WO2019211470A1 - Extrait de coques de fèves de theobroma cacao pour lutter contre la rosacée et les rougeurs cutanées - Google Patents
Extrait de coques de fèves de theobroma cacao pour lutter contre la rosacée et les rougeurs cutanées Download PDFInfo
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- WO2019211470A1 WO2019211470A1 PCT/EP2019/061448 EP2019061448W WO2019211470A1 WO 2019211470 A1 WO2019211470 A1 WO 2019211470A1 EP 2019061448 W EP2019061448 W EP 2019061448W WO 2019211470 A1 WO2019211470 A1 WO 2019211470A1
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- extract
- rosacea
- theobroma cacao
- theobroma
- cosmetic
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- 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]
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- 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)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- 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
- A61Q19/005—Preparations for sensitive skin
Definitions
- the present invention relates to a shell extract of Theobroma cocoa beans and compositions containing this extract for application in the fields of cosmetics and dermatology to fight against skin redness.
- the present invention relates to a shell extract of Theobroma cacao beans and compositions containing this extract for the control of rosacea.
- the skin is the organ of the largest human body, nearly 2m 2 of surface. It plays several fundamental roles, including external protection, thermal regulation, hormonal synthesis and has an immune function.
- the skin consists of three superimposed layers that are the epidermis, in permanent renewal, the dermis and the hypoderm which ensures the fibrous framework.
- the skin's color, texture and quality also have an undeniable psychosocial function.
- Sensitive skins have in common to react quickly and excessively to a change in temperature, cold, wind, irritating hygiene or toilet products, unsuitable care.
- the redness of the face is the prerogative of the sensitive skins, these skins which are distinguished by an exacerbated reactivity of the skin and cutaneous vessels.
- the redness is more or less intermittent, but always uncomfortable and embarrassing.
- Intermittent redness also called “flush” is a reaction of acute vasodilation that may be due to a commonplace or a little “stressful” such as a question for a student, a job interview, a emotionally emotional or conflictual conversation but still a change in temperature that solicits the circulation of blood in the face.
- a diet too hot, alcoholic beverages or certain foods can also cause this redness.
- redness can occur in people with vaso- reactive skin, a cutaneous feature that can be familial; or skin aging: from 25 years the skin is more sensitive to redness.
- redness can become permanent, especially in the cheeks. This is called erythrosis which is a diffuse but permanent redness localized most often on the cheeks in the form of red patches.
- the rosacea represents an aggravation of the erythrose with appearance of small dilated vessels. When pimples appear and the redness becomes permanent, it is called rosacea. It was formerly known as "rosacea" because, in addition to redness, it also has pimples reminiscent of adolescent acne.
- Rosacea is a chronic and progressive joint inflammatory dermatosis related to vascular relaxation. It is a condition that affects the small vessels of the face. It frequently affects fair-skinned people and can have significant psycho-emotional consequences.
- the name of this pathology refers to the color characteristic that takes the face during the disease.
- Rosacea is a fairly common disease, since in France 2 to 3% of the adult population is concerned. Women are particularly affected, since there are two women for a man suffering from rosacea.
- ocular rosacea mainly affects the central part of the face and is characterized by facial redness or flushing, facial erythema, papules, pustules, telangiectasia and sometimes ocular lesions called ocular rosacea.
- the soft tissue of the nose can swell and produce bulbous swelling called rhinophyma.
- Rosacea evolves, but not obligatorily, over several years by exacerbations aggravated by different stimuli such as temperature variations, alcohol, spices, sun exposure or emotions.
- the mechanisms of occurrence of rosacea are still very poorly understood.
- vascular origin of the disease mainly affects the central part of the face and is characterized by facial redness or flushing, facial erythema, papules, pustules, telangiectasia and sometimes ocular lesions called ocular rosacea.
- the soft tissue of the nose can swell and produce bulbous swelling called rhinophyma.
- Rosacea evolves, but
- Blood vessels are thought to carry an abnormality of functioning, especially in Nordic-type subjects with fair skin, light eyes and light hair. This geographical predisposition is found in France, where the disease is very rare in the south and much more common north of the Loire. On the other side of the Mediterranean, and especially on black skin, the disease is practically non-existent.
