JP2009203182A - Hyaluronidase inhibitor, and composition comprising the same - Google Patents
Hyaluronidase inhibitor, and composition comprising the same Download PDFInfo
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本発明はニキビなどの炎症の予防又は改善に有用なヒアルロニダーゼ阻害剤及びそれを含有する食品などの組成物に関する。 The present invention relates to a hyaluronidase inhibitor useful for preventing or ameliorating inflammation such as acne and a composition such as a food containing the same.
昔から植物には様々な作用があり、生薬として怪我や病気の治療に利用されてきた。生薬として治療に用いられる際には、主に伝統的に有用とされる植物の種、葉、花、根などを煎じて飲用したり、患部に直接植物のエキスを塗布するなど様々な形で用いられてきた。 Plants have a variety of effects and have been used as a herbal medicine to treat injuries and diseases. When used as a crude drug for treatment, it is mainly used in various forms such as decocting and drinking plant seeds, leaves, flowers, roots, etc. that are traditionally useful, and applying plant extracts directly to the affected area. Has been used.
生薬は医食同源の考え方に基づき、日頃から摂取することで免疫力を向上させ、病気にならないよう予防的に用いられるもの、治療に用いられるもの等様々な目的で使用されてきた。特に近年では、生薬が抗炎症作用や抗HIV活性をもつこと、癌の治療に有用であることなどが報告されている(例えば、特許文献1、特許文献2及び非特許文献1を参照)。 Herbal medicines have been used for a variety of purposes, such as those used prophylactically to prevent illness and those used for treatment, based on the concept of medical foods, improving daily immunity by ingestion. Particularly in recent years, it has been reported that herbal medicines have anti-inflammatory action and anti-HIV activity and are useful for cancer treatment (see, for example, Patent Document 1, Patent Document 2, and Non-Patent Document 1).
特に甘草はグリチルリチン酸塩を含有し、抗炎症作用があることが知られており、全身性の炎症、皮膚疾患に利用されている他、食品の甘味料やフレーバーとして食品添加物として用いられ非常に汎用されている生薬のひとつである(例えば、特許文献3及び非特許文献2を参照)。また、このものを含有するニキビ用の食品(例えば、特許文献4を参照)もすでに知られている。 In particular, licorice contains glycyrrhizinate and is known to have anti-inflammatory activity, and is used for systemic inflammation and skin diseases. It is also used as a food additive as a food sweetener and flavor. Is one of the herbal medicines widely used (see, for example, Patent Document 3 and Non-Patent Document 2). In addition, foods for acne containing this are already known (for example, see Patent Document 4).
甘草はGlychyrrhiza 属の植物で、Glychyrrhiza uralensisが主に用いられている他、Glychyrrhiza glabra、Glychyrrhiza inflataなどの種類があり、これらの抽出物からキサンチンオキシダーゼ阻害やモノアミンオキダーゼ阻害活性成分として、フェノール性成分が報告されている(例えば、非特許文献3を参照)。その他の作用として、抗酸化活性についても知られている(例えば、特許文献5を参照) Licorice is a plant belonging to the genus Glychyrrhiza, and Glychyrrhiza uralensis is mainly used. Has been reported (for example, see Non-Patent Document 3). As other actions, it is also known about antioxidant activity (see, for example, Patent Document 5).
さらに、Glychyrrhiza uralensisについては、有用な成分として、Licorice-saponinsD3, E2, F3, G2, H2, J2, K2等のオレアノンタイプのトリテルペンオリゴグルコシドが知られている(例えば、非特許文献4を参照)。しかしながら、Glychyrrhiza glabra、Glychyrrhiza inflataについては、知見が少なく、有効成分や有効性に関して明らかにされていない。 Furthermore, for Glychyrrhiza uralensis, oleanone-type triterpene oligoglucosides such as Licorice-saponins D3, E2, F3, G2, H2, J2, and K2 are known as useful components (see, for example, Non-Patent Document 4). ). However, there is little knowledge about Glychyrrhiza glabra and Glychyrrhiza inflata, and the active ingredient and effectiveness are not clarified.
一方、ニキビといった炎症を伴う肌の悩みに対しては、亜鉛を経口摂取することで改善効果があるとの報告があるものの、亜鉛摂取により銅の体内からの***が促進されるため、亜鉛摂取時には銅を亜鉛摂取量の10分の1量を摂取することが亜鉛摂取には有用であることが知られている(特許文献6)。また、ニキビの改善には亜鉛の摂取に加えて、ビタミンB群を摂取することで、皮脂分泌の抑制、ホルモンバランスの調整作用が期待できるとの報告もある(特許文献6)。 On the other hand, although there is a report that it is effective to take zinc orally for skin troubles accompanied by inflammation such as acne, since the excretion of copper from the body is promoted by zinc intake, zinc intake It is known that sometimes taking copper one-tenth of zinc intake is useful for zinc intake (Patent Document 6). There is also a report that acne can be improved by suppressing the sebum secretion and adjusting the hormone balance by ingesting vitamin B group in addition to ingestion of zinc (Patent Document 6).
