WO2008059906A1 - Préparation à usage externe pour la peau et préparation à usage externe pour les muqueuses - Google Patents

Préparation à usage externe pour la peau et préparation à usage externe pour les muqueuses Download PDF

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WO2008059906A1
WO2008059906A1 PCT/JP2007/072150 JP2007072150W WO2008059906A1 WO 2008059906 A1 WO2008059906 A1 WO 2008059906A1 JP 2007072150 W JP2007072150 W JP 2007072150W WO 2008059906 A1 WO2008059906 A1 WO 2008059906A1
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Prior art keywords
skin
external preparation
extract
effect
mucosa
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PCT/JP2007/072150
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English (en)
Japanese (ja)
Inventor
Yoshiharu Kawagoe
Masafumi Akatsuka
Yumi Ohara
Original Assignee
Nozaki, Katsunori
Kamata, Yasushi
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Priority claimed from JP2007285634A external-priority patent/JP2008273922A/ja
Application filed by Nozaki, Katsunori, Kamata, Yasushi filed Critical Nozaki, Katsunori
Publication of WO2008059906A1 publication Critical patent/WO2008059906A1/fr

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/73Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics 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
    • A61K8/9755Gymnosperms [Coniferophyta]
    • A61K8/9761Cupressaceae [Cypress family], e.g. juniper or cypress
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics 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
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/08Anti-ageing preparations

Definitions

  • the present invention allows the skin to penetrate the inside of the skin percutaneously by applying, immersing, rubbing or contacting the skin, thereby reducing or fading the stains and soaks that have already been formed.
  • external preparations for skin used to restore the original color of the skin external preparations for external use for skin can be used mainly as basic cosmetics such as lotions, cosmetic creams, bath preparations, soaps for medicinal use, etc.
  • the present invention relates to an external preparation for mucous membrane which exerts an excellent antiallergic action and an antihistamine action by acting on mucous membranes. Background art
  • vitamin C tocopherol
  • SOD dodismutase
  • vitamins C and E are generally unstable, and have an adverse effect on oxidized vitamin A and oxidized vitamin E that are produced after oxidation with active oxygen. It is not satisfactory in terms of points. Synthetic antioxidants with excellent stability tend to be reluctant from recent consumer safety, natural and health concerns.
  • Patent Document 1 discloses, as a melanin production inhibitor based on the inhibition of tyrosinase activity, a skin cosmetic containing a herbal extract such as curcuma versifolium and cucumber.
  • the cucon extract used herein is an extract obtained by extracting the rhizome of cucon with a hydrophilic organic solvent such as water, methanol, or ethanol.
  • crude drug extracts such as banshu, cowpea, and persimmon are excellent in the antioxidant action against unsaturated fatty acid and active oxygen scavenging action, and the external preparation for skin containing these is superior to vitamin E for the improvement of blur.
  • the extract of Bankon used in this case is a hot water extract of the rhizome, an ethanol extract of whole grass, an extract of 1, 3-butylene glycol of the rhizome, and the excellent antioxidant of the extract By action, it is intended to improve skin, skin, skin and dullness.
  • Patent Document 3 discloses water-soluble thickeners such as glycerol and hyaluronic acid Na, antibacterial alcohols such as ethanol, antioxidant vitamins such as tocopherols, and anti-inflammatory agents such as mefenamic acid and tranexamic acid.
  • a cosmetic composition to which a botan extract, a button, an aloe, a carrot, a plant extract such as curcuma has been added as a whitening component.
  • Patent Document 1 Japanese Patent Application Laid-Open No. 6-2 2 7 9 6 0
  • Patent Document 2 Japanese Patent Application Laid-Open No. 200002 1 2 1 1 4 4
  • Patent Document 3 Japanese Patent Application Laid-Open Publication No. 200002-2 0 1 2 0 5 2
  • the scavenging of reactive oxygen species by the antioxidant component is intended to suppress the formation of stains and griefs by ultraviolet irradiation, and against the whitening effects such as reduction, disappearance, and fading of stains and romances that have already been formed, Further improvement is desired.
  • it also has a moisturizing effect to keep the skin moist, inflammation, anti-allergy, and skin lightening effects as long as it is effective in preventing and suppressing skin aging. There is a strong demand for development of such external skin preparations.
