EP3917492A1 - Novel cosmetic uses of a rose extract - Google Patents
Novel cosmetic uses of a rose extractInfo
- Publication number
- EP3917492A1 EP3917492A1 EP20712004.9A EP20712004A EP3917492A1 EP 3917492 A1 EP3917492 A1 EP 3917492A1 EP 20712004 A EP20712004 A EP 20712004A EP 3917492 A1 EP3917492 A1 EP 3917492A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- rose
- essential oil
- skin
- cosmetic
- water
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
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Classifications
-
- 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
- A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
- A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
-
- 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)
- A61K36/73—Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
- A61K36/738—Rosa (rose)
-
- 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
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
-
- 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
Definitions
- the present invention relates to the cosmetic field, in particular to cosmetic agents for combating the effects of stress and fatigue on the skin.
- the skin is the first barrier protecting the body from external aggressions.
- This organ is made up of several layers of tissue.
- the epidermis is made up of several cell layers of keratinocytes.
- basal layer containing, in particular, cutaneous stem cells
- spiny layer Stratum spinosum
- Stratum granulosum made up of several layers of polygonal cells
- the granular layer Stratum granulosum, comprising one to three layers of flattened cells containing cytoplasmic inclusions, the keratohyaline grains
- comeocytes which correspond to the terminal stage of differentiation of keratinocytes.
- the outermost cells of the stratum corneum are continuously shed and replaced by cells from a lower layer, in a process called desquamation.
- Cellular regeneration of the stratum corneum is based on a process of cell maturation in which the cells of the basal layer of the epidermis differentiate and gradually migrate through the different layers of the epidermis until they reach the stratum corneum below. the form of comeocytes.
- the skin is subjected to multiple attacks including exposure to tobacco, pollution, various chemicals, in particular volatile organic compounds, and climatic conditions such as wind, cold and heat.
- the skin must also cope with less direct sources of stress, but all equally deleterious, linked to the urban lifestyle, for example psychological stress linked to working conditions or to the family sphere, lack of sleep, food hygiene. bad or unbalanced, or the occasional alcohol intake. Women leading family life and work and young working people in urban areas are particularly exposed to these sources of stress and to chronic fatigue.
- Psychological stress occurs when the individual faces mental, physical or emotional pressure that goes beyond their ability to adapt. This stress is perceived by the brain and causes the secretion of stress hormones. Recent research has shown that the skin is both a stress perceiver and a target of stress responses.
- the Applicant has, itself, developed active agents aimed at combating the effects of pollution, for example anti-pollution agents and / or agents for protecting the skin against external aggressions such as the active Lanacityn TM PF, which combines an extract of Chrysanthellum Indicum and a marine polysaccharide, the active Exo-P TM comprising an exopolysaccharide extracted from Kopara and the active Detoxium TM, a salt of Nigari encapsulated in an Ionosome TM.
- active agents aimed at combating the effects of pollution, for example anti-pollution agents and / or agents for protecting the skin against external aggressions
- the active Lanacityn TM PF which combines an extract of Chrysanthellum Indicum and a marine polysaccharide
- the active Exo-P TM comprising an exopolysaccharide extracted from Kopara and the active Detoxium TM, a salt of Nigari encapsulated in an Ion
- the present invention relates to the cosmetic use of a rose water and a rose essential oil in combination for preventing or treating one or more skin effects of fatigue or exposure to stress.
- rose water and rose essential oil in combination are used as activating agents of an olfactory receptor expressed in the skin, preferably selected from the group consisting of OR10A6, OR2AG2, OR11H4 and their combinations.
- the skin effect (s) caused by fatigue or exposure to stress can be chosen from loss of skin radiance, dull complexion, blurred complexion, loss of uniformity of skin tone, drawn facial features , undereye bags at eye level, bags at eye level, swollen eyelids and their combinations.
- the stress suffered by the subject can be of any type.
- the essential oil of rose and rose water are used in combination as anti-fatigue agent, revitalizing agent, anti-skin agent, and / or agent for reviving the radiance of the complexion.
- Rose essential oil and rose water are generally obtained by a preparation process comprising a stage of hydrodistillation of the flowers of Rosa damascena.
- rose essential oil and rose water together have a methyl eugenol content of less than 500 ppm.
- rose water and rose essential oil are used in a “rose water / rose essential oil” mass ratio ranging from 1/4. to 4/1, preferably 2/3 to 3/2, and more preferably 1/1 to 3/2.
- rose water and rose essential oil are used as a mixture.
- This mixture can be characterized in that:
- the rose water present in the mixture is concentrated rose water
- the "rose water / rose essential oil" mass ratio is within a range of 2/3 to 3/2, preferably from 0.7 to 1.4, or from 1.1 to 1.4 and
- - rose water and rose essential oil are preferably obtained by a process comprising a stage of hydrodistillation of Damascus rose flowers.
- the mixture can be combined, ie dispersed or dissolved, in a cosmetically acceptable vehicle, preferably pentylene glycol.
- rose water and rose essential oil in combination are used in combination with an additional active cosmetic agent, preferably selected from the group consisting of anti-wrinkle agents, anti-aging agents, antioxidants. , moisturizing agents, soothing agents, anti-redness agents, decongestants, exfoliating or exfoliating agents, matifying agents, sebum-regulating agents, lightening active agents, anti-dark spots or anti-skin agents, tightening agents, anti-pollution active agents, filters and sunscreens, and their combinations.
- an additional active cosmetic agent preferably selected from the group consisting of anti-wrinkle agents, anti-aging agents, antioxidants. , moisturizing agents, soothing agents, anti-redness agents, decongestants, exfoliating or exfoliating agents, matifying agents, sebum-regulating agents, lightening active agents, anti-dark spots or anti-skin agents, tightening agents, anti-pollution active agents, filters and sunscreens, and their combinations.
- the combination of rose essential oil and rose water can be included in
- It may be a cosmetic composition chosen from the group consisting of aqueous solutions, hydroalcoholic solutions, oil-in-water (O / W) or water-in-oil (W / O) emulsions or multiple (triple : E / O / E or O / E / H), nanoemulsions, in particular O / W nanoemulsions, the drop size of which is less than 100nm, aqueous gels, or dispersions of a fatty phase in an aqueous phase using spherules, suspensions, preferably in aqueous or hydroalcoholic media, suspensions of liposomes, powders, lotions, milks, creams, ointments, gels, foams, and ointments.
- a cosmetic composition chosen from the group consisting of aqueous solutions, hydroalcoholic solutions, oil-in-water (O / W) or water-in-oil (W / O) emulsions or multiple (triple : E
- the cosmetic composition can be chosen from the group consisting of a serum, a lotion, a day cream, a night cream, an eye care product, a gel-cream, a foundation, and a spray for the skin. body
- the invention relates to a cosmetic composition for preventing or treating the cutaneous effects caused by fatigue or by exposure to stress, said composition comprising from 0.0001% to 10% by weight of a mixture of rose water and rose essential oil.
- a subject of the invention is also a precursor composition for the preparation of a cosmetic composition, comprising:
- the invention relates to a cosmetic process for preventing or treating one or more skin effects of fatigue or exposure to stress in an individual, said process comprising the application of a cosmetically effective amount of an essential oil of rose and a rose water on the skin of the individual, preferably on the face.
- the uses and methods according to the invention are preferably intended for subjects under the age of 45, in particular women under 45, preferably 25 to 40 years.
- the rose extract is used as an agonist of an olfactory receptor expressed at the level of the skin chosen from the group consisting of OR10A6, OR2AG2, OR11H4 and theirs. combinations.
