JP6697479B2 - Composition for promoting hair growth or hair growth and for anti-inflammatory - Google Patents
Composition for promoting hair growth or hair growth and for anti-inflammatory Download PDFInfo
- Publication number
- JP6697479B2 JP6697479B2 JP2017550108A JP2017550108A JP6697479B2 JP 6697479 B2 JP6697479 B2 JP 6697479B2 JP 2017550108 A JP2017550108 A JP 2017550108A JP 2017550108 A JP2017550108 A JP 2017550108A JP 6697479 B2 JP6697479 B2 JP 6697479B2
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- JP
- Japan
- Prior art keywords
- theasaponin
- composition
- assamsaponin
- hair
- hair growth
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 239000000203 mixture Substances 0.000 title claims description 91
- 230000003779 hair growth Effects 0.000 title claims description 37
- 230000001737 promoting effect Effects 0.000 title claims description 16
- 230000003110 anti-inflammatory effect Effects 0.000 title claims description 11
- NEDXBOYHFHZBAP-UHFFFAOYSA-N assamsaponin D Natural products CC=C(C)/C(=O)OC1C(OC(=O)C)C2(CO)C(O)CC3(C)C(=CCC4C5(C)CCC(OC6OC(C(O)C(OC7OC(O)C(O)CC7OC8OCC(O)C(O)C8O)C6OC9OC(CO)C(O)C(O)C9O)C(=O)O)C(C)(CO)C5CCC34C)C2CC1(C)C NEDXBOYHFHZBAP-UHFFFAOYSA-N 0.000 claims description 61
- RPFAABJEBARVGF-MWQJAWBESA-N O=C(O[C@H]1[C@H](O)[C@]2(COC(=O)C)[C@H](O)C[C@@]3(C)[C@@]4(C)[C@@H]([C@]5(C)[C@H]([C@@](C=O)(C)[C@@H](O[C@H]6[C@H](O[C@H]7[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O7)[C@@H](O[C@H]7[C@H](O[C@H]8[C@H](O)[C@@H](O)[C@H](O)CO8)[C@@H](O)[C@@H](O)CO7)[C@H](O)[C@@H](C(=O)O)O6)CC5)CC4)CC=C3[C@@H]2CC1(C)C)/C(=C\C)/C Chemical compound O=C(O[C@H]1[C@H](O)[C@]2(COC(=O)C)[C@H](O)C[C@@]3(C)[C@@]4(C)[C@@H]([C@]5(C)[C@H]([C@@](C=O)(C)[C@@H](O[C@H]6[C@H](O[C@H]7[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O7)[C@@H](O[C@H]7[C@H](O[C@H]8[C@H](O)[C@@H](O)[C@H](O)CO8)[C@@H](O)[C@@H](O)CO7)[C@H](O)[C@@H](C(=O)O)O6)CC5)CC4)CC=C3[C@@H]2CC1(C)C)/C(=C\C)/C RPFAABJEBARVGF-MWQJAWBESA-N 0.000 claims description 44
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- WWVKOCDDDWJQLC-MWQJAWBESA-N (2s,3s,4s,5r,6r)-6-[[(3s,4s,4ar,6ar,6bs,8r,8ar,9r,10r,12as,14ar,14br)-9-acetyloxy-4-formyl-8-hydroxy-8a-(hydroxymethyl)-4,6a,6b,11,11,14b-hexamethyl-10-[(z)-2-methylbut-2-enoyl]oxy-1,2,3,4a,5,6,7,8,9,10,12,12a,14,14a-tetradecahydropicen-3-yl]oxy]-4-[(2s,3 Chemical compound O([C@@H]1[C@@H](O)[C@@H](O)CO[C@H]1O[C@H]1[C@H](O)[C@H](O[C@H]([C@@H]1O[C@H]1[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO)O1)O)O[C@H]1CC[C@]2(C)[C@H]3CC=C4[C@@]([C@@]3(CC[C@H]2[C@@]1(C=O)C)C)(C)C[C@@H](O)[C@@]1(CO)[C@@H](OC(C)=O)[C@@H](C(C[C@H]14)(C)C)OC(=O)C(\C)=C/C)C(O)=O)[C@@H]1OC[C@@H](O)[C@H](O)[C@H]1O WWVKOCDDDWJQLC-MWQJAWBESA-N 0.000 claims description 37
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- 239000004480 active ingredient Substances 0.000 claims description 25
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/82—Theaceae (Tea family), e.g. camellia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q7/00—Preparations for affecting hair growth
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Dermatology (AREA)
- Engineering & Computer Science (AREA)
- Mycology (AREA)
- Biotechnology (AREA)
- Medical Informatics (AREA)
- Microbiology (AREA)
- Alternative & Traditional Medicine (AREA)
- Birds (AREA)
- Molecular Biology (AREA)
- Botany (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Cosmetics (AREA)
- Medicines Containing Plant Substances (AREA)
- Nutrition Science (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
Description
本明細書には、発毛又は育毛促進用組成物及び抗炎用組成物が開示される。 Disclosed herein are compositions for promoting hair growth or hair growth and compositions for anti-inflammatory.
脱毛の原因としては、男性ホルモンの作用過剰説、皮脂分泌の過剰説、血液循環の不良説、過酸化物、細菌などによる頭皮機能の低下説、遺伝的要因、老化、ストレスなどが挙げられている。これに加え、社会的ストレスの増加とともに、環境汚染及びインスタントフードなど西欧化した食習慣、頻繁なパーマや染色などにより脱毛人口が増加しつつある。毛髪の周期は、毛髪を成長させる成長期（ａｎａｇｅｎ）、成長を終了し、毛球部が縮小する時期である退化期（ｃａｔａｇｅｎ）、毛乳頭が活動を停止し、毛髪が頭皮にとどまっているだけの時期である休止期（ｔａｌｏｇｅｎ）、毛乳頭が活動を開始し、または新しい毛髪を発生させ、古くなった毛髪を押し出す時期である発生期に分けられる。 Causes of hair loss include the over-effect theory of male hormones, over-secretion of sebum secretion, hypothesis of poor blood circulation, hypothesis of scalp function deterioration due to peroxides and bacteria, genetic factors, aging, stress, etc. There is. In addition to this, along with the increase in social stress, the hair loss population is increasing due to environmental pollution, westernized eating habits such as instant food, and frequent perms and dyeing. The hair cycle is the growth phase (anagen) for growing hair, the degeneration phase (catagen) when growth ends and the hair bulb part shrinks, the papilla ceases to be active, and the hair stays on the scalp. It is divided into a resting period (talogen), a period in which the papilla becomes active, or new hair is generated and old hair is pushed out.
