CN108685744A - The new opplication of Chinese medicine natural plants molecule - Google Patents
The new opplication of Chinese medicine natural plants molecule Download PDFInfo
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- CN108685744A CN108685744A CN201710224429.2A CN201710224429A CN108685744A CN 108685744 A CN108685744 A CN 108685744A CN 201710224429 A CN201710224429 A CN 201710224429A CN 108685744 A CN108685744 A CN 108685744A
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- chinese medicine
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- 239000003814 drug Substances 0.000 title claims abstract description 55
- 241000196324 Embryophyta Species 0.000 claims abstract description 59
- 230000000694 effects Effects 0.000 claims abstract description 48
- 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 claims abstract description 46
- 102000003425 Tyrosinase Human genes 0.000 claims abstract description 28
- 108060008724 Tyrosinase Proteins 0.000 claims abstract description 28
- 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 claims abstract description 23
- 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 claims abstract description 23
- MWDZOUNAPSSOEL-UHFFFAOYSA-N kaempferol Natural products OC1=C(C(=O)c2cc(O)cc(O)c2O1)c3ccc(O)cc3 MWDZOUNAPSSOEL-UHFFFAOYSA-N 0.000 claims abstract description 23
- 229960001285 quercetin Drugs 0.000 claims abstract description 23
- 235000005875 quercetin Nutrition 0.000 claims abstract description 23
- 235000009694 Quassia amara Nutrition 0.000 claims abstract description 21
- 229940013788 quassia Drugs 0.000 claims abstract description 21
- QMNWISYXSJWHRY-YLNUDOOFSA-N astragaloside IV Chemical compound O1[C@H](C(C)(O)C)CC[C@]1(C)[C@@H]1[C@@]2(C)CC[C@]34C[C@]4(CC[C@H](O[C@H]4[C@@H]([C@@H](O)[C@H](O)CO4)O)C4(C)C)[C@H]4[C@@H](O[C@H]4[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O4)O)C[C@H]3[C@]2(C)C[C@@H]1O QMNWISYXSJWHRY-YLNUDOOFSA-N 0.000 claims abstract description 19
- QMNWISYXSJWHRY-BCBPIKMJSA-N astragaloside IV Natural products CC(C)(O)[C@@H]1CC[C@@](C)(O1)[C@H]2[C@@H](O)C[C@@]3(C)[C@@H]4C[C@H](O[C@@H]5O[C@H](CO)[C@H](O)[C@@H](O)[C@H]5O)[C@H]6C(C)(C)[C@H](CC[C@@]67C[C@@]47CC[C@]23C)O[C@@H]8OC[C@@H](O)[C@H](O)[C@H]8O QMNWISYXSJWHRY-BCBPIKMJSA-N 0.000 claims abstract description 19
- PFKIBRPYVNVMRU-UHFFFAOYSA-N cyclosieversioside F Natural products CC(C)(O)C1COC(C)(C1)C2C(O)CC3(C)C4CC(OC5OC(CO)C(O)C(O)C5O)C6C(C)(C)C(CCC67CC47CCC23C)OC8OCC(O)C(O)C8O PFKIBRPYVNVMRU-UHFFFAOYSA-N 0.000 claims abstract description 19
- 150000002576 ketones Chemical class 0.000 claims abstract description 19
- 239000002537 cosmetic Substances 0.000 claims abstract description 13
- 235000013305 food Nutrition 0.000 claims abstract description 11
- 229940079593 drug Drugs 0.000 claims abstract description 10
- 241000158615 Quassia Species 0.000 claims description 20
- 239000000470 constituent Substances 0.000 claims description 5
- 230000002708 enhancing effect Effects 0.000 claims description 5
- 238000002360 preparation method Methods 0.000 claims description 3
- PJANXHGTPQOBST-VAWYXSNFSA-N Stilbene Natural products C=1C=CC=CC=1/C=C/C1=CC=CC=C1 PJANXHGTPQOBST-VAWYXSNFSA-N 0.000 claims description 2
- 229930182470 glycoside Natural products 0.000 claims description 2
- 150000002338 glycosides Chemical class 0.000 claims description 2
- PJANXHGTPQOBST-UHFFFAOYSA-N stilbene Chemical compound C=1C=CC=CC=1C=CC1=CC=CC=C1 PJANXHGTPQOBST-UHFFFAOYSA-N 0.000 claims description 2
- 235000021286 stilbenes Nutrition 0.000 claims 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 abstract description 26
- 201000009030 Carcinoma Diseases 0.000 abstract description 5
- 239000003795 chemical substances by application Substances 0.000 abstract description 3