- a subject of the invention is also the cosmetic use of an agonist of an olfactory receptor chosen from the group consisting of OR10A6, OR2AG2, OR11H4 and their combinations for preventing or treating one or more cutaneous effects of fatigue or fatigue. exposure to stress, said agonist being applied through the skin. DESCRIPTION OF FIGURES
- Figure 1 shows the results of the ex vivo study performed on skin explants. This study is described in Example 1 below.
- Figures 1A-C show the variations in immunolabeling of loricrin, gH2AC and G6pDH, respectively, obtained for histological sections prepared on day 9.
- the groups studied are: untreated explants (control), explants treated with F ′′ Extract ”(combination of rose essential oil / rose water), explants treated with epinephrine and explants treated with epinephrine and F“ Extract ”. Unlike epinephrine, F "Extract" does not significantly alter the immunostaining of the various markers studied.
- F "Extract” counteracts the effects of epinephrine and maintains immunolabelling for the various markers studied at levels equivalent to those obtained for the group of untreated explants. The results are expressed in% relative to the data obtained for the untreated group.
- Figure 1D shows the evolution of melanin production in skin explants in the different experiment groups. The Extract is seen to prevent the overproduction of melanin induced by epinephrine.
- Figure 2 shows the results obtained in the in vitro study of Example 2.
- the "Extract” inhibits the production of melanin by melanocytes induced by ⁇ -MSH. The observed effect is dose-dependent. The results are expressed as a percentage relative to the Control group (cells exposed to a-MSH without treatment with F "Extract”).
- Figure 3 shows the results of the clinical trial presented in Example 7.
- Figures 3A, 3B and 3C show the variations in brightness, intensity of pigmentation and skin lightening after 7 days (D7-D0) or 28 days of. treatment compared to T0 (D28-D0), for the placebo cream (cream A) and the cream containing F "Extract” at 1% (cream B).
- Cream B A marked improvement in the appearance of the skin is seen in the group of women treated with the cream according to the invention (Cream B).
- FIG. 4 shows the results of the clinical trial of Example 8 aimed at evaluating the effect of the combination "rose water and rose essential oil” on dark circles.
- FIG. 4 shows that gel B containing F “Extract” at 1% makes it possible to significantly reduce the extent and color of dark circles, and this from 7 days of application, in comparison with a placebo gel A.
- FIG. 5 shows the percentage of inhibition on tyrosinase exerted by the combination “rose water and essential oil” according to the invention (“Active”), essential rose oil alone and concentrated rose water alone.
- Figure 6 shows the presence of OR10A6, OR11H4 and OR2AG2 on skin explant by immunohistochemistry.
- the rose is the flower of the rosebush, a shrub of the genus Rosa and of the Rosaceae family. It is one of the most widely cultivated plants in the world and it ranks number one in the flower market. Rose extracts find different industrial applications. Rose essential oil, also called rose essence, is obtained by hydrodistillation of the petals of the flower and is particularly appreciated for the composition of perfumes. It is also used in the composition of many cosmetic products, mainly as an excipient to provide a perfumed note. It can also be used, as a cosmetic active, in particular as an anti-aging agent as proposed in patent FR 2 948 023.
- Rose water which generally corresponds to the hydrosol obtained during the hydrodistillation, is used as a flavoring in the food industry but also in cosmetics, in particular in make-up removing compositions.
- the Applicant has shown that the combined use of rose water and essential rose oil makes it possible to protect the skin against the harmful effects of stress and fatigue.
- rose water and rose essential oil used in combination help protect skin cells from the effects of epinephrine, a hormone that is secreted under stress.
- the Applicant has shown that the use of a new active ingredient combining rose water and essential oil of rose inhibits the production of melanin in melanocytes, a production which is moreover induced under stress conditions (Example 2).
- This active agent has also been shown to prevent overactivation of metabolism and cell differentiation as well as DNA damage, at the level of the epidermis of human skin explants exposed to epinephrine (Example 1).
- this new active ingredient combining both a rose essential oil and a rose water is a more powerful tyrosinase inhibitor than rose essential oil alone and is capable of inhibiting the production of melanin induced by 1 ' a-MSH more effectively than rose water alone:
- the new active agent according to the invention decreases the disturbance of melanogenesis induced by stress more strongly than do the essential oil of rose and water. rose taken separately (Examples 3 and 4).
- the Applicant has shown that the essential oil of rose and rose water in combination work synergistically to prevent and treat the effects of stress on the skin.
- the Applicant believes that the anti-stress effect of the active agent according to the invention would be, at least partially, linked to the activation of certain olfactory receptors expressed by the keratinocytes, this activation being able to lead to inactivation of the 2-adrenergic receptor and desensitization of cells to epinephrine.
- the Applicant has demonstrated, for the first time, the expression of olfactory receptors OR10A6, OR2AG2 and OR11H4 in the keratinocytes obtained from human skin samples, and in the epidermis of human skin explants.
- the active agent according to the invention as well as 2-phenylethanol, a compound present in the active agent, are capable of activating these receptors.
- the active agent according to the invention also makes it possible to counteract the decrease in the expression of OR2AG2 in skin explants exposed to epinephrine, which tends to show that the protective role of the “extract The stress induced by epinephrine is mediated, at least in part, by a biological pathway involving OR2AG2 (Example 5).
- rose extracts especially rose water and rose essential oil in combination, help prevent and treat the skin effects of stress as well as the skin signs of fatigue.
- the present invention relates to the cosmetic, non-therapeutic use of a rose extract, in particular as an anti-fatigue, anti-fatigue or anti-stress agent. More generally, rose extract is used to treat, prevent, or reduce a cutaneous effect of fatigue or stress. Rose extract is typically an extract obtained from the flowers or petals of a rose. The extract is preferably chosen from rose water, rose essential oil and combinations thereof.
- the invention relates to the cosmetic, non-therapeutic use of a rose water and a rose essential oil in combination for treating, preventing, or reducing a cutaneous effect of fatigue or of stress.
- rose water and rose essential oil are used in combination, for example in the form of a mixture, which may further comprise a pharmaceutically acceptable carrier.
- the cosmetic combination according to the invention can in particular be included in a cosmetic composition for the implementation of the cosmetic uses and processes according to the invention, as is detailed below.
- the essential oil of rose and rose water are preferably obtained by a process comprising a stage of hydrodistillation or of steam distillation of the rose flowers.
- Rose essential oil contains liposo fad volatile compounds from hydro distillation or the distillation of rose flowers while rose water contains water soluble volatile compounds.
- the essential oil and rose water are obtained by hydrodistillation.
- Hydrodistillation is a process of extracting volatile compounds present in the plant matrix, that is to say in rose flowers by steam entrainment.
- Hydrodistillation can be performed from a plant matrix consisting of whole fresh flowers, flower petals, or crushed flowers. Typically, the plant matrix is suspended in water and is heated. The vapor which is released entrains the volatile compounds which are condensed and then collected in a settling vessel. It is possible to use a still, or any distillation device comprising a distillation column, a condenser and a decanter.
- Rose water and rose essential oil can be obtained directly from the fractions obtained from the hydrodistillation of rose flowers. Where appropriate, the aqueous fractions and organic obtained from the hydrodistillation can undergo one or more treatments in order to obtain the desired rose water and rose essential oil, respectively.
- these treatments include, in particular, chromatography, concentration, extraction or distillation steps.
- the aqueous fraction obtained from hydrodistillation can undergo a concentration step by adsorption-desorption making it possible to recover only the volatile compounds of interest and to remove the water.
- a concentration step can be carried out on a suitable resin, typically a hydrophobic resin capable of retaining the volatile organic compounds present in rose water.