- Erythematotelangiectatic rosacea It is mainly characterized by flushing and persistent central facial erythema. The presence of telangiectasia is common, but not essential to the diagnosis of this type. Central facial edema, burning and stinging, and roughness or desquamation are also sometimes observed.
- Papulopustular rosacea it is characterized by persistent central facial erythema and transient papules and / or pustules distributed in the center of the face. However, papules and pustules can also affect periorifical areas, such as perioral, perineal or periocular. This type of rosacea is reminiscent of acne, but comedones are absent. But rosacea and acne can coexist. Patients with this type of rosacea sometimes complain of burning and stinging. This type is often observed before or at the same time as the previous type, including the presence of telangiectasia. These may be masked by persistent erythema and papules or pustules.
- Rhinophyma it is manifested by a thickening of the skin, nodules with an irregular surface and swelling. Rhinophyma is the most common presentation, but phymatous rosacea can affect other areas, such as the chin, forehead, cheeks or ears. In patients with this type of rosacea, the presence of enlarged and prominent follicular openings is sometimes reported in the affected area, as well as telangiectasia. This type is often observed before or at the same time as types 1 or 2. In the case of rhinophyma, these additional stigmas may be particularly pronounced in the nasal region.
- ocular or ophthalmic rosacea The diagnosis of ocular rosacea should be considered when a patient presents with one or more of the following eye signs and symptoms: tearful or bloodshot appearance, foreign body sensation, burning or stinging, dryness, itching , photosensitivity, blurred vision, telangiectasia of the conjunctiva and eyelid margin or erythema of the eyelid and periocular. Blepharitis, conjunctivitis and irregular margins of the eyelid are other signs that may be detected.
- a chalazion or chronic staphylococcal infection manifested by a stye and the cause of which is a malfunction of the Meibomian glands is a common sign of ocular disease associated with rosacea.
- the diagnosis of ocular rosacea is most often made when cutaneous signs and symptoms are also detected.
- Corticosteroids can also be incriminated, especially in 2 situations.
- the first is rosacea which is aggravated by the application of corticosteroids.
- the second is the appearance of the disease following long-term use of this type of medicine, we even talk about steroid rosacea.
- Oral treatments with tetracycline derivatives are problematic for several reasons but in particular for their non-negligible side effects.
- Oral administration of tetracyclines, such as doxycycline may induce photosensitivity, or even phototoxicity or gastrointestinal disorders.
- the application WO2002 / 074290 describes the topical use of at least one non-steroidal anti-inflammatory compound for treating rosacea, these compounds may be combined with a nitroimidazole compound. However, it is reported that the combination of this treatment induces significant side effects, including gastrointestinal and renal (Edwards, Br. J. Vener Dis., 56, 285-290, 1980).
- the present invention thus relates to an extract of bean shells of Theobroma cacao for its use in the prevention and / or treatment of rosacea.
- the present invention also relates to a cosmetic or dermatological composition
- a cosmetic or dermatological composition comprising at least one shell extract of Theobroma cocoa beans and at least one excipient cosmetically or dermatologically acceptable for use in the prevention and / or treatment of rosacea.
- this treatment or prevention is performed topically, which significantly reduces any systemic side effect.
- the subject of the present invention is also an extract of bovine hulls of Theobroma cacao for its use in the prevention and / or treatment of cutaneous redness.
- the subject of the present invention is also a cosmetic or dermatological composition
- a cosmetic or dermatological composition comprising at least one extract of Theobroma cacao bean shells and at least one cosmetically or dermatologically acceptable excipient for its use in the prevention and / or treatment of cutaneous redness.
- the subject of the present invention is also the cosmetic use of an extract of bean shells of Theobroma cacao to prevent and / or fight against skin rashes.
- the subject of the present invention is also the cosmetic use of a cosmetic or dermatological composition
- a cosmetic or dermatological composition comprising at least one extract of Theobroma cocoa bean shells and at least one cosmetically or dermatologically acceptable excipient for preventing and / or combating cutaneous redness.
