FR3130609A1 - Combination of Astragalin and Miquelianin to inhibit S aureus lipase activity. - Google Patents
Combination of Astragalin and Miquelianin to inhibit S aureus lipase activity. Download PDFInfo
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- FR3130609A1 FR3130609A1 FR2114152A FR2114152A FR3130609A1 FR 3130609 A1 FR3130609 A1 FR 3130609A1 FR 2114152 A FR2114152 A FR 2114152A FR 2114152 A FR2114152 A FR 2114152A FR 3130609 A1 FR3130609 A1 FR 3130609A1
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- DUBCCGAQYVUYEU-ZUGPOPFOSA-N miquelianin Chemical compound O1[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1OC1=C(C=2C=C(O)C(O)=CC=2)OC2=CC(O)=CC(O)=C2C1=O DUBCCGAQYVUYEU-ZUGPOPFOSA-N 0.000 title claims abstract description 18
- MQVRGDZCYDEQML-UHFFFAOYSA-N Astragalin Natural products C1=CC(OC)=CC=C1C1=C(OC2C(C(O)C(O)C(CO)O2)O)C(=O)C2=C(O)C=C(O)C=C2O1 MQVRGDZCYDEQML-UHFFFAOYSA-N 0.000 title claims abstract description 17
- JPUKWEQWGBDDQB-QSOFNFLRSA-N kaempferol 3-O-beta-D-glucoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C(C=2C=CC(O)=CC=2)OC2=CC(O)=CC(O)=C2C1=O JPUKWEQWGBDDQB-QSOFNFLRSA-N 0.000 title claims abstract description 17
- DUBCCGAQYVUYEU-VFKUPZNOSA-N Miquelianin Natural products O=C(O)[C@@H]1[C@@H](O)[C@@H](O)[C@H](O)[C@H](OC2=C(c3cc(O)c(O)cc3)Oc3c(c(O)cc(O)c3)C2=O)O1 DUBCCGAQYVUYEU-VFKUPZNOSA-N 0.000 title claims abstract description 16
- 235000019626 lipase activity Nutrition 0.000 title description 2
- 210000004400 mucous membrane Anatomy 0.000 claims abstract description 41
- 239000000203 mixture Substances 0.000 claims abstract description 32
- 230000036074 healthy skin Effects 0.000 claims abstract description 25
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- 239000000284 extract Substances 0.000 claims description 16
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- 239000003795 chemical substances by application Substances 0.000 claims description 11
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- 208000010668 atopic eczema Diseases 0.000 claims description 4
- 230000037336 dry skin Effects 0.000 claims description 4
- 231100000321 erythema Toxicity 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- 208000008742 seborrheic dermatitis Diseases 0.000 claims description 4
- 208000002874 Acne Vulgaris Diseases 0.000 claims description 3
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- 206010000496 acne Diseases 0.000 claims description 3
- 239000003242 anti bacterial agent Substances 0.000 claims description 3
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- 239000002260 anti-inflammatory agent Substances 0.000 claims description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 3
- 238000000605 extraction Methods 0.000 claims description 2
- 238000000034 method Methods 0.000 claims description 2
- 239000000419 plant extract Substances 0.000 claims description 2
- 238000011200 topical administration Methods 0.000 claims description 2
- 230000000699 topical effect Effects 0.000 claims description 2
- 230000000694 effects Effects 0.000 description 8
- 108090001060 Lipase Proteins 0.000 description 6
- 102000004882 Lipase Human genes 0.000 description 5
- 239000004367 Lipase Substances 0.000 description 5
- 235000019421 lipase Nutrition 0.000 description 5
- 208000003251 Pruritus Diseases 0.000 description 4
- 230000007803 itching Effects 0.000 description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- 235000021588 free fatty acids Nutrition 0.000 description 3
- 230000005764 inhibitory process Effects 0.000 description 3
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 2
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 2
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 2
- 241000196324 Embryophyta Species 0.000 description 2
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 2
- 239000005642 Oleic acid Substances 0.000 description 2
- REFJWTPEDVJJIY-UHFFFAOYSA-N Quercetin Chemical compound C=1C(O)=CC(O)=C(C(C=2O)=O)C=1OC=2C1=CC=C(O)C(O)=C1 REFJWTPEDVJJIY-UHFFFAOYSA-N 0.000 description 2
- DUBCCGAQYVUYEU-UHFFFAOYSA-N Querciturone Natural products O1C(C(O)=O)C(O)C(O)C(O)C1OC1=C(C=2C=C(O)C(O)=CC=2)OC2=CC(O)=CC(O)=C2C1=O DUBCCGAQYVUYEU-UHFFFAOYSA-N 0.000 description 2
