CN108524478A - Application of sanshool in preparation of external preparation for repairing skin photodamage - Google Patents
Application of sanshool in preparation of external preparation for repairing skin photodamage Download PDFInfo
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- CN108524478A CN108524478A CN201810595681.9A CN201810595681A CN108524478A CN 108524478 A CN108524478 A CN 108524478A CN 201810595681 A CN201810595681 A CN 201810595681A CN 108524478 A CN108524478 A CN 108524478A
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- Prior art keywords
- sanshool
- cosmetics
- purposes
- drug
- hydroxyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 229920001144 Hydroxy alpha sanshool Polymers 0.000 title claims abstract description 46
- PSKIOIDCXFHNJA-UHFFFAOYSA-N Sanshool Natural products CC=CC=CC=CCCC=CC=CC(=O)NC(C)C PSKIOIDCXFHNJA-UHFFFAOYSA-N 0.000 title claims abstract description 46
- SBXYHCVXUCYYJT-UEOYEZOQSA-N alpha-Sanshool Chemical compound C\C=C\C=C\C=C/CC\C=C\C(=O)NCC(C)C SBXYHCVXUCYYJT-UEOYEZOQSA-N 0.000 title claims abstract description 41
- 230000008832 photodamage Effects 0.000 title claims abstract description 21
- 238000002360 preparation method Methods 0.000 title claims description 10
- 239000002537 cosmetic Substances 0.000 claims abstract description 18
- 239000003814 drug Substances 0.000 claims abstract description 16
- 229940079593 drug Drugs 0.000 claims abstract description 15
- VKUYLANQOAKALN-UHFFFAOYSA-N 2-[benzyl-(4-methoxyphenyl)sulfonylamino]-n-hydroxy-4-methylpentanamide Chemical compound C1=CC(OC)=CC=C1S(=O)(=O)N(C(CC(C)C)C(=O)NO)CC1=CC=CC=C1 VKUYLANQOAKALN-UHFFFAOYSA-N 0.000 claims abstract description 11
- 102000000380 Matrix Metalloproteinase 1 Human genes 0.000 claims abstract description 11
- 108010016113 Matrix Metalloproteinase 1 Proteins 0.000 claims abstract description 11
- 102100030416 Stromelysin-1 Human genes 0.000 claims abstract description 11
- 101710108790 Stromelysin-1 Proteins 0.000 claims abstract description 11
- 239000000284 extract Substances 0.000 claims abstract description 10
- 210000002950 fibroblast Anatomy 0.000 claims abstract description 10
- 230000035755 proliferation Effects 0.000 claims abstract description 8
- 108010037362 Extracellular Matrix Proteins Proteins 0.000 claims abstract description 6
- 102000010834 Extracellular Matrix Proteins Human genes 0.000 claims abstract description 6
- 230000015556 catabolic process Effects 0.000 claims abstract description 6
- 238000006731 degradation reaction Methods 0.000 claims abstract description 6
- 210000002744 extracellular matrix Anatomy 0.000 claims abstract description 6
- 230000002500 effect on skin Effects 0.000 claims description 15
- 239000000126 substance Substances 0.000 claims description 11
- 229940116257 pepper extract Drugs 0.000 claims description 9
- 244000089698 Zanthoxylum simulans Species 0.000 claims description 8
- LHFKHAVGGJJQFF-UHFFFAOYSA-N hydroxyl-alpha-sanshool Natural products CC=CC=CC=CCCC=CC(=O)NCC(C)(C)O LHFKHAVGGJJQFF-UHFFFAOYSA-N 0.000 claims description 8
- 208000028990 Skin injury Diseases 0.000 claims description 5
- 239000000835 fiber Substances 0.000 claims description 5
- KVUKDCFEXVWYBN-UHFFFAOYSA-N gamma-sanshooel Natural products CC=CC=CC=CCCC=CC=CC(=O)NCC(C)C KVUKDCFEXVWYBN-UHFFFAOYSA-N 0.000 claims description 5
- KVUKDCFEXVWYBN-FMBIJHKPSA-N N-Isobutyl-2,4,8,10,12-tetradecapentaenamide Chemical compound C\C=C\C=C\C=C\CC\C=C\C=C\C(=O)NCC(C)C KVUKDCFEXVWYBN-FMBIJHKPSA-N 0.000 claims description 3
- 239000000463 material Substances 0.000 claims description 3
- 238000011282 treatment Methods 0.000 claims description 3
- LHFKHAVGGJJQFF-UMYNZBAMSA-N (2e,6e,8e,10e)-n-(2-hydroxy-2-methylpropyl)dodeca-2,6,8,10-tetraenamide Chemical compound C\C=C\C=C\C=C\CC\C=C\C(=O)NCC(C)(C)O LHFKHAVGGJJQFF-UMYNZBAMSA-N 0.000 claims description 2
