Composition for inhibiting melanin, its applications and methods

Abstract

The present invention provides a composition for inhibiting tyrosinase, its applications and methods. The composition comprises grains in an amount of about 50 wt.% to about 95 wt.% based on the total weight of the composition and coconut powder in an amount of about 4.5 wt.% to about 50 wt.%. The present invention also provides a composition for inhibiting tyrosinase, which comprises oats, coconut powder, white kidney beans, coix seed powder, yam powder, Poria cocos rice flakes, niacinamide and zinc. The present invention further provides the application of the above composition in the preparation of a functional preparation for inhibiting the generation of tyrosinase, and a non-therapeutic method for inhibiting the generation of tyrosinase. The composition of the present invention can achieve a relatively high tyrosinase inhibition rate, thereby inhibiting the generation of melanin and having a good whitening effect.

Description

Technical Field

[0001] The present invention relates to a composition for inhibiting tyrosinase, particularly a composition for inhibiting melanogenesis by inhibiting tyrosinase activity, and its applications and methods. Background Art

[0002] With the increase of age, there are more and more adverse skin symptoms such as pigment deposition and dull skin tone. Improving skin color has become an increasingly important issue for Eastern women in the pursuit of beauty. The reasons affecting skin color mainly include abnormal melanin metabolism, damaged skin barrier, stagnant skin blood circulation, accumulation of oxygen free radicals, and inflammatory reactions, etc. In particular, due to the influence of ultraviolet rays or hormones, excessive melanin is produced by melanocytes existing between the epidermis and the dermis, or melanin excretion is hindered due to inflammation, etc., which will cause pigment deposition such as skin brown spots and freckles.

[0003] In the prior art, acidic components such as kojic acid, azelaic acid, vitamin C, and linoleic acid are the main active substances for inhibiting melanin formation, but they have characteristics such as poor solubility, poor compatibility, and instability. Natural plant extracts, such as chamomile extract, licorice extract, and bugloss extract, etc., have the advantages of low irritation, high safety, and good efficacy, etc., but most of them are limited to cosmetics, and are easily affected by factors such as high production cost, small dosage, and low utilization rate of skin barrier penetration and absorption.

[0004] As a traditional diet of Chinese people, grains have been one of the indispensable foods on the tables of ordinary people for thousands of years, occupying an important position in the diet of our country and being regarded as traditional staple foods. With the pursuit of health and dietary diversification by consumers in modern society, grains are made into various foods that take into account both health and deliciousness, such as cereal flakes, oatmeal, yogurt containing grains, beverages, biscuits, and so on. Grains are rich in carbohydrates, proteins, vitamins, and minerals, etc., and have high nutritional value. However, there has been no reported technology on using grains to inhibit melanin formation so far. Summary of the Invention

[0005] The present invention provides a composition for inhibiting tyrosinase and its applications and methods.

[0006] In one aspect, the present invention provides a composition for inhibiting tyrosinase, which composition comprises grains in an amount of about 50 wt.% to about 95 wt.% based on the total weight of the composition and coconut powder in an amount of about 4.5 wt.% to about 50 wt.%.

[0007] In some of these embodiments, the composition comprises oats and coconut powder. In some of these embodiments, the composition further comprises at least one of white kidney beans, coix seeds, Chinese yams, poria cocos, niacinamide, and zinc.

[0008] In another aspect, the present invention provides a composition for inhibiting tyrosinase, which composition comprises oats, coconut powder, white kidney beans, coix seed powder, yam powder, Poria cocos rice slices, niacinamide, and zinc.

[0009] In yet another aspect, the present invention further provides the use of the above composition in the preparation of a functional preparation for inhibiting the production of tyrosinase.

[0010] In yet another aspect, the present invention further provides a non-therapeutic method for inhibiting the production of tyrosinase, which method comprises: providing an effective amount of the above composition to a subject in need thereof.

[0011] Other features and aspects of the present invention will be elaborated in more detail below. Detailed Description of the Invention

[0012] The present invention will be described in further detail below so that those of ordinary skill in the art to which the present invention pertains can easily put the present invention into practice. However, it should be understood that the present invention can be implemented in various forms and is not limited to the specific embodiments described herein, and the embodiments of the present invention are only examples.

[0013] As used herein, the term "about" or "approximately" when applied to a numerical value encompasses both the exact value and reasonable variance.

[0014] Unless otherwise specified, the terms "comprising" and "including" and their grammatical variants are intended to be "open-ended" or "inclusive" language, such that they include the recited elements but also permit the inclusion of additional, unrecited elements.

[0015] Unless otherwise specified, all percentages in this specification refer to percentages by weight. The expressions "percent by weight of...", "weight percent", "percent by weight", and "wt.%" are synonyms and refer to an amount expressed as a percentage based on the dry weight.