- 240000006365 Vitis vinifera Species 0.000 description 2
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- 239000003963 antioxidant agent Substances 0.000 description 2
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- 150000007946 flavonol Chemical class 0.000 description 2
- HVQAJTFOCKOKIN-UHFFFAOYSA-N flavonol Natural products O1C2=CC=CC=C2C(=O)C(O)=C1C1=CC=CC=C1 HVQAJTFOCKOKIN-UHFFFAOYSA-N 0.000 description 2
- 235000011957 flavonols Nutrition 0.000 description 2
- 235000002532 grape seed extract Nutrition 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 239000002085 irritant Substances 0.000 description 2
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- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 2
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 2
- LOJXBHNAFUDMIQ-UHFFFAOYSA-N quercetin-3-alpha-glucuronide Natural products OC1OC(C(O)C(O)C1O)C(=O)Oc1c(oc2cc(O)cc(O)c2c1=O)-c1ccc(O)c(O)c1 LOJXBHNAFUDMIQ-UHFFFAOYSA-N 0.000 description 2
- DUBCCGAQYVUYEU-GGTBVAQXSA-N quercetin-3-glucuronide Natural products O1[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@@H](O)[C@H]1OC1=C(C=2C=C(O)C(O)=CC=2)OC2=CC(O)=CC(O)=C2C1=O DUBCCGAQYVUYEU-GGTBVAQXSA-N 0.000 description 2
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- 244000005852 Adiantum capillus veneris Species 0.000 description 1
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- 102000004127 Cytokines Human genes 0.000 description 1
- 108090000695 Cytokines Proteins 0.000 description 1
- 206010012442 Dermatitis contact Diseases 0.000 description 1
- 240000006927 Foeniculum vulgare Species 0.000 description 1
- 235000004204 Foeniculum vulgare Nutrition 0.000 description 1
- 244000307700 Fragaria vesca Species 0.000 description 1
- 235000016623 Fragaria vesca Nutrition 0.000 description 1
- 235000011363 Fragaria x ananassa Nutrition 0.000 description 1
- 244000144229 Gaultheria miqueliana Species 0.000 description 1
- 235000010050 Gaultheria miqueliana Nutrition 0.000 description 1
- 235000017309 Hypericum perforatum Nutrition 0.000 description 1
- 244000141009 Hypericum perforatum Species 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 102000004125 Interleukin-1alpha Human genes 0.000 description 1
- 108010082786 Interleukin-1alpha Proteins 0.000 description 1
- 241000736262 Microbiota Species 0.000 description 1
- 206010028111 Mucosal dryness Diseases 0.000 description 1
- 241001646133 Myrothamnus flabellifolia Species 0.000 description 1
- 240000002853 Nelumbo nucifera Species 0.000 description 1
- 235000006508 Nelumbo nucifera Nutrition 0.000 description 1
- 206010030113 Oedema Diseases 0.000 description 1
- 240000008916 Oenothera biennis Species 0.000 description 1
- 235000004496 Oenothera biennis Nutrition 0.000 description 1
- 244000046052 Phaseolus vulgaris Species 0.000 description 1
- 235000010627 Phaseolus vulgaris Nutrition 0.000 description 1
- ZVOLCUVKHLEPEV-UHFFFAOYSA-N Quercetagetin Natural products C1=C(O)C(O)=CC=C1C1=C(O)C(=O)C2=C(O)C(O)=C(O)C=C2O1 ZVOLCUVKHLEPEV-UHFFFAOYSA-N 0.000 description 1
- HWTZYBCRDDUBJY-UHFFFAOYSA-N Rhynchosin Natural products C1=C(O)C(O)=CC=C1C1=C(O)C(=O)C2=CC(O)=C(O)C=C2O1 HWTZYBCRDDUBJY-UHFFFAOYSA-N 0.000 description 1
- 244000235659 Rubus idaeus Species 0.000 description 1
- 235000009122 Rubus idaeus Nutrition 0.000 description 1
- 241000191967 Staphylococcus aureus Species 0.000 description 1
- 239000013566 allergen Substances 0.000 description 1
- 230000000172 allergic effect Effects 0.000 description 1
- 230000001430 anti-depressive effect Effects 0.000 description 1
- 230000003178 anti-diabetic effect Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 239000000935 antidepressant agent Substances 0.000 description 1
- 229940005513 antidepressants Drugs 0.000 description 1
- 239000003472 antidiabetic agent Substances 0.000 description 1
- 235000006533 astragalus Nutrition 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 208000010247 contact dermatitis Diseases 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000003344 environmental pollutant Substances 0.000 description 1