- 102000008186 Collagen Human genes 0.000 claims description 2
- 108010035532 Collagen Proteins 0.000 claims description 2
- 102000002274 Matrix Metalloproteinases Human genes 0.000 claims description 2
- 108010000684 Matrix Metalloproteinases Proteins 0.000 claims description 2
- SBXYHCVXUCYYJT-UMYNZBAMSA-N beta-sanshool Chemical compound C\C=C\C=C\C=C\CC\C=C\C(=O)NCC(C)C SBXYHCVXUCYYJT-UMYNZBAMSA-N 0.000 claims description 2
- 229920002678 cellulose Polymers 0.000 claims description 2
- 239000001913 cellulose Substances 0.000 claims description 2
- 229920001436 collagen Polymers 0.000 claims description 2
- 239000000470 constituent Substances 0.000 claims description 2
- 229920001971 elastomer Polymers 0.000 claims description 2
- 239000000806 elastomer Substances 0.000 claims description 2
- KVUKDCFEXVWYBN-JDXPBYPHSA-N gamma-sanshool Chemical compound C\C=C\C=C\C=C/CC\C=C\C=C\C(=O)NCC(C)C KVUKDCFEXVWYBN-JDXPBYPHSA-N 0.000 claims description 2
- 229920005610 lignin Polymers 0.000 claims description 2
- 230000001737 promoting effect Effects 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 abstract description 8
- 208000024891 symptom Diseases 0.000 abstract description 3
- 210000003491 skin Anatomy 0.000 description 17
- 241000699666 Mus <mouse, genus> Species 0.000 description 9
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 8
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 8
- 210000004027 cell Anatomy 0.000 description 8
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 description 8
- 229920005573 silicon-containing polymer Polymers 0.000 description 8
- 238000012360 testing method Methods 0.000 description 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 6
- 230000006378 damage Effects 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 238000002835 absorbance Methods 0.000 description 5
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 150000002148 esters Chemical class 0.000 description 4
- 238000000605 extraction Methods 0.000 description 4
- 229930182478 glucoside Natural products 0.000 description 4
- 150000008131 glucosides Chemical class 0.000 description 4
- 235000011187 glycerol Nutrition 0.000 description 4
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 description 4
- 208000014674 injury Diseases 0.000 description 4
- WXZMFSXDPGVJKK-UHFFFAOYSA-N pentaerythritol Chemical compound OCC(CO)(CO)CO WXZMFSXDPGVJKK-UHFFFAOYSA-N 0.000 description 4
- UWJJYHHHVWZFEP-UHFFFAOYSA-N pentane-1,1-diol Chemical compound CCCCC(O)O UWJJYHHHVWZFEP-UHFFFAOYSA-N 0.000 description 4
- 238000012545 processing Methods 0.000 description 4
- 230000008439 repair process Effects 0.000 description 4
- IZTQOLKUZKXIRV-YRVFCXMDSA-N sincalide Chemical compound C([C@@H](C(=O)N[C@@H](CCSC)C(=O)NCC(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(N)=O)NC(=O)[C@@H](N)CC(O)=O)C1=CC=C(OS(O)(=O)=O)C=C1 IZTQOLKUZKXIRV-YRVFCXMDSA-N 0.000 description 4
- 208000017520 skin disease Diseases 0.000 description 4
- 238000003756 stirring Methods 0.000 description 4
- 150000003626 triacylglycerols Chemical class 0.000 description 4
- QXKHYNVANLEOEG-UHFFFAOYSA-N Methoxsalen Chemical compound C1=CC(=O)OC2=C1C=C1C=COC1=C2OC QXKHYNVANLEOEG-UHFFFAOYSA-N 0.000 description 3
- 108010087230 Sincalide Proteins 0.000 description 3
- 238000010609 cell counting kit-8 assay Methods 0.000 description 3
- 230000008859 change Effects 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 230000003328 fibroblastic effect Effects 0.000 description 3
- -1 hydroxyl sanshool Chemical compound 0.000 description 3
- 238000002386 leaching Methods 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 229940027041 8-mop Drugs 0.000 description 2
