JP2016041666A - Skin whitening composition - Google Patents
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- JP2016041666A JP2016041666A JP2014166274A JP2014166274A JP2016041666A JP 2016041666 A JP2016041666 A JP 2016041666A JP 2014166274 A JP2014166274 A JP 2014166274A JP 2014166274 A JP2014166274 A JP 2014166274A JP 2016041666 A JP2016041666 A JP 2016041666A
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本発明は美白剤に関する。さらに詳しくは、マメ科（Ｌｅｇｕｍｉｎｏｓａｅ）オジギソウ属（Ｍｉｍｏｓａ）センシティーヴァ（Ｍｉｍｏｓａ ｐｕｄｉｃａ）の植物またはその抽出物であるメラニン産生抑制剤及び／又はチロシナーゼ阻害剤とこれを含有する美白用の医薬組成物、化粧料組成物、並びに食品などに関する。 The present invention relates to a whitening agent. In more detail, a melanin production inhibitor and / or a tyrosinase inhibitor, which is a plant of Leguminosae, Mimosa pudicica, or an extract thereof, and a whitening pharmaceutical composition containing the same , Cosmetic compositions, and foods.
加齢に伴うシミ、ソバカスや日焼け後の皮膚色素沈着は、皮膚内に存在する色素細胞（メラノサイト）の活性化によりメラニン産生が著しく亢進した結果として生ずるものであり、中高年齢層における肌の悩みの一つになっている。 Skin pigmentation due to aging, skin freckles and sunburn are caused as a result of markedly increased melanin production due to activation of pigment cells (melanocytes) present in the skin. It has become one of
一般に、メラニンは色素細胞の中で生合成される酵素であるチロシナーゼの働きによって、チロシンからドーパ、ドーパからドーパキノンに変化し、ついで５,６−ジヒドロキシインドフェノール等の中間体を経て形成されるものとされている。従って、皮膚色素沈着症等を予防・治療するためには、メラニン産生過程を阻害することが有効である。 In general, melanin is converted from tyrosine to dopa and from dopa to dopaquinone by the action of tyrosinase, an enzyme biosynthesized in pigment cells, and then formed through intermediates such as 5,6-dihydroxyindophenol. It is said that. Therefore, in order to prevent and treat skin pigmentation etc., it is effective to inhibit the melanin production process.
このような考えに基づき、従来から種々の美白成分が提案されている。例えば、チロシナーゼ活性を阻害してメラニン産生を抑制するものとして、コロイド硫酸やグルタチオンに代表される硫黄化合物等、コウジ酸、アルブチンなどが知られている。 Based on such an idea, various whitening components have been conventionally proposed. For example, as compounds that inhibit tyrosinase activity and suppress melanin production, sulfur compounds such as colloidal sulfate and glutathione, kojic acid, arbutin, and the like are known.
このうち特に、コウジ酸及びその誘導体はチロシナーゼ阻害剤、メラニン産生抑制剤として、美白用化粧料に使用されてきた（特許文献１−３参照）。しかし近年になって、コウジ酸が発がん性及び遺伝毒性を有する可能性が指摘され、これに替わる安全なチロシナーゼ阻害剤、メラニン産生抑制剤が求められている。 Of these, kojic acid and its derivatives have been used in whitening cosmetics as tyrosinase inhibitors and melanin production inhibitors (see Patent Documents 1-3). However, in recent years, the possibility that kojic acid has carcinogenicity and genotoxicity has been pointed out, and a safe tyrosinase inhibitor and a melanin production inhibitor are demanded instead.
さらに、美白用化粧料においては、皮膚に対する低刺激性の要求や天然指向を反映して、植物の抽出物中にメラニン産生抑制作用を有するものを見いだそうとする試みがなされている（特許文献４−８参照）。 Furthermore, in whitening cosmetics, an attempt has been made to find a plant extract having an inhibitory effect on melanin production, reflecting the demand for low skin irritation and natural orientation (Patent Document 4). See -8).
本発明は、上述のような現状に鑑み、安全性及び皮膚官能性に優れ、高いチロシナーゼ阻害作用及び／又はメラニン産生抑制作用を有する新規美白剤を提供することを主な目的とする。 In view of the present situation as described above, the main object of the present invention is to provide a novel whitening agent that is excellent in safety and skin functionality and has a high tyrosinase inhibitory action and / or melanin production inhibitory action.
