CN114796046A - Whitening spot-lightening antioxidant composition and application thereof - Google Patents

Abstract

The invention relates to a whitening and spot-lightening antioxidant composition and application thereof, wherein the whitening and spot-lightening antioxidant composition comprises the following components in parts by weight: n-acetylneuraminic acid, tranexamic acid, hops extract and lotus embryo extract. The four active ingredients are creatively matched for whitening, spot-lightening and antioxidation, the four active ingredients supplement each other and can be synergistic, and the ingredients respectively inhibit the generation or transfer of melanin in an all-around and multi-angle manner through different ways or mechanisms, so that the whitening, spot-lightening and antioxidation effects of the product are obvious and long-acting.

Description

Whitening spot-lightening antioxidant composition and application thereof

Technical Field

The invention belongs to the technical field of cosmetics, and relates to a whitening and spot-lightening antioxidant composition and application thereof, in particular to a whitening and spot-lightening antioxidant composition and essence with whitening and spot-lightening antioxidant effects.

Background

"whitening" has always been an unchanging theme in the beauty market and has always been a great market demand. Whitening, spot lightening, freckle removing, yellow removing, black fading and the like become main requirements of the beautifying and whitening functions. The color of skin is controlled by various factors, mainly depending on the content and distribution of melanin. Melanin is an amino acid derivative formed by a series of chemical reactions, usually in the form of polymerization, of tyrosine or 3, 4-dihydroxyphenylalanine. The melanin is synthesized by melanocytes in the basal layer of human epidermis, when ultraviolet rays irradiate the skin, the skin is in a self-protection state, the activity of tyrosinase is activated, and the oxidation of tyrosine or 3, 4-dihydroxyphenylalanine is catalyzed to generate the melanin, so that the skin cells are protected. Melanin moves layer by layer through cell metabolism, and forms freckles, sunburn, black spots and the like on the skin epidermis.

The enzymes mainly involved in the melanin synthesis process comprise tyrosinase, dopachrome tautomerase and dihydroxyindole carboxylic acid oxidase, wherein the tyrosinase belongs to oxidoreductase and is the main rate-limiting enzyme for melanin synthesis, and the activity of the tyrosinase determines the formation amount of melanin. Tyrosinase has both monophenolase and diphenolase properties, i.e.functions as oxygenase and oxidase. During melanin synthesis, it can catalyze the hydroxylation of L-tyrosine to levodopa (monophenolase activity); the second step oxidizes levodopa to produce dopaquinone (diphenolase activity), which is unstable in nature and finally produces melanin after various complex non-enzymatic reactions.

Whitening oral products such as whitening pills, whitening tablets, anti-glycation oral liquids and the like have non-negligible side effects: the whitening tablet has side effect, and if the tablet is taken excessively, the risk of thrombus is caused; the important principle of the whitening tablet is to promote skin metabolism melanin, but the whitening tablet contains excessive vitamin c, and if the whitening tablet is taken for a long time, symptoms of abdominal pain, diarrhea and blood deficiency can appear, hyperuricemia is probably caused, so that generation of kidney stones can be accelerated, and great influence can be caused on the kidney.

The patent CN202110818300.0 discloses a whitening and moisturizing essence emulsion and a preparation method thereof, and the whitening and moisturizing essence emulsion comprises the following raw materials, by weight, 2-5 parts of water, 3-6 parts of glycerol, 5-8 parts of cucumber juice, 4-6 parts of essence, 2-5 parts of carbomer, 5-8 parts of mink oil, 2-4 parts of petrolatum, 4-6 parts of triethanolamine, 2-5 parts of glyceryl stearate, 4-6 parts of an antioxidant, 4-6 parts of anti-inflammatory light make-up water, 4-6 parts of honey water, 8-10 parts of a clitocybe herb liquid medicine, 4-6 parts of vitamins, 8-10 parts of a ginseng extract and 1-3 parts of a pilose antler extract. The whitening lotion has stronger water replenishing capacity, but the whitening effect is not proved by specific data, and the spot fading effect is not mentioned.

Patent CN201710391557.6 discloses a whitening and freckle-removing composition and a cosmetic, wherein the whitening and freckle-removing composition comprises the following components in parts by weight: 0.01-15 parts of raw materials for inhibiting tyrosinase activity or converting eumelanin into light melanin; 0.1-15 parts of raw materials for inhibiting tyrosinase expression; 0.01-10 parts of raw materials for increasing the activity of melanocyte-stimulating hormone receptors; 0.1-8 parts of liquid crystal emulsifier; the whitening and freckle-removing composition disclosed by the invention fully exerts the synergistic effect of all the components, and can effectively improve the darkness of the skin and brighten the skin color.

