Food and drink composition

Abstract

To provide a food or drink composition capable of improving the state of spots that appear on the skin. 【Solution】Provided is a food or drink composition comprising a fat-soluble vitamin C derivative and at least one selected from the group consisting of an indigo plant extract containing resveratrol, a red wine extract containing resveratrol, a Japanese knotweed root extract containing resveratrol, and a grape peel extract containing resveratrol.

Description

Technical Field

[0001] The present invention relates to a food and drink composition for improving the state of spots that appear on the skin.

Background Art

[0002] Melanin and lipofuscin produced in the skin appear on the skin as pigmented spots, thereby forming spots on the skin surface. Spots are classified into, for example, senile lentigo / solar lentigo, freckles, post-inflammatory hyperpigmentation, melasma, and the like.

[0003] When such spots are formed on the skin surface, the aesthetic appearance deteriorates. Conventionally, in order to solve this problem, compositions for suppressing the occurrence of spots and the like have been developed (see, for example, Patent Document 1 below).

[0004] In addition, vitamin C is used in such compositions. Regarding the effects and efficacy of preventing pigmentation caused by sunburn and sunburn, vitamin C is approved as a Class 3 pharmaceutical in the Japanese Pharmacopoeia.

Prior Art Documents

Patent Documents

[0005]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0006] The present inventors faced the problem that vitamin C is not necessarily stable in a solution state or in the blood. Then, through various studies, the present inventors prepared by adding an extract extracted mainly from the tree Indian quinine (growing wild without pesticide spraying), which has been traditionally and heavily used in Indian traditional medicine for many years, to a fat-soluble vitamin C derivative, and found that spots can be improved.

[0007] Therefore, an object of the present invention is to provide a food and drink composition capable of improving the state of spots that appear on the skin.

Means for Solving the Problems

[0008] The present invention relates to a food and drink composition comprising a fat-soluble vitamin C derivative and at least one selected from the group consisting of an Indian mulberry extract containing resveratrol, a red wine extract containing resveratrol, a Japanese knotweed root extract containing resveratrol, and a grape skin extract containing resveratrol.

Effects of the Invention

[0009] According to the food and drink composition of the present invention, the state of spots that appear on the skin can be improved.

Modes for Carrying Out the Invention

[0010] 1. Food and Drink Composition The food and drink composition of the present invention comprises a fat-soluble vitamin C derivative and at least one selected from the group consisting of an Indian mulberry extract containing resveratrol, a red wine extract containing resveratrol, a Japanese knotweed root extract containing resveratrol, and a grape skin extract containing resveratrol.

[0011] The food and drink composition is not particularly limited, and includes solid, powdery, liquid, sol, and gel forms. For example, supplements (spot-improving supplements) can be mentioned as the food and drink composition.

[0012] 2. Fat-Soluble Vitamin C Derivative The fat-soluble vitamin C derivatives used in the present invention are not particularly limited, and examples thereof include 6-O-palmitoyl-L-ascorbic acid, 6-O-stearoyl-L-ascorbic acid, 6-O-palmitoyl-L-ascorbic acid-phosphate ester, 2,6-O-dipalmitoyl-L-ascorbic acid, ascorbic acid-3-O-ethyl ether, 2-glyceryl-3-octyl ascorbic acid, etc. Preferably, 6-O-palmitoyl-L-ascorbic acid, 6-O-stearoyl-L-ascorbic acid, 6-O-palmitoyl-L-ascorbic acid-phosphate ester can be mentioned, and more preferably, 6-O-palmitoyl-L-ascorbic acid can be mentioned.

[0013] 3. Resveratrol-containing extract The resveratrol-containing extract used in the present invention includes an indokinochi extract. Further, the resveratrol-containing extract that can be used is not particularly limited, and examples thereof include red wine extract, polygonum cuspidatum root extract, grape peel extract, etc.

[0014] The indokinochi extract is not particularly limited, and for example, an extract extracted from the tree indokinochi that has been traditionally and repeatedly used in Indian traditional medicine (Ayurveda) for many years can be used.

[0015] 4. Ratio of the number of carbon atoms of the hydrocarbon group to the number of hydroxyl groups in the molecule of the fat-soluble vitamin C derivative In the fat-soluble vitamin C derivative used in the present invention, the ratio of the number of carbon atoms of the hydrocarbon group to the number of hydroxyl groups in the molecule of the fat-soluble vitamin C derivative is, for example, 0.05 to 18, preferably 3 to 7, more preferably 4.0 to 6, and even more preferably 5.3, although not particularly limited.

[0016] 5. Ratio of the content of the resveratrol-containing extract to the content of the fat-soluble vitamin C derivative When using Indian quinoa extract as the resveratrol-containing extract used in the present invention, the ratio of the content of the Indian quinoa extract to the content of the fat-soluble vitamin C derivative is not particularly limited, but for example, it is 0.01 to 0.30, preferably 0.03 to 0.20, and more preferably 0.05 to 0.10.

[0017] When using red wine extract as the resveratrol-containing extract used in the present invention, the ratio of the content of the red wine extract to the content of the fat-soluble vitamin C derivative is not particularly limited, but for example, it is 0.01 to 0.20, preferably 0.03 to 0.15, and more preferably 0.05 to 0.10.

[0018] 6. Contents of various active ingredients in the food and beverage composition The content of the fat-soluble vitamin C derivative in the food and beverage composition of the present invention is not particularly limited, but for example, it is 20 to 30% by mass, preferably 23 to 27% by mass, and more preferably 24 to 26% by mass.

[0019] The content of the Indian quinoa extract in the food and beverage composition of the present invention is not particularly limited, but for example, it is 1.0 to 2.0% by mass, preferably 1.3 to 1.9% by mass, and more preferably 1.5 to 1.7% by mass.

[0020] When using red wine extract as the resveratrol-containing extract in the food and beverage composition of the present invention, the content of the red wine extract is not particularly limited, but for example, it is 0.5 to 1.5% by mass, preferably 0.7 to 1.3% by mass, and more preferably 0.8 to 1.2% by mass.

[0021] When using a Japanese knotweed root extract as the resveratrol-containing extract in the food and drink composition of the present invention, the content of the Japanese knotweed root extract is not particularly limited. For example, it is 0.5 to 1.5% by mass, preferably 0.7 to 1.3% by mass, and more preferably 0.8 to 1.2% by mass.

[0022] When using a grape skin extract as the resveratrol-containing extract in the food and drink composition of the present invention, the content of the grape skin extract is not particularly limited. For example, it is 0.5 to 1.5% by mass, preferably 0.7 to 1.3% by mass, and more preferably 0.8 to 1.2% by mass.

[0023] 7. Use The food and drink composition of the present invention can be used, for example, as a supplement (a supplement for improving skin blemishes). In addition, examples of the form of the food and drink composition of the present invention include tablets and granules.

[0024] 8. Manufacturing method The food and drink composition of the present invention can be manufactured by a known manufacturing method. For example, when manufacturing a tablet product as the food and drink composition of the present invention, the raw materials used are measured with an electronic balance, and after mixing each material while removing foreign substances, tableting is performed, followed by appearance inspection and packaging of the tablets. Also, for example, when manufacturing a granule product as the food and drink composition of the present invention, the raw materials used are measured with an electronic balance, and after mixing each material while removing foreign substances, granulation and sizing are performed, and then the granules are packaged.

Examples

[0025] Hereinafter, examples and comparative examples will be shown to specifically explain the present invention, but the present invention is not limited to the following examples.

[0026] 1. Production example <Manufacture of supplement> As an active ingredient, 6-O-palmitoyl-L-ascorbic acid, resveratrol-containing indigo plant extract, and resveratrol-containing red wine extract were formulated, and as a base, maltodextrin, maltitol, silicon dioxide, and pullulan were formulated to produce a supplement. The composition details are shown in Table 1.

[0027]

Table 1

[0028] 2. Test Examples <Test Example 1> Nine healthy subjects were evenly divided into 3 test groups by the test implementer A in secrecy from the test evaluator B and made to ingest the supplement. Specifically, (1) the placebo group (P group) ingested only the base (Comparative Example 1), (2) the control group (C group) ingested a formulation with 6-O-palmitoyl-L-ascorbic acid added to the base (Comparative Example 2), and (3) the present invention (resveratrol combination) group (R group) ingested a formulation with the base, 6-O-palmitoyl-L-ascorbic acid, and resveratrol-containing extract (Example 1).

[0029] Then, immediately before the start of the test and 1 month later, the test implementer photographed the subjects' freckles together with the "Freckle Density Gradation Index Plate with Scales" under the same conditions such as shooting angle, illuminance, and shooting distance (Xperia 1 II SO-51A, Photography Pro BASIC mode (manufactured by Sony Corporation)). Using the adjacent skin without freckles as ±0, the freckle images were comprehensively judged in 6 grades from +1 to +5 based on the density of the freckles, the gradation of the freckles, the area, and the number of fusions.

[0030] As a specific determination method, Test Evaluator B determined the similarity degree from the simulation images provided in a random order while keeping the assignment of the test groups concealed, and compared it with the similarity degree separately determined by Test Judge C. If they were the same score, it was taken as the final determination. And when the scores determined by each were different, after re-determining independently by B and C, they had a discussion and made a decision. Each subject also took the test while keeping concealed what test group they received (randomized double-blind test).

[0031] The parts where similarity was confirmed for each subject were the front, left side, and right side of the face, and in some cases, the décolletage and upper limbs were also confirmed as similarity parts.

[0032] The determination results are shown in Table 2.

[0033]

Table 2

[0034] <Test Example 2> To examine the inhibitory effect of resveratrol-containing extract and lipid-soluble vitamin C derivative (6-O-palmitoyl-L-ascorbic acid) on freckles / melanin, a culture test was conducted using human-derived pigment cells HMV-II. Specifically, HMV-II cells were cultured in a 24-well culture plate filled with a medium (Ham F12 medium containing 10% heat-inactivated fetal bovine serum (FBS) / 4 mM L-glutamine (Gln)) until they reached 90% confluence. In this culture state, ultraviolet A wave (315 - 400 nm) was irradiated 3 times every 30 minutes at a dose of 650 mJ / cm2 using a UVA irradiation device (HYPERCURE200, manufactured by Yamashita Electric Co., Ltd.). Three hours later, resveratrol-containing extract and lipid-soluble vitamin C derivative (6-O-palmitoyl-L-ascorbic acid) of various compositions (Examples 2 - 11, Comparative Examples 3 - 14) in Table 3 were added to a Spitz tube containing 100 mL of the above-mentioned medium, and homogenized with a Potter-type Teflon homogenizer for 5 strokes, then mixed with a Vortex mixer for 3 minutes. After another 72 hours, the cells were fixed by treating with paraformaldehyde for 30 minutes, dehydrated with ethanol, and the cells were stained with Masson-Fontana silver stain. With a Hoffman-adjusted phase contrast microscope (ECLIPSE TE2000-3, manufactured by Nikon Corporation), 5 wells in a separate culture plate were set for each test group, and 9 micrographs were taken for each test group. The melanin count was measured for 45 fields each using NIH-Image software, and the experiment was independently conducted 3 times, and statistically processed by Student’s t test, and presented as mean value ± standard deviation. The results are shown in Table 3.

[0035]

Table 3

[0036]

Table 4

[0037] <Test Example 4> The simi / melanin inhibitory effect was examined using a human three-dimensional skin model. Specifically, a Falcon 6-well culture insert (manufactured by Corning) was placed on a plate, and three-dimensional skin (constructed from a co-culture of type I-A collagen and human gingival fibroblasts HGF in the dermal region and a 1:10 mixed cell co-culture of human pigment cells HMV-II and human skin keratinocytes HaCaT in the epidermal region) was formed therein. After 24 hours, for melanin production, an ultraviolet A wave lamp (wavelength: 365 nm) was irradiated vertically 4 times every 30 minutes from 4 directions with an angle change of 90 degrees in the horizontal direction, for a total dose of 8 J / cm2. Three hours later, resveratrol-containing extracts and a fat-soluble vitamin C derivative (6-O-palmitoyl-L-ascorbic acid) of the various compositions in Table 5 (Examples 21 to 27, Comparative Examples 28 to 44) were administered, and 4 days after administration, the melanin content was measured. Specifically, 4 wells in a separate culture plate were set for each test group, 10 micrographs were taken for each test group, the melanin count was measured for every 40 fields using Image-J software, and the experiment was independently carried out 3 times, followed by statistical processing using Student's t test and presented as the mean ± standard deviation. The results are shown in Table 5.

[0038] For the resveratrol standard product in Table 5, a standard product for food analysis / biochemistry (JAN 4987481407107 / JAN 4548995007667, manufactured by Fujifilm Wako Pure Chemical Corporation) was used. The properties are white to light brown, crystalline powder to powder or lumps, soluble in ethanol, methanol, and acetone respectively, and hardly soluble in water.

[0039]

Table 5

[0040] <Test Example 5> In order to examine the effect of various fat-soluble vitamin C derivatives on the freckle / melanin inhibitory effect of a mixture of a resveratrol-containing Indian quince extract and a resveratrol-containing red wine extract, the compositions shown in Table 6 (Examples 28 to 36, Comparative Examples 45 to 63, and Reference Examples 1 to 9) were added in the same procedure as in Test Example 2, and the freckle / melanin inhibitory effect in human-derived pigment cells HMV-II was measured. The results are shown in Table 6.

[0041]

Table 6

[0042] <Test Example 6> The freckle / melanin inhibitory effect was examined using a human three-dimensional skin model. Specifically, the compositions shown in Table 7 (Examples 37 to 41, Comparative Examples 64 to 82) were added in the same procedure as in Test Example 4, and the amount of melanin present was measured. The results are shown in Table 7.

[0043]

Table 7

[0044] 3. Discussion From Table 2, among the total of 51 moles on 3 subjects with 21, 12, and 18 moles who took counterfeit drugs orally for 1 month, no overall change in mole degree before and after oral administration was observed (upper part of Table 2: P group). Among the total of 123 moles on 3 subjects with 36, 56, and 31 moles who took 6-O-palmitoyl-L-ascorbic acid orally, although 1 subject showed a significant improvement in mole degree, no significant difference was observed when all 3 subjects were considered together (middle part of Table 2: C group). Among the total of 65 moles on 3 subjects with 21, 27, and 17 moles who took a resveratrol-containing extract added to 6-O-palmitoyl-L-ascorbic acid, all 3 subjects were able to recognize a significant improvement in mole degree (lower part of Table 2: R group). From this, it can be seen that a food and drink composition obtained by adding a resveratrol-containing extract to 6-O-palmitoyl-L-ascorbic acid is effective in improving moles.

[0045] From Table 3, it can be seen that the melanin production in human pigment cells HMV-II has a small inhibitory effect with 6-O-palmitoyl-L-ascorbic acid alone. In contrast, when a mixture of 50 mg / dL of indokinok extract and 33 mg / dL of red wine extract is co-administered with 6-O-palmitoyl-L-ascorbic acid, it has been verified that the number of administration points with a significantly enhanced melanin inhibitory effect increases, and the range of administration concentrations showing a marked effect expands. As this mechanism, it is presumed that in 6-O-palmitoyl-L-ascorbic acid and the resveratrol-containing extract, an interaction between the two molecules works and contributes to enhancing mole suppression. Also, it is presumed that the interaction is an intermolecular force between the palmitoyl group and the hydrophobic region of resveratrol.

[0046] From Table 4, it was found that melanogenesis in human pigment cells HMV-II was not inhibited by any of 6-O-palmitoyl-L-ascorbic acid alone, indokinet extract containing resveratrol alone, or red wine extract containing resveratrol alone. Furthermore, even in the presence of 6-O-palmitoyl-L-ascorbic acid, no melanin inhibitory effect was observed with indokinet extract alone or red wine extract alone. On the other hand, when a mixture of indokinet extract and red wine extract containing resveratrol was co-administered with 6-O-palmitoyl-L-ascorbic acid, a melanin inhibitory effect was observed. Therefore, there are differences in the types of resveratrol analogs contained in indokinet extract or red wine extract, and it is presumed that the combination of non-common unique analogs (ε-viniferin, oligostilbenes, piceatannol, pterostilbene), the abundance of these analogs, the glycon moiety and its glycosidic bond pattern, and the types of contaminants brought about a synergistic effect. Furthermore, it was confirmed that the concentration range of the combination of indokinet extract and red wine extract, which is 40-90 mg / dL and 20-50 mg / dL respectively, has a wide range of effective administration concentrations in the co-presence of 750 mg / dL of 6-O-palmitoyl-L-ascorbic acid.

[0047] From Table 5, it can be seen that melanogenesis in a human three-dimensional skin tissue model incorporating human pigment cells HMV-II was not inhibited by resveratrol standard products with a purity of 80% or more by HPLC analysis even in the presence of 6-O-palmitoyl-L-ascorbic acid, when compared in the same range of administration concentrations. From this, it is presumed that the combination of resveratrol analogs (ε-viniferin, oligostilbenes, piceatannol, pterostilbene) contained in indokinet extract or red wine extract, the abundance of these analogs, the glycon moiety and its glycosidic bond pattern, and the types of contaminants brought about a synergistic effect.

[0048] From Table 6, it can be seen that when various fat-soluble vitamin C derivatives are used alone, no melanin / freckle suppression effect is observed. When combined with 50 mg of indigo plant extract containing resveratrol and 33 mg of red wine extract, 2,6-O-dipalmitoyl-L-ascorbic acid, ascorbic acid-3-O-ethyl ether, and 2-glyceryl-3-octyl ascorbic acid, in which the ratio of the number of carbon atoms of the hydrocarbon group to the number of hydroxyl groups in the molecule of the fat-soluble vitamin C derivative is outside the range of 2 to 6, are found to have a slightly lower effect. In the case of the combined use of 6-O-palmitoyl-L-ascorbic acid, 6-O-stearoyl-L-ascorbic acid, and 6-O-palmitoyl-L-ascorbic acid-2-phosphate ester, in which the ratio of the number of carbon atoms of the hydrocarbon group to the number of hydroxyl groups in the molecule of the fat-soluble vitamin C derivative is within the range of 4 to 6, with the indigo plant extract containing resveratrol and the red wine extract, a significant effect is shown. That is, when the fat-soluble vitamin C derivative is administered in combination with the indigo plant extract containing resveratrol and the red wine extract, a freckle / melanin suppression effect is brought about. Furthermore, it is found that among the lipid-soluble ascorbic acid derivatives showing a numerical range of 4 to 6 for the ratio of the number of carbon atoms of the hydrocarbon group to the number of hydroxyl groups in the molecule of the fat-soluble vitamin C derivative, a significant effect is shown.

[0049] From Table 7, it can be seen that when the synthetic standard product of resveratrol is administered alone, no melanin / freckle suppression effect is observed. Although the various extracts containing resveratrol also have little effect when administered alone, when any one of the extracts of red wine, Japanese knotweed root, and grape peel is combined with 6-O-palmitoyl-L-ascorbic acid and added to the indigo plant extract alone, it is found to be effective.

[0050] Thus, it can be seen that by preparing a fat-soluble vitamin C derivative mainly containing an indolequinone extract containing resveratrol, the appearance of freckles can be improved. Although the mechanism is not clear, it is inferred that it may be due to (1) differences in the mixing ratio of aglycone:sugar moiety:glycoside, (2) differences in the mixing ratio of trans / cis resveratrol, and (3) differences in the abundance ratio of polyphenols other than resveratrol.

Industrial Applicability

[0051] The food and drink composition of the present invention can be used as a food and drink composition capable of improving the condition of freckles appearing on the skin.

Claims

**Claim 1**: A food or drink composition comprising 6-O-palmitoyl-L-ascorbic acid, an indokinochi extract containing resveratrol, and a red wine extract containing resveratrol, wherein the ratio of the content of the indokinochi extract to the content of the 6-O-palmitoyl-L-ascorbic acid is 0.01 to 0.30, and the ratio of the content of the red wine extract to the content of the 6-O-palmitoyl-L-ascorbic acid is 0.01 to 0.20.

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