- the volatile organic compounds are then recovered using a suitable solvent, which is then removed to obtain concentrated rose water.
- This concentrated rose water can then be mixed with the essential oil to obtain an active ingredient comprising all the volatile compounds of the rose.
- the aqueous fraction and the organic fraction resulting from the hydrodistillation can undergo an additional step allowing them to be refined.
- the aqueous fraction can undergo an additional distillation step in order to collect the residual essential oil fraction potentially present in the aqueous phase.
- the organic phase can undergo rectification, namely vacuum distillation.
- the organic fraction and / or the aqueous fraction resulting from the hydrodistillation can undergo an additional distillation step, for example a fractional distillation step, in order to remove the methyl eugenol.
- the essential oil of rose and / or rose water comprises less than 0.05%, preferably less than 500 ppm of methyl eugenol.
- Rose essential oil and rose water can be prepared from rose flowers of different species.
- the species of interest include, but are not limited to, Rosa centifolia, Rosa alba, Rosa rugosa, Rosa gallica or Rosa damascena.
- Rosa damascena Mill Commonly known as Damascus rose.
- the rose extract in particular the combination of rose water and rose essential oil, is applied to the skin.
- rose extract preferably corresponds to the combination of rose water and rose essential oil.
- the invention relates to the use of rose water and rose oil in combination.
- “use in combination” means that rose water and rose essential oil can be applied to the skin simultaneously or separately.
- rose water can be applied to the skin and some minutes later, for example 1 to 30 minutes later, preferably immediately after, the essential oil of rose is applied, or vice versa.
- rose essential oil and rose water are used simultaneously.
- rose water and rose essential oil are used in the form of a mixture and / or incorporated in a cosmetic composition.
- the “rose water / rose essential oil” mass ratio in the mixture or in the cosmetic composition is typically within a range going from 1/4 to 4/1, for example from 2/3 to 3/2 or else from 1/1 to 3/2.
- the “rose water / rose essential oil” mass ratio is within a range ranging from 0.7 to 1.4, preferably from 1.1 to 1.4.
- the rose extract according to the invention is a mixture of rose water and rose essential oil in which:
- the rose water present in the mixture is concentrated rose water
- the rose water / rose essential oil mass ratio is in a range from 0.7 to 1.4, preferably from 1.1 to 1.4,
- - rose water and rose essential oil are preferably obtained by a process comprising a step of hydrodistillation of rose flowers such as Damask rose flowers.
- concentrated rose water is understood to mean rose water in which at least part of the water (that is to say at least 50%, preferably at least 95% or even 99.9% and even 100 %) present at the end of the hydrodistillation or initial distillation stage has been eliminated.
- rose water obtained by hydrodistillation or distillation can be concentrated by a concentration step, preferably an adsorption-desorption step on a hydrophobic resin.
- the mixture of rose essential oil comprises less than 0.05%, preferably less than 500 ppm of methyl eugenol.
- a methyl eugenol content can be obtained by subjecting the mixture and / or the essential oil of rose to a fractional distillation step.
- rose water and rose essential oil together (i.e. in combination, and preferably as a mixture) comprise 2-phenylethanol, nerol, citronellol , and geraniol.
- 2-phenylethanol and citronellol together represent from 50% to 90% by weight based on the weight of the combination, preferably the mixture of rosewater and rose essential oil.
- the 2-phenylethanol can represent at least 40%, preferably at least 50%, and up to 70%, by weight relative to the weight of the combination, preferably of the mixture of rose water and essential oil of pink.
- citronellol can represent at least 10%, and up to 30%, by weight of the combination or of said mixture.
- rose water and rose essential oil together include (i.e. as a combination or mixture) of:
- the percentages being expressed by weight relative to the total weight of the combination, preferably of the mixture of rose water and rose essential oil ("rose water” weight plus “rose essential oil” weight).
- the composition of volatile compounds of the mixture or of the combination according to the invention is determined by gas chromatography, preferably with detection by mass spectrometry and / or UV absorption.
- the Applicant has shown that the combined application of rose water and a rose essential oil on the skin makes it possible to prevent and treat the cutaneous effects of stress and fatigue. More generally, the combined use of a rose water and an essential oil of rose, for example in the form of a mixture and / or incorporated separately in a cosmetic composition, makes it possible to combat the visible effects of stress. or fatigue in the skin.
- skin and “cutaneous” refer to any part of the skin of the human body, in particular the skin of the face, including the lips and eyelids, the neck, and the skin of the human body. hands. Preferably, it is the skin on the face, including the eye area and the lip area, and on the neck.
- skin signs or effects is understood to mean any alteration, damage or non-pathological modification of the visual appearance or of the mechanical properties of the skin.
- skin signs or effects are caused by, or associated with, fatigue or stress.
- preventing a sign or an effect is understood to mean the fact of delaying or preventing the appearance of said sign or effect on the skin.
- treating a sign or an effect is meant the fact of reducing, attenuating, fading, correcting or slowing the development of said sign or effect on the skin.
- stress or exposure to stress is meant the exposure of the individual to any type of stress, whether of a psychological, environmental or physical nature, which may lead, directly or indirectly, to an alteration or modification, not pathological, visual or mechanical properties of the skin.
- psychological stress resulting from stressful living or working conditions such as overwork, or stressful work events (such as exam preparation, public presentations), psychological pressures at work or in the private sphere, or even emotional overloads due, for example, to family problems.
- VOCs volatile organic compounds
- Stress can also be linked to lifestyle, in particular an unbalanced diet, and the consumption of foods comprising additives or hyper-processed foods, exposure or consumption of tobacco and / or alcohol, a lack of of sleep (for example less than 8 hours, preferably less than 6 hours per night), a shifted work rhythm (for example night work), jet lag (jet-lag) or even commuting times home- long desk.
- lifestyle in particular an unbalanced diet, and the consumption of foods comprising additives or hyper-processed foods, exposure or consumption of tobacco and / or alcohol, a lack of of sleep (for example less than 8 hours, preferably less than 6 hours per night), a shifted work rhythm (for example night work), jet lag (jet-lag) or even commuting times home- long desk.
- stress is caused by the urban lifestyle. It may in particular be chronic stress, namely stress to which the individual is exposed continuously or repeatedly, for several days (eg at least 1, 2, 3, 4, 5, 6 or 7 days), several weeks (eg at least 1, 2, 3, 4, 5, 6, 7 or 8 weeks) or even several months (eg at least 1, 2, 3, 4, 5, or 6 months).
- chronic stress namely stress to which the individual is exposed continuously or repeatedly, for several days (eg at least 1, 2, 3, 4, 5, 6 or 7 days), several weeks (eg at least 1, 2, 3, 4, 5, 6, 7 or 8 weeks) or even several months (eg at least 1, 2, 3, 4, 5, or 6 months).
- the skin is directly exposed to stress.
- it is generally an environmental stress such as pollution, tobacco or extreme climatic conditions such as heat, cold or wind.
- the subject is exposed to one or more stresses chosen from the group consisting of: tobacco, alcohol, pollution, lack of sleep, psychological stress, unbalanced diet, dietary exposure to additives or hyper-processed foods, and exposure to high or low temperatures.
- the subject is exposed to one or more stresses selected from the group consisting of tobacco, pollution, lack of sleep, psychological stress, and an unbalanced diet.
- the skin signs caused by fatigue or exposure to stress include, but are not limited to, an alteration in skin tone, in particular a dull complexion, a dull complexion, a loss of skin tone. radiance or loss of uniformity of skin tone, irregularities in skin pigmentation including the appearance of pigment spots, drawn out facial features, the appearance of bags and / or dark circles in the eyes, swelling eyelids and their combinations.
