CN112451403A

CN112451403A - Application of combination of ectoin and 4-methoxy potassium salicylate in cosmetics

Info

Publication number: CN112451403A
Application number: CN202011459053.1A
Authority: CN
Inventors: 刘蒙蒙; 吴越
Original assignee: Bloomage Biotech Co Ltd
Current assignee: Bloomage Biotech Co Ltd
Priority date: 2020-12-11
Filing date: 2020-12-11
Publication date: 2021-03-09
Anticipated expiration: 2040-12-11
Also published as: CN112451403B

Abstract

The invention discloses an application of a combination of ectoin and 4-methoxy potassium salicylate in cosmetics, and particularly relates to an application of a combination of ectoin and 4-methoxy potassium salicylate as whitening components in cosmetics. According to the invention, the ectoin and the 4-methoxy potassium salicylate are combined for use, so that the whitening synergistic effect is obvious, under the effect, the 4-methoxy potassium salicylate with the concentration lower than that of the cosmetics in the market can be used under the condition of realizing the same whitening effect, and thus, the raw material cost can be reduced, the skin irritation can be reduced, the whitening effect can be achieved, and the excellent effect is achieved.

Description

Application of combination of ectoin and 4-methoxy potassium salicylate in cosmetics

Technical Field

The invention relates to an application of a combination of ectoin and 4-methoxy potassium salicylate in cosmetics, relates to an application of ectoin and 4-methoxy potassium salicylate as whitening components in cosmetics, and belongs to the technical field of cosmetics.

Background

With the continuous progress of economy and technology and the increasing consumption level of the people, the demand of consumers for functional cosmetics is increasing. Data from intein (Mintel) show: the new variety of Asia-Tai region 2015-2019 declares the proportion of whitening and brightening cosmetics-Chinese new variety ranks first (proportion 29%), and then Japan and Korea. That is, the cosmetic having the whitening effect is very popular with consumers. Whitening cosmetics are formally brought into the management category of special-purpose cosmetics in 2014, and the reasonable collocation of functional raw materials of the products is also paid more and more attention. Therefore, the development of safe, non-irritant, pigmentation-improving cosmetic raw material formulations is a focus of common attention of research and development engineers, manufacturers and consumers.

The skin color tone is influenced by various factors, but is mainly influenced by the amount of melanin in cells and the number, size, distribution, degree of blackening, etc. of secretory melanin granules. The formation of skin melanin can be summarized as: melanocytes produce melanin, that is, melanocytes of the skin generate melanin by using tyrosine as their own substrate under the oxidation action of various enzymes, and the formed melanin granules are transported to basal layer cells of the epidermal layer of the skin through dendrites of the melanocytes, are further carried to the stratum corneum along with cell metabolism, and are finally discharged along with the periodic shedding of the stratum corneum. There are various biological enzymes involved in melanin formation, among which tyrosinase is an enzyme that plays a central role in melanin synthesis, and the size of its activity determines the amount of melanin formation. That is, by regulating the activity of tyrosinase, melanin production can be reduced, thereby achieving a whitening effect.

4-MSK (potassium 4-methoxysalicylate), a tyrosinase inhibitor, can inhibit melanin production and accelerate the turnover of stratum corneum. The seniority in vivo studies indicated that the test article containing 1% to 5% 4MSK had a concentration-dependent effect on uv-induced pigmentation. In 2007, the department of health approves potassium 4-methoxysalicylate as a cosmetic raw material, and the concentration cannot exceed 3%. In the field of cosmetics, 4-MSK plays an important role in whitening, and 4-MSK is already added into whitening products of brand skin care varieties such as a senior, an European Peltier and the like.

However, 4-MSK has structural similarity with salicylic acid, has certain irritation to skin, and the irritation is increased along with the increase of the content. In order to improve the whitening effect, 4-MSK is often added into the existing cosmetics at high concentration, but the result has certain irritation to the skin and certain limitation on the application of the efficacy of the cosmetics. Therefore, how to reduce the irritation of the 4-MSK and keep the whitening effect of the 4-MSK without losing is of great research significance for the application of the 4-MSK in cosmetics.

