CN114794469A

CN114794469A - Compositions for inhibiting melanin and uses and methods thereof

Info

Publication number: CN114794469A
Application number: CN202210519924.7A
Authority: CN
Inventors: 田茜; 贾兰星; 冯妹元; 周希瑞; 杨晨光; 刘锋
Original assignee: Quaker Oats Co
Current assignee: Quaker Oats Co
Priority date: 2022-05-12
Filing date: 2022-05-12
Publication date: 2022-07-29

Abstract

The present invention provides a composition for inhibiting tyrosinase comprising grain in an amount of about 50 wt.% to about 95 wt.% and coconut flour in an amount of about 4.5 wt.% to about 50 wt.%, based on the total weight of the composition, and uses and methods thereof. The invention also provides a composition for inhibiting tyrosinase, which comprises oat, coconut powder, white kidney bean, coix seed powder, yam powder, tuckahoe rice flakes, nicotinamide and zinc. The invention also provides application of the composition in preparing a functional preparation for inhibiting tyrosinase production and a method for inhibiting tyrosinase production for non-treatment purposes. The composition disclosed by the invention can realize a higher tyrosinase inhibition rate, so that the generation of melanin is inhibited, and the composition has a good whitening effect.

Description

Compositions for inhibiting melanin and uses and methods thereof

Technical Field

The present invention relates to compositions for inhibiting tyrosinase, in particular for inhibiting melanin production by inhibiting tyrosinase activity, and uses and methods thereof.

Background

With the increase of age, adverse skin symptoms such as pigmentation, dark yellow skin color and the like are increased, and the improvement of the skin color becomes a problem that oriental women pay more and more attention in the process of pursuing beauty. The skin color is affected by abnormal melanin metabolism, impaired skin barrier, blood circulation stasis, oxygen free radical accumulation, and inflammation. In particular, melanin produced by melanocytes existing between epidermis and dermis is excessive due to the influence of ultraviolet rays or hormones, or melanin removal is inhibited by inflammation or the like, which causes pigment deposition such as speckle, freckle or the like on the skin.

In the prior art, the acidic components such as kojic acid, azelaic acid, vitamin C, linoleic acid and the like are main effective substances for inhibiting melanin formation, but have the characteristics of poor solubility, poor compatibility, instability and the like. The natural plant extracts, such as chamomile extract, liquorice extract, and hedyotis diffusa extract, have the advantages of small irritation, high safety, good curative effect and the like, but are mostly limited in cosmetics, and are easily influenced by factors such as high production cost, small dosage, low skin barrier permeation and absorption utilization rate and the like.

As the traditional diet of Chinese people, the grain is one of the indispensable foods on the dining table of common people for thousands of years, plays an important role in the diet of China and is taken as the traditional staple food. With the pursuit of health and dietary diversification of consumers in modern society, cereals are made into various foods having both health and deliciousness, such as cereal flakes, oatmeal, yogurt containing cereals, beverages, biscuits and the like. The grains are rich in carbohydrate, protein, vitamins and minerals, and have high nutritive value. However, no technique for inhibiting melanin formation has been reported for cereals.

Disclosure of Invention

The invention provides a composition for inhibiting tyrosinase, and applications and methods thereof.

In one aspect, the present invention provides a composition for inhibiting tyrosinase comprising grain in an amount of about 50 wt.% to about 95 wt.% and coconut flour in an amount of about 4.5 wt.% to about 50 wt.%, based on the total weight of the composition.

In some of these embodiments, the composition comprises oat and coconut flour. In some embodiments, the composition further comprises at least one of navy bean, coix seed, yam, poria, niacinamide, and zinc.

In another aspect, the present invention provides a composition for inhibiting tyrosinase comprising oat, coconut flour, navy bean, coix seed flour, yam flour, poria cocos rice flakes, niacinamide, and zinc.

In yet another aspect, the present invention also provides the use of the above composition for the preparation of a functional preparation for inhibiting tyrosinase production.

In yet another aspect, the present invention also provides a method for non-therapeutic purposes of inhibiting tyrosinase production, the method comprising: providing an effective amount of the above composition to a subject in need thereof.

Other features and aspects of the present invention are set forth in more detail below.

Detailed Description

The present invention will be described in further detail below so that those skilled in the art to which the present invention pertains can easily put the present invention into practice. It should be understood, however, that the present invention may be embodied in various forms and is not limited to the specific embodiments described herein, and that the embodiments of the present invention are merely exemplary.

The term "about" or "approximately" as applied to numerical values as described herein encompasses precise values and reasonable variances.

Unless otherwise specified, the terms "include" and "comprise," as well as grammatical variants thereof, are intended to mean "open" or "inclusive" language such that it includes the recited elements but also allows for inclusion of additional, unrecited elements.

All percentages in this specification refer to weight percentages unless otherwise indicated. The expressions "% by weight of …" "% by weight", "% by weight" and "wt.%" are synonyms that refer to the amounts expressed as percentages on a dry weight basis.

