JP2015086187A - Tyrosinase inhibitors and external preparations for skin whitening - Google Patents
Tyrosinase inhibitors and external preparations for skin whitening Download PDFInfo
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- JP2015086187A JP2015086187A JP2013227202A JP2013227202A JP2015086187A JP 2015086187 A JP2015086187 A JP 2015086187A JP 2013227202 A JP2013227202 A JP 2013227202A JP 2013227202 A JP2013227202 A JP 2013227202A JP 2015086187 A JP2015086187 A JP 2015086187A
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Abstract
Description
本発明は、植物抽出物を含有するチロシナーゼ活性阻害剤、及びそれを配合した美白用皮膚外用剤に関する。 The present invention relates to a tyrosinase activity inhibitor containing a plant extract, and a skin whitening external preparation containing the same.
シミやそばかす等の色素の沈着は、皮膚細胞内でメラニンが生成し、蓄積することによって生じることが知られている。メラニンは色素細胞の中でチロシンの酸化反応により生成することが知られおり、チロシンからドーパ、ドーパからドーパキノンへの反応が律速段階であるといわれている。そのため、この反応に関与する酵素であるチロシナーゼに着目し、チロシナーゼの活性及び作用を阻害して皮膚のメラニン生成を抑制するアルブチン、コウジ酸、エラグ酸等が美白剤として使用されてきた。 It is known that the deposition of pigments such as spots and freckles is caused by the production and accumulation of melanin in skin cells. Melanin is known to be generated in the pigment cells by the oxidation reaction of tyrosine, and the reaction from tyrosine to dopa and from dopa to dopaquinone is said to be the rate-limiting step. Therefore, focusing on tyrosinase, an enzyme involved in this reaction, arbutin, kojic acid, ellagic acid and the like that inhibit the activity and action of tyrosinase and suppress the production of melanin in the skin have been used as whitening agents.
また、植物由来のチロシナーゼ活性阻害についても広く研究されているが（特許文献１〜７）、さらに効果が高く、新しいチロシナーゼ活性阻害剤が望まれている。 In addition, although plant-derived tyrosinase activity inhibition has been extensively studied (Patent Documents 1 to 7), there is a demand for new tyrosinase activity inhibitors that are more effective.
本発明の課題は、新たな植物由来のチロシナーゼ活性阻害剤、及びそれを配合した美白用皮膚外用剤を提供することにある。 An object of the present invention is to provide a new plant-derived tyrosinase activity inhibitor and a whitening skin external preparation containing the same.
本発明者らは、上記課題を解決すべく検討していく中で、特定の植物から得られた抽出物に優れたチロシナーゼ活性阻害効果があることを見出し、本発明を完成するに至った。 The inventors have found that an extract obtained from a specific plant has an excellent inhibitory effect on tyrosinase activity while studying to solve the above problems, and have completed the present invention.
すなわち、本発明に係るチロシナーゼ活性阻害剤は、シマヤマヒハツ実部抽出物、ホンダワラ抽出物、バンジロウ茎部抽出物、ギンネム抽出物、イジュ抽出物、スダジイ抽出物、モモタマナ抽出物、フクギ抽出物、アダン抽出物、オキナワキョウチクトウ抽出物、ヤエヤマカズラ抽出物、フダンソウ抽出物、シマアザミ抽出物、アメリカハマグルマ抽出物、ニガナ抽出物、タンカン抽出物、パパイヤ抽出物、ダイジョ抽出物、アナアオサ抽出物、ドラゴンフルーツ抽出物、ミズイモ抽出物、スイゼンジナ抽出物、ツワブキ抽出物、シマラッキョウ抽出物、クビレズタ抽出物、ヒジキ抽出物、及びモンパノキ抽出物からなる群より選ばれた１種又は２種以上の植物抽出物を含有するものである。 That is, the tyrosinase activity inhibitor according to the present invention includes: Shimahihihatsu real part extract, honda walla extract, bunjirou stalk extract, ginnem extract, Iju extract, Sudagii extract, Momotamana extract, Fukugi extract, Adan extract , Okinawa oleander extract, yellow sprout extract, chard extract, striped thrip extract, American clam extract, crab extract, tankan extract, papaya extract, daijo extract, ana aosa extract, dragon fruit extract, Containing one or more plant extracts selected from the group consisting of a mosquito extract, a suizendina extract, a camellia extract, a sea bream extract, a terrestrial extract, a hijiki extract, and a monpan extract It is.
本発明に係る美白用皮膚外用剤は、該チロシナーゼ活性阻害剤を含有するものである。 The skin whitening external preparation for whitening which concerns on this invention contains this tyrosinase activity inhibitor.
本発明によれば、シミ、ソバカス、皮膚色素沈着等の原因となるメラニンの産生に関与するチロシナーゼの活性を阻害することによって美白作用を発揮することができ、シミ、ソバカス、皮膚色素沈着症等の予防・治療に有効であるチロシナーゼ活性阻害剤を提供することができる。 According to the present invention, it is possible to exert a whitening effect by inhibiting the activity of tyrosinase involved in the production of melanin that causes spots, buckwheat, skin pigmentation, etc., such as spots, buckwheat, skin pigmentation, etc. It is possible to provide a tyrosinase activity inhibitor that is effective for the prevention and treatment of.
以下、本発明の実施に関連する事項について詳細に説明する。 Hereinafter, matters related to the implementation of the present invention will be described in detail.
本実施形態に係るチロシナーゼ活性阻害剤において、抽出原料となる植物は、シマヤマヒハツ、ホンダワラ、バンジロウ、ギンネム、イジュ、スダジイ、モモタマナ、フクギ、アダン、オキナワキョウチクトウ、ヤエヤマカズラ、フダンソウ、シマアザミ、アメリカハマグルマ、ニガナ、タンカン、パパイヤ、ダイジョ、アナアオサ、ドラゴンフルーツ、ミズイモ、スイゼンジナ、ツワブキ、シマラッキョウ、クビレズタ、ヒジキ、及びモンパノキから選択される少なくとも１種である。 In the tyrosinase activity inhibitor according to the present embodiment, the plant that is the raw material for extraction is Shimahihihatsu, Honda Walla, Vanjirou, Ginnemu, Iju, Sudajii, Momotana, Fukugi, Adan, Okinawan Kakutora, Yaeyamakazura, Fudansou, Shimahagumi, Hanaguru , Tankan, Papaya, Daijo, Anaaaosa, Dragon Fruit, Mizuimo, Suizenjina, Tsukibuki, Shimaraki, Kubilezuta, Hijiki, and Monpanoki.