  • the present invention has been made in view of these circumstances, and it has a skin-whitening effect to rejuvenate the skin's original color and wrinkles by reducing sunburn due to ultraviolet irradiation, reducing stains due to aging and fading off. At the same time, it is effective in removing active oxygen, moisturizing, inflammation, anti-allergy, prevention of skin aging, etc., and it is possible to obtain a more beautiful skin effect.
  • An external preparation for skin which can be expected to treat or alleviate eryrgic dermatitis and the like, and an external preparation for mucous membrane which exerts an excellent antiallergic action and an antihistaminic action by acting on mucous membranes To aim. Means to solve the problem
  • the external preparation for skin of the present invention is characterized in that it contains an extract of leaves and Z or a stem of a plant belonging to the genus Rosaceae of the family Rosaceae as an active ingredient.
  • the external preparation for mucous membrane of the present invention is characterized by containing extracts of leaves and stems of a plant belonging to the genus Rosaceae of the family Rosaceae as active ingredients. Effect of the invention
  • the external preparation for skin of the present invention is percutaneously incorporated into the skin to inhibit the activity of tyrosinase, thereby suppressing the formation of melanin which is a cause of the stain, and further along with the turnover of the skin. Since it can be expected to reduce stains and stains that have already been made, it is effective as a whitening essence to be added to cosmetics and bath agents. In addition to the tyrosinase inhibitory activity effect, the external preparation for skin of the present invention also exhibits an active oxygen scavenging effect because it exhibits an excellent SOD-like activity value.
  • the external preparation for skin of the present invention exhibits excellent hyaluronidase inhibition value together with tyrosinase inhibitory activity effect and active oxygen scavenging effect, and thus a moisturizing effect for keeping the skin moist, inflammation, anti-allergy One symptom ⁇
  • a moisturizing effect for keeping the skin moist, inflammation, anti-allergy One symptom ⁇ A more beautiful skin effect can be obtained if it is effective in preventing and suppressing skin aging.
  • due to its excellent anti-allergic action it can also be expected to have a therapeutic or alleviating effect on allergies such as dermatitis.
  • the external preparation for mucous membrane of the present invention acts on the mucous membrane to exert an excellent anti-allergic action and anti-histamine action, and in particular, acts on the nasal mucous membrane to alleviate the symptoms of so-called pollinosis such as runny nose and sores. Can. Brief description of the drawings
  • Fig. 1 Fraction of strawberry leaf extract and measurement results of tyrosinase inhibitory activity.
  • Figure 3 shows the structural formula of q u e r c t i n — 3 — o — D — g l.
  • Figure 5 shows the estimated structure of C o m p o u n d 1
  • FIG. 8 Spectrum of 13 C- NMR of Casuarictin.
  • Figure 9 shows the structural formula of C asuarictin.
  • the external preparation for skin of the present invention contains the extract of leaves and Z or stems of a Rosaceae L. plant as a active ingredient.
  • Rosaceae family Dutch strawberry plant used in the present invention if it is a so-called edible Dutch strawberry, it is possible to use a variety of mulberry species.
  • mulberry species For example, Toyo Noka, Nyoho, Tochiotome, Chapter princess (Akihime), Iberly, Tochihime, Red pearl, Sachi's power Ama, Treasure early birth, Benihopope, etc. Plants can be used.
  • the plant to be used needs to be a plant belonging to the genus Rosaceae, but not intended to be limited to the above-mentioned varieties.
  • an extraction solvent used to extract an extract of the genus Rosaceae L. planta the purpose of use of the product to be provided, type or processing to be performed later although it may be selected in consideration of the etc., it is preferable to use the extract of leaves and Z or stem of the above-mentioned Rosaceae Lubifer plant as extract extracted with water and / or alcohol. By doing this, it is considered that it is possible to extract effectively without destroying the effective ingredients for the beautifying skin.
  • lower alcohols such as methanol, ethanol, propyl alcohol, isopro pinole alcohol, butanol, etc .
  • polyhydric alcohols such as propylidene alcohol, 1, 3-butyleneglycolone, glycerin etc. are used. be able to. These can be used alone or in combination.
