Combination of phyllanthus emblica and hibiscus syriacus for inhibiting production of melanin

Abstract

The present invention provides a combination of phyllanthus emblica and hibiscus syriacus for inhibiting the production of melanin. The present invention addresses the problem of providing a combination of phyllanthus emblica and hibiscus syriacus for inhibiting the production of melanin. The solution is a combination of phyllanthus emblica and hibiscus syriacus for inhibiting the production of melanin.

Description

Technical Field

[0001] The present invention relates to a combination of Phyllanthus emblica and Hibiscus sylvestris for inhibiting the production of melanin. Background Art

[0002] Melanin generally refers to a brown to black pigment that is biosynthesized from phenols from tyrosine through enzymatic and non-enzymatic oxidation, decarbonation, and coupling reactions. It is represented by the body surface and is widely distributed in animals and plants. It is believed that it plays a role in absorbing excess light.

[0003] On the other hand, skin pigmentation such as spots and freckles is caused by the deposition of melanin produced by melanocytes. In other words, when melanin is produced excessively, it will induce pigmentation such as spots and freckles. Inhibiting the production of melanin is considered to be an effective way to achieve skin whitening by preventing or improving this skin pigmentation.

[0004] So far, various natural ingredients such as arbutin, kojic acid, and ascorbic acid have been reported as ingredients that have a melanin production inhibitory effect, and some of these ingredients have been formulated and actually used in various products such as cosmetics, foods, and medicines.

[0005] For example, Patent Document 1 discloses a melanin production inhibitor containing a dinoflagellates extract.

[0006] As described above, various ingredients have been discovered as ingredients having a melanin production inhibitory effect, but the effects thereof are not always sufficient, and there is a need to develop ingredients and products having an excellent melanin production inhibitory effect.

[0007] Prior art literature

[0008] Patent Literature

[0009] Patent Document 1: Japanese Patent Application Publication No. 2022-011108 Summary of the invention

[0010] The present inventors have found that the combination of Phyllanthus emblica and Hibiscus sylvestris can effectively inhibit the production of melanin. The present invention is based on this finding.

[0011] Therefore, the present invention provides a combination of Emblica officinalis and Hibiscus sylvestris for inhibiting the production of melanin.

[0012] According to the present invention, the following inventions are provided.

[0013] (1) A composition for use in combination with hibiscus sylvestris, the composition comprising emblica emblica and for inhibiting the production of melanin.

[0014] (2) A composition for use in combination with Emblica officinalis, the composition comprising Hibiscus sylvestris and for inhibiting the production of melanin.

[0015] (3) A composition for inhibiting melanin production, comprising Emblica officinalis and Hibiscus sylvestris.

[0016] (4) A composition for use in combination with hibiscus sylvestris, the composition comprising emblica buds, and for improving at least one selected from the group consisting of skin transparency, skin brightness, skin dullness, and skin spots.

[0017] (5) A composition for use in combination with Emblica officinalis, the composition comprising Hibiscus sylvestris and for improving one or more selected from the group consisting of skin transparency, skin brightness, skin dullness, and skin spots.

[0018] (6) A composition comprising emblica officinalis and hibiscus syriacus, and for improving at least one selected from the group consisting of skin transparency, skin brightness, skin dullness, and skin spots.

[0019] (7) The composition according to any one of (1) to (6), wherein the composition is used so that CA / CB is 0.3 to 2.5, when the dry weight of Emblica officinalis is CA and the dry weight of Hibiscus sylvestris is CB.

[0020] (8) The composition according to any one of (1) to (7), which is a composition for oral use.

[0021] (9) Use of a combination of Phyllanthus emblica and Hibiscus sylvestris for the manufacture of a drug for the purpose of inhibiting the production of melanin.

[0022] (10) Use of a combination of Emblica officinalis and Hibiscus sylvestris for the manufacture of a drug for the purpose of improving at least one selected from the group consisting of skin transparency, skin brightness, skin dullness, and skin spots.

[0023] (11) The use according to (9) or (10), wherein when the dry weight of Phyllanthus emblica is CA and the dry weight of Hibiscus sylvestris is CB, CA / CB is 0.3 to 2.5.