- 208000002874 Acne Vulgaris Diseases 0.000 description 2
- 206010004146 Basal cell carcinoma Diseases 0.000 description 2
- 206010008570 Chloasma Diseases 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- XUMBMVFBXHLACL-UHFFFAOYSA-N Melanin Chemical compound O=C1C(=O)C(C2=CNC3=C(C(C(=O)C4=C32)=O)C)=C2C4=CNC2=C1C XUMBMVFBXHLACL-UHFFFAOYSA-N 0.000 description 2
- 208000003351 Melanosis Diseases 0.000 description 2
- 208000012641 Pigmentation disease Diseases 0.000 description 2
- 206010036087 Polymorphic light eruption Diseases 0.000 description 2
- 241001093501 Rutaceae Species 0.000 description 2
- 241000949456 Zanthoxylum Species 0.000 description 2
- 235000009932 Zanthoxylum simulans Nutrition 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 206010000496 acne Diseases 0.000 description 2
- 229920006243 acrylic copolymer Polymers 0.000 description 2
- 208000009621 actinic keratosis Diseases 0.000 description 2
- 230000032683 aging Effects 0.000 description 2
- 150000001336 alkenes Chemical class 0.000 description 2
- 230000001139 anti-pruritic effect Effects 0.000 description 2
- 239000003908 antipruritic agent Substances 0.000 description 2
- 238000004140 cleaning Methods 0.000 description 2
- 239000012141 concentrate Substances 0.000 description 2
- 229920001577 copolymer Polymers 0.000 description 2
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- 230000002401 inhibitory effect Effects 0.000 description 2
- 230000003020 moisturizing effect Effects 0.000 description 2
- JRZJOMJEPLMPRA-UHFFFAOYSA-N olefin Natural products CCCCCCCC=C JRZJOMJEPLMPRA-UHFFFAOYSA-N 0.000 description 2
- 244000045947 parasite Species 0.000 description 2
- 230000019612 pigmentation Effects 0.000 description 2
- 239000002994 raw material Substances 0.000 description 2
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- 238000001179 sorption measurement Methods 0.000 description 2
- 206010041823 squamous cell carcinoma Diseases 0.000 description 2
- 241000251468 Actinopterygii Species 0.000 description 1
- 206010003694 Atrophy Diseases 0.000 description 1
- 235000008534 Capsicum annuum var annuum Nutrition 0.000 description 1
- 240000008384 Capsicum annuum var. annuum Species 0.000 description 1
- 206010072578 Chronic actinic dermatitis Diseases 0.000 description 1
- 102000001187 Collagen Type III Human genes 0.000 description 1
- 108010069502 Collagen Type III Proteins 0.000 description 1
- 238000002965 ELISA Methods 0.000 description 1
- 238000008157 ELISA kit Methods 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 206010015150 Erythema Diseases 0.000 description 1
- WKWYNAMJWDRHBP-GQCTYLIASA-N Fagaramide Chemical compound CC(C)CNC(=O)\C=C\C1=CC=C2OCOC2=C1 WKWYNAMJWDRHBP-GQCTYLIASA-N 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 229920002683 Glycosaminoglycan Polymers 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 206010051246 Photodermatosis Diseases 0.000 description 1
- 108010067787 Proteoglycans Proteins 0.000 description 1
- 206010043189 Telangiectasia Diseases 0.000 description 1
- 230000037338 UVA radiation Effects 0.000 description 1
- 239000002250 absorbent Substances 0.000 description 1
- 230000002745 absorbent Effects 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 239000003463 adsorbent Substances 0.000 description 1
- 230000036592 analgesia Effects 0.000 description 1
- 230000000259 anti-tumor effect Effects 0.000 description 1
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- 239000002775 capsule Substances 0.000 description 1
- 231100000315 carcinogenic Toxicity 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 230000003833 cell viability Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
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- 230000001684 chronic effect Effects 0.000 description 1