- 238000003786 synthesis reaction Methods 0.000 abstract description 3
- 239000004615 ingredient Substances 0.000 abstract description 2
- 240000003085 Quassia amara Species 0.000 abstract 1
- 239000000243 solution Substances 0.000 description 23
- 210000002752 melanocyte Anatomy 0.000 description 16
- 210000003491 skin Anatomy 0.000 description 13
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 12
- RXKJFZQQPQGTFL-UHFFFAOYSA-N dihydroxyacetone Chemical compound OCC(=O)CO RXKJFZQQPQGTFL-UHFFFAOYSA-N 0.000 description 8
- VJNCICVKUHKIIV-UHFFFAOYSA-N dopachrome Chemical compound O=C1C(=O)C=C2NC(C(=O)O)CC2=C1 VJNCICVKUHKIIV-UHFFFAOYSA-N 0.000 description 8
- 238000012360 testing method Methods 0.000 description 7
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 6
- 238000002474 experimental method Methods 0.000 description 6
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 6
- 238000002835 absorbance Methods 0.000 description 5
- 238000000034 method Methods 0.000 description 5
- 230000000638 stimulation Effects 0.000 description 5
- 102100032742 Histone-lysine N-methyltransferase SETD2 Human genes 0.000 description 4
- 101000654725 Homo sapiens Histone-lysine N-methyltransferase SETD2 Proteins 0.000 description 4
- 239000009636 Huang Qi Substances 0.000 description 4
- 210000004027 cell Anatomy 0.000 description 4
- 229940120503 dihydroxyacetone Drugs 0.000 description 4
- 239000001963 growth medium Substances 0.000 description 4
- 230000008099 melanin synthesis Effects 0.000 description 4
- 210000002780 melanosome Anatomy 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- WHNFPRLDDSXQCL-UAZQEYIDSA-N α-msh Chemical compound C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(N)=O)NC(=O)[C@H](CO)NC(C)=O)C1=CC=C(O)C=C1 WHNFPRLDDSXQCL-UAZQEYIDSA-N 0.000 description 4
- 206010021143 Hypoxia Diseases 0.000 description 3
- 230000003796 beauty Effects 0.000 description 3
- 102000015694 estrogen receptors Human genes 0.000 description 3
- 108010038795 estrogen receptors Proteins 0.000 description 3
- 230000007954 hypoxia Effects 0.000 description 3
- SHZGCJCMOBCMKK-UHFFFAOYSA-N D-mannomethylose Natural products CC1OC(O)C(O)C(O)C1O SHZGCJCMOBCMKK-UHFFFAOYSA-N 0.000 description 2
- 239000006144 Dulbecco’s modified Eagle's medium Substances 0.000 description 2
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 description 2
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 description 2
- 101800001751 Melanocyte-stimulating hormone alpha Proteins 0.000 description 2
- 102400000740 Melanocyte-stimulating hormone alpha Human genes 0.000 description 2
- 101710200814 Melanotropin alpha Proteins 0.000 description 2
- LOUPRKONTZGTKE-WZBLMQSHSA-N Quinine Chemical compound C([C@H]([C@H](C1)C=C)C2)C[N@@]1[C@@H]2[C@H](O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-WZBLMQSHSA-N 0.000 description 2
- 230000004913 activation Effects 0.000 description 2
- 235000019658 bitter taste Nutrition 0.000 description 2
- 230000015556 catabolic process Effects 0.000 description 2
- 238000006731 degradation reaction Methods 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- 235000013399 edible fruits Nutrition 0.000 description 2
- 238000006911 enzymatic reaction Methods 0.000 description 2
- 210000002615 epidermis Anatomy 0.000 description 2
- 239000007789 gas Substances 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 229960004502 levodopa Drugs 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 239000013641 positive control Substances 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- 238000012216 screening Methods 0.000 description 2
- 210000004927 skin cell Anatomy 0.000 description 2
- 206010000087 Abdominal pain upper Diseases 0.000 description 1
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 1