- 210000001339 epidermal cell Anatomy 0.000 description 1
- 229940045761 evening primrose extract Drugs 0.000 description 1
- 235000008524 evening primrose extract Nutrition 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- MWDZOUNAPSSOEL-UHFFFAOYSA-N kaempferol Natural products OC1=C(C(=O)c2cc(O)cc(O)c2O1)c3ccc(O)cc3 MWDZOUNAPSSOEL-UHFFFAOYSA-N 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 231100000344 non-irritating Toxicity 0.000 description 1
- 235000015097 nutrients Nutrition 0.000 description 1
- 231100000719 pollutant Toxicity 0.000 description 1
- 230000001012 protector Effects 0.000 description 1
- 235000005875 quercetin Nutrition 0.000 description 1
- 229960001285 quercetin Drugs 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- 210000004761 scalp Anatomy 0.000 description 1
- 210000002374 sebum Anatomy 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 210000004233 talus Anatomy 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
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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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
- A61K8/602—Glycosides, e.g. rutin
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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- 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)
- A61K36/49—Fagaceae (Beech family), e.g. oak or chestnut
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- 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
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- A—HUMAN NECESSITIES
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- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
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- A—HUMAN NECESSITIES
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- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
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Abstract
L’invention a pour objet une composition comprenant l’Astragaline (K) et la Miquélianine (Q) dans un ratio massique K/Q compris entre 1/1,5 et 1/3,5. L’invention porte également sur l’utilisation d’une composition selon l’invention, notamment pour prévenir et/ou diminuer la virulence de S. aureus, et/ou pour prévenir et/ou en diminuer les manifestations inconfortables et/ou inesthétiques au niveau de la peau saine et/ou des muqueuses saines, et/ou pour traiter les infections de la peau et/ou des muqueuses causées par S aureus.The subject of the invention is a composition comprising Astragalin (K) and Miquelianin (Q) in a K/Q mass ratio of between 1/1.5 and 1/3.5. The invention also relates to the use of a composition according to the invention, in particular for preventing and/or reducing the virulence of S. aureus, and/or for preventing and/or reducing the uncomfortable and/or unsightly manifestations thereof healthy skin and/or mucous membranes, and/or to treat skin and/or mucous membrane infections caused by S aureus.
Description
L’invention appartient au domaine des compositions dermatologiques ou cosmétiques et notamment des compositions pour prévenir et/ou diminuer la virulence deS. aureuset/ou pour prévenir et/ou en diminuer les manifestations inconfortables et/ou inesthétiques au niveau de la peau saine et/ou des muqueuses saines et/ou pour traiter les infections de la peau et/ou des muqueuses causées parS aureus. L’invention porte en particulier sur une combinaison de deux composés, la kampferol-3-O-glucoside et la quercetin-3-O-glucuronide, ayant un effet synergique, notamment pour inhiber l’activité de la lipase deS aureus.The invention belongs to the field of dermatological or cosmetic compositions and in particular compositions for preventing and/or reducing the virulence of S. aureus and/or for preventing and/or reducing its uncomfortable and/or unsightly manifestations in healthy skin. and/or healthy mucous membranes and/or to treat infections of the skin and/or mucous membranes caused by S aureus . The invention relates in particular to a combination of two compounds, kampferol-3-O-glucoside and quercetin-3-O-glucuronide, having a synergistic effect, in particular for inhibiting the activity of the lipase of S aureus .