成長期（Ａｎａｇｅｎ Ｓｔａｇｅ；２〜７年）は、毛髪が成長する期間であって、さらに毛髪が毛球から毛包に出ようとする毛髪生成段階と、硬いケラチンが毛嚢の中で作られる段階とに分けられる。毛髪は、退行期まで自己成長を続ける。退行期（Ｃａｔａｇｅｎ Ｓｔａｇｅ；２〜３週）は、成長期が終わり、毛髪の形態を維持しつつ代謝過程が遅くなる時期で、この段階では、ケラチンを作り出さない。退化期は、毛髪全体の１％を占める。このとき、毛球部が収縮して毛乳頭から分かれ、毛嚢に覆われて上方に上がっていき、細胞***は停止状態となる。休止期（Ｔａｌｏｇｅｎ Ｓｔａｇｅ；３ヶ月）は、毛乳頭が萎縮し、毛嚢が徐々に萎びていき、毛根が上方に押し上げられて抜ける。毛髪がなくなる時期であり、次の成長期段階が始まるまでの寿命は３〜４ヶ月である。 The anagen stage (2 to 7 years) is the period during which hair grows, and the hair-forming stage in which hair tries to move from the bulb to the follicle and hard keratin is formed in the hair follicle. It is divided into stages. Hair continues to grow until regression. The catagen stage (Catagen Stage; 2-3 weeks) is a period in which the growth phase ends and the metabolic process is slowed down while maintaining the hair morphology, and keratin is not produced at this stage. The degeneration period accounts for 1% of all hair. At this time, the hair bulb part contracts and separates from the papilla of the hair, is covered with hair follicles and rises upward, and cell division is stopped. During the resting period (Talogen Stage; 3 months), the papilla of the hair is atrophied, the hair follicle is gradually atrophied, and the root of the hair is pushed up to come out. It is the time when the hair is gone, and the life span before the start of the next growth phase is 3-4 months.
正常な人は成長期状態の毛髪が多いのに比べ、脱毛症（Ａｌｏｐｅｃｉａ）の人は休止期状態の毛髪が多く、目に見える脱毛現象が現れるようになる。脱毛が進行するほど成長期の期間が短くなり、これにより、毛髪数はますます減少する。したがって、脱毛の治療のためには、休止期状態の毛嚢を、成長期に速やかに進むことができるようにし、短くなった成長期を長くしてやることが重要である。 A normal person has a lot of hair in a growing state, whereas a person with alopecia (Alopecia) has a lot of hair in a resting state, and a visible hair loss phenomenon appears. The more hair loss progresses, the shorter the growing period becomes, and the number of hairs further decreases. Therefore, for the treatment of hair loss, it is important to allow the hair follicles in the quiescent state to advance rapidly to the growth phase and to lengthen the shortened growth phase.
男性型脱毛症は、テストステロン（Ｔｅｓｔｏｓｔｅｒｏｎｅ）という男性ホルモンによって現れる現象で、このテストステロンが５α−リダクターゼ（５α−ｒｅｄｕｃｔａｓｅ）という酵素によって、より強力なホルモンであるジヒドロテストステロン（Ｄｉｈｙｄｒｏｔｅｓｔｏｓｔｅｒｏｎｅ、ＤＨＴ）に変わると、このホルモンが毛嚢に作用して毛嚢を成長期段階から退化期段階へと誘導して、脱毛を引き起こさせる。したがって、男性型脱毛症を治療するために、５α−リダクターゼによるＤＨＴの生成を抑制する方法が主に使用される。 Androgenetic alopecia is a phenomenon that is manifested by a male hormone called testosterone (Testosterone), and when this testosterone is changed to a more potent hormone, dihydrotestosterone (DHT), by the enzyme 5α-reductase (5α-reductase), This hormone acts on the hair follicles to induce them from the anagen phase to the degeneration phase, causing hair loss. Therefore, methods for suppressing the production of DHT by 5α-reductase are mainly used for treating androgenetic alopecia.
女性型脱毛症は、主に閉経後のエストロゲン量の減少によって発生する。女性型脱毛症のための治療剤としては、主にミノキシジルやエストロゲンが使用されている。 Female pattern baldness is caused mainly by a decrease in the amount of estrogen after menopause. Minoxidil and estrogen are mainly used as therapeutic agents for female pattern baldness.
円形脱毛症は、自己免疫疾患や精神的ストレス、遺伝的素因によって発生する。このような円形脱毛症は、アンドロゲン性脱毛症とは根本的に原因が異なり、治療法もまた異なるため、副腎皮質ホルモン剤を処理する方法を用いたり、ミノキシジルを患部に塗ったり、人為的に患部に刺激を誘発したりする方法を用いる。 Alopecia areata is caused by autoimmune diseases, mental stress, and genetic predisposition. Such alopecia areata has a fundamentally different cause from androgenic alopecia, and its treatment method is also different.Therefore, a method of treating corticosteroids, applying minoxidil to the affected area, or artificially treating it. A method of inducing irritation to the affected area is used.
しかし、これまで、脱毛を防止し、発毛促進及び毛髪の生長に効果を持っていると知られているミノキシジル（ｍｉｎｏｘｉｄｉｌ）やトリコサッカライド（ｔｒｉｃｈｏｓａｃｃｈａｒｉｄｅ）などの製剤の場合、はっきりとした効能の不在及び人体安定性、皮膚刺激誘発などの副作用の問題が台頭していることから、安全性及び効能が確保された組成物の開発が急がれている実情である。 However, in the case of preparations such as minoxidil and trichosaccharide, which are known to have effects on hair loss prevention, promotion of hair growth and hair growth, there is no clear indication of efficacy. In addition, since the problems of side effects such as human body stability and induction of skin irritation are emerging, it is an urgent situation to develop a composition having safety and efficacy.