However, the whitening and freckle-removing effects of the products disclosed by the prior art are not very obvious and long-acting, so that the development of a product which is simple in preparation method and has a remarkable and long-acting whitening and freckle-removing effect is very meaningful.

Disclosure of Invention

Aiming at the defects of the prior art, the invention aims to provide a whitening and spot-lightening antioxidant composition and application thereof, and particularly provides a whitening and spot-lightening antioxidant composition and essence with whitening and spot-lightening antioxidant effects.

In order to achieve the purpose, the invention adopts the following technical scheme:

in a first aspect, the present invention provides a whitening and spot-lightening antioxidant composition comprising: n-acetylneuraminic acid, tranexamic acid, hops extract and lotus embryo extract.

N-acetylneuraminic Acid, also known as Sialic Acid (SA for short), is a naturally occurring amino sugar, and has the effects of resisting aging, brightening the skin, lightening fine lines of canthus and the like when being applied to cosmetics; and it is very soluble in water. Biochemical derivatives of sialic acid are also commonly used in the synthesis of pharmaceuticals.

Tranexamic acid is also known as trans-para-aminomethylcyclohexane carboxylic acid, fibrinolysin, tranexamic acid, and Xueshing. Tranexamic acid is used as a skin conditioner, a moisturizer and a whitening agent in cosmetics. It has the factor group for inhibiting melanin enhancement, thereby completely blocking the melanin formation path due to ultraviolet irradiation, preventing the black spot from thickening and enlarging, and effectively preventing skin pigmentation.

The flos Lupuli (Humulus LUPULUS) extract is rich in lupulone, tannin, volatile oil, humulone-II, gamma-dehydrocalamene, astragalin, isoquercitrin, rutin, kaempferol-3-rhamnosyl diglucoside, quercetin-3-rhamnosyl diglucoside, etc. The inhibition effect on elastase, the promotion effect on cerebral amide formation and the anti-oxidation property show that the composition can be used for preventing skin aging and wrinkle; leukocyte subsequent inhibition and activation of PPAR have been shown to be useful in preventing skin damage and skin inflammation, inhibiting inflammatory pigmentation; has strong antibacterial, enzyme inhibiting and antiseptic effects, and can be used for preparing oral preparation for removing halitosis and relieving itching of scalp.

The extract of plumule of Nelumbo NUCIFERA (Nelumbo NUCIFERA) contains liensinine, isoliensinine, neferine, nuciferine, pronucine, Calotropin, and desmethyl-linderane; it also contains flavonoid such as luteolin, hyperoside, and rutin. The extract has stimulating effect on the generation of collagen and elastin which constitute protein fiber, and has effect in enhancing skin activity, and can be used in anti-aging and anti-wrinkle cosmetics. Alkaloid contained in lotus embryo bud has effect of scavenging oxygen free radical, and oxygen free radical reacts with polyunsaturated fatty acid to cause various oxidative damage to organism.

The enzymes mainly involved in the process of melanin synthesis comprise tyrosinase, dopachrome tautomerase and dihydroxyindole carboxylic acid oxidase, wherein the tyrosinase belongs to oxidoreductase and is the main rate-limiting enzyme of melanin synthesis, and the activity of the tyrosinase determines the quantity of melanin formation. Tyrosinase is a copper-containing oxygen-requiring enzyme, and oxygen radicals must participate in the reaction process of converting tyrosine into melanin, so that the oxygen radicals can be removed to block the catalytic reaction of tyrosinase, thereby weakening the intensity of the tyrosine oxidation reaction.

The four active ingredients are creatively matched for whitening, spot-lightening and antioxidation, the four active ingredients supplement each other and can be synergistic, and the ingredients respectively inhibit the generation or transfer of melanin in an all-around and multi-angle manner through different ways or mechanisms, so that the whitening, spot-lightening and antioxidation effects of the product are obvious and long-acting.

Preferably, the whitening and spot-lightening antioxidant composition comprises the following components in parts by weight: 0.01-2 parts of N-acetylneuraminic acid, 0.05-2 parts of tranexamic acid, 0.1-4 parts of hop extract and 1-7 parts of lotus embryo extract.

The weight parts of the N-acetylneuraminic acid can be 0.01 part, 0.05 part, 0.1 part, 0.3 part, 0.5 part, 0.8 part, 1 part, 1.2 parts, 1.5 parts, 2 parts and the like.

The tranexamic acid may be present in an amount of 0.05 parts, 0.1 parts, 0.3 parts, 0.5 parts, 0.8 parts, 1 part, 1.2 parts, 1.5 parts, 2 parts, etc.