Arrière-plan technologiqueTechnology background
Les dermatites sont des inflammations cutanées superficielles, caractérisées par des vésicules, un érythème, un œdème, des lésions suintantes, desquamantes ou croûteuses et des démangeaisons intenses. Il existe différents types de dermatites : les dermatites de contact, qui peuvent être provoquées par des irritants avec lesquels la peau est en contact ou par des substances non irritantes auxquelles le sujet est allergique ; la dermatite atopique, une maladie chronique caractérisée par de fortes démangeaisons; la dermatite séborrhéique, une maladie squameuse qui affecte principalement le visage et le cuir chevelu.Dermatitis is superficial skin inflammation characterized by vesicles, erythema, edema, oozing, scaling or crusty lesions and intense itching. There are different types of dermatitis: contact dermatitis, which can be caused by irritants with which the skin is in contact or by non-irritating substances to which the subject is allergic; atopic dermatitis, a chronic disease characterized by severe itching; seborrheic dermatitis, a scaly disease that primarily affects the face and scalp.
Les dermatites sont notamment induites par un déséquilibre du microbiote cutané qui implique une réduction de la diversité bactérienne et une colonisation majeure par une bactérie opportunisteStaphylococcus aureus (S aureus). La lipase deS aureus(SAL), également connue sous le nom de glycérol ester hydrolase, hydrolyse les triglycérides du sébum en glycérol et acides gras libres. Certains acides gras libres serviront de nutriments et ainsi favorisent la croissance deS aureus. Par ailleurs d’autres acides gras libres tels que l’acide oléique perturbent la fonction barrière de la peau qui devient plus perméable aux allergènes et aux polluants. L’acide oléique est aussi un irritant pour les cellules de l’épiderme qui peut provoquer la sécrétion de cytokines inflammatoires telles que l’interleukine 1 alpha.Dermatitis is notably induced by an imbalance of the skin microbiota which involves a reduction in bacterial diversity and major colonization by an opportunistic bacterium Staphylococcus aureus (S aureus) . S aureus lipase (SAL), also known as glycerol ester hydrolase, hydrolyzes sebum triglycerides into glycerol and free fatty acids. Some free fatty acids will serve as nutrients and thus promote the growth of S aureus . Furthermore, other free fatty acids such as oleic acid disrupt the barrier function of the skin, which becomes more permeable to allergens and pollutants. Oleic acid is also an irritant for epidermal cells which can cause the secretion of inflammatory cytokines such as interleukin 1 alpha.
L’inhibition de l’activité de la lipase deS aureus(SAL) permet donc de traiter les infections de la peau causées parS aureus, et notamment les dermatites.Inhibition of the activity of S aureus lipase (SAL) therefore makes it possible to treat skin infections caused by S aureus , and in particular dermatitis.
L’activité lipase deS. aureusne cause pas nécessairement des pathologies au niveau de la peau et/ou des muqueuses. Sur une peau saine, elle peut également être responsable d’un certain nombre de manifestations inconfortables et/ou inesthétiques comme par exemple la sècheresse cutanée et/ou mucosale, une perte d’homogénéité du teint de la peau et/ou des muqueuses notamment par l’apparition de rougeurs, des sensations de tiraillements, picotements, fourmillements, tension et/ou démangeaisons de la peau et/ou des muqueuses, un aspect rugueux de la peau et/ou des muqueuses et/ou une perte de douceur au toucher. Ces manifestations inconfortables et/ou inesthétiques sont accentuées dans le cas des peaux et/ou muqueuses sensibles, sensibilisées, fragiles, fragilisées, sèches, et/ou à tendance atopique.The lipase activity of S. aureus does not necessarily cause pathologies in the skin and/or mucous membranes. On healthy skin, it can also be responsible for a certain number of uncomfortable and/or unsightly manifestations such as, for example, cutaneous and/or mucosal dryness, a loss of homogeneity in the complexion of the skin and/or mucous membranes, in particular by the appearance of redness, feelings of tightness, tingling, tingling, tension and/or itching of the skin and/or mucous membranes, a rough appearance of the skin and/or mucous membranes and/or a loss of softness to the touch. These uncomfortable and/or unsightly manifestations are accentuated in the case of sensitive, sensitized, fragile, weakened, dry, and/or atopic-prone skin and/or mucous membranes.