[0024] (12) The use according to any one of (9) to (11), wherein the emblica emblica or hibiscus syriacus is in the form of an oral composition.

[0025] (13) Use of a combination of Phyllanthus emblica and Hibiscus sylvestris for inhibiting the production of melanin.

[0026] (14) Use of a combination of Emblica officinalis and Hibiscus sylvestris for improving one or more selected from the group consisting of skin translucency, skin brightness, skin dullness, and skin spots.

[0027] (15) The use according to (13) or (14), wherein when the dry weight of Phyllanthus emblica is CA and the dry weight of Hibiscus sylvestris is CB, CA / CB is 0.3 to 2.5.

[0028] (16) The use according to any one of (13) to (15), wherein the emblica emblica or hibiscus syriacus is in the form of an oral composition.

[0029] (17) A combination of Phyllanthus emblica and Hibiscus sylvestris for inhibiting the production of melanin.

[0030] (18) A combination of Phyllanthus emblica and Hibiscus sylvestris for use in improving at least one selected from the group consisting of skin transparency, skin brightness, skin dullness, and skin spots.

[0031] (19) The combination according to (17) or (18), wherein when the dry weight of Phyllanthus emblica is CA and the dry weight of Hibiscus sylvestris is CB, CA / CB is 0.3 to 2.5.

[0032] (20) The combination according to any one of (17) to (19), wherein the emblica emblica or hibiscus syriacus is in the form of an oral composition.

[0033] (21) A method for inhibiting melanin production in a subject, comprising the step of administering an effective amount of a combination of Emblica officinalis and Hibiscus syriacus.

[0034] (22) A method for improving one or more selected from the group consisting of skin transparency, skin brightness, skin dullness, and skin spots of a subject, comprising the step of administering an effective amount of a combination of Phyllanthus emblica and Hibiscus syriacus.

[0035] (23) The method according to (21) or (22), wherein when the dry weight of Phyllanthus emblica is defined as CA and the dry weight of Hibiscus sylvestris is defined as CB, CA / CB is used in a manner of 0.3 to 2.5.

[0036] (24) The method according to any one of (21) to (23), wherein the emblica emblica or hibiscus syriacus is in the form of an oral composition.

[0037] According to the present invention, a combination of Phyllanthus emblica and Hibiscus sylvestris for inhibiting the production of melanin is provided. By using the combination of the present invention, the production of melanin can be effectively inhibited. BRIEF DESCRIPTION OF THE DRAWINGS

[0038] Figure 1 This is a diagram for evaluating the melanin production inhibitory effect of Phyllanthus emblica and / or Hibiscus sylvestris.

[0039] Figure 2 This is a graph for evaluating the effect of Phyllanthus emblica and / or Hibiscus sylvestris on improving skin transparency.

[0040] Figure 3 This is a graph for evaluating the effect of Phyllanthus emblica and / or Hibiscus sylvestris on improving skin brightness.

[0041] Figure 4 The graph is a graph for evaluating the improvement effect of Phyllanthus emblica and / or Hibiscus sylvestris on the dull yellow color of the skin.

[0042] Figure 5 This is a graph for evaluating the improvement effect of Phyllanthus emblica and / or Hibiscus sylvestris on skin pigmentation. DETAILED DESCRIPTION

[0043] According to one embodiment of the present invention, a melanin production inhibitor containing Emblica officinalis for use in combination with Hibiscus tiliaceus or a composition containing Hibiscus tiliaceus is provided. Such a melanin production inhibitor containing Emblica officinalis may be a composition containing Emblica officinalis for inhibiting the production of melanin.

[0044] According to another aspect of the present invention, a melanin production inhibitor comprising hibiscus is provided for use in combination with emblica emblica or a composition comprising emblica emblica. Such a melanin production inhibitor comprising hibiscus may be a composition comprising hibiscus for inhibiting the production of melanin.

[0045] According to another aspect of the present invention, a melanin production inhibitor comprising Emblica officinalis and Hibiscus sylvestris is provided. Such a melanin production inhibitor comprising Emblica officinalis and Hibiscus sylvestris may be a composition comprising Emblica officinalis and Hibiscus sylvestris for inhibiting the production of melanin.