The term "effective amount" is a predetermined amount calculated to achieve the desired effect, i.e., to prevent, counter, alleviate, ameliorate, prevent, inhibit, block, or reverse an undesired condition in a patient.

Unless otherwise defined, all terms have, and should be given, the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs.

Tyrosinase, also known as polyphenol oxidase, is an about 75kD copper-containing oxidoreductase, widely exists in animals, plants, microorganisms and human bodies, is a rate-limiting enzyme for melanin synthesis, and directly influences the synthesis of melanin. The tyrosinase is composed of a plurality of subunits, each subunit contains 2 metallic copper ions, the 2 copper ions are respectively and covalently bonded with imino groups of 3 histidine residues and fixed on an active center, and in addition, 1 endogenous bridge group links the 2 copper ions together to form the active center of the tyrosinase. If the copper is oxidized, the enzyme is inactivated and can be reactivated by means of an electron donor, such as L-3,4 dihydroxyphenylalanine, ascorbic acid, superoxide anion, and possibly nitric oxide. The tyrosinase gene family has 3 kinds of genes in total, namely TYR, TYRP1 and TYRP2, wherein TYRP1 and TYRP2 play a catalytic role in controlling the final steps of melanin type production by melanocytes, TYR is a key rate-limiting enzyme in the initial process of melanin synthesis, and has at least two activities of tyrosine hydroxylase and dopa oxidase, and oxidation and transport of tyrosine are involved in the process of melanin synthesis. Under the catalytic action of tyrosinase, L-tyrosine is hydroxylated into dopa, dopa is oxidized into dopaquinone, and dopaquinone forms the final reaction product melanin. The expression and activity of tyrosinase determines the rate and yield of melanin production, and the higher the tyrosinase activity, the greater the amount of melanin formation in the skin.

Melanin generally plays an important role in protecting the human body from the radiation of ultraviolet rays, and thus, the ultraviolet rays can activate the activity of tyrosinase, and after tyrosine or 3, 4-dihydroxyphenylalanine is oxidized, melanin is formed through the above-mentioned series of chemical reactions. Melanin is continuously produced and deposited and forms uniform melanin particles, thereby making the skin appear darker color, and excessive local production may cause chloasma and freckles. Therefore, the production of melanin can be inhibited by inhibiting the activity of tyrosinase, thereby preventing skin pigmentation.

The reagent with tyrosinase activity inhibition effect can slow down the catalytic conversion of L-tyrosine into dopaquinone by tyrosinase, so that the inhibition effect of a test object on the tyrosinase activity can be evaluated by measuring the absorbance of the dopaquinone at 475nm according to the change of the absorbance, thereby evaluating the inhibition effect on the melanin generation.

The invention relates to a composition for inhibiting tyrosinase, which comprises raw materials such as grains and coconut powder. By selectively controlling various aspects of the composition, the inventor finds that the obtained composition can realize higher tyrosinase inhibition rate, thereby inhibiting the generation of melanin and having good whitening effect. The inventors have also found that the combined use of grain and coconut flours provides a higher tyrosinase inhibition than the use of the same amount of grain and coconut flours alone, indicating a synergistic effect of the combined use of grain and coconut flours.

As used herein, the term "grain" refers to a monocotyledonous or dicotyledonous plant grown for its edible seed, including plants selected from the group consisting of rice (Oryza), wheat (Triticum) belonging to the family Poaceae (Poaceae), and combinations thereof. The grains suitable for use in the present invention may be selected from, for example, glutinous rice, brown rice, black rice, purple rice, oat, buckwheat, barley, whole wheat, sorghum rice, millet, or the like. In some embodiments, the grain is selected from at least one of oat, brown rice, and rice. In other embodiments, the cereal comprises oat and brown rice. In still other embodiments, the cereal comprises oats and rice. In some embodiments, the cereal is oat.

The form of the grain is not particularly limited and may be adjusted as desired, and includes, but is not limited to, powder, granules, flakes, suspension, cakes, and the like. In some embodiments, when the composition is a food composition, the grain may be a powder, granules, flakes, chunks, or the like.

"oats" refers to annual herbaceous plants of the genus Avena (Avena L.) of the family Gramineae, and is generally classified into the palea type (oats husked) and the grain type (oats naked). Oat is rich in various nutritional ingredients such as protein, fat, carbohydrate, vitamins and trace elements, and compared with crops such as wheat, rice, corn, barley and sorghum, the five index contents of protein, fat, mineral elements, cellulose and vitamins in grains of oat are in the top position. In addition, the amino acid composition of the oat flour protein is relatively balanced, wherein the content of lysine is 1.5-3.0 times higher than that of grain crops such as wheat. The oat also contains natural antioxidants such as polyphenol, enrichin, tocopherol and carotenoid, has excellent effects of resisting oxidation and eliminating free radicals in vivo, and the colloidal extract can remarkably increase skin moisture and improve dry and rough skin.