シマヤマヒハツ（学名：Antidesma pentandrum (Blanco) Merr.）は、琉球諸島から台湾、フィリピンにかけて分布するトウダイグサ科ヤマヒハツ属の常緑低木であり、直径５ミリくらいの楕円形の実を房状につける。本実施形態では、シマヤマヒハツの実を抽出部位として使用することを特徴とする。シマヤマヒハツ（コウトウヤマヒハツ）については、上記特許文献１に幹部、地上部、根部、全草が抽出部位として記載されているが、実部を抽出部位とすることは記載されていない。実部は、他の部位に比べて顕著に優れたチロシナーゼ活性阻害効果を有し、そのため、本実施形態では、シマヤマヒハツの中でも実部を抽出部位とする。 Shimahihihatsu (scientific name: Antitidesma pentandrum (Blanco) Merr.) Is an evergreen shrub belonging to the genus Amaranthaceae that ranges from the Ryukyu Islands to Taiwan and the Philippines. In this embodiment, the fruit of Shimahihatsu is used as an extraction part. About Shimayamahihatsu (Koutuyamahihatsu), although the trunk part, the above-ground part, the root part, and the whole grass are described in the said patent document 1 as an extraction part, it does not describe making a real part an extraction part. The real part has a remarkably superior tyrosinase activity inhibitory effect as compared with other parts. Therefore, in this embodiment, the real part is used as an extraction part in Shimahihatsu.
ホンダワラ（学名：Sargassum fulvellum (Turner) C.Agardh）は、褐藻綱ホンダワラ科ホンダワラ属の海藻であり、本州、四国、九州などに分布する。抽出部位としては、例えば、茎部、葉部、全草等が挙げられる。 Honda Walla (scientific name: Sargassum fulvellum (Turner) C. Agardh) is a seaweed belonging to the genus Honda Walla, a brown alga, and is distributed in Honshu, Shikoku and Kyushu. As an extraction site | part, a stem part, a leaf part, whole grass etc. are mentioned, for example.
バンジロウ（学名：Psidium guajava L.）は、フトモモ科バンジロウ属に属する熱帯性の低木であり、グアバとも称される。本実施形態では、バンジロウの茎部（即ち、幹や枝）を抽出部位として使用することを特徴とする。バンジロウ（グアバ）については、上記特許文献７に葉部の抽出物が記載されているが、茎部を抽出部位とすることは記載されていない。また、上記特許文献３ではバンジロウの葉部及び実部の抽出物についてチロシナーゼ阻害活性を測定するが、阻害活性は認められていない。バンジロウの茎部は、他の部位に比べて顕著に優れたチロシナーゼ活性阻害効果を有し、そのため、本実施形態では、バンジロウの枝部や幹部といった茎部を抽出部位とする。 Banjiro (scientific name: Psidium guajava L.) is a tropical shrub belonging to the genus Banjiro, which is also called guava. The present embodiment is characterized in that the stem portion (that is, the trunk or the branch) of bunjirou is used as the extraction site. As for bunjirou (guava), although the extract of a leaf part is described in the above-mentioned patent document 7, it is not described that a stem part is used as an extraction part. Moreover, in the said patent document 3, although the tyrosinase inhibitory activity is measured about the extract of a leaf part and a real part of bunjiro, inhibitory activity is not recognized. The stem part of the bunjiro has a significantly superior tyrosinase activity inhibitory effect as compared with other parts. Therefore, in this embodiment, the stem part such as a branch part or a stem part of the bungyrow is used as the extraction part.
ギンネム（学名：Leucaena leucocephala (Lam.) de Wit）は、中南米を原産とするマメ科ネムノキ亜科ギンゴウカン属の落葉低木である。抽出部位としては、例えば、葉部、枝部、幹部等が挙げられ、好ましくは葉部である。 Ginnemu (scientific name: Leucaena leucocephala (Lam.) De Wit) is a deciduous shrub belonging to the genus Ginkgocan, which is native to Latin America. As an extraction part, a leaf part, a branch part, a trunk part, etc. are mentioned, for example, Preferably it is a leaf part.
イジュ（学名：Schima wallichii (DC.) Korth. subsp. noronhae (Reinw. ex Blume) Bloemb.）は、沖縄、奄美諸島等に分布するツバキ科ヒメツバキ属の常緑高木である。抽出部位としては、例えば、葉部、枝部、幹部等が挙げられ、好ましくは葉部である。 Iju (scientific name: Schima wallichii (DC.) Korth. Subsp. Noronhae (Reinw. Ex Blume) Bloemb.) Is an evergreen tree belonging to the genus Himetsubu, distributed in Okinawa, the Amami Islands, and the like. As an extraction part, a leaf part, a branch part, a trunk part, etc. are mentioned, for example, Preferably it is a leaf part.
スダジイ（学名：Castanopsis sieboldii (Makino) Hatus. ex T.Yamaz. et Mashiba）は、新潟県以南の地域等に分布するブナ科シイ属の常緑広葉樹である。抽出部位としては、例えば、葉部、実部、枝部、幹部等が挙げられ、好ましくは葉部である。 Sudajii (scientific name: Castanopsis sieboldii (Makino) Hatus. Ex T. Yamaz. Et Mashiba) is an evergreen broad-leaved tree belonging to the genus Beechidae that is distributed in areas south of Niigata Prefecture. As an extraction part, a leaf part, a real part, a branch part, a trunk part, etc. are mentioned, for example, Preferably it is a leaf part.
モモタマナ（学名：Terminalia catappa L.）は、アジアの亜熱帯や熱帯等の地域に分布するシクンシ科モモタマナ属の半落葉樹である。抽出部位としては、例えば、葉部、枝部、幹部等が挙げられ、好ましくは葉部である。 Momotamana (scientific name: Terminalia catappa L.) is a semi-deciduous tree of the genus Motamamana, which is distributed in subtropical and tropical regions of Asia. As an extraction part, a leaf part, a branch part, a trunk part, etc. are mentioned, for example, Preferably it is a leaf part.
フクギ（学名：Garcinia subelliptica Merr.）は、フィリピンや台湾等に分布するオトギリソウ科（又は、テリハボク科）の常緑高木である。抽出部位としては、例えば、葉部、枝部、幹部等が挙げられ、好ましくは葉部である。 Fukugi (scientific name: Garcinia subelliptica Merr.) Is an evergreen Takagi of Hypericaceae (or Terriaceae) distributed in the Philippines and Taiwan. As an extraction part, a leaf part, a branch part, a trunk part, etc. are mentioned, for example, Preferably it is a leaf part.