Il existe donc un besoin constant d’identifier des inhibiteurs de l’activité de la lipase deS. aureus(SAL) comme alternatives à ceux déjà décrits et commercialisés, notamment pour leur utilisation dans le traitement des pathologies causées parS. aureusnotamment les dermatites mais également pour améliorer l’apparence et/ou le confort des peaux et/ou muqueuses sensibles, sensibilisées, fragiles, fragilisées, sèches, et/ou à tendance atopique.There is therefore a constant need to identify inhibitors of the activity of the lipase of S. aureus (SAL) as alternatives to those already described and marketed, in particular for their use in the treatment of pathologies caused by S. aureus in particular the dermatitis but also to improve the appearance and/or the comfort of sensitive, sensitized, fragile, weakened, dry skin and/or mucous membranes.
La Miquélianine (Q), également appelée quercetin-3-O-glucuronide, est un flavonol de formule (Q) ci-dessous ([Chem 1]). La Miquélianine est notamment connue pour ses propriétés antidiabétique, antioxydant et antidépresseur. Cette molécule est notamment présente dans les végétaux suivants :Castanea sativa(feuilles, fleurs),Hypericum perforatum,Nelumbo nucifera,Gaultheria miqueliana, Adiantum capillus veneris,Phaseolus vulgaris,Achillea millefolium,Arnica montana,Centella asiatica,Foeniculum vulgare,Rubus idaeus, Myrothamnus flabellifolius, Oenothera biennis, Vitis vinifera,,etStrawberry cultivars.Miquelianin (Q), also called quercetin-3-O-glucuronide, is a flavonol of formula (Q) below ([Chem 1]). Miquelianin is particularly known for its antidiabetic, antioxidant and antidepressant properties. This molecule is present in particular in the following plants: Castanea sativa (leaves, flowers), Hypericum perforatum , Nelumbo nucifera , Gaultheria miqueliana, Adiantum capillus veneris, Phaseolus vulgaris , Achillea millefolium , Arnica montana , Centella asiatica , Foeniculum vulgare , Rubus idaeus, Myrothamnus flabellifolius, Oenothera biennis, Vitis vinifera, and Strawberry cultivars .
L’Astragaline (K), également appelée kampferol-3-O-glucoside, est un flavonol de formule (K) ci-dessous ([Chem 2]). Cette molécule se retrouve notamment dans les végétaux suivants :Castanea sativa, Astragalus spetVitis vinifera.L’Astragaline (K) est connue en tant qu’agent anti-inflammatoire, antioxydant, anti-ROS, et protecteur de la peau contre les rayonnements UV et le stress (JP07118151; US7211567 ; et WO2004/037184).Astragalin (K), also called kampferol-3-O-glucoside, is a flavonol with formula (K) below ([Chem 2]). This molecule is found in particular in the following plants: Castanea sativa, Astragalus sp and Vitis vinifera. Astragalin (K) is known as an anti-inflammatory, antioxidant, anti-ROS agent, and protector of the skin against UV radiation and stress (JP07118151; US7211567; and WO2004/037184).
Une combinaison de l’Astragaline avec la Quercétine dans un ratio 1/1 est divulguée dans la demande de brevet coréen KR20120121684, pour son activité sur la dermatite atopique, l’irritation et l’inflammation. Cette combinaison est notamment utilisée pour son activité contre les démangeaisons.A combination of Astragalin with Quercetin in a 1:1 ratio is disclosed in Korean patent application KR20120121684, for its activity on atopic dermatitis, irritation and inflammation. This combination is used in particular for its activity against itching.