- 238000004440 column chromatography Methods 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 230000001086 cytosolic effect Effects 0.000 description 1
- 230000035622 drinking Effects 0.000 description 1
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- 238000004043 dyeing Methods 0.000 description 1
- 239000003480 eluent Substances 0.000 description 1
- 210000002615 epidermis Anatomy 0.000 description 1
- 231100000321 erythema Toxicity 0.000 description 1
- IDGUHHHQCWSQLU-UHFFFAOYSA-N ethanol;hydrate Chemical compound O.CCO IDGUHHHQCWSQLU-UHFFFAOYSA-N 0.000 description 1
- 239000003777 experimental drug Substances 0.000 description 1
- 230000001605 fetal effect Effects 0.000 description 1
- 210000003953 foreskin Anatomy 0.000 description 1
- WKWYNAMJWDRHBP-UHFFFAOYSA-N fragaramide Natural products CC(C)CNC(=O)C=CC1=CC=C2OCOC2=C1 WKWYNAMJWDRHBP-UHFFFAOYSA-N 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 241000411851 herbal medicine Species 0.000 description 1
- 235000008216 herbs Nutrition 0.000 description 1
- 239000012535 impurity Substances 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000010354 integration Effects 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 238000011068 loading method Methods 0.000 description 1
- 230000004630 mental health Effects 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 230000036407 pain Effects 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 208000017983 photosensitivity disease Diseases 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000037075 skin appearance Effects 0.000 description 1
- 238000002791 soaking Methods 0.000 description 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 239000000516 sunscreening agent Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 208000009056 telangiectasis Diseases 0.000 description 1
- BPJYAXCTOHRFDQ-UHFFFAOYSA-L tetracopper;2,4,6-trioxido-1,3,5,2,4,6-trioxatriarsinane;diacetate Chemical compound [Cu+2].[Cu+2].[Cu+2].[Cu+2].CC([O-])=O.CC([O-])=O.[O-][As]1O[As]([O-])O[As]([O-])O1.[O-][As]1O[As]([O-])O[As]([O-])O1 BPJYAXCTOHRFDQ-UHFFFAOYSA-L 0.000 description 1
- 230000002477 vacuolizing effect Effects 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/75—Rutaceae (Rue family)
- A61K36/758—Zanthoxylum, e.g. pricklyash
-
- 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
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/42—Amides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/16—Emollients or protectives, e.g. against radiation
-
- 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
- A61Q19/004—Aftersun preparations
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/74—Biological properties of particular ingredients
- A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
- A61K2800/782—Enzyme inhibitors; Enzyme antagonists
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Botany (AREA)
- Dermatology (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Biotechnology (AREA)
- Birds (AREA)
- Alternative & Traditional Medicine (AREA)
- Medical Informatics (AREA)
- Toxicology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Cosmetics (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The invention provides application of sanshool or isomers thereof or extracts containing the sanshool in preparing medicines or cosmetics for preventing and/or treating skin photodamage. The experimental result shows that the sanshool can improve the proliferation activity of the fibroblasts; can also inhibit the expression of MMP-1 and MMP-3, and reduce the degradation of extracellular matrix; and can significantly alleviate the symptoms of photodamage to the skin; can be used for preparing cosmetics or medicines for repairing skin photodamage, and has wide market application prospect.
