JP2006347934A - Glutathione production accelerator - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a glutathione production accelerator capable of accelerating production of glutathione in a living body and capable of being daily used. <P>SOLUTION: This glutathione production accelerator contains an extract of a plant belonging to the genus Gardenia as an active ingredient for accelerating the production of the glutathione. Further, a glutathione production accelerating composition which contains the extract of the plant belonging to the genus Gardenia as the glutathione production accelerator and therefore is excellent in safety is provided. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

The present invention relates to a glutathione production promoter that exhibits excellent effects. More specifically, the present invention relates to a glutathione production promoter characterized by containing an extract of one or more plants selected from among Gardenia plants.

  Glutathione is a bioactive tripeptide that plays an important role, and its biochemical action is involved in redox reactions, action as a coenzyme, production of mercapturic acid and other detoxification mechanisms, enzymes or The protective effect of other cell components is known. For this reason, glutathione itself has already been used as an effective medicine for eczema, dermatitis, urticaria, Lille dermatoses, melasma, post-inflammation pigmentation, corneal damage healing, etc. It has been reported that it is blended in beverages (see Patent Documents 1 and 2).

JP-A-2-193931 JP-A-5-146279

  However, there are still many unclear points regarding detailed physiological activities and side effects when glutathione itself is ingested, and there are problems with daily use because of the unstable stability of glutathione itself. it was thought.

Therefore, in the present invention, in order to promote the production of glutathione present in the living body and find components that can be ingested on a daily basis, various components were examined for the glutathione production promoting action. As a result, they discovered an excellent glutathione production promoting effect on gardenia genus (Gardenia) plant extracts, and completed the present invention.

That is, the present invention relates to glutathione production promoter having for an active ingredient a gardenia genus (Gardenia) plant extracts, the glutathione production enhancer is routinely used for the purpose of promoting the glutathione production in vivo be able to. Moreover, the glutathione production promoter according to the present invention can be blended in various compositions, and these compositions exhibit an excellent glutathione production promoting action.

  ADVANTAGE OF THE INVENTION According to this invention, the glutathione production promoter which exhibits the outstanding effect can be provided. Moreover, the composition excellent in the glutathione production promoting action can be provided by blending this glutathione production promoter in various compositions.

Gardenia genus (Gardenia) plant is a plant used as the raw material of the present invention is a plant Rubiaceae (Rubiaceae), gardenia (Gardenia jasminoides), Kokuchinashi (Gardenia radicans) and the like are known. Moreover, the fruit of the gardenia genus ( Gardenia ) plant is called Sanshishi ( Gardeniae Fructus ) and has been known as a herbal medicine for a long time.

When using a Gardenia plant, it can be ground and used as it is, but an extract may be used. For extraction, any part such as trunk, branch, leaf, flower, fruit, bark, sap, root, stem, bud, etc. of gardenia plant may be used. From the viewpoint of effectiveness, it is preferable to use fruits. In the extraction, it may be used as it is, but considering the extraction efficiency, it is preferable to perform the extraction after performing processing such as shredding, drying, and pulverization. The extraction can be performed by immersing in an extraction solvent or by an extraction method using a supercritical fluid or a subcritical fluid. In order to increase the extraction efficiency, the mixture may be homogenized in stirring or an extraction solvent. The extraction temperature is suitably about 5 ° C. to the boiling point of the extraction solvent. The extraction time varies depending on the type of extraction solvent and the extraction temperature, but it is appropriate to set it to about 1 hour to 14 days.

  Extraction solvents include water, lower alcohols such as methanol, ethanol, propanol and isopropanol, polyhydric alcohols such as 1,3-butylene glycol, propylene glycol, dipropylene glycol and glycerin, ethers such as ethyl ether and propyl ether. And solvents such as esters such as butyl acetate and ethyl acetate, and ketones such as acetone and ethyl methyl ketone can be used, and one or more of these can be selected and used. Further, physiological saline, phosphate buffer, phosphate buffered saline, or the like may be used. Furthermore, you may use 1 type, or 2 or more types of supercritical fluids and subcritical fluids, such as water, a carbon dioxide, ethylene, propylene, ethanol, methanol, ammonia.

The above-mentioned extract of Gardenia plant with the above solvent can be used as it is, but the concentrated and dried product can be used again by dissolving it in water or a polar solvent. It may be used after performing purification treatment such as decolorization, deodorization, desalting, etc. or fractionation treatment by column chromatography or the like within a range not impairing. The said extract of malvanic acid, its processed material, and a fraction are freeze-dried after each process and fractionation, It can also be melt | dissolved and used for a solvent at the time of use.

