Alcoholic extract of citrus aurantium peel method for obtaining same and cosmetic or dermatological composition comprising same
The Hirami lemon peel extract, enriched with hesperidin, nobiletin, and isosinensetin, addresses excessive skin desquamation by inhibiting kallikreins KLK5 and KLK7, enhancing skin comfort and barrier function.
Patent Information
- Application Number
- JP2025235953
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2022-09-16
- Filing Date
- 2025-12-05
- Publication Date
- 2026-02-27
AI Technical Summary
Existing cosmetic solutions fail to effectively inhibit or prevent excessive skin desquamation, leading to unsightly and uncomfortable conditions such as scales or dandruff, and compromise the skin's barrier function.
An alcoholic extract of Hirami lemon peel, enriched with hesperidin, nobiletin, and isosinensetin, is obtained through a specific extraction process, which reduces the gene expression of kallikreins KLK5 and KLK7, key enzymes involved in desquamation.
The extract effectively limits desquamation by inhibiting these enzymes, thereby improving skin comfort and maintaining the skin's barrier function.
Smart Images

Figure 2026034492000001_ABST
Abstract
Description
[Technical Field]
[0001] The present invention relates to an extract of the peel of Citrus depressa, a process for obtaining it, cosmetic or dermatological compositions containing it, and its cosmetic uses. [Background technology]
[0002] The skin is mainly composed of three layers: the epidermis, the dermis, and the subcutaneous tissue.
[0003] The epidermis, the outer layer of the skin, is stratified and contributes greatly to protecting the skin from external aggressions. It is composed of three main cell types: keratinocytes (highly predominant), melanocytes, and Langerhans cells. Through their respective functions, these cell types contribute to the essential role that skin plays in the body, in particular its "barrier function," which protects the body from external aggressors (such as weather, UV rays, and tobacco).
[0004] Epidermal aging is primarily manifested as a decrease in thickness. Epidermal atrophy is the result of delayed keratinocyte proliferation and the accumulation of senescent keratinocytes. The stratum corneum of the skin becomes dull.
[0005] Desquamation is a natural phenomenon associated with the fact that the epidermis, which constitutes the upper layer of the skin, is constantly regenerating. The epidermis is composed of several layers of cells, the deepest of which is the stratum basale, which is composed of undifferentiated cells. Over time, these cells differentiate and migrate to the surface of the epidermis, where they constitute the various layers of the epidermis, forming keratinocytes, the dead cells that are removed by desquamation. This surface loss is compensated for by the migration of cells from the stratum basale to the surface of the epidermis. This is the regular renewal of the skin.
[0006] However, excessive or irregular shedding of the keratinocyte layer can lead to the formation of large, thick clumps of cells visible to the naked eye, called "scales" or "dandruff" on the scalp, or in other cases, thinning of the stratum corneum, causing a tense and uncomfortable sensation. Desquamation disorders resulting from abnormal or irregular shedding can also lead to weaknesses or even deficiencies in the barrier properties of the epidermis.
[0007] The presence of scale and dandruff is often a recurring condition that can be unsightly and downright annoying. [Prior art documents] [Patent documents]
[0008] [Patent Document 1] KR2012 / 0043288 Summary of the Invention [Problem to be solved by the invention]
[0009] There is therefore a need to have new active agents that act against excessive desquamation of the skin or scalp in order to limit and / or prevent desquamation and thereby contribute to skin comfort. [Means for solving the problem]
[0010] Hirami lemon is a citrus fruit from the Rutaceae family that grows in Japan. Generally, aqueous extracts of these fruits can be explored for cosmetic applications.
[0011] For example, document KR2012 / 0043288 proposes the use of an extract of lemongrass as a skin lightening agent, stimulating skin renewal.
[0012] The authors of the present invention have now demonstrated, quite surprisingly, that an alcoholic extract of the peel of Lemon japonica exhibits activity in the mechanisms involved in desquamation, in particular by inhibiting certain enzymes involved in desquamation.
[0013] This finding leads to the development of novel non-therapeutic cosmetic compositions that are useful in all applications where it is desired to improve skin comfort, especially by inhibiting or limiting desquamation.
[0014] Thus, according to a first aspect, the present invention relates to an alcoholic extract of the peel of Lemon jasmine, comprising a mixture of hesperidin, nobiletin, and isosinensetin.