一方、炎症を担う媒介体としては、血管活性アミン（Ｖａｓｏ−ａｃｔｉｖｅ ａｍｉｎｅｓ）、血管活性ポリペプチド（Ｂａｓｏ−ａｃｔｉｖｅ ｐｏｌｙｐｅｐｔｉｄｅ）、及びその他の媒介物質などがあり、血管活性アミンとしては、肥満細胞から分泌されるヒスタミンとセレトニンなどがあり、主に血管拡張や透過性を増進させる作用をする。また、血管活性ポリペプチドとしては、キニン（ｋｉｎｉｎ）、プラスミン（ｐｌａｓｍｉｎ）、 補体（ｃｏｍｐｌｅｍｅｎｔ）などがあり、これらは血管収縮作用をし、その他、インターロイキン−６（ＩＬ−６）などのようなリンホカインとアラキドン酸（ａｒａｃｈｉｄｏｎｉｃ ａｃｉｄ）などが炎症反応を担う。 On the other hand, mediators responsible for inflammation include vasoactive amines (Vazo-active amines), vasoactive polypeptides (Basso-active polypeptides), and other mediators. The vasoactive amines are secreted from mast cells. There are histamine and serotonin, etc., which mainly act to enhance vasodilation and permeability. In addition, vasoactive polypeptides include kinin, plasmin, complement, etc., which have a vasoconstrictor action, and other factors such as interleukin-6 (IL-6). Lymphokines and arachidonic acid are responsible for the inflammatory response.
物理的や化学的刺激によって活性化したホスホリパーゼにより生成されたアラキドン酸は、さらにシクロオキシゲナーゼ（ｃｙｃｌｏｏｘｙｇｅｎａｓｅ、ＣＯＸ）或いはリポオキシゲナーゼ（ｌｉｐｏｏｘｙｇｅｎａｓｅ）の二つの経路を経て炎症反応媒介体であるプロスタグランジン（ｐｒｏｓｔａｇｌａｎｄｉｎ）、ロイコトリエン（ｌｅｕｋｏｔｒｉｅｎｅ）で代謝され、多様な炎症反応を媒介する（非特許文献１、特許文献１）。 Arachidonic acid produced by phospholipase activated by physical or chemical stimulus is further pro-staglandin (prostaglandin) which is an inflammatory reaction mediator via two pathways of cyclooxygenase (COX) or lipoxygenase. , Is metabolized by leukotriene and mediates various inflammatory reactions (Non-patent Documents 1 and 1).
一側面において、本明細書は、アッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）及びテアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）からなる群より選択される一つ以上を有効成分として含む発毛又は育毛促進用組成物を提供することを目的とする。 In one aspect, the present description refers to Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponins D, Assasaponins D, and Assasaponins D. It is an object of the present invention to provide a composition for promoting hair growth or hair growth, which comprises one or more selected from the group consisting of Theasaponin C1) as an active ingredient.
他の側面において、本明細書は、アッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）及びテアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）からなる群より選択される一つ以上を有効成分として含む抗炎用組成物を提供することを目的とする。 In another aspect, the present specification refers to Assamsaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Assamsaponin D, and Assamsaponin D. It is an object of the present invention to provide an anti-inflammatory composition containing, as an active ingredient, one or more selected from the group consisting of (Theasaponin C1).
一側面において、本明細書に開示された技術は、前記化学式で表されるアッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）及びテアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）からなる群より選択される一つ以上を有効成分として含む発毛又は育毛促進用組成物を提供する。 In one aspect, the technology disclosed in the present specification provides the assamsaponin B (Assamsaponin B), theasasaponin E1 (theasaponin E2), and the assamsaponin H (Assaponin H) that are represented by the chemical formulas. Provided is a composition for promoting hair growth or hair growth, which comprises, as an active ingredient, one or more selected from the group consisting of Assamsaponin D and Theasaponin C1.
他の側面において、本明細書に開示された技術は、前記化学式で表されるアッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）及びテアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）からなる群より選択される一つ以上を有効成分として含む抗炎用組成物を提供する。 In another aspect, the technology disclosed in the present specification provides the assamsaponin B (Assasaponin B), theasaponin E1 (theasaponin E2), and the assamsaponin H (Assampon H) that are represented by the above chemical formulas. The present invention provides an anti-inflammatory composition comprising as an active ingredient one or more selected from the group consisting of Assamsaponin D and Theasaponin C1.
例示的な一具現例によれば、前記有効成分は、椿種子（Ｃａｍｅｌｌｉａ Ｓｅｅｄ）抽出物から分離されたものであってよい。 According to an exemplary embodiment, the active ingredient may be separated from Camellia Seed extract.
例示的な一具現例によれば、当該組成物は、毛嚢毛乳頭細胞を増殖させるものであってよい。 According to an exemplary embodiment, the composition may be one that proliferates hair follicle papilla cells.
例示的な一具現例によれば、当該組成物は、ＰＧＥ２、ＩＬ−６又はＩＬ−８の生成を抑制するものであってよい。 According to one exemplary embodiment, the composition may suppress the production of PGE2, IL-6 or IL-8.
例示的な一具現例によれば、前記有効成分は、当該組成物の総質量を基準として０．００１〜２０質量％の範囲で含まれていてよい。 According to an exemplary embodiment, the active ingredient may be included in the range of 0.001 to 20 mass% based on the total mass of the composition.
例示的な一具現例によれば、当該組成物は薬学組成物であってよい。 According to one exemplary embodiment, the composition may be a pharmaceutical composition.
例示的な一具現例によれば、当該組成物は化粧料組成物であってよい。 According to one exemplary embodiment, the composition may be a cosmetic composition.
例示的な一具現例によれば、当該組成物は食品組成物であってよい。 According to one exemplary embodiment, the composition may be a food composition.