Gardenia genus (Gardenia) plant extract has excellent glutathione production promoting action, it can be utilized as a glutathione production enhancer. Moreover, the glutathione production promoter which uses Gardenia plant extract as an active ingredient is blended with various compositions such as pharmaceuticals, foods, cosmetics, bathing agents, etc., so that a composition having a glutathione production promoting action can be obtained. Can be obtained. The composition containing the obtained glutathione production promoter can be used as a composition for promoting glutathione production. By promoting the production of glutathione, eczema, dermatitis, urticaria, Lille melanosis, melasma, inflammation It can be used for the purpose of improving the later pigmentation and the promotion of healing of corneal damage.

Gardenia genus (Gardenia) dosage form of glutathione production promoting composition for formulating glutathione production promoter having for an active ingredient a plant extract of the present invention is arbitrary, the skin external preparation, detergent, when such bath agents Can be provided in various dosage forms such as a solubilizing system such as lotion, an emulsifying system such as emulsion, a dispersion system such as calamine lotion, an aerosol filled with a propellant, an ointment, a powder, and a granule. If the composition is an oral medicine or food, use a general dosage form such as liquids such as drinks and drops, solid preparations such as gums and candy, capsules, powders, granules, and tablets. Can do.

The composition containing a glutathione production promoter containing Gardenia plant extract as an active ingredient includes, in addition to Gardenia plant extract, a normal pharmaceutical, quasi drug, Skin cosmetics, bath preparations, cleaning agents, oily ingredients blended in foods, moisturizers, powders, pigments, emulsifiers, solubilizers, cleaning agents, UV absorbers, thickeners, drugs, fragrances, resins, Alcohols, fortified substances, seasonings and the like can be added as appropriate, and can also be used in combination with other glutathione production promoters.

The amount of the various compositions of glutathione production enhancer of the gardenia genus (Gardenia) plant extract of the present invention as an active ingredient, but may be adjusted depending on the type and purpose of the composition and the like, glutathione production promoting effect From the viewpoint of usability and the like, the content is preferably 0.01% by weight or more, more preferably 0.1% by weight or more, and most preferably 1.0% by weight or more based on the total amount of the composition.

Hereinafter, production examples of extracts of Gardenia , tests for evaluating each action, formulation examples as external preparations for skin and foods, and use tests will be described in more detail, but the technical scope of the present invention Is not limited in any way by this.

First, the preparation method of the extract of Gardenia of this invention is shown.

[Production Example 1]
A 40-fold amount of 50% by weight aqueous ethanol solution was added to a dried pulverized product of Gardenia plant fruit, and the mixture was extracted with stirring at room temperature for 2 hours. The extract was collected by filtration, and after removing the solvent, a Gardenia plant extract was obtained.

[Production Example 2]
Ten times the amount of water was added to the dried pulverized product of Gardenia plant fruit, and the mixture was extracted by refluxing at 90 ° C. for 2 hours. The extract was collected by filtration, and after removing the solvent, a Gardenia plant extract was obtained.

[Production Example 3]
10 volumes of methanol was added to the gardenia genus (Gardenia) dry pulverized fruit plants were immersed for 7 days at room temperature. The extract was collected by filtration, and after removing the solvent, a Gardenia plant extract was obtained.

[Production Example 4]
The fruits of Gardenia plants were put into a supercritical extraction apparatus, and extracted using a supercritical fluid of carbon dioxide at 40 ° C. under a pressure of 15 MPa. The extract was collected to obtain a Gardenia plant extract.

[Evaluation of intracellular glutathione production promoting effect]
Next, the evaluation of glutathione production suppressing action of gardenia genus (Gardenia) plant extract. As a sample, gardenia extract extracted from Gardenia jasminoides using Production Example 1 was used.