本発明者は、上記課題の解決のため、種々の天然物を探索し、マメ科オジギソウ属の植物に強いチロシナーゼ阻害作用及びメラニン産生抑制作用があることを初めて見出し、本願発明を完成するに至った。 In order to solve the above problems, the present inventors have searched for various natural products and found for the first time that plants of the genus Leguminosae have a strong tyrosinase inhibitory action and a melanin production inhibitory action, thereby completing the present invention. It was.
本発明は、以下のチロシナーゼ阻害剤及び／又はメラニン産生抑制剤を提供するものである。
１．マメ科オジギソウ属の植物又はその抽出物を有効成分とするチロシナーゼ阻害剤及び／又はメラニン産生抑制剤。
２． １の植物がセンシティーヴァ（Ｍｉｍｏｓａ ｐｕｄｉｃａ）であるチロシナーゼ阻害剤及び／又はメラニン産生抑制剤。
３．前記抽出物が水、アルコールまたはこれらの混合溶媒による抽出物である、１〜２に記載のチロシナーゼ阻害剤及び／又はメラニン産生抑制剤。
４．前期記載のアルコールがエタノールであることを特徴とする１〜３に記載のチロシナーゼ阻害剤及び／又はメラニン産生抑制剤。
５．前期記載の溶媒のエタノール濃度が１０〜１００容量％であることを特徴とする１〜４に記載のチロシナーゼ阻害剤及び／又はメラニン産生抑制剤。
６．1~５を配合してなる美白剤。
７．1~５を配合してなる皮膚外用剤。
The present invention provides the following tyrosinase inhibitors and / or melanin production inhibitors.
1. A tyrosinase inhibitor and / or a melanin production inhibitor containing a leguminous genus plant or an extract thereof as an active ingredient.
2. A tyrosinase inhibitor and / or a melanin production inhibitor, wherein one plant is Senmosiva (Mimosa pudicica).
3. The tyrosinase inhibitor and / or melanin production inhibitor according to 1-2, wherein the extract is an extract of water, alcohol, or a mixed solvent thereof.
4). The tyrosinase inhibitor and / or melanin production inhibitor according to 1 to 3, wherein the alcohol described in the previous period is ethanol.
5. The tyrosinase inhibitor and / or melanin production inhibitor according to 1-4, wherein the ethanol concentration of the solvent described in the previous period is 10 to 100% by volume.
6. A whitening agent comprising 1 to 5.
7. An external preparation for skin comprising 1 to 5.
皮膚の着色の原因となるメラニン色素は、皮膚組織中の色素細胞（メラノサイト）で生
成される。皮膚のシミやソバカス等の色素沈着は、日光からの紫外線暴露による刺激やホ
ルモン異常、または遺伝的要因等が原因となって、色素細胞が活性化された結果、メラニ
ン色素が異常沈着して発生するものと考えられている。通常、皮膚組織の代謝（ターンオ
ーバー）によりメラニンは代謝されるが、加齢に伴う皮膚組織の代謝の低下なども、色素
沈着の原因となる。
Melanin pigments that cause skin coloring are produced by pigment cells (melanocytes) in the skin tissue. Pigmentation such as skin spots and buckwheat is caused by abnormal deposition of melanin as a result of activation of pigment cells due to stimulation by ultraviolet exposure from sunlight, hormonal abnormalities, or genetic factors. It is thought to do. Normally, melanin is metabolized by metabolism (turnover) of skin tissue, but a decrease in metabolism of skin tissue with aging also causes pigmentation.
本発明において使用されるマメ科オジギソウ属の植物またはその抽出物、例えばセンシティーヴァまたはその抽出物は、原産地ブラジルで煎剤又は入浴剤として使用されている安全性の高い素材である。センシティーヴァは、後述する実験例で示すように、メラニン合成に関わる酵素チロシナーゼに対して、阻害作用が知られているアルブチンよりも優れた阻害活性を示し、メラニン産生を抑制する作用を有する事から、美白（色素沈着やくすみの改善）作用を有する。このため、センシティーヴァはチロシナーゼ阻害剤、メラニン生成抑制剤、美白剤の有効成分として有用であるとともに、美白の効果を目的とする皮膚外用剤（美白外用剤）の有効成分として有用である。 Leguminosae plants or extracts thereof, such as Sensiva or extracts thereof, used in the present invention are highly safe materials used as a decoction or bathing agent in the country of origin Brazil. As shown in the experimental examples to be described later, Sensiva has an inhibitory activity superior to arbutin, which has an inhibitory effect on the enzyme tyrosinase involved in melanin synthesis, and has an action of suppressing melanin production. To whitening (improves pigmentation and dullness). For this reason, Sensiva is useful as an active ingredient of a tyrosinase inhibitor, a melanin production inhibitor, and a whitening agent, and is also useful as an active ingredient of a skin external preparation (whitening external preparation) for the purpose of whitening effect.
