JP3597068B2 - Antioxidant and composition containing the same - Google Patents

Description

【００２８】
［実施例１］（クリーム）
下記記載の配合量においてＢ成分をＡ成分に混合し、均一に加熱溶解して温度を８０℃にした。次いでＣ成分を注入撹拌混合した後、撹拌しながら３０℃まで冷却しクリームを得た。

【００２９】
［比較例１］（クリーム）
実施例１において成分（Ｂ）ブルセラ・ランシフォリア（Ｂｕｒｓｅｒａ ｌａｎｃｉｆｏｌｉａ）抽出物を除いた以外はすべて実施例１と同様にして調製し、前述した各試験に使用した。
【００３０】
［実施例２］（二相型ローション）
下記記載の配合量においてＡ成分を室温にて均一に混合溶解し、Ｂ成分をゆっくり撹拌添加し二相型ローションを得た。

【００３１】
［比較例２］（二相型ローション）
実施例２において成分（Ｂ）ブルセラ・ランシフォリア（Ｂｕｒｓｅｒａ ｌａｎｃｉｆｏｌｉａ）抽出物を除いた以外はすべて実施例２と同様にして調製し、前述した各試験に使用した。
【００３２】
［試験例２］有用性評価試験
健康な女性（２５〜４０才）８０名を２０名ずつに４群に分け、それぞれ実施例１、２及び比較例１，２の試料を１日２回ずつ塗布し、塗布開始後３ヶ月後の老化防止効果（肌荒れ防止、皮膚の艶・張り）についてアンケート調査を行って評価した。アンケートの評価基準は、有効なものを「優」、やや有効なものを「良」、わずかに有効なものを「可」、無効なものを「不可」として、比較例と比較して評価を行った。
第２表（表２）に示すごとく、比較例１、２に比べ実施例１、２では良好な結果が得られた。
【００３３】
【表２】