A 96-well microplate coated with collagen is seeded with normal human melanocytes at 3.0 × 10 ⁴ cells per well, 2% FCS, fibroblast growth factor (hereinafter FGF) (3 ng / mL), insulin (5 μg / mL) and hydrocortisone (0.18 μg / mL) were added to MGM medium and cultured at 37 ° C. for 24 hours under 5% CO ₂ . Thereafter, each concentration of sample was added to DMSO-dissolved medium to a final concentration of 100 μM and cultured for 48 hours. After culturing, after washing with phosphate buffered saline (hereinafter referred to as PBS) (pH 7.5) containing phenylmethylsulfonyl fluoride ((PMSF) 0.1 mM), 100 mL of PBS containing PMSF (0.1 mM) was added. The ultrasonic crushing process was performed for 5 seconds. The treatment solution was transferred to another plate, and 25 μL of 5% aqueous sodium bicarbonate solution containing 2 mM NADPH, 0 containing ethylenediaminetetraacetic acid (0.5 mM), BSA (1 mg / mL) and glutathione reductase (12.5 / mL) Add 125 μL of phosphate buffer containing 0.5 mM ethylenediaminetetraacetic acid to which 25 μL of 1 M phosphate buffer was added, and let stand at 37 ° C. for 10 minutes, then 0.5 mM ethylenediaminetetraacetic acid and 10 mM 5,5′- 25 μL of 0.1 M phosphate buffer containing dithiobis (2-nitrobenzoic acid) was added to each well, and the glutathione concentration was measured from the absorbance at 450 nm. The amount of glutathione was determined by comparing with the amount of protein measured with the protein analysis kit BCA-200. The amount of glutathione when each sample was added was the relative amount when the amount of glutathione when no sample was added was taken as 100 as an index of the effect of promoting intracellular glutathione production. The results are shown in Table 1.

As is clear from Table 1, when a medium supplemented with Gardenia plant extract was used, a significant glutathione production promoting effect was observed. In particular, when 0.1 mg / mL of Gardenia plant extract was added, a significant effect was observed with a risk rate of less than 1%. Therefore, gardenia genus (Gardenia) plant extract was found to have excellent glutathione production promoting action.

Then, the formulation example of the composition which mix | blended Gardenia ( Gardenia ) plant extract which concerns on this invention is shown.

[Formulation Example 1] Emulsion (1) Squalane 10.0 (wt%)
(2) Methylphenylpolysiloxane 4.0
(3) Hydrogenated palm kernel oil 0.5
(4) Hydrogenated soybean phospholipid 0.1
(5) Polyoxyethylene monostearate
Sorbitan (20E.O.) 1.3
(6) Sorbitan monostearate 1.0
(7) Glycerin 4.0
(8) Methyl paraoxybenzoate 0.1
(9) Carboxyvinyl polymer 0.15
(10) Purified water 53.85
(11) Arginine (1 wt% aqueous solution) 20.0
(12) Gardenia extract [Production Example 1] 5.0
Production method: The oil phase components (1) to (6) are heated and dissolved at 80 ° C. On the other hand, the aqueous phase components (7) to (10) are dissolved by heating at 80 ° C. The oil phase component is added to this while stirring and uniformly emulsified with a homogenizer. After emulsification, start cooling and add (11) and (12) sequentially and mix uniformly.

[Prescription Example 2] Lotion (1) Ethanol 15.0 (% by weight)
(2) Polyoxyethylene (40E.O.) hydrogenated castor oil 0.3
(3) Fragrance 0.1
(4) Purified water 78.38
(5) Citric acid 0.02
(6) Sodium citrate 0.1
(7) Glycerin 1.0
(8) Hydroxyethyl cellulose 0.1
(9) Gardenia extract [Production Example 3] 5.0
Production method: (2) and (3) are dissolved in (1). After dissolution, (4) to (8) are sequentially added, and then sufficiently stirred, (9) is added and mixed uniformly.

[Prescription Example 3] Cream (1) Squalane 10.0 (% by weight)
(2) Stearic acid 2.0
(3) Hydrogenated palm kernel oil 0.5
(4) Hydrogenated soybean phospholipid 0.1
(5) Cetanol 3.6
(6) Lipophilic glyceryl monostearate 2.0
(7) Glycerin 10.0
(8) Methyl paraoxybenzoate 0.1
(9) Arginine (20% by weight aqueous solution) 15.0
(10) Purified water 40.7
(11) Carboxyvinyl polymer (1% by weight aqueous solution) 15.0
(12) Gardenia extract [Production Example 1] 1.0
Production method: The oil phase components (1) to (6) are heated and dissolved at 80 ° C. On the other hand, the aqueous phase components (7) to (10) are dissolved by heating at 80 ° C. The oil phase component is added to this while stirring and uniformly emulsified with a homogenizer. After the emulsification is completed, add (11), start cooling, add (12) at 40 ° C., and mix uniformly.