  • the extraction may be performed in multiple steps, for example, extraction with leaves of leaves and stems of the genus Rosaceae and the stem with water and then extraction with medanol, but in order to increase the content of the whitening component It is preferable to include an extraction step with a mixture of water and ethanol.
  • the extract-containing solution extracted with these solvents may be used as it is as a skin external preparation, or may be used after being subjected to processing such as concentration, dilution, filtration, drying and the like as necessary.
  • the alcohol may be volatilized by drying or the like to obtain a powder having a high content of the whitening component.
  • the leaves and stems of the above-mentioned Rosaceae Lubiferus plants can be used as long as the plants are grown as edible fruits. It is preferred to use. This is because leaves and / or stems after fruit harvest which have been conventionally discarded are effectively used from the viewpoint of recycling.
  • the leaves and Z or stalks of the above-mentioned Rosaceae L. plant are collected and can be extracted with water and Z or alcohol as they are. Forced after extraction, natural drying or artificial After being dried Extraction with water and / or alcohol is preferred. By doing this, it is considered that the extract concentrated by drying can be extracted. In addition, drying stabilizes the condition of leaves and green leaves or stems, reduces variations in conditions, stabilizes the quality of the extract to be extracted, and improves the shelf life of leaves and Z or stems. This is because the handling is significantly improved.
  • the extraction method may be extraction with water only or alcohol only, or extraction with a mixture of water and alcohol. It can also be extracted by heating, but extraction at normal temperature is preferred. It is because it is thought that the breakage of the extract due to heating is reduced and the effective ingredient for the beautifying skin is effectively extracted.
  • the external preparation for skin of the present invention may be used by adding the extract of leaves and Z of stem or sock of the Rosaceae family to an appropriate solvent and base, or the extract as an essence, and cosmetics. Or add it to quasi-drugs. More specifically, skin cleansing agents such as cleansing creams, cleansing lotions, facial cleansing creams, soaps, etc. as well as whitening agents; moisturizing lotions, soft lotions, skin conditioning agents such as astringent lotions; Milky lotions Protection agents such as emollient milk and vanishing cream; activators such as massage cream, massage system, foam pack, peel off pack etc .; bath additives; and whitening agents may be added as whitening ingredients. In any case, the active ingredient is incorporated into the skin and can be used to cause stains and buckwheat discoloration, reduction and disappearance.
  • the content ratio of leaf and Z or stem extract of Rosaceae L. plant in the final product is appropriately selected according to the type of final product, but in the case of cosmetics, about 1 to 80 mass% is preferable .
  • the external preparation for skin of the present invention does not impair the effect of the extract depending on the final product.
  • base moisturizer, thickener, surfactant, pH adjustment agent, preservative, fragrance, moisturizer, UV absorber, thickener, pigment, antioxidant, chelate component can do.
  • solid oily raw materials such as beeswax, cacao oil; carnaval roux, higher fatty acids, solid paraffin, cetyl alcohol, stearyl alcohol etc .; semi-solid oily raw materials such as wa- seline, lanolin etc; Leave oil, castor oil, palm oil, peanut oil, liquid paraffin, oleic acid, linoleic acid, octoyldodecyl dodecyl myristate, silicone oil, etc. can be used.
  • moisturizing agents such as glycerin, sorbitol, polyethylene glycol, pyrrolidone carboxylic acid and salts thereof, collagen, hyaluronic acid and salts thereof, chondroitin sulfate and salts thereof, and the like; And polyvinyl cinolea / leconole, xanthan gum, ruboxy vinyl polymer, hydroxy propyl cellulose, thickeners such as arabic gum, and the like are used.
  • non-ionic surfactants such as polyethylene glycol isostearylate, sorbitan stearate, glyceryl fatty acid ester, polyoxyethylene hexyl decyl ether, etc .; sodium lauryl sulfate, lauryl phosphate
  • Anionic surfactants such as sodium phosphate
  • cationic surfactants such as stearyldimethylbenzyl ammonium
  • natural surfactants such as sucrose fatty acid ester, sodium caseinate, lecithin, collagen etc.
  • pH adjusters examples include carbonated lithium, sodium bicarbonate, ammonium bicarbonate and the like.
  • paradimethylamino benzoic acid, urocanic acid ethyl, diisopropyl cinnamic acid ethyl, and 2-hydric acid may be added as required.