- Skin rash may be intermittent redness (i.e., flush) or erythrosis, with redness particularly localized to the cheeks.
- bean shell extract of Theobroma cacao is intended to mean the bean shell extract product of one or more species of Theobroma cacao.
- extractative product means the product obtained after extraction of Theobroma cacao bean shell with a solvent, referred to as extraction solvent, (ie a liquid solution in the extraction solvent ) optionally in a concentrated or dry form after partial or total evaporation of the extraction solvent.
- hydrophilic extract is meant an extract obtained by the use of at least one hydrophilic solvent as extraction solvent. Preferably, it is an extract obtained by extraction with one or more hydrophilic solvents.
- aqueous extract is meant an extract obtained by the use of at least one aqueous solvent as extraction solvent. Preferably, it is an extract obtained by extraction with one or more aqueous solvents.
- hydro-glycolic extract an extract obtained by the use of at least one hydro-glycolic solvent as extraction solvent. Preferably, it is an extract obtained by extraction with one or more hydro-glycol solvents.
- hydrophilic solvent is meant a solvent selected from the group consisting of water, C1 to C5 alcohols (for example ethanol), C3 to C5 glycols (for example butylene glycol), glycerol, polyol acetone, C1 to C5 alkyl esters (e.g., ethyl acetate, isopropyl acetate) and mixtures thereof.
- C1 to C5 alcohols for example ethanol
- C3 to C5 glycols for example butylene glycol
- glycerol polyol acetone
- C1 to C5 alkyl esters e.g., ethyl acetate, isopropyl acetate
- aqueous solvent is meant a solvent selected from the group consisting of water alone and water in combination with one or more C1 to C5 alcohols (eg ethanol), one or more C3 to C5 glycols. and combinations thereof.
- hydro-glycolic solvent is meant a mixture of water and at least one C3-C5 glycol, especially propylene glycol, butylene glycol, pentylene glycol or a combination thereof.
- it is a water / butylene glycol mixture.
- dry extract is meant in the sense of the present invention, an extract free of extraction solvent or support or containing only non-significant trace. Such a dry extract thus contains only material from the bean shells of Theobroma cacao. It may also contain insignificant traces of extraction solvent.
- topical application is meant an application on the skin, mucous membranes and / or integuments, especially on the skin.
- treatment or "treat” rosacea, it is intended to reduce and / or inhibit the development of rosacea and / or at least one of its symptoms.
- prevention or “prevent” rosacea, it is intended to reduce and / or prevent the appearance of at least one of the symptoms of rosacea.
- Rosacea symptom means persistent redness, burning and stinging, hot flashes or telangiectasia.
- Skin rash refers more particularly to intermittent cutaneous redness (such as flushes or redness due to external factors such as cold or wind) or permanent redness (such as erythrosis), more particularly localized at the level of the skin. play.
- treatment or “treat” or “fight against” or “fight against” skin redness is meant to reduce and / or eliminate the development of redness of the skin.
- prevention or “prevent” skin redness is meant to reduce and / or prevent the appearance of redness of the skin.
- cosmetic or dermatologically acceptable is intended to mean that which is useful in the preparation of a cosmetic or dermatological composition, which is generally safe, non-toxic and neither biologically nor otherwise undesirable and which is acceptable for a particular cosmetic or dermatological composition.
- cosmetic or dermatological use especially by topical application and / or oral administration.
- cocoa or cocoa tree the cocoa tree (Theobroma cacao) is a small evergreen tree of the genus Theobroma family Sterculiaceae according to the classical classification, or Malvaceae according to the phylogenetic classification. It produces edible beans with different flavors depending on the varieties of cacao, from which cocoa, the basic product of chocolate, is made.
- the cocoa tree is a tropical species native to Mexico. It grows naturally in the Orinoco Basin and the Amazon at low altitude, at the foot of the Andes Mountains. It is a tree that is 10 to 15 meters tall, cauliflora and evergreen. It flowers from three years and gives flowers, fruits and leaves all year round.
- the pods contain many seeds, from 25 to 75, grouped in ears and called cocoa beans, rich in starch, fat and alkaloids. Each mature seed is surrounded by a pulp called mucilage.