[Formulation Example 4] Cosmetic liquid (1) Purified water 27.45 (% by weight)
(2) Glycerin 10.0
(3) Sucrose fatty acid ester 1.3
(4) Carboxyvinyl polymer (1% by weight aqueous solution) 17.5
(5) Sodium alginate (1 wt% aqueous solution) 15.0
(6) Polyglyceryl monolaurate 1.0
(7) Macadamia nut oil fatty acid phytosteryl 3.0
(8) N-lauroyl-L-glutamic acid di (phytosteryl-2-octyldodecyl) 2.0
(9) Hardened palm oil 2.0
(10) Squalane (from olive) 1.0
(11) Behenyl alcohol 0.75
(12) Beeswax 1.0
(13) Jojoba oil 1.0
(14) 1,3-butylene glycol 10.0
(15) Arginine (10 wt% aqueous solution) 2.0
(16) Gardenia extract [Production Example 1] 5.0
Production method: The aqueous phase components (1) to (6) are mixed and dissolved by heating at 75 ° C. On the other hand, the oil phase components (7) to (14) are mixed and dissolved by heating at 75 ° C. Next, the oil phase component is added to the aqueous phase component and preliminary emulsification is performed, followed by uniform emulsification with a homomixer. Cooling is started after completion of emulsification, and (15) is added at 50 ° C. Cool further to 40 ° C, add (16) and mix evenly.

[Formulation Example 5] Aqueous gel (1) Carboxyvinyl polymer 0.5 (% by weight)
(2) Purified water 86.7
(3) Sodium hydroxide (10% by weight aqueous solution) 0.5
(4) Ethanol 10.0
(5) Methyl paraoxybenzoate 0.1
(6) Fragrance 0.1
(7) Gardenia extract [Production Example 4] 2.0
(8) Polyoxyethylene (60E.O.) hydrogenated castor oil 0.1
Manufacturing method: (1) is added to (2), and after stirring uniformly, (3) is added. After stirring uniformly, (5) previously dissolved in (4) is added. After stirring uniformly, the previously mixed (6) to (8) are added and stirred and mixed uniformly.

[Formulation Example 6] Cleansing Fee (1) Squalane 81.0 (wt%)
(2) Polyoxyethylene glyceryl isostearate 15.0
(3) Purified water 3.0
(4) Gardenia extract [Production Example 4] 1.0
Manufacturing method: (1) and (2) are uniformly dissolved. (3) and (4) are sequentially added to this and mixed uniformly.

[Prescription Example 7] Face-wash foam (1) Stearic acid 16.0 (% by weight)
(2) Myristic acid 16.0
(3) Lipophilic glyceryl monostearate 2.0
(4) Glycerin 20.0
(5) Sodium hydroxide 7.5
(6) Palm oil fatty acid amidopropyl betaine 1.0
(7) Purified water 36.5
(8) Gardenia extract [Production Example 3] 1.0
Production method: The oil phase components (1) to (4) are heated and dissolved at 80 ° C. On the other hand, the aqueous phase components (5) to (7) are heated and dissolved at 80 ° C., and mixed and stirred uniformly with the oil phase components. Cooling is started, and (8) is added at 40 ° C. and mixed uniformly.

[Prescription Example 8] Make-up base cream (1) Squalane 10.0 (% by weight)
(2) Cetanol 2.0
(3) Glycerin tri-2-ethylhexanoate 2.5
(4) Lipophilic glyceryl monostearate 1.0
(5) Propylene glycol 11.0
(6) Sucrose fatty acid ester 1.3
(7) Purified water 69.4
(8) Titanium oxide 1.0
(9) Bengala 0.1
(10) Yellow iron oxide 0.4
(11) Fragrance 0.1
(12) Gardenia extract [Production Example 2] 1.2
Production method: The oil phase components (1) to (4) are mixed and dissolved by heating at 75 ° C. On the other hand, the aqueous phase components (5) to (7) are mixed and dissolved by heating at 75 ° C., and the pigments (8) to (10) are added thereto and dispersed uniformly with a homomixer. The oil phase component is added to the water phase component and emulsified with a homomixer. Cooling is started after the emulsification is completed, and the components (11) and (12) are added at 40 ° C. and mixed uniformly.

[Formulation Example 9] Emulsion foundation (1) Methylpolysiloxane 2.0 (wt%)
(2) Squalane 5.0
(3) Octyldodecyl myristate 5.0
(4) Cetanol 1.0
(5) Polyoxyethylene (20E.O.)
Sorbitan monostearate 1.3
(6) Sorbitan monostearate 0.7
(7) 1,3-butylene glycol 8.0
(8) Xanthan gum 0.1
(9) Methyl paraoxybenzoate 0.1
(10) Purified water 57.4
(11) Titanium oxide 9.0
(12) Talc 7.4
(13) Bengala 0.5
(14) Yellow iron oxide 1.1
(15) Black iron oxide 0.1
(16) Fragrance 0.1
(17) Gardenia extract [Production Example 4] 1.0
Production method: The oil phase components (1) to (6) are mixed and dissolved by heating at 75 ° C. On the other hand, the aqueous phase components (7) to (10) are mixed and dissolved by heating at 75 ° C., and the pigments (11) to (15) are added thereto and uniformly dispersed with a homomixer. Add oil phase ingredients and emulsify. Cooling is started after the emulsification is completed, and components (16) and (17) are sequentially added at 40 ° C. and mixed uniformly.