  • UV absorbers such as droxy 4-methoxybenzophenone and salicylate triethanolamine; preservatives such as cetylparaben and butylparaben; glycyrrhizinic acid derivatives, glycyrrhetinic acid derivatives, salicylic acid derivatives, Hinokitiol, zinc oxide, allan Anti-inflammatory agents such as toin etc.
  • Vitamins A such as retinol palmitate, vitamins B such as riboflavin, nicotinic acid amide, vitamins D such as colecalciferol, d 1 ⁇ ⁇ -tocopherol etc.
  • Antioxidants such as vitamins and cetaceans; antioxidants such as sodium sorbirate sodium, sage extract, parahydroxyl sole, etc .; active agents such as royal jelly, collesterol derivative various amino acids; ⁇ — orizanol , Blood circulation enhancers such as sodium dextran sulfate; It includes other plant extracts; low force Sami down, colorant safflower like.
  • Extract sample 1 (leaf) and extract sample 2 (stem) were examined for their inhibitory effect on tyroxinase activity, an enzyme involved in the formation of melanin.
  • Tyrosinase (EC1.14.18.1) is a bioenzyme that oxidizes L-tyroosine to L-DOPA and oxidizes L-DOPA to DOPA-quinone. Since DOPA quinone is a causative agent of melanine which is a causative agent of stains and freckles, it is considered that inhibiting tyrosinase can prevent the formation of stains and freckles.
  • the sample (20 ⁇ L) dissolved in phosphate buffer (pH 6. 8) containing 20% DM SO was suspended on a substrate (100; z L) containing 0.1 ML-DO.
  • the turbid enzyme solution (mushroom-derived tyrosinase 30 U, manufactured by SIGMA, 20 ⁇ L ⁇ ) was thoroughly mixed and subjected to enzyme reaction for 15 minutes in a thermostat bath at 37 ° C. After that, 0.1 N aqueous solution of HCl (20 ⁇ L) was added as a reaction stop solution (S).
  • S reaction stop solution
  • the phosphate buffer pH 6.8 was used as a measurement blank, and the absorbance at 45 nm was measured, and the tyrosinase inhibition rate (%) was calculated according to formula 1.
  • the sample concentration was 5 mg zml (water dilution).
  • Inhibition rate (%) B 1-(S-S ⁇ B 1) / B 1 X 1 0 0-. '(Equation 1) [S OD like activity; active oxygen scavenging effect]
  • tyrosinase is triggered by active oxygen generated by ultraviolet light and is produced in cells called melanosite present in the basal layer of the skin. Be That is, in addition to the inhibition of tyrosinase, if it is possible to effectively suppress the active oxygen causing the activity of tyrosinase, it is considered that a whitening effect can be expected.
  • the reactive oxygen inhibition effect was measured according to a standard operation method using S O D A c t i t i d i d t e i t i t i o i K i t (manufactured by Wako Pure Chemical Industries, Ltd.). That is, a coloring reagent (containing 0.5 ⁇ m of xanthine and 0.42 ⁇ m of nitro bluet triazolium) in 10 ⁇ l of a sample solution dissolved in distilled water containing a 20% aqueous solution of DM SO. 1 phosphate buffer ( ⁇ ⁇ 8. 0)) 0. lm L was added and stirred for 1 minute.
  • an enzyme suspension (a suspension of 0.10 4 9 U ml of Xanthine Oxidase (derived from Buttermilk) in 0.1 M phosphate buffer (pH 8. 0)) 0.1 m
  • the mixture was allowed to react for 28 minutes in a 37 ° C constant temperature bath, and then the reaction stopping solution (69 O mM sodium dodecyl sulfate, 20 L) was added rapidly and stirred for 5 minutes (S ).
  • the concentration of the sample was 100 ⁇ g / mL (water dilution).
  • Reactive oxygen inhibition rate (%) (B 1-B 1 ⁇ B 1)-(S-S ⁇ B 1) / (B 1-B 1 ⁇ B 1) X 1 0 0 ⁇ ⁇ ⁇ ⁇ (Equation 2)
  • the enzyme activity is N-acetyl hexoside produced by hydrolysis of hyaluronic acid.
  • the increase in reducing power of tetrasaccharides having a reducing end with samin was measured by colorimetric determination with absorbance at 585 nm (Goery Journal, 31: 23-3237, 19) 9 0).