[0015] Another object of the present invention is a cosmetic composition comprising, in a pharmaceutically acceptable medium, at least one alcoholic extract of the peel of the Horhirami lemon of the present invention.
[0016] According to a third aspect, the present invention provides a method for producing a medicament for the preparation of ... a) extraction of pre-dried and crushed lemon peel with at least one alcoholic solvent; b) filtering the mixture obtained from step a) and optionally decolorizing the obtained filtrate by adsorption on activated carbon; c) concentrating the dry extract by evaporation to a dry extract content of 5-20%, preferably 9-12%; d) allowing the mixture obtained in c) to stand for at least 6 hours until four distinct phases are obtained; e) separating the phases formed in step d) by removing the two solid and oily lower phases and the upper layer of essential oils, and collecting the alcoholic phase containing the extract of lemon peel; The present invention relates to a method for extracting lemon juice from the peel of lemon limon.
[0017] Finally, an object of the invention according to a fourth aspect is the non-therapeutic cosmetic use of the alcoholic extract of lemon peel as described above to limit / protect excessive desquamation and contribute to skin comfort. [Brief explanation of the drawings]
[0018] [Figure 1]FIG. 1 shows the decrease in gene expression of kallikreins (KLK) KLK5 and KLK7, two serine proteases involved in skin desquamation, after treatment with the alcoholic extract of lemon peel of the present invention at 0.033%. DETAILED DESCRIPTION OF THE INVENTION
[0019] Hirami Lemon Hirami lemon, also known as Shikuwasa, is a citrus fruit from the Rutaceae family that grows in Japan.
[0020] The word Shikuwasa refers to both the plant and the fruit.
[0021] It is a small, branchy tree about 5 m tall, vigorous, densely fruiting. White flowers appear in April (flowers 3 cm in diameter). The fruits are harvested in October-November.
[0022] The fruit is small (2.5-4 cm in diameter, 2-3 cm in height, 25-60 g in weight), slightly concave at both poles, and has a thin pericarp (skin). It contains 8 or 10 juice-containing segments and seeds. The flesh is soft and gelatinous, and the juice is acidic. The essence contained within the skin has the aroma of Satsuma Mandarin. Therefore, the juice is primarily used in the food industry, and the peel is used to prepare essential oils.
[0023] The extract of the present invention is obtained from the peel of the Hirami lemon, preferably after pressing of the fruit to obtain the juice.
[0024] Alcohol extract of Hirami lemon peel The alcoholic extract of lemon peel according to the present invention contains a mixture of hesperidin, nobiletin, and isosinensetin.
[0025] The combination of these three remarkable molecules, obtained by means of a very specific extraction process, actually makes it possible to reduce the gene expression of two serine proteases involved in skin desquamation, the kallikreins (KLK) KLK5 and KLK7, thus limiting / preventing excessive desquamation and contributing to skin comfort.
[0026] According to a preferred embodiment, the alcoholic extract of lemon peel according to the invention comprises: 0.1 to 5% by weight, preferably 0.5 to 2% by weight, of hesperidin relative to the weight of the dry extract, - 0.1 to 5% by mass, preferably 1 to 2% by mass, of nobiletin; 0.1 to 3% by weight, preferably 0.5 to 1% by weight, of isosinensetin (percentages expressed by weight relative to the weight of the dry extract).
[0027] Preferably, hesperidin, nobiletin, and isosinensetin are present in a mass ratio of hesperidin / nobiletin / isosinensetin between 0.5 / 1 / 1.5 and 1.5 / 3 / 4, preferably a mass ratio of 1.1 / 1.4 / 0.7.
[0028] Method for preparing alcohol extract of Hirami lemon peel According to one particular embodiment, the object of the present invention is to provide a method for producing a pharmaceutical composition comprising the steps of: a) extraction of pre-dried and crushed lemon peel with at least one alcoholic solvent; b) filtering the mixture obtained from step a) and optionally decolorizing the obtained filtrate by adsorption on activated carbon; c) concentrating the dry extract by evaporation until a dry extract content of 5-20%, preferably 9-12% is reached; d) allowing the mixture obtained in c) to stand for at least 6 hours until four distinct phases are obtained; e) separating the phases formed in step d) by removing the two solid and oily lower phases and the upper layer of essential oils, and collecting the alcoholic phase containing the extract of lemon peel; This method involves extracting the compound from the peel of the lemon tree.