- the extract of rose preferably rose water and essential oil of rose in combination, can / vent be used (es), for at least one (1, 2 , 3, 4, 5, 6, 7, 8, 9 or 10) for the following purposes:
- the present invention relates to the use of a rose extract, preferably a rose water and a rose essential oil in combination, as an agent. anti-fatigue, anti-fatigue agent, anti-stress agent, protective agent against the effects of stress, soothing agent, or skin revitalizing agent, in particular in an individual exposed to stress or fatigue.
- the rose extract according to the invention preferably rose water and a rose essential oil in combination, can also be used as a lightening agent for the complexion or depigmenting agent, in particular in an individual exposed to stress. or fatigue.
- the combined use of rose water and rose essential oil helps prevent the effects of epinephrine, the stress hormone, on the skin cells, especially of the epidermis.
- Rose water and rose essential oil in combination thus make it possible to fight against the overactivation of metabolism and of cell differentiation induced by stress, in particular the production of epinephrine. It has also been shown that rose water and rose essential oil used in combination prevent the overproduction of melanin by melanocytes induced by a-MSH.
- a subject of the invention is also the cosmetic use of a rose extract, preferably of a rose water and of a rose essential oil in combination, in an individual exposed to stress and / or to fatigue, for:
- rose water and rose essential oil are used in combination to regulate the expression of loricrin and G6DPH in the cells of the epidermis of an individual exposed to stress.
- the essential oil of rose and rose water are used as modulators, preferably as activators or agonists of an olfactory receptor expressed by the cells of the skin, preferably chosen from among OR10A6, OR2AG2 and OR11H4.
- rose essential oil and rose water are used as a modulator of a stress response cell signaling pathway involving an olfactory receptor, preferably chosen from OR10A6, OR2AG2 and OR11H4.
- an olfactory receptor preferably chosen from OR10A6, OR2AG2 and OR11H4.
- the individuals targeted by the present invention can be of any age and gender. However, in a preferred embodiment, it is an individual who is less than 45 years old and preferably more than 20 years old. It could be, for example, a woman or a man between 25 and 45 years old. Preferably a woman between the ages of 25 and 40.
- rose water and rose essential oil are used in combination with one or more active agent (s) with additional cosmetic effect.
- active ingredient with cosmetic effect is understood to mean a compound capable of exerting at least one cosmetic effect on the skin or its appendages.
- cosmetic effect is understood to mean any non-therapeutic effect intended to modify and / or improve the visual appearance and the mechanical properties of the skin or of the mucous membranes such as the lips, to protect them from external aggressions (sun, wind, humidity, etc. dryness, chemicals), to prevent and / or correct phenomena related to their aging, or to prevent or treat the effects caused by stress or fatigue on the skin.
- Such agents include, among others, anti-wrinkle agents, anti-aging agents, antioxidants, moisturizers, soothing agents, anti-redness agents, decongestants, exfoliating or exfoliating agents, matifying agents, sebum-regulating agents, lightening active agents, anti-dark spots, anti-skin or anti-puffiness agents, anti-pollution active agents, tightening agents, sun filters and screens, and their combinations.
- rose essential oil and rose water are generally present as a cosmetic agent in a cosmetic composition.
- rose essential oil and rose water are typically applied to the skin of the individual to be treated through a cosmetic composition.
- Rose essential oil and rose water can together (i.e. as a combination, preferably as a mixture) represent 0.0001% to 10%, preferably 0.0001 % to 5% by weight, for example from 0.0005% to 1% by weight of the cosmetic composition, or alternatively from 0.0005% to 0.01% by weight of the total cosmetic composition.
- said cosmetic composition comprises:
- the cosmetically acceptable excipient (s) present in the composition can be chosen from diluting agents, dispersing agents, gelling agents, emollients, vectoring agents such as polycationic polymers or phospholipids, gums, resins, etc.
- solvents in particular lower alcohols, in particular ethanol, isopropanol, dipropylene glycol, butylene glycol, propanediol, glycerin, sorbitol, and propylene glycol
- fillers such as modified and polymerized starches, dioxide titanium, or a metal stearate, preservatives, essential oils, pearlescent agents, colorants, odor absorbers, pH regulating agents or neutralizing agents, lubricating agents, thickening agents, surfactants including anionic, cationic, amphoteric or nonionic surfactants, humectants, wetting agents, dispersing agents, perfumes, pi organic or even mineral gments such as iron oxides, oily agents such as oils or fats of plant origin, fats of animal origin, synthetic oils such as petrolatum, silicone oils (cyclomethicone), esters of fatty alcohol, fluorinated oils, waxes, modified clays, bentones, fatty acid metal salts, silica, polyethylenes
- the additional cosmetic active ingredient (s) can be chosen from the group consisting of anti-wrinkle agents, anti-aging agents, antioxidants, moisturizers, soothing agents, anti-redness agents, decongestants, exfoliating or exfoliating agents. , matifying agents, sebum-regulating agents, lightening active agents, anti-dark spots, sunscreens and filters, and their combinations.
- the cosmetic composition can comprise tocopherols, and / or plant extracts such as extracts of flax seeds, extracts of exopolysaccharides of Vibrio, peptides such as trifluoroacetyl tripeptide-2.
- the cosmetic composition can comprise an active agent chosen from an anti-wrinkle agent, an anti-redness agent, an antioxidant agent, a moisturizing agent, a soothing agent, a sebum-regulating agent, an anti-stain or lightening agent, an agent. tensor, an anti-pollution active, an anti-skin or anti-pocket agent, a filter or a sunscreen, and their combinations.
- an anti-pollution agent mention may be made of extracts of Chrysanthellum Indicum, polysaccharides, in particular marine polysaccharides obtained from an Alteromonas fermentation medium and Nigari salts.
- anticeme agents By way of example of anticeme agents, mention may be made of extracts of Chrysantellum Indicum or also of extracts and sulphated polysaccharides of algae, in particular of Ascophyllum nodosum or of Asparagopsis Armata.
- moisturizing agents By way of example of moisturizing agents, mention may be made of urea, pidolic acid (PCA) and its derivatives, in particular its salts such as arginine PCA, chitosan PCA, its copper salts (Copper PCA) , magnesium (magnesium PCA), sodium (sodium PCA) or zinc, ethylhexyl PCA, calcium gluconate, hyaluronic acid and its salts and other glycosaminoglycans, frucose, glucose, isomaltose, lactose, trehalose, polydextrose, sucrose (Sucrose), maltitol, mannitol, sorbitol, xylitol and other carbohydrates and derivatives, polyethylene glycols such as PEG-7, PEG-8, PEG- 10, PEG-12 or PEG-14, glycerin, propylene glycol, butylene glycol, betaine, citrulline, collagen and
- anti-aging agents By way of example of anti-aging agents, mention may be made of ascorbic acid and its derivatives such as magnesium ascorbyl phosphate, glycosaminoglycans and their derivatives, Cyathea polysaccharides, collagen, extracts of flax seeds. (Linum usitatissimum), peptides such as Caprooyl-Tetrapeptide-3 and trifluoroacetyl tripeptide-2, extracts of Polygonum aviculare, extracts of brown algae, in particular of Ascophyllum nodosum, extracts of ferns, in particular of Cyathea cumingii.