For convenience of description, the present invention uses the term "coconut flour", but is not intended to be limited to the powder form, but may be coconut milk, coconut juice, coconut milk powder, etc. In the present invention, the coconut powder may be derived from coconut meat, coconut extract, coconut milk, and the like. Coconut meat contains abundant vitamins, minerals, free amino acids, enzymes and growth promoting factors, wherein L-arginine and polyphenol compounds have strong scavenging capacity on superoxide anion free radicals, DPPH free radicals and hydroxyl free radicals. The coconut extract can promote the expression of skin keratinocyte components to increase the protective barrier effect of stratum corneum after medium-wave ultraviolet irradiation. In addition, coconut flour has a natural sweet taste and can be added to food compositions as a sweetener. In some embodiments of the invention, the composition is free of sweeteners other than coconut flour.

Specifically, in the composition, the cereal is present in an amount of about 50 wt.% to about 95 wt.% and the coconut flour is present in an amount of about 4.5 wt.% to about 50 wt.%, based on the total weight of the composition. In some embodiments, the cereal is present in the composition in an amount of about 60 wt.% to about 95 wt.% and the coconut flour is present in an amount of about 4.5 wt.% to about 15 wt.%, based on the total weight of the composition. In some embodiments, the cereal is present in the composition in an amount of about 65 wt.% to about 90 wt.% and the coconut flour is present in an amount of about 6 wt.% to about 13 wt.%, based on the total weight of the composition. In some embodiments, the cereal is present in the composition in an amount of about 65 wt.% to about 85 wt.% and the coconut flour is present in an amount of about 7 wt.% to about 12 wt.%, based on the total weight of the composition. In some embodiments, the cereal is present in the composition in an amount of about 70 wt.% to about 80 wt.% and the coconut flour is present in an amount of about 8 wt.% to about 10 wt.%, based on the total weight of the composition. In some embodiments, the cereal is present in the composition in an amount of about 75 wt.% to about 80 wt.% and the coconut flour is present in an amount of about 9 wt.% to about 10 wt.%, based on the total weight of the composition.

In order to enhance the efficacy of the composition, the composition can also comprise suitable medicinal and edible raw materials. As used herein, the term "raw materials having homology of medicine and food" refers to raw materials that are included in "the material catalog management regulation according to the tradition of both foods and traditional Chinese medicinal materials" published by the national standard for safety of health and welfare food and testing evaluation in 2021, have both nutritive value and medicinal value, and are widely researched and applied in the fields of general foods, medicines and functional foods. In some embodiments, the medicinal and edible raw materials may include, but are not limited to, at least one of white kidney bean, red bean, tremella, coix seed, yam, poria, lotus seed, lily, and pueraria root. In other embodiments, the medicinal and edible raw materials may include at least one of white kidney bean, white fungus, coix seed, Chinese yam and poria cocos. In other embodiments, the medicinal and edible raw materials may include at least one of tremella, coix seed, yam, and poria. In other embodiments, the medicinal and edible material may comprise at least one of navy bean, coix seed, yam, and poria. In other embodiments, the medicinal and edible raw materials may include at least one of tremella, coix seed, lotus seed, and poria.

In order to exert the effects of the medicinal and edible raw materials per se without affecting the overall texture or mouthfeel of the composition, the content of the medicinal and edible raw materials is preferably about 2 wt.% to about 25 wt.%, based on the total weight of the composition. In some embodiments, the amount of the edible and pharmaceutical raw material is from about 8 wt.% to about 15 wt.%. In other embodiments, the amount of the edible and pharmaceutical raw material is from about 10 wt.% to about 12 wt.%.

These medicated homologous materials will be described in detail below.

White kidney bean (Phaseolus lunatus Billb. ex Bean.) belongs to subfamily of Papilionaceae of Leguminosae and Phaseolus vulgaris, is a bean crop widely planted in the world, and has 18-21% of protein, 40-60% of starch and 1.6-2.15% of fat in kidney bean seeds, so that the white kidney bean is rich in nutrition and has medicinal value. The white kidney bean contains amylase inhibitor, can inhibit the activity of amylase in saliva and prevent the hydrolysis and digestion of carbohydrate in food, and is widely applied to health-care food for losing weight, controlling blood sugar and the like. In the examples of the present invention, the form of white kidney beans is not particularly limited, and may be powder, flakes, slurry, or the like.

Semen Phaseoli (Abrus precatorius L.) is seed of red bean of Leguminosae, also called semen Phaseoli and semen Phaseoli. The red bean contains rich nutrient elements such as protein, carbohydrate, fat, dietary fiber, various vitamins, carotene, inorganic salt and the like, and has the effects of relaxing bowels, promoting urination, promoting normal development of bones and teeth, nourishing five internal organs, maintaining beauty and keeping young and the like. In the embodiment of the present invention, the form of red beans is not particularly limited, and may be powder, flake, slurry, or the like.