また、近年皮膚における炎症を抑制する成分の探索方法として、ヒアルロニダーゼ阻害作用を指標とするものが比較的多く報告されるようになってきた。しかしながら、甘草特にGlychyrrhiza glabra、Glychyrrhiza inflataについて、そのエキスあるいはエキス中の特定の化合物に強いヒアルロニダーゼ阻害作用を有すことは知られていなかった。さらに、甘草中のLicorice-saponinH2が非常に高いヒアルロニダーゼ阻害活性があり、従来から報告されている甘草中の抗炎症作用成分グリチルリチン酸と比べても強い活性化合物であるとの報告はなく、このようなヒアルロニダーゼ阻害活性効果を期待した、食品組成物などの経口投与組成物として用いられることはなかった。当然、肌荒れ、ニキビなどの炎症を伴う肌の悩みの予防や治療に甘草中のLicorice-saponinH2が有用であることは全く知られていなかった。 In recent years, relatively many methods for searching for a component that suppresses inflammation in the skin have been reported using hyaluronidase inhibitory action as an index. However, it has not been known that licorice, especially Glychyrrhiza glabra and Glychyrrhiza inflata, has a strong hyaluronidase inhibitory action on the extract or on specific compounds in the extract. Furthermore, Licorice-saponin H2 in licorice has a very high hyaluronidase inhibitory activity, and there is no report that it is a strong active compound compared with the anti-inflammatory activity component glycyrrhizic acid in licorice that has been reported so far. Therefore, it was never used as a composition for oral administration such as a food composition, which expected a hyaluronidase inhibitory activity effect. Naturally, Licorice-saponinH2 in licorice was not known to be useful for the prevention and treatment of skin problems accompanied by inflammation such as rough skin and acne.
本発明は、この様な状況下為されたものであり、優れたヒアルロニダーゼ阻害作用を有し、ニキビなどの予防、改善に有用な素材及びそれを含有する食品組成物提供することを課題とする。 The present invention has been made under such circumstances, and an object thereof is to provide a material having an excellent hyaluronidase inhibitory action and useful for preventing and improving acne and a food composition containing the same. .
この様な実状に鑑みて、本発明者らは、ニキビなどの炎症抑制に有用な素材を求めて、鋭意研究努力を重ねた結果、ヒアルロニダーゼ阻害作用に優れる成分が、このような効果に優れることを見いだした。更に検討を重ねた結果、このような成分として、甘草の抽出物中に含有されるLicorice-saponinH2を見いだし、発明を完成させるに至った。即ち、本発明は、以下に示すとおりである。
(1) Licorice-saponinH2及び/又はその塩からなるヒアルロニダーゼ阻害剤。
(2) 抗炎症効果を有することを特徴とする、(1)に記載のヒアルロニダーゼ阻害剤。
(3) 前記炎症は、ニキビによるものであることを特徴とする、(1)又は(2)に記載のヒアルロニダーゼ阻害剤。
(4) (1)〜(3)いずれか1項に記載のヒアルロニダーゼ阻害剤の基源がGlychyrrhiza 属の植物を水を含んでも良い親水性有機溶媒で抽出したエキスであることを特徴とする、ヒアルロニダーゼ阻害剤
(5) 前記Glychyrrhiza 属の植物がGlychyrrhiza glabraであることを特徴とする(4)記載のヒアルロニダーゼ阻害剤
(6) (1)〜(5)いずれか1項に記載のヒアルロニダーゼ阻害剤を含有する、ニキビ用の食品組成物。
(7)更に、グルコン酸亜鉛及びグルコン酸銅を含有することを特徴とする、(6)項に記載のニキビ用の食品組成物。
(8)更にビタミンB群を含有することを特徴とする、(6)又は(7)に記載のニキビ用の食品組成物。
(9)前記ビタミンB群がビタミンB2及び/又はビタミンB6であることを特徴とする、(8)のニキビ用の食品組成物。
In view of such a situation, the present inventors have sought for a material useful for suppressing inflammation such as acne, and as a result of intensive research efforts, a component excellent in hyaluronidase inhibitory action is excellent in such an effect. I found. As a result of further studies, Licorice-saponinH2 contained in the licorice extract was found as such a component, and the present invention was completed. That is, the present invention is as follows.
(1) A hyaluronidase inhibitor comprising Licorice-saponinH2 and / or a salt thereof.
(2) The hyaluronidase inhibitor according to (1), which has an anti-inflammatory effect.
(3) The hyaluronidase inhibitor according to (1) or (2), wherein the inflammation is caused by acne.
(4) The hyaluronidase inhibitor base source according to any one of (1) to (3) is an extract obtained by extracting a plant of the genus Glychyrrhiza with a hydrophilic organic solvent that may contain water, Hyaluronidase inhibitor (5) The hyaluronidase inhibitor according to any one of (4) to (5), wherein the plant belonging to the genus Glychyrrhiza is Glychyrrhiza glabra. A food composition for acne containing.
(7) The acetic acid food composition according to (6), further comprising zinc gluconate and copper gluconate.