一側面において、本明細書に開示された技術は、アッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）及びテアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）からなる群より選択される一つ以上を有効成分として含む発毛又は育毛促進用組成物を提供する効果がある。 In one aspect, the technology disclosed herein includes Assamsaponin B (Assamsaponin B), Theasaponin E1 (Theasaponin E2), Assamsaponins D (Assasaponin H), Assamsaponin D (Assasaponin H), and Assamsaponin D (Assamsaponin D). ) And the thesaponin C1 (Theasaponin C1) is effective in providing a composition for promoting hair growth or hair growth, which comprises one or more selected from the group consisting of Theasaponin C1.
他の側面において、本明細書に開示された技術は、アッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）及びテアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）からなる群より選択される一つ以上を有効成分として含む抗炎用組成物を提供する効果がある。 In another aspect, the techniques disclosed herein include Assamsaponin B, Asasaponin E1, Theasaponin E2, Assamsaponins H, Assamsaponin H, Assamsaponin H, Assamsaponin H, Assamsaponin H, Assamsaponin H, Assamsaponin H, Assamsaponin H, Assamsaponin H, Assamsaponin H, Assamsaponin H, Assamsaponin H, Assamsaponin H, Assamsaponin H, Assamsaponin H. D) and the thesaponin C1 (Theasaponin C1) is effective in providing an anti-flame composition containing at least one selected from the group consisting of.
また他の側面において、本明細書に開示された技術は、植物性天然物質を有効成分として含むことで副作用がなく且つ安定性に優れる、発毛又は育毛促進用、抗炎用薬学組成物、化粧料組成物、食品組成物を提供する効果がある。 In still another aspect, the technology disclosed in the present specification has no side effects and is excellent in stability by including a natural plant substance as an active ingredient, for promoting hair growth or hair growth, and an anti-inflammatory pharmaceutical composition, It is effective in providing a cosmetic composition and a food composition.
以下、本発明を詳細に説明する。 Hereinafter, the present invention will be described in detail.
一側面において、本明細書に開示された技術は、前記化学式で表されるアッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）及びテアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）からなる群より選択される一つ以上を有効成分として含む発毛又は育毛促進用組成物を提供する。 In one aspect, the technology disclosed in the present specification provides the assamsaponin B (Assamsaponin B), theasasaponin E1 (theasaponin E2), and the assamsaponin H (Assaponin H) that are represented by the chemical formulas. Provided is a composition for promoting hair growth or hair growth, which comprises, as an active ingredient, one or more selected from the group consisting of Assamsaponin D and Theasaponin C1.
他の側面において、本明細書に開示された技術は、発毛又は育毛促進に用いるための、前記化学式で表されるアッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）及びテアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）からなる群より選択されるいずれか一つ以上を提供する。 In another aspect, the technology disclosed herein is for use in promoting hair growth or hair growth, Assam saponin B (Thesasaponin B1), Theasaponin E1 and Theasaponin E2 (Theasaponin E2) represented by the above formula. E2), one or more selected from the group consisting of Assamsaponin H (Assamsaponin H), Assamsaponin D (Thesassaponin D), and Theasaponin C1.
また他の側面において、本明細書に開示された技術は、前記化学式で表されるアッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）及びテアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）からなる群より選択される一つ以上、又はこれらを有効成分として含む発毛又は育毛促進用組成物を、発毛又は育毛が必要な個体に投与することを含む発毛又は育毛促進方法を提供する。本発明の一側面における前記投与は、本明細書に記載された投与方法及び投与用量に従って行われていてよい。 In still another aspect, the technology disclosed in the present specification provides an assamsaponin B (Assamsaponin B), a theasaponin E1 (theasaponin E1), a theasaponin E2 (thesasaponin E2), and an assamsaponin H (Assamsapn H). ), One or more selected from the group consisting of Assamsaponin D (Assamasponin D) and Theasaponin C1 (Theasaponin C1), or a composition for promoting hair growth containing these as an active ingredient is required for hair growth or hair growth. The present invention provides a method for promoting hair growth or hair growth, which method comprises the administration to any individual. The administration according to one aspect of the present invention may be performed according to the administration method and administration dose described in the present specification.
また他の側面において、本明細書に開示された技術は、発毛又は育毛促進用組成物を製造するための、前記化学式で表されるアッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）及びテアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）からなる群より選択される一つ以上の用途を提供する。 In still another aspect, the technique disclosed in the present specification is for producing a composition for promoting hair growth or hair growth, which is represented by the above chemical formula, Assam saponin B (Assa saponin B), Theasaponin E1 (Theasaponin E1). , One or more uses selected from the group consisting of: Theasaponin E2, Assamsaponin H, Assamsaponin D, and Theasaponin C1.
また、一側面において、本明細書に開示された技術は、前記化学式で表されるアッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）及びテアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）からなる群より選択される一つ以上を有効成分として含む抗炎用組成物を提供する。 In addition, in one aspect, the technology disclosed in the present specification provides the assamsaponin B (Assamsaponin B), theasasaponin E1 (theasaponin E2), and the assamsaponin H (Assamsapon H) that are represented by the chemical formulas. ), Assamsaponin D (Assasaponin D) and Theasaponin C1 (Theasaponin C1) are provided as an active ingredient.
他の側面において、本明細書に開示された技術は、抗炎に用いるための、前記化学式で表されるアッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）及びテアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）からなる群より選択されるいずれか一つ以上を提供する。 In another aspect, the technology disclosed herein is for use in anti-inflammatory, assamsaponin B (Assasaponin B), theasaponin E1 (theasaponin E1), theasaponin E2 (Theasaponin E2), represented by the above formula. There is provided at least one selected from the group consisting of Assamsaponin H, Assamsaponin D, and Theasaponin C1.