Dans ce contexte, les inventeurs ont découvert que la combinaison de deux composés, l’Astragaline (K) et la Miquélianine (Q), permet d’inhiber de manière significative la virulence deS. aureus, en particulier l’activité de la lipase deS aureus(SAL). Cette inhibition est significativement supérieure à l’inhibition induite par chacun des composés pris isolément. Les inventeurs ont donc découvert un effet synergique de la combinaison de l’Astragaline et la Miquélianine, pour inhiber l’activité de la SAL et donc pour diminuer la virulence deS. aureus.In this context, the inventors have discovered that the combination of two compounds, Astragalin (K) and Miquelianin (Q), makes it possible to significantly inhibit the virulence of S. aureus , in particular the activity of lipase of S aureus (SAL). This inhibition is significantly greater than the inhibition induced by each of the compounds taken separately. The inventors have therefore discovered a synergistic effect of the combination of Astragalin and Miquelianin, to inhibit the activity of SAL and therefore to reduce the virulence of S. aureus .
Les inventeurs ont notamment découvert que cette combinaison peut être utilisée comme agent cosmétique, notamment pour améliorer l’apparence et/ou le confort des peaux saines et/ou muqueuses saines, et/ou pour le soin cosmétique des peaux saines et/ou muqueuses saines, notamment sensibles, sensibilisées, fragiles, fragilisées, sèches, et/ou des peaux saines à tendance atopique. Cette combinaison par ses propriétés inhibitrices de l’activité deS. aureuspermet de prévenir et/ou empêcher la dégradation de la barrière cutanée et donc de limiter les pertes insensibles en eau. Elle est donc également utile comme agent apaisant de la peau et/ou des muqueuses et/ou agent hydratant de la peau et/ou des muqueuses. Cette combinaison peut également être utilisée en tant que principe actif dans une composition pharmaceutique ou dermatologique, notamment en tant qu’agent anti-inflammatoire, agent antibactérien en ce qu’elle inhibe la virulence deS. aureuset/ou, dans le traitement et/ou la prévention des infections de la peau causées parS aureustelles que l’eczéma, la dermatite séborrhéique ou atopique, l’acné, et l’inflammation cutanée ou mucosale causée parS. aureus, et/ou de l’érythème en particulier l’érythème fessier du nourrisson, et/ou dans la prévention et/ou le traitement pharmaceutique notamment dermatologique des pathologies liées aux peaux réactives et/ou atopiques. Cette combinaison est utile pour le soin dermatologique des peaux atopiques et/ou réactives et/ou des peaux des nourrissons pour prévenir l’érythème fessier du nourrisson.The inventors have in particular discovered that this combination can be used as a cosmetic agent, in particular to improve the appearance and/or the comfort of healthy skin and/or healthy mucous membranes, and/or for the cosmetic care of healthy skin and/or healthy mucous membranes. , in particular sensitive, sensitized, fragile, weakened, dry, and/or healthy skin with an atopic tendency. This combination by its inhibiting properties of the activity of S. aureus makes it possible to prevent and/or prevent the degradation of the cutaneous barrier and thus to limit the insensible water losses. It is therefore also useful as a soothing agent for the skin and/or the mucous membranes and/or a moisturizing agent for the skin and/or the mucous membranes. This combination can also be used as an active principle in a pharmaceutical or dermatological composition, in particular as an anti-inflammatory agent, an antibacterial agent in that it inhibits the virulence of S. aureus and/or, in the treatment and /or the prevention of skin infections caused by S. aureus such as eczema, seborrheic or atopic dermatitis, acne, and skin or mucosal inflammation caused by S. aureus , and/or erythema in in particular diaper rash in infants, and/or in the prevention and/or pharmaceutical treatment, in particular dermatological treatment, of pathologies linked to reactive and/or atopic skin. This combination is useful for the dermatological care of atopic and/or reactive skin and/or the skin of infants to prevent diaper rash in infants.