  • ⁇ P-DA reagent 10 g of p-DAB, 2.5 m 1 of 10 N hydrochloric acid solution, and 8 7.5 m 1 of acetic acid were mixed and diluted 10-fold with acetic acid immediately before use.
  • sample solution 200 ⁇ l diluted with water was mixed with 5 mg 1 and hyaluronidase 100 / il (40 0 n i t s) mixed and cultured at 37 ° C. for 20 minutes.
  • Reaction solution 1401 and p-DAB solution 600 AZ 1 were mixed and incubated at 37 ° C. for 20 minutes. 7) Absorbance at 585 nm was measured.
  • the measurement samples of S amp 1 e, C ontro 1, S-B lank and C-B lank prepared according to Table 1 below are prepared and their respective absorbances are measured, and the hyaluronidase inhibition rate (inhibition from Activity) was calculated.
  • the X mark indicates that the above-mentioned acetate buffer was used instead of the solution in the left column.
  • Hyalid nidase inhibition rate (%) (C-C-B L)-(S-S-B L) / (S-S-B L) X I O O- ⁇ '(Equation 3)
  • Table 2 The measurement results of the tyrosinase inhibition rate, the S OD-like activity, and the hyaluronidase inhibition rate measured as described above are shown in Table 2 below. As a comparative example, measurement results of extracts obtained by similarly extracting the leaves of Niugori are also shown. Table 2 Sample Tyrosinase inhibition rate (%) SOD-like activity (3 ⁇ 4) Hyaluronidase inhibition rate (%) Strawberry leaf 81.1 99.5 97.0
  • Examples (Extract samples 1 and 2) have extremely high values of tyrosinase inhibition rate, SOD-like activity, and hyaluronidase inhibition rate.
  • the comparative example hardly inhibits the hyaluronidase inhibition rate, and has a significantly low value for the tyrosinase inhibition rate and the SOD-like activity.
  • Extract sample 1 (leaf) was prepared at 200 c c and mixed and diluted in 400 c c glycerol to prepare a cosmetic.
  • Paneler 2 (woman of 65 years old): The stain of about 10 yen hardening has broken. In addition, it has very high moisturizing properties and fine-grained skin, and there is more than double the extension of the foundation.
  • Paneler 3 (a woman of 64 years old): The overall age spots became pale, and it was said that the skin became white. I have no experience so far It is moisturizing.
  • Paneler 4 (40-year-old woman): Although it is dry skin, after using the sample products, it became possible to feel a sense of security without taking any care. In addition, the number of blowouts due to the quality of allergies has decreased.
  • Paneler 5 (36-year-old woman): It was felt that the pores became large and cosmetic makeup was bad after one use. Moreover, I was getting darker around my eyes.
  • Paneler 6 (34-year-old woman): I found that the difference in cosmetic makeup was clear when used only once. Things like Kusumi in the whole face have disappeared. In addition, after being well moisturized, I have not been doing anything until now.
  • Paneler 7 (Male, 51 years old): Some buckwheat have become thinner and smaller. I noticed in about 10 days.
  • Paneler 8 (65-year-old man): The skin was oily and bothersome, but the sample became used and the oiliness was improved and nothing bothered. In addition, when the remaining sample is used only in the left hand, it becomes white, and I am surprised that the difference between the right hand and the color is clearly seen.
  • the cosmetic composition of the present invention is very moisturizing, and is effective in decolorization, reduction, and elimination of Shiva, etc. Also, many of the participants commented that most of the participants said, "The skin seems to have revived.” Also, there was no such thing as side effects such as itching or irritation.
  • the sample (87. 6 g) crushed by hand with a finger and crushed to several mm to several cm is mixed with 50% aqueous ethanol solution (1.8 1) Immersed in 1) and extracted at room temperature for 3 days. After the obtained extract was filtered, the above sample was added to a solution to which the same amount of 50% aqueous ethanol solution was added again, and extraction was performed for 3 days at normal temperature. The extracts after filtration were combined and concentrated under reduced pressure until the volume became 50 cc to obtain a solution solution of 50% ethanol extract of Dutch strawberry leaves.