Disclosure of Invention

Aiming at the technical problems of whitening and skin irritation of 4-MSK, the invention provides an effective solution, namely the ectoin and the 4-methoxy potassium salicylate are jointly used in cosmetics, so that the use amount of the 4-methoxy potassium salicylate can be reduced, the skin irritation is reduced, and the combination of the ectoin and the 4-methoxy potassium salicylate has an obvious whitening synergistic effect, so that the whitening effect cannot be reduced or cannot be obviously reduced when the content of the 4-methoxy potassium salicylate is reduced.

Ectoin (1,4,5,6-Tetrahydro-2-methyl-4-pyrimidinecarboxylic acid), named as Ectoin (2-methyl-1, 4,5, 6-Tetrahydro-methyl pyrimidine-4-carboxylic acid), was first isolated from the extreme halophilic Rhodospirillum thioparvum in 1985 by the German scientist Galinski, and the cyclic structure of the molecule has strong electronegativity and readily forms hydrogen bonds with water molecules, thereby enhancing the association ability of water molecules, orienting the water molecules around them, changing the spatial arrangement of water molecules, and thus forming a separation layer around cells, enzymes, proteins and other biomolecules. Due to the existence of the isolation layer, the skin cells are equivalently armed, have better anti-impact capability and can block or reduce the stimulation of external stimulation factors to the skin cells. Research by Bitop AG in germany indicates that 0.5% ectoin is effective in protecting langerhans cells (located between corneocytes of the epidermis layer of the skin, belonging to immune cells, and protecting the skin against microorganisms, UV light, allergens, etc.) under UV irradiation to the skin completely.

Creatively discovers in research that the combination of 4-MSK and ectoin has the effects of inhibiting tyrosinase activity and melanin content generation, can improve the whitening effect of the 4-MSK, and has synergistic skin whitening effect. And when the low-content 4-MSK is compounded with the ectoin, the skin irritation can be reduced, the whitening effect can be improved, and the preparation method has a remarkable significance for development of efficacy type cosmetics.

The specific technical scheme of the invention is as follows:

use of a combination of ectoin and 4-methoxysalicylic acid potassium in cosmetics.

Further, in the above application, the combination of ectoin and 4-methoxysalicylic acid potassium is used as a whitening component of cosmetics.

Furthermore, in the application, the content of the ectoin in the cosmetic is 0.01-1wt%, and the content of the 4-methoxy potassium salicylate in the cosmetic is 0.001-0.1 wt%.

Furthermore, in the above application, the content of ectoin in the cosmetic is preferably 0.1-0.5wt%, and the content of 4-methoxy potassium salicylate in the cosmetic is preferably 0.01-0.1 wt%.

Further, in the above application, the content of ectoin in the cosmetic is more preferably 0.3 to 0.5wt%, and the content of 4-methoxysalicylic acid potassium in the cosmetic is more preferably 0.1 wt%.

The invention also provides a composition with whitening effect, which contains whitening active ingredients, wherein the whitening active ingredients refer to active ingredients with the capability of reducing tyrosinase activity and melanin content generation, and preferably active ingredients with the capability of reducing cell tyrosinase activity and melanin generation. Preferably, the whitening active ingredient contains ectoin and 4-methoxy potassium salicylate.

Furthermore, the invention also provides a cosmetic which contains the composition with the whitening effect.

Furthermore, in the cosmetic, the content of ectoin in the cosmetic is 0.01-1wt%, and the content of 4-methoxy potassium salicylate in the cosmetic is 0.001-0.1 wt%.

Further, in the above cosmetic, the content of ectoin in the cosmetic is preferably 0.1 to 0.5wt%, and the content of potassium 4-methoxysalicylate in the cosmetic is preferably 0.01 to 0.1 wt%.

Further, in the above cosmetic, the content of ectoin in the cosmetic is more preferably 0.3 to 0.5wt%, and the content of potassium 4-methoxysalicylate in the cosmetic is more preferably 0.1 wt%.

Further, the above cosmetics refer to products which are spread on any part of the surface of the human body, such as skin, hair, nails, lips, and teeth, by painting, spraying, or the like, so as to clean, maintain, beautify, modify, and change the appearance, or correct the smell of the human body. The form of the cosmetic is not particularly limited, and may be determined according to the use, such as cleansing cream, essence, lotion, cream, lotion (such as smoothing toner, toner), pack, makeup remover, gel, aerosol or spray, and the like, and the preparation method thereof is a conventional preparation method in the art.