Les inventeurs ont également découvert qu’une meilleure synergie est obtenue avec un ratio massique K/Q compris entre 1/1,5 et 1/3,5.The inventors have also discovered that better synergy is obtained with a K/Q mass ratio of between 1/1.5 and 1/3.5.
L’invention a donc pour objet une composition comprenant une combinaison d’Astragaline (K) et la Miquélianine (Q) caractérisée en ce que le ratio massique K/Q est compris entre 1/1,5 et 1/3.5, de préférence entre 1/2 et 1/3.3.A subject of the invention is therefore a composition comprising a combination of Astragalin (K) and Miquelianin (Q) characterized in that the K/Q mass ratio is between 1/1.5 and 1/3.5, preferably between 1/2 and 1/3.3.
La composition selon l’invention est avantageusement destinée à une administration topique.The composition according to the invention is advantageously intended for topical administration.
La composition selon l’invention est avantageusement caractérisée en ce que la combinaison d’Astragaline (K) et la Miquélianine (Q) est comprise dans un extrait végétal, de préférence un extrait de feuilles deCastanea sativa,enrichi en Astragaline (K) et Miquélianine (Q) de manière à présenter un ratio massique K/Q compris entre 1/1,5 et 1/3.5, de préférence entre 1/2 et 1/3.3.The composition according to the invention is advantageously characterized in that the combination of Astragalin (K) and Miquelianin (Q) is included in a plant extract, preferably an extract of Castanea sativa leaves, enriched with Astragalin (K) and Miquelianin (Q) so as to have a K/Q mass ratio of between 1/1.5 and 1/3.5, preferably between 1/2 and 1/3.3.
De manière avantageuse, l’extrait est obtenu par extraction dans l’eau, de préférence à une température comprise entre 70 et 90 °C, par exemple pendant 30 minutes à 2 heures.Advantageously, the extract is obtained by extraction in water, preferably at a temperature of between 70 and 90° C., for example for 30 minutes to 2 hours.
De manière avantageuse, l’extrait comprend la combinaison d’Astragaline (K) et Miquélianine (Q) en une quantité comprise entre 0,001 g/100 ml d’extrait et 1 g/100 ml d’extrait, de préférence 0,01 g/100 ml d’extrait et 0.1 g/100 ml d’extrait, en particulier entre 0.02 g/100 ml d’extrait et 0,03 g/100 ml..Advantageously, the extract comprises the combination of Astragalin (K) and Miquelianin (Q) in an amount of between 0.001 g/100 ml of extract and 1 g/100 ml of extract, preferably 0.01 g /100 ml of extract and 0.1 g/100 ml of extract, in particular between 0.02 g/100 ml of extract and 0.03 g/100 ml.
La composition selon l’invention comprend avantageusement une teneur en la combinaison d’Astragaline (K) et Miquélianine (Q) comprise entre 0,4 et 0,6 % en masse par rapport à la masse totale de la composition.The composition according to the invention advantageously comprises a content of the combination of Astragalin (K) and Miquelianin (Q) of between 0.4 and 0.6% by mass relative to the total mass of the composition.
L’invention a également pour objet une composition cosmétique comprenant une composition selon l’invention et un excipient cosmétiquement acceptable.A subject of the invention is also a cosmetic composition comprising a composition according to the invention and a cosmetically acceptable excipient.
L’invention a également pour objet l’utilisation cosmétique non thérapeutique d’une composition cosmétique selon l’invention, pour prévenir et/ou diminuer les manifestations inconfortables et/ou inesthétiques au niveau de la peau et/ou des muqueuses de la virulence deS. aureuset/ou pour le traitement cosmétique des peaux et/ou muqueuses saines sensibles, des peaux et/ou muqueuses saines sensibilisées, des peaux et/ou muqueuses saines fragiles et/ou fragilisées, des peaux et/ou muqueuses sèches saines, et des peaux et/ou muqueuses saines à tendance atopique, et/ou en tant qu’agent apaisant ou agent hydratant.The invention also relates to the non-therapeutic cosmetic use of a cosmetic composition according to the invention, to prevent and/or reduce the uncomfortable and/or unsightly manifestations on the skin and/or mucous membranes of the virulence of S. aureus and/or for the cosmetic treatment of sensitive healthy skin and/or mucous membranes, sensitized healthy skin and/or mucous membranes, fragile and/or weakened healthy skin and/or mucous membranes, healthy dry skin and/or mucous membranes, and healthy atopic-prone skin and/or mucous membranes, and/or as a soothing agent or moisturizing agent.