- the fresh beans collected in the pod are fermented and then dried to give the so-called cocoa beans which will be used for the preparation of the cocoa proper. These beans contain a purple embryo with 2 large fleshy cotyledons, curled around a remnant of albumen.
- the beans are protected by a hard integument, the hull, which envelops them completely.
- the cocoa beans are rich in xanthine bases and more particularly in theobromine and caffeine.
- the hulls of cocoa beans have significant levels of polyphenols (anthocyanins, flavonoids).
- the bean shell extract of Theobroma cacao is a liquid extract, more particularly a hydrophilic extract, more particularly an aqueous extract and even more particularly a hydro-glycolic extract.
- This extract may in particular be obtained by extraction with at least one hydrophilic solvent, preferably with at least one aqueous solvent and even more preferably with at least one hydro-glycolic solvent.
- this extract is obtained by extraction of the hulls of Theobroma cocoa beans, preferably previously crushed or crushed, for example previously crushed, using one or more hydro-glycolic solvent (s) ( s), such as a water / butylene glycol mixture, for example in a water / butylene glycol ratio of 25/75 to 40/60.
- s hydro-glycolic solvent
- the bean shell extract of Theobroma cacao according to the invention advantageously contains 45% to 65% by weight of caffeine relative to the weight of the dry extract.
- the bean shell extract of Theobroma cacao according to the invention will also advantageously contain 1.5% to 3.0% by weight of theobromine relative to the weight of the dry extract.
- the extract according to the present invention can be obtained by extraction of shells of Theobroma cocoa beans crushed with a water / butylene glycol mixture as extraction solvent, for example in a water / butylene glycol ratio. from 25/75 to 40/60.
- the bean shell extract of Theobroma cacao obtainable by such an example of extraction will advantageously contain 1.5 to 2.1% by weight of caffeine and 0.05 to 0.09% by weight. in weight of theobromine relative to the total weight of the extract.
- Such an extract advantageously contains 1 to 5%, especially 2 to 4% by weight of dry extract.
- Such an extract may be used as it is (solution with the extraction solvent) or in the form of a concentrated extract or of a dry extract after partial or total evaporation of the extraction solvent.
- the invention relates to an extract of bean shells of Theobroma cacao, in particular as defined above, for its use in the treatment and / or prevention of rosacea.
- the invention also relates to the use of an extract of bovine hulls of Theobroma cacao, in particular as defined above, for the manufacture of a medicament for the prevention and / or treatment of rosacea.
- the invention also relates to a method for preventing and / or treating rosacea comprising administering to an individual in need of an effective amount of coconut shell extract of Theobroma cacao, especially as defined herein. above.
- the purpose of the invention is therefore to propose a treatment for rosacea, which in particular reduces the side effects for the patient.
- this treatment is performed topically, which significantly reduces any systemic side effect.
- Rosacea may be selected from the group consisting of erythematotelangiectatic rosacea, papulopustular rosacea, phymatous rosacea, and ocular rosacea.
- the subject of the present invention is also an extract of bean shells of Theobroma cacao, in particular as defined above, for its use in the prevention and / or the treatment of cutaneous redness.
- the invention also relates to the use of an extract of bean shells of Theobroma cacao, in particular as defined above, for the manufacture of a medicament intended for the prevention and / or treatment of skin rashes.
- the invention also relates to a method for the prevention and / or treatment of cutaneous redness comprising administering to an individual in need of an effective amount of a coconut shell extract of Theobroma cacao, in particular as defined above. above.
- the subject of the present invention is also the cosmetic use of an extract of bovine hulls of Theobroma cacao, in particular as defined above, for preventing and / or combating cutaneous redness.
- the present invention thus also aims at a cosmetic method for preventing and / or combating cutaneous redness comprising the use, preferably by topical application, of a shell extract of Theobroma cocoa beans, especially as defined above.
- the use of Theobroma cocoa bean shell extract according to the invention is preferentially topically.
- the skin rashes are as defined above.
- the redness of the skin is localized in the cheeks.