また他の側面において、本明細書に開示された技術は、前記化学式で表されるアッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）及びテアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）からなる群より選択される一つ以上、又はこれらを有効成分として含む抗炎用組成物を、炎症の緩和が必要な個体に投与することを含む炎症緩和方法を提供する。本発明の一側面における前記投与は、本明細書に記載された投与方法及び投与用量に従って行われていてよい。 In still another aspect, the technology disclosed in the present specification provides an assamsaponin B (Assamsaponin B), a theasaponin E1 (theasaponin E1), a theasaponin E2 (thesasaponin E2), and an assamsaponin H (Assamsapn H). ), One or more selected from the group consisting of Assamsaponin D and Theasaponin C1 or an anti-inflammatory composition containing these as an active ingredient is administered to an individual in need of alleviation of inflammation. A method for alleviating inflammation is provided. The administration according to one aspect of the present invention may be performed according to the administration method and administration dose described in the present specification.
また他の側面において、本明細書に開示された技術は、抗炎用組成物を製造するための、前記化学式で表されるアッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）及びテアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）からなる群より選択される一つ以上の用途を提供する。 In still another aspect, the technique disclosed in the present specification provides an assamsaponin B (Thesasaponin E1), a theasaponin E2, or a theasaponin E2 represented by the above chemical formula for producing an anti-flame composition. (Theasaponin E2), Assamsaponin H (Assassaponin H), Assamsaponin D (Assamasponin D), and thesaponin C1 (Theasaponin C1) are provided in one or more applications.
例示的な一具現例によれば、前記有効成分は、椿種子（Ｃａｍｅｌｌｉａ Ｓｅｅｄ）抽出物から分離されたものであってよい。椿種子抽出物から分離されたサポニンのＡｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ又はＴｈｅａｓａｐｏｎｉｎ Ｃ１は、椿種子から水又は有機溶媒を用いてサポニンを含有する抽出物を収得する段階；及び前記抽出物からＡｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１を分離する段階；を含む製造方法によって製造されていてよい。 According to an exemplary embodiment, the active ingredient may be separated from Camellia Seed extract. The saponins isolated from the camellia seed extract are Assamaponin B, Theasaponin E1, Theasaponin E2, Assasaponin H, Assasaponin D, or Asasasaponin D or Theasaponin C1 which is a saponin extracted from the camellia seeds; And a step of separating Assasaponin B, Theasasaponin E1, Theasaponin E2, Assasaponin H, Assasaponin D, and Theasaponin C1 from the extract.
前記椿種子からサポニンを含有する抽出物を収得する段階は、通常の技術者が当該技術分野において用いられている抽出物の製造方法から適宜選択して適宜適用、変形、又は応用することができる。 The step of obtaining the saponin-containing extract from the camellia seeds can be appropriately applied, modified, or applied by an ordinary technician by appropriately selecting from the extract manufacturing methods used in the art. ..
例示的な一具現例によれば、前記有機溶媒は、エタノール、メタノール、ブタノール、エーテル、エチルアセテート、及びクロロホルムからなる群より選択された一つ以上の有機溶媒又はこれらと水との混合物であって、一側面において５０％エタノールを用いていてよい。 According to an exemplary embodiment, the organic solvent is at least one organic solvent selected from the group consisting of ethanol, methanol, butanol, ether, ethyl acetate, and chloroform, or a mixture thereof with water. Thus, in one aspect 50% ethanol may be used.
また、例示的な一具現例によれば、溶媒を用いて分画した後、減圧濃縮して溶媒を除去して生成物を収得した後、収得された粗生成物をＣ１８カラムクロマトグラフィー（アセトニトリル：水＝８：１〜４：１）にて分離して、Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１を収得していてよい。 In addition, according to an exemplary embodiment, after fractionating with a solvent and concentrating under reduced pressure to remove the solvent to obtain a product, the obtained crude product is subjected to C18 column chromatography (acetonitrile). : Water = 8: 1 to 4: 1) to obtain Assemsaponin B, Theasaponin E1, Theasaponin E2, Assemsaponin H, Assemsaponin D, and Theasaponin C1.
例示的な一具現例によれば、前記組成物は、毛嚢毛乳頭細胞を増殖させるものであってよい。前記組成物は、毛嚢毛乳頭細胞を増殖させてケラチン形成細胞を活性化し、毛髪成長因子ＶＥＧＦの発現を増進させて毛髪の生成を促進する効果がある。また、前記組成物は、毛髪の成長周期のうち休止期から成長期に移行する周期を短縮させて毛髪の成長を促進させ、脱毛を予防又は改善する効果がある。 According to an exemplary embodiment, the composition may proliferate hair follicle papilla cells. The composition has the effects of proliferating hair follicle papilla cells and activating keratinocytes, enhancing expression of the hair growth factor VEGF, and promoting hair production. Further, the composition has an effect of preventing the hair loss or improving hair loss by shortening the cycle of transition from the resting phase to the growing phase in the hair growth cycle to promote hair growth.
例示的な一具現例によれば、前記組成物は、ＰＧＥ２、ＩＬ−６又はＩＬ−８の生成を抑制するものであってよい。 According to an exemplary embodiment, the composition may suppress the production of PGE2, IL-6 or IL-8.
例示的な一具現例によれば、前記有効成分は、組成物の総質量を基準として０．００１〜２０質量％の範囲で含まれていてよい。他の一具現例によれば、前記有効成分は、組成物の総質量を基準として０．０１〜１５質量％、０．０１〜１０質量％、又は０．１〜５質量％の範囲で含まれていてよい。 According to an exemplary embodiment, the active ingredient may be included in the range of 0.001 to 20% by weight based on the total weight of the composition. According to another embodiment, the active ingredient is included in the range of 0.01 to 15% by mass, 0.01 to 10% by mass, or 0.1 to 5% by mass based on the total mass of the composition. It may be.
