Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
  • A61Q19/08—Anti-ageing preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/77—Sapindaceae (Soapberry family), e.g. lychee or soapberry
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
  • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
  • A61K8/9783—Angiosperms [Magnoliophyta]
  • A61K8/9789—Magnoliopsida [dicotyledons]
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/74—Biological properties of particular ingredients
  • A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
  • A61K2800/782—Enzyme inhibitors; Enzyme antagonists

Definitions

• Cosmetic or pharmaceutical composition in particular dermatological and culture medium, containing an extract of Smelophyllum capense.
• the present invention essentially relates to a cosmetic or pharmaceutical composition, in particular dermatological and culture medium, containing an extract of Smelophyllum capense.
• the present invention relates to the use of an extract of Smelophyllum capense, for the preparation of a cosmetic or pharmaceutical composition, in particular a dermatological composition, in particular stimulating the synthesis of collagen, and intended in particular for combating the effects skin aging, to obtain a skin tightening, to improve healing or to treat various pathologies accompanied by a collagen deficiency; or as one of the active principles or adjuvants of a cell or tissue culture medium, especially for the mass culture of skin cells, in particular fibroblasts, as well as cosmetic or pharmaceutical compositions or culture media with application.
• the Smelophyllum capense plant belongs to the Sapindaceae family which includes around 1,700 plant species.
• the plants of this family contain saponins which have long been used as detergent and fishing poison.
• the Smelophyllum capense plant is a tree of relatively modest height, measuring 3 to 4 m, which is found endemic in particular in the forests of the southern part of South Africa (see RB Drumont, " Trees of Southern Africa, C. Struik Publisher, Capetown, 1984, page 531) It has now been discovered that extracts of Smelophyllum capense are of great interest in cosmetics, especially for skin care.
• collagen I collagen type I
• the skin essentially contains collagen I, a protein synthesized by fibroblasts, the major cells of the dermis. This protein plays a supporting role and is responsible for the rheological qualities of the dermis, in particular for its firmness and for maintaining its architecture (EU KUCHARZ, "The collagens Biochemistry and pathophysiology", Springer Verlag, Berlin 1992).
• EU KUCHARZ "The collagens Biochemistry and pathophysiology", Springer Verlag, Berlin 1992.
• fibroblasts in the dermis of the elderly secrete less collagen than those of young subjects (M. DUMAS et al, Mech, Aging Dev.
• the main object of the present invention is therefore to solve the new technical problem consisting in providing a new formulation of a cosmetic or pharmaceutical composition, in particular a dermatological composition, having good efficacy in preventing or treating the effects of skin aging, as well as on skin tightening, or to improve healing.
• the main object of the present invention is also to solve this new technical problem in a particularly simple, satisfactory and usable manner on an industrial scale, especially in the cosmetic or pharmaceutical industry.
• the present invention relates to the use of an extract of Smelophyllum capense as a cosmetic agent, in particular for the care of the skin.
• an extract of Smelophyllum capense is used for the preparation of a cosmetic or pharmaceutical composition, in particular dermatological, stimulating in particular the synthesis of collagen, in particular that of collagen I, and intended in particular for improve skin healing, improve biomechanical properties and surface appearance of the skin, obtain skin firming, combat the effects of skin aging or treat various pathologies accompanied by collagen deficiency.
• the extract of Smelophyllum capense is used for the preparation of a composition, with anti-aging skin effect, in particular anti-wrinkle, intended to prevent the appearance of wrinkles or attenuate their depth.
• Smelophyllum capense above is obtained by extraction with a polar solvent, such than a lower alcohol, advantageously chosen from methanol or a hydro-ethanolic mixture, preferably from the bark of the plant, more preferably from the root bark of this plant.
• a polar solvent such than a lower alcohol, advantageously chosen from methanol or a hydro-ethanolic mixture, preferably from the bark of the plant, more preferably from the root bark of this plant.
• the extract of Smelophyllum capense can be obtained according to the method described below by way of indication, but in no way limiting.
• a first extraction of the bark, preferably from the root bark, from the plant, is carried out with a polar solvent, advantageously chosen from the group consisting of: water, alcohols preferably containing from 1 to 4 atoms carbon, chlorinated solvents preferably having 1 to 2 carbon atoms, organic esters preferably having 3 to 6 carbon atoms; or a mixed solvent based on any mixture of the aforementioned solvents.