[0029] Indeed, it is to the Applicant's credit that it has proven possible to obtain an extract from the peel of the Hirami lemon, by extraction under very specific conditions, that is enriched in molecules of interest in preventing desquamation, such as hesperidin, nobiletin and isosinensetin.
[0030] The method according to the invention involves a first step a) of extracting the peel of the lemongrass with at least one alcoholic solvent.
[0031] The skins obtained from the pressing of the fruit are preferably dried and then reduced to a dispersible powder by any grinding process conventionally known to those skilled in the art, such as, for example, grinding in a knife mill at room temperature or, in preferred embodiments, at low temperature.
[0032] Preferably, the dispersible powder of lemon peel used for preparing the extract according to the invention has an average particle size of less than 500 μm, preferably less than 300 μm.
[0033] In step a), the peel of Hirami lemon is dissolved in one or more alcoholic solvents, such as: C1-C4 monoalcohols, such as methanol, ethanol or isopropanol; and diols, such as propylene glycol, 1,3-propanediol, or dipropylene glycol, The extract is subjected to extraction with an alcohol solvent selected from the group consisting of:
[0034] Preferably, the alcohol solvent is a monoalcohol containing 2 to 4 carbon atoms, more preferably ethanol.
[0035] The extraction is generally carried out by macerating the peel of the lemongrass in one or more of the above-mentioned solvents for a period of 30 minutes to 8 hours, for example, at a temperature ranging from room temperature to 80°C, with stirring. Preferably, the extraction in step a) is carried out at a temperature of 50°C to 70°C for a period of 1 to 5 hours.
[0036] In particular, the mass ratio of lemon peel to alcohol solvent is between 1 / 1 and 1 / 15, preferably 1 / 8.
[0037] Following the extraction step, the material is preferably sieved through a sieve between 50 μm and 150 μm, preferably 100 μm.
[0038] According to one particular embodiment, the extraction step a) is carried out twice, and the method of the invention comprises: a) first extracting pre-dried and crushed lemon peel with an alcoholic solvent, preferably ethanol, at a temperature of 50°C to 70°C for 1 to 5 hours, and then sieving to a sieve size of 50 μm to 150 μm; a') subjecting the residue of lemon peel obtained in step a) to a second extraction with an alcohol solvent, preferably ethanol, at a temperature of 50°C to 70°C for 1 to 5 hours, and then sieving the residue through a 50 μm to 150 μm sieve.
[0039] After step a), the method according to the invention preferably carries out a filtration step b), which is carried out to a threshold of 30 μm, preferably 15 μm.
[0040] Step b) also optionally comprises decolorizing the obtained filtrate by adsorption of the dye on activated carbon. The decolorizing of the filtrate on activated carbon is carried out, for example, for 1 to 6 hours, preferably 3 hours, with stirring, at a temperature between 20°C and 30°C, preferably at room temperature (20°C).
[0041] For decolorization, the activated carbon content is generally between 20 and 40% by weight, preferably about 30% by weight, relative to the total weight of dry matter of the extract.
[0042] At the end of the decolorization, the activated carbon is removed by filtration to a threshold of 5 μm, preferably 2 μm.
[0043] The optionally decolorized alcoholic filtrate obtained from step b) is then concentrated by evaporating the solvent until a dry extract content of 5-20%, preferably 9-12%, is obtained (step c). Evaporation of the solvent can be carried out, for example, by a rotary evaporator or a falling film evaporator.
[0044] The concentrated extract obtained from step c) is then left to stand for at least 6 hours until four distinct phases are obtained: two solid and oily lower phases, an upper layer of essential oils, and a middle alcoholic phase containing the extract of lemon peel.Standing can be carried out, for example, in ampoules.
[0045] According to a preferred embodiment, the standing step d) is carried out for at least 12 hours, preferably at least 24 hours, more preferably between 24 and 48 hours.
[0046] The standing is carried out at a temperature of 0 to 25°C, preferably 1 to 10°C, more preferably 4 to 5°C.