- ascorbic acid and its derivatives such as magnesium ascorbyl phosphate, glycosaminoglycans and their derivatives, Cyathea polysaccharides, collagen, extracts of flax seeds. (Linum usitatissimum), peptides such as Caprooyl-Tetrapeptide-3 and trifluoroacety
- soothing agents there may be mentioned allantoin, extracts of aloe, birch (for example Betula alba), fireweed (Epilobium angustifolium), chestnut (for example Castenea sativa), blueberry (e.g. Centaurea cyanus), centella (e.g. Centella asiatica), horsetail (e.g. Equisetum arvense), fennel (e.g. Foeniculum vulgare), witch hazel (e.g. Hamamelis virginiana), ivy (e.g. Hedera helix), habiscus sabdariffa, lily (e.g. Lilium candidum), mallow (e.g.
- Malva sylvestris Malva sylvestris
- lemon balm e.g. Melissa officinalis
- skullcap e.g. Scutellaria baicalensis
- mimosa e.g. Mimosa tenuiflora
- cinquefoil e.g. Potentilla erecta
- an oligosaccharide extract or an oligosaccharide for example of flax, peptides such as palmitoyl tripeptide-8, extracts of polysaccharides, in particular extracts of exopolysaccharides obtained from the Alteromonas fermentation medium and combinations thereof.
- antioxidants examples include HMR (hydroxy methyl resorcinol), ascorbic acid and its derivatives, vitamin B9, histidine hydrochloride, or an extract of fireweed (Epilobium augustifoliuwi).
- HMR hydroxy methyl resorcinol
- ascorbic acid and its derivatives examples include ascorbic acid and its derivatives, vitamin B9, histidine hydrochloride, or an extract of fireweed (Epilobium augustifoliuwi).
- the active ingredients with an antioxidant effect and of vitamin type are generally used in a percentage by mass of at least 1% relative to the total weight of the cosmetic composition.
- sebum-regulating agents By way of example of sebum-regulating agents, mention may be made of flax lignans, rice powder, zinc gluconate, sarcosine, an extract of Cinnamomum zeylanicum bark, an extract of avocado, an extract of Backhousia citriodora and combinations of these.
- anti-redness agents mention may be made of saponins, flavonoids, ruscogenins, esculosides, and extracts containing them, for example extracts of Ruscus, as well as certain essential oils, for example of lavender or rosemary. .
- extracts such as liquorice (Glycyrrhyza glabra), jackfruit extract (Artocarpus heterophyllus), extracts of Rumex (R.occidentalis), plant extracts belonging to of the citrus genus, resveratrol, peptides such as oligopeptide-68, nonapeptide-1, kojic acid, magnesium ascorbyl phosphate and combinations thereof.
- the rose extract preferably the combination of rose water and essential rose oil according to the invention, in particular the mixture according to the invention, can be incorporated into any type of cosmetic composition.
- it is a cosmetic composition having a form suitable for topical administration, in particular suitable for application to the skin.
- Said cosmetic composition may be in the form of aqueous, hydroalcoholic solutions, oil-in-water (O / W) or water-in-oil (W / O) or multiple (triple: W / O / W or H) emulsions. / W / O), nanoemulsions, in particular O / W nanoemulsions, the drop size of which is less than 100nm, aqueous gels, dispersions or even a powder.
- the cosmetic composition according to the invention can be in the form of a lotion, a milk, a cream, an ointment, a gel, a foam, a solution, an ointment. More generally, the composition according to the invention can also be in the form of a cosmetic product of any type.
- It may be a cosmetic care or a make-up or personal hygiene product, for example a lotion, a milk, a serum, an aqueous or oily gel, an emulsion, a cream, a gel-cream , a treatment water, an ointment, a balm, a foundation, a spray, an eye shadow, a stick, a lipstick, a gloss, a mousse, a deodorant, a nourishing mask, a spray, in particular for the bust and the face, a shower gel, and an exfoliating or exfoliating product.
- a cosmetic care or a make-up or personal hygiene product for example a lotion, a milk, a serum, an aqueous or oily gel, an emulsion, a cream, a gel-cream , a treatment water, an ointment, a balm, a foundation, a spray, an eye shadow, a stick, a lipstick, a gloss, a mousse, a deodorant,
- the combination in particular the mixture, of rose water and essential oil of rose according to the invention can be present as an anti-fatigue or anti-stress agent in a day cream.
- said combination can be present in an anti-fatigue eye treatment as an anticeme agent.
- Said combination can also be present in a conditioning serum as an agent to protect or repair damage related to environmental stress.
- the combination according to the invention can be present in a night cream as an agent for promoting cell recovery in the epidermis following exposure to stress.
- a subject of the invention is also the use of a cosmetic composition comprising a rose essential oil and a rose water as cosmetic agents for treating or preventing a cutaneous sign of fatigue or of exposure to stress.
- rose essential oil and rose water are present in the composition as modulators, preferably as agonists of an odor receptor expressed by skin cells, preferably selected from OR10A6, OR2AG2 and OR11H4.
- An additional object according to the invention is a cosmetic process for treating or preventing a cutaneous sign of fatigue or exposure to stress in an individual, comprising the administration in combination of a cosmetically acceptable amount of an extract of pink, preferably topically, to said individual.
- the rose extract can be chosen from rose water, rose essential oil and their combinations.
- it is rose water and rose essential oil.
- the application is typically carried out on the skin to be treated, for example on the face, in particular around the eyes.
- the combination of water and essential oil of rose is present in a cosmetic composition as described above, and is therefore applied in the form of a cosmetic composition, for example in the form of a cream.
- the aim of the cosmetic process according to the invention is to treat or prevent one or more skin effects of stress and fatigue, preferably chosen from an alteration of the skin tone, in particular a dull complexion, a dull complexion, a loss of skin tone. 'radiance of the complexion or a loss of uniformity of the complexion, in particular the appearance of pigment spots, drawn facial features, the appearance of bags and / or dark circles in the eyes.
- the method according to the invention can make it possible to obtain any of the following effects in an individual exposed to stress or fatigue:
- the dose to be administered and the frequency of administration of the combination according to the invention vary as a function of the desired cosmetic effect, of the characteristics of the individual, in particular of his sex. , age and skin type.
- rose extract in particular rose water and rose essential oil in combination
- the patient can apply a dose of 1 g to 2 g of cosmetic composition on his face, morning and evening.
- a subject of the invention is also a cosmetic composition comprising a combination of rose water and rose essential oil.
- said cosmetic composition comprises:
- said cosmetic composition comprises - from 0.0001% to 0.01% of a combination of rose water and rose essential oil
- the rose water / rose essential oil mass ratio in the cosmetic composition is as described above, in particular within a range going from 1/4 to 4/1, for example from 2/3 to 3/2.
- the cosmetic composition can be of any type, as explained previously.
- the cosmetic composition is for preventing or treating a skin sign of fatigue or exposure to stress, in particular environmental stress.
- rose water and rose essential oil are used as a mixture.
- this mixture can be characterized in particular in that:
- the rose water present in the mixture is concentrated rose water
- the rose water / rose essential oil mass ratio is in a range from 0.7 to 1.4, preferably from 1.1 to 1.4,
- the mixture comprises less than 0.05%, preferably less than 500 ppm of methyl eugenol.
- This mixture can be combined with a cosmetically acceptable vehicle.
- the cosmetically acceptable vehicle can be of any type.
- the cosmetically acceptable vehicle can be chosen from the group consisting of water, solvents in particular lower alcohols, in particular ethanol, isopropanol, dipropylene glycol, butylene glycol, propanediol, glycerin, sorbitol, propylene glycol and pentylene glycol, an aqueous solution, or a mixture of these vehicles.
- the cosmetically acceptable vehicle may be pentylene glycol.