[0016] The term "effective amount" is a predetermined amount calculated to achieve the desired effect, i.e., to prevent, counteract, alleviate, improve, prevent, inhibit, block, or reverse an undesirable condition in a patient.

[0017] Unless otherwise defined, all terms have and should be given the same meaning as commonly understood by those of ordinary skill in the art to which the present invention pertains.

[0018] Tyrosinase, also known as polyphenol oxidase, is a copper-containing oxidoreductase with a molecular weight of approximately 75 kDa. It is widely present in animals, plants, microorganisms, and the human body and is the rate-limiting enzyme for melanin synthesis, directly affecting melanin production. Tyrosinase consists of multiple subunits, each subunit containing two metal copper ions. The two copper ions are covalently bound to the imino groups of three histidine residues and fixed at the active center. Additionally, there is an endogenous bridging group that links the two copper ions together to form the active center of tyrosinase. If the copper is oxidized, the enzyme becomes inactivated and can be reactivated by electron donors such as L-3,4-dihydroxyphenylalanine, ascorbic acid, superoxide anions, and possibly nitric oxide. There are three types in the tyrosinase gene family that play a role in catalyzing melanin production, namely TYR, TYRP1, and TYRP2. Among them, TYRP1 and TYRP2 play a catalytic role in the last few steps of controlling the type of melanin produced by melanocytes. TYR is a key rate-limiting enzyme in the initial process of melanin synthesis and has at least two activities: tyrosine hydroxylase and dopa oxidase, and is involved in the oxidation and transport of tyrosine during melanin synthesis. Under the catalytic action of tyrosinase, L-tyrosine is hydroxylated to dopa, dopa is oxidized to dopaquinone, and dopaquinone forms the final reaction product melanin. The expression and activity of tyrosinase determine the rate and yield of melanin production. The higher the tyrosinase activity, the more melanin is formed in the skin.

[0019] Melanin generally plays an important role in protecting the human body from ultraviolet radiation. Therefore, ultraviolet light can activate the activity of tyrosinase. After oxidizing tyrosine or 3,4-dihydroxyphenylalanine, melanin is formed through the above series of chemical reactions. Melanin is continuously produced and deposited to form uniform melanin granules, making the skin appear darker. Excessive local production can lead to chloasma and freckles. Therefore, by inhibiting the activity of tyrosinase, melanin production can be inhibited, thereby preventing skin pigment deposition.

[0020] Reagents with tyrosinase activity inhibitory effects can slow down the conversion of L-tyrosine to dopaquinone catalyzed by tyrosinase. Therefore, the inhibitory effect of the test substance on tyrosinase activity can be evaluated by measuring the absorbance of dopaquinone at 475 nm and based on the change in absorbance, thereby evaluating the inhibitory effect on melanin production.

[0021] The present invention relates to a composition for inhibiting tyrosinase, which comprises raw materials such as cereal and coconut powder. By selectively controlling various aspects of the composition, the inventors found that the resulting composition can achieve a high tyrosinase inhibition rate, thereby inhibiting melanin production and having a good whitening effect. The inventors also found that the tyrosinase inhibition rate of the combination of cereal and coconut powder is higher than that of the same dose of cereal and coconut powder used alone, indicating that the combination of cereal and coconut powder has a synergistic effect.

[0022] As used herein, the term "grain" refers to monocotyledonous or dicotyledonous plants grown for their edible seeds, including plants selected from the genus Oryza of the family Poaceae, the genus Triticum, and combinations thereof. Grains suitable for use in the present invention may be selected from, for example, glutinous rice, rice, brown rice, black rice, purple rice, oats, buckwheat, barley, whole wheat, sorghum, or millet, etc. In some embodiments, the grain is selected from at least one of oats, brown rice, and rice. In other embodiments, the grain comprises oats and brown rice. In still other embodiments, the grain comprises oats and rice. In some embodiments, the grain is oats.

[0023] The form of the grain is not particularly limited and can be adjusted as needed, including but not limited to powder, granule, flake, suspension, block, etc. In some embodiments, when the composition is a food composition, the grain can be in the form of powder, granule, flake, or block, etc.

[0024] "Oats" refers to an annual herbaceous plant of the genus Avena L. in the family Poaceae, generally divided into two major categories: hulled type (hulled oats) and naked type (naked oats). Oats are rich in various nutrients such as protein, fat, carbohydrates, vitamins, and trace elements. Compared with crops such as wheat, rice, corn, barley, and sorghum, the contents of the five major indicators of protein, fat, mineral elements, cellulose, and vitamins in its grains rank first. In addition, the amino acid composition of oat flour protein is relatively balanced, and the content of lysine is 1.5 - 3.0 times higher than that of food crops such as wheat. Oats also contain natural antioxidants such as polyphenols, avenanthramides, tocopherols, and carotenoids, which have excellent antioxidant effects and can eliminate free radicals in the body. Its colloidal extract can significantly increase skin moisture and improve skin dryness and roughness.