(8) The food composition for acne according to (6) or (7), further comprising vitamin B group.
(9) The acne food composition for (8), wherein the vitamin B group is vitamin B2 and / or vitamin B6.
本発明によれば、優れたヒアルロニダーゼ阻害作用を有し、ニキビなどの予防、改善に有用な素材及びそれを含有する食品組成物提供することができる。 ADVANTAGE OF THE INVENTION According to this invention, it has the outstanding hyaluronidase inhibitory effect and can provide the raw material useful for prevention and improvement of acne etc., and the food composition containing it.
<1>本発明のヒアルロニダーゼ阻害剤
本発明のヒアルロニダーゼ阻害剤は、Licorice-saponinH2及び/又はその塩からなることを特徴とする。Licorice-saponinH2は甘草中に0.01〜2.00質量%含有されており、これをエタノールなどの親水性有機溶媒で抽出することにより、得ることができる。このような抽出は、例えば、甘草の全草、取り分け根茎部を、所望により乾燥させた後、細切し、親水性有機溶媒単独あるいは水を含有した親水性有機溶媒を植物体の1〜20質量倍加え、室温であれば数日間、沸点付近の温度であれば数時間から12時間程度浸漬すればよい。場合により攪拌を加えてもよい。冷却後、必要に応じて濾過などで不溶物を除去し、減圧濃縮などを行うことにより抽出物は製造される。本発明のLicorice-saponinH2は、このような抽出物を更に分画することによって濃縮し、分画濃縮物として組成物中へ含有させることもできるし、該分画濃縮物を更にカラム等を用いて精製し、Licorice-saponinH2を単離して用いることもできる。Licorice-saponinH2はそのまま用いることもできるし、アルカリを反応させて塩となし利用することもできる。塩としては、例えば、ナトリウム塩、カリウム塩などのアルカリ金属塩、カルシウム塩、マグネシウム塩などのアルカリ土類金属塩、アンモニウム塩、トリエチルアミン塩、モルフォリン塩等の有機アミン塩、アルギニン塩、リシン塩などの塩基性アミノ酸塩などが好適に例示できる。かかるLicorice-saponinH2は後記に示すように優れたヒアルロニダーゼ阻害作用を有し、これに基づいて抗炎症効果を発現する。このような抗炎症効果はニキビに付随する炎症に対して特に顕著な予防、改善効果を示す。
このような本発明のヒアルロニダーゼ阻害剤の基源となる、甘草、即ち、Glychyrrhiza 属の植物としては、Glychyrrhiza uralensis、Glychyrrhiza glabra、Glychyrrhiza inflataが例示でき、Glychyrrhiza glabraが好ましい。かかる甘草において、植物全体を用いてエキスを抽出することも出来るが、有効成分であるLicorice-saponinH2を多く含む部位としては根茎部が好ましく例示できる。
<1> Hyaluronidase inhibitor of the present invention The hyaluronidase inhibitor of the present invention is characterized by comprising Licorice-saponinH2 and / or a salt thereof. Licorice-saponinH2 is contained in licorice in an amount of 0.01 to 2.00% by mass and can be obtained by extracting it with a hydrophilic organic solvent such as ethanol. Such extraction is performed by, for example, drying the whole licorice plant, especially the rhizome part, if desired, and then chopping it, and using the hydrophilic organic solvent alone or water-containing hydrophilic organic solvent 1 to 20 of the plant body. Addition of mass times, it is sufficient to immerse for several days at room temperature, and for several hours to 12 hours at temperatures near the boiling point. In some cases, stirring may be added. After cooling, the extract is produced by removing insoluble matters by filtration or the like, if necessary, and concentrating under reduced pressure. The Licorice-saponin H2 of the present invention is concentrated by further fractionating such an extract, and can be contained in the composition as a fraction concentrate, and the fraction concentrate is further used in a column or the like. Licorice-saponinH2 can be isolated and used. Licorice-saponinH2 can be used as it is, or it can be used as a salt by reacting with alkali. Examples of the salt include alkali metal salts such as sodium salt and potassium salt, alkaline earth metal salts such as calcium salt and magnesium salt, organic amine salts such as ammonium salt, triethylamine salt and morpholine salt, arginine salt and lysine salt. Preferred examples include basic amino acid salts such as Such Licorice-saponinH2 has an excellent hyaluronidase inhibitory action as described later, and develops an anti-inflammatory effect based on this. Such an anti-inflammatory effect has a particularly remarkable preventive and ameliorating effect on inflammation associated with acne.
Glychyrrhiza uralensis, Glychyrrhiza glabra, and Glychyrrhiza inflata can be exemplified as a licorice, that is, a plant belonging to the genus Glychyrrhiza, which is a base source for the hyaluronidase inhibitor of the present invention, and Glychyrrhiza glabra is preferable. In such licorice, an extract can be extracted using the whole plant, but a rhizome part is preferably exemplified as a site containing a large amount of the active ingredient Licorice-saponinH2.