【００３４】
［実施例３］（油性軟膏）
下記記載の配合量において各成分を混合し、８０℃まで加温し徐々に冷却し油性軟膏を得た。

【００３５】
［試験例３］
実施例３において調製された油性軟膏を試験例１の抗酸化効果の評価試験法に示す方法と同様の方法に準じ抗酸化試験を行った。その結果、該油性軟膏は（Ｂ）成分を配合しない以外は、全ての成分を含む油性軟膏と比べて、ＤＰＰＨラジカル消去作用及び活性酸素消去作用に優れていた。
【００３６】
【発明の効果】
以上記載の如く、本発明の抗酸化剤を含む化粧品、医薬品、医薬部外品、食品等の組成物は、生体内に生成した活性酸素や過酸化脂質によって引き起こされる障害を抑制する効果がある。従って、健康上、美容上の障害についての治療に有効であり、さらに飲食品の安定化・保存性の向上にも有用である。[0001]
TECHNICAL FIELD OF THE INVENTION
The present invention relates to an antioxidant and a composition containing the antioxidant. Furthermore, the present invention relates to an external preparation for skin that can be used in the fields of pharmaceuticals, quasi-drugs, cosmetics and the like containing the antioxidant.
[0002]
[Prior art]
In recent years, it has become clear that active oxygen generated in a living body reacts with unsaturated fatty acids to generate lipid peroxide, which has an adverse effect on the human body. For example, active oxygen ischemic injury and radiation injury, lipid peroxide and its oxidative degradation products act on nucleic acids and proteins, and cause arteriosclerosis, hypertension, vascular injury, hepatic dysfunction, retinopathy caused by them. And cataracts. In particular, the skin is directly stimulated by environmental factors such as ultraviolet rays, so active oxygen is likely to be generated, increasing the active oxygen concentration, abnormal pigmentation such as spots and freckles such as lipid peroxide, inflammation, edema, The effects are remarkable such as necrosis, wrinkles and aging.
[0003]
In addition, many cosmetics, pharmaceuticals, foods and beverages contain fats and oils, which react with active oxygen during storage and use to generate lipid peroxides, resulting in reduced quality and reduced nutrition and the human body. The development of toxicity is a major problem.
[0004]
For this reason, in order to improve the abnormalities of lipid peroxide in the living body, research for searching for a drug having an antioxidant effect has been widely conducted. Representative examples include fat-soluble tocopherol (vitamin E) and water-soluble ascorbic acid (vitamin C) as natural product antioxidants, and BHT (3,5-tert-butyl-) as a synthetic antioxidant. Examples thereof include 4-hydroxytolen and BHA (2, (3) -tert-butyl-hydroxyanysol) and the like, but their effects were not satisfactory.
[0005]
On the other hand, many attempts have been made to obtain a substance having a high antioxidant activity in order to improve the abnormalities of lipid peroxide in the living body, and various crude drug extracts have been disclosed (for example, Japanese Patent Application Laid-Open No. Hei 5- 246877, JP-A-8-92053, JP-A-8-301745).
[0006]
[Problems to be solved by the invention]
However, the crude drug extract has a somewhat higher antioxidant activity than tocopherol, ascorbic acid, etc., but the activity is not satisfactory. Further, the synthetic antioxidants BHT and BHA have problems such as suspected carcinogenicity. Therefore, in addition to these antioxidants, there is a demand for a substance which has similar means for suppressing the production of lipid peroxide and is highly safe.
[0007]
[Means for Solving the Problems]
In view of such circumstances, the present inventors have conducted intensive studies to improve the problems of the prior art, and as a result, surprisingly, Brucella lansifolia (Gomosilla), a plant of the family Orchidaceae, has been surprisingly obtained. )] Was found to have strong free radical scavenging and antioxidant effects.
[0008]
That is, the present invention provides an antioxidant containing an extract of Brucella lansifolia (Gomosilla) (GOMOSILLA), which is a plant of the family Orchidaceae, and cosmetics and foods containing the antioxidant. And compositions for pharmaceuticals and the like.
[0009]
BEST MODE FOR CARRYING OUT THE INVENTION
Hereinafter, embodiments of the present invention will be described in detail.
Bursera lancifolia used in the present invention is a plant belonging to the genus Brucellaaceae, which is native to Mexico.
[0010]
The extract of Brucella lancifolia used in the present invention is obtained by extracting from a part or all of a plant such as a leaf, a stem, a flower, a seed, a fruit, a bark, a rhizome, a root, etc. of the plant. It is something that can be done. Preferably, it is obtained by extracting from one of the leaves or the stem, or a mixture of both. In general, dried or raw plants are used as they are or cut. As the extraction solvent to be used, the following extraction solvent is used in an amount of 5 to 50 parts based on the dry matter of the dried or fresh plant.
[0011]
As the extraction solvent, generally, water, lower monohydric alcohols (methanol, ethanol, 1-propanol, 2-propanol, 1-butanol, 2-butanol, etc.), liquid polyhydric alcohol (1,3-butylene glycol) , Propylene glycol, etc.), lower alkyl esters (ethyl acetate, etc.), hydrocarbons (benzene, hexane, pentane, etc.), ketones (acetone, methyl ethyl ketone, etc.), ethers (diethyl ether, tetrahydrofuran, dipropyl ether), acetonitrile, etc. Is mentioned. These solvents may be used alone or as a mixture of two or more. Preferably, one or more of water or a water-soluble solvent (a solvent that can be mixed with water at an arbitrary ratio, for example, ethanol, methanol, propylene glycol, etc.) is used.
[0012]
Although the extraction method is not particularly limited, the extraction is carried out at normal temperature or under heating, and examples of the method include ordinary extraction and Soxhlet extraction. The extraction time is not limited, but is generally preferably 1 hour to 1 week.
[0013]
The extract may be used as it is, or may be subjected to various treatments before use. For example, a concentrated solution obtained by concentrating them under normal pressure or reduced pressure, or a solid obtained by evaporating the solvent in the concentrated solution to dryness, or a solid obtained by crystallization from the concentrated solution and drying by filtration, or freezing the concentrated solution Dry solids and the like can be mentioned.
[0014]
The amount (blended amount) of the extract of Bursella lancifolia according to the present invention per dry matter as an antioxidant as an antioxidant is not particularly limited, but is 0.001 to 20.0% by weight based on the total amount. (Hereinafter referred to as “wt%”), particularly preferably 0.01 to 10 wt%.
[0015]
The composition containing the antioxidant of the present invention is characterized by blending the above-mentioned antioxidant, and its use is optional, but it is widely used in cosmetics, foods, pharmaceuticals, quasi-drugs, toiletries and the like. Can be.
[0016]