  • the enzyme solution (mushroom-derived tyrosinase 30 U, manufactured by SIGMA, 2 ⁇ M) was mixed well and subjected to enzyme reaction in a thermostat at 37 ° C. for 15 minutes. After that, 0.1 NHCL aqueous solution (20 ⁇ l) was added as a reaction stop solution (S).
  • S reaction stop solution
  • the above-described extract sample solution showed 81. 1% tyrosinase inhibitory activity.
  • the above extract (about 20. 4 g) is liquid-liquid partitioned between water and ethyl acetate to obtain a water fraction (about 11. 4 g) and an ethyl acetate fraction (about 2.6 g).
  • the water fraction showed 79.5% tyrosinase inhibitory activity, which was higher than 47.8% of the ethyl acetate fraction.
  • the above water fraction was fractionated with DI ANON HP-20 column chromatography, and the water fraction (about 3.9 g), the fraction eluted with 25% methanol aqueous solution (about 1. 9 g), 50% methanol aqueous solution elution fraction (about 1.3 g), The fraction eluted with 75% aqueous methanol solution (about 134.0 mg) and the fraction eluted with methanol (about 33.9 mg) were obtained.
  • the respective tyrosinase inhibitory activity was 20. 1% in water fraction, 87.8% in 25% methanol aqueous solution eluted fraction,
  • the fraction eluted with 50% methanol aqueous solution is 75.5%, the fraction eluted with 75% methanol aqueous solution is 55.1%, and the fraction eluted with methanol is 18.2%,
  • Dissolution solvent 18% acetonitrile
  • UV detector 2 5 4 n m, 3 3 0 n m
  • Reactive oxygen suppression effect is S OD A ctivity D etection It measured according to the standard procedure using Kit (made by Wako Pure Chemical Industries, Ltd.). That is, the color reagent (Xanthine 0.4 M and NitroBluete trazolium 0.24 ⁇ m contained) in 10 ⁇ L of the sample solution dissolved in distilled water containing 20% aqueous DM 2 SO 4. 1 M phosphate buffer ( ⁇ ⁇ 8. 0)) 0. lm L was added and stirred for 1 minute. Enzyme suspension (Xanthine oxidase (derived from Buttermilk) 0. OS UZmL suspended in 0. IM acid buffer (pH 800) 0. 1 ml added to 0.
  • Kit made by Wako Pure Chemical Industries, Ltd.
  • Reactive oxygen inhibition rate (%) (B 1-B 1 ⁇ B 1)-(S-S ⁇ B 1) / (B 1-B 1 ⁇ B 1) X 1 0 0 ⁇ ⁇ ⁇ ⁇ (Equation 5)
  • F r. 2, F r. 3 and F r. 4 are respectively C ompound 1, C ompound 2 and C ompound 3, mass spectrometry (F AB-MS), nuclear magnetic resonance spectroscopy ( Structural analysis was performed by NMR) and the like.
  • F AB-MS mass spectrometry
  • NMR nuclear magnetic resonance spectroscopy
  • C o m p o u n d 3 was identified as q u e r c e t i n-3-o-D-g 1 u c u r o n i d e.
  • the structure is shown in Fig.3.
  • C o m p o u n d 1 is a compound obtained by adding a sugar having 4 ash to C o m o p o u n d 3 (q u e r c e t i n-3-o _ D-g 1 u c u r o n i d e).
  • the estimated structure of Com po u n d 1 is shown in Fig.5.
  • C ompound 2 is a compound having many hydroxyl groups. Further, the 13 C-NMR spectrum of C ompound 2 shown in FIG. 7 is very similar to the 13 C- NMR spectrum of C asuarictin shown in FIG. 8. Figure 9 shows the structural formula of Casuarictin.
  • C ompound 3 is very likely to be a hydrolyzable derivative of tannic acid, and 4 to 5 gallic acid esters are present around a sugar having 6 carbons such as C asuarictin. It can be inferred that the structure has something like a bond. However, because the carbon number of C o m p o u n d 2 is as large as 66, it is suggested that the two types of compounds may be mixed as an isomer.
  • Compo n d 2 exhibited high tyrosinase inhibitory activity as compared to the activity indicator substance, albumin.
  • C o m p o u n d 1 and 3 showed an S OD-like activity almost similar to that of the activity indicator (+)-force tekin. From the above results, it can be said that C o m p o u n d 1 to 3 are physiologically active substances contained in strawberry leaves.