- the present invention also relates to a cosmetic or dermatological composition
- a cosmetic or dermatological composition comprising at least one shell extract of Theobroma cocoa beans, in particular as defined above, with at least one cosmetically or dermatologically acceptable excipient, for its use in the treatment and / or prevention of rosacea.
- the invention also relates to the use of a cosmetic or dermatological composition
- a cosmetic or dermatological composition comprising at least one extract of bean shells of Theobroma cacao, in particular as defined above, with at least one cosmetically or dermatologically acceptable excipient, for the manufacture of a medicine for the prevention and / or treatment of rosacea.
- the invention also relates to a method for preventing and / or treating rosacea comprising administering an individual in need of an effective amount of a cosmetic or dermatological composition comprising at least one shell extract of Theobroma cocoa beans, especially as defined above, with at least one cosmetically or dermatologically acceptable excipient.
- the composition according to the invention is in a form suitable for topical application.
- the present invention also relates to a cosmetic or dermatological composition comprising at least one shell extract of Theobroma cocoa beans, in particular as defined above, with at least one cosmetically or dermatologically acceptable excipient, for its use in the treatment and / or prevention of skin rashes.
- the invention also relates to the use of a cosmetic or dermatological composition
- a cosmetic or dermatological composition comprising at least one extract of bean shells of Theobroma cacao, in particular as defined above, with at least one cosmetically or dermatologically acceptable excipient, for the manufacture of a drug for the prevention and / or treatment of skin rashes.
- the invention also relates to a method for preventing and / or treating cutaneous redness comprising administering to an individual in need of an effective amount of a cosmetic or dermatological composition comprising at least one extract of Theobroma bean shells. cocoa, especially as defined above, with at least one cosmetically or dermatologically acceptable excipient.
- the subject of the present invention is also the cosmetic use of a cosmetic or dermatological composition comprising at least one extract of bean shells of Theobroma cacao, in particular as defined above, with at least one cosmetically or dermatologically acceptable excipient, for prevent and / or fight against skin rashes.
- the present invention thus also aims at a cosmetic method for preventing and / or combating cutaneous redness comprising the use, preferably by topical application, of a cosmetic or dermatological composition comprising at least one extract of cocoa bean shells from Theobroma cacao, in particular as defined above, with at least one cosmetically or dermatologically acceptable excipient.
- the use of the cosmetic or dermatological composition according to the invention is preferably topically.
- the skin rashes are as defined above.
- the redness of the skin is localized in the cheeks.
- the cosmetic or dermatological compositions according to the third or fourth aspect of the invention may be in the forms which are usually known for topical administration, that is to say in particular lotions, foams, gels, dispersions, emulsions , sprays, serums, masks or creams, jellies, especially micellar jellies, with excipients allowing in particular skin penetration to improve the properties and accessibility of the active ingredient.
- it will be a cream, an emulsion, or a jelly.
- compositions generally contain, besides the compounds of the extract according to the present invention, a physiologically acceptable medium, generally based on water or solvent, for example alcohols, ethers or glycols. They may also contain surfactants, complexing agents, preservatives, stabilizing agents, emulsifiers, thickeners, gelling agents, humectants, emollients, trace elements, essential oils, perfumes, dyes, mattifying agents, chemical or mineral filters, moisturizing agents, thermal waters, etc.
- the compositions according to the present invention will comprise 0.1 to 5% by weight, preferably 0.5 to 4% by weight, more preferably 0.5 to 3% by weight, more preferably 1 to 2% by weight.
- compositions according to the present invention will comprise 1% by weight of Theobroma cacao bean shell extract relative to the total weight of the composition. In a most preferred manner, the compositions according to the present invention will comprise 2% by weight of Theobroma cacao bean shell extract based on the total weight of the composition. In another equally preferred manner, the compositions according to the present invention will comprise 3% by weight of Theobroma cacao bean shell extract based on the total weight of the composition.
- the extracts of Theobroma cacao bean shells used in the compositions according to the invention will advantageously comprise a solids content of 1% to 5%, preferably 2% to 4%, by weight relative to the total weight of the product. 'extract.
