LU500951B1 - Composition with tyrosinase inhibiting effect and its application - Google Patents
Composition with tyrosinase inhibiting effect and its application Download PDFInfo
- Publication number
- LU500951B1 LU500951B1 LU500951A LU500951A LU500951B1 LU 500951 B1 LU500951 B1 LU 500951B1 LU 500951 A LU500951 A LU 500951A LU 500951 A LU500951 A LU 500951A LU 500951 B1 LU500951 B1 LU 500951B1
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- composition
- glabridin
- resveratrol
- tyrosinase
- application
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
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- 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
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/05—Phenols
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- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
-
- 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
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/347—Phenols
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
- A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Dermatology (AREA)
- Birds (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Emergency Medicine (AREA)
- Botany (AREA)
- Mycology (AREA)
- Nutrition Science (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
This invention provides composition with tyrosinase inhibiting effect and its application, which consists of glabridin and resveratrol in a mass ratio of 0.33-3. Experiments prove that the composition provided by the invention has the effect of synergistically inhibiting tyrosinase, which can be used for treating chloasma, acne healing, freckle, senile plaque, post-sun repair and antioxidation.
Description
Description 4500951 Composition with tyrosinase inhibiting effect and its application Technical Heid This invention relates to à composition, particularly relates to composition with tyrosinase inhibiting effect and its application Background Pigmentation is the pigment change of human skin with different colors, different rañges and different shades due {0 Various reasons. The common symploms are chioasma, acnse healing, freckles and age spots. Take chicasma as an example, if is the most common melasma disease, which often occurs in the exposed paris of young and middis-aged women's faces, it is an aesthetic issue that is difficult to be cured. itis a major obstacle that is hard to solve in the medical field. Its characteristics arg: the incidence is influenced by many factors (ultraviciet stimulation, inflammatory reaction, etc), and it is a recurring Hiness that is easy to relapse. Al present, there are many treatment technologies and freckle removing products for chioasma, but most of tham are expensive, and the curative effect is unsatisfactory, and almost all of them are accompanied by adverse reactions. Therefore, there is an urgent need for a pharmaceutical composition for inhibiting tyrosinase with low cost, definite curative effect and no adverse reaction, Summary The purpose of the present invention is to overcomes the shortcomings of the prior art and provide a pharmaceutical composition with tyrosinase inhibiting effect The other object of the present invention is to provide the application of the above composition in preparing cosmetics or drugs for inhibiting tyrosinase.
A composition with tyrosinase inhibiting effect is composed of glabridin and resveratrol in a mass ratio of 0.33-3.
Preferably, the mass ratio of glabridin io resverairol is 1.
The application of the composition in the preparation of drugs or cosmetics with 4500951 tyrosinase inhibition, Experiments prove that the composition of the invention has the effect of synergistically inhibiting tyrosinase, and can be used for treating chicasma, acne healing, freckle, senile plague, post-sun repair and antioxidation, Description of the present invention in the following, the present invention will be further explained with specific examples. The sxampiss of the present invention are intended to enable the technicians in the field to better understand the present invention, but they do not Hmit the present invention in any way.
Embodiment 1 À composition with tyrosinase inhibiting effect is composed of glabridin and resveratrol in a mass ratio of 0.331.
Embodiment 2 A composition with tyrosinase inhibiting effect is composed of glabridin and resveratrol in a mass ratio of 1:1.
Ernbodiment 3 À composition with tyrosinase inhibiting effect is composed of glabridin and resveratrol in 3 mass ratio of 301.
Embodiment 4, Experiment of Inhibiting Tyrosinasse Action 1 instruments and reagents.
1.1 Experimental instruments as table 1 shown Table 1 List of instruments used in the experiment microporous plate detector instrument factory (Hundred thousandth)
96 pore plate Tianjin Kangkede Tech company LU500951
1.2 Experimental reagents as table Z shown, Table 2 List of reagents used in the experiment Batch number Resveratrol 98% Shanxi kangsheng 100401 Biotech company China National Institute Glabridin 98% for Food and Drug 100081-200907 Control Tyrosinase specific activity | Shanghai Baili Biotech 33K14431 25kU company . Shanghai Baoman 0, - - Biotech Company cote Tianjin Chinese medicine colleauge Distilled water Preparation Center of Chinese Medicine Research Institute Dimethyl sulfoxide (DMSO), methyl alcohol, absolute ethyl alcohol, sodium dihydrogen phosphate, Tianjin Kangkede Tech disodium hydrogen company phosphate, monopotassium phosphate, dipotassium phosphate
2. sample preparation FERS (pH = 8.0) Accurately weigh 5.580¢g of dipotassium hydrogen phosphate and 0.410g of potassium dihydrogen phosphate respectively, add a small amount of water to dissolve, and keep the volume to 1000mi at 0 ~ 4°C for later use. PBS (pH = 6.8) Accurately weigh 1.1869 of disodium hydrogen phosphate and
1.0009 of sodium dihydrogen phosphate respectively, add a small amount of water to dissolve, and keep the volume to 500mi at 0 ~ 4°C for later use.
Tyrosing solution (substrate): Accurately weigh 4.500mg of tyrosine, add 1001p 1 4500951 hydrochloric acid (2%), and dilute It to 10mb with PBS with pH = 8 for later use.
20% DMSO solution. take 2mi dimethyl sulfoxide (DMSO) and dilute it to 10m] with PES with pH = 6.8 for later use.
Preparation of test solution: Accurately weigh 10mg of glabndin and 10 mg of resveratrol respectively, dissolve them in 20% DMSO solution, and put them indo a 10mi volumetric flask with PBS with pH = 6.8 to obtain main mother liquor for later use.
Sample configuration of glabridin, the mother Hquor of glabridin 1mga/mi was diluted 10 times to obtain 100ug/mb stock solution, and the 1DO0ug/mEL stock solution was diluted 8 times, 10 times, 16 times, 50 times and 320 times respectively to obtain
12.5, 10 times, 8.25 times, 1.25 times, 0.625 times and 0.31 3ugml sample solutions, The configuration of resveratrol sample is the same as that of glabridin sample.
Sample preparation of Embodiment 1 composition: glabridin and resveratrol were diluted to 8-foid, 10-foid, 16-fold, 80-fold and 320-fold solutions, and 1 part of glabridin solution and 3 parts of resveratroi solution with the same concentration were mixed svenly, thus oblaining the sample solution with the mass ratio of glabrioin and resveratroi of 0.331.
Sample preparation of Embodiment 2 composition: glabridin and resveratrol were diluted to Sold, 10-fold, 16-fold, 80-fold and 320-foild solutions, respectively, and 1 part of glabridin solution and 1 part of resveratrol solution with the same concentration were mixed evenly to obtain the sample solution with the mass ratio of glabridin and resveratrol of 1:1.
Sample preparation of Embodiment 3 composition: giabridin and resveratrol were diluted to S-fold, 10-fold, 16-fold, 80-fold and 320-fold solutions, respectively, and 3 parts of glabridin solution and 1 part of resveratro! solution with the same concentration were evenly mixed to obtain the sample solution with the mass ratio of glabridin and resveratrol of 3:1
3. Experimental methods
Prepare according to ihe following contents: À: 20% DMSO 30 ul+410 ui PRS = 17900991 G.85+50 ji tyrosine 8: 20% DMSO 30 u L+150 ul PHH = 65 PBS ©: Sample (20% DMSO) 30 ui+110 ul PBS = 8.8450 ul tyrosine D: Sample (20% DMSO) 30u HSU PES with PHH = 6,8 To completes the above operation, keep the 96-well plate in a water bath at 37°C for 10min, then add SOUL of tyrosinase with 581UmL to sach well, and quickly Qui it in the microplate reader after 40min of reaction, and messure the absorbance at 475nm.
A-B-(C-D) Inhibition ratio. == eee x 100% A-B 4, Experimental data Table 3 Inhibitory effect of glabridin and resveratrol on tyrosinase Lu Élabrieis Resveratrol Lamebration à ape 5 toh Edition ratio Concentration {pgheld Inhibätion retio {tt ALE 11d {LIES ELSE E28 Sia EN 44,61 Hy EN 10 36.78
0 . . . LU500951 Table 4 Inhibitory effect of composition (different ratio of glabridin to resveratrol) on iyrosinase Frnkexiimmem ! ERNE a. Ne NN
ES ARK BATT Embediment 2 FEE HEN Sas Eon Frmtiodimerr 3 San 5 WAM ERE With the increase of the mass concentration of glabriding the inhibition raie of tyrosinase increases. The experimental results are shown in Table 3. The 1050 of glabridin is 1.72 uo/rnL. With the increase of resveratrol concentration, the inhibdion rate of tyrosinase increases. The experimental results are shown in Table 3 The ICSO of resveratrol is 7 50ug/mL. The 1050 value of the composition of embodiment 1 (0331) is 1.098ug/mL, and the experimental results are shown in Table 4. Embodiment 2 composition (1:1), 1050 values is 0.238ug/mb, and the experimental results are shown in Table 4. The 1250 value of the composition (3: 1) in embodiment 2 is 0 146ug/mL, and the experimental results ara shown in Table 4. Statistical methods
Can LU500951 Male TTT Rowe Fe Wane Wasa Wiesmann ICSdAmix and ICS0BmMIiIX are the 1C50 values of a (glabridin) and b (resveratrol) tyrosinase inhibilors in the composition respectively.
ICSOA and 1C50B are ICSO values of À and B acting alone, respectively. F1 and PZ are the proportions of À and B in total substances, respectively, Hy = 1, the interaction is additive, If y<1, the interaction is synergistic, and the smaller the y value, the stronger the synergistic effect, I v>1, the interaction is antagonistic, 8 Statistical results Table 5 Statistical analysis results of inhibition rates of glabridin and resveratrol on ivrosinase ot 8.130 fim 159 as date *; P<0.01
3. Result When the composition ratio of glabridin and resveratrol is 0321, the ICSOrrmix value is less than IC50add, and the interaction index y is less than 1, which indicates that glabridin and resveratrol have a synergistic effect. The experimental results are shown in Table 5, When the composition ratio of glabridin and resveratrol is 1.1, the ICEOmix value is less than ICS0add, and the interaction index v is lass than 1, which indicates that glabridin and resveratrol have a synergistic effect. The experimental results are shown in Table 5.
When the composition ratio of glabridin and resveratrol is 3:1, the 1ICE0mix value 79500951 is less than IC50add, and the interaction index y is less than 1, which indicates that glabridin and resveratrol have a synergistic effect The experimental results are shown in Table 5,
The 1C50mix values are all less than IC50add, and the interaction index y is all less than 1, which indicates that glabridin and resveratrol have synergistic effect, and the synergistic effect of glabridin and resveratrol is 3:1>1:1>0 33:1,
The composition of the invention can be prepared info cream, gel and film by corvertional methods for the treatment of chioasma, acne healing, freckles and senile plaques.
Claims (3)
1. Composition with tyrosinase inhibiting effect and its application is characterized in consisting of glabridin and resverairoi in a mass ratio of 0.33-3.
à. The composition, according to claim 1, is characterized in that the mass ratio of glabridin and resveratrol is 1.
3. The composition, according to claim 1 or claim 2, is characterized in being Used for preparation of drugs or cosmetics for inhibiting tyrosinase.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| LU500951A LU500951B1 (en) | 2021-12-03 | 2021-12-03 | Composition with tyrosinase inhibiting effect and its application |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| LU500951A LU500951B1 (en) | 2021-12-03 | 2021-12-03 | Composition with tyrosinase inhibiting effect and its application |
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| Publication Number | Publication Date |
|---|---|
| LU500951B1 true LU500951B1 (en) | 2022-06-03 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| LU500951A LU500951B1 (en) | 2021-12-03 | 2021-12-03 | Composition with tyrosinase inhibiting effect and its application |
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| Country | Link |
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| LU (1) | LU500951B1 (en) |
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2021
- 2021-12-03 LU LU500951A patent/LU500951B1/en active IP Right Grant
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