppm of ethanol.

  To obtain such a standard, water can be separated during concentration, which will then be evaporated. Evaporation is carried out until twice the weight of nasturtium extract is obtained. Finally we add to this

  70% alkyl ether sulfate triethanolamine concentrate.

  The concentration of glucosinolates can be between 0.1 and 5% by weight in the extract and the extract can be incorporated into the compositions in the right manner

io from 0.5 to 10% by weight.

  Activity on yIsyloxidase The activity of plant extracts and in particular of nasturtium extract on the inhibition of lysyloxidase was determined according to the method described by Guanmei Liu, Kaliappanadar Nellaiappan, and Herbert M. Kagan "Irreversible Inhibition of Lysyl Oxidase by Homocysteine Thiolactone and its Selenium and Oxygen Analogues ", The Journal of Biological Chemistry, vol. 272, n 51, issue of December 19, pp. 32370-32377, 1997: Five different extracts were examined to determine their effect on the activity of lysyloxidase. Each product in solution was tested at two dilutions in duplicate, in tests for the activity of a constant amount of purified bovine aortic lysyloxidase, against a biologically prepared tropoelastin substrate. The substrate was labeled with 1- [4,5-3H] lysine in a

system expressed by E. coli.

  The [3H] -tropoelastine was purified and aliquots of 125,000 cpm were added to each tube as a substrate for the lysyloxidase in the presence or in the absence of dilutions of the various extracts. The oxidation of peptidyl lysine by lysyloxidase induces the loss of carbon 5 tritium which is then

  isolated from the medium and counted in [3H] H2O, as an index of the enzymatic activity.

  All data have been corrected for non-enzymatic background noise in the release of tritium (negligible) and for non-specific effects of the extracts

  on the substrate in the absence of exogenous lysyloxidase (negligible).

  The results obtained are as follows: Sample activity Enzymatic dilution: 3H20% cpm / 2h release activity. Bovine lysyloxidase control 1047 + 69 100 Extract 1: 1:50 436 + 95 41.6 Bourse-à-Pasteur 1: 5 42 + 42 4 Extract 2: 1:50 510 + 9 48.7 Nasturtium 1: 5 16 +4 1.5 Extract 3: 1:50 0 + 0 0 Nasturtium 1: 5 0 + 17 0 Extract 4: 1:50 812 + 57 77.6 Radish 1: 5 147 + 50 14 Thus, extract 3 allows completely inhibit lysyloxidase activity.

EXAMPLE

  An example of a composition according to the invention will be given below: Gel-type composition - guarana extract 6.25 g - nasturtium extract 3.00 g - viburnum extract 1.00 g - ethanol 27% by volume - perfume blackberry

- gelled excipient q.s.p. 100g.

Claims (7)

  1. Cosmetic or pharmaceutical composition for the prevention and topical treatment of cellulite, comprising, as active principle, an effective amount of a plant extract containing sulfur heterosides, in a cosmetic or pharmaceutical base for topical application. 2. Composition according to claim 1, characterized in that the extract is   a plant extract chosen from plants containing glucosinolates.   3. Composition according to claim 1 or claim 2, characterized in that the extract comes from a plant chosen from Tropaeolum majus   (Nasturtium), Pentadiplandra brazzeana, Brassica barrelieri, Capsella bursa-   pastoris, Diplotaxis catholica, Erysimum allionii, Raphanus sativus, Sinapis   arvensis, Moringa oleifera, Phytolacca americana, Reseda phyteum.   4. Composition according to any one of claims 1 to 3,   further comprising an agent promoting microcirculation.   5. Composition according to claim 4, in which the agent promoting local microcirculation is an extract of Ginkgo biloba, ruscus, sweet clover, vine red or viburnum.   6. Composition according to any one of claims 1 to 5,   comprising an agent for activating lipolysis.   7. Composition according to claim 6, comprising, as an agent for activating lipolysis, an extract of ground ivy, of Angelica root,   of Paullinia, of Maté, or a xantical base.