- One or more cosmetically acceptable excipients may be present.
- Said excipient (s) can be chosen from the group consisting of stabilizers, preservatives, pH agents, vectoring agents, bulking agents, hydrotropes, in particular surfactants.
- the vectoring agent can be chosen from the group consisting of micelles, liposomes, including unilamellar or multilamellar liposomes, niosomes, ethosomes, lamellar systems, nanosomes, lipid or polymeric vesicles, nanospheres, micro or nano-particles of natural or non-natural polymers, hydrogels.
- liposomes and of lamellar systems for the implementation of the present invention are described, among others, in French patent applications No. 1358589 and No. 1262303 filed in the name of the Applicant.
- the mixture of rose water and essential oil of rose associated with the cosmetically acceptable vehicle and with or more optional excipients as defined above form a so-called “precursor” cosmetic composition intended to be incorporated into a cosmetic product. .
- an additional object according to the invention is a "precursor" cosmetic composition.
- Such a “precursor” cosmetic composition generally comprises from 0.01% to 10%, for example from 0.1% to 2% of a mixture of essential rose oil and rose water, and from 90% to 99.99%, for example from 98% to 99.9% of a cosmetically acceptable vehicle such as pentylene glycol, the percentages being expressed by weight relative to the total weight of the composition.
- the additional cosmetic excipient (s) may represent from 0% to 10%, in particular from 0% to 2% by weight of the “precursor” cosmetic composition.
- a subject of the present invention is also the use of said "precursor" composition for the preparation of a cosmetic composition. It goes without saying that said final cosmetic composition is particularly suitable for the implementation of any of the cosmetic uses according to the invention, and can exhibit any of the characteristics described above.
- the precursor cosmetic composition comprises:
- the "precursor" composition comprises less than 20 ppm, preferably less than 10 ppm of methyl eugenol.
- the “precursor” composition comprises from 0.1% to 2% rose water and rose essential oil, and from 98% to 99.9% of pentylene glycol.
- the “precursor” composition according to the invention generally represents from 0.01% to 10%, preferably from 0.1% to 5% by weight of the final cosmetic composition.
- Said cosmetic composition can be obtained by mixing a "precursor" composition according to the invention with one or more cosmetically excipients and / or with one or more additional active ingredients with a cosmetic effect.
- the Applicant has shown for the first time that the olfactory receptors OR10A6, OR2AG2 and OR11H4 are expressed in the keratinocytes of the skin in humans.
- the Applicant has shown that the rose extract according to the invention, in particular an extract combining an essential oil of rose and a rose water, is an agonist of these receptors.
- the Applicant has also shown that 2-phenylethanol, a compound present in the active agent according to the invention, activates these receptors.
- the Applicant is of the opinion that the anti-stress effect of the active agent according to the invention could, at least partially, result from an activation of the olfactory receptor OR10A6 and / or OR2AG2 and / or OR11H4.
- an additional object according to the invention is the use of an agonist of an olfactory receptor chosen from OR10A6, OR2AG2 and OR11H4 as a cosmetic agent.
- OR10A6 olfactory receptor called as such according to conventional nomenclature (see https://genome.weizmann.ac.il/horde), is also referred to in the literature under the name of “Olfactory receptor 10A6”, with the number UniProt access: Q8NH74 and GenelD access number: 390093.
- OR2AG2 olfactory receptor called as such according to conventional nomenclature (see https://genome.weizmann.ac.il/horde), is also referred to in the literature under the name of “Olfactory receptor 2AG2”, under the number UniProt access: A6NM03 and GenelD access number: 338755.
- OR11H4 olfactory receptor called as such according to the classical nomenclature (see https://genome.weizmann.ac.il/horde), is also referred to in the literature under the name of “Olfactory receptor 11H4”, under the number of UniProt access: Q8NGC9 and GenelD access number: 390442.
- the object of the invention is the use of an agonist of an olfactory receptor chosen from OR10A6, OR2AG2 and OR11H4 to prevent or treat one or several skin effects of fatigue or exposure to stress.
- an agonist of an olfactory receptor chosen from OR10A6, OR2AG2 and OR11H4 to prevent or treat one or several skin effects of fatigue or exposure to stress.
- the cutaneous effects of fatigue or exposure to stress are as described above.
- This agonist can be of any type.
- it can be an antibody or a fragment of the binding site thereof, an aptamer, a synthetic chemical molecule, a natural molecule, plant extracts and combinations thereof.
- It may in particular be a rose extract as described above, for example a combination of rose water and a rose essential oil as described above, or 2-phenylethanol.
- it can be any molecule or combination of molecules for which an agonist effect vis-à-vis these receptors is shown.
- Such molecules or combinations can in particular be identified via an activity test as illustrated in Example 3. This test can aim to determine whether a candidate molecule or combination is capable of activating the olfactory receptor of interest co-transfected. with a CRE-Luc reporter vector for the cAMP gene in a cell of interest, the activation of the receptor being determined by measuring the cAMP generated in the presence of different concentrations of the molecule or of the combination tested.
- a molecule or a combination of molecules can be considered as an agonist of interest if it exhibits an EC50, in this test, of less than 10 mM, preferably less than 1 mM or even less than 500 mM.
- Candidate molecules and combinations of interest include, but are not limited to, odorous molecules and their combinations, these molecules being derived in particular from essential plant oils, plant waters such as floral waters, and plant extracts. obtained for example by extraction with an organic solvent.
- said agonist is chosen from an odorous molecule or an essential oil other than 2-phenylethanol or a rose extract.
- the agonist according to the invention is typically administered topically, that is to say applied to a region of the skin of the subject to be treated such as the face, in particular the eye area, and the neck.
- Said agonist can be formulated in cosmetic compositions as described above for the rose extract according to the invention.
- the “Active” composition corresponds to a mixture of concentrated rose water and essential rose oil obtained by a process comprising a step of hydrodistillation of the flowers of Rosa damascena.
- fresh Damascus rose flowers have been processed by hydrodistillation.
- the organic fraction, corresponding to the essential oil, and the aqueous phase, corresponding to a crude rose water, were collected.
- the aqueous phase has undergone a second distillation in order to be refined.
- the organic phase collected at the end of this second distillation was combined with the essential oil obtained by hydrodistillation.
- the aqueous phase thus treated was concentrated by adsorption / desorption on a suitable resin in order to recover only the volatile compounds of interest and to remove the water.
- This concentrated rose water was added to the essential oil according to a “rose water / rose essential oil” mass ratio of approximately 1.3.
- the mixture thus obtained underwent a fractional distillation step in order to remove the methyl eugenol and obtain the “Active” composition.
- the “Extract” composition is composed of 0.5% by weight of the "Active” and 99.5% of pentylene glycol.
- the “Extract” composition therefore corresponds to a "precursor” cosmetic composition according to the invention.
- EXAMPLE 1 Evaluation of the protective effect of the combination of rose water / essential oil of rose on human skin explants with respect to stress
- Skin explants are distributed in 4 batches and cultured for 9 days, in the presence or absence of a hormone released in the event of stress, epinephrine, and in the presence or absence of the “Extract” composition which is added up to 1% by volume in the culture medium.
- Histological sections from the skin explants were made on day 0 and day 9. To this end, sections 5 qm thick are made using a Leica RM 2125 Minot-type microtome, and sections are mounted on Superfrost® histological glass coverslips. Immunostaining
- paraffin blocks underwent sections 4 qm thick then these sections were fixed on glass slides and stained with the Fontana-Masson technique to observe the distribution of melanin.
- the percentage of the epidermis covered by the purple marking is determined by image analysis software. The percentage of marked surface for each treatment is compared with respect to the untreated control, at 9 days.