L’invention a également pour objet un procédé de soin cosmétique caractérisé en ce qu’il comprend l’application par voie topique sur au moins une zone de peau saine et/ou muqueuse saine d’une composition cosmétique selon l’invention, pour le traitement cosmétique des peaux saines et/ou muqueuses saines sensibles, des peaux saines et/ou muqueuses saines sensibilisées, des peaux saines et/ou muqueuses saines fragiles et/ou fragilisées, des peaux saines et/ou muqueuses sèches saines, et des peaux saines et/ou muqueuses saines à tendance atopique, et/ou en tant qu’agent apaisant ou agent hydratant.The invention also relates to a cosmetic care process characterized in that it comprises the topical application to at least one area of healthy skin and/or healthy mucous membrane of a cosmetic composition according to the invention, for the cosmetic treatment of sensitive healthy skin and/or healthy mucous membranes, sensitized healthy skin and/or healthy mucous membranes, fragile and/or weakened healthy skin and/or healthy mucous membranes, healthy dry skin and/or healthy mucous membranes, and healthy skin and/or healthy atopic-prone mucous membranes, and/or as soothing agent or moisturizing agent.
L’invention a également pour objet une composition pharmaceutique et/ou dermatologique comprenant une composition selon l’invention et un excipient pharmaceutiquement et/ou dermatologiquement acceptable.A subject of the invention is also a pharmaceutical and/or dermatological composition comprising a composition according to the invention and a pharmaceutically and/or dermatologically acceptable excipient.
L’invention a également pour objet une composition pharmaceutique et/ou dermatologique selon l’invention, pour son utilisation en tant qu’agent anti-inflammatoire, agent antibactérien et/ou, dans le traitement et/ou la prévention des infections de la peau et/ou des muqueuses associées àS. aureustelles que l’eczéma, la dermatite séborrhéique ou atopique, l’acné, et l’inflammation cutanée ou mucosale causée parS. aureus, et/ou de l’érythème en particulier l’érythème fessier du nourrisson, et/ou dans la prévention et/ou le traitement pharmaceutique notamment dermatologique des pathologies liées aux peaux réactives et/ou atopiques.The invention also relates to a pharmaceutical and/or dermatological composition according to the invention, for its use as an anti-inflammatory agent, antibacterial agent and/or, in the treatment and/or prevention of infections of the skin. and/or mucous membranes associated with S. aureus such as eczema, seborrheic or atopic dermatitis, acne, and skin or mucosal inflammation caused by S. aureus , and/or erythema in particular the diaper rash in infants, and/or in the prevention and/or pharmaceutical treatment, in particular dermatological treatment, of pathologies linked to reactive and/or atopic skin.
Claims (11)
Pharmaceutical and/or dermatological composition as defined in claim 10, for its use as an anti-inflammatory agent, antibacterial agent and/or, in the treatment and/or prevention of infections of the skin and/or mucous membranes associated with S. aureus such as eczema, seborrheic or atopic dermatitis, acne, and skin or mucosal inflammation caused by S. aureus , and/or erythema, in particular diaper rash, and/or in the prevention and/or pharmaceutical, in particular dermatological, treatment of pathologies linked to reactive and/or atopic skin.
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| FR2114152A FR3130609A1 (en) | 2021-12-21 | 2021-12-21 | Combination of Astragalin and Miquelianin to inhibit S aureus lipase activity. |
| CN202211645411.7A CN116270277A (en) | 2021-12-21 | 2022-12-16 | A combination of astragalin and Mi Kuilian for inhibiting Staphylococcus aureus lipase activity |
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