JP5412798B2 - Production inhibitor of final glycation product, cosmetics and food and drink - Google Patents

Description

  The present invention relates to a final glycation product production inhibitor containing a peel extract of a leguminous diarum indum (Dialium Indum), a cosmetic and a food and drink containing the same.

Japan today is facing a full-fledged aging society in which the population over 75 years old exceeds 10% of the population. In proportion to this, various diseases such as diabetic complications due to aging, arteriosclerosis, and Alzheimer's disease are rapidly increasing. As these related substances, advanced glycation end products (AGE) are attracting attention. AGE is an irreversible polymer cross-linking substance formed through several chemical reactions when a reducing sugar such as glucose reacts with an amino group of a protein non-enzymatically (Maillard reaction). The reaction is generated through a slow chemical reaction over a long period of time.
The progress of Maillard reaction in living tissue causes aging (decrease in elasticity) in skin tissue due to cross-linking of skin elastic fibers, etc., and AGE deposition on vascular wall tissue and neurofibrils is said to cause arteriosclerosis and Alzheimer's disease. ing. Moreover, AGE is considered to have a great influence on the onset and progress of diabetic complications.
For this reason, various studies have been made for the purpose of inhibiting the generation of AGE, and aminoguanidine, aminopropionitrile, penicillamine and the like are already well known. In addition, urea, guanidine (patent document 1), silicon compounds such as methyltrisilanol (patent document 2), benzophenones (patent document 3), ogon flavonoids (patent document 4), various plant extracts, etc. (patent documents 5 and 6) , 7, 8, 9) have been reported.
However, although aminoguanidine and aminopropionitrile are effective, they are thought to cause malformation by inhibiting cross-linking of collagen and other substances that are required for growth when they are eaten by childhood animals. . In addition, other compounds are weak in action and are not satisfactory for practical use.

By the way, a whitening effect (Patent Document 10), a collagenase inhibitory action (Patent Document 11), an antioxidant action (Patent Document 12), an anti-aging action by inhibiting elastase (Patent Document) 13) is reported. However, the use of timber and fruits of the diarium genus belonging to the genus Diarrium belonging to the subfamily Legumaceae subsidaceae is acceptable, and the use of the pericarp has not been studied at all.
JP-A-62-249908 JP-A-62-249909 JP-A-4-368320 JP-A-3-240725 JP 2004-189663 A JP 2005-35911 A JP 2006-28090 A JP 2006-238711 A JP 2007-254345 A JP 2006-265141 A JP 2003-286179 A Japanese Patent Laid-Open No. 10-045528 Japanese Patent Laid-Open No. 10-029926

The subject of this invention is providing the agent which suppresses the production | generation of a final glycation product known to be related to skin aging, arteriosclerosis, Alzheimer's disease, diabetic complication.
Another object of the present invention is to provide a cosmetic and a food and drink that can be expected to suppress the production of the final glycation product and can prevent the above-described various symptoms.

As a result of diversified researches for the purpose of searching for a composition having an effect of inhibiting skin aging, arteriosclerosis, Alzheimer's disease, and diabetic complications using natural plants, The present inventors have found that the extract has an excellent effect of suppressing the production of final glycation product (AGE) and completed the present invention.
That is, according to the present invention, there is provided an AGE production inhibitor containing, as an active ingredient, a peel extract of a leguminous diarium indam.
Moreover, according to this invention, the cosmetics or food-drinks containing this production | generation inhibitor of AGE are provided.

The inhibitor of the present invention contains an extract of pericarp of dialium indam, which is a natural plant, as an active ingredient, and the fruit containing the pericarp of dialium indam used as the active ingredient is safe for food use. Since it is high, there is no adverse effect on the living body, and the production of AGE by the Maillard reaction of glucose and bovine serum albumin is suppressed at a high inhibition rate, so that it can be used for the prevention of various symptoms related to AGE. For example, it can be applied to cosmetics and foods and drinks containing an external preparation for skin.
In addition, the evaluation of the AGE production inhibitory effect is carried out, for example, when protein and reducing sugar are mixed in a solution and allowed to stand in a heated state, an adduct of protein and reducing sugar is formed. It is known that measurement can be performed using this fluorescence intensity.