Description
Technical field
The purposes in the external preparation for repairing dermal photodamage is prepared the present invention relates to sanshool.
Background technology
Ultraviolet light irradiates, and especially ultraviolet B radiation (UVB) can cause a series of damages of skin, and it is red to induce skin appearance
Spot, blister, inflammation, it is coarse, thicken, pigmentation, telangiectasis, a series of acute and chronic reactions such as light aging.Light injury
The epidermal thickness of skin differs, with focal atrophy or hyperplasia and different degrees of melanin pigmentation.The visible bullet of skin corium
Property fiber alignment is disorderly, mucopolysaccharide hyperplasia and fibroblast proliferation reduced capability.Photodamaged skin disease is a kind of by daylight,
Especially ultraviolet light irradiates skin directly or indirectly caused skin disease, includes mainly:1. light aging;2. light sensitive dermatoses,
Such as:Polymorphous light eruption (polymorphous light eruption, PLE), farmer's skin (chronic
actinic dermatitis,CAD);3. light aggravates dermatoses, such as:It is acne (acne), chloasma (chloasma), quick
Perceptual skin etc.;4. light is carcinogenic, such as:Solar keratosis (actinic keratosis), squamous cell carcinoma (squamous
Cell carcinoma, SCC), basal-cell carcinoma (basal cell carcinoma, BCC), (the He Li skins such as chromoma
Skin disease and venereal disease, 2013, (2):78-79.).Such disease is a kind of more typical, and the interpretation of the cause, onset and process of an illness is complicated, the disease of diverse clinical manifestations,
Often betide exposure position, easily repeatedly, it is refractory more, even be easy induce canceration, seriously endanger the physical and mental health of the people,
Therefore it is studied and has become current medical domain one of important topic urgently to be resolved hurrily.At present to dermal photodamage and photodamaged
Dermopathic protection mainly avoids excessive solarization, uses suncream and sun-proof measure, due to many reasons, the effect acquired by it
Fruit is very limited.
Chinese prickly ash is Rutaceae (Rutaceae) Zanthoxylum (Zanthoxylum genus), and fragrance, oil plant and Chinese medicine have
More than 2000 years history,《Pharmacopoeia of People's Republic of China》It goes through version to record, " integration of drinking and medicinal herbs ", modern Chinese herbal medicine concludes its effect and is:
Warm in pain, expelling parasite, external application eliminating dampness, desinsection are antipruritic.Sanshool (sanshool) extracts from Chinese prickly ash, Japanese for the first time in 1913
Scholar village mountain justice temperature finds and names, and belongs to fagaramide substance, is Chinese prickly ash fiber crops taste source, and recent research has shown that it has and promotees
A variety of effects such as WeiDongLi Capsule, analgesia, expelling parasite, antipruritic, antitumor, platelet aggregation-against.Up to the present it yet there are no mountain
Green pepper element is used to repair the report of dermal photodamage.
Invention content
Exist in order to solve the above technical problem, the present invention provides sanshool or its isomer or containing its extract
Prepare the drug for preventing and/or treating dermal photodamage or the purposes in cosmetics.
Further, the drug or cosmetics are the substances for promoting fibroblast proliferation.
Further, the drug or cosmetics are the substances for inhibiting matrix metalloproteinase MMP-1, MMP-3 expression.
Further, the drug or cosmetics are the substances for inhibiting extracellular matrix degradation.
Further, the drug or cosmetics are to increase epidermal thickness, improve skin corium elastomer and collagenous fibres
The substance of arrangement.