- 235000001258 Cinchona calisaya Nutrition 0.000 description 1
- 102100022875 Hypoxia-inducible factor 1-alpha Human genes 0.000 description 1
- 108050009527 Hypoxia-inducible factor-1 alpha Proteins 0.000 description 1
- SHZGCJCMOBCMKK-JFNONXLTSA-N L-rhamnopyranose Chemical compound C[C@@H]1OC(O)[C@H](O)[C@H](O)[C@H]1O SHZGCJCMOBCMKK-JFNONXLTSA-N 0.000 description 1
- PNNNRSAQSRJVSB-UHFFFAOYSA-N L-rhamnose Natural products CC(O)C(O)C(O)C(O)C=O PNNNRSAQSRJVSB-UHFFFAOYSA-N 0.000 description 1
- PGFKZUOYIFDMQJ-UHFFFAOYSA-N Nigakinone Natural products C12=CC=CC=C2C2=CC=NC3=C2N1C(=O)C(O)=C3OC PGFKZUOYIFDMQJ-UHFFFAOYSA-N 0.000 description 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 102100027467 Pro-opiomelanocortin Human genes 0.000 description 1
- NSZQOXBBEWYGQH-UHFFFAOYSA-N Quercetin-3-rhamnosid Natural products CC1OC(O)C(O)C(OC2=C(Oc3cc(O)cc(O)c3C2=O)c4ccc(O)c(O)c4)C1O NSZQOXBBEWYGQH-UHFFFAOYSA-N 0.000 description 1
- 241000209140 Triticum Species 0.000 description 1
- 235000021307 Triticum Nutrition 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 206010000496 acne Diseases 0.000 description 1
- 229930013930 alkaloid Natural products 0.000 description 1
- 150000003797 alkaloid derivatives Chemical class 0.000 description 1
- 230000001754 anti-pyretic effect Effects 0.000 description 1
- 239000002221 antipyretic Substances 0.000 description 1
- 235000019789 appetite Nutrition 0.000 description 1
- 230000036528 appetite Effects 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 235000013361 beverage Nutrition 0.000 description 1
- 229940098773 bovine serum albumin Drugs 0.000 description 1
- 230000000711 cancerogenic effect Effects 0.000 description 1
- 231100000315 carcinogenic Toxicity 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- LOUPRKONTZGTKE-UHFFFAOYSA-N cinchonine Natural products C1C(C(C2)C=C)CCN2C1C(O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-UHFFFAOYSA-N 0.000 description 1
- 238000004040 coloring Methods 0.000 description 1
- 230000002860 competitive effect Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 230000002255 enzymatic effect Effects 0.000 description 1
- 239000012091 fetal bovine serum Substances 0.000 description 1
- 229930003935 flavonoid Natural products 0.000 description 1
- 150000002215 flavonoids Chemical class 0.000 description 1
- 235000017173 flavonoids Nutrition 0.000 description 1
- 235000013373 food additive Nutrition 0.000 description 1
- 239000002778 food additive Substances 0.000 description 1
- 229930182478 glucoside Natural products 0.000 description 1
- 150000008131 glucosides Chemical class 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 239000002917 insecticide Substances 0.000 description 1
- 230000002452 interceptive effect Effects 0.000 description 1
- 210000002510 keratinocyte Anatomy 0.000 description 1
- 230000002045 lasting effect Effects 0.000 description 1
- 230000000670 limiting effect Effects 0.000 description 1
- 230000035800 maturation Effects 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 239000011259 mixed solution Substances 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- MKOHWARXSAUSPK-UHFFFAOYSA-N nigakinone Chemical compound C12=CC=CC=C2N2C3=C1C=CNC3=C(OC)C(=O)C2=O MKOHWARXSAUSPK-UHFFFAOYSA-N 0.000 description 1
- 230000036963 noncompetitive effect Effects 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 230000035764 nutrition Effects 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 239000000902 placebo Substances 0.000 description 1
- 229940068196 placebo Drugs 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- QDAMORAIRIHJCS-UHFFFAOYSA-N quercetin 3-rhamnoside Natural products CC1OC(OC2=C(Oc3ccc(O)c(O)c3C2=O)c4ccc(O)c(O)c4)C(O)C(O)C1O QDAMORAIRIHJCS-UHFFFAOYSA-N 0.000 description 1