[0025] For ease of description, the present invention uses the term "coconut powder", but it is not intended to be limited to the powder form, and it can also be coconut milk, coconut juice, coconut milk powder, etc. In the present invention, coconut powder can be derived from coconut meat, coconut extract, coconut milk, coconut juice, etc. Coconut meat contains rich vitamins, minerals, free amino acids, enzymes, and growth promoting factors. Among them, L-arginine and polyphenolic compounds have strong scavenging abilities for superoxide anion radicals, DPPH· radicals, and hydroxyl radicals. Coconut extract can promote the increased expression of skin keratinocyte components and enhance the protective barrier function of the stratum corneum after ultraviolet B irradiation. In addition, coconut powder also has a natural sweetness and can be added as a sweetener to food compositions. In some embodiments of the present invention, except for coconut powder, the composition does not contain a sweetener.

[0026] Specifically, in this composition, based on the total weight of the composition, the content of grains is about 50 wt.% to about 95 wt.%, and the content of coconut powder is about 4.5 wt.% to about 50 wt.%. In some embodiments, in this composition, based on the total weight of the composition, the content of grains is about 60 wt.% to about 95 wt.%, and the content of coconut powder is about 4.5 wt.% to about 15 wt.%. In some embodiments, in this composition, based on the total weight of the composition, the content of grains is about 65 wt.% to about 90 wt.%, and the content of coconut powder is about 6 wt.% to about 13 wt.%. In some embodiments, in this composition, based on the total weight of the composition, the content of grains is about 65 wt.% to about 85 wt.%, and the content of coconut powder is about 7 wt.% to about 12 wt.%. In some embodiments, in this composition, based on the total weight of the composition, the content of grains is about 70 wt.% to about 80 wt.%, and the content of coconut powder is about 8 wt.% to about 10 wt.%. In some embodiments, in this composition, based on the total weight of the composition, the content of grains is about 75 wt.% to about 80 wt.%, and the content of coconut powder is about 9 wt.% to about 10 wt.%.

[0027] To enhance the efficacy of the composition, the composition may further comprise suitable raw materials that are both food and medicine. As used herein, the term "raw materials that are both food and medicine" refers to the raw materials included in the "Regulations on the Administration of Substances That Are Both Food and Chinese Medicinal Materials in Accordance with Tradition" issued by the Department of Food Safety Standards, Inspection and Assessment of the National Health Commission in 2021. These raw materials have both nutritional value and medicinal value and are widely studied and applied in the fields of ordinary food, medicine, and functional food. In some embodiments, the raw materials that are both food and medicine may include, but are not limited to, at least one of white kidney beans, red beans, tremella, coix seeds, Chinese yams, poria cocos, lotus seeds, lilies, and kudzu roots. In some other embodiments, the raw materials that are both food and medicine may include at least one of white kidney beans, tremella, coix seeds, Chinese yams, and poria cocos. In some other embodiments, the raw materials that are both food and medicine may include at least one of tremella, coix seeds, Chinese yams, and poria cocos. In some other embodiments, the raw materials that are both food and medicine may include at least one of white kidney beans, coix seeds, Chinese yams, and poria cocos. In some other embodiments, the raw materials that are both food and medicine may include at least one of tremella, coix seeds, lotus seeds, and poria cocos.

[0028] To exert the efficacy of the raw materials that are both food and medicine while not affecting the overall texture or taste of the composition, based on the total weight of the composition, the content of the raw materials that are both food and medicine is preferably about 2 wt.% to about 25 wt.%. In some embodiments, the content of the raw materials that are both food and medicine is about 8 wt.% to about 15 wt.%. In some other embodiments, the content of the raw materials that are both food and medicine is about 10 wt.% to about 12 wt.%.

[0029] The following will provide a detailed introduction to these raw materials of medicine and food homology.

[0030] White kidney bean (Phaseolus lunatus Billb.ex Beurl.) belongs to the Fabaceae family, Papilionoideae subfamily, Phaseoleae tribe, and Phaseolus genus. It is a leguminous crop widely cultivated worldwide. The kidney bean grains contain 18% - 21% protein, 40% - 60% starch, and 1.6% - 2.15% fat. White kidney bean is not only rich in nutrition but also has medicinal value. It contains amylase inhibitors, which can inhibit the activity of amylase in saliva and hinder the hydrolysis and digestion of carbohydrates in food. It has a wide range of applications in health foods such as weight loss and blood sugar control. In the embodiments of the present invention, the form of white kidney bean is not particularly limited and can be powder, tablet, slurry, etc.