The weight parts of the hop extract can be 0.1 part, 0.5 part, 1 part, 1.5 parts, 2 parts, 2.3 parts, 2.5 parts, 3 parts, 3.5 parts, 4 parts and the like.

The lotus embryo extract can be 1 part, 1.5 parts, 2 parts, 2.5 parts, 3 parts, 3.5 parts, 4 parts, 5 parts, 6 parts, 7 parts and the like in parts by weight.

Other specific point values within the above numerical ranges can be selected, and are not described in detail herein.

The hop (Humulus LUPULUS) extract or lotus (Nelumbo NUCIFERA) germ extract related to the present invention can be obtained from commercially available raw materials or by self-production. The hop extract prepared by the method has better effect when being used in the product of the invention.

Preferably, the hop extract is prepared by a preparation method comprising the following steps:

(1) mixing hops and an ethanol water solution for ethanol extraction, and concentrating an extracting solution until no alcohol smell exists;

(2) extracting the concentrated solution obtained in the step (1) by using an organic solvent;

(3) and (3) purifying and drying the extracted aqueous solution obtained in the step (2) to obtain the compound.

Preferably, the concentration of the ethanol aqueous solution in the step (1) is 80-95%, such as 80%, 82%, 85%, 87%, 90%, 92%, 95% and the like.

Preferably, the mass ratio of the ethanol aqueous solution to the hops in the step (1) is 8-15 times, such as 8 times, 9 times, 10 times, 11 times, 12 times, 13 times, 14 times, 15 times, etc.

Preferably, the organic solvent in step (2) comprises any one of petroleum ether, pentane, hexane or heptane or a combination of at least two thereof.

Preferably, the purification in step (3) is performed by passing through a polyamide resin column and eluting with an aqueous solution of ethanol.

Preferably, the elution is a gradient elution from low concentration to high concentration with 25-60% ethanol aqueous solution. For example, the elution is performed sequentially with 25%, 40%, and 60% ethanol aqueous solutions, and the 60% ethanol eluate is collected.

In a second aspect, the present invention provides a use of the whitening and spot-lightening antioxidant composition according to the first aspect in the preparation of cosmetics.

Preferably, the cosmetic comprises essence, essence oil, lotion, cream, mask, eye cream, and facial cleanser.

In a third aspect, the invention provides an essence with whitening, spot-lightening and antioxidant effects, which comprises: the whitening spot-lightening antioxidant composition comprises a whitening spot-lightening antioxidant composition, a humectant, a thickening agent, an antibacterial preservative and water.

Preferably, the essence comprises the following components in parts by weight: 1-15 parts of whitening, spot-lightening and antioxidant composition, 0.1-10 parts of humectant, 0.1-5 parts of thickening agent, 0.01-1 part of antibacterial preservative and water.

The whitening and spot-lightening antioxidant composition can be prepared from 1 part, 3 parts, 5 parts, 8 parts, 10 parts, 12 parts, 14 parts, 15 parts and the like in parts by weight.

The humectant can be 0.1 part, 0.3 part, 0.5 part, 0.8 part, 1 part, 2 parts, 4 parts, 5 parts, 7 parts, 8 parts, 10 parts and the like by weight.

The weight portion of the thickening agent can be 0.1 portion, 0.3 portion, 0.5 portion, 0.8 portion, 1 portion, 2 portions, 4 portions, 5 portions and the like.

The weight portion of the antibacterial preservative can be 0.01 portion, 0.03 portion, 0.05 portion, 0.08 portion, 0.1 portion, 0.2 portion, 0.4 portion, 0.5 portion, 0.7 portion, 0.8 portion, 1 portion and the like.

Other specific point values within the above numerical ranges can be selected, and are not described in detail herein.

Preferably, the moisturizer comprises any one of jojoba esters, sodium hyaluronate, methyl propylene glycol, chlorella extract, dipotassium glycyrrhizinate, squalane, betaine or 1, 2-pentanediol or a combination of at least two of them.

A combination of squalane, dipotassium glycyrrhizinate and 1, 2-pentanediol is preferred.

Preferably, the thickener comprises any one of or a combination of at least two of hydroxypropyl guar, cetyl esters, glyceryl tribehenate, cellulose gum or carboxymethyl hydroxyethyl cellulose.

Preferably, the antimicrobial preservative comprises any one or a combination of at least two of methylparaben, 1, 2-hexanediol, caprylyl glycol, caprylyl hydroxamic acid, or 1, 2-pentanediol.

Compared with the prior art, the invention has the following beneficial effects:

the composition provided by the invention has the advantages that the four components are compatible, the component formula is reasonable, the active ingredients supplement each other, the synergistic effect can be realized, the generation or transfer of melanin can be inhibited in all directions and at multiple angles through different ways or mechanisms, and the whitening, freckle removing and oxidation resisting effects of the product are obvious and long-acting. The composition is applied to cosmetics, so that the prepared product has high safety performance and obvious long-acting whitening, freckle-removing and antioxidant effects.