Hereinafter, the present invention will be described in more detail.
The dialium indum used in the present invention is an evergreen tree mainly distributed in Southeast Asia, which is a plant belonging to the genus Leguminosae, Jacques subfamily and Dialium. Also known as Velvet Tamarind and Asam Keranji.

The AGE production inhibitor of the present invention contains a peel extract of diarium indum as an active ingredient.
The fruit skin only needs to have an outer skin obtained by removing seeds and pulp from the fruit, and may be in a state where the skin is attached to the skin. The pericarp may be used for extraction as it is, or it may be, for example, dried for 24 hours at a temperature of about 60 ° C. in the sun. In the extraction, in consideration of extraction efficiency, it is preferable that the skin is finely chopped and pulverized.

  The pericarp extract can be prepared, for example, by a method of subjecting the pericarp to solvent extraction. Preferred examples of the solvent include water, hydrophilic solvents such as ethanol, 1,3-butylene glycol, glycerin, and propylene glycol, or a mixture of two or more of these. More preferably, 60 to 100% by mass of ethanol or an aqueous ethanol solution is preferable from the viewpoint of a high inhibition rate of AGE formation in the obtained fruit skin extract.

The amount of the solvent for the peel of Dearium Indum and / or its dried product during extraction is usually preferably 5 to 50 times, and more preferably about 5 to 20 times when considering the subsequent concentration operation and effect expression concentration. .
The extraction time is usually about 2 to 10 days, and the temperature at the time of extraction is preferably 4 to 60 ° C. From the viewpoint of easy extraction, about 7 days at room temperature is more preferable.
The extract can be used in a state containing a solvent, but can usually be used after purification, concentration and drying. Purification can be performed using techniques such as distillation, filtration, chromatography, and drying. Concentration and drying can be performed, for example, by warming concentration, vacuum concentration, spray drying, or freeze drying.
The extract obtained may be in the form of a solution, paste, gel, or powder.

Administration of the AGE production inhibitor of the present invention can be performed, for example, by oral administration or application by skin absorption.
The effective dose of the AGE production inhibitor of the present invention varies depending on the type of the extraction solvent of the extract, the age of the administration subject, the body weight, etc., and can be appropriately selected. However, the pericarp extract is dried per day. In terms of solid content, it is usually 100 mg or more, preferably about 500 mg to 2 g.

  The dosage form of the AGE production inhibitor of the present invention is not particularly limited, and for example, ampoules, capsules, powders, granules, pills, tablets, solids, liquids, gels, bubbles, emulsions, creams, ointments, sheets Can do.

  The component used in order to make the production | generation inhibitor of AGE of this invention into a desired dosage form is not specifically limited, What is normally used for a pharmaceutical and a quasi-drug is mentioned. For example, hydrocarbons such as solid or liquid paraffin, crystal oil, ceresin, ozokerite and montan wax; vegetable or animal oils and waxes such as silicone oil, olive oil, ground wax, carnauba wax and lanolin; stearic acid, palmitic acid , Oleic acid, glycerin stearic acid ester, glycerin monooleic acid ester, isopropyl myristate propyl, isopropyl stearic acid ester, etc .; branched fatty acid monohydric alcohol or polyhydric alcohol ester; ethyl alcohol, isopropyl Alcohols such as alcohol, cetyl alcohol and palmityl alcohol; polyhydric alcohols such as glycol, glycerin and sorbitol or esters thereof; nonionic surfactant, anionic field Active agents, surfactants such as cationic surfactants.

In addition to the above, for example, polysaccharides; cholesterols; plant extracts such as placenta extract and licorice; glycyrrhizic acid and its derivatives, glycyrrhetinic acid and its derivatives, tocopherol and its derivatives, ascorbic acid and its derivatives, kojic acid and its Antioxidants or ultraviolet absorbers such as derivatives, hydroquinones, flavonoids, retinol, hinokitiol, indomethacin, butylhydroxytoluene and the like can also be blended.
Further, for example, metal sequestering agents such as disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, gluconic acid; caffeine, tannin, verapamil, tranexamic acid and its derivatives, grabridine, various Drugs such as crude drugs, tocopherol acetate, glycyrrhizic acid, and salts thereof; whitening agents such as vitamin C, magnesium ascorbate phosphate, glucoside ascorbate, arbutin, and kojic acid; sugars such as glucose, fructose, mannose, sucrose, and trehalose It can mix | blend suitably.
The blending ratio of these other components can be selected and determined as appropriate within a range not impairing the effects of the present invention.