- OXGUCUVFOIWWQJ-HQBVPOQASA-N quercitrin Chemical compound O[C@@H]1[C@H](O)[C@@H](O)[C@H](C)O[C@H]1OC1=C(C=2C=C(O)C(O)=CC=2)OC2=CC(O)=CC(O)=C2C1=O OXGUCUVFOIWWQJ-HQBVPOQASA-N 0.000 description 1
- 229960000948 quinine Drugs 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 150000008265 rhamnosides Chemical class 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 238000012549 training Methods 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 230000002087 whitening effect Effects 0.000 description 1
- 230000037303 wrinkles Effects 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
- A61K8/4926—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having six membered rings
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- A61K31/70—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
-
- 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
-
- 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
- A61Q19/04—Preparations for care of the skin for chemically tanning the skin
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Birds (AREA)
- Dermatology (AREA)
- Molecular Biology (AREA)
- Cosmetics (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The present invention relates to the new opplications of Chinese medicine natural plants molecule.Some first public Chinese medicine natural plants molecules of the present invention can enhance tyrosinase activity, can promote the generation of melanin, be finally reached the effect of colour of skin blackening, have U.S. black effect.Wherein, black effect of U.S. of quassia ketone, Astragaloside IV and Quercetin -3- rhamnosides is the most notable.Using Chinese medicine natural plants molecule as U.S. black effect ingredient, apply the risk that can substantially lower on cosmetic products (such as cosmetics), drug or food and other external application big health-oriented products of class and cause cutaneum carcinoma because using chemical synthesis class tanning agent and excessive sun to bathe, and U.S. black significant effect, there is huge market potential.
Description
Technical field
The present invention relates to the applied technical fields of Chinese medicine natural plants molecule, more particularly to a kind of Chinese medicine natural plants point
Son is preparing the application in having effects that U.S. black product.
Background technology
It is U.S. it is black be exactly to allow skin darkening.With the development of the times, understanding increasingly diversification of the people to fashion, in vain
It is not that the unique of beauty embodies, more and more people pursue bronze-colored or wheat skin.
Solarization sunbath is simplest natural beauty black method, but skin can be damaged by being excessively exposed to the sun, and
And have found the skin that can lead to wrinkle, brown spot, pimple and cortex, relax.In the worst case, it is excessively exposed to
Sunlight can cause have disfiguring or even fatefulue cutaneum carcinoma.Therefore, more and more U.S. black Related products come into being.
Common U.S. black product currently on the market, active constituent is chemically synthesized drug, such as dihydroxyacetone (DHA)
(DHA), skin darkening can be made under conditions of being not exposed to sunlight.DHA is a kind of no sugar colour, can be with dead land for building
Skin cell acts in the cuticula of epidermis.Skin Cell changes colour to obtain due to this effect tanned outer of the sun
It sees.This color change just gradually subsides after typically lasting for about 5~7 days, and therefore, U.S. is black, and the effect is unsatisfactory.Also, have
There is also certain risks for causing cutaneum carcinoma for a little chemically synthesized black products of U.S..