Detailed Description

To further illustrate the technical means and effects of the present invention, the following further describes the technical solution of the present invention with reference to the preferred embodiments of the present invention, but the present invention is not limited to the scope of the embodiments.

The following examples, comparative examples, application examples, and comparative application examples relate to N-Acetylneuraminic acid, a product available from Wuhan's Keoguang Green Biotechnology, Inc. under the model number N-Acetylneuraminic acid; tranexamic acid is a product of tranexamic acid type purchased from Hunan Dongting drug Co., Ltd; the hop extract is a product of KPL-0048 (except examples 4-5) purchased from Shanxi Kepler Biotech Co., Ltd.; the lotus embryo extract is a product available from macro biotechnology limited of Nanjing beauty under model number LIENSININE.

Example 1

The embodiment provides a whitening and spot-lightening antioxidant composition (I), which comprises the following components in parts by weight: 1 part of N-acetylneuraminic acid, 0.5 part of tranexamic acid, 2.5 parts of a hop extract, 3 parts of a lotus embryo extract and 7 parts of deionized water. The components are mixed and dissolved uniformly at 45 ℃.

Example 2

The embodiment provides a whitening and spot-lightening antioxidant composition (II), which comprises the following components in parts by weight: 0.5 part of N-acetylneuraminic acid, 0.9 part of tranexamic acid, 1.6 parts of hop extract, 4 parts of lotus embryo extract and 7 parts of deionized water. The components are mixed and dissolved uniformly at 45 ℃.

Example 3

The embodiment provides a whitening and spot-lightening antioxidant composition (III), which comprises the following components in parts by weight: 2 parts of N-acetylneuraminic acid, 0.5 part of tranexamic acid, 3.5 parts of a hop extract, 1 part of a lotus embryo extract and 7 parts of deionized water. The components are mixed and dissolved uniformly at 45 ℃.

Example 4

This example provides a whitening spot-lightening antioxidant composition (iv) which differs from example 1 only in that the hop extract is prepared by the following method:

(1) mixing hops and 85% ethanol water solution with the mass of 10 times of the hops for 2 times of ethanol extraction, combining the extracting solutions, and concentrating under reduced pressure at 80 ℃ until no alcohol smell exists;

(2) extracting the concentrated solution obtained in the step (1) for 3 times by using petroleum ether, and collecting the extracted aqueous solution;

(3) passing the extracted aqueous solution obtained in the step (2) through a polyamide resin column, sequentially carrying out gradient elution by using 25%, 40% and 60% ethanol aqueous solutions, and collecting 60% eluent; concentrating the eluate under reduced pressure, and drying.

Example 5

This example provides a whitening spot-lightening antioxidant composition (v) which differs from example 1 only in that the hop extract is prepared by the following method:

(1) mixing hops and 70% ethanol water solution with the mass of 10 times of the hops for 2 times of ethanol extraction, combining the extracting solutions, and concentrating under reduced pressure at 80 ℃ until no alcohol smell exists;

(2) extracting the concentrated solution obtained in the step (1) for 3 times by using petroleum ether, and collecting the extracted aqueous solution;

(3) passing the extracted aqueous solution obtained in the step (2) through a polyamide resin column, sequentially carrying out gradient elution by using 25%, 40% and 60% ethanol aqueous solutions, and collecting 60% eluent; concentrating the eluate under reduced pressure, and drying.

Comparative example 1

This comparative example provides a composition (a) which differs from example 1 only in the absence of the N-acetylneuraminic acid component, the reduced fraction of which is added to the tranexamic acid, the hop extract and the lotus embryo extract in the ratio of the original fractions, all other conditions remaining unchanged.

Comparative example 2

This comparative example provides a composition (B) which differs from example 1 only in the absence of the tranexamic acid component, the reduced fraction of which is added to the N-acetylneuraminic acid, the hop extract and the lotus embryo extract in the ratio of the original fractions, all other conditions remaining unchanged.

Comparative example 3

This comparative example provides a composition (C) which differs from example 1 only in the absence of the hop extract component, the reduced fraction of which is added to the N-acetylneuraminic acid, tranexamic acid and lotus embryo extract in the ratio of the original fractions, all other conditions remaining unchanged.

Comparative example 4

This comparative example provides a composition (D) which differs from example 1 only in the absence of the lotus embryo extract fraction, the reduced fraction of which is added to the N-acetylneuraminic acid, tranexamic acid and hop extract in the ratio of the original fractions, all other conditions remaining unchanged.