[0047] Once settling is complete and four phases have been obtained, the phase of interest is extracted by removing the two solid and oily lower phases and the upper layer containing the essential oil, and the alcoholic phase containing the extract of Hirami lemon peel is collected.
[0048] The alcoholic extract of the peel of Hirami lemon can then be filtered to a threshold of 5 μm, preferably 2 μm (step f) and then diluted in an alcoholic solvent different from the extraction solvent used in step a).
[0049] The extraction solvent introduced in step a) is then evaporated (step g) until a residual concentration of extraction solvent of less than 1%, preferably less than 0.5%, is reached.
[0050] Finally, the mixture obtained at the end of step g) is left to stand for at least 6 hours, preferably 12 hours, and then filtered to a threshold of 5 μm, preferably 2 μm, typically at a temperature of 0 to 25° C., preferably 1 to 10° C., more preferably 4 to 5° C.
[0051] Therefore, according to a preferred embodiment, the method for extraction from the peel of Hirami lemon comprises the following steps: a) first extracting pre-dried and crushed lemon peel with an alcohol solvent, preferably ethanol, at a temperature of 50°C to 70°C for 1 to 5 hours, and then sieving to a sieve size of 50 μm to 150 μm; a') subjecting the residue of lemon peel obtained in step a) to a second extraction with an alcohol solvent, preferably ethanol, at a temperature of 50°C to 70°C for 1 to 5 hours, and then sieving the residue through a 50 μm to 150 μm sieve; b) filtering the mixture obtained from step a) and optionally decolorizing the obtained filtrate by adsorption on activated carbon; c) concentrating the dry extract by evaporation to a dry extract content of 5-20%, preferably 9-12%; d) allowing the mixture obtained in c) to stand for at least 6 hours until four distinct phases are obtained; e) separating the phases formed in step d) by removing the two solid and oily lower phases and the upper layer of essential oils, and collecting the alcoholic phase containing the extract of lemon peel; f) filtering the alcoholic fraction collected in step e) to a threshold of 5 μm, preferably 2 μm, followed by final dilution of the filtered extract in another alcoholic solvent; g) evaporating the extraction solvent introduced in step a) until a residual concentration of extraction solvent of less than 1%, preferably less than 0.5% is reached; h) leaving the mixture obtained in g) to stand for at least 6 hours, followed by filtration to a threshold of 5 μm, preferably 2 μm; Includes:
[0052] Even more preferably, the method for extraction from the peel of Hirami lemon comprises the following steps: a) first extracting pre-dried and crushed lemon peel with ethanol at a lemon peel / ethanol mass ratio of 1 / 8 at a temperature of 50°C to 70°C for 1 to 5 hours, and then sieving through a 100 μm sieve; a') secondly extracting the lemon peel residue obtained in step a) with ethanol at a lemon peel / ethanol mass ratio of 1 / 8 at a temperature of 50°C to 70°C for 1 to 5 hours, and then sieving through a 100 μm sieve; b) filtering the mixture obtained from step a) and decolorizing the obtained filtrate by adsorption on activated carbon for 3 hours at room temperature; c) concentrating the dry extract by evaporation to a dry extract content of 10-11%; d) allowing the mixture obtained in c) to stand for at least 12 hours at a temperature of 4-5°C until four distinct phases are obtained; e) separating the four phases formed in step d) by removing the two solid and oily lower phases and the upper layer of essential oils, and collecting the ethanolic phase containing the extract of lemon peel; f) filtering the ethanol fraction collected in step e) to a threshold of 2 μm, followed by final dilution of the filtered extract in pentylene glycol; g) evaporating the extraction ethanol introduced in step a) until a residual ethanol concentration of less than 0.5% is reached; h) leaving the mixture obtained in step g) at rest for at least 12 hours at a temperature of 4-5°C, followed by filtering to a threshold of 2 μm; Includes:
[0053] Cosmetic Composition A further object of the present invention is a cosmetic composition comprising, in a pharmaceutically acceptable solvent, at least one alcoholic extract of the peel of the above-mentioned lemon.
[0054] The compositions used according to the invention generally comprise, in addition to the extracts mentioned above, a pharmaceutically acceptable, preferably cosmetically acceptable vehicle, meaning one that is suitable for use in contact with human skin, without toxicity, incompatibility, instability, risk of allergic reactions, and in particular without causing discomfort (redness, tightness, stinging).
