Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Conjugate or complex
Reexamination Certificate
1998-06-23
2002-07-02
Travers, Russell (Department: 1617)
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Conjugate or complex
Reexamination Certificate
active
06413519
ABSTRACT:
BACKGROUND OF THE INVENTION
The invention relates to uses of an extract of the plant
Terminalia catappa
in the cosmetic and pharmaceutical fields, especially the dermatological field.
It relates more precisely to uses of an extract of this plant as a cosmetic agent.
The plant
Terminalia catappa
belongs to the Combretaceae family, which is found particularly in New Caledonia.
The systematic experiments carried out by the inventors have made it possible to demonstrate a number of surprising enzymatic actions of the extracts of this plant, particularly inhibitory actions on several enzymes, especially phospholipase A
2
, 5′-lipoxygenase, tyrosinase and 3 ′,5′-cAMP phosphodiesterase, which has made it possible to consider its use in cosmetic and pharmaceutical products, especially dermatological products.
Phospholipase A
2
(PLA
2
) is an enzyme produced by membrane cells. It predominates in cells associated with inflammation phenomena, such as mastocytes. Through its action it releases the arachidonic acid bound to the membrane phospholipids. This acid then metabolizes to different lipidic mediators of inflammation and allergy, such as leukotrienes and prostaglandins.
Like PLA
2
, 5′-lipoxygenase, hereafter called “lipoxygenase” , is a membrane enzyme. It is involved in the “inflammation cascade” downstream of the release of arachidonic acid by PLA
2
, converting this acid to leukotrienes, which are mediators of inflammation.
3′,5′-cAMP phosphodiesterase, hereafter called “phosphodiesterase” or “PDE”, is the enzyme which converts cAMP—a second messenger involved in controlling the cell metabolism—to inactive AMP. Consequently, the inhibition of PDE by an inhibitor makes it possible to maintain a high intracellular level of cAMP, which has the effect especially of activating the protein kinases A and, via this process, makes it possible to promote lipid degradation.
Furthermore, it is also known that cAMP plays a part in counteracting certain inflammatory processes (M. Hitchcock, J. Immunol. (1977) 188 557). Also, it has been described that phosphodiesterase increases with age (S. K. Puri and L. Volicer, Mechanisms of Aging and Dev. (1981) 15 239). The inhibition of phosphodiesterase will therefore make a contribution to combating the effects of ageing, particularly on the skin.
Tyrosinase is the key enzyme in the synthesis of melanin and hence in the metabolism of skin pigmentation. In cosmetics, the inhibition of tyrosinase by appropriate agents has applications in the local treatment of skin hyperpigmentations such as liver spots.
SUMMARY OF THE INVENTION
Thus it has been demonstrated by the inventors that, by virtue of their inhibitory action on the above-mentioned enzymes, extracts of the plant Terminalia catappa are of great value in cosmetics and therapeutics.
In fact, through the discovery of the inhibitory activity of extracts of the plant Terminalia catappa on the action of enzymes, the invention provides different solutions in the cosmetic and therapeutic fields, especially the dermatological field. As regards the inhibition of phospholipase A
2
on the one hand and lipoxygenase on the other, the compositions according to the invention thus have a dual action in the process of formation of the mediators of skin allergy and inflammation, by limiting or blocking this process.
The inhibition of phosphodiesterase (PDE) gives the compositions of the invention a slimming, anti-inflammatory and anti-ageing action. The inhibition of tyrosinase gives them a skin depigmenting effect.
Other advantages of the invention will become apparent from the iption and the Examples which follow.
DETAILED DESCRIPTION OF THE INVENTION
Thus, according to one of its essential characteristics, the invention relates to cosmetic compositions containing an extract of the plant Terminalia catappa in the presence of a cosmetically acceptable vehicle.
It is essentially the leaves which are found to be of value in the preparation of the extracts of the invention.
The extract is advantageously obtained by maceration of the plant or part of the plant in a solvent or solvent mixture, followed by filtration. The solvent of the solution obtained can be evaporated off, if necessary, to give the dry extract.
The evaporation will preferably be performed under reduced pressure.
The following may be mentioned as solvents which are advantageously used:
water
chlorinated solvents, especially dichloromethane
ethers such as ethyl or diisopropyl ether
acetone
C
2
to C
8
esters such as ethyl acetate and butyl acetate
C
1
to C
6
alcohols such as methanol, ethanol and isopropanol
C
2
to C
6
polyols such as propylene glycol or glycerol.
The plant extract can also be obtained by the so-called supercritical carbon dioxide extraction technique.
In one advantageous embodiment, this composition comprises from 0.001 to 10% by weight and particularly from 0.02 to 1% by weight of dry plant extract, based on the total weight of the final composition.
Furthermore, the experiments carried out by the inventors have clearly shown that not only the extraction yield but also the enzymatic activity of the extract is related to the nature of the solvent used. The attached Examples clearly show the effect of the choice of solvent on the enzymatic activity of the extract.
The compositions according to the invention can be formulated in any form acceptable for their use in cosmetology. In particular, the composition can be in a form appropriate for topical application, specifically in the form of a cream or gel and particularly a cream or gel for the face, hands, bust or body.
According to another aspect, the invention relates to the use of the plant extract as a cosmetic agent, said agent being incorporated in a cosmetic composition as defined above.
This cosmetic agent will be used especially in all applications which are aimed in particular at inhibiting the action of phospholipase A
2
and/or lipoxygenase and/or phosphodiesterase and/or tyrosinase.
The compositions according to the invention will also be used to combat the effects of skin ageing, especially by preserving or improving the biomechanical properties of the skin, particularly its elasticity, by delaying the appearance of wrinkles or reducing their depth and by improving the firmness of the skin.
They will also be used for the care of sensitive skin, especially by reducing or eliminating the phenomena of irritation, inflammation or allergy which generally manifest themselves on the skin in the form of red blotches or burning or smarting sensations.
They may also be used to achieve slimming on different parts of the body, particularly the hips. They may also be used for the purpose of reducing or eliminating freckles.
Thus the cosmetic compositions of the invention will be used especially for any cosmetic applications which are aimed at inhibiting the activity of the above-mentioned enzymes.
Thus, according to another aspect, the invention relates to cosmetic compositions intended for skin care and particularly for combating the effects of skin ageing or inflammation phenomena.
They are also found to be of value for their slimming action or their depigmenting action.
As seen previously, it has been possible to correlate the efficacy of the above-described cosmetic compositions with a number of enzymatic activities. The demonstration of these enzymatic activities has also made it possible to consider using the above-defined extracts for the preparation of pharmaceutical compositions, especially dermatological compositions, in which such activities are desired. The experiments carried out by the inventors of the present invention have confirmed the efficacy of these pharmaceutical compositions.
Thus it has been possible to correlate the inhibition of phospholipase A
2
and the inhibition of 5′-lipoxygenase with efficacy in the prevention and treatment of inflammation phenomena.
It has been possible to correlate the inhibition of tyrosinase with an action in the local treatment of skin hyperpigmentation.
The inhibition of PDE re
Andre Patrice
Olivier Marc
Renimel Isabelle
Dennison, Scheiner & Schultz
Parfums Christian Dior
Travers Russell
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