Tremella fuciformis Berk is a fruiting body of basidiomycota fungus Tremella, consists of more than 10 thin and multi-fold flat leaves, is also called Tremella fuciformis, Tremella fuciformis and the like, has the name of 'crown in fungus', is a famous and precious nutritional nourishing product, and is a tonic for strengthening body resistance. Mild in nature, sweet and light in taste, and non-toxic. Has effects in moistening lung, promoting salivation, nourishing yin, invigorating stomach, invigorating qi, tranquilizing mind, tonifying heart, and strengthening brain. Tremella contains abundant proteins, vitamins, etc., so the Tremella powder has effects of resisting aging, removing wrinkle and firming skin, and can be used for removing freckle, chloasma, etc. when being applied. In the embodiment of the present invention, the form of tremella is not particularly limited, and may be powder, flake, slurry, etc. In some embodiments, when used as a food composition, tremella improves the texture of the composition, making it rich in a smooth mouthfeel.

Coix lacryma-jobi L is dried mature kernel of a plant belonging to genus Coix of family Gramineae. Sweet and light taste, cool in nature, and has the effects of promoting diuresis, invigorating spleen, relieving diarrhea, eliminating arthralgia, expelling pus, removing toxic substance, and resolving hard mass. The Coicis semen contains Coix seed oil, Coix seed ester, amino acids, fatty oil, etc. Coix seed oil and coixol have muscle contraction inhibiting effect, and coixol also has tranquilizing, antipyretic, cooling and analgesic effects on central nervous system. The extract of Coicis semen can enhance humoral immunity, enhance NK cell activity or cytotoxicity, and has antiviral and anticancer effects. In addition, experiments prove that the medicine has the effect of inducing ovulation and can reduce blood sugar. A heat stable protease inhibitor was also found from the soft-shelled coixseed bran. In the embodiment of the present invention, the form of the coix seed is not particularly limited, and may be powder, tablet, slurry, etc.

Rhizoma Dioscoreae (Dioscorea opposita) is dried rhizome of Dioscorea opposita of Dioscoreaceae. Can be used for treating epidemic febrile disease, fever, bloody dysentery, carbuncle, ulcer, toxic swelling, lymphoid tuberculosis, and anal fistula. Contains nutrients related to mucus and amylase, and has tonic and digestion promoting effects. In the examples of the present invention, the form of yam is not particularly limited, and may be powder, tablet, slurry, or the like.

Poria cocos (Wolfipora cocos (Schw.) Ryv. & Gibn) is a fungus plant parasitic on pine roots, shaped like a sweet potato, dark brown in the outer skin, white or pink in the inner side. Poria has sweet and light taste and mild nature, and has effects of promoting diuresis, eliminating dampness, invigorating spleen, regulating stomach function, calming heart, tranquilizing mind, and whitening skin. Modern medical research shows that tuckahoe can enhance the immune function of organisms, and pachyman has obvious anti-tumor and liver-protecting effects. In the embodiment of the present invention, the form of poria cocos is not particularly limited, and may be powder, tablet, slurry, or the like. In some embodiments, when used as a food composition, the poria may be mixed with brown rice or rice to make poria rice flakes to enhance the crispy mouthfeel of the composition.

Semen Nelumbinis (Semen Nelumbini) is dry mature seed of Nymphaeaceae aquatic herbaceous plant flos Nelumbinis, also called Semen Nelumbinis, and Semen Nelumbinis. The lotus seed is rich in nutrition, and contains beta-sitosterol, alkaloid, rich mineral substances such as calcium, phosphorus, iron and the like and vitamins besides a large amount of starch. Modern pharmacological research also proves that the lotus seeds have various effects of calming, strengthening heart, resisting aging and the like. In the embodiment of the present invention, the form of the lotus seed is not particularly limited, and may be powder, flake, slurry, or the like.

Lily (Lilium brownii var. virididuum) is fleshy scaly leaf of Lilium brownii (Lilium lancifolium Thunb.) plant, lily (Lilium brownii f.e. brown var. virididum Baker) or Lilium microphyllum DC (Lilium pullium DC.) and has the effects of nourishing yin, moistening lung, clearing heart and tranquilizing mind. It is often used to treat dry cough due to yin deficiency, cough with blood, vexation, pavor, insomnia, dreaminess, absentmindedness. In the examples of the present invention, the form of lily is not particularly limited, and may be powder, tablet, slurry, or the like.

Radix Puerariae (Radix Puerariae) is a Leguminosae plant Pueraria lobata, has cool nature, mild smell and sweet taste, and has effects of clearing heat, lowering fire, removing toxic substance, etc. Further analysis by modern medical methods shows that the root of kudzu vine is rich in up to 13 isoflavones, including puerarin, miroestrol, puerarin xyloside, daidzein, etc., and puerarin has therapeutic effects on hypertension, hyperlipidemia, hyperglycemia and cardiovascular and cerebrovascular diseases. Puerarin can lower blood sugar and obviously lower serum cholesterol. In the embodiment of the present invention, the form of pueraria lobata is not particularly limited, and may be powder, tablet, slurry, etc.