• a polar solvent advantageously chosen from the group consisting of: water, alcohols preferably containing from 1 to 4 atoms carbon, chlorinated solvents preferably having 1 to 2 carbon atoms, organic esters preferably having 3 to 6 carbon atoms; or a mixed solvent based on any mixture of the aforementioned solvents.
• the solvent of first extraction is chosen from the group consisting of water, methanol, ethanol, a methanol-water mixture or an ethanol-water mixture, chloroform, dichloromethane. More preferably, it is water, methanol, ethanol or their mixtures.
• the ratio of the bark to the extractant is not critical and will generally be between 1: 5 and 1:20 parts by weight.
• the extraction is generally carried out at temperatures between room temperature and the boiling point of the solvent used for the extraction.
• this first extraction is carried out at reflux under atmospheric pressure for a period of 2 to 4 h.
• it is advantageously preceded by cold maceration for 2 to 4 hours in the extraction solvent.
• the present invention also relates to a cosmetic composition characterized in that it comprises, as active ingredient, a cosmetically effective amount of an extract of Smelophyllum capense preferably dispersed in a cosmetically acceptable excipient.
• this cosmetic composition stimulates the synthesis of collagen, in particular that of collagen I, and is intended in particular to combat the effects of skin aging, or to get skin firming.
• a composition for example, can advantageously be used as a composition to prevent the appearance of wrinkles or attenuate their depth.
• the invention also relates to a pharmaceutical composition, in particular a dermatological composition, stimulating the synthesis of collagen, in particular that of collagen I, characterized in that it comprises, as active ingredient, a pharmaceutically effective amount of an extract of Smelophyllum capense dispersed in a pharmaceutically acceptable excipient.
• said composition is intended to improve skin healing or to treat various pathologies accompanied by a deficiency in collagen.
• the invention also covers a cosmetic or pharmaceutical treatment process, in particular dermatological treatment, characterized in that it comprises the application of a cosmetically or pharmaceu ⁇ tically effective amount for a cosmetic or pharmaceutical treatment of a Smelophyllum capense extract, in particular dispersed in a cosmetic or pharmaceutically acceptable excipient.
• a cosmetic or pharmaceutical treatment process in particular dermatological treatment, characterized in that it comprises the application of a cosmetically or pharmaceu ⁇ tically effective amount for a cosmetic or pharmaceutical treatment of a Smelophyllum capense extract, in particular dispersed in a cosmetic or pharmaceutically acceptable excipient.
• the extract of Smelophyllum capense will preferably be used at a concentration of between 0.0001% and 1% by weight relative to the total weight of the final composition. Preferably, this concentration is between 0.01% and 0.25% by weight relative to the total weight of the final composition.
• the composition according to the invention preferably also contains an active substance chosen from the group consisting of ascorbic acid, madecassic acid, asian acid, madecassoside, asiaticoside, alpha-1-proteinase inhibitor, collagenase inhibitors, such as retinoic acid, elastase inhibitors, lysine, proline, 2-oxoglutarate, and ginsenoside Rrj-
• the present invention also relates to the use of an extract of Smelophyllum capense as one of the active principles or one of the adjuvants of a cell or tissue culture medium, in particular for the mass culture of skin cells, in particular fibroblasts.
• this use relates to the preparation of skin or an artificial dermis.
• the invention also relates in this aspect to a method of treating fibroblasts in culture by an effective concentration of an extract of Smelophyllum capense to obtain stimulation of the synthesis of collagen, in particular collagen I.
• the fibroblasts are treated with an extract of Smelophyllum capense at a concentration at the time of culture of between 0.3 / g / ml and 30 / g / ml of culture medium.
• ascorbic acid or one of its derivatives can be added to the culture medium at a non-cytotoxic concentration, in particular between 0.001 mM and 0.5 mM.
• one or more of the following substances can be added to the culture medium: L-glutamine, L-lysine, 5-hydroxy-L-lysine, L-proline and 4-hydroxy-L-proline, said substances may each be present at a concentration of between 2 and 10 mM.
• Smelophyllum capense root bark powder is prepared by grinding dried root bark of this plant from South Africa. Then 200 g of this powder are macerated for 2 h in 2 l of methanol. The whole is brought to reflux for 3 h, then it is allowed to cool and filtered. on sintered glass. The filtrate is evaporated to dryness. The residue, weighing 44.6 g, is taken up in 350 ml of methanol. Precipitation is carried out by adding 1.75 l of ethyl ether to this solution, then filtering. The precipitate is then dried over a solid dehydrating agent such as P2O5. An amount of approximately 27 g of this precipitate is then dialyzed for 4 days against 270 ml of demineralized water, then lyophilized. 13.6 g of extract according to the invention, called extract 1, are thus obtained.