- Loricrin is a protein synthesized in the epidermis in the Stratum granulosum. It then migrates to the periphery of the cell to be covalently linked to other cytosolic proteins to form the horny envelope. Loricrin makes up almost 80% of the total protein mass of the horny envelope, that is, the Stratum corneum.
- gH2AC is a histone protein involved in the formation of the nucleosome. This is the first marker of the break of the double-stranded DNA, as phosphorylation of H2AX histone is the iere stage of the recruitment of repair proteins to DNA. Epinephrine has been shown to increase DNA damage, interfere with DNA repair, and impair transcriptional regulation of the cell cycle.
- G6pDH Glucose-6-phosphate dehydrogenase
- NADPH NADPH
- the “Extract” added to the culture medium at a level of 1% by volume makes it possible to regulate the acceleration of the metabolism and of the cellular activity of the cell, bringing it back to a state of rest, while limiting. DNA damage and pigment disorders caused by constant stress over 9 days, in this epinephrine-treated explant model.
- the combination of rose water and rose essential oil according to the invention protects the epidermis from the deleterious effects of stress.
- EXAMPLE 2 Evaluation of the effect of the combination of rose water and essential oil of rose on melanin synthesis
- keratinocytes are capable of synthesize epinephrine, and that this could stimulate the synthesis of melanin via the adrenergic receptors a1 and b2 present on the melanocytes.
- the aim of this study was to evaluate the effect of the composition "Extract" on the production of melanin in a culture of murine B16F1 melanocytes after exposure to a-MSH.
- the “Extract” composition was tested at the following concentrations in the culture medium: 0.3; 0.15; 0.075 and 0.037%.
- the ⁇ -MSH chosen to induce melanogenesis was tested at lnM.
- B16F1 cells are maintained in a specific medium composed of DMEM supplemented with 10% fetal calf serum, 1% antibiotics (penicillin / streptomycin) and 1% L-Glutamine at 37 ° C under 5% C02 and 95 % humidity.
- Figure 2 shows the percent inhibition of melanin production in treated cells compared to untreated cells.
- EXAMPLE 3 Comparison of the effect of rose water alone, essential oil alone and the combination of rose water / rose essential oil ("Active") on tyrosinase activity:
- the aim of this study is to show that the combination is more effective than the ingredients taken separately, on one of the enzymes responsible for the synthesis of melanin.
- the "Active” that is to say the mixture of concentrated rose water and essential rose oil without the support of pentylene glycol
- concentrated rose water and essential rose oil are evaluated at the following concentrations: 0.04, 0.02 and 0.01%.
- the activity of tyrosinase is measured by a colorimetric assay of DOPAchrome, the product of the enzymatic reaction on L-tyrosine.
- the mushroom tyrosinase enzyme is diluted to 50U / mL in 50 mM phosphate buffer except in the blank and the negative control. In each well, are added: 100 ⁇ l of enzyme, 25 ⁇ L of sample to be evaluated, and 125 ⁇ L of L-DOPA (4 mM). The absorbance is read at 450 nm after 15min.
- the results are expressed as a percentage inhibition of tyrosinase, inversely correlated with absorbance and shown in Figure 5.
- the "Active” that is to say the combination of rose water and oil. rose essential oil, is significantly more effective at inhibiting tyrosinase activity than essential oil alone. It is noted that the concentrated rose water exhibits tyrosinase inhibiting activity equivalent to that of the "Active" according to the invention.
- Example 3 shows that the "Active” and rose water have similar mushroom tyrosinase inhibitory activity. The Applicant has therefore investigated the activity of the “Active” and of rose water on cellular melanogenesis.
- the “Active” and the concentrated rose water were tested at the following concentrations in the culture medium: 0.00003% and 0.00006%.
- ⁇ -MSH chosen to induce melanogenesis
- B16F1 cells are maintained in a specific medium composed of DMEM supplemented with 10% fetal calf serum, 1% antibiotics (penicillin / streptomycin) and 1% L-Glutamine at 37 ° C under 5% C02 and 95 % humidity.
- 1.3.10 4 cells were seeded per microplate well. After 24 hours, the a-MSH is added to the medium with or without the “Active” or the concentrated rose water. After 2 or 3 days of culture, the secretion of melanin is measured in the extracellular medium.
- Table 2 shows the percentage inhibition of melanin production in treated cells compared to untreated cells. Although a similar inhibitory activity was observed on mushroom tyrosinase, "Active” T induces an inhibition of melanin production induced by ⁇ -MSH significantly greater than that observed by rose water concentrated at same concentration. The “Active” containing the combination of “concentrated rose water and essential oil” thus more strongly reduces the disruption of melanogenesis potentially induced by stress.
- EXAMPLE 5 Demonstration of the expression of the olfactory receptors OR2AG2, OR11H4 and OR10A6 in the skin and of their activation by the combination of rose water / rose essential oil according to the invention Determination of the agonist effect of 'Active against different human olfactory receptors fhQR)
- the olfactory receptor activation test was performed on HEK293T-RTP1S / RTP2 cells.
- the cells were seeded on 96 well plates and transfected using TransIT-LT1 as the transfecting agent.
- the cells were then co-transfected with vectors encoding each olfactory receptor as well as the CRE-Luc reporter vector for the cAMP gene.
- the culture medium was replaced with serum-free medium containing the compounds to be tested. 10 different concentrations of each compound were tested for each receptor.
- the cells were lysed by adding 50 ⁇ L of lysis buffer then the measurement by luminescence was carried out. The measurement was read with a Spectra Max M5 reader (Molecular Devices, Sunnyvale, CA).
- HL activation level
- HL (Luminescence Compound-Lurninescence Buffer) / Luminescence Buffer in which Luminescence Buffer and Compound luminescence represent the experimental measure of the response of a hOR by luminescence after application of the buffer and the test compound, respectively
- the dose-response curves were analyzed with Excel software.
- the results were qualified as positive or negative depending on the shape of the curve obtained and the EC50 value determined.
- the keratinocytes used in this study were isolated from human epidermis from the company Alphenyx.
- the NHEK cells are maintained in culture in a KGM2 medium (Promocell, ref C-20011) with 1% Penicillin / Streptomycin (P0781-100mL, Sigma) and the supplements of Promocell medium at 37 ° C under 5% C02 and 95% d 'humidity.
- RNA with Maxima Lirst Strand cDNA Synthesis Kit (ThermoLisher, # K1671) as well as the SureCycler 8800 Thermal Cycler (Agilent).
- the DNA was then quantified by quantitative triplicate PCR for each donor using the TaqMan TM Last Advanced Master Mix (ThermoLisher, # 4444557) as well as the Taqman probes targeting the olfactory receptors of interest (ThermoLisher, # 4448892, Hs01943152_sl for OR11H4, Hs02786624_gl for GAPDH, Hs01943048_sl for OR10A6 and Hs02338961_sl for OR2AG2).
- Quantitative PCR was performed with the AriaMx system (Agilent) using GAPDH as internal control.
- the level of expression of olfactory receptors vs. GAPDH was determined using the method for comparing the Ct value calculated using the AriaMx 1.6 software.
- the cells are seeded on a 4-well Labteck plate (Dutscher, # 055078) at 5.10 4 cells / well for a volume of 500 ⁇ L for 48 hours at 37 ° C. under 5% CO 2 and 95% humidity. Fixation is then carried out with 10% formalin (Sigma, # HT501 l-15mL).