To further enhance the nutritional efficacy of the composition, the composition may further comprise at least one suitable nutritional enhancer. In some embodiments, the nutritional fortifier may be present in an amount of about 0.01 wt.% to about 1.5 wt.%, based on the total weight of the composition. In other embodiments, the nutritional supplement may be present in an amount of about 0.05 wt.% to about 1 wt.%, based on the total weight of the composition. In some embodiments, the at least one nutritional enhancer may be selected from at least one of dairy products, niacinamide, vitamins, and trace elements.

The dairy product may be, for example, cow's milk, goat's milk, yogurt, cheese, or the like. In some particular embodiments, the dairy product is milk. The form of the dairy product is not particularly limited, and may be a powder, a cake, a liquid, a semisolid form, or the like.

Nicotinamide is a derivative of vitamin B3, is widely used for treating pellagra, light dermatitis and cosmetic dermatitis in clinic, can improve skin quality by inhibiting melanin from transferring to keratinocytes and accelerating skin cell metabolism, and can be used in cosmetics, foods and pharmaceuticals. When the composition of the invention is a food composition, the nicotinamide is a food grade nicotinamide.

The trace elements include trace elements necessary for human body, such as iron, copper, zinc, calcium, magnesium, sodium, cobalt, manganese, chromium, selenium, iodine, nickel, fluorine, molybdenum, vanadium, tin, silicon, strontium, boron, rubidium, arsenic, etc. In some embodiments, the trace elements are selected from at least one of zinc, iron, calcium, magnesium, sodium. In some particular embodiments, the trace element is zinc. Zinc is an important trace element necessary for human body, and is helpful for growth and development, intelligence development, immunity improvement, and normal appetite maintenance.

Vitamins include, for example, but are not limited to, at least one of vitamin a, vitamin B, vitamin C, vitamin D, vitamin E. In some embodiments, the vitamin may be selected from at least one of vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B12, vitamin B9, and vitamin B7. In some embodiments, the vitamin is vitamin B2. Vitamin B2, also called riboflavin, is a water-soluble vitamin which is easy to digest and absorb and has the effects of curing canker sores and maintaining mucous membrane health.

In some of these embodiments, exemplary formulations of the compositions of the present invention are shown in table 1 below.

TABLE 1 exemplary formulations of the compositions of the present invention

In some embodiments of the above formulation, the oat, coix seed, yam, poria, lotus seed, etc. may be in powder form for ease of mixing and absorption.

The composition of the invention can be used alone as a functional preparation, for example as a nutritional supplement or dietary fibre supplement or the like. In addition, the composition can be ingested as a food product, such as a cereal porridge, cereal flakes, beverage, yogurt, and the like. In particular embodiments, the composition may be a mixed instant oatmeal that may satisfy the health, beauty and convenience needs of modern fast-paced urban women.

The invention also relates to a composition for inhibiting tyrosinase, which comprises oat, coconut powder, white kidney bean, coix seed powder, yam powder, tuckahoe rice flakes, nicotinamide and zinc. By selectively controlling the content of each component of the composition, the inventor finds that the obtained composition can realize higher tyrosinase inhibition rate, thereby inhibiting the generation of melanin and having good whitening effect. The inventors have also found that the tyrosinase inhibition rate of the combination of oat and coconut flour is higher than that of the same amount of oat and coconut flour alone, indicating that the combination of grain and coconut flour has a synergistic effect.

In some embodiments, the composition consists of, based on the total weight of the composition: oat: about 50 wt.% to about 95 wt.%, coconut flour: about 4.5 wt.% to about 50 wt.%, white kidney bean: about 6 wt.% to about 15 wt.%, coix seed powder: about 0.7 wt.% to about 10 wt.%, yam flour: about 1 wt.% to about 10 wt.%, poria cocos rice flakes: about 6 wt.% to about 25 wt.%, zinc nicotinamide: about 0.01 wt.% to about 0.5 wt.%. In other embodiments, the composition consists of, based on the total weight of the composition: oat: about 62 wt.% to about 75 wt.%, coconut flour: about 4.5 wt.% to about 15 wt.%, white kidney bean: about 6 wt.% to about 15 wt.%, coix seed powder: about 0.7 wt.% to about 2.1 wt.%, yam flour: about 1 wt.% to about 2 wt.%, poria cocos rice flakes: about 11 wt.% to about 18.4 wt.%, zinc nicotinamide: about 0.01 wt.% to about 0.5 wt.%. In a particular embodiment, the composition consists of, based on the total weight of the composition: oat: about 70.15 wt.%, coconut flour: about 9.3 wt.%, white kidney bean: about 6 wt.%, coix seed powder: about 2 wt.%, yam flour: about 1.5 wt.%, poria cocos rice flakes: about 11 wt.%, zinc nicotinamide: about 0.05 wt.%.