The cosmetics to which the present invention is applied are not particularly limited in dosage form, and include, for example, lotions, emulsions, creams, foundations, packs, lipsticks, facial cleansers, shampoos, rinses, hair tonics, and the like. These cosmetics include various components generally used in cosmetics, that is, aqueous components, oily components, powder components, alcohols, esters, surfactants, humectants, whitening components, ultraviolet absorbers, thickeners, Components such as coloring agents, fragrances, antioxidants, pH adjusters, chelating agents, preservatives and the like can be added.
[0017]
The food to which the present invention is applied is not particularly limited, and can be obtained, for example, by adding a required amount of an extract to each food raw material as a general food and processing and manufacturing the same by a normal manufacturing method.
[0018]
Pharmaceuticals to which the present invention is applied, quasi-drugs, the dosage form is not particularly limited, for example, tablets, granules, capsules, oral medicines such as drenches, ointments, cataplasms, creams, solutions and the like Examples include external preparations, injections such as sterile solutions and suspensions, and bath preparations. These pharmaceuticals can take the required unit dosage forms with physiologically acceptable vehicles, carriers, excipients, binders, stabilizers, flavoring agents, and the like. For example, compositions for tablets and capsules include binders such as tragacanth, acacia, gelatin, excipients such as microcrystalline cellulose, gelatinized starch, leavening agents such as alginic acid, lubricating agents such as magnesium stearate. A sweetener such as sucrose, lactose and saccharin, a flavoring agent such as peppermint, reddish oil and cherry can be mixed together and formulated by a usual method. Sterile compositions for injections also dissolve the active substance in vehicles such as water for injection, naturally occurring vegetable oils such as sesame oil, coconut oil, peanut oil, cottonseed oil, or synthetic fat vehicles such as ethyl oleate. Alternatively, it can be formulated by a usual method of suspending. As an external preparation, vaseline, paraffin, oils and fats, lanolin, macrogol and the like are used as bases, and ointments and creams are prepared by a usual method.
[0019]
The skin external preparation of the present invention means any dosage form that can be used externally, for example, lotion, emulsion, cream, foundation, pack, essence, lipstick, facial cleanser, gel, aerosol, ointment, poultice, Examples include pastes, plasters, baths, detergents and the like applied to the skin, and shampoos, rinses, treatments, hair tonics and other hairs. Further, the external preparation for skin of the present invention can be used for any of medicine, quasi-drug, and cosmetic.
[0020]
The skin external preparation of the present invention includes an aqueous component, an oily component, a powder component, a wax, fatty acids, alcohols, esters, a surfactant, a humectant, and a whitening component, which are components used in ordinary skin external preparations. A UV absorber, a thickener, a coloring agent, a fragrance, an antioxidant, a pH adjuster, a chelating agent, a preservative, and the like can be appropriately compounded within a range that achieves the object of the present invention.
[0021]
【Example】
Hereinafter, the present invention will be described in detail based on examples. Note that the present invention is not limited to these.
[0022]
[Extraction Example 1] (Production of Brucella lancifolia extract I)
After 100 g of dried Bursella lancifolia was extracted with 1 L of methanol at room temperature for 24 hours, and then similarly twice, the extracts were combined, concentrated and dried to obtain a powdery solid. 3 g were obtained.
[0023]
[Extraction Example 2] (Production of Brucella lancifolia extract II)
100 g of dried Bursella lancifolia was placed in 1 L of a water / ethanol (1: 1, volume ratio) solvent, extracted with stirring at room temperature for 24 hours, filtered, and the filtrate was concentrated to dryness. Thus, 15.8 g of a powdery solid was obtained.
[0024]
[Extraction Example 3] (Production of Bursella lancifolia extract III)
100 g of dried Brucella lancifolia was extracted with 1 L of a mixture of 1,3-butylene glycol and water (1: 1) at room temperature for 10 days, filtered, and the filtrate was concentrated to dryness. 17 g of a solid were obtained.
[0025]
[Test Example 1]
The evaluation test method used in the present invention for examining the antioxidant ability of the above extract is as follows. For comparison, a 50% ethanol extract of rosemary (Rosmarinus officinalis), which is already known to have antioxidant activity, was subjected to the same evaluation, and the test was performed at 100 ug / ml and 10 ug / ml of the sample. The radical removal rate (%) was determined.
(1) Active oxygen elimination test 3.8 mU / ml xanthine oxidase (XOD, manufactured by Sigma), 0.2 mM EDTA, 100 ug / ml BSA (Bovine serum album, manufactured by Sigma) in 80 mM sodium carbonate buffer (pH 10.2), Dissolve so as to give 50 uM NBT (nitro blue tetrazolium), add 0.03 ml of the sample to 1.5 ml of this mixture, and pre-incubate for 5 minutes at 30 ° C. To this solution, 1.5 ml of a 0.2 mM sodium xanthine solution is added, and after standing at 30 ° C. for 20 minutes, the reaction is stopped by adding 0.1 ml of a 6 mM cupric chloride solution, and the absorbance (A) is measured at 560 nm. Measure the absorbance (B) of the buffer with buffer instead of XOD, the absorbance of the buffer with buffer instead of the test sample (C), and the absorbance of the buffer with buffer instead of the test sample and XOD (D). Then, the inhibition rate was determined according to the following equation.
Active oxygen scavenging rate (%) = (1− (AB) / (CD)) × 100
[0026]
(2) DPPH Radical Scavenging Test Using an ethanol solution of the neutral radical Diphenyl-p-picrhydrhydril (DPPH), the effect of the above extract on inhibiting the radical chain reaction of lipids was examined. 800 ul of 250 mM acetate buffer (pH 5.5) is mixed with 800 ul of ethanol and 20 ul of a sample, and pre-incubated at 30 ° C. for 5 minutes. To this solution, 400 ul of 250 uM DPPH / ethanol solution was added and mixed, left at 30 ° C. for 30 minutes, and the absorbance at 517 nm was measured. Then, 20 ul of 300 ug / ml BHT (3,5-tert-butyl-4-hydroxytolen) was added. Then, the absorbance when the DPPH radical is completely removed is measured. From this difference, the radical removal rate is determined.
The results are shown in Table 1 (Table 1). It was found that the Brucella lancifolia extract of Extraction Examples 1, 2, and 3 had a DPPH radical scavenging action and an active oxygen scavenging action comparable to that of a rosemary extract.
[0027]
[Table 1]