Quassia ketone (Nigakinone) is a kind of alkaloid, is quassia leaf (Ramulus et Folium Picrasmae)
The bitter taste in the source of middle bitter taste, quassia leaf is even more stronger than quinine.Quassia leaf is commonly used as antipyretic and insecticide, and treatment
The replenishers had a stomachache and stimulated appetite.
Astragaloside IV is the biologically active significant compound contained in a kind of common Chinese medicine-Radix Astragali.According to
Theory of traditional Chinese medical science, " gas " is a kind of form of life energy, and Radix Astragali can then promote the cycle of " gas " in our body, therefore
The Radix Astragali of different proportion can be added in this many famous ancient times Traditional Chinese medicinal prescription.
Quercetin -3- rhamnosides are the glucosides formed by flavonoids Quercetin and desoxysugar rhamnose, contain several phenol
Base.Quercetin is a kind of inhibitor of nonspecific proteins kinases.
To so far, there are no the relevant reports applied in U.S. black product about Chinese medicine natural plants molecule.
Invention content
Based on this, the present invention provides a kind of new opplications of Chinese medicine natural plants molecule.
Specific technical solution is as follows:
Application of the Chinese medicine natural plants molecule in the product for preparing enhancing tyrosinase activity.
Chinese medicine natural plants molecule has effects that apply in U.S. black product in preparation.
Chinese medicine natural plants molecule described in some embodiments are selected from quassia ketone, Astragaloside IV and Quercetin -3- wherein
At least one of rhamnoside.
In wherein some embodiments, the product is cosmetic products, drug or food.The cosmetic products being
Cosmetic, the food can be food additives, beverage or nutrition fortifier.
Having effects that U.S. black cosmetics the present invention also provides a kind of.
Specific technical solution is as follows:
It is a kind of to have effects that U.S. black cosmetics, the active constituent in the cosmetics include Chinese medicine natural plants point
Son, the Chinese medicine natural plants molecule are selected from least one of quassia ketone, Astragaloside IV and Quercetin -3- rhamnosides.
Having effects that U.S. black drug the present invention also provides a kind of.
Specific technical solution is as follows:
A kind of to have effects that U.S. black drug, the active constituent in the drug includes Chinese medicine natural plants molecule, institute
It states Chinese medicine natural plants molecule and is selected from least one of quassia ketone, Astragaloside IV and Quercetin -3- rhamnosides.
Having effects that U.S. black food the present invention also provides a kind of.
Specific technical solution is as follows:
It is a kind of to have effects that U.S. black food, include Chinese medicine natural plants molecule in the food, the Chinese medicine is natural
Plant molecular is selected from least one of quassia ketone, Astragaloside IV and Quercetin -3- rhamnosides.
The present inventor has found that some Chinese medicine natural plants molecules can enhance tyrosine by lot of experiments
Enzymatic activity can promote the generation of melanin, be finally reached the effect of colour of skin blackening, have U.S. black effect.Wherein, quassia ketone,
Black effect of U.S. of Astragaloside IV and Quercetin -3- rhamnosides is the most notable.
Using Chinese medicine natural plants molecule as U.S. black effect ingredient, apply in cosmetic products (such as cosmetics), medicine
Can substantially it lower because using chemical synthesis class tanning agent and excessive sun to bathe on product or food and other external application big health-oriented products of class
The risk of cutaneum carcinoma caused by and, and U.S. black significant effect, have huge market potential.
Description of the drawings
Fig. 1 is the chemical constitution of Chinese medicine natural plants molecule quassia ketone, Astragaloside IV and Quercetin -3- rhamnosides;
Fig. 2 is that the Chinese medicine natural plants molecule of the various concentration in embodiment 1 generates melanocyte the rush of melanin
Into exercising result;
Fig. 3 is humidification knot of the Chinese medicine natural plants molecule to tyrosinase activity of the various concentration in embodiment 2
Fruit;
Fig. 4 is the schematic diagram for finding out Km and Vmax in enzyme reaction using Michaelis-Menten equation by double reciprocal plot;
Fig. 5 is humidification knot of the Chinese medicine natural plants molecule to tyrosinase activity of the various concentration in embodiment 2
The double reciprocal plot of fruit.