  Generally, AGE causes arteriosclerosis by accumulating in the vascular endothelium, damages kidney cells and causes diabetic nephropathy, crosslinks collagen fibers in the dermis, and causes skin wrinkles and tarmi Therefore, the AGE production inhibitor of the present invention can be expected to suppress the cause of these pathological conditions.

The cosmetics or food / beverage products of this invention contain the production | generation inhibitor of AGE of this invention.
In the cosmetic or food / beverage product of the present invention, the content ratio of the AGE production inhibitor of the present invention can be appropriately selected depending on the type and form thereof, but it is converted into a dry solid content of a peel extract of Diarium Indam, which is an active ingredient. And preferably 0.0001% by mass or more, more preferably 0.01 to 50% by mass.
When the cosmetic or food / beverage product is liquid, the concentration of the extract is not particularly limited as long as the content of the dry solid content as the solute is within the above range.

The cosmetics or food / beverage products of this invention can be manufactured by a well-known method according to the kind and form.
Cosmetics include, for example, basic cosmetics such as lotions, emulsions, creams, ointments, lotions, oils, packs, etc .; external preparations for skin; facial cleansers and skin cleansers, foundations, white powder, funny, lipsticks, blushers, eye shadows Makeup cosmetics such as eyeliner, mascara, eyebrows and eyelashes.
Examples of the food and drink include supplements, drinks, cereals, powdered beverages, jellies, biscuits, strawberries, and gums.

EXAMPLES The present invention will be further described below with reference to examples and comparative examples, but the present invention is not limited to these.
Example 1
Preparation of pericarp extract of Dearium Indum 50 ml of various solvents shown in Table 1 were added to every 5 g of dried fruit obtained by removing seeds and flesh from the fruit of Dearium Indum in the sun, and at room temperature. Left for a week. These solutions were filtered to prepare samples of Dearium Indama peel extract.
AGE Production Inhibition Test A solution (Glucose-BSA-PBS solution) of 0.36 g glucose and 8 mg bovine serum albumin (BSA) dissolved in 10 ml phosphate buffered saline (PBS) was added to 10 μL of the sample solution. 4 ml was added. Immediately after the addition, 0.4 μl of a sample addition solution for 0 hour reaction time was previously added with 40 μL of a 100% (W / V) trichloroacetic acid (TCA) aqueous solution so that no saccharification reaction occurred. It was collected. The remaining sample addition liquid was allowed to stand at 60 ° C. to advance the saccharification reaction. After 48 hours, 0.4 ml of the reaction solution was collected in a tube to which 40 μL of 100% TCA aqueous solution had been added in advance to stop the saccharification reaction. The obtained reaction solution was centrifuged at 12000 rpm for 20 minutes, and the supernatant was removed to recover the precipitated modified BSA.
To the obtained BSA precipitate, an alkaline PBS solution adjusted to pH 10 with a 0.1N sodium hydroxide aqueous solution was added to dissolve the precipitate. 0.1 ml each was added to a 96-well plate, and the fluorescence intensity at an excitation wavelength of 360 nm and a fluorescence wavelength of 460 nm was measured. Based on this fluorescence intensity, the AGE production inhibition rate was calculated according to the following equation. The results are shown in Table 1.

A is fluorescence intensity after 48 hours reaction after addition of sample, B is fluorescence intensity after reaction for 0 hours after addition of sample, X is fluorescence intensity after 0 hour reaction without addition of sample, and Y is 48 hours reaction without addition of sample. Each subsequent fluorescence intensity is shown.

Comparative Example 1
Ages fruit (Rosaceae), Dokudami leaves (Dulaceae), Grape leaves (Vineaceae), Akebet stems (Acariaceae), Daio roots (Tapaceae), Eucommia leaves (Asteraceae), and soybeans Each of the berries (Leguminosae) was extracted with the solvent shown in Table 1 in the same manner as in Example 1 to prepare samples of various plant extracts.
Using each sample obtained and aminoguanidine known to have an AGE production inhibitory action, the fluorescence intensity was measured in the same manner as in Example 1 to calculate the AGE production inhibition rate. The results are shown in Table 1.