甘草より、Licorice-saponinH2を抽出濃縮する過程について更に詳細に説明する。
前記有効成分を前記のGlychyrrhiza 属の植物から抽出する溶媒としては、極性溶媒を用いることが出来、水、低級脂肪族アルコール、中極性溶媒等が例示でき、中極性溶媒は水に任意の割合で混じらない中極性溶媒が例示でき、酢酸エチル、ギ酸メチルが好適に例示できる。これらの溶媒を組み合わせても良い。このうち、人での摂取を考慮すると好ましくはエタノールが例示でき、さらに好ましくは水とエタノールの混液による抽出が例示できる。この際の混液の割合としては10〜90%(v/v)のエタノール水溶液とすることが例示できるが、好ましくは30〜90%である。さらに好ましくは50〜90%の割合としエタノール含有量を増やした抽出がよい。これらの抽出溶媒に前記植物を1−30質量%好ましくは5−15%の割合で加え、10分から24時間、操作の短縮を考え、好ましくは4時間程度撹拌する。その際の抽出温度は室温から100度で行うことが出来る。溶媒と植物体を撹拌抽出後、市販の濾紙を用いて濾過し、濾液を得る濾液はそのまま皮膚に適用したり、飲用可能である。好ましくはこの濾液を濃縮乾固して、これを食品組成物等の経口組成物に含有させて、使用することが好ましい。
The process of extracting and concentrating Licorice-saponinH2 from licorice will be described in more detail.
As the solvent for extracting the active ingredient from the plant of the genus Glychyrrhiza, a polar solvent can be used, and examples thereof include water, lower aliphatic alcohols, medium polar solvents, and the like. Non-mixed medium polar solvents can be exemplified, and ethyl acetate and methyl formate can be suitably exemplified. These solvents may be combined. Among these, taking into account human ingestion, ethanol can be exemplified, and extraction with a mixture of water and ethanol is more preferred. The ratio of the mixed liquid at this time can be exemplified by an ethanol aqueous solution of 10 to 90% (v / v), preferably 30 to 90%. More preferably, extraction with a ratio of 50 to 90% and increased ethanol content is preferable. The plant is added to these extraction solvents in a proportion of 1-30% by mass, preferably 5-15%, and the operation is shortened for 10 minutes to 24 hours, and the mixture is preferably stirred for about 4 hours. The extraction temperature at that time can be performed from room temperature to 100 degrees. The solvent and the plant body are stirred and extracted, and then filtered using a commercially available filter paper to obtain a filtrate. The filtrate can be applied to the skin as it is or can be drunk. Preferably, the filtrate is concentrated to dryness, and this is contained in an oral composition such as a food composition for use.
本発明の組成物は、経口組成物であり、食品組成物に好適に適用される。
前記の抽出物を経口組成物として使用する場合には、前記で抽出濾液あるいは乾固物特段の限定無く適用できる。このとき、前記抽出物、抽出分画物ないしは抽出精製物は、それらにおけるLicorice-saponinH2及びその塩の含有量が、食品組成物に対して0.05質量%〜5質量%になるように含有させることが、前記ヒアルロニダーゼ阻害作用をより顕著に発現するためには、好ましい。通常の甘草の抽出物を含有させた場合、Licorice-saponinH2及びその塩の含有量は0.001質量%〜0.05質量%であり、前記ヒアルロニダーゼ阻害作用を奏しない場合が存する。このため、前述のごとくに分画、精製を行うことがより好ましい。例えば、特定保健用食品などを包含する食品組成物 、医薬組成物 などとして使用することが例示でき、食品組成物 に適用することが特に好ましい。さらに、グルコン酸銅、グルコン酸亜鉛は市販のものを使用することが出来、フソウ株式会社から発売されている「グルコン酸銅」、「グルコン酸銅」が好適に例示できる。また、グルコン酸銅はグルコン酸を塩化銅を塩交換により製造できるし、グルコン酸亜鉛はグルクロノラクトンと酸化亜鉛を水性担体中で加熱し、開環させて製造することも出来る。グルコン酸銅、グルコン酸亜鉛の割合は、1:100から1:10の質量比で混合して配合することが好ましいが、さらに好ましくは1:20から1:10が例示できる。これに加えてビタミンB群を経口組成物に加えることが好ましく、ビタミンB群としては、市販のビタミンB2、ビタミンB6,ビタミンB12が例示でき、好ましくはビタミンB2、ビタミンB6を配合することが例示できる。また、ビタミンB群の分解を防ぐため、油脂によりコートすることが好ましく、コートする油脂としては、菜種、パーム、ヤシ、大豆等を原料とした植物硬化油脂、カルナバロウ等の油脂が例示できるが、菜種油を油脂としてビタミンBにコートすることが更に好ましい。油脂コートはビタミンをヘンシェルミキサーに入れて90℃程度で溶解させた菜種硬化油を加え、低速で撹拌することで製造できる。また、市販のものとしてVB6-MC70R、VB2-MC70R(日本油脂株式会社製)を用いることも出来る。もちろん本発明の食品組成物には、勿論、上記成分以外の製剤上の任意成分を含有することができる。かかる任意成分としては、例えば、砂糖、でんぷん、結晶セルロース、乳糖などの賦形剤、アラビアゴム、ヒドロキシプロピルセルロースなどの結合剤、POE硬化ひまし油などの乳化・分散剤、嬌味嬌臭剤、着色剤などが好適に例示できる。これらの必須成分、好ましい成分、任意成分を常法に従って処理することより、本発明の食品組成物は製造できる。食品組成物としては、例えば、スープ、麺類などの通常の食品はもとより、キャンディー、グミ、クッキーなどの菓子類、ジュース、ドリンクなどの飲料、錠剤、散剤、顆粒剤などの、機能性を訴求した食品などが好ましく例示できる。
The composition of the present invention is an oral composition and is suitably applied to a food composition.
When the above extract is used as an oral composition, it can be applied without any particular limitation on the extract filtrate or dry solid. At this time, the extract, extract fraction or extract purified product should be contained so that the content of Licorice-saponinH2 and the salt thereof is 0.05% by mass to 5% by mass with respect to the food composition. However, it is preferable in order to more significantly express the hyaluronidase inhibitory action. When a normal licorice extract is contained, the content of Licorice-saponinH2 and its salt is 0.001% by mass to 0.05% by mass, and there is a case where the hyaluronidase inhibitory action is not achieved. For this reason, it is more preferable to perform fractionation and purification as described above. For example, it can be exemplified as a food composition including a food for specified health use, a pharmaceutical composition and the like, and it is particularly preferable to apply to a food composition. Furthermore, commercially available copper gluconate and zinc gluconate can be used, and examples thereof include “copper gluconate” and “copper gluconate” sold by Fuso Corporation. Further, copper gluconate can be produced by salt exchange of gluconic acid and copper chloride, and zinc gluconate can be produced by heating glucuronolactone and zinc oxide in an aqueous carrier to cause ring opening. The ratio of copper gluconate and zinc gluconate is preferably mixed and blended at a mass ratio of 1: 100 to 1:10, more preferably 1:20 to 1:10. In addition to this, it is preferable to add vitamin B group to the oral composition, and examples of vitamin B group include commercially available vitamin B2, vitamin B6, and vitamin B12, preferably including vitamin B2 and vitamin B6 it can. In addition, in order to prevent the decomposition of the vitamin B group, it is preferable to coat with fats and oils, and examples of the fats and oils to be coated include oils and fats such as rapeseed, palm, palm, soybean, etc. More preferably, rapeseed oil is coated as an oil on vitamin B. The oil coat can be produced by adding rapeseed hardened oil in which vitamins are put in a Henschel mixer and dissolved at about 90 ° C., and stirring at low speed. Moreover, VB6-MC70R and VB2-MC70R (made by NOF Corporation) can also be used as a commercially available thing. Of course, the food composition of the present invention can of course contain optional ingredients on the preparation other than the above ingredients. Such optional components include, for example, excipients such as sugar, starch, crystalline cellulose, and lactose, binders such as gum arabic and hydroxypropyl cellulose, emulsifying / dispersing agents such as POE hydrogenated castor oil, miso odorants, coloring An agent etc. can be illustrated suitably. The food composition of the present invention can be produced by treating these essential components, preferred components, and optional components according to a conventional method. As a food composition, for example, not only ordinary foods such as soups and noodles, but also confectionery such as candies, gummi and cookies, beverages such as juices and drinks, tablets, powders, granules, etc. Preferred examples include foods.
以下に、実施例を挙げて、本発明について更に詳細に説明を加えるが、本発明がかかる実施例にのみに限定されないことは言うまでもない。 Hereinafter, the present invention will be described in more detail with reference to examples, but it goes without saying that the present invention is not limited to such examples.
<製造例1>
Glychyrrhiza uralensis、Glychyrrhiza glabra、Glychyrrhiza inflataの根茎部1Kgを細切し、70%エタノール水溶液 10Lにて24時間浸漬後、濾紙(5A ADVANTEC製)にて濾過し、濾液を得た。濾液の一部を採取しHPLC(ポンプ:
型番515、オートサンプラー:717、UV検出器:486: Waters製)にて有効成分Licorice-saponinH2、glycrrcizin, licochalconeA, glabridinの含有率を測定した。詳細なHPLC測定条件は、カラムはTSKgel ODS-80TsQA(内径4.6mm×長さ25cm東ソー製)、移動層にはアセトニトリルと水、酢酸の混液(40:55:5 または20:75:5)、流速1.2mL/min、検出UV254nmの条件である。結果を表1に示す。この結果からGlychyrrhiza glabraに他の種に比べてLicorice-saponinH2が多く含まれていることがわかる。
<Production Example 1>
Glychyrrhiza uralensis, Glychyrrhiza glabra and Glychyrrhiza inflata 1Kg of rhizome were cut into pieces, soaked in 10 L of 70% ethanol aqueous solution for 24 hours, and filtered through filter paper (5A ADVANTEC) to obtain a filtrate. A portion of the filtrate is collected and HPLC (pump:
The content of the active ingredients Licorice-saponinH2, glycrrcizin, licochalconeA, glabridin was measured using a model number 515, an autosampler: 717, a UV detector: 486 (manufactured by Waters). Detailed HPLC measurement conditions are as follows: TSKgel ODS-80TsQA column (4.6 mm inner diameter x 25 cm length manufactured by Tosoh Corporation), acetonitrile / water / acetic acid mixture (40: 55: 5 or 20: 75: 5) in the moving bed, The conditions are a flow rate of 1.2 mL / min and a detection UV of 254 nm. The results are shown in Table 1. This result indicates that Glychyrrhiza glabra contains more Licorice-saponinH2 than other species.
<製造例2>
Glychyrrhiza uralensis、Glychyrrhiza glabra、Glychyrrhiza inflataの部根茎部1Kgを細切し、50%エタノール水溶液 10Lにて24時間浸漬後、濾紙(5A ADVANTEC製)にて濾過して濾液を得た。濾液をロータリーエバポレーター(B-480 ビュッヒ製)にて乾固し、乾燥物224gを得た。乾固物中のLicorice-saponinH2の含有量を測定するため、得られた乾固物20mgを水25mLに加え、30分間超音波処理装置(UT-204 シャープ製)で分散・破砕しながら溶解し、99%エタノールで50mLとなるようにメスアップし、0.45μmのフィルター(Millex-HT ミリポア製)にて濾過した。濾液を前記HPLCシステムを用い前記と同様の条件にて測定した。結果を表2に示す。この結果からGlychyrrhiza glabraに他の種に比べてLicorice-saponinH2が多く含まれていることがわかる。
<Production Example 2>
Glychyrrhiza uralensis, Glychyrrhiza glabra, and Glychyrrhiza inflata were obtained by chopping 1 Kg of the rhizome part, soaking in 10 L of 50% ethanol aqueous solution for 24 hours, and filtering with filter paper (5A ADVANTEC) to obtain a filtrate. The filtrate was dried with a rotary evaporator (B-480 manufactured by Büch) to obtain 224 g of a dried product. In order to measure the content of Licorice-saponinH2 in the dried product, add 20 mg of the obtained dried product to 25 mL of water and dissolve for 30 minutes while dispersing and crushing with an ultrasonic treatment device (UT-204 Sharp). The volume was adjusted to 50 mL with 99% ethanol and filtered through a 0.45 μm filter (Millex-HT Millipore). The filtrate was measured using the HPLC system under the same conditions as described above. The results are shown in Table 2. This result indicates that Glychyrrhiza glabra contains more Licorice-saponinH2 than other species.
<試験例1>
前記で得られたLicorice-saponinH2、glabridinと市販のグリチルリチン(和光純薬社製)のヒアルロニダーゼに対する阻害作用の比較を行った。
各化合物2mg/mLとなるよう0.1M酢酸緩衝液(pH4)溶液に溶解し、サンプルを調製した。調製した各サンプルを0.2mL量り取り、ヒアロニダーゼ(和光純薬社製)の0.1M酢酸緩衝液(pH4)溶液0.1mLに加え、37℃にて20分間インキュベートした。この際、コントロールとしてサンプルの代わりに酢酸緩衝液のみのものを同様に処理した。さらにコントロールブランクとして、サンプル及びヒアロニダーゼを加えず、酢酸緩衝液のみのもの、並びにサンプルブランクとしてサンプルと緩衝液のみで酵素を加えないものを調製した。これらに0.5mg/mLに調製したCompound 48/80(シグマ社製)0.1M酢酸緩衝液(pH4)0.2mLをに加えて37℃にて20分間インキュベートした。さらに、0.5mg/mLに調製したのヒアルロン酸ナトリウム(和光純薬社製)0.1M酢酸緩衝液(pH4)0.5mLを加え、37℃にて40分間インキュベートした後、氷上に置き、0.4N NaOH0.2mL次いでホウ酸溶液を加え、酵素反応を停止した。この際用いたホウ酸溶液はホウ酸4.95gに水を加え、1NのNaOHでpH9.1とし、100mLにメスアップしたものである。その後、反応停止後の各溶液は、100℃の水で3分間処理して酵素活性を失活させ、氷上で室温まで冷却し、ジメチルアミノベンズアルデヒド溶液6mLを加え、37℃で20分間放置した。この際用いたジメチルアミノベンズアルデヒド溶液はパラジメチルアミノベンズアルデヒド1gに10N 塩酸1.25mLと酢酸8.75mLを混和し、使用直前に酢酸にて10倍希釈したものである。以上の操作を行った後、585nmにて吸光度を測定し、以下の式からヒアルロニダーゼ阻害率(%)を算出した。
ヒアルロニダーゼ阻害率(%)
=[(コントロールーコントロールブランク)−(サンプル−サンプルブランク)]
/(コントロールーコントロールブランク)×100
その結果を表3に示す。
<Test Example 1>
The inhibitory action of Licorice-saponinH2 and glabridin obtained above and commercially available glycyrrhizin (manufactured by Wako Pure Chemical Industries, Ltd.) on hyaluronidase was compared.
Samples were prepared by dissolving in 0.1 M acetate buffer (pH 4) solution to 2 mg / mL of each compound. 0.2 mL of each prepared sample was weighed, added to 0.1 mL of 0.1 M acetate buffer (pH 4) solution of hyalonidase (manufactured by Wako Pure Chemical Industries, Ltd.), and incubated at 37 ° C. for 20 minutes. At this time, as a control, an acetate buffer solution alone was treated in the same manner instead of the sample. Further, as a control blank, a sample and a hyaluronidase were not added, and only an acetate buffer was prepared, and a sample blank and an enzyme were not added only with a sample and a buffer. To this, 0.2 mL of Compound 48/80 (manufactured by Sigma) 0.1 M acetate buffer (pH 4) prepared to 0.5 mg / mL was added and incubated at 37 ° C. for 20 minutes. Furthermore, after adding 0.5 mL of sodium hyaluronate (manufactured by Wako Pure Chemical Industries, Ltd.) 0.1 M acetate buffer (pH 4) prepared to 0.5 mg / mL and incubating at 37 ° C. for 40 minutes, the mixture was placed on ice, The enzyme reaction was stopped by adding 0.2 mL of 0.4N NaOH and then a boric acid solution. The boric acid solution used here was prepared by adding water to 4.95 g of boric acid, adjusting the pH to 9.1 with 1N NaOH, and increasing the volume to 100 mL. Thereafter, each solution after stopping the reaction was treated with water at 100 ° C. for 3 minutes to deactivate the enzyme activity, cooled to room temperature on ice, added with 6 mL of dimethylaminobenzaldehyde solution, and left at 37 ° C. for 20 minutes. The dimethylaminobenzaldehyde solution used here was prepared by mixing 1.25 mL of 10N hydrochloric acid and 8.75 mL of acetic acid with 1 g of paradimethylaminobenzaldehyde and diluting 10 times with acetic acid immediately before use. After performing the above operation, the absorbance was measured at 585 nm, and the hyaluronidase inhibition rate (%) was calculated from the following formula.
Hyaluronidase inhibition rate (%)
= [(Control-Control Blank)-(Sample-Sample Blank)]
/ (Control-control blank) x 100
The results are shown in Table 3.
<試験例2>
前記で得られたGlychyrrhiza uralensis、Glychyrrhiza glabra、Glychyrrhiza inflataの70%エタノール水溶液抽出エキスのヒアルロニダーゼに対する阻害作用の比較を行った。各エキス乾燥物を10mg量り取り、2mg/mLとなるよう0.1M酢酸緩衝液(pH4)溶液に溶解し、サンプルを調製した。ヒアルロニダーゼの阻害率は上記と同様に行い測定した。
その結果を表4に示す。
<Test Example 2>
Comparison of the inhibitory action against hyaluronidase of 70% aqueous ethanol extract of Glychyrrhiza uralensis, Glychyrrhiza glabra and Glychyrrhiza inflata obtained above was performed. 10 mg of each dried extract was weighed and dissolved in a 0.1 M acetate buffer (pH 4) solution to 2 mg / mL to prepare a sample. The inhibition rate of hyaluronidase was measured in the same manner as described above.
The results are shown in Table 4.
<試験例3>
前記の製造例と同様にしてGlychyrrhiza glabraを細切して、これに抽出溶媒としてエタノール含有量を0,30、50,70%としたエタノール水溶液をそれぞれ加え、得られた抽出エキスのヒアルロニダーゼに対する阻害作用の比較を行った。各エキス乾燥物を10mg量り取り、2mg/mLとなるよう0.1M酢酸緩衝液(pH4)溶液に溶解し、サンプルを調製した。ヒアルロニダーゼの阻害率は上記と同様に行い測定した。その結果を表3に示す。
<Test Example 3>
Glychyrrhiza glabra was chopped in the same manner as in the above production example, and ethanol aqueous solutions with ethanol contents of 0, 30, 50, and 70% were added to this as an extraction solvent, respectively, and the resulting extract was inhibited against hyaluronidase. The effect was compared. 10 mg of each dried extract was weighed and dissolved in a 0.1 M acetate buffer (pH 4) solution to 2 mg / mL to prepare a sample. The inhibition rate of hyaluronidase was measured in the same manner as described above. The results are shown in Table 3.
<本発明の経口投与組成物>
本発明の経口投与組成物は、前記Glychyrrhiza glabra抽出液あるいは乾固物を経口投与組成物とすることを特徴とする。本発明の経口投与組成物としては、食品や飲料などが好ましく例示でき、例えば、健康、美容のために摂取する食品や嗜好性に従って摂取される食品などの食品がより好ましく例示できる。特に好ましいものは、美容の目的、特に肌荒れ、ニキビ改善の目的で摂取される食品が例示できる。かかる食品としては、散剤、顆粒剤、錠剤などが好適に例示でき、錠剤が特に好ましい。錠剤は糖衣されていても、被覆剤で被覆されていても良い。本発明の経口投与組成物には、前記成分以外に通常経口投与組成物で使用される任意成分を含有することが出来る。この様な任意成分としては、例えば、乳糖や結晶セルロースのような賦形剤、ヒドロキシプロピルセルロースやアラビアゴムのような結合剤、糖衣剤、被覆剤、ショ糖脂肪酸エステルなどの分散助剤、ステアリン酸マグネシウムのような滑沢剤などが好適に例示できる。これらの必須成分、任意成分を常法に従って処理することにより、本発明の経口組成物は製造できる。
<The composition for oral administration of the present invention>
The composition for oral administration of the present invention is characterized in that the Glychyrrhiza glabra extract or dried product is used as an composition for oral administration. Preferred examples of the composition for oral administration of the present invention include foods and beverages. For example, foods such as foods taken for health and beauty and foods taken according to palatability are more preferred. Particularly preferred are foods taken for the purpose of beauty, especially for rough skin and acne. As such foods, powders, granules, tablets and the like can be suitably exemplified, and tablets are particularly preferable. The tablet may be sugar-coated or coated with a coating agent. The oral administration composition of the present invention can contain optional components usually used in oral administration compositions in addition to the above components. Examples of such optional components include excipients such as lactose and crystalline cellulose, binders such as hydroxypropylcellulose and gum arabic, sugar coating agents, coating agents, dispersion aids such as sucrose fatty acid esters, stearin A lubricant such as magnesium acid can be suitably exemplified. The oral composition of the present invention can be produced by treating these essential components and optional components according to a conventional method.
以下に、実施例を挙げて、更に詳細に本発明について説明を加える。 Hereinafter, the present invention will be described in more detail with reference to examples.
下記処方に従って、本発明の経口投与組成物である、肌荒れ、ニキビの予防、改善する美肌用の食品(錠剤)を製造した。即ち、処方成分をV型混合機に仕込み、均一に混合させた。これを打錠機で244mg錠に打錠成形し、本発明の経口投与組成物1を得た。 According to the following prescription, an orally-administered composition of the present invention, a food (tablet) for beautifying skin that prevents and improves rough skin and acne was produced. That is, the prescription ingredients were charged into a V-type mixer and mixed uniformly. This was tableted into 244 mg tablets with a tableting machine to obtain the composition for oral administration 1 of the present invention.
経口投与組成物1と同様に、表7に処方を示す処方の対照例を調製した。 As in the case of the composition for oral administration 1, a control example of the formulation whose formulation is shown in Table 7 was prepared.
経口投与組成物1と同様に、表8に処方を示す処方の対照例を調製した。 As in the case of the composition for oral administration 1, a control example of the formulation whose formulation is shown in Table 8 was prepared.
<有効性確認試験>
前記の経口組成物の思春期後のニキビあるいは肌荒れに悩んでいる女性を対象にニキビや肌状態への影響を調査した。前記の各経口組成物を1日4錠(1錠244mg)摂取し、12週間のニキビの改善効果を調査した。その結果、表7及び表8の処方に比べて、表6の甘草エキスを入れた経口組成物がニキビ数および医師の所見ともに顕著に改善された。結果は表9に示す。
<Effectiveness confirmation test>
The effect of the oral composition on acne and skin condition was investigated in women suffering from post-pubertal acne or rough skin. Each of the above oral compositions was ingested 4 tablets per day (1 tablet 244 mg), and the effect of improving acne for 12 weeks was investigated. As a result, compared with the formulations of Tables 7 and 8, the oral composition containing the licorice extract of Table 6 markedly improved both the number of acne and the doctor's findings. The results are shown in Table 9.
本発明は、食品として応用できる。 The present invention can be applied as food.
Claims (9)
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CN104208171A (en) * | 2014-09-29 | 2014-12-17 | 刘昆 | Traditional Chinese medicine composite for treating acne |
WO2022249952A1 (en) * | 2021-05-25 | 2022-12-01 | 学校法人鈴鹿医療科学大学 | Antiviral agent |
WO2024075329A1 (en) | 2022-10-04 | 2024-04-11 | 誉郎 大西 | Licorice extract |
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JPN6012065902; Liu, Hong-Min et al: 'Constituents and Their Sweetness of Food Additive Enzymatically Modified Licorice Extract' Journal of Agricultural and Food Chemistry 48(12), 2000, pp.6044-6047 * |
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CN103933166A (en) * | 2014-03-31 | 2014-07-23 | 何梅 | Traditional Chinese medicine for treating acne, and preparation method thereof |
CN104208171A (en) * | 2014-09-29 | 2014-12-17 | 刘昆 | Traditional Chinese medicine composite for treating acne |
WO2022249952A1 (en) * | 2021-05-25 | 2022-12-01 | 学校法人鈴鹿医療科学大学 | Antiviral agent |
WO2024075329A1 (en) | 2022-10-04 | 2024-04-11 | 誉郎 大西 | Licorice extract |
WO2024075330A1 (en) | 2022-10-04 | 2024-04-11 | 誉郎 大西 | Method for improving health condition of mammal or farm animal |
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