[0028]
[Example 1] (cream)
The B component was mixed with the A component in the following blending amount, and the mixture was uniformly heated and melted to a temperature of 80 ° C. Next, the C component was injected, stirred and mixed, and then cooled to 30 ° C. with stirring to obtain a cream.

[0029]
[Comparative Example 1] (cream)
All were prepared in the same manner as in Example 1 except that the component (B) Brucella lancifolia extract was omitted, and used in each of the tests described above.
[0030]
[Example 2] (two-phase lotion)
The component A was uniformly mixed and dissolved at room temperature in the following amount, and the component B was slowly added by stirring to obtain a two-phase lotion.

[0031]
[Comparative Example 2] (Two-phase lotion)
All were prepared in the same manner as in Example 2 except that the component (B) Brucella lancifolia extract was not used, and used in each of the tests described above.
[0032]
[Test Example 2] Usefulness evaluation test Eighty healthy women (25 to 40 years old) were divided into four groups of 20 each, and the samples of Examples 1 and 2 and Comparative Examples 1 and 2 were each twice a day. After the application, the anti-aging effect (prevention of skin roughness, skin gloss / tension) three months after the start of application was evaluated by conducting a questionnaire survey. The evaluation criteria of the questionnaire were evaluated as "excellent" for valid items, "good" for slightly effective items, "acceptable" for slightly effective items, and "impossible" for invalid items. went.
As shown in Table 2 (Table 2), better results were obtained in Examples 1 and 2 than in Comparative Examples 1 and 2.
[0033]
[Table 2]

[0034]
[Example 3] (oil-based ointment)
The components were mixed in the following amounts, heated to 80 ° C., and gradually cooled to obtain an oily ointment.

[0035]
[Test Example 3]
The oil-based ointment prepared in Example 3 was subjected to an antioxidant test according to a method similar to the method shown in Test Method for Evaluation of Antioxidant Effect of Test Example 1. As a result, the oil-based ointment was superior in the DPPH radical scavenging action and the active oxygen scavenging action as compared to the oil-based ointment containing all components except that the component (B) was not blended.
[0036]
【The invention's effect】
As described above, compositions such as cosmetics, pharmaceuticals, quasi-drugs, and foods containing the antioxidant of the present invention have an effect of suppressing a disorder caused by active oxygen or lipid peroxide generated in a living body. . Therefore, it is effective for treatment of health and cosmetic disorders, and is also useful for stabilizing food and drink and improving storage stability.

Claims (3)

An antioxidant comprising an extract of Bursella lancifolia. A composition comprising the antioxidant according to claim 1. An external preparation for skin, comprising the antioxidant according to claim 1.