Specific implementation mode
Further details of theory is done to the new opplication of the Chinese medicine natural plants molecule of the present invention below in conjunction with specific embodiment
It is bright.
1 B16 melanocyte melanins of embodiment generate experiment
1, prepare Chinese medicine natural plants molecular solution:
Following Chinese medicine natural plants molecule is weighed respectively:Quassia ketone, Astragaloside IV, Quercetin -3- rhamnosides, with DMSO
It dissolves and is dissolved in 100mM surely;
The natural plants molecular solution of 100mM respectively with the pure water of Bioexperiment rank be diluted to 100 μM, 10 μM and
1 μM of natural plants molecular solution;
It will be respectively used to melanin production experiment test by diluted Chinese medicine natural plants molecular solution, while not have
Solution (ratio of DMSO and water and the diluted Chinese medicine natural plants molecular solution phase of process of any natural plants molecule is added
It is blank control together).Use 1nM α-melanocyte-stimulating hormone α-melanocyte stimulation hormone (α-
MSH) it is used as positive control.
2, prepare B16 melanocytes:
B16 melanocytes (CRL-6323TM;ATCC, Manassas, VA) in 5%CO2With 37 DEG C under conditions of carry out
Culture, culture medium Dulbecco's Modified Eagle'S Medium (DMEM, Invitrogen, Carlsbad, CA),
And 10% fetal bovine serum albumin and Pen .- Strep (100U/mL) are supplemented in the culture medium.Only P8 to P18 it
Between B16 melanocytes can be used for carrying out this experiment.In 4 days, melanocyte is containing ripe melanosome and can will be black
In colouring matter secretion to culture medium, culture medium should be about 0.5-0.7 in the absorbance of 405nm, if melanocyte fails to reach
This absorbance standard is considered as then the purpose for not being suitable for this experiment screening.
3, melanin production is tested:
B16 melanocytes are seeded on 96 well culture plates by each Kong Erwan, the training described in step 2 is added per hole
Base 100 μ L are supported, and it includes quassia ketone, Astragaloside IV and Quercetin-to be separately added into 1 μM, 10 μM or 100 μM of step 1 preparation
Chinese medicine natural plants molecular solution or placebo solution including 3- rhamnosides or 100 μ L of positive control solution, 5%
CO2With 37 DEG C under conditions of cultivate 2-4 days.
The absorbance of the mixed solution after cultivating 2-4 days is directly detected at 405nm, and absorbance is converted into melanin
Concentration.The result of experimental group is compared with blank control group, the melanin concentration of experimental group is converted into blank control group
Melanin concentration multiple, the results are shown in Figure 2.As can be seen from Figure:100 μM of quassia ketone, Astragaloside IV and
Quercetin -3- rhamnoside molecular solution has the effect of significantly promoting melanin production.
2 tyrosinase activity of embodiment is tested
1, prepare Chinese medicine natural plants molecular solution:
Following Chinese medicine natural plants molecule is weighed respectively:Quassia ketone, Astragaloside IV, Quercetin -3- rhamnosides, with DMSO
It dissolves and is dissolved in 100mM surely;
The natural plants molecular solution of 100mM respectively with the pure water of Bioexperiment rank be diluted to 100 μM, 10 μM and
1 μM of natural plants molecular solution;
Tyrosinase activity effect test will be respectively used to by diluted Chinese medicine natural plants molecular solution, while not have
There are solution (ratio of DMSO and water and the diluted Chinese medicine natural plants molecular solution phase of process that any natural plants molecule is added
It is blank control together).