- the compositions according to the present invention will comprise 0.001 to 0.25%, preferably 0.005 to 0.20%, more preferably 0.005 to 0.15%, even more preferably 0.01 to 0.10% of Theobroma cocoa bean shell extract by weight of dry extract relative to the total weight of the composition.
- the extracts of Theobroma cacao bean shells used in the compositions according to the invention will advantageously comprise a solids content of 1% to 5%, preferably 2% to 4%, by weight relative to the total weight of the product. 'extract.
- compositions may be made according to methods well known to those skilled in the art.
- Rosacea is a chronic disorder characterized by inflammation and vascular abnormalities of the facial skin. Cutaneous biopsies in patients with rosacea are characterized by perivascular infiltrates associated with vasodilation. ⁇ 2 -adrenergic receptor agonists exhibit vasoconstrictor activity. New approaches are expected for the treatment of facial erythema of rosacea. A recent approach has been to reduce erythema by vasoconstricting cutaneous blood vessels by targeting both ⁇ -adrenergic receptors with oxymetazoline (selective oti-adrenergic receptors, Shanler and Ondon, Arch Dermatol, 143 (11), pp. 1369-1371, 2007) and brimonidine (selective ot2-adrenergic receptors, Fowler et al., J.
- oxymetazoline selective oti-adrenergic receptors
- ⁇ 2-adrenergic receptors belong to the broad family of 7-transmembrane G protein-coupled receptors. Agonists for ⁇ 2 -adrenergic receptors cause an increase in adenylate cyclase activity resulting in an increase in intracellular cAMP .
- the purpose of this test is to evaluate the effects of a Theobroma cacao bean shell extract on the activity of human ⁇ 2-adrenergic receptors expressed in HEK-293 cells. This activity is measured by cAMP production.
- a specific agonist of this subtype is added to the incubation medium, it is 3mM dexmedetomidine which will serve as a positive control.
- the cAMP production that results is then quantified by the HTRF® (Homogeneous Time-Resolved) detection method. Fluorescence).
- the results presented come from 3 independent experiments.
- the extract tested in this study was obtained by the hydroglycolic extraction of Theobroma cacao bean shell using a water / butylene glycol mixture as an extraction solvent.
- This extract comprises approximately 69.2% of butylene glycol, 27.5% of water and 3.3% of dry extract.
- This is a commercial material Caobromine® UP, sold by the company Solabia.
- the INCI name of this material Butylene glycol / Aqua / Theobroma cacao.
- the CAS number of Theobroma cacao is: 84649-99-0.
- Dexmedet Dexmedetominidine
- Avg average
- SEM standard error at the mean.
- Dexmedetomidine at 3mM results in an ot2 B - adrenergic agonist response, inducing significant cAMP production. This result was expected and validates this experience.
- the inventors thus demonstrate that an extract of bean shells of Theobroma cacao has a vasoconstrictor activity making it possible to reveal anti-redness properties.
- VEGF Vascular Endothelial Growth Factor growth factor
- VEGF Vascular Endothelial Growth Factor growth factor
- VEGF increases vascular permeability, stimulates endothelial cell migration and proliferation, and induces neovascularization.
- VEGF is secreted by several cell types, such as endothelial cells, lymphocytes and monocytes, but also keratinocytes. Its biological effects are mediated by VEGF-R1 and VEGF-R2 receptors. The cutaneous vascular network in adults is remarkably stable and does not activate angiogenesis.
- angiogenesis is involved in the pathogenesis of several diseases including rosacea. This process of angiogenesis is associated with the inflammatory response where VEGF plays a crucial role, particularly in the recruitment of inflammatory cells from the blood to the inflamed tissue.
- VEGF plays a crucial role, particularly in the recruitment of inflammatory cells from the blood to the inflamed tissue.
- keratinocytes secrete VEGF and express VEGF-R whereas in the case of inflammatory skin diseases, VEGF and its receptor are overexpressed.