[0055] Advantageously, said cosmetic or dermatological composition may be in the form of a powder, emulsion, microemulsion, nanoemulsion, suspension, solution, lotion, cream, aqueous or aqueous alcoholic gel, foam, serum, aerosol solution or dispersion, or dispersion of lipid vesicles.
[0056] In the case of emulsions, the composition may be a water-in-oil or oil-in-water emulsion.
[0057] The cosmetic or dermatological compositions of the present invention may also contain a solvent, which is selected depending on the various ingredients and the mode of administration.
[0058] For example, water (preferably demineralized water or floral water) or alcohol such as ethanol may be mentioned.
[0059] In addition to the extract according to the present invention, the cosmetic composition may comprise, for example, at least one compound selected from emollients or wetting agents, gelling and / or thickening agents, surfactants, oils, active agents, colorants, preservatives, antioxidants, active agents, organic or mineral powders, sunscreens, and fragrances, and at least one additive conventionally recognized in the art, in particular the following additives:
[0060] - one or more wetting agents such as polyols (glycerin, diglycerin, propylene glycol, caprylyl glycol, pentylene glycol, hexanediol), sugars, glycosaminoglycans such as hyaluronic acid and its salts and esters; and polyquaterniums such as Lipidure-PMB. The wetting agents may be present in the composition in a content of 0 to 30% by weight, preferably 0.005 to 10% by weight, of the total weight of the composition.
[0061] one or more emollients, which may be chosen, for example, from esters such as jojoba esters, esters of fatty acids and fatty alcohols (octyldodecyl myristate, triethylhexanoin, dicaprylyl carbonate, isostearyl isostearate, caprylic / capric triglyceride), butters such as shea butter (butyrospermum parkii butter extract, shea butter ethyl ester, trade names LIPEX SHEASOFT, LIPEX SHEA-U, LIPEX SHEA, LIPEX SHEALIGHT, LIPEX SHEA TRIS) or moringa butter (moringa oil / hydrogenated moringa oil esters), waxes (acacia decurrens flower wax and helianthus annuus seed cera seed wax, C10-C18 triglycerides), vegetable oils, phytosqualane, alkanes (undecane, tridecane). The softener may be present in the composition in an amount of 0.1 to 30% by weight, preferably 0.5 to 10% by weight, based on the total weight of the composition.
[0062] one or more gelling and / or thickening agents for the aqueous phase, selected for example from cellulose derivatives, gums of plant origin (guar, carob, alginates, carrageenan, pectin), gums of microbial origin (xanthan), clays (laponite), crosslinked or non-crosslinked hydrophilic or amphiphilic homopolymers and copolymers of acrylamidomethylpropanesulfonic acid (AMPS), and / or acrylamide, and / or acrylic acid, and / or salts or esters of acrylic acid (trade names ARISTOFLEX AVC, Aristoflex AVS, Aristoflex HMB, SIMULGEL NS, Simulgel EG, Simulgel 600, Simulgel 800, Pemulen, carbopol, Sepiplus 400, Seppimax zen, Sepiplus S, COSMEDIA SP), which may be present in the composition in a content of 0.1 to 10% by weight of the total weight of the composition.
[0063] one or more surfactants, in particular: Anionic surfactants such as isethionates, taurates, sarcosinates, glycinates, glutamates, and phosphates (C20-22 alkyl phosphates, trade name SENSANOV WR) Amphoteric surfactants such as betaine derivatives and amphoacetates Non-ionic surfactants such as polyglycerol derivatives, sugar derivatives (glucoside or xyloside derivatives, trade names MONTANOV 68, MONTANOV 202, Montanov 82, MONTANOV L, EASYNOV), and lecithin
[0064] The surfactant may be present in a content of about 0.1 to 15% by weight, preferably 0.5 to 10% by weight, relative to the total weight of the composition.