  • Paneler 2 (Housewife 4 and 7 years old): My hobby is gardening, but when pollen was about to fly, I was plagued by hay fever. "If I apply it to the nasal cavity,” I have a strawberry leaf extract, and if I apply it with a cotton swab, I get a squeeze once and only blow my nose. I could do gardening comfortably until the evening.
  • Paneler 3 (Housewife 3 to 8 years old): Every time I washed the laundry out because of hay fever, I had a hard time thinking. I applied the strawberry leaf extract and was convinced that if it was a strawberry, I applied it to the nasal cavity with a cotton swab, and I was happy because the bad runny nose stopped and it worked for a long time. I can not let go.
  • Paneler 4 (Instructor 2 6 years old): I went to work by bicycle, but my nose was blocked, sore, and my runny nose stopped working. It was in the state where I could not do makeup. One day, I applied it to my nasal cavity and got a sample of fig leaf extract, and I used it immediately, and I had a runny nose, sneezing, and a bitter stuffy nose. Please sell products that are effective against rhinitis so quickly.
  • Paneler 5 A full-time housewife 5 4 years old: I really appreciate the strawberry leaf extract. I went to the doctor and gave me various medicines, but I also had problems with my stomach and getting concerned. The strawberry leaf extract smells better, and I prefer house dust than hay fever, but the mucous membranes become loose and exfoliate, nosebleeds, stuffy nose, and runny nose does not stop. Was in the middle of the year. Because of that, thanks to the strawberry leaf extract, the mucous membranes are normal, the nose is not clogged, and the nasal discharge is not much. A quick product for many suffering people.
  • Paneler 6 (unemployed old man 7 2 years old): I go to the pool every day, Even if you get older, you suddenly have hay fever. At first I went to the doctor's office thinking that I had a cold, and I was diagnosed with hay fever. I thought this age, but I got a medicine from a doctor, but it didn't work very well. A clerk from the pool told me, “I put a strawberry leaf extract on a cotton swab and applied it to the nose hole”. After about 15 minutes of painting, the runny nose and sneezing stopped. If it is good, I will have you kindly when I raise a sample. I am now happy to be in the pool. It has immediate effect, and it smells good even if it's painted in the nose, so I spend my time in good mood. Please make it a product soon.
  • Paneler 7 (38-year-old housewife): Even though I took measures against pollinosis such as injection for a month or more and burning the mucous membranes of the nose in anticipation of flying pollen, the painful symptoms did not change from the previous year. The When I applied the strawberry leaf extract to the back of my nose with a cotton swab, it became very easy. As conventional medicines cause stomach upset and side effects such as having to take stomach medicines appear, I would like you to use strawberry leaf extract as a product.
  • Paneler 8 (64-year-old housewife): Pollinosis history 20 years. If this time was this, I gave up, but when I applied the strawberry leaf extract to the back of the nasal cavity, in the moment Kushami went out five times in a row, and it became very easy from now on, when I had a runny nose. I can breathe suussu with my nose. Also, it was easier for my eyes to be crushing. In the past, it was difficult to make the nasal mucous membrane a power subta, and when I took it I got nosebleed, and then I made a physical subta and repeated it, but the strawberry leaf extract was repeated 3 times a day. I have been able to spend an easy day by painting four times.
  • Hay fever is the most important nose to breathe, so I thought that I would be glad if I could apply for this medicine, because I had been suffering for many years.
  • it was very easy with strawberry leaves.
  • it acts on the mucous membrane to exert excellent anti-allergic and antihistamine actions, and in particular it acts on the nasal mucous membrane to alleviate the symptoms of so-called pollinosis such as runny nose and mucilage, etc.
  • It can be used as an external preparation for mucous membranes such as mucous membranes.
  • therapeutic and alleviating effects such as allergic dermatitis can be expected.
  • the external preparation for skin of the present invention has a high tyrosinase activity inhibitory action and also an antibacterial activity, it is an external preparation for skin care intended for the prevention of acne and stains and treatment including skin lightening cosmetics. Can be used. It can also be used as an external preparation for mucous membranes such as nasal mucous membranes.