- the cells are then incubated with the primary antibody OR10A6 (Thermofisher, # PA5-38193) or OR11H4 (Thermofisher, # PA5-562685) or OR2AG2 (Thermofisher, # PA5-538166) overnight at 4 ° C diluted to 1 / 50 in PBS + 1% BSA before adding the secondary antibody "goat anti-rabbit IgG secondary antibody, AlexaFluor 546" (ThermoFisher, # A11035) diluted at 1: 800 in PBS + 1% BSA for 1 hour in a black piece.
- OR10A6 Thermofisher, # PA5-38193
- OR11H4 Thermofisher, # PA5-562685
- OR2AG2 Thermofisher, # PA5-538166
- the nucleus is labeled with DAPI (2- (4-Amidinophenyl) -6-indolecarbamidine dihydrochloride, 4 ', 6-Diamidino-2-phenylindole dihydrochloride) contained in the mounting medium (Santa Cruz, # sc-24941).
- DAPI 2- (4-Amidinophenyl) -6-indolecarbamidine dihydrochloride, 4 ', 6-Diamidino-2-phenylindole dihydrochloride
- the cells are then observed and captured using an LSM880 confocal microscope (Cari Zeiss) and analyzed using the J 2.0 image software.
- Example 1 The skin explants used in Example 1 (whether or not incubated with F “Extract” in the presence of epinephrine), placed at -80 ° C in the OCT (Cell Path, # KMA-0100-00A), are cut in 5pm section. The sections are then placed at -20 ° C until labeling.
- the olfactory receptors are labeled, after a permeabilization step in PBS with 0.1% Triton X-100 (Sigma-Aldrich, # T8787), using the primary antibody OR10A6 (Thermofisher, # PA5- 38193) or OR11H4 (Thermofisher, # PA5-562685) or OR2AG2 (Thermofisher, # PA5-538166) overnight at 4 ° C diluted to 1/200 in PBS + 3% BSA.
- OR10A6 Thermofisher, # PA5- 38193
- OR11H4 Thermofisher, # PA5-562685
- OR2AG2 Thermofisher, # PA5-538166
- the secondary antibody “goat anti-rabbit IgG secondary antibody, AlexaLluor 546” (ThermoLisher, # A11035) diluted at 1: 800 in PBS + 1% BSA is then added for 1 hour in a black room.
- the nucleus is labeled with DAPI (2- (4-Amidinophenyl) -6-indolecarbamidine dihydrochloride, 4 ', 6-Diamidino-2-phenylindole dihydrochloride) contained in the mounting medium (Santa Cruz, # sc-24941).
- the cells are then observed and captured using an LSM880 confocal microscope (Cari Zeiss) then analyzed and quantified using the J 2.0 image software.
- Olfactory receptors were first discovered in 1991 in the nasal olfactory epithelium. These receptors can be activated by scent molecules to send a signal to the brain and give the perception of scent as the final messenger. Recently, it has been shown that some olfactory receptors are expressed in other tissues. The role of olfactory receptors in these tissues remains unknown.
- the "Extract” according to the invention comprises odorous molecules.
- the Applicant sought to determine whether the Extract, or one of these components, 2-phenylethanol, was capable of activating certain olfactory receptors expressed in the skin.
- the agonist activity of the “Active” and of 2-phenylethanol was evaluated with respect to 150 human olfactory receptors by the screening test proposed by the company ChemCom.
- This test showed that the "Active” and 2-phenylethanol activate, among other things, the OR10A6, OR2AG2 and OR11H4 receptors with the following EC50s: 1.3.10 4 %, 1.0.10 3 % and 2.0.10 4 % for the "Active” and 63 mM, 158 mM and 20 mM for 2-phenylethanol, respectively.
- RNA quantification and immunostaining tests in keratinocytes from human skin samples have demonstrated for the first time the expression of the OR10A6, OR2AG2 and OR11H4 receptors in the skin.
- OR11H4 is mainly localized at the level of the cells of the basal layer of the epidermis while OR2AG2 is mainly detected at the level of the cells of the granular layer of the epidermis.
- OR10A6 is detected over the entire thickness of the epidermis and mainly in the granular layer ( Figure 6).
- Example 1 demonstrated that epinephrine significantly decreases (-20%) the level of expression of the olfactory receptor OR2AG2, compared with the skin explants. controls (not exposed to epinephrine). Such a decrease in the expression of OR2AG2 is not observed on the explants exposed to epinephrine in the presence of the "Extract", the level of expression being maintained at a basal level. Such a result tends to show that the protective role of the "Extract" Epinephrine-induced stress is mediated, at least in part, by a biological pathway involving OR2AG2.
- Epinephrine synthesized in keratinocytes has been shown to cause stress and fatigue of the skin through beta-2 adrenergic receptors (ADRB2).
- ADRB2 adrenergic receptors ADRB2 adrenergic receptors
- the results of immunostaining on skin explants show that epinephrine has an impact on the level of expression of certain olfactory receptors, and in particular leads to a decrease in the expression of OR2AG2.
- the olfactory receptor and the p2-adrcncrgiquc receptor could form a heterodimer which would cause, once the olfactory receptor is activated, a modification of the conformation of ADRB2 leading to a loss of function of the latter.
- Example 1 the protective effect of the Extract against epinephrine demonstrated in Example 1 could result, at least in part, from activation of the OR10A6, OR2AG2 and / or OR11H4 receptors expressed by the keratinocytes.
- Example 6 Cream B (see Example 6) comprising 1% of the “Extract” composition (0.005% of the “Active” composition)
- Cream A Placebo cream having the same composition as cream B except that "Extract” has been replaced by a solution comprising 99.5% pentylene glycol and 0.5% deionized water.
- Cream B product (containing 1% of the "Extract” composition) was carried out in comparison with the Cream A product containing pentylene glycol but not the “Active” composition, according to the following protocol: Application in the hemi-face morning and evening in 14 volunteers, young women aged 30 to 40 years (average age: 36.3 years), with dry skin, drawn features and having a stressful rhythm of life, phototypes I to III.
- VISIA photos were taken with several lighting modes (normal, cross-polarized and UV light), making it possible to analyze the radiance and uniformity of the complexion. Image analyzes were performed by Newton.
- Cream B containing rose extract has shown an effect on the radiance and uniformity of the complexion, characterized by:
- cream B comprising rose water and rose essential oil on the skin reduces the signs of skin fatigue and stress, compared to the control group. This effect is visible from 7 days after the start of application.
- Using rose water and rose essential oil in combination helps the skin regain vitality and radiance.
- Gel B acrylate gel comprising 1% of the composition “Extract” (0.005% of the composition “Active”)
- Gel A Placebo gel having the same composition as gel B except that "Extract” was replaced by a solution comprising 99.5% pentylene glycol and 0.5% deionized water.
- gel B comprising rose water and rose essential oil on the skin makes it possible to reduce the intensity (surface, color) of dark circles due to skin fatigue and stress, compared to a group of witnesses. This effect is visible from 7 days after the start of application.
- using rose water and rose essential oil in combination helps make the eyes look less tired, more rested and brighter.
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FR1900834A FR3091994B1 (en) | 2019-01-30 | 2019-01-30 | New cosmetic uses of a rose extract |
FR1911233 | 2019-10-10 | ||
PCT/FR2020/050133 WO2020157428A1 (en) | 2019-01-30 | 2020-01-29 | Novel cosmetic uses of a rose extract |
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FR2581875B1 (en) * | 1985-05-17 | 1987-06-26 | Caloc Elie | COSMETIC COMPOSITION BASED ON SOFTENING AND SOFTENING AGENTS FOR EXTERNAL APPLICATION FOR BODY SOFTENING |
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