The composition of the present invention may be a food composition or a functional preparation. In some embodiments, the composition is free of sweeteners other than coconut flour. When used as a food composition, the coconut powder has light fragrance and natural sweet taste due to its natural coconut powder, and is free of sweeteners such as sucrose and honey, low in calorie, and healthy and delicious. The composition has the efficacy of eliminating dampness and nourishing, has beautiful vision and is more popular with consumers because of containing white medicinal and edible raw materials such as white kidney beans, coix seed powder, yam powder, tuckahoe rice flakes and the like.

The invention also relates to application of the composition in preparing a functional preparation for inhibiting tyrosinase production. The functional agent may be, for example, a cosmetic agent, a food agent, a pharmaceutical agent, or the like. Since melanin is generally generated by the action of tyrosinase on tyrosine, the generation of melanin can be inhibited by inhibiting the generation of tyrosinase, thereby achieving the effect of whitening skin. Therefore, the composition can be used for preparing a functional preparation for inhibiting melanin generation.

The present invention also relates to a method for non-therapeutic purposes of inhibiting tyrosinase production, the method comprising: providing an effective amount of the above composition to a subject in need thereof. Means provided include, but are not limited to, oral administration, topical administration, and the like. In some embodiments, the method of non-therapeutic interest comprises orally administering to a subject in need thereof an effective amount of the above composition to inhibit melanin production.

Hereinafter, the composition of the present invention will be described in detail with reference to specific examples, but the present invention is not limited thereto. Unless otherwise indicated, the raw materials and chemicals in the following examples are food grade and are from commercially available products.

Examples

Example 1: taste and mouthfeel evaluation of Mixed oatmeal

The formulation of the mixed oatmeal of this example is shown in table 2 below.

TABLE 2 formulation of Mixed oatmeal of example 1

Components	Weight (g)	Percent (wt.%)
			Oatmeal	24.55	70.15
Coconut powder	3.26	9.30
			Poria cocos rice tablet	3.85	11.00
White kidney bean	2.10	6.00
			Coix seed powder	0.70	2.00
Yam powder	0.53	1.50
			Nicotinamide zinc	0.02	0.05
Total of	35.00	100.00

The mixed oatmeal of this example was brewed with hot water at 90 ℃ or higher for about 3 to about 5 minutes, and then consumed and evaluated for sweetness and mouthfeel by 20 tasters. The evaluation results are summarized in table 3 below.

TABLE 3 taste test results for the blended oatmeal of example 1

	Is very satisfactory	Satisfaction	In general terms	Is unsatisfactory
					Sweetness level	17	2	1	0
Taste of the product	16	3	1	0

As can be seen from the above table, most of the members evaluated the sweetness and mouthfeel of the mixed oatmeal of this example better. The mixed oatmeal is easy to be brewed, has smooth taste, has the faint scent of coconut and natural sweetness.

Example 2: tyrosinase activity inhibition assay (in vitro method)

The mixed oatmeal of example 1 and the combination of oatmeal, coconut flour, zinc nicotinate, and oat coconut flour therein were each tested for tyrosinase activity inhibition.

The reagents used in this example were as follows: distilled water; phosphate Buffered Saline (PBS): pH 6.8, 0.1 mol/L; l-tyrosine: analytically pure, T3754, purity > 98%, supplied by Sigma company; tyrosinase, and (c) an enzyme: t3824, 1000 units/mg, supplied by Sigma Inc.; kojic acid: s30151, available from Shanghai-derived leaf Biotechnology, Inc.

1. Experimental methods

The ingredients and percentages of the blended oatmeal are as set forth in the formula of table 2, and the oat and coconut flours in the oat coconut flour combination are also in accordance with the mutual mass ratios in table 2, being about 88.3 wt.% and about 11.7 wt.%, respectively. Respectively grinding oatmeal, coconut powder, oat coconut powder, and mixed oatmeal with nanometer grinder. Weighing oatmeal, coconut powder, oat and coconut powder combination, 70.71mg of mixed oatmeal grinding powder, 9.3mg of mixed oatmeal grinding powder, 79.45mg of mixed oatmeal grinding powder and 100mg of mixed oatmeal grinding powder into a 10mL volumetric flask, respectively adding PBS solution, carrying out ultrasonic treatment at 37 ℃ for 30min, fixing the volume to 10mL, transferring to a 15mL centrifuge tube, carrying out vortex centrifugation for 5min, and preparing suspension to be tested. Weigh 0.05mg zinc nicotinamide, dissolve in 1000mL PBS solution, mix well to be tested. The amounts and dilution times of the samples are shown in Table 4.