- Rosacea is a chronic skin disease whose etiology remains poorly understood. Rosacea is characterized by vascular and inflammatory abnormalities of the skin of the face and the ocular surface. VEGF and its receptor are expressed in skin biopsies of patients with rosacea showing the likely importance of this growth factor in this pathology. Biopsies are characterized by perivascular infiltration associated with vasodilation. The endothelium expresses both VEGF receptors. Although VEGF is present in the epidermis and endothelium, VEGF is not expressed by the endothelium but rather by the infiltration of inflammatory immune cells such as lymphocytes and macrophages. The VEGF pathway may contribute to vascular changes and immune infiltration observed in rosacea.
- the purpose of this study is to evaluate the possible effects of Theobroma cacao bean shell extract on the release of IL8 and VEGF (Steinhoff et al., JAAD, 69: S15).
- Normal human keratinocytes were obtained from pieces of skin derived from surgical waste of mammary or abdominal plasty. The keratinocytes thus obtained are placed in culture on plates of 12 or 24 wells and are exposed for one hour to the compounds to be tested and then placed for 5 or 24h in a rosacea-like environment. Based on the article by Steinhoff et al., JAAD, 69: S15-26, 2013, the rosacea environment is mimicked by the mixture of: a mediator of inflammation selected from TNF activating agents, a mediator of innate immunity selected from TRP receptor activating agents (TRPV1, TRPA1) and a bacterial component which is LL37 peptide. The culture supernatant is then removed, centrifuged and frozen at -20 ° C. The productions of TNF activating agents, a mediator of innate immunity selected from TRP receptor activating agents (TRPV1, TRPA1) and a bacterial component which is LL37 peptide. The culture supernatant is then removed, centr
- VEGF and IL-8 are quantified by ELISA (Enzyme-Linked Immunosorbent Assay). A percentage inhibition of the production of VEGF and IL-8 after exposure to the various compounds tested is calculated. The statistical analysis is performed using a one-way analysis of variance (ANOVA) followed by Dunnett's test.
- ANOVA analysis of variance
- Ext shells of cocoa beans extract of bean shells of Theobroma cacao; Conc: concentration. ** p ⁇ 0.01 versus control.
- Doxycycline is used as a reference inhibitor on the production of VEGF, the results are convincing, the use of doxycycline allowed to validate this test.
- Theobroma cacao bean shell extract has a vascular component, anti-redness, decreasing the vasodilatation of the blood vessels of the face and reducing angiogenesis.
- Theobroma cocoa bean shell extract induces an inhibition of IL8 protein expression in vitro on cells stimulated by a rosacea-like environment, demonstrating anti-inflammatory activity.
- An extract according to the invention can be obtained by extraction of hulls of Theobroma cocoa beans crushed by a mixture of butylene glycol and water, followed by filtration.
- Theobroma cocoa extract 3-4%
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- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
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- Natural Medicines & Medicinal Plants (AREA)
- Dermatology (AREA)
- Botany (AREA)
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Abstract
Description
Claims
Priority Applications (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1020207034379A KR20210005203A (ko) | 2018-05-04 | 2019-05-03 | 장미증 및 피부 발진을 조절하기 위한 테오브로마 카카오 원두의 외피 추출물 |
CA3098361A CA3098361A1 (fr) | 2018-05-04 | 2019-05-03 | Extrait de coques de feves de theobroma cacao pour lutter contre la rosacee et les rougeurs cutanees |
BR112020021956-8A BR112020021956A2 (pt) | 2018-05-04 | 2019-05-03 | extrato de cascas de favas de theobroma cacao para controle de rosácea e vermelhidão cutânea |