2, tyrosinase activity is tested:
Tyrosinase activity test is carried out according to a conventional method.Tyrosinase activity test is screening whitening or U.S. black powder product
Conventional test methodologies.Tyrosine can be converted to levodopa (L-DOPA) because of the effect of tyrosinase, and it is more to be then converted into
Bar pigment (Dopachrome).Dopachrome has absorbance under 492nm wavelength, so can quantify and calculate tyrosinase
Activity.Dopachrome only keeps in object, it can be converted to melanin (Melanin).Melanin on human skin is by black
Dopachrome caused by plain cell (Melanocytes) is transformed.Melanin can be gradually in melanocyte
Ripe in melanosome (Melanosome), melanosome will turn along the dendron (Dentrite) of melanocyte after maturation
Horn cell (Keratinocytes) is moved on to, the colour of skin is made to deepen.Dopachrome and melanin can be reduced by inhibiting tyrosinase activity
Generation, so that the colour of skin is become lighter whiter.Conversely, enhancing tyrosinase activity can be effectively increased the production of dopachrome and melanin
It is raw, to make the colour of skin become deeper more black.
Since tyrosinase can convert tyrosine to dopachrome, in the test, dopachrome production quantity
It is higher, illustrate that natural plants molecular solution is better to the stimulation of tyrosinase, the activity of tyrosinase is higher.Test result
(enhancing rate of each experimental group relative to blank control group) as shown in Figure 3.From Fig. 3 results:Quassia ketone, the Huang of various concentration
The solution of stilbene first glycosides and Quercetin -3- rhamnosides, has tyrosinase different degrees of stimulation, wherein 100 μM of hardship
The wooden ketone, Astragaloside IV and Quercetin -3- rhamnosides molecular solution can significantly increase the activity of tyrosinase.
How using Michaelis-Menten equation the Km and Vmax in enzyme reaction are found out by double reciprocal plot displaying (see attached drawing 4).From
The natural plants molecule of various concentration makees double reciprocal plot to the result of tyrosinase humidification, then find out opposite Km and
Vmax can know humidification is which kind of belongs to using these Km and Vmax with the variation of natural plants molecular concentration
Mechanism.As shown in figure 5, in stimulation by double reciprocal plot from the natural plants molecule of various concentration to tyrosinase,
It was found that as the Vmax in the increase tyrosinase reaction of natural plants molecular concentration starts to increase and the then constant (Non- of Km
Competitive is noncompetitive).The constant normal knots for illustrating natural plants molecule and not interfering with tyrosine and tyrosinase of Km
It closes, and Vmax indicates that natural plants molecule can enhance the work that tyrosinase converts tyrosine as natural plants molecular concentration increases
Property.The mechanism of action that the mechanism is significantly followed by the α-MSH of carcinogenic risk is completely different.α-MSH are the letters by cell merely
Road increases the expression number of tyrosinase, and natural plants molecule is then the transformation efficiency for enhancing tyrosine.Therefore, natural to plant
Object molecule has very big potential development at the safe black product of U.S..
It is by above-mentioned experiment it is found that of the present invention including quassia ketone, Astragaloside IV and Quercetin -3- rhamnosides
Natural plants molecule can be played the role of by the stimulation to tyrosinase it is U.S. black.It is black to can be used for preparing various U.S.s
Product.
Inventor further analyzes Astragaloside IV and Quercetin -3- rhamnosides may be such as with the reason of U.S. black effect
Under:Radix Astragali can inhibit degradation of the hypoxia-inducible factor-1 alpha (HIF-1 α) under normal oxygen environment, and lead to the accumulation of HIF-1 α, cause
Cell generates a false micro-environmental hypoxia.And the melanocyte of skin epidermis substrate is deposited on always situated in multilayer skin
In most anoxic region, melanocyte in the micro-environmental hypoxia of skin can pass through HIF-1 α and Akt accesses promote melanocyte
It generates.Astragaloside IV may be by inhibiting the activity of HIF-1 α degradations in melanocyte to generate false micro-environmental hypoxia, then
Increase in melanocyte the generation of melanin by the channels Akt- by reaches U.S. black effect.