一側面において、本明細書に開示される組成物に含まれる有効成分は、組成物の総質量を基準として０．００１質量％以上、０．０１質量％以上、０．１質量％以上、又は１．０質量％以上含まれていてよく、他の一側面において、２０質量％以下、１５質量％以下、１０質量％以下、又は５質量％以下含まれていてよい。前記含有量に特に限定されるものではないが、含有量が０．００１質量％以上含まれることで組成物の発毛又は育毛、抗炎効果に優れ、また、２０質量％以下で含まれることで安全性又は剤形上の製造が容易であり且つ副作用を生じることなく優れた効能を示すことができる。 In one aspect, the active ingredient included in the compositions disclosed herein is 0.001 wt% or more, 0.01 wt% or more, 0.1 wt% or more, based on the total weight of the composition, or 1.0 mass% or more may be contained, and in another aspect, 20 mass% or less, 15 mass% or less, 10 mass% or less, or 5 mass% or less may be contained. Although the content is not particularly limited, the content of 0.001% by mass or more is excellent in hair growth or hair growth of the composition, the anti-inflammatory effect, and 20% by mass or less. It is safe and easy to manufacture in dosage form, and can exhibit excellent efficacy without causing side effects.
例示的な一具現例によれば、前記組成物は薬学組成物であってよい。 According to one exemplary embodiment, the composition may be a pharmaceutical composition.
前記薬学組成物は、本明細書に開示された有効成分の他に、防腐剤、安定化剤、水和剤又は乳化促進剤、浸透圧調節のための塩及び／又は緩衝剤などの薬剤学的補助剤、並びにその他治療的に有用な物質を更に含有していてよく、通常の方法に従って多様な経口投与剤又は非経口投与剤の形態で剤形化していてよい。 In addition to the active ingredients disclosed herein, the pharmaceutical composition is a pharmaceutical composition such as a preservative, a stabilizer, a hydrating agent or an emulsifying agent, a salt for adjusting osmotic pressure, and / or a buffering agent. The present invention may further contain a therapeutic adjuvant, as well as other therapeutically useful substances, and may be formulated into various oral administration agents or parenteral administration agents according to a conventional method.
前記経口投与剤は、例えば、錠剤、丸剤、硬質及び軟質カプセル剤、液剤、懸濁剤、乳化剤、シロップ剤、粉剤、散剤、細粒剤、顆粒剤、ペレット剤などがあり、これらの剤形は、有効成分の他に、界面活性剤、希釈剤（例：ラクトース、デキストロース、スクロース、マンニトール、ソルビトール、セルロース及びグリシン）、滑沢剤（例：シリカ、タルク、ステアリン酸及びそのマグネシウム又はカルシウム塩、並びにポリエチレングリコール）を含有していてよい。錠剤は、また、マグネシウムアルミニウムシリケート、澱粉ペースト、ゼラチン、トラガカンス、メチルセルロース、ナトリウムカルボキシメチルセルロース及びポリビニルピロリジンといった結合剤を含有していてよく、場合に応じて、澱粉、寒天、アルギン酸又はそのナトリウム塩といった崩解剤、吸収剤、着色剤、香味剤、及び甘味料などの薬剤学的添加剤を含有していてよい。前記錠剤は、通常の混合、顆粒化又はコーティング方法によって製造されていてよい。 Examples of the orally-administered agent include tablets, pills, hard and soft capsules, solutions, suspensions, emulsifiers, syrups, powders, powders, fine granules, granules and pellets. As for the form, in addition to the active ingredient, surfactants, diluents (eg lactose, dextrose, sucrose, mannitol, sorbitol, cellulose and glycine), lubricants (eg silica, talc, stearic acid and its magnesium or calcium) Salt, as well as polyethylene glycol). Tablets may also contain binders such as magnesium aluminum silicate, starch paste, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose and polyvinylpyrrolidine, and in some cases, starch, agar, alginic acid or its sodium salt. It may contain pharmaceutical additives such as solubilizers, absorbents, coloring agents, flavoring agents, and sweeteners. The tablets may be manufactured by conventional mixing, granulating or coating methods.
また、前記非経口投与形態としては、経皮投与型剤形であってよく、例えば、注射剤、点滴剤、軟膏、ローション、ゲル、クリーム、スプレー、懸濁剤、乳剤、坐剤、パッチなどの剤形であってよいが、これらに限定されるものではない。 The parenteral dosage form may be a transdermal dosage form, for example, injections, drops, ointments, lotions, gels, creams, sprays, suspensions, emulsions, suppositories, patches and the like. However, the dosage form is not limited to these.
前記薬学組成物は、非経口、直腸、局所、経皮、皮下などに投与されていてよい。本発明の一実施例に係る薬学組成物は、例えば、頭皮に局所投与されていてよい。 The pharmaceutical composition may be administered parenterally, rectally, topically, transdermally, subcutaneously and the like. The pharmaceutical composition according to one embodiment of the present invention may be locally administered to the scalp, for example.
前記有効成分の投与量の決定は、通常の技術者の水準内にあり、薬物の１日投与用量は、投与しようとする対象の進行程度、発症時期、年齢、健康状態、合併症などの多様な要因によって異なるが、成人を基準としたとき、一側面において、前記組成物１μｇ／ｋｇ〜２００ｍｇ／ｋｇ、他の側面において、５０μｇ／ｋｇ〜５０ｍｇ／ｋｇを、１日１〜３回に分割して投与していてよく、前記投与量は、いかなる方法であれ、本発明の範囲を限定するものではない。 The determination of the dose of the active ingredient is within the level of ordinary skill in the art, and the daily dose of the drug varies depending on the degree of progress, onset, age, health condition, complications, etc. of the subject to be administered. Although it depends on various factors, the composition is divided into 1 μg / kg to 200 mg / kg in one aspect and 50 μg / kg to 50 mg / kg in another aspect 1 to 3 times a day based on an adult. The dose is not limited to the scope of the present invention by any method.
前記薬学組成物は皮膚外用剤であってよく、前記皮膚外用剤とは、皮膚外部において塗布されるものであればいかなるものであっても含まれ得るものの総称であって、多様な剤形の医薬品がこれに含まれ得る。 The pharmaceutical composition may be an external preparation for the skin, and the external preparation for the skin is a general term for anything that can be included as long as it is applied on the outside of the skin, and has various dosage forms. Pharmaceutical products may be included in this.
例示的な一具現例によれば、前記組成物は化粧料組成物であってよい。 According to an exemplary embodiment, the composition may be a cosmetic composition.