MX2020011473A MX2020011473A (es) | 2018-05-04 | 2019-05-03 | Extracto de cascaras de granos de theobroma cacao para controlar la rosacea y el enrojecimiento de la piel. |
EP19720687.3A EP3787754A1 (fr) | 2018-05-04 | 2019-05-03 | Extrait de coques de fèves de theobroma cacao pour lutter contre la rosacée et les rougeurs cutanées |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR1853865 | 2018-05-04 | ||
FR1853865A FR3080767B1 (fr) | 2018-05-04 | 2018-05-04 | Extrait de coques de feves de theobroma cacao pour lutter contre la rosacee et les rougeurs cutanees |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2019211470A1 true WO2019211470A1 (fr) | 2019-11-07 |
Family
ID=63722473
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/EP2019/061448 WO2019211470A1 (fr) | 2018-05-04 | 2019-05-03 | Extrait de coques de fèves de theobroma cacao pour lutter contre la rosacée et les rougeurs cutanées |
Country Status (7)
Country | Link |
---|---|
EP (1) | EP3787754A1 (fr) |
KR (1) | KR20210005203A (fr) |
BR (1) | BR112020021956A2 (fr) |
CA (1) | CA3098361A1 (fr) |
FR (1) | FR3080767B1 (fr) |
MX (1) | MX2020011473A (fr) |
WO (1) | WO2019211470A1 (fr) |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2002074290A2 (fr) | 2001-03-15 | 2002-09-26 | Agis Industries (1983) Ltd. | Preparations dermatologiques |
FR2838055A1 (fr) * | 2002-04-05 | 2003-10-10 | Cep | Nouvelle utilisation d'un extrait de cacao et les compositions cosmetiques et/ou dermatologiques a cet effet |
EP1479374A1 (fr) * | 2003-05-22 | 2004-11-24 | L'oreal | Procédé de traitement cosmétique des rougeurs |
FR2857588A1 (fr) * | 2003-07-17 | 2005-01-21 | Oreal | Utilisation de beta-endorphine, d'agents exercant une activite beta-endorphine-like en cosmetique et dermatologie |
-
2018
- 2018-05-04 FR FR1853865A patent/FR3080767B1/fr active Active
-
2019
- 2019-05-03 CA CA3098361A patent/CA3098361A1/fr active Pending
- 2019-05-03 KR KR1020207034379A patent/KR20210005203A/ko active Search and Examination
- 2019-05-03 MX MX2020011473A patent/MX2020011473A/es unknown
- 2019-05-03 EP EP19720687.3A patent/EP3787754A1/fr not_active Withdrawn
- 2019-05-03 BR BR112020021956-8A patent/BR112020021956A2/pt not_active Application Discontinuation
- 2019-05-03 WO PCT/EP2019/061448 patent/WO2019211470A1/fr unknown
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2002074290A2 (fr) | 2001-03-15 | 2002-09-26 | Agis Industries (1983) Ltd. | Preparations dermatologiques |
FR2838055A1 (fr) * | 2002-04-05 | 2003-10-10 | Cep | Nouvelle utilisation d'un extrait de cacao et les compositions cosmetiques et/ou dermatologiques a cet effet |
EP1479374A1 (fr) * | 2003-05-22 | 2004-11-24 | L'oreal | Procédé de traitement cosmétique des rougeurs |
FR2857588A1 (fr) * | 2003-07-17 | 2005-01-21 | Oreal | Utilisation de beta-endorphine, d'agents exercant une activite beta-endorphine-like en cosmetique et dermatologie |
Non-Patent Citations (6)
Title |
---|
"A c t i v e i n g r e d i e n t s", 27 August 2010 (2010-08-27), pages 1 - 10, XP055038817, Retrieved from the Internet <URL:http://web.archive.org/web/20100827083129/http://www.solabia.fr/solabia/content/NT00005516.pdf> [retrieved on 20120921] * |
EDWARDS, BR, J. VENER DIS., vol. 56, 1980, pages 285 - 290 |
FOWLER ET AL., J. DRUGS DERMATOL., vol. 12, no. 6, 2013, pages 650 - 656 |
SHANLER; ONDON, ARCH DERMATOL, vol. 143, no. 11, 2007, pages 1369 - 1371 |
STEINHOFF ET AL., JAAD, vol. 69, 2013, pages 15 - 26 |
WILKIN ET AL., J. AM. ACAD. DERMATOL., vol. 46, no. 4, 2002, pages 584 - 587 |
Also Published As
Publication number | Publication date |
---|---|
EP3787754A1 (fr) | 2021-03-10 |
MX2020011473A (es) | 2020-12-07 |
BR112020021956A2 (pt) | 2021-01-26 |
KR20210005203A (ko) | 2021-01-13 |
FR3080767B1 (fr) | 2020-10-30 |
CA3098361A1 (fr) | 2019-11-07 |
FR3080767A1 (fr) | 2019-11-08 |
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