Quercetin possesses the ability of activation estrogen receptor, and activation estrogen receptor may be with Quercetin -3- rhamnosides
U.S. black effect it is related because tyrosinase is to keep skin U.S. black through melanin production, and the channels Wnt- are one of them
The channel of tyrosinase expression is controlled, the receptor Frizzled of Wnt- channels is one of estrogen receptor again.Therefore,
May be relevant property between Quercetin -3- rhamnosides, the channels Wnt- and U.S. black effect three.
Application of the Chinese medicine natural plants molecule disclosed in this invention in U.S. black effect, compared with traditional U.S. black method,
The risk of cutaneum carcinoma caused by due to using chemical synthesis class tanning agent and excessive sun to bathe can substantially be lowered.In addition, raw material at
Originally it substantially reduces, so as to reduce product price, can be widely used in drug, health products, food and beauty product, have huge
Big market potential.
Each technical characteristic of embodiment described above can be combined arbitrarily, to keep description succinct, not to above-mentioned reality
It applies all possible combination of each technical characteristic in example to be all described, as long as however, the combination of these technical characteristics is not deposited
In contradiction, it is all considered to be the range of this specification record.
Several embodiments of the invention above described embodiment only expresses, the description thereof is more specific and detailed, but simultaneously
It cannot therefore be construed as limiting the scope of the patent.It should be pointed out that coming for those of ordinary skill in the art
It says, without departing from the inventive concept of the premise, various modifications and improvements can be made, these belong to the protection of the present invention
Range.Therefore, the protection domain of patent of the present invention should be determined by the appended claims.
Claims (7)
1. application of the Chinese medicine natural plants molecule in the product for preparing enhancing tyrosinase activity.
2. Chinese medicine natural plants molecule has effects that apply in U.S. black product in preparation.
3. application according to claim 1 or 2, which is characterized in that the Chinese medicine natural plants molecule is selected from quassia ketone, Huang
At least one of stilbene first glycosides and Quercetin -3- rhamnosides.
4. application according to claim 1 or 2, which is characterized in that the product is cosmetics, drug or food.
5. a kind of having effects that U.S. black cosmetics, which is characterized in that the active constituent in the cosmetics includes Chinese medicine day
Right plant molecular, the Chinese medicine natural plants molecule in quassia ketone, Astragaloside IV and Quercetin -3- rhamnosides at least
It is a kind of.
6. a kind of having effects that U.S. black drug, which is characterized in that the active constituent in the drug includes that Chinese medicine is naturally planted
Object molecule, the Chinese medicine natural plants molecule in quassia ketone, Astragaloside IV and Quercetin -3- rhamnosides at least one
Kind.
7. a kind of having effects that U.S. black food, which is characterized in that include Chinese medicine natural plants molecule in the food, it is described
Chinese medicine natural plants molecule is selected from least one of quassia ketone, Astragaloside IV and Quercetin -3- rhamnosides.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116549469A (en) * | 2023-02-27 | 2023-08-08 | 中国科学院新疆理化技术研究所 | Application of flavonoid compound quercetin-3-O- (6' -caffeoyl) -beta-D-glucoside |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103058974A (en) * | 2012-11-26 | 2013-04-24 | 中国人民解放军军事医学科学院毒物药物研究所 | Natural compound and preparation method and application thereof |
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2017
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103058974A (en) * | 2012-11-26 | 2013-04-24 | 中国人民解放军军事医学科学院毒物药物研究所 | Natural compound and preparation method and application thereof |
Non-Patent Citations (1)
| Title |
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| GALLANT K. L. CHAN等: "A High Throughput Screening Platform for Skin Tuning Properties from Natural Products: Identification of Skin Tanning Compounds", 《JOURNAL OF COSMETICS, DERMATOLOGICAL SCIENCES AND APPLICATIONS》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN116549469A (en) * | 2023-02-27 | 2023-08-08 | 中国科学院新疆理化技术研究所 | Application of flavonoid compound quercetin-3-O- (6' -caffeoyl) -beta-D-glucoside |
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