Furthermore, the cosmetic can also comprise other functional components, such as components with the functions of whitening, moisturizing, removing acnes, resisting wrinkles and the like, besides the ectoin and the 4-methoxy potassium salicylate. In addition to the efficacy ingredient, the cosmetic may further include adjuvants necessary for making into various usable forms, such as thickening agents, solubilizers, stabilizers, softeners, aerosol solvents, preservatives, surfactants, controlled-release agents, sustained-release agents, fragrances, toners, penetration enhancers, moisturizers, emulsifiers, plasticizers, pearlizing agents, and the like.

Further, the kind of the cosmetic is not particularly limited, and it may be a basic cosmetic, a face makeup cosmetic, a body makeup cosmetic, or the like.

According to the invention, the ectoin and the 4-methoxy potassium salicylate are combined for use, so that the whitening synergistic effect is obvious, under the effect, the 4-methoxy potassium salicylate with the concentration lower than that of the cosmetics in the market can be used under the condition of realizing the same whitening effect, and thus, the raw material cost can be reduced, the skin irritation can be reduced, the whitening effect can be achieved, and the excellent effect is achieved.

Detailed Description

The invention is further illustrated by the following examples, which are not intended to limit the scope of the invention. The experimental methods without specifying specific conditions in the following examples were selected according to the conventional methods and conditions, or according to the commercial instructions.

The reagents and starting materials used in the present invention are commercially available.

Example 1

Experimental materials: active substance ectoin, 4-methoxy potassium salicylate, DMEM medium.

Test sample solutions: diluting ectoin and 4-methoxy potassium salicylate with culture medium respectively to prepare experimental sample solutions with different final concentrations.

And (3) toxicity detection: after co-culturing the B16 cells with different experimental sample solutions for 1 day, removing the experimental sample solution, adding MTT, carefully removing supernatant after 3 hours, adding dimethyl sulfoxide (DMSO), and detecting at 550 nm; with reference to the untreated well, the sample well is defined as T, the untreated well as NT, NT is defined as 100%, and the ratio of T/NT in the sample well is defined as the increment rate.

The normal growth and metabolism status of B16 cells is a precondition for detecting the efficacy of the active substances, if the number of cells is not obviously reduced after the addition of the ectoine and the 4-methoxy potassium salicylate active substances, the concentration is considered to be the nontoxic dose of the ectoine and the 4-methoxy potassium salicylate active substances, and the cell proliferation rate is lower than 90 percent, and the cells are considered to be cytotoxic.

The specific test results are shown in table 1 below.

TABLE 1

Sample (I)	Cell proliferation Rate
		Ectoin-0.01 wt%	101％
Ectoin-0.05 wt%	102％
		Ectoin-0.1 wt%	100％
Ectoin-0.3 wt%	97％
		Ectoin-0.5 wt%	95％
Ectoin-0.8 wt%	95％
		Ectoin-1.0 wt%	94％
Ectoin-1.05 wt%	94％
		4MSK-0.01wt％	103％
4MSK-0.05wt％	99％
		4MSK-0.1wt％	95％
4MSK-0.3wt％	60％
		4MSK-0.5wt％	50％
4MSK-0.8wt％	19％
		4MSK-1.0wt％	14％
4MSK-1.05wt％	15％
		Control group (NT)	100％

From the above results, it can be seen that the cell proliferation rate of ectoin is not much changed, but not less than 90%, and it is considered that the cell proliferation rate is a nontoxic dose when the concentration of ectoin is not more than 1.05%, and the cell proliferation rate is significantly decreased when the concentration of 4-methoxysalicylic acid is more than 0.1%, and it is considered that the cell proliferation rate is a nontoxic dose when the concentration of 4-methoxysalicylic acid is not more than 0.1%.

Example 2

Test sample solutions: mixing ectoin and 4-methoxy potassium salicylate, diluting with culture medium to obtain experimental sample solutions with final concentration of 0.3% of 4-methoxy potassium salicylate and different final concentrations of ectoin.

The specific test results are shown in table 2 below.