Comparative example 5

The comparative example provides a composition (E) consisting of, in parts by weight: 7 parts of N-acetylneuraminic acid and 7 parts of deionized water. The components are mixed and dissolved uniformly at 45 ℃.

Comparative example 6

The comparative example provides a composition (F) consisting of, in parts by weight: 7 parts of tranexamic acid and 7 parts of deionized water. The components are mixed and dissolved uniformly at 45 ℃.

Comparative example 7

The present comparative example provides a composition (G) consisting of, in parts by weight: 7 parts of hop extract and 7 parts of deionized water. The components are mixed and dissolved uniformly at 45 ℃.

Comparative example 8

The comparative example provides a composition (H) consisting of, in parts by weight: 7 parts of lotus embryo extract and 7 parts of deionized water. The components are mixed and dissolved uniformly at 45 ℃.

Application example 1

The application example provides essence with whitening, spot-lightening and antioxidant effects, which comprises the following components in parts by weight: 14 parts of whitening and spot-lightening antioxidant composition (I), 5 parts of squalane, 3 parts of dipotassium glycyrrhizinate, 0.5 part of 1, 2-pentanediol, 0.8 part of cetyl esters, 0.3 part of caprylyl glycol and 76.4 parts of water. The components are mixed and dissolved uniformly at 45 ℃.

Application example 2

The application example provides essence with whitening, spot-lightening and antioxidant effects, which comprises the following components in parts by weight: 14 parts of whitening spot-lightening antioxidant composition (II), 5 parts of sodium hyaluronate, 3 parts of methyl propylene glycol, 0.5 part of 1, 2-pentanediol, 0.8 part of hydroxypropyl guar gum, 0.3 part of methylparaben and 76.4 parts of water. The components are mixed and dissolved uniformly at 45 ℃.

Application example 3

The application example provides essence with whitening, spot-lightening and antioxidant effects, which comprises the following components in parts by weight: 14 parts of whitening spot-fading antioxidant composition (III), 5 parts of chlorella extract, 3 parts of squalane, 0.5 part of methyl propylene glycol, 0.8 part of glyceryl tribehenate, 0.3 part of methyl hydroxybenzoate and 76.4 parts of water. The components are mixed and dissolved uniformly at 45 ℃.

Application examples 4 to 5

The application example provides two essences with whitening and spot-lightening antioxidant effects, and the essences are different from the application example 1 only in that the whitening and spot-lightening antioxidant composition (I) is equivalently replaced by a whitening and spot-lightening antioxidant composition (IV) and a whitening and spot-lightening antioxidant composition (V), and other conditions are kept unchanged.

Comparative application examples 1 to 8

The present application example provides eight kinds of essences, which are different from application example 1 only in that the whitening and spot-lightening antioxidant composition (i) is equally replaced with the whitening and spot-lightening antioxidant compositions (a to H), and other conditions are kept unchanged.

Application example 6

The application example provides essence with whitening, spot-lightening and antioxidant effects, and the essence is only different from the application example 1 in that 5 parts of squalane, 3 parts of dipotassium glycyrrhizinate and 0.5 part of 1, 2-pentanediol are replaced by 7.3 parts of dipotassium glycyrrhizinate and 1.2 parts of 1, 2-pentanediol, and other conditions are kept unchanged.

Application example 7

The application example provides essence with whitening, spot-lightening and antioxidant effects, and the essence is only different from the application example 1 in that 5 parts of squalane, 3 parts of dipotassium glycyrrhizinate and 0.5 part of 1, 2-pentanediol are replaced by 5.3 parts of squalane and 3.2 parts of dipotassium glycyrrhizinate, and other conditions are kept unchanged.

Application example 8

The application example provides essence with whitening, spot-lightening and antioxidant effects, and the essence is only different from the application example 1 in that 5 parts of squalane, 3 parts of dipotassium glycyrrhizinate and 0.5 part of 1, 2-pentanediol are replaced by 7.5 parts of squalane and 1 part of 1, 2-pentanediol, and other conditions are kept unchanged.

Test example 1

The essences prepared in application examples 1 to 8 and comparative application examples 1 to 8 were subjected to a safety test.

The specific method comprises the following steps: putting the tested object into a spot tester with the dosage of about 0.020-0.025g, sticking the spot tester with the tested object on the bent side of the forearm of the tested object by using a non-irritating adhesive tape, and lightly pressing with the palm to uniformly stick on the skin for 24 hours. And (5) removing the tested spot tester for 30min, and observing skin reaction after the indentation disappears. If the result is negative, the test is observed once more at 24h and 48h after the patch test.