[0046] In the present invention, the objects to which the combination of Phyllanthus emblica and Hibiscus syriacus is applied are of course not limited, and examples thereof include: primates including humans and chimpanzees; pet animals such as dogs and cats; livestock animals such as cattle, horses, sheep, and goats; mammals such as rodents such as mice and rats, etc. As the object to which the combination of Phyllanthus emblica and Hibiscus syriacus in the present invention is applied, humans are preferred.

[0047] Generally, melanin is produced as follows: tyrosine is oxidized by copper ion-dependent tyrosinase in melanosomes present in melanocytes to generate dihydroxyphenylalanine (DOPA), and then dopaquinone is formed by DOPA-oxidase, and then polymerized with dopachrome and indolequinone in melanocytes in a non-enzymatic manner. The melanin produced in this way is called true melanin (true melanin) and is dark brown. In addition to this true melanin, as melanin, orange-red brown melanin (pheomelanin, sub-melanin) and hair pigments (Trichochromes) are also known to be biosynthesized by dopaquinone and cysteine ​​via dihydrobenzothiazine.

[0048] It is reported that, in general, when eumelanin is formed and deposited on the skin, black pigmentation, increased dullness, decreased transparency, etc. occur, thereby impairing beauty, etc. In addition, it is reported that pheomelanin has cytotoxicity, such as causing hyperoxidation stress, reducing the activity of antioxidant substances in the body, etc. The melanin whose production is inhibited by the composition of the present invention is not particularly limited, and therefore, the composition of the present invention can improve these conditions.

[0049] Improvement in the present invention includes: restoring the state of a subject that is not equivalent to the state of a healthy person or bringing it close to the state equivalent to that of a healthy person, and maintaining the state of a subject that is equivalent to that of a healthy person or making it better than the state equivalent to that of a healthy person.

[0050] According to another embodiment of the present invention, there is provided an improving agent selected from the group consisting of the transparency of the skin, the brightness of the skin, the dark yellow color of the skin and the color spots of the skin, which is used in combination with hibiscus or a composition comprising hibiscus, and which comprises emblica. Such improving agent selected from the group consisting of the transparency of the skin, the brightness of the skin, the dark yellow color of the skin and the color spots of the skin, which comprises emblica, can be a composition comprising emblica for improving the transparency of the skin, the brightness of the skin, the dark yellow color of the skin and the color spots of the skin, which comprises emblica. Such improvement selected from the group consisting of the transparency of the skin, the brightness of the skin, the dark yellow color of the skin and the color spots of the skin, which comprises emblica, can be achieved by suppressing the production of melanin, can not be achieved by suppressing the production of melanin, and is preferably achieved by suppressing the production of melanin.

[0051] According to another embodiment of the present invention, there is provided an improving agent selected from the group consisting of the transparency of the skin, the brightness of the skin, the dark yellow color of the skin, and the color spots of the skin, which is used in combination with Phyllanthus emblica or a composition comprising Phyllanthus emblica, and one or more improving agents of the group consisting of the transparency of the skin, the brightness of the skin, the dark yellow color of the skin, and the color spots of the skin, which is selected from Hibiscus sylvestris. Such improving agents selected from the group consisting of the transparency of the skin, the brightness of the skin, the dark yellow color of the skin, and the color spots of the skin, which is selected from Hibiscus sylvestris, can be a composition comprising Hibiscus sylvestris for improving the transparency of the skin, the brightness of the skin, the dark yellow color of the skin, and the color spots of the skin. Such improvements selected from the group consisting of the transparency of the skin, the brightness of the skin, the dark yellow color of the skin, and the color spots of the skin can be achieved by suppressing the production of melanin, can not be achieved by suppressing the production of melanin, and are preferably achieved by suppressing the production of melanin.