[Formulation Example 10] Water-in-oil emollient cream (1) Liquid paraffin 30.0 (% by weight)
(2) Microcrystalline wax 2.0
(3) Vaseline 5.0
(4) Diglycerin oleate 5.0
(5) Sodium chloride 1.3
(6) Potassium chloride 0.1
(7) Propylene glycol 3.0
(8) 1,3-butylene glycol 5.0
(9) Methyl paraoxybenzoate 0.1
(10) Gardenia extract [Production Example 1] 1.0
(11) Purified water 47.4
(12) Fragrance 0.1
Production method: Dissolve (5) and (6) in a part of (11) to 50 ° C., and gradually add to (4) heated to 50 ° C. with stirring. After mixing this, it disperse | distributes uniformly to (1)-(3) heated and melt | dissolved at 70 degreeC. (7) to (10) are added to the remainder of (11) heated and dissolved at 70 ° C. while stirring and emulsified with a homomixer. Cooling is started after completion of emulsification, and (12) is added at 40 ° C. and mixed uniformly.

[Prescription Example 11] Pack (1) Purified water 58.9 (% by weight)
(2) Polyvinyl alcohol 12.0
(3) Ethanol 17.0
(4) Glycerin 5.0
(5) Polyethylene glycol (average molecular weight 1000) 2.0
(6) Gardenia extract [Production Example 2] 5.0
(7) Fragrance 0.1
Production method: (2) and (3) are mixed, heated to 80 ° C, and then dissolved in (1) heated to 80 ° C. After uniformly dissolving, add (4) and (5), and start cooling while stirring. Cool to 40 ° C, add (6) and (7) and mix uniformly.

[Prescription Example 12] Bath agent (1) Fragrance 0.3 (% by weight)
(2) Gardenia extract [Production Example 1] 1.0
(3) Sodium bicarbonate 50.0
(4) Sodium sulfate 48.7
Production method: (1) to (4) are mixed uniformly.

[Prescription Example 13] Hair wax (1) Stearic acid 3.0 (% by weight)
(2) Microcrystalline wax 2.0
(3) Cetyl alcohol 3.0
(4) Highly polymerized methylpolysiloxane 2.0
(5) Methylpolysiloxane 5.0
(6) Poly (oxyethylene / oxypropylene)
Methylpolysiloxane copolymer 1.0
(7) Methyl paraoxybenzoate 0.1
(8) 1,3-butylene glycol 7.5
(9) Arginine 0.7
(10) Purified water 73.6
(11) Gardenia extract [Production Example 1] 2.0
(12) Fragrance 0.1
Production method: The oil phase components (1) to (6) are mixed and heated and dissolved at 75 ° C. On the other hand, the aqueous phase components (7) to (10) are dissolved by heating at 75 ° C., the oil phase component is added, and the mixture is emulsified with a homomixer. Cooling is started after the emulsification is completed, and the components (11) and (12) are added at 40 ° C. and mixed uniformly.

[Prescription Example 14] Hair artic (1) Ethanol 50.0 (% by weight)
(2) Purified water 48.9
(3) Gardenia extract [Production Example 3] 1.0
(4) Fragrance 0.1
Production method: Components (1) to (4) are mixed and homogenized.

[Prescription Example 15] Beverage (1) Gardenia Extract [Production Example 1] 8.0 (wt%)
(2) Erythritol 1.0
(3) Citric acid 0.1
(4) Stevia 0.01
(5) Purified water 90.89
Production method: (1) to (5) are mixed uniformly.

Next, the use tested using the gardenia genus (Gardenia) formulation containing a combination of plant extracts, were evaluated for safety. At that time, the gardenia extract described in Table 2 was blended with the emulsion formulation shown in Formulation Example 1, and tests were conducted as Examples 1-5.

For each example, 10 panelists were allowed to use for 1 month to observe skin conditions such as rough skin, but no skin problems such as rough skin were observed after use. From this, it was found that Gardenia plant extracts have excellent safety.
From the above results, it was revealed that Gardenia plant extract has an excellent glutathione production promoting action and can be used as a highly safe glutathione production promoter.

Claims (2)

A glutathione production promoter characterized by containing an extract of one or more plants selected from among Gardenia plants. Glutathione production enhancer according to claim 1, characterized by containing an extract of gardenia (Gardenia jasminoides).