TABLE 2

Sample (I)	Concentration of ectoin	Concentration of 4-methoxy potassium salicylate	Cell proliferation Rate
				1	0.01wt％	0.3wt％	61％
2	0.05wt％	0.3wt％	62％
				3	0.1wt％	0.3wt％	70％
4	0.3wt％	0.3wt％	72％
				5	0.5wt％	0.3wt％	75％
6	0.8wt％	0.3wt％	78％
				7	1.0wt％	0.3wt％	80％

As can be seen from the results in the above table, the addition of ectoin can reduce the toxic stimulation of potassium 4-methoxysalicylate to cells, and the effect is more obvious as the content of ectoin is increased.

Example 3

Test sample solutions: mixing the ectoin and the 4-methoxy potassium salicylate, diluting the mixture by using a culture medium to prepare experimental sample solutions with different final concentrations of the 4-methoxy potassium salicylate and the ectoin.

Control sample solution: and diluting the ectoin and the 4-methoxy potassium salicylate with culture media respectively to prepare a control sample solution.

And (3) tyrosinase activity detection: b16 cells are normally cultured for 1 day, then the experimental sample solution and the control sample solution with different concentrations are added for culturing, and after 3 days of culturing, tyrosinase activity detection is carried out, wherein an untreated hole is taken as a reference, a sample hole is defined as T, an untreated hole is defined as NT, NT is taken as 100%, and the ratio of the T/NT of the sample hole is taken as the tyrosinase activity rate.

The specific test results are shown in table 3 below.

TABLE 3

Sample (I)	Ectoine concentration/%)	Concentration/% of 4-methoxysalicylic acid potassium	Rate of tyrosinase activity
				1	0.01	0.1	70％
2	1	0.001	74％
				3	0.5	0.01	67％
4	0.1	0.1	62％
				5	0.2	0.1	57％
6	0.3	0.1	53％
				7	0.4	0.1	51％
8	0.5	0.1	50％
				9	——	0.1	78％
10	0.5	——	97％
				11	——	——	100％
12	——	0.5	55％

From the results in the table, it can be seen that 4-methoxy potassium salicylate has the effect of inhibiting tyrosinase activity, ectoin hardly has the effect of inhibiting tyrosinase activity, the inhibition effect of 4-methoxy potassium salicylate on tyrosinase activity can be enhanced by compounding ectoin different concentrations, and the inhibition effect of high-concentration 4-methoxy potassium salicylate on tyrosinase can be achieved by compounding low-concentration 4-methoxy potassium salicylate with a certain amount of ectoin.

Example 4

And (3) detecting the melanin content: b16 cells are normally cultured for 1 day, then the experimental sample solution and the control sample solution with different concentrations are added for culture, and then melanin detection is carried out after 3 days of culture, wherein detection takes an untreated hole as a reference, a sample hole is defined as T, the untreated hole is NT, NT is taken as 100%, and the ratio of the T/NT of the sample hole is taken as the melanin generation rate.

The specific test results are shown in table 4 below.

TABLE 4

Sample (I)	Ectoine concentration/%)	Concentration/% of 4-methoxysalicylic acid potassium	Rate of melanin production
				1	0.01	0.1	77％
2	1	0.001	89％
				3	0.5	0.01	84％
4	0.1	0.1	74％
				5	0.2	0.1	70％
6	0.3	0.1	67％
				7	0.4	0.1	65％
8	0.5	0.1	64％
				9	——	0.1	80％
10	0.5	——	95％
				11	——	——	100％
12	——	0.5	65％

From the results in the table, it can be seen that the 4-methoxy potassium salicylate has the effect of reducing the generation of melanin, and the reduction of the concentration of the 4-methoxy potassium salicylate and the compounding of ectoin have the additive effect of reducing the generation of melanin.

Application example

The composition of the 4-methoxy potassium salicylate and the ectoine is used in cosmetics, wherein the content of the 4-methoxy potassium salicylate in the cosmetics is 0.01-0.1wt%, the content of the ectoine in the cosmetics is 0.01-1wt%, and the content of the composition of the 4-methoxy potassium salicylate and the ectoine in the cosmetics is 1-2 wt%. According to the experimental results of examples 1 to 4, the effect was most excellent when the content of potassium 4-methoxysalicylate in the cosmetic was 0.1wt% and the content of ectoin in the cosmetic was 0.5 wt%.