Further, the sanshool is hydroxyl-alpha-sanshool, hydroxy-beta-sanshool, hydroxyl-γ-sanshool, hydroxyl-
One kind in δ-sanshool, hydroxyl-ε-sanshool, α-sanshool, β-sanshool, γ-sanshool, δ-sanshool, ε-sanshool
Or a variety of, preferably hydroxyl-alpha-sanshool.
Further, the extract containing sanshool is pepper extract.
Further, the pepper extract is the substance removed after cellulose and lignin.
Further, the dermal photodamage refers to skin injury caused by ultraviolet light.
Further, it is sanshool or its isomer or is active constituent containing its extract, adds drug
Or the preparation that acceptable auxiliary material is prepared in cosmetics.
The experiment results show that fibroblastic proliferation activity can be improved in sanshool;It may also suppress MMP-1's and MMP-3
Expression, reduces the degradation of extracellular matrix;And it can significantly mitigate dermal photodamage symptom;It can be used for preparing and repair skin light
The cosmetics or drug of damage, have a vast market application prospect.
Obviously, the above according to the present invention is not being departed from according to the ordinary technical knowledge and customary means of this field
Under the premise of the above-mentioned basic fundamental thought of the present invention, the modification, replacement or change of other diversified forms can also be made.
The specific implementation mode of form by the following examples remakes further specifically the above of the present invention
It is bright.But the range that this should not be interpreted as to the above-mentioned theme of the present invention is only limitted to example below.It is all to be based on the above of the present invention
The technology realized all belongs to the scope of the present invention.
Description of the drawings
Fig. 1 is the HE colored graphs of mouse skin, wherein 1 meaning is epidermis, and 2 is signified for skin corium fiber.
Specific implementation mode
The preparation of embodiment 1, pepper extract containing sanshool
Take dry Chinese prickly ash pericarp 2kg broken, the ethanol water for being 85% with 16kg volume fractions is to Chinese prickly ash pericarp powder
Cold soaking extraction is carried out, extraction time 48h is extracted 3 times, is merged leaching liquor, is abandoned the dregs of a decoction, and concentrate is concentrated under reduced pressure to obtain in leaching liquor,
The volume of concentrate is the 1/5~1/4 of leaching liquor, obtains hydroxyl sanshool mixture;By the hydroxyl sanshool mixture of gained
It is 20% to be diluted with water to volumes of aqueous ethanol score, is isolated and purified by HP-20 type macroporous adsorbent resin column chromatographies, is done
Dry Pericarpium Zanthoxyli fruit weight is 1Kg with macroporous absorbent resin volume ratio:0.7L, Dynamic Adsorption loading, adsorption rate are controlled every
Hour 2.5BV after absorption, first uses the water of 2.5BV and 55% ethanol solution elution removal of impurities respectively, then with the 85% of 3BV
Ethanol solution elution, collect eluent, hydroxyl sanshool mixture medicinal extract is concentrated under reduced pressure to obtain.The sanshool mixing extraction of concentration
Object can be used directly, be used after can also further being isolated and purified by organic solvent.
Embodiment 2,
A kind of cosmetics for repairing dermal photodamage, it is that the raw material matched by following weight forms:Deionized water 73%,
1,3-PD 8%, pentanediol 3.5%, ring five dimethyl silicone polymer 3%, dimethyl silicone polymer 3%, containing sanshool
Pepper extract 2%, Fructus Hordei Germinatus oligose glucoside 2%, triglycerides 2%, four ester 2% of pentaerythrite, pungent glycol/glycerine/poly- third
Olefin(e) acid copolymer 1 .5%.
Preparation method:The deionized water of formula ratio, 1,3-PD, pentanediol and Fructus Hordei Germinatus oligose glucoside are mixed
It is heated to 85-90 DEG C;The ring five dimethyl silicone polymer of addition formula ratio, dimethyl silicone polymer, triglycerides, pentaerythrite
Four esters and pungent glycol/glycerine/acrylic copolymer continue heating stirring, and formula ratio is added after being cooled to room temperature contains sanshool
Pepper extract stir and evenly mix.