[0065] - Vitamin C and its derivatives (ascorbic acid glucoside, 3-O-ethyl ascorbic acid, ascorbic acid tetraisopalmitate), vitamin A and its derivatives, vitamin E and its derivatives, vitamins such as vitamin B3 or niacinamide, panthenol, trace elements, allatoin, adenosine, peptides (palmitoyl tetrapeptide-7, palmitoyl tripeptide-1, palmitoyl pentapeptide-4, acetyl dipeptide-1 cetyl ester, acetyl tetrapeptide-5, trade names NP RIGIN, MATRIXYL 3000, IDEALIFT, EYESERYL), plant extracts (Glycyrrhiza glabra extract, Centella asiatica leaf extract, Rye (secale One or more active agents of natural, biotechnological or synthetic origin, which are biologically active and exert their effect on the skin through biological sites, for example selected from the group consisting of (cereale) seed extract, yeast extract, alpha hydroxy acids such as glycolic acid or lactic acid, tranexamic acid and its derivatives such as cetyl tranexamate, etc. The active agent may be present in the composition in a content of about 0.1 to 10% by weight of the total weight of the composition.
[0066] Other additives normally used in cosmetics may be present in the compositions according to the invention, in particular preservatives, antioxidants or fragrances well known in the art.
[0067] From all of these possible additives, the skilled artisan can select both the nature and the amounts of those added to the composition so that the composition retains all of its properties.
[0068] The present invention also relates to the non-therapeutic cosmetic use of an alcoholic extract of lemon peel to limit / protect excessive desquamation and contribute to skin comfort.
[0069] In this embodiment, the extract or composition is applied to altered, but non-diseased, skin.
[0070] A further object of the present invention is the non-therapeutic cosmetic use of an alcoholic extract of the peel of Lemon japonica as described above as an inhibitor of the gene expression of the kallikreins (KLK) KLK5 and KLK7. [Example]
[0071] The invention may be illustrated by the following non-limiting examples.
[0072] Example 1: Inhibition of the expression of enzymes involved in desquamation in normal human keratinocytes treated with an alcoholic extract of lemon peel according to the invention Extract preparation: The alcoholic extract of lemon peel according to the present invention was prepared by the following steps: a) 1 kg of dried peel was ground to a powder. Extraction from the peel was carried out in 8 kg of 96° ethanol at 60°C with stirring for 2 hours. The mixture was sieved through a 100 μm sieve to collect the peel residue and set the extract aside. a') The peel residue was again subjected to extraction in 8 kg of 96° ethanol with stirring for 2 hours at 60° C. The mixture was sieved through a 100 μm sieve. b) The liquid fractions from steps a) and a') were combined and then filtered at 15 μm. The ethanolic fraction was decolorized with 70 g of activated carbon (30% by weight relative to the dry substance of the extract) for 3 hours under stirring at room temperature. The activated carbon was then removed by filtration at 2 μm. c) The ethanol extract was concentrated by evaporating the ethanol in a rotary evaporator or falling film evaporator to obtain a concentrated extract with a dry matter content of 10%-11%. d) The whole was left to stand in the ampoule at 4°C for 1 to 2 days. e) The lower solid and oily phase was removed as well as the upper phase containing the essential oil. f) The ethanol fraction was collected and filtered at 2 μm. A dry matter determination was carried out on the extract, which contained 135 g of dry extract. 1215 g of pentylene glycol was added to the ethanol extract and the final extract was diluted to 10% dry matter. g) Ethanol was evaporated completely in a rotary evaporator or falling film evaporator (final ethanol concentration less than 0.5%). h) The extract was kept overnight at 4°C and filtered through a 2 μm filter. 1350 g of final extract 1701EXT was obtained.
[0073] procedure: Normal human epidermal keratinocytes from three different donors were seeded into 24-well plates and cultured in keratinocyte-SFM (k-SFM)-supplemented medium for 48 h at 37°C and 5% CO2. Cells were then incubated with 0.033% extract or without extract (non-treated condition) for 48 h. Each condition was performed in duplicate. Total RNA was extracted using TriPure Isolation Reagent® according to the supplier's recommended procedure. Complementary DNA was synthesized, and transcriptomes were generated on Affymetrix GeneChip Human Transcriptome Array 2.0 chips. Bioinformatics analysis of genes whose expression was regulated by at least two factors was performed using Ingenuity Pathway Analysis software (IPA®, QIAGEN).
[0074] result: The extract can reduce the transcriptional expression of kallikreins (KLKs) KLK5 and KLK7, two serine proteases involved in skin desquamation. 1 It is expressed in the upper layers of the epidermis and is involved in epidermal homeostasis. 2 These enzymes, including KLK5 and KLK7, are involved in the keratinocyte repair process and contain 15 isoforms. In fact, these two enzymes are capable of degrading the superficial corneodesmosomes that ensure the connections between the keratinocytes that make up the stratum corneum.