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Abstract

L'invention concerne une préparation à usage externe pour la peau, permettant d'améliorer l'aspect de cette dernière par un effet de suppression de l'oxygène actif, d'hydratation, de prévention des inflammations, anti-allergique, ou de prévention du vieillissement ou analogues, combiné à un effet de blanchiment; et une préparation à usage externe pour les muqueuses exerçant une excellente action antiallergique et antihistaminique au niveau de la muqueuse. La préparation à usage externe pour la peau contient un extrait de feuilles et/ou de tiges d'une plante appartenant au genre Fragaria de la famille des Rosacées en tant qu'ingrédient actif. Cette préparation à usage externe pour la peau permet d'améliorer l'aspect de la peau par un effet de suppression de l'oxygène actif, d'hydratation, de prévention des inflammations, antiallergique, ou de prévention du vieillissement ou analogues, et possède en outre un effet blanchissant permettant de restaurer la couleur et l'éclat d'origine de la peau en réduisant, en atténuant ou en éliminant la pigmentation ou les taches apparaissant avec le vieillissement. La préparation à usage externe pour les muqueuses possède une excellente action antiallergique et antihistaminique au niveau de la muqueuse, et permet en particulier de soulager les symptômes de la rhinite dite 'rhume des foins', tels que l'écoulement nasal où les éternuements, en agissant sur la muqueuse nasale.
PCT/JP2007/072150 2006-11-14 2007-11-08 Préparation à usage externe pour la peau et préparation à usage externe pour les muqueuses WO2008059906A1 (fr)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
JP2006-307365 2006-11-14
JP2006307365 2006-11-14
JP2007-099276 2007-04-05
JP2007099276 2007-04-05
JP2007-285634 2007-11-02
JP2007285634A JP2008273922A (ja) 2006-11-14 2007-11-02 皮膚外用剤および粘膜外用剤

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WO2008059906A1 true WO2008059906A1 (fr) 2008-05-22

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Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH03188014A (ja) * 1989-12-15 1991-08-16 Shiseido Co Ltd 化粧料
JPH03188008A (ja) * 1989-12-15 1991-08-16 Shiseido Co Ltd 化粧料
WO1997002807A1 (fr) * 1995-07-07 1997-01-30 C 3 D Composition dermocosmetique depigmentante et son utilisation
JP2002179586A (ja) * 2000-12-15 2002-06-26 Fancl Corp リパーゼ阻害剤
JP2003261454A (ja) * 2002-03-06 2003-09-16 Pias Arise Kk 抗炎症剤、PGE2産生抑制剤、IL−1α産生抑制剤及びIL−6産生抑制剤
JP2003261455A (ja) * 2002-03-07 2003-09-16 Pias Arise Kk 抗アレルギー剤
JP2004115466A (ja) * 2002-09-27 2004-04-15 Toyo Shinyaku:Kk 皮膚外用剤
JP2004123622A (ja) * 2002-10-03 2004-04-22 Toyo Shinyaku:Kk 血流改善外用剤
JP2004131500A (ja) * 2002-09-19 2004-04-30 Fancl Corp 皮膚老化防止剤又は改善剤

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH03188014A (ja) * 1989-12-15 1991-08-16 Shiseido Co Ltd 化粧料
JPH03188008A (ja) * 1989-12-15 1991-08-16 Shiseido Co Ltd 化粧料
WO1997002807A1 (fr) * 1995-07-07 1997-01-30 C 3 D Composition dermocosmetique depigmentante et son utilisation
JP2002179586A (ja) * 2000-12-15 2002-06-26 Fancl Corp リパーゼ阻害剤
JP2003261454A (ja) * 2002-03-06 2003-09-16 Pias Arise Kk 抗炎症剤、PGE2産生抑制剤、IL−1α産生抑制剤及びIL−6産生抑制剤
JP2003261455A (ja) * 2002-03-07 2003-09-16 Pias Arise Kk 抗アレルギー剤
JP2004131500A (ja) * 2002-09-19 2004-04-30 Fancl Corp 皮膚老化防止剤又は改善剤
JP2004115466A (ja) * 2002-09-27 2004-04-15 Toyo Shinyaku:Kk 皮膚外用剤
JP2004123622A (ja) * 2002-10-03 2004-04-22 Toyo Shinyaku:Kk 血流改善外用剤

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