TABLE 4 sample weighing and dilution factor

A96-well microplate is provided with a solvent bottom well (Ta), a solvent reaction well (Tb), a sample bottom well (Tc), and a sample reaction well (Td). Wherein, the Ta group is a solvent background group, and a substrate L-tyrosine solution and a sample solution are not added; the Tb group is a solvent reaction group, and the substrate L-tyrosine solution is added but no sample solution is added; the Tc group is a sample background group, and a substrate L-tyrosine solution and a sample solution are not added; td group is the sample reaction group, to which both the substrate L-tyrosine solution and the sample solution are added. Each group was plated with three replicate wells and the mean was taken. At the same time, a positive control group of kojic acid solution and a blank control group except for the sample were set at the following doses, and 3 replicates were set.

Weighing 0.025g L-tyrosine, dissolving with PBS buffer solution, ultrasonic-assisted dissolving for 5min, and diluting to 50mL to obtain L-tyrosine solution. Weighing 2.5mg of tyrosinase, and diluting the PBS solution to 5mL to obtain a tyrosinase solution, and preserving at-20 ℃ to avoid secondary freeze thawing. Weighing 40mg of kojic acid, fixing the volume of the PBS solution to 1L, preparing the standard solution of 0.040g/L of kojic acid, gradually diluting the PBS solution in a gradient manner, and finally preparing the standard solution of 0.040g/L, 0.050g/L, 0.010g/L, 0.008g/L, 0.005g/L and 0.002 g/L.

According to table 5, PBS solution, L-tyrosine solution and 5 sample suspensions with corresponding volumes are sequentially added into a 2.5mL centrifuge tube, after oscillation and uniform mixing, the mixture is incubated in a 37 ℃ incubator for 10min, 40 mul of tyrosinase solution is added into each hole, uniform mixing is carried out, the mixture is incubated in the 37 ℃ incubator for 5min, the mixture is centrifuged for 5min at 20000r/min in a 4 ℃ refrigerated centrifuge, 100 mul of each sample is added into a 96-hole ELISA plate, an ELISA reader (BioTek F4 ELISA reader, Baote, USA) is used for detecting the absorbance OD value of each hole, and the detection wavelength is set to 475 nm. The wells were kept consistent (5 min. + -.5 s) from the addition of the tyrosinase solution to the measurement of absorbance.

Each batch of the test requires the addition of a positive control test, the IC of the positive control kojic acid ₅₀ The test system is considered to be effective when the concentration of the compound is 0.005g/L to 0.03 g/L.

TABLE 5 tyrosinase activity inhibition test sample application table

The tyrosinase activity inhibition rate was calculated as follows:

in the formula: y is the tyrosinase activity inhibition rate; a. the _d Absorbance of the sample reaction well; a. the _c Absorbance of the sample background wells; a. the _b Is the average value of absorbance of the solvent reaction wells; a. the _a The absorbance average of the background wells of the solvent is shown.

2. Results of the experiment

This positive control kojic acid IC ₅₀ The corresponding concentration was 0.014557g/L, ranging from 0.005g/L to 0.03g/L, and the test system was considered to be effective.

The results of tyrosinase inhibition assay for 5 samples were averaged in triplicate, as shown in table 6.

TABLE 6 sample concentration and tyrosinase activity inhibition

As can be seen from the detection results, the tyrosinase inhibition rates of the oats, the coconut powder and the nicotinamide which are independently used are respectively about 11.62%, about 8.44% and about 1.54%; the tyrosinase inhibition rate of the oat coconut powder used in combination is about 23.93%, which is far greater than the sum of the inhibition rates of the oat and the coconut powder used alone, and a certain synergistic effect is presented; the tyrosinase inhibition rate of the mixed oatmeal is about 23.79%, the inhibition effect of the mixed oatmeal is not very different when the mixed oatmeal is combined with oat coconut powder, and the two components of the oat and coconut powder which play a main role in inhibiting tyrosinase in the mixed oatmeal are shown, which is probably related to the fact that the total ratio of the oat and coconut powder components in the mixed oatmeal is higher.

However, it is understood by those skilled in the art that other ingredients in the oatmeal can still supplement other nutrition, for example, white kidney beans have the functions of eliminating dampness and blocking starch absorption, coix seeds have the functions of whitening and eliminating dampness, Chinese yam has the functions of nourishing and promoting digestion, poria cocos has the functions of whitening and enhancing the immune function of the organism, and zinc is helpful for growth and development, intelligence development and immunity improvement.

The mixed oatmeal disclosed by the invention is added with the zinc nicotinamide on the basis that the oat, the coconut powder and the like can be directly added into food products, and is reasonably matched with raw materials with whitening effects in a medicine-food homologous list, so that the purpose of improving the skin state is achieved by an edible mode. Through detection, the mixed oatmeal has a certain inhibition effect on tyrosinase, the inhibition rate of the mixed oatmeal is lower than the effects of common medicines or plant extracts such as tranexamic acid, vitamin C, arbutin and the like, but the abnormal reactions of rash, digestive systems and the like caused by the tranexamic acid and the dosage limit requirement of the plant extracts, particularly part of traditional Chinese medicine extracts in food addition are effectively avoided.