[0075] FIG. 1 shows the inhibition of transcriptional expression of KLK5 and KLK7 by 0.033% extract in normal human keratinocytes.
[0076] Example 2: Cosmetic Composition The following compositions may be prepared by methods familiar to those skilled in the art. The values given below are expressed as percentages by weight. Materials in capital letters are identified by their INCI names.
[0077] [Table 1]
[0078] [Table 2]
[0079] [Table 3]
[0080] These compositions can be applied to the skin daily, morning and / or night. They prevent excessive scaling and provide comfort to the user.
Claims
1. An alcoholic extract of the peel of Hirami lemon (Citrus depressa) containing a mixture of hesperidin, nobiletin, and isosinensetin.
2. - 0.1 to 5% by weight, preferably 0.5 to 2% by weight, of hesperidin relative to the weight of the dry extract, - 0.1 to 5% by weight, preferably 1 to 2% by weight, of nobiletin, - 0.1 to 3% by weight, preferably 0.5 to 1% by weight, of isocinensetin, 2. The alcoholic extract according to claim 1, wherein the percentages are expressed by weight relative to the weight of the dry extract.
3. 3. The alcoholic extract according to claim 1 or 2, wherein hesperidin, nobiletin, and isosinensetin are present in a mass ratio of hesperidin / nobiletin / isosinensetin of between 0.5 / 1 / 1.5 and 1.5 / 3 / 4, preferably a mass ratio of 1.1 / 1.4 / 0.
7.
4. A cosmetic or dermatological composition comprising an alcoholic extract of the peel of Lemon sieboldii according to any one of claims 1 to 3 in a cosmetically or pharmaceutically acceptable medium.
5. 5. Cosmetic or dermatological composition according to claim 4, characterized in that it is suitable for external application.
6. The following steps: a) extracting pre-dried and crushed lemon peel with at least one alcoholic solvent; b) filtering the mixture obtained from step a) and optionally decolorizing the obtained filtrate by adsorption on activated carbon; c) concentrating the dry extract by evaporation to a dry extract content of 5-20%, preferably 9-12%; d) allowing the mixture obtained in c) to stand for at least 6 hours until four distinct phases are obtained; e) separating the phases formed in step d) by removing the two solid and oily lower phases and the upper layer of essential oils, and collecting the alcoholic phase containing the extract of lemon peel; A method for extracting from the peel of Hirami lemon, including
7. 7. The method of claim 6, wherein step a) is carried out in ethanol at a temperature of 50°C to 70°C for 1 hour to 5 hours.
8. The extraction is done in two steps: a) first extracting pre-dried and crushed lemon peel with ethanol at a temperature of 50°C to 70°C for 1 to 5 hours, followed by sieving to a size of 50 μm to 150 μm; a') subjecting the residue of lemon peel obtained in step a) to a second extraction with ethanol at a temperature of 50°C to 70°C for 1 to 5 hours, followed by sieving through a 50 μm to 150 μm sieve; The method according to claim 6 or 7, wherein the method is carried out by
9. 9. The method according to any one of claims 6 to 8, wherein the filtration in step b) is carried out to a threshold of 30 μm, preferably 15 μm, and decolorization of the filtrate on activated carbon is carried out for 1 hour to 6 hours, preferably 3 hours, after which the carbon is removed by filtration to a threshold of 5 μm, preferably 2 μm.
10. The following steps: f) filtering the alcoholic fraction collected in step e) to a threshold of 5 μm, preferably 2 μm, followed by a final dilution of the filtered extract with another alcoholic solvent; g) evaporating the extraction solvent introduced in step a) until a residual concentration of extraction solvent of less than 1%, preferably less than 0.5%, is reached; h) leaving the mixture obtained in g) to stand for at least 6 hours, followed by filtration to a threshold of 5 μm, preferably 2 μm; The method of any one of claims 6 to 9, further comprising:
11. Cosmetic use of an alcoholic extract of lemon peel according to any one of claims 1 to 3 to limit / protect excessive desquamation and contribute to skin comfort.
Citation Information
Patent Citations
KR2012/0043288