本発明のチロシナーゼ阻害剤、メラニン生成抑制剤、美白剤を含む美白外用剤は、安全で、優れた美白作用を有し、日焼け後の色素沈着、シミ、ソバカス、紅斑等の淡色化、くすみを目立たなくさせるなど、美肌効果を有し、健康な肌を維持できるため、特に美白化粧料、美肌化粧料、スキンケア化粧料などとして有用である。
A whitening external preparation containing a tyrosinase inhibitor, a melanin production inhibitor, and a whitening agent of the present invention is safe and has an excellent whitening action, and is capable of reducing pigmentation, blemishes, freckles, erythema and the like after sunburn. Since it has a beautifying effect such as making it inconspicuous and can maintain healthy skin, it is particularly useful as a whitening cosmetic, a beautiful skin cosmetic, a skin care cosmetic, and the like.
本発明において、チロシナーゼ阻害作用及び／又はメラニン産生抑制作用を有する有効成分は、マメ科オジギソウ属の植物に由来し、これら植物の抽出物が好ましく使用される。
マメ科オジギソウ属の植物としては、センシティーヴァ（Ｍｉｍｏｓａ ｐｕｄｉｃａ Ｌ．）、ミモザ・テニュイフローラ（ Ｍｉｍｏｓａ ｔｅｎｕｉｆｌｏｒａ）、マイヤラープ・ヤック（Ｍｉｍｏｓａ ｐｉｇｒａ）などが挙げられ、好ましくはセンシティーヴァが例示される。
In the present invention, the active ingredient having a tyrosinase inhibitory action and / or a melanin production inhibitory action is derived from a plant belonging to the genus Leguminosae, and extracts of these plants are preferably used.
Examples of the leguminous genus Genus include Sensiva (Mimosa pudicica L.), Mimosa tenuiflora (Mimosa tenuiflora), Miyarap yak (Mimosa pigra), etc., preferably Sensiva is exemplified. .
センシティーヴァ（学名：Ｍｉｍｏｓａ ｐｕｄｉｃａ、オジギソウ、ネムリグサ、ミモザ、含羞草、Ｓｅｎｓｉｔｉｖｅ ｐｌａｎｔ、Ａｃｔｉｏｎ ｐｌａｎｔ、Ｈｕｍｂｅｌ ｐｌａｎｔ、Ｓｈａｍｅ ｐｌａｎｔ、Ｔｏｕｃｈ−ｍｅ−ｎｏｔ、Ｌｉｖｅ−ａｎｄ−ｄｉｅ、Ｓｅｎｓｉｔｉｖａ、Ｄｏｒｍｉｄｅｉｒａ、Ｍａｌíｃｉаｄａｓ−ｍｕｌｈｅｒｅｓ、Ｊｕｑｕｉｒｉ、Ｖｅｒｇｏｎｈａなどとしても知られている）は、マメ科オジギソウ属に属し、南米を原産国とする多年草である。南米ではマリッシアとも呼ばれ、また、発音による表記の違いでメリッシア、メリッサなど表記されることがあるが、これらは同一の植物を指す。生理活性機能として、糖尿病の予防効果（Ｕｍａｍａｈｅｓｗａｒｉら, Ａｃｔａ ｐｏｌｏｎｉａｅ ｐｈａｒｍａｃｅｕｔｉｃａ ６４．１： ５３−６１， ２００７）、抗菌作用（ＡＫＴＥＲら, ｎｄｉａｎ ｊｏｕｒｎａｌ ｏｆ ｐｈａｒｍａｃｅｕｔｉｃａｌ ｓｃｉｅｎｃｅｓ ７２．３： ３８８， ２０１０）、創傷治癒（Ｋｏｋａｎｅら, Ｊｏｕｒｎａｌ ｏｆ Ｅｔｈｎｏｐｈａｒｍａｃｏｌｏｇｙ １２４．２： ３１１−３１５, ２００９）、コラーゲン産生促進作用（特許第３６２６７２７号）などが報告されているが、チロシナーゼ阻害活性による美白作用に関する報告はまだない。 Sensitiva (scientific names: Mimosa pudica, white mullet, Nemrigusa, mimosa, garlic, Sensitive plant, Action plant, Humbell plant, sham plant, ture-me-not-L, Mulheres, Juquiri, Vergonha, etc.) is a perennial that belongs to the genus Leguminosae and originates in South America. In South America, it is also called marissia, and there are cases where notation such as melissia, melissa, etc. is used depending on pronunciation, but these indicate the same plant. As a physiologically active function, diabetes prevention effect (Umaheswari et al., Acta polloniae pharmaceuticala 64.1: 53-61, 2007), antibacterial action (AKTER et al., Ndian journal of pharmaceutical 3 wounds, 38). Kokane et al., Journal of Ethnopharmacology 124.2: 311-315, 2009), collagen production promoting action (Japanese Patent No. 3626727), etc. have been reported, but there is no report on the whitening effect by tyrosinase inhibitory activity.
本発明で使用するマメ科オジギソウ属の植物（例えばセンシティーヴァ）の抽出物とは、該植物の葉、樹皮（茎ないし幹）、花、実、根等の植物体の一部又は全草／全植物体から抽出して得られるものである。植物がセンシティーヴァの場合、好ましくは葉、枝、根からの抽出物が好ましく例示される。抽出物の製造方法は特に限定されず、例えば、適当な抽出溶媒を用いて常温ないし加熱抽出したものが例示される。抽出溶媒としては、例えば、水、含水アルコール（例えば含水エタノール）、炭素数１〜４の低級アルコール（例えばメタノール、エタノール、ｎ-プロパノール、イソプロパノール）、アセトン、メチルエチルケトンなどのケトン類、酢酸エチルなどのエステル類、多価アルコール（エチレングリコール、１，３-ブチレングリコール、プロピレングリコール、グリセリン等）、テトラヒドロフラン、ジエチルエーテルなどのエーテル類、ヘキサンなどの有機溶媒が挙げられる。好ましくは、水、含水溶媒、或いは水混和性溶媒であり、特に好ましくは、水、エタノール、含水エタノールが挙げられる。含水エタノールの場合、エタノール濃度としては、制限されないものの、２０〜９０容量％、特に４０〜８０容量％を好適に挙げることができる。これらの溶媒は単独でも２種以上を混合して用いてもよい。
植物抽出物は、抽出した溶液のまま用いても良く、必要に応じて、濃縮、希釈、濾過等の処理をして用いてもよく、抽出液を蒸発乾固、噴霧乾燥、凍結乾燥等の処理を行い、乾燥物(粉末)として用いても良い。
The extract of the leguminous genus Euglena used in the present invention (for example, Sensiva) is a part of the plant body such as leaves, bark (stem or stem), flower, fruit, root, or whole plant of the plant. / It is obtained by extracting from the whole plant body. When the plant is Sensiva, extracts from leaves, branches and roots are preferably exemplified. The method for producing the extract is not particularly limited, and examples thereof include those extracted at normal temperature or heat using an appropriate extraction solvent. Examples of the extraction solvent include water, hydrous alcohol (eg, hydrous ethanol), lower alcohols having 1 to 4 carbon atoms (eg, methanol, ethanol, n-propanol, isopropanol), ketones such as acetone and methyl ethyl ketone, and ethyl acetate. Examples thereof include esters, polyhydric alcohols (ethylene glycol, 1,3-butylene glycol, propylene glycol, glycerin and the like), ethers such as tetrahydrofuran and diethyl ether, and organic solvents such as hexane. Water, a water-containing solvent, or a water-miscible solvent is preferable, and water, ethanol, and water-containing ethanol are particularly preferable. In the case of water-containing ethanol, although the ethanol concentration is not limited, 20 to 90% by volume, particularly 40 to 80% by volume can be preferably mentioned. These solvents may be used alone or in combination of two or more.
The plant extract may be used as it is in the extracted solution, and may be used after treatment such as concentration, dilution, filtration, etc. if necessary, and the extract may be evaporated to dryness, spray dried, freeze dried, etc. It may be processed and used as a dry product (powder).
本発明のチロシナーゼ阻害剤及び／又はメラニン産生抑制剤において、マメ科ネムノキ亜科の植物の抽出物の配合量は、メラニン生成抑制作用を有する限り特に制限されないが、乾燥換算として、０．０００１〜１００重量％、好ましくは０．００１〜５０重量％、より好ましくは０．０１〜２５重量％を挙げることができる。 In the tyrosinase inhibitor and / or melanin production inhibitor of the present invention, the blending amount of the plant leguminous plant belonging to the subfamily Lemaceae is not particularly limited as long as it has a melanin production inhibitory effect, but in terms of dryness, 0.0001 to 100% by weight, preferably 0.001 to 50% by weight, more preferably 0.01 to 25% by weight.