  According to Table 1, the diarum indum peel extract of Example 1 has a stronger inhibition of AGE production compared to other plant extracts and aminoguanidines known to have AGE production inhibitory activity. It was found to show the rate. Among them, the peel extract of Dialium Indam extracted using 60 to 100% by mass of ethanol or an aqueous ethanol solution had an extremely high inhibition rate.

Comparative Example 2
In order to examine the inhibitory effect of AGE formation by sites other than the peel of Dialium Indam, each of the flowers, leaves and bark of Dialium Indam was extracted with the solvents shown in Table 1 in the same manner as in Example 1. Samples of each extract were prepared.
Using each of the obtained samples, the fluorescence intensity was measured in the same manner as in Example 1, and the AGE production inhibition rate was calculated. The results are shown in Table 2.

From Table 2, the AGE formation inhibitory effect was not recognized in the flowers, leaves, and bark of Dialium Indam.

Formulation Example 1
0.1% by mass of diarum indum skin extract with 60% by mass ethanol aqueous solution, 5.0% by mass of glycerin, 1.0% by mass of polyoxyethylene sorbitan monolaurate (20E.O), 1,3-butylene A lotion was prepared according to a conventional method using 3.0% by mass of glycol, 10.0% by mass of ethanol, an appropriate amount of preservatives and antioxidants, and the remainder of the purified water.

Formulation Example 2
50% by mass of 1,3-butylene glycol aqueous solution of diarium indum peel extract 0.5% by mass, stearic acid 2.0% by mass, stearyl alcohol 7.0% by mass, beeswax 2.0% by mass, squalane 5 0.0% by weight, glycerin monostearate glycerin 2.0% by weight, polyoxyethylene cetyl ether (20E.O) 3.0% by weight, glycerin 5.0% by weight, preservatives / antioxidants in appropriate amounts, perfume A cosmetic cream was prepared according to a conventional method using an appropriate amount of the remaining purified water.

Formulation Example 3
50% by weight of an aqueous solution of 1,3-butyleneglycol with an extract of perium peel of 0.05% by weight, squalane 5.0% by weight, jojoba oil 5.0% by weight, glycerin monostearate 2.0% by weight, Polyoxyethylene cetyl ether (20E.O) 3.0% by mass, glycerin 2.0% by mass, ethanol 3.0% by mass, preservatives / antioxidants in appropriate amounts, perfumes in appropriate amounts, and using purified water balance, An emulsion was prepared according to the method.

Formulation Example 4
50% by mass of an aqueous solution of 1,3-butyleneglycol with a peel of diarium indum 0.05% by mass, 0.5% by mass of tocopherol acetate, 4.0% by mass of octyl paradimethylaminobenzoate, 4.0% of stearyl alcohol An ointment was prepared according to a conventional method using 1% by mass, 18.0% by mass of owl, 33.0% by mass of petrolatum, an appropriate amount of preservatives and antioxidants, an appropriate amount of fragrance, and the remainder of purified water.

Formulation Example 5
4. Dry mass of Derium indum peel extract with 100% ethanol, 3.0% by mass, crystalline cellulose 10.0% by mass, corn starch 20.0% by mass, lactose 60.0% by mass, hydroxypropylcellulose 5. Tablets were prepared according to a conventional method using 0% by mass and 2.0% by mass of magnesium stearate.

Claims (4)

  An inhibitor of the formation of final glycation products that contains pericarp extract of leguminous diarum indum as an active ingredient.   A peel extract of a leguminous diarum indum is an extract obtained by extracting the peel of a dialium indum with a solvent containing at least one selected from water, ethanol, 1,3-butylene glycol, propylene glycol, and glycerin. The production inhibitor of a final glycation product according to claim 1.   The production inhibitor of a final saccharified product according to claim 2, wherein the solvent is 60 to 100% by mass of ethanol or an aqueous ethanol solution.   Cosmetics containing the production inhibitor of the final glycation product of any one of Claims 1-3.