前記化粧料組成物には、本明細書に開示された有効成分の他、機能性添加物及び一般的な化粧料組成物に含まれる成分が更に含まれていてよい。前記機能性添加物としては、水溶性ビタミン、油溶性ビタミン、高分子ペプチド、高分子多糖、スフィンゴ脂質及び海藻エキスからなる群より選択された成分を含んでいてよい。これらの他に含まれる配合成分としては、油脂成分、保湿剤、エモリエント剤、界面活性剤、有機及び無機顔料、有機粉体、紫外線吸収剤、防腐剤、殺菌剤、酸化防止剤、植物抽出物、ｐＨ調整剤、アルコール、色素、香料、血行促進剤、冷感剤、制汗剤、精製水などが挙げられる。 In addition to the active ingredients disclosed herein, the cosmetic composition may further include functional additives and ingredients contained in general cosmetic compositions. The functional additive may include a component selected from the group consisting of water-soluble vitamins, oil-soluble vitamins, polymeric peptides, polymeric polysaccharides, sphingolipids and seaweed extracts. Other components contained in these include fats and oils, moisturizers, emollients, surfactants, organic and inorganic pigments, organic powders, ultraviolet absorbers, preservatives, bactericides, antioxidants, plant extracts. , PH adjusting agents, alcohols, dyes, fragrances, blood circulation promoters, cooling sensations, antiperspirants, purified water and the like.
前記化粧料組成物は、その剤形において特に限定されることなく、目的とするところに応じて適宜選択してよい。例えば、スキンローション、スキンソフナー、スキントナー、アストリンゼント、ローション、ミルクローション、モイスチャーローション、栄養ローション、マッサージクリーム、栄養クリーム、モイスチャークリーム、ハンドクリーム、ファウンデーション、エッセンス、栄養エッセンス、パック、石鹸、クレンジングフォーム、クレジングローション、クレンジングクリーム、ボディーローション及びボディークレンザーからなる群より選択されたいずれか一つ以上の剤形で製造されていてよいが、これらに制限されるものではない。 The cosmetic composition is not particularly limited in its dosage form and may be appropriately selected depending on the intended purpose. For example, skin lotion, skin softener, skin toner, astringent, lotion, milk lotion, moisture lotion, nourishing lotion, massage cream, nourishing cream, moisturizing cream, hand cream, foundation, essence, nourishing essence, pack, soap, cleansing foam, It may be prepared in any one or more dosage forms selected from the group consisting of crazing lotion, cleansing cream, body lotion and body cleanser, but is not limited thereto.
本発明の剤形がペースト、クリームまたはゲルである場合には、担体成分として動物繊維、植物繊維、ワックス、パラフィン、澱粉、トラガカント、セルロース誘導体、ポリエチレングリコール、シリコン、ベントナイト、シリカ、タルクまたは酸化亜鉛などが利用されていてよい。 When the dosage form of the present invention is a paste, cream or gel, as a carrier component, animal fiber, vegetable fiber, wax, paraffin, starch, tragacanth, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide. Etc. may be used.
本発明の剤形がパウダーまたはスプレーである場合には、担体成分として、ラクトース、タルク、シリカ、アルミニウムヒドロキシド、カルシウムシリケートまたはポリアミドパウダーが利用されていてよく、特に、スプレーである場合には、更にクロロフルオロヒドロカーボン、プロパン／ブタンまたはジメチルエーテルといった推進剤を含んでいてよい。 When the dosage form of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component, particularly when it is a spray, It may also contain propellants such as chlorofluorohydrocarbons, propane / butane or dimethyl ether.
本発明の剤形が溶液または乳濁液である場合には、担体成分として、溶媒、溶媒和剤または乳濁化剤が利用されていてよく、例えば、水、エタノール、イソプロパノール、エチルカーボネート、酢酸エチル、ベンジルアルコール、ベンジルベンゾエート、プロピレングリコール、１,３−ブチルグリコールオイル、グリセロール脂肪族エステル、ポリエチレングリコールまたはソルビタンの脂肪酸エステルがある。 When the dosage form of the present invention is a solution or emulsion, a solvent, a solvating agent or an emulsifying agent may be used as a carrier component, and examples thereof include water, ethanol, isopropanol, ethyl carbonate and acetic acid. There are fatty acid esters of ethyl, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3-butyl glycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan.
本発明の剤形が懸濁液である場合には、担体成分として、水、エタノールまたはプロピレングリコールといった液状希釈剤、エトキシル化イソステアリルアルコール、ポリオキシエチレンソルビトールエステル及びポリオキシエチレンソルビタンエステルといった懸濁剤、微小結晶性セルロース、アルミニウムメタヒドロキシド、ベントナイト、アガーまたはトラガカントなどが利用されていてよい。 When the dosage form of the present invention is a suspension, water, a liquid diluent such as ethanol or propylene glycol, an ethoxylated isostearyl alcohol, a polyoxyethylene sorbitol ester and a polyoxyethylene sorbitan ester are suspended as carrier components. Agents, microcrystalline cellulose, aluminum metahydroxide, bentonite, agar or tragacanth and the like may be utilized.
本発明の剤形が界面活性剤含有クレンジングである場合には、担体成分として、脂肪族アルコールスルフェート、脂肪族アルコールエーテルスルフェート、スルホコハク酸モノエステル、イセチオネート、イミダゾリニウム誘導体、メチルタウレート、サルコシネート、脂肪酸アミドエーテルスルフェート、アルキルアミドベタイン、脂肪族アルコール、脂肪酸グリセリド、脂肪酸ジエタノールアミド、植物性油、リノリン誘導体またはエトキシル化グリセロール脂肪酸エステルなどが利用されていてよい。 When the dosage form of the present invention is a surfactant-containing cleansing agent, as a carrier component, aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyl taurate, Sarcosinates, fatty acid amide ether sulphates, alkylamide betaines, fatty alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, linolin derivatives or ethoxylated glycerol fatty acid esters may be used.