本発明のチロシナーゼ阻害剤及び／又はメラニン産生抑制剤は、メラニンの産生を抑制する作用を有し、美白剤の有効成分として、また美白の効果を目的とする化粧料の有効成分として、好適に使用することができる。 The tyrosinase inhibitor and / or melanin production inhibitor of the present invention has an action of suppressing the production of melanin, and is suitably used as an active ingredient of a whitening agent and as an active ingredient of a cosmetic for the purpose of a whitening effect. Can be used.
本発明の美白剤は、前述するチロシナーゼ及び／又はメラニン産生抑制剤を有効成分として含有することを特徴とする。当該美白剤に配合するメラニン生成抑制剤の割合は、チロシナーゼ及び／又はメラニン産生抑制剤のチロシナーゼ及び／又はメラニン産生抑作用に基づいて美白作用を有する限り特に制限されないが、通常、マメ科オジギソウ属の植物またはそれらの抽出物の配合量に換算して（乾燥物換算）、０．０００５〜２０重量％、好ましくは０．００１〜１０重量％、より好ましくは０．０１〜１重量％である。 The whitening agent of the present invention is characterized by containing the aforementioned tyrosinase and / or melanin production inhibitor as an active ingredient. The ratio of the melanin production inhibitor to be added to the whitening agent is not particularly limited as long as it has a whitening action based on the tyrosinase and / or melanin production inhibitory action of tyrosinase and / or melanin production. In terms of the amount of the plant or the extract thereof (in terms of dry matter), it is 0.0005 to 20% by weight, preferably 0.001 to 10% by weight, more preferably 0.01 to 1% by weight. .
本発明の美白剤は、その形態を特に問うものではなく、例えば粉末状、顆粒状、錠剤状、カプセル状などの固形製剤形態を有していてもよいし、また液状、懸濁液状、乳液状などの液状製剤形態を有していてもよい。 The form of the whitening agent of the present invention is not particularly limited. For example, the whitening agent may have a solid preparation form such as powder, granule, tablet, capsule or the like, and may be liquid, suspension, emulsion. You may have liquid formulation forms, such as a shape.
本発明の美白剤は、マメ科オジギソウ属の植物の抽出物のチロシナーゼ阻害活性に基づいて、メラニンの産生を抑制する作用を有するため、美白（シミやくすみの予防および低減を含む）を効果とする皮膚外用剤（美白外用剤）、特に美白化粧料の有効成分として、好適に使用することができる。 Since the whitening agent of the present invention has an action of suppressing the production of melanin based on the tyrosinase inhibitory activity of the plant leguminous plant extract, it is effective for whitening (including prevention and reduction of spots and dullness). It can be suitably used as an active ingredient in skin external preparations (whitening external preparations), particularly whitening cosmetics.
本発明の美白剤には、マメ科オジギソウ属の植物あるいはこれらの抽出物以外に、従来公知の美白剤を組み合わせて配合してもよい。また、通常、化粧料に用いられる成分、例えば、保湿剤、皮膜剤、酸化防止剤、油性成分、紫外線吸収剤、界面活性剤、増粘剤、アルコール類、粉末成分、色材、水性成分、水、各種皮膚栄養剤等を必要に応じて適宜配合することができる。 You may mix | blend conventionally well-known whitening agent with the whitening agent of this invention in combination with the plant of the leguminous genus Coleoptera or these extracts. In addition, components usually used in cosmetics, such as humectants, film agents, antioxidants, oily components, ultraviolet absorbers, surfactants, thickeners, alcohols, powder components, color materials, aqueous components, Water, various skin nutrients, and the like can be appropriately blended as necessary.
本発明の美白剤の剤型は、水溶液系、可溶化系、乳化系、粉末系、油液系、ゲル系、軟
膏系、エアゾール系、水−油２層系、および水−油−粉末３層系等、幅広い剤型を採るこ
とができる。例えば、その形態として、化粧液、乳液、クリーム、ジェル、美容液、パック、マスク等を挙げることができる。
The dosage forms of the whitening agent of the present invention are aqueous solution system, solubilization system, emulsification system, powder system, oil liquid system, gel system, ointment system, aerosol system, water-oil two-layer system, and water-oil-powder 3 A wide range of dosage forms such as layer systems can be adopted. For example, the cosmetic liquid, milky lotion, cream, gel, cosmetic liquid, pack, mask, etc. can be mentioned as the form.
また本発明の美白剤は、美白の効果を目的とする皮膚外用剤、特に化粧料の有効成分としても使用することができる。この場合の美白剤の皮膚外用剤（好ましくは化粧料）に対する配合割合としては、皮膚外用剤が美白効果を発揮する限り特に制限されないが、マメ科ミモザ属の植物またはそれらの抽出物の配合量に換算して（乾燥物換算）、０．０００５〜２０重量％、好ましくは０．００１〜１０重量％、より好ましくは０．０１〜１重量％を挙げることができる。皮膚外用剤の形態は特に制限されず、例えば皮膚外用剤が基礎化粧品である場合、その形態として、化粧水、乳液、クリーム、ジェル、エッセンス、美容液、パック、マスク等が挙げられる。また、皮膚外用剤がメークアップ化粧品であれば、その形態として、ファンデーション、口紅、頬紅、アイシャドウ、アイライナー、マスカラなどが挙げられる。その他の形態として、洗顔料、マッサージ用剤、クレンジング用剤、アフターシェーブローション、プレシェーブローション、シェービングクリーム、ボディソープ、ボディークリーム、石けん等を挙げることができる。 The whitening agent of the present invention can also be used as an external preparation for skin for the purpose of whitening, particularly as an active ingredient in cosmetics. In this case, the blending ratio of the whitening agent to the external preparation for skin (preferably cosmetic) is not particularly limited as long as the external preparation for skin exhibits a whitening effect, but the blending amount of leguminous mimosa plants or their extracts In terms of dry matter (in terms of dry matter), 0.0005 to 20% by weight, preferably 0.001 to 10% by weight, and more preferably 0.01 to 1% by weight. The form of the external preparation for skin is not particularly limited. For example, when the external preparation for skin is a basic cosmetic, examples of the form include lotion, milky lotion, cream, gel, essence, cosmetic liquid, pack, and mask. In addition, if the external preparation for skin is a makeup cosmetic, examples of the form include foundation, lipstick, blusher, eye shadow, eyeliner, mascara and the like. Other forms include facial cleansing agents, massage agents, cleansing agents, after-shave lotions, pre-shave lotions, shaving creams, body soaps, body creams, soaps and the like.
以下、本発明を実施例、試験例、および処方例により詳細に説明するが、これらの実施例等によって本発明は何ら限定されるものではない。 EXAMPLES Hereinafter, although an Example, a test example, and a formulation example demonstrate this invention in detail, this invention is not limited at all by these Examples.
（実施例1） センシティーヴァの含水エタノール抽出物の調製
乾燥した植物体５gに、８０容量％の含水エタノール（エタノール：精製水＝８：２（ｖ／ｖ））を５０ｍｌ加え、室温で１晩振とう混和した。その後、回転数３，０００ ｒｐｍで１５分間遠心分離し上清を得た。得られた上清をロータリーエバポレーターに供し、エタノールをある程度除いた後に、凍結乾燥し含水エタノール抽出物（５２７ ｍｇ）を得た。
(Example 1) Preparation of hydrous ethanol extract of Sensiva 50 ml of 80% by volume of hydrous ethanol (ethanol: purified water = 8: 2 (v / v)) was added to 5 g of the dried plant body, and 1 at room temperature. Mixed with shaking overnight. Thereafter, the mixture was centrifuged at 3,000 rpm for 15 minutes to obtain a supernatant. The obtained supernatant was subjected to a rotary evaporator to remove ethanol to some extent and then freeze-dried to obtain a hydrous ethanol extract (527 mg).
（試験例1） チロシナーゼ阻害活性の測定
実施例１で調製したセンシティーヴァ抽出物を試験試料として、次の方法でチロシナーゼ阻害活性を測定した。
（１）試験方法
９６ウェルプレートに、２０ ｎｇ／ｍｌ ＭＳＨ ／ ＤＭＥＭ培地（ギブコ社）に懸濁したマウスメラノーマＢ１６細胞を５×１０３ ｃｅｌｌｓ／ウェルの割合で播種し、３７℃、５％ＣＯ２の条件下で24時間インキュベートした。その後、被験試料としてセンシティーヴァ抽出物、アルブチン、コントロールとして溶媒（ＤＭＳＯ）を加え、３７℃、５％ＣＯ２の条件下で３日間培養した。培養後、上清を除去し、ＰＢＳでウェルを洗浄後、１％ＴＲＩＴＯＮ ／ ＰＢＳ溶液、１．９７ｍｇ／ｍｌ Ｌ−ＤＯＰＡを９：１の割合で添加し、添加０、１時間後のＡｂｓ４９２を測定した。
(Test Example 1) Measurement of Tyrosinase Inhibitory Activity Tyrosinase inhibitory activity was measured by the following method using the Sensiva extract prepared in Example 1 as a test sample.
(1) Test Method Mouse melanoma B16 cells suspended in 20 ng / ml MSH / DMEM medium (Gibco) were seeded in a 96-well plate at a rate of 5 × 10 3 cells / well, 37 ° C., 5% CO Incubated for 24 hours under 2 conditions. Thereafter, Sensiva extract and arbutin as a test sample and a solvent (DMSO) as a control were added, and the cells were cultured at 37 ° C. under 5% CO 2 for 3 days. After culturing, the supernatant was removed, the wells were washed with PBS, 1% TRITON / PBS solution, 1.97 mg / ml L-DOPA was added at a ratio of 9: 1, and Abs492 after 1 hour was added. It was measured.
チロシナーゼ阻害活性（％）を下記の計算式より導き、得られた阻害活性（％）から各
被験試料のＩＣ５０を求めた。
The tyrosinase inhibitory activity (%) was derived from the following formula, and the IC50 of each test sample was determined from the obtained inhibitory activity (%).
（数１）
チロシナーゼ阻害活性（％）=（［測定値］Ｂ−［測定値］Ｓ）／［測定値］Ｂ×１００
［測定値］Ｂ：コントロール測定値（１時間）―コントロール測定値（０時間）
［測定値］Ｓ：被験試料測定値（１時間）―被験試料測定値（０時間）
(Equation 1)
Tyrosinase inhibitory activity (%) = ([measured value] B− [measured value] S ) / [measured value] B × 100
[Measured value] B : Control measured value (1 hour)-Control measured value (0 hour)
[Measured value] S : Test sample measurement value (1 hour)-Test sample measurement value (0 hour)
（２）試験結果
各被験試料のＩＣ５０値を表１に示す。
(2) Test result Table 1 shows the IC50 value of each test sample.
上記の結果から、本発明のセンシティーヴァ抽出物は、
美白剤として一般的に使用されているアルブチンより強いチロシナーゼ阻害活性を有することが明らかになった。
From the above results, the Sensiva extract of the present invention is
It became clear that it has stronger tyrosinase inhibitory activity than arbutin which is generally used as a whitening agent.
（試験例２） 細胞のメラニン産生に対する抑制作用
実施例１で調製したセンシティーヴァ抽出物を試験試料として、メラニン生成抑制作用を測定した。
（１）試験方法
細胞培養用１０ｃｍディッシュに、ＤＭＥＭ培地（ギブコ社）に懸濁したマウスメラノーマＢ１６細胞を３×１０５ ｃｅｌｌｓ播種し、３７℃、５％ＣＯ２の条件下で２４時間インキュベートした。その後、被験試料としてセンシティーヴァ抽出物、アルブチン、コントロールとして溶媒（ＤＭＳＯ）を加え、３７℃、５％ＣＯ２の条件下で３日間培養した。培養後、上清を除去し、ＰＢＳでウェルを洗浄後、トリプシン-ＥＤＴＡ溶液（ギブコ社）を加えて細胞を剥離させ、得られた細胞懸濁液をチューブに回収した。得られた細胞懸濁液のうち２０μｌをＣｅｌｌＴｉｔｅｒ−Ｇｌｏキット（プロメガ社）を用いた生存細胞測定に供した。
細胞懸濁液を回収したチューブを１５，０００ｒｐｍにて１０分間遠心し、細胞をチューブの底に集積した後、上清を除いた。細胞数に対応する量の１Ｎ ＮａＯＨを加え、９５℃で６０分間インキュベートしてメラニンを抽出し、写真を撮影後４０５ ｎｍの吸光度を測定し、測定値（被験試料測定値、コントロール測定値）とした。同時に１Ｎ ＮａＯＨの吸光度を測定し、バックグラウンド値とした。
(Test Example 2) Inhibitory Action on Cell Melanin Production Using the Sensiva extract prepared in Example 1 as a test sample, the melanin production inhibitory action was measured.
(1) Test method Mouse melanoma B16 cells suspended in DMEM medium (Gibco) were seeded in 10 cm dishes for cell culture at 3 × 10 5 cells and incubated at 37 ° C. under 5% CO 2 for 24 hours. . Thereafter, Sensiva extract and arbutin as a test sample and a solvent (DMSO) as a control were added, and the cells were cultured at 37 ° C. under 5% CO 2 for 3 days. After culturing, the supernatant was removed, the wells were washed with PBS, trypsin-EDTA solution (Gibco) was added to detach the cells, and the resulting cell suspension was collected in a tube. 20 μl of the obtained cell suspension was subjected to viable cell measurement using CellTiter-Glo kit (Promega).
The tube from which the cell suspension was collected was centrifuged at 15,000 rpm for 10 minutes to accumulate the cells at the bottom of the tube, and then the supernatant was removed. Add 1N NaOH in an amount corresponding to the number of cells, incubate at 95 ° C. for 60 minutes to extract melanin, measure the absorbance at 405 nm after taking a photograph, and measure values (test sample measured values, control measured values) did. Simultaneously, the absorbance of 1N NaOH was measured and used as a background value.
得られた測定値から、下式を用いて、各被験試料およびコントロールについてメラニン産生抑制率（％）を求めた。
（数２）
メラニン生成抑制率（％）＝
｛（コントロールの吸光度−被験試料の吸光度）／コントロールの吸光度 ｝× １００
被験試料の吸光度：被験試料測定値−バックグラウンド値
コントロールの吸光度：コントロール測定値−バックグラウンド値
From the measured values obtained, the melanin production inhibition rate (%) was determined for each test sample and control using the following formula.
(Equation 2)
Melanin production inhibition rate (%) =
{(Absorbance of control−absorbance of test sample) / absorbance of control} × 100
Absorbance of test sample: measured value of test sample-background value
Absorbance of control: Control measurement value-background value
（２）試験結果
結果を表２に示す。
(2) The test results are shown in Table 2.
上記の結果から、本発明のセンシティーヴァ抽出物は、メラニン生成抑制作用を有することが明らかになった。このことから、これらセンシティーヴァ抽出物はメラニン生成抑制作用に基づいて、メラニン生成抑制剤として、また美白剤、および美白を効果とする化粧料の有効成分として有用であると考えられる。 From the above results, it was revealed that the Sensiva extract of the present invention has a melanin production inhibitory action. From these facts, these Sensiva extracts are considered useful as melanin production inhibitors and as whitening agents and active ingredients of cosmetics that have whitening effects, based on the melanin production inhibitory action.
処方例１：化粧水形態を有する美白剤
以下の表３に示される各成分を用い、常法に従い化粧水形態を有する美白剤を調製した。
Formulation Example 1: Whitening agent having skin lotion form Using each component shown in Table 3 below, a whitening agent having a skin lotion form was prepared according to a conventional method.
処方例２：美容液形態を有する美白剤
以下の表５に示される各成分を用い、常法に従い美容液形態を有する美白剤を製造した。
Formulation Example 2: Whitening agent having a cosmetic liquid form Using each of the components shown in Table 5 below, a whitening agent having a cosmetic liquid form was produced according to a conventional method.
処方例３：乳液形態を有する美白剤
以下の表５に示される各成分を用い、常法に従い乳液を製造した。
Formulation Example 3: Whitening agent having emulsion form An emulsion was prepared according to a conventional method using each component shown in Table 5 below.
処方例４：クリーム形態を有する美白剤
以下の表６に示される各成分を用い、常法に従いクリームを製造した。
Formulation Example 4: Whitening Agent with Cream Form A cream was produced according to a conventional method using each component shown in Table 6 below.
処方例５：バスソルト形態を有する美白剤
以下の表７に示される各成分を用い、常法に従いバスソルトを製造した。
Formulation example 5: Whitening agent which has bath salt form Bath salt was manufactured according to the conventional method using each component shown in the following Table 7.
処方例６：茶葉
センシティーヴァの葉を必要に応じて滅菌加工をした後、短冊状、刻み状、粉末あるいは顆粒に粉砕加工した後、大袋、ティーパック、スティックあるいは三方シールに充填し包装した。また、滅菌処理後に焙煎工程を加えてもよい。
処方例７：錠剤
以下の表８に示される各成分を用い、常法に従い錠剤を製造した。
Formulation Example 6: After sterilizing tea leaf sensiva leaves as necessary, pulverized into strips, chops, powders or granules, filled into large bags, tea packs, sticks or three-way seals and packaged . Moreover, you may add a roasting process after a sterilization process.
Formulation Example 7: Tablet Tablets were produced according to a conventional method using the components shown in Table 8 below.
処方例８：カプセル剤
以下常法に従い、表９に示される各成分を混合し、カプセルに充填し、カプセル製剤を得た。
Formulation Example 8: Capsule According to a conventional method, each component shown in Table 9 was mixed and filled into a capsule to obtain a capsule preparation.
Claims (5)
The skin external preparation formed by mix | blending Claims 1-4.
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