[0052] According to another embodiment of the present invention, there is provided an improver comprising one or more of the group consisting of the transparency of the skin, the brightness of the skin, the dark yellow color of the skin, and the color spots of the skin, which comprises emblica and hibiscus. Such an improver comprising one or more of the group consisting of the transparency of the skin, the brightness of the skin, the dark yellow color of the skin, and the color spots of the skin, which comprises emblica and hibiscus, can be a composition comprising emblica and hibiscus for improving one or more of the group consisting of the transparency of the skin, the brightness of the skin, the dark yellow color of the skin, and the color spots of the skin. Such an improvement comprising one or more of the group consisting of the transparency of the skin, the brightness of the skin, the dark yellow color of the skin, and the color spots of the skin can be achieved by suppressing the generation of melanin, can not be achieved by suppressing the generation of melanin, and is preferably achieved by suppressing the generation of melanin.

[0053] The amounts of emblica and hibiscus used in the composition of the present invention can be appropriately determined depending on the intended use. When the dry weight of emblica is CA and the dry weight of hibiscus is CB, CA / CB is preferably 0.3 to 2.5, and more preferably 0.5 to 1.5.

[0054] The "emblica emblica" in the present invention is Phyllanthus emblica or Emblica officinale (Chinese name: Amla), which is a plant of the genus Emblica of the Euphorbiaceae family, and is also called emblica, oil orange, amla, cowberry fruit, Indian gooseberry, etc. In the present invention, ordinary emblica emblica can be used.

[0055] In the present invention, as the part of Phyllanthus emblica, for example, fruit (immature fruit, mature fruit, dry fruit), leaf, root tuber, flower, seed etc. can be used, preferably fruit. In addition, in the present invention, Phyllanthus emblica itself (for example fresh fruit) can also be used.

[0056] In the present invention, the emblica fruit may be used directly or after drying. According to one embodiment of the present invention, the emblica fruit is an emblica fruit extract produced using the whole emblica fruit or a part of the emblica fruit.

[0057] The "hibiscus" in the present invention refers to Hibiscus sabdariffa or Hibiscus rosa-sinensis (Chinese name: Roselle), which is a plant of the genus Hibiscus of the Malvaceae family, and is also called Roselle and Zhujin, respectively. Generally speaking, hibiscus is a plant native to Africa, and is used as a sauce for French and Italian cuisines due to its refreshing sour taste, and is also used as a herb. In the present invention, common hibiscus can be used, and Roselle is preferably used.

[0058] In the present invention, as the parts of hibiscus, for example, flowers, calyx, buds, fruits, pericarps, seeds, seed coats, stems, leaves, branches, twigs and leaves, trunks, barks, roots, rhizomes, root barks, etc. can be used, and calyx and / or flowers are preferably used.

[0059] In the present invention, hibiscus can be used directly, dried, or extracted with a solvent. According to one embodiment of the present invention, "hibiscus" is a hibiscus extract produced using all or part of hibiscus.

[0060] The method for producing the emblica extract or hibiscus extract of the present invention is not particularly limited, and can be produced according to the method commonly used in the art, for example, by extracting the emblica or hibiscus as a raw material. As the above-mentioned extraction method, there is no particular limitation, and examples thereof include hot water extraction, ultrasonic extraction, filtration, reflux extraction, solvent extraction, etc. These can be performed alone, or two or more methods can be used in combination. In addition, the extract can be further extracted more than once by the same method to obtain a high-purity extract.

[0061] The type of solvent used to prepare the emblica extract or hibiscus extract of the present invention is not particularly limited, and any solvent known in the art can be used as long as the extract having the target effect of the present invention can be obtained. Examples of such solvents are, of course, not limited, and include, for example, water, hexane, ether, ethyl acetate, butanol, acetone, propanol, ethanol, methanol, propylene glycol, 1,3-butanediol, etc., and two or more of these can be used in combination.

[0062] When emblica emblica (including dried products, extracts, etc.) or hibiscus sylvestris (including dried products, extracts, etc.) are commercially available, they may be used as long as a composition having the intended effect of the present invention can be obtained.

[0063] The composition of the present invention is of course not limited, and may be any of a pharmaceutical composition, a cosmetic composition, and a food composition. As the composition of the present invention, a food composition is preferred.

[0064] The composition of the present invention may be any one of an oral composition and a topical composition. The emblica emblica and hibiscus sylvestris in the present invention are preferably absorbed by the digestive tract through oral ingestion, and their active ingredients act in vivo. Therefore, according to a preferred embodiment of the present invention, the composition of the present invention is an oral composition.

[0065] When the composition of the present invention is an oral composition, it can further be matched with known ingredients (additives) that can be matched with the oral composition. As such ingredients, there is no particular limitation, and examples thereof include emulsifiers, wettable powders, solvents, emollients, stabilizers, thickeners, preservatives, lubricants, chelating agents, fillers, excipients, powders, aromatics, spices, absorbents, dyes, opalescents, antioxidants, preservatives, vitamins, amino acids, nutrients, minerals (electrolytes), flavoring agents such as synthetic flavors and natural flavors, pectin acid and its salts, alginic acid and its salts, organic acids, pH regulators, glycerol, alcohols, carbonating agents for carbonated beverages, etc.

[0066] The oral composition of the present invention may be in the form of a liquid, a semisolid, or a solid.

[0067] When the composition of the present invention is a topical composition, it can be further formulated with known ingredients (additives) that can be formulated in topical compositions. Such ingredients are, of course, not limited, and examples thereof include emulsifiers, wettable powders, solvents, emollients, stabilizers, thickeners, preservatives, lubricants, chelating agents, fillers, excipients, powders, aromatics, fragrances, absorbents, dyes, opalescents, antioxidants, vitamins, amino acids, and the like.

[0068] The topical composition of the present invention may be in the form of liquid, semisolid or solid.

[0069] [Example]

[0070] The present invention will be specifically described based on the following examples, but the present invention is not limited to these examples. Unless otherwise specified, the content is expressed in mass %.

[0071] Drugs applied to skin models

[0072] As the drugs, the drugs listed in the following Table 1 were used.

[0073]

Table 1

[0074] Table 1: List of medicines

[0075]

[0076] Cultivation of skin model

[0077] A stainless steel gasket was placed on a 6-well plate, and 5 mL of a culture medium (EPI-100NMM, manufactured by KURABO Co., Ltd.) heated to 37°C was added to each well. A culture cup containing a purchased three-dimensional skin model containing melanocytes (MEL-300, manufactured by KURABO Co., Ltd.) was placed on the plate. The plate was incubated at 37°C under 5% CO according to a conventional method. 2 The cells were cultured in an incubator for more than 1 hour. After the culture, the drug was added to each well so that the emblica extract in the culture medium reached 60 μg / mL by dry weight, or the hibiscus extract in the culture medium reached 30 μg / mL by dry weight, or the emblica extract in the culture medium reached 30 μg / mL by dry weight and the hibiscus extract reached 15 μg / mL by dry weight, and the cells were incubated again. As a control, a culture medium without drug addition was used.

[0078] The medium was replaced every 2 days, and each time the medium was replaced, each drug or control was added so as to achieve the concentration before the medium replacement (the concentration at the time of drug addition). The culture was carried out for 14 days after the start of the culture.

[0079] Evaluation of the effects of drugs on melanin production in skin models

[0080] The amount of melanin in the skin model was measured according to the following steps. The culture cup with the skin model added was washed three times with PBS. The washed skin model was cut out from the culture cup, and each skin model was placed in a 1.5 mL tube to which 200 μL of 1M NaOH was added, and the skin model was immersed in NaOH and allowed to stand at 60°C overnight. Afterwards, after confirming that the skin model was completely dissolved (no dissolved residue), 100 μL of each sample solution was transferred to each well of a 96-well plate, and the absorbance of each sample solution at 405 nm was measured, and the amount of melanin produced was evaluated based on the measurement results.

[0081] Statistical processing was performed by using the Tukey-Kramer method as a multiple comparison test to determine whether or not there was a significant improvement relative to the groups being compared. When p<0.05, it was indicated as *.

[0082] The measurement results are shown in Figure 1 . It was confirmed that the group using emblica alone and the group using hibiscus alone significantly suppressed the production of melanin compared with the control group. In addition, it was shown that the group using emblica and hibiscus in combination significantly suppressed the production of melanin compared with the control group, the group using emblica alone, and the group using hibiscus alone.

[0083] Evaluation of the effects of Phyllanthus emblica and Hibiscus sylvestris on human skin color

[0084] A continuous use test was conducted by a panel of experts, and the effect of the present invention was confirmed by the test shown below. Four test samples (tablets) were prepared for the continuous use test, which were divided into groups A to D for implementation. The number of panel members was: 15 people in Group A (placebo group), 15 people in Group B (60 mg (dry weight) / day of emblica extract), 15 people in Group C (72 mg (dry weight) / day of hibiscus extract), and 15 people in Group D (30 mg (dry weight) of emblica extract + 36 mg (dry weight) of hibiscus extract / day). The panel members were healthy Japanese women aged 35 to 50 years, excluding those who met one or more of the conditions listed in Table 2 below.

[0085]

Table 2

[0086] Table 2: Overview of panelist exclusion criteria

[0087]

[0088] Each panelist took one test sample (tablet) per day for 28 days, and took it orally with water or warm water before going to bed every day. For the tablet, the emblica extract listed in Table 2 was used as the emblica, and the hibiscus extract listed in Table 2 was used as the hibiscus.

[0089] Questionnaire evaluation

[0090] (Test method)

[0091] A questionnaire survey on items related to the color of human skin was conducted before the start of the continuous use test and 1 day, 3 days, 7 days, 14 days, 21 days, and 28 days after the start of the continuous use test.

[0092] The questionnaire survey was evaluated based on VAS (Visual Analog Scale), which is a commonly used evaluation scale. That is, on each survey day, a piece of paper with a 10 cm horizontal straight line drawn on it was handed to the subjects. The left end of the straight line was regarded as the "worst state", and the right end was regarded as the "best state". The actual degree of feeling was filled in as the position on the straight line (the subjects marked a position on the line segment), and the distance moved to the right (or left) based on the test start position was used as the scale value for evaluation. The results of "skin transparency" are shown in Figure 2 , the results of "skin brightness" are shown in Figure 3 , the result of "dark yellow skin color" is shown in Figure 4 , the results of "skin spots" are shown in Figure 5 . Figures 2 to 5In the table, P represents the evaluation result of group A (placebo), A represents the evaluation result of group B (emblica emblica), H represents the evaluation result of group C (hibiscus syriacus), and A+H represents the evaluation result of group D (emblica emblica+hibiscus syriacus).

[0093] Figures 2 to 5 The results showed that group D (Emblica officinalis + Hibiscus sylvestris) had the effect of improving skin transparency, skin brightness, skin dull yellow color and skin spots compared with any of group A (placebo), group B (Emblica officinalis) and group C (Hibiscus sylvestris). In addition, the effect of group D (Emblica officinalis + Hibiscus sylvestris) was higher than the simple addition of the effect of group B (Emblica officinalis) and the effect of group C (Hibiscus sylvestris), indicating that the combination of Emblica officinalis and Hibiscus sylvestris had a synergistic effect in improving skin transparency, skin brightness, skin dull yellow color and skin spots.

Claims

1. A composition for use in combination with hibiscus, the composition comprising emblica emblica and for inhibiting the production of melanin.

2. A composition for use in combination with Emblica officinalis, the composition comprising Hibiscus sylvestris and for inhibiting the production of melanin.

3. A composition for inhibiting the production of melanin, comprising Emblica officinalis and Hibiscus sylvestris.

4. A composition for use in combination with hibiscus sylvestris, the composition comprising emblica buds, and for improving one or more selected from the group consisting of skin transparency, skin brightness, skin dullness, and skin spots.

5. A composition for use in combination with Emblica officinalis, the composition comprising Hibiscus sylvestris and for improving one or more selected from the group consisting of skin transparency, skin brightness, skin dullness and skin spots.

6. A composition comprising Emblica officinalis and Hibiscus sylvestris, and for improving at least one selected from the group consisting of skin transparency, skin brightness, skin dullness, and skin spots.

7. The composition according to any one of claims 1 to 6, wherein When the dry weight of emblica emblica is defined as CA and the dry weight of hibiscus jelly is defined as CB, the composition is used so that CA / CB is 0.3 to 2.

5. 8 . The composition according to claim 1 , which is a composition for oral use.

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