例示的な一具現例によれば、前記組成物は食品組成物であってよい。 According to one exemplary embodiment, the composition may be a food composition.
前記食品組成物は、液状または固状の剤形であってよく、例えば、各種の食品類、飲料、ガム、茶、ビタミン複合剤、健康補助食品類などがあり、粉末、顆粒、錠剤、カプセルまたは飲料の剤形であってよい。各剤形の食品組成物は、本明細書に開示された有効成分の他、当該分野で通常に用いられる成分を剤形または使用目的に応じて当業者が難なく適宜選定して配合していてよく、他の原料と同時に適用した場合、相乗効果が生じることがある。 The food composition may be in a liquid or solid dosage form, for example, various foods, beverages, gums, teas, vitamin complex agents, dietary supplements, etc., powders, granules, tablets, capsules. Alternatively, it may be in the form of a beverage. The food composition of each dosage form, in addition to the active ingredients disclosed herein, those commonly used in the art are appropriately selected and blended by those skilled in the art without difficulty according to the dosage form or purpose of use. Often, when applied at the same time as other ingredients, a synergistic effect may occur.
本明細書に開示された有効成分の他に含有していてよい液状成分には、特に制限点がなく、通常の飲料と同様、種々の香味剤または天然炭水化物などを追加成分として含んでいてよい。前記天然炭水化物の例としては、ブドウ糖、果糖などの単糖、マルトース、スクロースなどの二糖、多糖、デキストリン、シクロデキストリンなどの通常の糖、及びキシリトール、ソルビトール、エリトリトールなどの糖アルコールである。前記した香味剤としては天然香味剤（タウマチン、ステビア抽出物（例えば、レバウディオシドＡ、グリチルリチンなど）及び合成香味剤（サッカリン、アスパルテームなど）を有利に用いていてよい。前記天然炭水化物の割合は、本明細書に開示された組成物１００ｍｌ当り一般的に約１〜２０ｇ、一側面において５〜１２ｇであってもよい。 The liquid component that may be contained in addition to the active ingredient disclosed herein is not particularly limited, and may contain various flavors or natural carbohydrates as additional components, similar to ordinary beverages. .. Examples of the natural carbohydrates are monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, ordinary sugars such as polysaccharides, dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol and erythritol. As the above-mentioned flavoring agents, natural flavoring agents (thaumatin, stevia extract (eg rebaudioside A, glycyrrhizin etc.) and synthetic flavoring agents (saccharin, aspartame etc.) may be advantageously used. Generally about 1 to 20 g, and in one aspect 5 to 12 g may be present per 100 ml of the composition disclosed herein.
前記食品組成物は、一側面において、種々の栄養剤、ビタミン、鉱物（電解質）、合成風味剤及び天然風味剤などの風味剤、着色剤及び充填剤（チーズ、チョコレートなど）、ペクチン酸及びその塩、アルギン酸及びその塩、有機酸、保護性コロイド増粘剤、ｐＨ調節剤、安定化剤、防腐剤、グリセリン、水、炭酸飲料に使用される炭酸化剤などを含んでいてよい。他の側面において、天然果実ジュース、果実ジュース飲料、野菜飲料を製造するための果肉を含んでいてよい。これらの成分は単独で又は組み合わせて用いられていてよい。前記添加剤の割合は多様であってよいが、本明細書に開示された組成物１００重量部当たり０．００１〜約２０重量部の範囲で選択されるのが一般的である。 The food composition, in one aspect, various nutrients, vitamins, minerals (electrolytes), flavoring agents such as synthetic flavoring agents and natural flavoring agents, coloring agents and fillers (cheese, chocolate, etc.), pectic acid and the like. It may contain salts, alginic acid and its salts, organic acids, protective colloid thickeners, pH adjusters, stabilizers, preservatives, glycerin, water, carbonating agents used in carbonated drinks, and the like. In another aspect, it may include pulp for making natural fruit juices, fruit juice drinks, vegetable drinks. These components may be used alone or in combination. The ratio of the additives may vary, but is generally selected in the range of 0.001 to about 20 parts by weight per 100 parts by weight of the composition disclosed herein.
以下、実施例を通して本発明をより詳細に説明する。なお、これらの実施例は本発明を例示するためのものに過ぎず、本発明の範囲がこれらの実施例によって制限されると解釈されないのは当業界における通常の知識を有する者にとって自明であろう。 Hereinafter, the present invention will be described in more detail through examples. It should be noted that these examples are merely for the purpose of illustrating the present invention, and it is obvious to those having ordinary skill in the art that the scope of the present invention should not be construed as being limited by these examples. Let's do it.
製造例１．アッサムサポニンＢ（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ）、テアサポニンＥ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１）、テアサポニンＥ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２）、アッサムサポニンＨ（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ）、アッサムサポニンＤ（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ）、テアサポニンＣ１（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１）の製造
椿種子（Ｃａｍｅｌｌｉａ Ｓｅｅｄ）１ｋｇにヘキサン３Ｌを入れ、常温で攪拌抽出して脱脂させた後、脱脂された椿種子０．５ｋｇに５０％エタノール４Ｌを入れ、３回還流抽出した後、１５℃で１日間浸漬させた。その後、ろ過布によるろ過と遠心分離を通じて残渣とろ液とを分離し、分離されたろ液を減圧濃縮して、椿種子抽出物を得た。
Production Example 1. Assamsaponin B (Assasaponin B), Theasaponin E1 (Theasaponin E1), Theasaponin E2 (Theasaponin E2), Assamsaponin H (Assaponin C) (Assaponin C) Seed) 1 kg of hexane and 3 L of hexane were stirred and extracted at room temperature for defatting, and 0.5 kg of defatted camellia seeds was added with 4 L of 50% ethanol, reflux extracted three times, and then immersed at 15 ° C. for 1 day. It was Then, the residue and the filtrate were separated through filtration with a filter cloth and centrifugation, and the separated filtrate was concentrated under reduced pressure to obtain a camellia seed extract.
次いで、前記得られた椿種子抽出物７．３７ｇを水に懸濁してｎ−ＢｕＯＨで分画を実施し、確保したