Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Conjugate for inhibiting melanin synthesis, and application of conjugate in medicines and cosmetics

A technology for inhibiting melanin and conjugates, applied in the field of biomedicine, can solve the problems of low whitening efficiency, the effect needs to be further improved, and the composition is complex.

Active Publication Date: 2020-01-14
深圳前海港影生物科技有限公司
View PDF8 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the composition of this invention is complicated, the preparation is unchanged, and the whitening efficiency is not high
[0006] CN1311834C discloses that ergosterol derivatives can be used to prepare melanin production inhibitors, and the minimum concentration for inhibiting melanin formation is 0.5 micrograms / ml, and the effect needs to be further improved

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Conjugate for inhibiting melanin synthesis, and application of conjugate in medicines and cosmetics
  • Conjugate for inhibiting melanin synthesis, and application of conjugate in medicines and cosmetics
  • Conjugate for inhibiting melanin synthesis, and application of conjugate in medicines and cosmetics

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Preparation of polypeptide-compound conjugates

[0030] The compound of formula (I) of the present invention was synthesized according to the synthetic route of the compound in CN104302635A. Add 1mmol of the compound of formula (I), 1mmol of O-benzotriazole-N,N,N',N'-tetramethylpirouentetrafluoroborate (TBTU), 5ml of DMF, nitrogen protection, drop Add 0.5mmol) N,N-diisopropylhexylamine (DIEA), stir at 25°C for 1.5h, add 0.1g targeting membrane-penetrating active peptide TMT, stir at 25°C for 2h, and terminate the reaction. After confirming the correct molecular weight using MS-IT-TOF, the crude product was purified using HPLC. The structural formula of the conjugated product obtained through structural analysis is as follows:

[0031] .

Embodiment 2

[0032] Example 2 MTT method to detect the proliferation of B16 cells

[0033] B16 cells in the logarithmic growth phase were taken, digested with 0.05% trypsin + 0.53 mmol / L EDTA solution, and prepared with fresh culture medium at a density of 6×10 3 cells / mL cell suspension, seeded in 96-well cell culture plate, 180 μL per well, in CO 2Incubate overnight in the incubator. Four sample mass concentration gradients were set for each sample, and each gradient was repeated 3 times. In a 96-well cell culture plate, add the sample diluent and supplement it with PBS to 20 μL, so that the final mass concentration of the samples in the cell culture plate (respectively compound, polypeptide, and conjugate) is 1 ug / L, 1 mg / L, 10 mg / L, 100 mg / L; add 20 μL PBS to the blank control well, and mix well. Place the cell plate in CO 2 After incubation in the incubator for 48 h, the culture solution was sucked off, and 100 μL of PBS and 10 μL of 5 mg / mL MTT solution were added to each well,...

Embodiment 3

[0037] Example 3 Detection of cell apoptosis by flow cytometry: PI single staining method

[0038] B16 cells in the logarithmic growth phase were taken, digested with 0.05% trypsin + 0.53 mmol / L EDTA solution, and prepared with fresh culture medium at a density of 6×10 3 cells / mL cell suspension, seeded in 96-well cell culture plate, 180 μL per well, in CO 2 Incubate overnight in the incubator. Four sample mass concentration gradients were set for each sample. In a 96-well cell culture plate, add the sample diluent and supplement it with PBS to 20 μL, so that the final mass concentration of the samples in the cell culture plate (respectively compound, polypeptide, and conjugate) is 1 ug / L, 1 mg / L, 10 mg / L, 100 mg / L; add 20 μL PBS to the blank control well, and mix well. Place the cell plate in CO 2 After incubation in the incubator for 48 h, the culture medium was aspirated, centrifuged at 500 r / min for 10 min, and the culture medium was discarded. Wash once with 3ml PB...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention provides a conjugate for inhibiting melanin synthesis, and shows a good inhibition activity for tyrosinase. Meanwhile, after the conjugate is prepared into the cosmetics, the cosmetics do not irritate skins and have a good whitening function.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a conjugate for inhibiting melanin synthesis and its application in medicine and cosmetics. Background technique [0002] The overall scale of my country's cosmetics market ranks second in the world. With the rapid development of the national economy, it surpassed the United States in 2018 to have the world's largest cosmetics market. Skin care products are the sub-sector with the largest scale and the largest absolute growth rate in the entire cosmetics industry. Among them, whitening products are favored by Chinese consumers. [0003] The current whitening principle in cosmetics is mainly to eliminate melanin. With the development of skin physiology, people have gradually discovered the principle of melanin production. Through model screening, many new whitening ingredients have been discovered. Adding these ingredients in cosmetics, they can be obtained from Inhibit melanin produc...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K47/64A61K31/5377A61P17/00A61K8/19A61K8/27A61K8/34A61K8/37A61K8/49A61K8/64A61K8/9789A61Q19/02C07K14/00C07K1/02
CPCA61K8/19A61K8/27A61K8/34A61K8/345A61K8/37A61K8/494A61K8/64A61K8/9789A61K31/5377A61K47/64A61P17/00A61Q19/02C07K14/00
Inventor 彭菲李静
Owner 深圳前海港影生物科技有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com