The technical features of the embodiments described above may be arbitrarily combined, and for the sake of brevity, all possible combinations of the technical features in the embodiments described above are not described, but should be considered as being within the scope of the present specification as long as there is no contradiction between the combinations of the technical features.

The above-mentioned embodiments only express several embodiments of the present invention, and the description thereof is more specific and detailed, but not construed as limiting the scope of the invention. It should be noted that, for a person skilled in the art, several variations and modifications can be made without departing from the inventive concept, which falls within the scope of the present invention. Therefore, the protection scope of the present patent shall be subject to the appended claims.

Claims

1. A composition for inhibiting tyrosinase comprising a cereal in an amount of 50 wt.% to 95 wt.% and coconut flour in an amount of 4.5 wt.% to 50 wt.%, based on the total weight of the composition.

2. The composition as defined in claim 1, wherein said grain is present in an amount of 60 wt.% to 95 wt.% and said coconut flour is present in an amount of 4.5 wt.% to 15 wt.%, based on the total weight of said composition.

3. The composition as defined in claim 1, wherein said grain is present in an amount of 65 wt.% to 85 wt.% and said coconut flour is present in an amount of 7 wt.% to 12 wt.%, based on the total weight of said composition.

4. The composition as defined in claim 1, wherein said grain is present in an amount of 70 wt.% to 80 wt.% and said coconut flour is present in an amount of 8 wt.% to 10 wt.%, based on the total weight of said composition.

5. The composition of claim 1, wherein the grain is selected from at least one of oat, brown rice, and rice.

6. The composition of claim 1, further comprising at least one of navy bean, red bean, tremella, coix seed, yam, tuckahoe, lotus seed, lily, and kudzu root.

7. The composition according to claim 1, characterized in that it further comprises at least one nutritional enhancer.

8. The composition according to claim 7, wherein the at least one dietary supplement is selected from at least one of dairy products, niacinamide, vitamins, and trace elements.

9. The composition of claim 8, wherein the trace element is selected from at least one of zinc, iron, calcium, magnesium, and sodium.

10. The composition of claim 9, wherein the trace element is zinc.

11. The composition of claim 8, wherein said vitamin is vitamin B2.

12. The composition of claim 1 wherein the composition is mixed instant oatmeal.

13. A composition for inhibiting tyrosinase comprises oat, coconut flour, navy bean, coix seed flour, yam flour, poria cocos rice flakes, niacinamide and zinc.

14. The composition according to claim 13, characterized in that it consists of, based on the total weight of the composition:

oat: 50 wt.% to 95 wt.%, coconut flour: 4.5 wt.% to 50 wt.%, white kidney bean: 6-15 wt.%, coix seed powder: 0.7 wt.% to 10 wt.%, yam flour: 1 wt.% to 10 wt.%, poria cocos rice flakes: 6 wt.% to 25 wt.%, zinc nicotinamide: 0.01 wt.% to 0.5 wt.%.

15. The composition according to claim 13, characterized in that it consists of, based on the total weight of the composition:

oat: 62 wt.% to 75 wt.%, coconut flour: 4.5 wt.% to 15 wt.%, white kidney bean: 6-15 wt.%, coix seed powder: 0.7 wt.% to 2.1 wt.%, yam flour: 1 wt.% to 2 wt.%, poria cocos rice flakes: 11 wt.% to 18.4 wt.%, zinc nicotinamide: 0.01 wt.% to 0.5 wt.%.

16. The composition according to claim 15, wherein the composition consists of, based on the total weight of the composition:

oat: 70.15 wt.%, coconut flour: 9.3 wt.%, white kidney bean: 6 wt.%, coix seed powder: 2 wt.%, yam flour: 1.5 wt.%, poria cocos rice flakes: 11 wt.%, zinc nicotinamide: 0.05 wt.%.

17. The composition according to any one of claims 1 to 16, wherein the composition is a food composition or a functional preparation.

18. A composition according to any one of claims 1 to 16, wherein the composition is for use in inhibiting melanin.

19. Use of a composition according to any one of claims 1-18 for the preparation of a functional formulation for inhibiting tyrosinase production.

20. The use according to claim 19, wherein the composition is used for the preparation of a functional preparation for inhibiting melanogenesis.

21. A method for non-therapeutic purposes of inhibiting tyrosinase production, comprising: providing an effective amount of the composition of any one of claims 1-18 to a subject in need thereof.

22. The method of non-therapeutic purpose according to claim 21, comprising: orally administering to a subject in need thereof an effective amount of the composition.

23. The non-therapeutic method of claim 21, wherein the non-therapeutic method is for inhibiting melanogenesis.