Evaluation criteria: level 0: negative reaction; level 1: suspicious reactions, only faint erythema; and 2, stage: weak positive reaction, erythema, infiltration, edema, and possibly pimple; and 3, level: strong positive reaction, erythema, infiltration, edema, pimple and reaction beyond the tested area; 4, level: very strong positive reaction, obvious erythema, severe infiltration, edema, herpes fusiformis and reaction beyond the tested area.

The results show that the skin reactions of the subjects are negative, which indicates that the composition and the essence disclosed by the invention are uniform in temperature, safe and non-irritant.

Test example 2

Tyrosinase activity inhibition experiments were performed on the compositions prepared in examples 1-5 and comparative examples 1-8.

Test apparatus and reagents:

the main apparatus is as follows: spectrophotometer SpectronicGENESSYS-5, Thermo corporation, USA.

The main reagents are as follows: tyrosinase powder, enzyme activity 25000U, Sigma Co., USA; l-tyrosine, analytically pure, Shanghai JCBIO; ascorbic acid, analytically pure, Shanghai national drug.

Solution preparation: weighing 7.8g of sodium dihydrogen phosphate and 17.91g of disodium hydrogen phosphate, dissolving with distilled water to a constant volume of 500mL, and preparing 0.1mol/L phosphate buffer solution with pH of 6.8; accurately measuring 0.431mL of hydrochloric acid with the mass fraction of 36% -38%, and preparing 0.1mol/L hydrochloric acid by using distilled water to fix the volume to 50 mL; weighing 0.05g L-tyrosine, dissolving in 35mL of 0.1mol/L hydrochloric acid, and adding 65mL of PBS buffer solution with the pH value of 6.8 to obtain an L-tyrosine solution with the mass fraction of 0.05%; dissolving tyrosinase with enzyme activity of 25000U in 250mL of pure water to prepare a tyrosinase solution with enzyme activity of 100U/mL, subpackaging the tyrosinase solution in 1.5mL of EP tubes, and storing 1mL of each in a refrigerator at the temperature of-40 ℃; each sample and ascorbic acid were diluted with PBS buffer to 5% mass fraction concentration.

The specific method comprises the following steps: the sample adding system for each group of tests is shown in the following table, and the PBS buffer solution, the L-tyrosine solution and each sample solution are mixed and put into a constant-temperature water bath kettle at 37 ℃ for water bath for 10-15 min; adding tyrosinase into the reaction solution, shaking up, accurately timing, and stopping the reaction for 15 min; the plates were sequentially spotted on a 96-well plate, and the absorbance thereof was measured with a microplate reader and the inhibition rate was calculated.

Reagent	C1/mL	C2/mL	S1/mL	S2/mL
					PBS	4	5	2	3
Sample (I)	0	0	2	2
					L-tyrosine	2	2	2	2
Tyrosinase solution	1	0	1	0

The formula for tyrosinase inhibition is shown below:

tyrosinase inhibition rate ═ [ (A1-A2) - (A3-A4) ]/(A1-A2) × 100%

Wherein A1, A2, A3 and A4 are absorbance values of C1, C2, S1 and S2 respectively.

The test results are shown in table 1:

TABLE 1

Group of	Tyrosinase inhibition (%)
		Example 1	87.36％
Example 2	85.23％
		Example 3	86.47％
Example 4	91.15％
		Example 5	90.02％
Comparative example 1	81.26％
		Comparative example 2	75.46％
Comparative example 3	83.11％
		Comparative example 4	82.83％
Comparative example 5	70.36％
		Comparative example 6	76.79％
Comparative example 7	73.90％
		Comparative example 8	70.54％

From the data in table 1: the tyrosinase inhibition rates of examples 1-5 are overall higher than those of comparative examples 1-8, indicating that the tyrosinase inhibition effect is reduced when either component is absent or is a single component in the composition, wherein the tyrosinase inhibition effects of examples 4-5 are slightly better than those of examples 1-3.

Test example 3

The DPPH radical scavenging test was performed on the compositions prepared in examples 1-5 and comparative examples 1-8.

Experimental apparatus and reagents:

the main apparatus is as follows: spectrophotometer SpectronicGENESSYS-5, Thermo corporation, USA.

The main reagents are as follows: DPPH, analytically pure, tianjin majo; methanol, analytically pure, Tianjin Daoluo; ascorbic acid, analytically pure, Shanghai national drug.

Solution preparation: firstly, 1mg of DPPH is dissolved in about 20mL of methanol, ultrasonic treatment is carried out for 5min, and the mixture is fully shaken to ensure that the upper part and the lower part are uniform. Taking 1mL of the DPPH solution, and measuring the value of A at 519nm to ensure that the value of A is between 1.2 and 1.3; preparing each sample solution: the compositions of examples 1 to 5 and comparative examples 1 to 8 were diluted with methanol to prepare a composition having a mass fraction of 1%.