アダン（学名：Pandanus odoratissimus L.f.）は、亜熱帯から熱帯の海岸沿いに生育するタコノキ科タコノキ属の常緑小高木である。抽出部位としては、例えば、葉部、実部、枝部、幹部等が挙げられ、好ましくは葉部である。 Adan (scientific name: Pandanus odoratissimus L.f.) is an evergreen small tree of the genus Taconoki that grows along the coast from subtropical to tropical. As an extraction part, a leaf part, a real part, a branch part, a trunk part, etc. are mentioned, for example, Preferably it is a leaf part.
オキナワキョウチクトウ（学名：Cerbera manghas L.）は、アジアの熱帯から亜熱帯の地域等に生育するキョウチクトウ科ミフクラギ属の常緑亜高木である。抽出部位としては、例えば、葉部、枝部、幹部等が挙げられ、好ましくは葉部である。 Okinawa oleander (scientific name: Cerbera manghas L.) is an evergreen sub-tree of the genus Oleanderaceae that grows in tropical and subtropical regions of Asia. As an extraction part, a leaf part, a branch part, a trunk part, etc. are mentioned, for example, Preferably it is a leaf part.
ヤエヤマカズラ（学名：Ipomoea batatas L．）は、琉球諸島で栽培されているヒルガオ科のつる性多年草であり、抽出部位としては、例えば、葉部、茎部、地上部、全草等が挙げられ、好ましくは葉部である。 Yaeyamakazura (scientific name: Ipomoea batatas L.) is a vine perennial plant that is cultivated in the Ryukyu Islands, and examples of extraction sites include leaves, stems, aboveground parts, whole grasses, etc. The leaf portion is preferred.
フダンソウ（学名：Beta vulgaris var. cicla (L.) K.Koch）は、アカザ科フダンソウ属の耐寒性一年草−二年草であり、抽出部位としては、例えば、葉部、地上部、全草等が挙げられ、好ましくは葉部である。 Chard (scientific name: Beta vulgaris var. Cicla (L.) K. Koch) is a cold-resistant annual-biennial plant of the genus Rhododendronceae. Examples include grass and the like, preferably the leaf portion.
シマアザミ（学名：Cirsium brevicaule A.Gray）は、トカラ列島から琉球各島に分布するキク科アザミ属の多年生草本である。抽出部位としては、例えば、葉部、茎部、地上部、全草等が挙げられ、好ましくは葉部である。 Thistle (scientific name: Cirsium brevicaule A.Gray) is a perennial herb belonging to the genus Asteraceae from the Tokara Islands to the Ryukyu Islands. As an extraction site | part, a leaf part, a stem part, an above-ground part, whole grass, etc. are mentioned, for example, Preferably it is a leaf part.
アメリカハマグルマ（学名：Wedelia trilobata (L.) Hitchc.）は、中央アメリカを原産地として沖縄にも帰化植物として定着しているキク目キク亜科スファグネティコラ属に分類される多年草である。抽出部位としては、例えば、葉部、花部、茎部、地上部、全草等が挙げられ、好ましくは花部である。 The American cuffed bean (scientific name: Wedelia trilobata (L.) Hitchc.) Is a perennial that is classified into the genus Sphagneticola of the order Asteraceae, which originates in Central America and has become a naturalized plant in Okinawa. As an extraction site | part, a leaf part, a flower part, a stem part, an above-ground part, whole grass etc. are mentioned, for example, Preferably it is a flower part.
ニガナ（学名：Crepidiastrum lanceolatum）は、沖縄等に生育するキク科アゼトウナ属の多年草である。抽出部位としては、例えば、葉部、茎部、地上部、全草等が挙げられ、好ましくは全草である。 Nigana (scientific name: Crepidiastrum lanceolatum) is a perennial plant belonging to the genus Astertoaceae that grows in Okinawa. As an extraction part, a leaf part, a stem part, an above-ground part, whole grass, etc. are mentioned, for example, Preferably it is whole grass.
タンカン（学名：Citrus tankan Hayata）は、中国の広東省を原産地として沖縄等で栽培されているミカン科ミカン属の常緑樹である。抽出部位としては、例えば、葉部、果皮部、枝部等が挙げられ、好ましくは葉部である。 Tankan (scientific name: Citrus tankan Hayata) is an evergreen tree belonging to the genus Citrus mandarin, which is cultivated in Okinawa etc. with its origin in Guangdong Province, China. As an extraction site | part, a leaf part, a fruit skin part, a branch part etc. are mentioned, for example, Preferably it is a leaf part.
パパイヤ（学名：Carica papaya）は、メキシコ南部を原産地とし主に熱帯地域で栽培されているパパイア科パパイア属の常緑小高木である。抽出部位としては、例えば、実部、葉部、枝部、幹部等が挙げられ、好ましくは実部である。 Papaya (scientific name: Carica papaya) is an evergreen small tree that belongs to the genus Papaya in the southern part of Mexico and is cultivated mainly in the tropical region. Examples of the extraction site include a real part, a leaf part, a branch part, and a trunk part, and the real part is preferable.
ダイジョ（学名：Dioscorea alata）は、ヤマノイモ科ヤマノイモ属に属し、アジアやオセアニア等の熱帯地域で広く栽培されるヤムイモの１種である。抽出部位としては、例えば、塊根部、茎部、葉部、地上部等が挙げられ、好ましくは塊根部である。 Daijo (scientific name: Dioscorea alata) belongs to the genus Dioscorea, and is a kind of yam that is widely cultivated in tropical regions such as Asia and Oceania. As an extraction site | part, a tuberous root part, a stem part, a leaf part, an above-ground part etc. are mentioned, for example, Preferably it is a tuberous root part.
アナアオサ（学名：Ulva pertusa Kjellman）は、アオサ目アオサ科アオサ属の緑藻であり、抽出部位は全草が好ましい。 Anaaaosa (scientific name: Ulva pertusa Kjellman) is a green alga belonging to the genus Aosa, Aosaaceae, and the extraction site is preferably whole grass.
ドラゴンフルーツ（学名：Hylocereus undatus）は、サボテン科ヒモサボテン属のサンカクサボテンの果実である。抽出部位としては、例えば、果実全体、果皮部、可食部等が挙げられ、好ましくは果皮部である。 Dragon fruit (scientific name: Hylocereus undatus) is the fruit of the cactus cactus belonging to the cactus family cactus genus. As an extraction site | part, the whole fruit, a fruit skin part, an edible part etc. are mentioned, for example, Preferably it is a fruit skin part.
ミズイモ（学名：Colocasia esculenta schott var. aquatilis Kitamura）は、主に南西諸島で栽培されているサトイモ科サトイモ属の植物であり、抽出部位としては、例えば、塊茎部、葉部、全草等が挙げられ、好ましくは塊茎部である。 Aquatilis Kitamura (scientific name: Colocasia esculenta schott var. Aquatilis Kitamura) is a plant belonging to the genus Araceae that is mainly cultivated in the Nansei Islands. Examples of extraction sites include tubers, leaves, and whole grasses. Preferably, it is a tuber part.
スイゼンジナ（学名：Gynura bicolor）は、熱帯アジア原産のキク科サンシチソウ属の多年草である。抽出部位としては、例えば、葉部、茎部、全草等が挙げられ、好ましくは全草である。 Suizinina (scientific name: Gynura bicolor) is a perennial plant belonging to the genus Asteraceae, native to tropical Asia. As an extraction site | part, a leaf part, a stem part, whole grass etc. are mentioned, for example, Preferably it is whole grass.
ツワブキ（学名：Farfugium japonicum (L.) Kitam）は、琉球諸島、九州、四国、本州等に分布するキク科ツワブキ属の多年草である。抽出部位としては、例えば、葉部、茎部、全草等が挙げられ、好ましくは葉部である。 Tsuwabuki (scientific name: Farfugium japonicum (L.) Kitam) is a perennial plant belonging to the genus Asteraceae that is distributed in the Ryukyu Islands, Kyushu, Shikoku, Honshu and other areas. As an extraction site | part, a leaf part, a stem part, whole grass etc. are mentioned, for example, Preferably it is a leaf part.
シマラッキョウ（学名：Allium chinense）は、主として沖縄で栽培されているユリ目ユリ科ネギ属の多年草であり、抽出部位は全草が好ましい。 Sima Rakkyo (scientific name: Allium chinense) is a perennial plant belonging to the genus Liliaceae, which is mainly cultivated in Okinawa, and the extraction site is preferably whole grass.
クビレズタ（学名：Caulerpa lentillifera）は、南西諸島などに分布するイワズタ科イワズタ属に属する海藻であり、抽出部位は全草が好ましい。 Kubirezta (scientific name: Caulerpa lentillifera) is a seaweed belonging to the genus Iwazuta, distributed in the Nansei Islands and the like, and the whole plant is preferred.
ヒジキ（学名：Sargassum fusiforme (Harvey) Setchell）は、日本や朝鮮半島などに分布する褐藻類ホンダワラ科ホンダワラ属の海藻であり、抽出部位は全草が好ましい。 Hijiki (scientific name: Sargassum fusiforme (Harvey) Setchell) is a seaweed belonging to the genus Hondawala, a brown algae found in Japan and the Korean Peninsula, and the extraction site is preferably whole grass.
モンパノキ（学名：Heliotropium foertherianum Diane et Hilger）は、熱帯から亜熱帯の海岸に生育するムラサキ科キダチルリソウ属の常緑低木ないし小高木である。抽出部位としては、例えば、葉部、枝部、幹部等が挙げられ、好ましくは葉部である。 Montanoki (scientific name: Heliotropium foertherianum Diane et Hilger) is an evergreen shrub or small tree of the genus Euphorbiaceae that grows on tropical to subtropical coasts. As an extraction part, a leaf part, a branch part, a trunk part, etc. are mentioned, for example, Preferably it is a leaf part.
本実施形態に係る植物抽出物としては、これらの植物を抽出原料として得られる抽出液、該抽出液の希釈液若しくは濃縮液、該抽出液を乾燥して得られる乾燥物、又はこれらの粗精製物若しくは精製物のいずれもが含まれる。 As the plant extract according to the present embodiment, an extract obtained using these plants as an extraction raw material, a diluted or concentrated solution of the extract, a dried product obtained by drying the extract, or a crude product thereof Both products and purified products are included.
抽出原料として使用する植物は、粉砕したものが適当である。また、部位によってはヘキサン等の非極性溶媒によって脱脂等の前処理を施してから抽出原料として使用してもよい。脱脂等の前処理を行うことにより、極性溶媒を用いた抽出処理を効率よく行うことができる。 The plant used as the extraction raw material is suitably pulverized. Further, depending on the site, a pretreatment such as degreasing may be performed with a nonpolar solvent such as hexane, and then used as an extraction material. By performing pretreatment such as degreasing, extraction treatment using a polar solvent can be performed efficiently.
抽出処理の際には、抽出溶媒として極性溶媒を使用することが好ましい。植物抽出物に含まれるチロシナーゼ活性阻害効果を示す成分は、極性溶媒を抽出溶媒とする抽出処理によって容易に抽出することができる。極性溶媒の具体例としては、水、水溶性有機溶媒等が挙げられ、これらを単独で又は２種以上を組み合わせて用いることができる。これら極性溶媒のうち、含水水溶性有機溶媒を使用することが好ましい。 In the extraction process, it is preferable to use a polar solvent as the extraction solvent. A component having a tyrosinase activity inhibitory effect contained in a plant extract can be easily extracted by an extraction treatment using a polar solvent as an extraction solvent. Specific examples of the polar solvent include water and water-soluble organic solvents, and these can be used alone or in combination of two or more. Of these polar solvents, it is preferable to use a water-containing water-soluble organic solvent.
抽出溶媒として使用し得る水溶性有機溶媒としては、低級脂肪族アルコール、低級脂肪族ケトン等が挙げられる。低級脂肪族アルコールの具体例としては、メタノール、エタノール、プロパノール、ブタノール等の炭素数１〜５の１価アルコール、１，３−ブチレングリコール、グリセリン、プロピレングリコール、イソプロピレングリコール等の炭素数２〜５の多価アルコール等が挙げられる。低級脂肪族ケトンの具体例としては、アセトン、メチルエチルケトン等が挙げられる。水溶性有機溶媒としては、例えば、酢酸エチル、酢酸ブチル、メチルセロソルブ等の中間極性溶媒を使用することもできる。 Examples of water-soluble organic solvents that can be used as the extraction solvent include lower aliphatic alcohols and lower aliphatic ketones. Specific examples of the lower aliphatic alcohol include monohydric alcohols having 1 to 5 carbon atoms such as methanol, ethanol, propanol, and butanol, 2 to 3 carbon atoms such as 1,3-butylene glycol, glycerin, propylene glycol, and isopropylene glycol. 5 polyhydric alcohol and the like. Specific examples of the lower aliphatic ketone include acetone and methyl ethyl ketone. As the water-soluble organic solvent, for example, an intermediate polar solvent such as ethyl acetate, butyl acetate, or methyl cellosolve can be used.
２種以上の極性溶媒の混合液を抽出溶媒として使用する場合、その混合比は適宜調整することができる。例えば、含水水溶性有機溶媒を使用する場合、一価アルコール、多価アルコール、アセトン等の含有量が５０体積％以上であることが好ましい。 When using the liquid mixture of 2 or more types of polar solvents as an extraction solvent, the mixing ratio can be adjusted suitably. For example, when a water-containing water-soluble organic solvent is used, the content of monohydric alcohol, polyhydric alcohol, acetone or the like is preferably 50% by volume or more.
抽出溶媒としては、水及び／又は低級脂肪族アルコールを用いることが好ましく、より好ましくは水と低級脂肪族アルコールの混液であり、更に好ましくは水とエタノールの混液である。水と低級脂肪族アルコールの混液の場合、低級脂肪族アルコールの含有量が５０体積％以上であることが好ましく、より好ましくは５０〜８０体積％である。 As the extraction solvent, it is preferable to use water and / or a lower aliphatic alcohol, more preferably a mixture of water and a lower aliphatic alcohol, and still more preferably a mixture of water and ethanol. In the case of a mixture of water and a lower aliphatic alcohol, the content of the lower aliphatic alcohol is preferably 50% by volume or more, more preferably 50 to 80% by volume.
抽出処理は、抽出原料である上記植物に含まれる可溶性成分を抽出溶媒に溶出させ得る限り、特に限定されず、常法に従って行うことができる。抽出処理の際には、特殊な抽出方法を採用する必要はなく、室温又は還流加熱下において任意の装置を使用することができる。抽出方法としては、例えば、抽出溶媒中に抽出原料を長時間常温で浸漬して抽出する方法、抽出溶媒の沸点以下の温度に加熱し攪拌しながら抽出する方法、抽出溶媒の沸点付近の温度で加熱還流下にて抽出する方法等が挙げられる。 An extraction process is not specifically limited as long as the soluble component contained in the said plant which is an extraction raw material can be eluted in an extraction solvent, It can carry out in accordance with a conventional method. In the extraction process, it is not necessary to adopt a special extraction method, and any apparatus can be used at room temperature or under reflux heating. Extraction methods include, for example, a method in which an extraction raw material is immersed in an extraction solvent at room temperature for a long time, a method in which extraction is performed while heating to a temperature below the boiling point of the extraction solvent and stirring, and a temperature near the boiling point of the extraction solvent. Examples include a method of extraction under heating and reflux.
抽出処理により可溶性成分を溶出させた後、ろ過、遠心分離等の処理を施して抽出残渣を除くことにより抽出液を得ることができる。得られた抽出液は、該抽出液の希釈液若しくは濃縮液、該抽出液の乾燥物、又はこれらの粗精製物若しくは精製物を得るために、常法に従って希釈、濃縮、乾燥、精製等の処理を施してもよい。精製は、具体的には活性炭処理、吸着樹脂処理、イオン交換樹脂処理等によって行うことができ、これらの処理は、生理活性、すなわちチロシナーゼ活性阻害効果の低下を招かない範囲で行えばよい。 After the soluble component is eluted by the extraction treatment, an extraction liquid can be obtained by performing a treatment such as filtration or centrifugation to remove the extraction residue. The obtained extract is diluted, concentrated, dried, purified, etc. according to a conventional method in order to obtain a diluted or concentrated solution of the extract, a dried product of the extract, or a crude purified product or a purified product thereof. Processing may be performed. Specifically, the purification can be performed by activated carbon treatment, adsorption resin treatment, ion exchange resin treatment, and the like, and these treatments may be performed within a range that does not cause a decrease in physiological activity, that is, tyrosinase activity inhibitory effect.
以上のようにして得られる植物抽出物は、チロシナーゼ活性阻害効果を有しており、この作用を利用してチロシナーゼ活性阻害剤の有効成分として使用することができる。すなわち、本実施形態に係るチロシナーゼ活性阻害剤は、上記植物抽出物を有効成分として含有するものである。また、該植物抽出物は、チロシナーゼ活性阻害効果を通じて美白作用を発揮し得るので、美白剤として使用することもできる。 The plant extract obtained as described above has a tyrosinase activity inhibitory effect, and can be used as an active ingredient of a tyrosinase activity inhibitor using this action. That is, the tyrosinase activity inhibitor according to the present embodiment contains the plant extract as an active ingredient. Moreover, since this plant extract can exhibit a whitening action through the tyrosinase activity inhibitory effect, it can also be used as a whitening agent.
上記植物抽出物は、そのままでもチロシナーゼ活性阻害剤として使用することができるが、常法に従って製剤化して使用することもできる。製剤化する場合、保存や取扱いを容易にするために、デキストリン、シクロデキストリン等の薬学的に許容され得るキャリアーその他任意の助剤を添加することができる。植物抽出物は、製剤化により粉末状、顆粒状、錠剤状等、任意の剤形とすることができる。 The plant extract can be used as it is as a tyrosinase activity inhibitor, but it can also be formulated and used according to a conventional method. In the case of formulating, a pharmaceutically acceptable carrier such as dextrin and cyclodextrin and other optional auxiliaries can be added to facilitate storage and handling. The plant extract can be made into any dosage form such as powder, granule, tablet, etc. by formulation.
本実施形態に係るチロシナーゼ活性阻害剤は、チロシナーゼ活性阻害効果を通じて美白作用を発揮することができるとともに、皮膚に適用した場合の安全性に優れているので、皮膚外用剤に配合するのに好適であり、美白用皮膚外用剤となる。ここで、「皮膚外用剤」とは、皮膚に適用される各種薬剤を意味し、例えば、化粧料、医薬部外品、医薬品等が含まれる。本実施形態では、好ましくは美白化粧料としての利用である。皮膚外用剤の具体例としては、肌に対するものとして、軟膏、クリーム、乳液、化粧水、ローション、パック、ジェル等が挙げられる。 The tyrosinase activity inhibitor according to this embodiment can exhibit a whitening action through a tyrosinase activity inhibitory effect and is excellent in safety when applied to the skin, and is therefore suitable for blending into an external preparation for skin. Yes, it is an external preparation for whitening skin. Here, “skin external preparation” means various drugs applied to the skin, and includes, for example, cosmetics, quasi drugs, pharmaceuticals and the like. In the present embodiment, it is preferably used as a whitening cosmetic. Specific examples of the external preparation for skin include ointments, creams, milky lotions, lotions, lotions, packs, gels and the like for the skin.
皮膚外用剤における植物抽出物の配合量は、皮膚外用剤の種類や植物抽出物の生理活性等によって適宜調整することができるが、好適な配合率は、乾燥物に換算して通常０．００１〜５質量％、好ましくは０．０１〜１質量％である。配合量を０．００１質量％以上とすることにより、チロシナーゼ活性阻害効果及び美白作用を十分に発揮しやすくでき、また、配合量を５質量％以下とすることにより、配合量の増加分に見合ったチロシナーゼ発現抑制作用及び美白作用を発揮させることができる。 The blending amount of the plant extract in the external preparation for skin can be adjusted as appropriate depending on the type of the external preparation for skin, the physiological activity of the plant extract, etc., but the suitable blending ratio is usually 0.001 in terms of dry matter. -5% by mass, preferably 0.01-1% by mass. By making the blending amount 0.001% by mass or more, the tyrosinase activity inhibitory effect and the whitening effect can be sufficiently exerted, and by making the blending amount 5% by mass or less, it is commensurate with the increase in the blending amount. In addition, it is possible to exert a tyrosinase expression suppressing action and a whitening action.
本実施形態に係る美白用皮膚外用剤には、上記植物抽出物が有するチロシナーゼ活性阻害効果を妨げない限り、通常の皮膚外用剤の製造に用いられる主剤、助剤またはその他の成分、例えば、収斂剤、殺菌・抗菌剤、防腐剤、金属イオン封鎖剤、ｐＨ調整剤、キレート剤、清涼剤、乳化剤、増泡剤、増粘剤、消臭・脱臭剤、紫外線吸収剤、保湿剤、細胞賦活剤、消炎・抗アレルギー剤、抗酸化・活性酸素除去剤、酵素、ホルモン類、油脂類、ロウ類、炭化水素類、脂肪酸類、アルコール類、エステル類、界面活性剤、香料、精製水などを配合することができる。 The skin whitening preparation for whitening according to the present embodiment has, as long as it does not interfere with the tyrosinase activity inhibitory effect of the plant extract, a main agent, an auxiliary agent or other components used in the production of a normal skin external preparation, such as astringent Agent, bactericidal / antibacterial agent, antiseptic agent, sequestering agent, pH adjuster, chelating agent, refreshing agent, emulsifier, foaming agent, thickener, deodorant / deodorant, UV absorber, moisturizer, cell activation Agents, anti-inflammatory / anti-allergic agents, antioxidant / reactive oxygen scavengers, enzymes, hormones, oils and fats, waxes, hydrocarbons, fatty acids, alcohols, esters, surfactants, perfumes, purified water, etc. Can be blended.
以下、実施例について説明するが、本発明はこれらに限定されるものではない。 Hereinafter, examples will be described, but the present invention is not limited thereto.
［製造例］各植物からの抽出物の製造
イジュの葉を５０℃で一昼夜送風乾燥し、乾燥したイジュの葉５０ｇを５００ｍＬの７０％（v/v）エタノール溶液（エタノール／水の体積比＝７０／３０）に投入し、３日間室温で保った後、ろ過した。ろ液を５０℃で減圧下にて濃縮し、さらに凍結乾燥機で乾燥して粗抽出物（粉末状）を得た。得られた粗抽出物の質量は８．４ｇ（収率＝１６．８質量％）であった。
[Production Example] Production of Extract from Each Plant Iju leaves were blown and dried overnight at 50 ° C., and 50 g of dried Iju leaves were added to 500 mL of a 70% (v / v) ethanol solution (volume ratio of ethanol / water = 70/30), kept at room temperature for 3 days, and then filtered. The filtrate was concentrated under reduced pressure at 50 ° C., and further dried with a freeze dryer to obtain a crude extract (powder). The mass of the obtained crude extract was 8.4 g (yield = 16.8% by mass).
上記と同様にして、シマヤマヒハツの実、シマヤマヒハツの葉、ホンダワラの全草、バンジロウの枝、バンジロウの葉、ギンネムの葉、スダジイの葉、スダジイの実、モモタマナの葉、フクギの葉、アダンの葉、オキナワキョウチクトウの葉、ヤエヤマカズラの葉、フダンソウの葉、シマアザミの葉、アメリカハマグルマの花、アメリカハナグルマの葉、ニガナの全草、タンカンの葉、パパイヤの実（果実）、ダイジョの塊根、ダイジョの茎、アナアオサの全草、ドラゴンフルーツの果皮、ドラゴンフルーツの可食部、ミズイモの塊茎、ミズイモの葉、スイゼンジナの全草、ツワブキの葉、シマラッキョウの全草、クビレズタの全草、ヒジキの全草、及び、モンパノキの葉を抽出原料として、それぞれ抽出処理を行い、粗抽出物を得た。 In the same manner as above, Shimahihihushi, Shimahihihatsu leaf, Honda walla whole plant, bunjirou branch, bunjirou leaf, ginnemu leaf, sudazii leaf, sudajii berry, peach tamana leaf, fukugi leaf, adan leaf , Okina oleander leaf, yamakazura leaf, chard leaf, striped thistle leaf, buffalo leaf flower, buffalo leaf, licorice whole plant, tankan leaf, papaya fruit (fruit), dijo tuber, dijo Stalk, Anaaaosa whole grass, dragon fruit peel, dragon fruit edible, horned tuber, hornbill leaf, suizenina leaf, swallow leaf, striped alley, cricket whole grass, hijiki Extraction processing was carried out using whole grass and cinnamon leaves as extraction raw materials to obtain crude extracts.
［精製例］粗抽出物の精製
シマヤマヒハツ実部、スダジイ葉部、モモタマナ葉部、オキナワキョウチクトウ葉部、フクギ葉部、及び、アダン葉部の各粗抽出物をそれぞれ水に溶解し、合成吸着剤（「ダイヤイオンＨＰ−２０」三菱化学株式会社製）１００ｍＬを充填したカラムに注入した。その後、水で未吸着物質を洗浄・除去し、エタノールで溶出される画分を分画した。分画物を５０℃で減圧下にて濃縮し、さらに凍結乾燥機で乾燥して精製後の抽出物（粉末状）を得た。
[Purification Example] Purification of Crude Extract Each crude extract of Shimayamahihatsu real part, Sudajii leaf part, Momotamana leaf part, Okinawa oleander leaf part, Fukugi leaf part and Adan leaf part is dissolved in water, respectively, and a synthetic adsorbent ("Diaion HP-20" manufactured by Mitsubishi Chemical Corporation) was injected into a column packed with 100 mL. Thereafter, unadsorbed substances were washed and removed with water, and fractions eluted with ethanol were fractionated. The fraction was concentrated at 50 ° C. under reduced pressure, and further dried with a freeze dryer to obtain a purified extract (powder).
［試験例１］チロシナーゼ活性阻害効果試験
上記製造例及び精製例で得られた各抽出物をサンプルとして、以下の方法により、チロシナーゼ活性阻害率を測定した。
[Test Example 1] Tyrosinase activity inhibition effect test The tyrosinase activity inhibition rate was measured by the following method using the extracts obtained in the above production examples and purification examples as samples.
チロシナーゼは、マッシュルーム由来チロシナーゼ（EC 1.14.18.1）Sigma Chemical 社（２５ＫＵ）を使用し、ストック溶液として１００００Ｕ／ｍＬとなるように超純水またはリン酸緩衝液（ｐＨ６．８）２．５ｍＬを用いて調整した。活性試験時には、ストック溶液を１００倍希釈し１００Ｕ／ｍＬで使用（終濃度２．５Ｕ）した。３，４−ジヒドロキシ−Ｌ−フェニルアラニン（Ｌ−ＤＯＰＡ）は、マイクロプレート上の終濃度２．５ｍＭとなるように１９．７２ｍｇ／１０ｍＬに調整した。リン酸緩衝液はｐＨ６．８に調整した。 As tyrosinase, mushroom-derived tyrosinase (EC 1.14.18.1) Sigma Chemical Co. (25 KU) was used, and 2.5 mL of ultrapure water or phosphate buffer (pH 6.8) was used as a stock solution so as to be 10,000 U / mL. Adjusted. During the activity test, the stock solution was diluted 100 times and used at 100 U / mL (final concentration 2.5 U). 3,4-Dihydroxy-L-phenylalanine (L-DOPA) was adjusted to 19.72 mg / 10 mL so that the final concentration on the microplate was 2.5 mM. The phosphate buffer was adjusted to pH 6.8.
試験方法は、次の通りである。リン酸緩衝液（ｐＨ６．８）４０μＬとサンプルのＤＭＳＯ溶液８０μＬに、チロシナーゼ溶液（２３０Ｕ／ｍＬ）４０μＬとＬ−ＤＯＰＡ（５ｍＭ）４０μＬを添加した。これを３７℃で１０分間反応させ、ＤＯＰＡクロムの形成をプレートリーダーで吸光度測定（４７５ｎｍ）した。同時にサンプル溶液の代わりにリン酸緩衝液を加えたもの（ブランクａ）、リン酸緩衝液１６０μＬにＬ−ＤＯＰＡのみ加えたもの（ブランクｂ）、チロシナーゼ溶液の代わりにリン酸緩衝液を加えたもの（ブランクｃ）を測定した。ポジティブコントロールにはアルブチンを使用した。サンプルおよびアルブチンは１質量％になるようにＤＭＳＯに溶解した後、リン酸緩衝液で０．５質量％に希釈して用いた。 The test method is as follows. 40 μL of tyrosinase solution (230 U / mL) and 40 μL of L-DOPA (5 mM) were added to 40 μL of phosphate buffer (pH 6.8) and 80 μL of sample DMSO solution. This was reacted at 37 ° C. for 10 minutes, and the formation of DOPA chromium was measured for absorbance (475 nm) with a plate reader. At the same time, phosphate buffer added to the sample solution (blank a), L-DOPA added to 160 μL phosphate buffer (blank b), phosphate buffer added instead of tyrosinase solution (Blank c) was measured. Arbutin was used as a positive control. The sample and arbutin were dissolved in DMSO to 1% by mass, and then diluted to 0.5% by mass with a phosphate buffer.
チロシナーゼ活性阻害率（％）は次式で算出した。
チロシナーゼ活性阻害率＝（(Ba-Bb)−(S-Bc)）／（Ba-Bb）×100
ここで、Ba：ブランクａの吸光度、Bb：ブランクｂの吸光度、Bc：ブランクｃの吸光度、S：サンプルの吸光度を表す。
The tyrosinase activity inhibition rate (%) was calculated by the following formula.
Tyrosinase activity inhibition rate = ((Ba-Bb) − (S-Bc)) / (Ba-Bb) × 100
Here, Ba represents the absorbance of blank a, Bb represents the absorbance of blank b, Bc represents the absorbance of blank c, and S represents the absorbance of the sample.
各抽出物についてのチロシナーゼ活性阻害率の結果を下記表１に示す。表１から明らかなように、本実施形態に係る植物抽出物はチロシナーゼ活性阻害効果を有していた。特に、シマヤマヒハツ実部、ホンダワラ、バンジロウ枝部、ギンネム、イジュ及びスダジイの抽出物では、美白剤として汎用されるアルブチンよりも高い効果を示した。粗抽出物のチロシナーゼ活性阻害率が比較的低い場合でも、精製することによって阻害率の改善が見られ、これら植物抽出物のチロシナーゼ活性阻害効果が高いことがわかる。 The results of the tyrosinase activity inhibition rate for each extract are shown in Table 1 below. As is clear from Table 1, the plant extract according to this embodiment had a tyrosinase activity inhibitory effect. In particular, the extracts of Shimayamahihatsu real part, Honda walla, bunjirou branch, ginnemu, Iju and Sudazii showed higher effects than arbutin, which is widely used as a whitening agent. Even when the tyrosinase activity inhibition rate of the crude extract is relatively low, the inhibition rate is improved by purification, and it can be seen that these plant extracts have a high tyrosinase activity inhibition effect.
シマヤマヒハツの実部の抽出物については、葉部の抽出物に比べて、チロシナーゼ活性阻害率が約１．４倍強であり、顕著な効果の違いが認められた。また、バンジロウの枝部抽出物については、葉部の抽出物に比べて、チロシナーゼ活性阻害率が約１．３倍であり、顕著な効果の違いが認められた。 About the extract of the real part of Shimayamahihatsu, the tyrosinase activity inhibition rate was about 1.4 times more than the extract of a leaf part, and the difference of a remarkable effect was recognized. In addition, the banzirou branch extract had a tyrosinase activity inhibition rate of about 1.3 times that of the leaf extract, indicating a marked difference in effect.
［試験例２］メラニン生成抑制試験
シマヤマヒハツ実部抽出物について、Ｂ１６メラノーマ細胞を用いたメラニン生成抑制試験を実施した。
[Test Example 2] Melanin Production Inhibition Test A melanin production inhibition test using B16 melanoma cells was performed on the extract of the real part of Shimahihihatsu.
試験対象としたサンプルは、上記製造例で得られたシマヤマヒハツの実部の粗抽出物と、上記精製例で得られたシマヤマヒハツの実部の精製物（粗精製物）である。また、ポジティブコントロールとしてコウジ酸を用いた。試験使用細胞は、Ｂ１６メラノーマ細胞（マウス由来・４Ａ５株）であり、培養条件および環境は３７℃、ＣＯ２５％濃度とし、基礎培養液としては１０％ＦＢＳ含有ＤＭＥＭ培地を使用した。 The samples to be tested are the crude extract of the real part of Shimahihatsu obtained in the above production example and the purified product (crude product) of the real part of Shimahihatsu obtained in the above purification example. Moreover, kojic acid was used as a positive control. The test cells were B16 melanoma cells (mouse-derived 4A5 strain), the culture conditions and environment were 37 ° C., CO 2 5% concentration, and 10% FBS-containing DMEM medium was used as the basic culture solution.
試験は次のように行った。Ｂ１６メラノーマ細胞を基礎培養後、細胞を試験プレート（24well cell culture plate×2）に播種した（1×105cells／1.0mL／well）。サンプルはＤＭＳＯに溶解し、公比２倍で希釈系列を作製した。播種した細胞を新しい培養液（０．９ｍＬ）に交換後、各濃度のサンプル希釈液５．０μＬを加えて、７２時間培養した。培養終了後、ＰＢＳで細胞を洗浄して１プレートはメラニン生成抑制率を求めるためにＮａＯＨでメラニンを溶出し、１プレートは細胞毒性率を求めるためにクリスタルバイオレットで染色後、メタノールで抽出した。この抽出液の吸光度を測定し、下記式により、メラニン生成抑制率と細胞毒性率を求めた。ここで、対照群とは、サンプル希釈液の代わりに、同量のＤＭＳＯを加えて培養したものである。 The test was conducted as follows. After basic culture of B16 melanoma cells, the cells were seeded on a test plate (24 well cell culture plate × 2) (1 × 10 5 cells / 1.0 mL / well). The sample was dissolved in DMSO, and a dilution series was prepared at a common ratio of 2 times. After replacing the seeded cells with a new culture solution (0.9 mL), 5.0 μL of each sample dilution was added and cultured for 72 hours. After completion of the culture, the cells were washed with PBS, one plate was eluted with NaOH to obtain the inhibition rate of melanin production, and one plate was stained with crystal violet and then extracted with methanol to obtain the cytotoxic rate. The absorbance of this extract was measured, and the melanin production inhibition rate and cytotoxicity rate were determined by the following formula. Here, the control group is a culture obtained by adding the same amount of DMSO instead of the sample diluent.
・細胞毒性率（％）＝
（対照群５４０ｎｍの吸光度−供試化合物５４０ｎｍの吸光度）／対照群５４０ｎｍの吸光度×１００
・メラニン生成抑制率（％）＝
（対照群４０５ｎｍの吸光度−供試化合物４０５ｎｍの吸光度）／ 対照群４０５ｎｍの吸光度×１００
表２にメラニン生成抑制率、表３に細胞毒性率の結果をそれぞれ示す。また、図１及び図２は、粗抽出物及び粗精製物について、濃度と、メラニン生成抑制率及び細胞毒性率との関係を示したグラフである。
・ Cytotoxicity rate (%) =
(Absorbance of control group 540 nm−absorbance of test compound 540 nm) / absorbance of control group 540 nm × 100
-Melanin production inhibition rate (%) =
(Absorbance at 405 nm for control group−absorbance at 405 nm for test compound) / absorbance at 405 nm for control group × 100
Table 2 shows the melanin production inhibition rate, and Table 3 shows the cytotoxicity result. Moreover, FIG.1 and FIG.2 is the graph which showed the relationship between a density | concentration, a melanin production | generation suppression rate, and a cytotoxic rate about a crude extract and a crudely refined product.
シマヤマヒハツ実部の粗抽出物では、５００ｐｐｍまでは、細胞毒性率は２０％程度で、メラニン生成抑制率は１０〜４０％程度であった。細胞毒性率は、１０００ｐｐｍで約４７％まで上昇したが、メラニン生成抑制率は変わらなかった。粗精製物では５００ｐｐｍ以上で７０％程度の細胞毒性を示したが、２５０ｐｐｍまでは細胞毒性率も２０％以下であり、メラニン生成抑制率も５０ｐｐｍで３４％、１００ｐｐｍで３９％、２５０ｐｐｍで４２％あり、濃度依存性を有することからメラニン生成抑制効果を有している。また、ポジティブコントロールであるコウジ酸では５００ｐｐｍで６０％程度、１００ｐｐｍで４０％程度であったことから、シマヤマヒハツ実部の粗精製物は、低濃度ではコウジ酸と同程度の活性を有することが示された。 In the crude extract of the real part of Shimayamahihatsu, the cytotoxicity rate was about 20% and the melanin production inhibition rate was about 10-40% up to 500 ppm. The cytotoxicity rate increased to about 47% at 1000 ppm, but the inhibition rate of melanin production was not changed. The crude product showed a cytotoxicity of about 70% at 500 ppm or more, but the cytotoxicity rate was 20% or less up to 250 ppm, and the inhibition rate of melanin production was 34% at 50 ppm, 39% at 100 ppm, and 42% at 250 ppm. In addition, since it has concentration dependency, it has a melanin production inhibitory effect. In addition, Kojic acid, which is a positive control, was about 60% at 500 ppm and about 40% at 100 ppm. Therefore, it was shown that the crude purified product of the real part of Shimahihatsu has the same activity as Kojic acid at low concentrations. It was done.
通常、粗精製物などの混合物では、ある程度濃度依存的に上昇した後は、メラニン生成抑制活性物質本体以外の濃度も高くなるため高濃度で毒性が発現したり、活性が頭打ちする場合がある。目安としては２００ｐｐｍで約４０％程度の活性があれば、精製度を高めることでさらに活性が上がると言われており、混合物の活性の程度を見分ける境目となる。本試験では、シマヤマヒハツ実部の粗精製物は１００ｐｐｍで約４０％の活性があることから精製度を上げることでメラニン生成抑制活性が高くなることが示唆された。また、１００ｐｐｍでは、毒性も約１０％以下と低く、細胞毒性の影響はほとんどないと考えられる。 Usually, in a mixture such as a crude product, the concentration other than the melanin production-inhibiting active substance itself becomes higher after increasing to a certain degree of concentration, so that toxicity may appear at a high concentration or activity may reach its peak. As a guideline, it is said that if the activity is about 40% at 200 ppm, it is said that the activity can be further increased by increasing the degree of purification. In this test, the crude purified product of the real part of Shimayamahihatsu has an activity of about 40% at 100 ppm, suggesting that the melanin production inhibitory activity is increased by increasing the degree of purification. Further, at 100 ppm, the toxicity is as low as about 10% or less, and it is considered that there is almost no influence of cytotoxicity.
本発明に係るチロシナーゼ活性阻害剤は、チロシナーゼ活性阻害効果を発揮することができるとともに、皮膚に適用した場合の安全性に優れているので、軟膏、クリーム、乳液、化粧水、ローション、パック、ジェル等の化粧料、医薬部外品等に用いることができる。 The tyrosinase activity inhibitor according to the present invention can exhibit a tyrosinase activity inhibitory effect and is excellent in safety when applied to the skin, so an ointment, cream, emulsion, lotion, lotion, pack, gel It can be used for cosmetics such as quasi-drugs and quasi drugs.
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