Application method:It takes appropriate directly external application to be applied to skin, once a day, without cleaning, uses preceding smearable moisturizing
Frost.
Embodiment 3,
A kind of cosmetics for repairing dermal photodamage, it is that the raw material matched by following weight forms:Deionized water 74%,
1,3-PD 8%, pentanediol 3.5%, ring five dimethyl silicone polymer 3%, dimethyl silicone polymer 3%, containing sanshool
Pepper extract 1%, Fructus Hordei Germinatus oligose glucoside 2%, triglycerides 2%, four ester 2% of pentaerythrite, pungent glycol/glycerine/poly- third
Olefin(e) acid copolymer 1 .5%.
Preparation method:The deionized water of formula ratio, 1,3-PD, pentanediol and Fructus Hordei Germinatus oligose glucoside are mixed
It is heated to 85-90 DEG C;The ring five dimethyl silicone polymer of addition formula ratio, dimethyl silicone polymer, triglycerides, pentaerythrite
Four esters and pungent glycol/glycerine/acrylic copolymer continue heating stirring, and formula ratio is added after being cooled to room temperature contains sanshool
Pepper extract stir and evenly mix.
Application method:It takes appropriate directly external application to be applied to skin, once a day, without cleaning, uses preceding smearable moisturizing
Frost.
Illustrate beneficial effects of the present invention below by way of test example.
Test example 1, sanshool repair the cell experiment of light injury
(1) cell photo-damage model is established
Chinese Fetal Foreskin Fibroblasts are taken, Fibroblast cell-culture is detached using conventional method, are frozen after being passaged to 3-5 generations, cell recovery
After be inoculated in culture dish, be added the 8-methoxsalen (8-MOP) of 50mg/L in culture medium, when irradiation abandons culture medium, to contain 50mg/
Row UVA irradiation after the PBS of the 8-MOP of L is rinsed 2 times, irradiation dose are 9J/cm2, Continuous irradiation 21 days.It is seen under microscope
It examines cell and the feature damaged change occurs:I.e. cell becomes larger, and intracellular particle increases, and cytoplasmic vacuolation and proliferation delay.
(2) experimental drug:Hydroxyl-alpha-sanshool
(3) promote fibroblastic increment active (%)
Experimental method:Fibroblast after UVA is irradiated is by 6 × 103A/hole is inoculated in 96 orifice plates, and culture 24 is small
When after the sanshool that 10 μ L concentration are respectively 0.01%, 0.02% and 0.04% is added, continue culture 24 hours after 10 μ L/ are added
The CCK-8 reagents in hole measure absorbance (A) value of 450nm with enzyme-linked immunosorbent assay instrument after being incubated for 3 hours.It is repeated 3 times.
Cell viability (%)=[A (test group)-A (0)]/[A (blank control)-A (0)] × 100%
Wherein, A (test group) indicates the absorbance in the hole of cell, CCK-8 solution and sanshool;A (0) indicates CCK-
8 solution, and the absorbance in acellular and sanshool hole;A (blank control) has cell, CCK-8 solution, and the hole without sanshool
Absorbance.
Influence of the 1. various concentration sanshool of table to fibroblast proliferation
As shown in Table 1, after sanshool acts on fibroblast, it is remarkably improved cell-proliferation activity.
(4) inhibit the expression of matrix metalloproteinase (MMP-1, MMP-3)
Experiment is divided into four groups, respectively untreated fish group (Normal group for not giving sanshool and UVA radiation treatments), Chinese pepper
Plain processing group (+0.01% sanshool of fibroblast), UVA processing group, UVA+ sanshool processing group (give after UVA irradiation
The processing of 0.01% sanshool), culture takes cell supernatant after 48 hours, illustrates sample-adding, temperature according to ELISA kit after extraction
Educate, wash after it is enzyme, incubate, washing, finally measure absorbance (OD values) under 450nm wavelength with microplate reader, it is bent to pass through standard
People MMP-1, MMP-3 concentration in line computation sample.