The specific method comprises the following steps: each set of sample adding system is shown in the following table, the reaction solution is shaken up and placed in a water bath at 37 ℃ for heating for 15min, and then taken out, and an ultraviolet-visible spectrophotometer is used for measuring the absorbance value of the solution.

Reagent	C1/mL	C2/mL	C3/mL
				DPPH solution	2	2	0
Sample solution	0	2	2
				Anhydrous methanol	2	0	2

The formula for calculation of DPPH free radical scavenging rate is shown as follows:

DPPH free radical clearance rate 1- (A2-A3)/A1 × 100%

In the formula, A1, A2 and A3 are absorbance values of C1, C2 and C3 respectively.

The test results are shown in table 2:

TABLE 2

As can be seen from the data in Table 2: the overall DPPH radical scavenging efficiency of examples 1-5 is higher than that of comparative examples 1-8, indicating that the DPPH radical scavenging effect is reduced when either component is absent or is present alone in the composition, with examples 4-5 having slightly better DPPH radical scavenging effects than examples 1-3.

Test example 4

The whitening effect test was performed on the essences prepared in application examples 1 to 8 and comparative application examples 1 to 8.

The specific method comprises the following steps: after 10 volunteers (5 males and 5 females) aged 20-50 and half of the male and female were selected for each test object, a multifunctional skin tester (model: MPA580) manufactured by Courage Khazaka, Germany was used. The skin whitening effect of the test subjects was evaluated by testing the ITA values (averaged) of each group of volunteers at week 0 and week 4, 2 times per day for 4 weeks, using the essences prepared in application examples 1 to 8 and comparative application examples 1 to 8, respectively, and the ITA test values (averaged) are shown in table 3:

TABLE 3

Group of	0 week	4 weeks
			Application example 1	39	66
Application example 2	42	65
			Application example 3	46	59
Application example 4	44	70
			Application example 5	40	63
Application example 6	41	67
			Application example 7	44	68
Application example 8	40	66
			Comparative application example 1	39	59
Comparative application example 2	42	52
			Comparative application example 3	43	60
Comparative application example 4	41	56
			Comparative application example 5	40	49
Comparative application example 6	41	51
			Comparative application example 7	40	46
Comparative application example 8	42	49

As can be seen from the data in Table 3: the whitening effects of application examples 1 to 8 were overall higher than those of comparative application examples 1 to 8, indicating that the whitening effect was somewhat reduced when either component was absent or only a single component was present in the composition, wherein the whitening effects of examples 4 to 5 were slightly superior to those of examples 1 to 3.

Test example 5

The moisturizing effect test was performed on the essences prepared in application examples 1 to 8.

The specific method comprises the following steps: after using 10 volunteers (5 males and 5 females) with the ages of 20-50 years and half of males and females under the environment of 24-26 ℃ and 50% relative humidity, the test subjects need to uniformly wash the inner sides of forearms of both hands with clear water before the test. After washing, test areas were marked on the forearms of the left and right hands of the subject at intervals of 1cm, and each test area was 5X 5cm ² . The essence liquids prepared in application examples 1-8 were respectively applied, and the test sample amount was 0.2 g. After the subject was rested in a constant environment for 30 minutes, the moisture content of the test site was measured and measured using a CorneometerThe water content increase rate (average value) is shown in Table 4.

TABLE 4

Group of	Moisture content increase rate (%)
		Application example 1	33.63％
Application example 2	32.45％
		Application example 3	29.74％
Application example 4	35.97％
		Application example 5	33.50％
Application example 6	31.26％
		Application example 7	28.64％
Application example 8	29.13％

From the data in table 4, it can be seen that: the essence disclosed by the invention has a superior moisturizing effect, and has a better moisturizing effect when the moisturizing agent component is a combination of squalane, dipotassium glycyrrhizinate and 1, 2-pentanediol.

Test example 6

Skin improvement satisfaction scores were made for the essences prepared in application examples 1-8 and comparative application examples 1-8.

The specific method comprises the following steps: 160 volunteers, 25-45 years old and female, were selected and divided into 16 groups. The essences prepared in application examples 1-8 and comparative application examples 1-8 were applied to facial skin 2 times a day for 12 weeks, and the skin care product was evaluated and scored according to the condition of improvement of the skin itself. The scoring criteria are shown in the following table:

scoring	Definition of evaluation
		1≤X＜3	General effect of improving the degree of skin
3≤X＜4	The skin becomes tender and smooth and has better whitening and spot-lightening effects
		4≤X≤5	The skin is obviously fine, smooth, white and has very obvious spot-lightening effect

The scoring results (mean) are shown in table 5:

TABLE 5

From the data in table 5, it can be seen that: the combination and the essence provided by the invention have good whitening and spot-fading effects, the scores of the application examples 1-8 are integrally higher than those of the comparative application examples 1-8, which shows that the whitening and spot-fading effects are reduced when any component is absent or only a single component is contained in the composition, wherein the whitening and spot-fading effects of the application examples 4-5 are slightly better than those of the comparative application examples 1-3.