The following best 4-methoxy potassium salicylate and ectoin are used as examples to prepare cosmetics, and the formula of the cosmetics is shown in the following table 5:

TABLE 5

TABLE 6

The emulsion with the formula is prepared according to a conventional cosmetic method, and comprises the following specific steps:

adding deionized water, glycerol tri (ethyl hexanoate), phenoxyethanol, glycerol stearate/PEG-100 stearate, butanediol, xanthan gum, ammonium acryloyldimethyl taurate/VP copolymer and glycerol into a water phase pot, heating and stirring at 80 deg.C for 30min to completely dissolve to obtain water phase; heating PPG-13-decyltetradecanol polyether-24 in an oil phase pot at 80 deg.C, stirring for 30min to completely dissolve to obtain an oil phase; then adding the water phase and the oil phase into an emulsifying pot, emulsifying and homogenizing at 65 ℃ for 15 min; cooling to 40 deg.C, adding active substance, and stirring; and finally, defoaming and filling to obtain the product.

The whitening experiment is carried out on the emulsions containing different 4-methoxy potassium salicylate and ectoin, 20 testers with dark faces, all women and ages of 24-40 years, are selected, the testers are divided into 4 groups, and different emulsions are respectively tried on each group. The using method of each tester is as follows: the face was cleaned and the lotion applied daily in the morning and evening, and the testers avoided using other related whitening products of the same type during this test. After the product is continuously used for 60 days, the evaluation conditions of the testers on the whitening and skin color brightening effects of the product are counted through questionnaire form, the evaluation conditions are divided into four stages of obvious, common and unobvious, the number of people at each stage is counted, and the results are shown in the following table 7:

TABLE 7

To summarize: from the results in table 7, it can be seen that the whitening and skin-lightening effects of the samples 8 and 12 are better than the whitening effect of the sample 9-10, after the 4-methoxy potassium salicylate and the ectoin are compounded, the whitening effect is obviously better than the effect of any single product of the two, the effects of the samples 8 and 12 are close, and the combined application value of the low-dose 4-methoxy potassium salicylate and the ectoin is higher in terms of raw material cost and irritation.

The embodiments of the present invention have been described in detail, but the embodiments are merely examples, and the present invention is not limited to the embodiments described above. Any equivalent modifications and substitutions to those skilled in the art are also within the scope of the present invention. Accordingly, equivalent changes and modifications made without departing from the spirit and scope of the present invention should be covered by the present invention.

Claims

1. The application of the combination of ectoin and 4-methoxy potassium oxyhydrate in cosmetics.

2. Use according to claim 1, characterized in that: the combination of ectoin and potassium 4-methoxyoxyhydrate is used as whitening component of cosmetic.

3. Use according to claim 1, characterized in that: the content of ectoin in the cosmetic is 0.01-1wt%, and the content of 4-methoxy potassium hydroxide in the cosmetic is 0.001-0.1 wt%.

4. Use according to claim 3, characterized in that: the content of ectoin in the cosmetic is 0.1-0.5wt%, and the content of 4-methoxy potassium oxyhydrate in the cosmetic is 0.01-0.1 wt%.

5. Use according to claim 3, characterized in that: the content of ectoin in the cosmetic is 0.3-0.5wt%, and the content of 4-methoxy potassium oxyhydrate in the cosmetic is 0.1 wt%.

6. A composition with whitening effect is characterized in that: contains ectoin and 4-methoxy potassium hydroxide.

7. A cosmetic, characterized by: a composition having whitening effect according to claim 6.

8. The cosmetic as set forth in claim 7, wherein: the content of ectoin in the cosmetic is 0.01-1wt%, and the content of 4-methoxy potassium hydroxide in the cosmetic is 0.001-0.1 wt%.

9. The cosmetic as set forth in claim 7, wherein: the content of ectoin in the cosmetic is 0.1-0.5wt%, and the content of 4-methoxy potassium oxyhydrate in the cosmetic is 0.01-0.1 wt%.

10. The cosmetic as set forth in claim 7, wherein: the content of ectoin in the cosmetic is 0.3-0.5wt%, and the content of 4-methoxy potassium oxyhydrate in the cosmetic is 0.1 wt%.