The influence that 2. sanshool of table expresses MMP-1 and MMP-3
As shown in Table 2, sanshool can inhibit the expression of MMP-1 and MMP-3, and MMP-1 and MMP-3 are to decompose extracellular base
The important enzyme of matter ingredient:Wherein MMP-1 mainly hydrolyzes I, II and type III collagen;MMP-3 hydrolyzes substrate then than wide, including
Collagen, proteoglycan and gelatin etc..Therefore inhibit the two activity that can reduce the degradation of extracellular matrix.
Test example 2, sanshool repair the zoopery of light injury
(1) animal photo damage model is established
It first uses scissors and electric shaver to reject mouse back hair, UVB is carried out after fully exposing its skin of back
(300mJ/cm2) irradiation mouse, once a day, for three days on end, modeling terminates, and the successful mouse back skin of modeling occurs apparent
The erythema scales of skin that peel off changes.
(2) experiment packet
Mouse after modeling successfully totally 20, control group and each 10 of test group.The next day that control group is disregarded, test group
A concentration of 2% hydroxyl-alpha-sanshool is administered locally to, is administered 2 weeks altogether.
(3) skin injury situation scoring (score by rules is shown in Table 3) is carried out to mouse back UVB irradiation areas, as a result such as table 4
It is shown:
3. mouse back UVB irradiation area skin injury situation standards of grading of table
The influence that 4. sanshool of table scores to light injury mouse back skin injury situation
As shown in Table 4, dermal photodamage can significantly be mitigated after Chinese pepper extract for treating 4 times.
(4) it draws materials after putting to death mouse, carries out HE dyeing and show that experimental mice epidermal thickness increases, skin corium fiber row
Row are neat (Fig. 1).
To sum up, fibroblastic proliferation activity can be improved in sanshool;The expression of MMP-1 and MMP-3 are may also suppress, is reduced
The degradation of extracellular matrix;And it can significantly mitigate dermal photodamage symptom;It can be used for preparing the change for repairing dermal photodamage
Cosmetic has a vast market application prospect.
Claims (10)
1. sanshool or its isomer or containing its extract prepare prevent and/or treatment dermal photodamage drug or
Purposes in cosmetics.
2. purposes according to claim 1, it is characterised in that:The drug or cosmetics are for promoting fibroblast
The substance of proliferation.
3. purposes according to claim 1, it is characterised in that:The drug or cosmetics are to inhibit matrix metalloproteinase
The substance of MMP-1, MMP-3 expression.
4. purposes according to claim 3, it is characterised in that:The drug or cosmetics are to inhibit extracellular matrix degradation
Substance.
5. purposes according to claim 1, it is characterised in that:The drug or cosmetics are to increase epidermal thickness, are improved
The substance of skin corium elastomer and arrangement of collagen fibers.
6. according to Claims 1 to 5 any one of them purposes, it is characterised in that:The sanshool be hydroxyl-alpha-sanshool,
Hydroxy-beta-sanshool, hydroxyl-γ-sanshool, hydroxyl-δ-sanshool, hydroxyl-ε-sanshool, α-sanshool, β-sanshool,
It is one or more in γ-sanshool, δ-sanshool, ε-sanshool, preferably hydroxyl-alpha-sanshool.
7. according to claim 1~6 any one of them purposes, it is characterised in that:The extract containing sanshool is Chinese prickly ash
Extract.
8. purposes according to claim 7, it is characterised in that:The pepper extract be remove cellulose and lignin it
Substance afterwards.
9. according to claim 1~8 any one of them purposes, it is characterised in that:The dermal photodamage refers to that ultraviolet light is led
The skin injury of cause.
10. the external preparation of a kind of prevention and/or treatment dermal photodamage, it is characterised in that:It is sanshool or it is different with dividing
Structure is active constituent containing its extract, along with the preparation that acceptable auxiliary material is prepared in drug or cosmetics.
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