The applicant states that the present invention is illustrated by the above examples to provide a whitening and spot-lightening antioxidant composition and its application, but the present invention is not limited to the above examples, i.e. it is not meant to be dependent on the above examples to practice the present invention. It should be understood by those skilled in the art that any modification of the present invention, equivalent substitutions of the raw materials of the product of the present invention, addition of auxiliary components, selection of specific modes, etc., are within the scope and disclosure of the present invention.

The preferred embodiments of the present invention have been described in detail, however, the present invention is not limited to the specific details of the above embodiments, and various simple modifications may be made to the technical solution of the present invention within the technical idea of the present invention, and these simple modifications are within the protective scope of the present invention.

It should be noted that the various technical features described in the above embodiments can be combined in any suitable manner without contradiction, and the invention is not described in any way for the possible combinations in order to avoid unnecessary repetition.

Claims (10)

1. A whitening and spot-lightening antioxidant composition is characterized by comprising the following components in parts by weight: n-acetylneuraminic acid, tranexamic acid, hops extract and lotus embryo extract.

2. The whitening spot-lightening antioxidant composition of claim 1, wherein the whitening spot-lightening antioxidant composition comprises, in parts by weight: 0.01-2 parts of N-acetylneuraminic acid, 0.05-2 parts of tranexamic acid, 0.1-4 parts of hop extract and 1-7 parts of lotus embryo extract.

3. The whitening, spot-lightening and antioxidant composition according to claim 1 or 2, wherein the hop extract is prepared by a preparation method comprising the steps of:

(1) mixing hops and an ethanol water solution for ethanol extraction, and concentrating an extracting solution until no alcohol smell exists;

(2) extracting the concentrated solution obtained in the step (1) by using an organic solvent;

(3) and (3) purifying and drying the extracted aqueous solution obtained in the step (2) to obtain the compound.

4. The whitening, spot-lightening and antioxidant composition of claim 3, wherein the concentration of the ethanol aqueous solution in step (1) is 80-95%;

preferably, the mass ratio of the ethanol aqueous solution to the hop in the step (1) is 8-15 times;

preferably, the organic solvent in step (2) comprises any one or a combination of at least two of petroleum ether, pentane, hexane or heptane;

preferably, the purification in step (3) is performed by passing through a polyamide resin column and eluting with an ethanol aqueous solution;

preferably, the elution is a gradient elution from low concentration to high concentration with 25-60% ethanol aqueous solution.

5. Use of the whitening and spot-lightening antioxidant composition according to any one of claims 1 to 4 in the preparation of cosmetics.

6. The use of claim 5, wherein the cosmetic comprises a serum, a serum oil, a lotion, a cream, a mask, an eye cream, a facial cleanser.

7. The essence with whitening, spot-lightening and antioxidant effects is characterized by comprising the following components in parts by weight: the whitening spot-lightening antioxidant composition of any one of claims 1 to 4, a humectant, a thickener, an antibacterial preservative and water.

8. The essence with whitening, spot-lightening and antioxidant effects as claimed in claim 7, wherein the essence comprises the following components in parts by weight: 1-15 parts of whitening, spot-lightening and antioxidant composition as defined in any one of claims 1-4, 0.1-10 parts of humectant, 0.1-5 parts of thickener, 0.01-1 part of antibacterial preservative and water.

9. The essence with whitening, spot-lightening and antioxidant effects according to claim 7 or 8, wherein the moisturizer comprises any one or a combination of at least two of jojoba esters, sodium hyaluronate, methyl propylene glycol, chlorella vulgaris extract, dipotassium glycyrrhizinate, squalane, betaine or 1, 2-pentanediol; a combination of squalane, dipotassium glycyrrhizinate and 1, 2-pentanediol is preferred.

10. The essence with whitening, spot-lightening and antioxidant effects according to claim 7 or 8, wherein the thickener comprises any one or a combination of at least two of hydroxypropyl guar gum, cetyl esters, glyceryl tribehenate, cellulose gum or carboxymethyl hydroxyethyl cellulose;

preferably, the antimicrobial preservative comprises any one or a combination of at least two of methylparaben, 1, 2-hexanediol, caprylyl glycol, caprylyl hydroxamic acid, or 1, 2-pentanediol.