[0031] Red bean (Abrus precatorius L.) is the seed of the Abrus precatorius plant, also known as adzuki bean and small red bean. Red bean contains rich nutritional elements such as protein, carbohydrates, fat, dietary fiber, various vitamins, carotene, inorganic salts, etc. It has the effects of promoting defecation and diuresis, promoting the normal development of bones and teeth, nourishing the five internal organs, and beautifying the skin. In the embodiments of the present invention, the form of red bean is not particularly limited and can be powder, tablet, slurry, etc.

[0032] Tremella fuciformis Berk. is the fruiting body of the fungus Tremella fuciformis in the Basidiomycota phylum. It consists of more than 10 thin and wrinkled flat petal-shaped pieces and is also known as white fungus, snow ear, Tremella fructification, etc. It has the reputation of "the crown of fungi". It is both a precious nutritional tonic and a tonic for strengthening the body. It is flat in nature, sweet, light, and non-toxic. It has the functions of moistening the lungs and promoting fluid production, nourishing the yin and stomach, replenishing qi and calming the nerves, strengthening the heart and nourishing the brain, etc. Tremella fuciformis contains rich proteins, vitamins, etc. Therefore, Tremella fuciformis powder has the effects of anti-aging, removing wrinkles, and tightening the skin. Regular application can also remove freckles, chloasma, etc. In the embodiments of the present invention, the form of Tremella fuciformis is not particularly limited and can be powder, crushed powder, tablet, slurry, etc. In some embodiments, when used as a food composition, Tremella fuciformis can improve the texture of the composition and give it a smooth taste.

[0033] Job's tears (Coix lacryma-jobi L) is the dry and ripe semen of the herbaceous plant Coix in the family Gramineae. It tastes sweet, light, and is cool in nature, with the effects of promoting diuresis and percolating dampness, strengthening the spleen and stopping diarrhea, dispelling obstruction in the meridians, discharging pus, and detoxifying and dissipating binds. Job's tears contains coixenolide, coixol, amino acids, fatty oil, etc. Coixenolide and coixenol have the effect of inhibiting muscle contraction, and coixenol also has sedative, antipyretic, hypothermic and analgesic effects on the central nervous system. The extract of Job's tears can enhance humoral immunity, enhance the activity or cytotoxicity of NK cells and show antiviral and anticancer effects. In addition, experiments have confirmed that it has the effect of inducing ovulation and can reduce blood sugar. A heat-stable protease inhibitor was also found in the bran of the soft-shelled Job's tears seeds. In the embodiments of the present invention, the form of Job's tears is not particularly limited and can be in the form of powder, flakes, slurry, etc.

[0034] Chinese yam (Dioscorea opposita) is the dry rhizome of Dioscorea opposita Thunb. in the Dioscoreaceae family. It is used to treat febrile diseases, heat-toxic dysentery, carbuncles, sores, scrofula, and hemorrhoids. The nutrients it contains are related to mucilage and amylase, and it has a tonic effect and can aid digestion. In the embodiments of the present invention, the form of Chinese yam is not particularly limited and can be in the form of powder, flakes, slurry, etc.

[0035] Poria cocos (Wolfiporia cocos (Schw.) Ryv. & Gibn) is a fungal plant parasitic on the roots of pine trees, shaped like a sweet potato, with a black-brown outer skin and white or pink inside. Poria cocos tastes sweet, light, and is neutral in nature. When used as medicine, it has the functions of promoting diuresis and percolating dampness, benefiting the spleen and stomach, calming the mind and tranquilizing the spirit, and whitening the skin. Modern medical research shows that Poria cocos can enhance the body's immune function, and Poria cocos polysaccharide has obvious anti-tumor and liver-protecting effects. In the embodiments of the present invention, the form of Poria cocos is not particularly limited and can be in the form of powder, flakes, slurry, etc. In some embodiments, when used as a food composition, Poria cocos can be mixed with brown rice or rice to make Poria cocos rice flakes to improve the crispy texture of the composition.

[0036] Lotus seed (Semen Nelumbinis) is the dry and ripe seed of the aquatic herbaceous plant Nelumbo nucifera Gaertn. in the Nymphaeaceae family, also known as lotus fruit, lotus rice, and lotus flesh. Lotus seeds are very nutritious. In addition to containing a large amount of starch, they also contain β-sitosterol, alkaloids, and rich minerals and vitamins such as calcium, phosphorus, and iron. Modern pharmacological research has also confirmed that lotus seeds have various effects such as sedation, strengthening the heart, and anti-aging. In the embodiments of the present invention, the form of lotus seeds is not particularly limited and can be in the form of powder, flakes, slurry, etc.