• Cultures of healthy adult dermis fibroblasts are carried out using the explant method using a facial skin sample obtained from a woman aged 60 years during a facelift.
• Fibroblasts are grown to confluence in 199 E medium (Gibco) supplemented with 2 mM L-glutamine (Gibco) and 10% v / v fetal calf serum (Gibco) at 37 ° C in an atmosphere of 5% of humidified CO2.
• the confluent primary cultures are harvested with a 0.1% solution of trypsin and 0.02% EDTA in phosphate buffered saline (PBS) at pH 7.2 and the cells are then seeded at the density of 10 ⁇ fibroblasts per well, in microculture plates (Falcon) with 96 wells, in the presence of the same culture medium as that described above.
• PBS phosphate buffered saline
• the medium is removed and replaced by a medium of the same composition as the medium described above, except that it does not contain serum and that 25 ⁇ M of acid have been added L-ascorbic in the form of sodium salt.
• this new medium contains or not the product to be tested (extract 1 ⁇ ) depending on whether it is a treated culture or a control culture. Then incubated for an additional 48 h at 37 * C.
• the test product (extract I j) was dissolved in DMSO prior to incorporation into the culture medium (final DMSO concentration in the medium is 0.1% v / v).
• the amount of type I collagen secreted by the cells in the serum-free medium after 48 h of incubation with the mixture or the individual component is determined by an ELISA test as previously described in the publication by Dumas M. et al. , Mech. Aging Dev. (1994) 73, 179-187, and that of Grimaud JP et al., In: Methods of Enzymatic Analysis (Bermeyer, HU, ed.), VCH Publishers, einheim, (1986), 186-201.
• the serum-free incubation mediums and the remaining cells homogenized by sonication in ice is collected and transferred to wells of a plastic immunoplate (NUNC) for an incubation of 24 hours at 4 ° C to allow the adhesion of secreted collagen.
• Protease inhibitors ethylmaleimide, phenylmethylsulfonyl fluoride, ethylenediaminetetraacetate, each in a final concentration of 1 mM
• the plates are then reinserted with PBS. A similar washing step is carried out after each plaque treatment.
• the percentage of stimulation A of the synthesis of collagen gene I is calculated by comparing the amounts of collagen I secreted in the control cultures (receiving no product to be tested) C 0 and in the treated cultures, from the following formula:
• Smelophyllum capense produced a significant activity of stimulation of the synthesis of collagen I by fibroblasts.
• the extract of Smelophyllum capense can be used for products intended to combat skin aging or requiring an increase in local synthesis of collagen as is the case during a treatment of wrinkles or to help improve the skin healing.
• the extracts of Smelophyllum capense can advantageously be used, thanks to their property of stimulating the synthesis of collagen, as active agent, in cosmetic or pharmaceutical compositions, in particular dermatological, as defined above.
• Part of the aqueous excipient is used with Carbopol to separately prepare a gel, the other part of the aqueous excipient is used to be mixed with the other components and the gel is added to the solution obtained in order to obtain a gelled composition forming the massage gel.
• This massage gel composition can be used three times a week for two months at the bust.
• Hyaluronic acid 1 g Aqueous excipient containing a possibly flavored preservative qs 100.00 g The extract is first dissolved in the solubilizing agent, then is added to the aqueous excipient to which hyaluronic acid is added.
• the lotion obtained can be used for a three-week treatment on areas sensitive to sagging, such as the belly, thighs.
• This cream applied twice a day, restores the qualities of firmness, elasticity as well as the skin barrier properties and the radiance of young skin.

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• 1994
  • 1994-12-23 FR FR9415576A patent/FR2728465B1/fr not_active Expired - Fee Related
• 1995
  • 1995-12-22 EP EP95943268A patent/EP0799049A1/de not_active Withdrawn
  • 1995-12-22 WO PCT/FR1995/001724 patent/WO1996020000A1/fr not_active Application Discontinuation
  • 1995-12-22 JP JP8520260A patent/JPH10511380A/ja active Pending
  • 1995-12-22 US US08/849,453 patent/US5807555A/en not_active Expired - Fee Related

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