[0037] Lily (Lilium brownii var. viridulum) is the fleshy scale leaf of Lilium lancifolium Thunb., Lilium brownii F.E.Brown var. viridulum Baker or Lilium pumilum DC. of the Liliaceae family, and has the effects of nourishing yin and moistening the lungs, clearing the heart and calming the mind. It is commonly used to treat dry cough due to yin deficiency, cough with blood in consumptive disease, restlessness due to deficiency, insomnia and dreaminess, and mental trance. In the embodiments of the present invention, the form of lily is not particularly limited and can be powder, sheet, slurry, etc.

[0038] Kudzu root (Radix Puerariae) is the root of Pueraria lobata of the Leguminosae family, with a cool nature, a flat qi and a sweet taste, and has the effects of clearing heat, reducing fire, expelling toxins, etc. Further analysis by modern medical methods shows that kudzu root is rich in up to 13 isoflavone substances, including puerarin, puerarin, puerarin xyloside, daidzein, etc. Puerarin has curative effects on hypertension, hyperlipidemia, hyperglycemia and cardiovascular and cerebrovascular diseases. Puerarin can reduce blood sugar and significantly reduce serum cholesterol. In the embodiments of the present invention, the form of kudzu root is not particularly limited and can be powder, sheet, slurry, etc.

[0039] In order to further enhance the nutritional efficacy of the composition, the composition may further comprise at least one suitable nutritional fortifier. In some embodiments, based on the total weight of the composition, the content of the nutritional fortifier may be about 0.01 wt.% to about 1.5 wt.%. In some other embodiments, based on the total weight of the composition, the content of the nutritional fortifier may be about 0.05 wt.% to about 1 wt.%. In some embodiments, the at least one nutritional fortifier may be selected from at least one of dairy products, niacinamide, vitamins, and trace elements.

[0040] Dairy products may be, for example, milk, goat milk, yogurt or cheese, etc. In some specific embodiments, the dairy product is milk. The form of the dairy product is not particularly limited and may be in the form of powder, block, liquid, or semi-solid, etc.

[0041] Niacinamide is a derivative of vitamin B3 and is widely used in clinical treatment of pellagra, photosensitive dermatitis and cosmetic dermatitis. It can improve the skin quality by inhibiting the transfer of melanin to keratinocytes and accelerating skin cell metabolism, and can be used in cosmetics, foods and pharmaceuticals. When the composition of the present invention is a food composition, the niacinamide is food-grade niacinamide.

[0042] Trace elements are, for example, trace elements essential for the 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, and sodium. In some specific embodiments, the trace element is zinc. Zinc contributes to growth and development, intellectual development, improving immunity, and at the same time maintaining normal appetite in the human body, and is an important trace element essential for the human body.

[0043] Vitamins include, for example, but are not limited to at least one of vitamin A, vitamin B, vitamin C, vitamin D, and vitamin E. In some embodiments, the vitamins can 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 known as riboflavin, is a water-soluble vitamin that is easily digested and absorbed and has the effects of curing oral ulcers and maintaining mucosal health.

[0044] In some of these embodiments, an exemplary formulation of the composition of the present invention is shown in Table 1 below.

[0045] Table 1. Exemplary formulation of the composition of the present invention

[0046]

[0047]

[0048] In some embodiments of the above formulation, oats, coix seeds, Chinese yams, poria cocos, lotus seeds, etc. can be in powder form for easy mixing and absorption.

[0049] The composition of the present invention can be used alone as a functional preparation, such as used as a nutritional supplement or dietary fiber supplement, etc. In addition, this composition can also be ingested as food, such as mixed in cereal porridge, oatmeal, beverages, yogurt, etc. In some specific embodiments, this composition can be instant mixed oatmeal, which can meet the needs of modern fast-paced urban women for health, beauty, and convenience.

[0050] The present invention also relates to a composition for inhibiting tyrosinase, which composition contains oats, coconut powder, white kidney beans, coix seed powder, Chinese yam powder, poria cocos rice flakes, niacinamide, and zinc. By selectively controlling the content of each component of the composition, the inventors have found that the resulting composition can achieve a relatively high tyrosinase inhibition rate, thereby inhibiting the production of melanin and having a good whitening effect. The inventors have also found that the tyrosinase inhibition rate of the combination of oats and coconut powder is higher than that of oats and coconut powder used alone at the same dose, indicating that the combination of grains and coconut powder has a synergistic effect.

[0051] In some embodiments, based on the total weight of the composition, the composition consists of the following components: oats: about 50 wt.% to about 95 wt.%, coconut powder: about 4.5 wt.% to about 50 wt.%, white kidney beans: about 6 wt.% to about 15 wt.%, coix seed powder: about 0.7 wt.% to about 10 wt.%, Chinese yam powder: about 1 wt.% to about 10 wt.%, poria cocos rice flakes: about 6 wt.% to about 25 wt.%, niacinamide and zinc: about 0.01 wt.% to about 0.5 wt.%. In some other embodiments, based on the total weight of the composition, the composition consists of the following components: oats: about 62 wt.% to about 75 wt.%, coconut powder: about 4.5 wt.% to about 15 wt.%, white kidney beans: about 6 wt.% to about 15 wt.%, coix seed powder: about 0.7 wt.% to about 2.1 wt.%, Chinese yam powder: about 1 wt.% to about 2 wt.%, poria cocos rice flakes: about 11 wt.% to about 18.4 wt.%, niacinamide and zinc: about 0.01 wt.% to about 0.5 wt.%. In a specific embodiment, based on the total weight of the composition, the composition consists of the following components: oats: about 70.15 wt.%, coconut powder: about 9.3 wt.%, white kidney beans: about 6 wt.%, coix seed powder: about 2 wt.%, Chinese yam powder: about 1.5 wt.%, poria cocos rice flakes: about 11 wt.%, niacinamide and zinc: about 0.05 wt.%.

[0052] The composition of the present invention can be a food composition or a functional preparation. In some embodiments, except for coconut powder, the composition does not contain sweeteners. When used as a food composition, due to the presence of natural coconut powder, it has a faint fragrance and natural sweetness, without the need to add additional sweeteners such as sucrose and honey, and has low calories, being healthy and delicious. Due to the inclusion of white kidney beans, coix seed powder, Chinese yam powder, and poria cocos rice flakes and other white medicinal and edible homologous raw materials, the composition has the dual effects of removing dampness and nourishing, and is visually appealing, making it more popular among consumers.

[0053] The present invention also relates to the use of the above composition in the preparation of a functional preparation for inhibiting the production of tyrosinase. The functional preparation can be, for example, a cosmetic preparation, a food preparation, or a pharmaceutical preparation, etc. Since melanin is usually generated by the action of tyrosinase on tyrosine, the production of melanin can be inhibited by inhibiting the production of tyrosinase, thereby achieving the effect of whitening the skin. Therefore, the composition can be used to prepare a functional preparation for inhibiting the production of melanin.

[0054] The present invention also relates to a non-therapeutic method for inhibiting the production of tyrosinase, which method comprises: providing an effective amount of the above composition to a subject in need. The providing means include but are not limited to oral administration, topical application, etc. In some embodiments, the non-therapeutic method comprises orally administering an effective amount of the above composition to a subject in need to inhibit melanogenesis.

[0055] Next, the composition of the present invention will be described in detail with reference to specific embodiments, but the present invention is not limited thereto. Unless otherwise specified, the raw materials and chemicals in the following embodiments are food-grade and are commercially available products.

[0056] Examples

[0057] Example 1: Taste and texture evaluation of mixed oatmeal

[0058] The formula of the mixed oatmeal in this example is shown in Table 2 below.

[0059] Table 2. Formula of the mixed oatmeal in Example 1

[0060]

[0061] After brewing the mixed oatmeal in this example with hot water above 90 °C for about 3 to about 5 minutes, it was consumed by 20 tasters and evaluated for its sweetness and texture. The evaluation results are summarized in Table 3 below.

[0062] Table 3. Taste test results of the mixed oatmeal in Example 1

[0063] Very satisfied Satisfied Average Dissatisfied Sweetness 17 2 1 0 Taste 16 3 1 0

[0064] As can be seen from the above table, most members gave good evaluations of the sweetness and texture of the mixed oatmeal in this example. The mixed oatmeal is easy to brew, has a smooth texture, a fresh coconut fragrance, and a natural sweetness.

[0065] Example 2: Tyrosinase activity inhibition test (in vitro method)

[0066] Tyrosinase activity inhibition tests were performed on the mixed oatmeal in Example 1, as well as on the oatmeal, coconut powder, niacinamide and zinc, and oatmeal-coconut powder combination therein, respectively.

[0067] The reagents used in this example are as follows: distilled water; phosphate buffer solution (PBS): pH = 6.8, 0.1 mol / L; L-tyrosine: analytical grade, T3754, purity > 98%, provided by Sigma; tyrosinase: T3824, 1000 unit / mg, provided by Sigma; kojic acid: S30151, provided by Shanghai Yuanye Bio-Technology Co., Ltd.

[0068] 1. Experimental method

[0069] The components and percentage contents of the mixed oatmeal are as described in the formula of Table 2. The oats and coconut powder in the oat-coconut powder combination also correspond to the mutual mass ratio in Table 2, which are approximately 88.3 wt.% and 11.7 wt.%, respectively. The oatmeal, coconut powder, oat-coconut powder combination, and mixed oatmeal are respectively ground using a nano grinder. Weigh 70.71 mg, 9.3 mg, 79.45 mg, and 100 mg of the ground powders of oatmeal, coconut powder, oat-coconut powder combination, and mixed oatmeal into 10 mL volumetric flasks, add PBS solution respectively, ultrasonicate for 30 min under the condition of constant temperature at 37 °C, and make up the volume to 10 mL. Transfer to 15 mL centrifuge tubes, vortex and centrifuge for 5 min to prepare the suspension for testing. Weigh 0.05 mg of niacinamide and zinc, dissolve them in 1000 mL of PBS solution, mix well for testing. The weighing amounts and dilution factors of each sample are shown in Table 4.

[0070] Table 4. Weighing amounts and dilution factors of samples

[0071]

[0072] Set the solvent background wells (Ta), solvent reaction wells (Tb), sample background wells (Tc), and sample reaction wells (Td) in a 96-well enzyme-linked immunosorbent assay (ELISA) plate. Among them, the Ta group is the solvent background group, without adding the substrate L-tyrosine solution and without adding the sample solution; the Tb group is the solvent reaction group, adding the substrate L-tyrosine solution but without adding the sample solution; the Tc group is the sample background group, without adding the substrate L-tyrosine solution and adding the sample solution; the Td group is the sample reaction group, adding both the substrate L-tyrosine solution and the sample solution. Each group is made with three replicate wells and the average value is taken. At the same time, set the kojic acid solution positive control group and the blank control group except for the samples according to the dosage described below, and each is set with 3 parallel samples.

[0073] Weigh 0.025 g of L-tyrosine, dissolve it using PBS buffer, ultrasonicate to assist dissolution for 5 min, and make up the volume to 50 mL to obtain the L-tyrosine solution. Weigh 2.5 mg of tyrosinase, make up the volume to 5 mL with PBS solution to obtain the tyrosinase solution, and store it at -20 °C to avoid secondary freezing and thawing. Weigh 40 mg of kojic acid, make up the volume to 1 L with PBS solution to prepare a 0.040 g / L kojic acid standard solution, and dilute it step by step with PBS solution to finally prepare standard solutions of 0.040 g / L, 0.050 g / L, 0.010 g / L, 0.008 g / L, 0.005 g / L, and 0.002 g / L.

[0074] According to Table 5, add the corresponding volumes of PBS solution, L-tyrosine solution, and 5 kinds of sample suspensions into a 2.5 mL centrifuge tube in sequence. After shaking and mixing evenly, incubate in a constant temperature incubator at 37 °C for 10 min. Add 40 μL of tyrosinase solution to each well, mix evenly, incubate in a constant temperature incubator at 37 °C for 5 min, centrifuge at 20000 r / min in a -4 °C refrigerated centrifuge for 5 min. Take 100 μL of each sample and add it to a 96-well microplate. Use a microplate reader (BioTek F4 microplate reader, manufactured by BioTek Instruments, Inc., USA) to detect the absorbance OD value of each well, and set the detection wavelength to 475 nm. From adding the tyrosinase solution to measuring the absorbance in each well, keep the time consistent (5 min ± 5 s).

[0075] For each batch of tests, a test with a positive control needs to be added. The IC 50 of the positive control kojic acid should be in the range of 0.005 g / L to 0.03 g / L, then the test system is considered effective.

[0076] Table 5. Sample addition table for tyrosinase activity inhibition test

[0077]

[0078]

[0079] The calculation formula for the inhibition rate of tyrosinase activity is as follows:

[0080]

[0081] In the formula: Y is the inhibition rate of tyrosinase activity; A d is the absorbance of the sample reaction well; A c is the absorbance of the sample blank well; A b is the average absorbance of the solvent reaction wells; A a is the average absorbance of the solvent blank wells.

[0082] 2. Experimental results

[0083] The concentration corresponding to the IC 50 of the positive control kojic acid in this test is 0.014557 g / L, which is within the range of 0.005 g / L to 0.03 g / L. Therefore, the test system is considered effective.

[0084] The detection results of the tyrosinase inhibition rates of the 5 samples were respectively averaged in triplicate, as shown in Table 6.

[0085] Table 6. Sample concentration and tyrosinase activity inhibition rate

[0086]

[0087] From the test results, it can be seen that the tyrosinase inhibition rates of oats, coconut powder, and niacinamide used alone are approximately 11.62%, approximately 8.44%, and approximately 1.54% respectively; the tyrosinase inhibition rate of the combination of oats and coconut powder is approximately 23.93%, which is much greater than the sum of the inhibition rates of oats and coconut powder used alone, showing a certain synergistic effect; the tyrosinase inhibition rate of the mixed oatmeal is approximately 23.79%, and there is little difference in the inhibition effect when used in combination with the oats and coconut powder combination, indicating that the two components of oats and coconut powder play a major role in inhibiting tyrosinase in the mixed oatmeal, which may be related to the relatively high overall proportion of oats and coconut powder in the mixed oatmeal.

[0088] However, those skilled in the art can understand that other components in the mixed oatmeal can still play a role in nutritional supplementation in other aspects. For example, white kidney beans have the effects of dispelling dampness and blocking starch absorption, coix seeds have the functions of whitening and dispelling dampness, Chinese yam has the effects of nourishing and aiding digestion, poria cocos has the effects of whitening and enhancing the body's immune function, and zinc is helpful for growth and development, intellectual development, and improving immunity.

[0089] Based on directly edible products such as oats and coconut powder, the mixed oatmeal of the present invention adds niacinamide and zinc, and reasonably combines raw materials with whitening effects in the list of medicated and edible homologous substances, and achieves the purpose of improving the skin condition through the edible method. After testing, the mixed oatmeal has a certain inhibitory effect on tyrosinase. Although its inhibition rate is lower than that of common drugs or plant extracts such as tranexamic acid, vitamin C, and arbutin, it effectively avoids the abnormal reactions such as rashes and digestive systems caused by tranexamic acid, as well as the dosage limit requirements of plant extracts, especially some traditional Chinese medicine extracts, in food additives.

[0090] The technical features of the above-described embodiments can be combined arbitrarily. For the sake of brevity of description, not all possible combinations of the technical features in the above-described embodiments are described. However, as long as there is no contradiction in the combination of these technical features, it should be considered as the scope described in this specification.

[0091] The above-described embodiments only represent several implementation manners of the present invention, and their descriptions are relatively specific and detailed, but they should not be construed as limiting the scope of the invention patent. It should be noted that for those of ordinary skill in the art, without departing from the concept of the present invention, several modifications and improvements can still be made, and these all belong to the protection scope of the present invention. Therefore, the protection scope of the present invention patent should be subject to the appended claims.

Claims

1. A composition for inhibiting tyrosinase, comprising oats in an amount of 70 wt.% to 80 wt.% based on the total weight of the composition and coconut powder in an amount of 8 wt.% to 10 wt.%.

2. The composition according to claim 1, wherein, the composition further comprises at least one of white kidney bean, adzuki bean, tremella, coix seed, Chinese yam, Poria cocos, lotus seed, lily, and kudzu root.

3. The composition according to claim 1, wherein, the composition further comprises at least one nutritional enhancer.

4. The composition according to claim 3, wherein, the nutritional enhancer is selected from at least one of dairy products, niacinamide, vitamins, and trace elements.

5. The composition according to claim 4, wherein, the trace elements are selected from at least one of zinc, iron, calcium, magnesium, and sodium.

6. The composition according to claim 5, wherein, the trace element is zinc.

7. The composition according to claim 4, wherein, the vitamin is vitamin B2.

8. The composition according to claim 1, wherein, the composition is a mixed instant oatmeal.

9. A composition for inhibiting tyrosinase, comprising oats, coconut powder, white kidney bean, coix seed powder, Chinese yam powder, Poria cocos rice flakes, niacinamide, and zinc, wherein, based on the total weight of the composition, the content of oats is 70 wt.% to 80 wt.%, and the content of coconut powder is 8 wt.% to 10 wt.%.

10. The composition according to claim 9, wherein, based on the total weight of the composition, the composition consists of the following components as follows: Oats: 70.15 wt.%, coconut powder: 9.3 wt.%, white kidney bean: 6 wt.%, coix seed powder: 2 wt.%, Chinese yam powder: 1.5 wt.%, Poria cocos rice flakes: 11 wt.%, niacinamide and zinc: 0.05 wt.%.

11. The composition according to any one of claims 1 - 10, wherein, the composition is a food composition or a functional preparation.

12. The composition according to any one of claims 1 - 10, wherein, the composition is used for inhibiting melanin.

13. Use of the composition according to any one of claims 1 - 10 in the preparation of a functional preparation for inhibiting the production of tyrosinase.

14. The use according to claim 13, wherein, the composition is used for the preparation of a functional preparation for inhibiting the production of melanin.

15. A non - therapeutic method for inhibiting the production of tyrosinase, comprising: providing an effective amount of the composition according to any one of claims 1 - 12 to a subject in need.

16. The non - therapeutic method according to claim 15, comprising: administering an effective amount of the composition orally to a subject in need.

17. The non - therapeutic method according to claim 15, wherein, the non - therapeutic method is used for inhibiting the production of melanin.

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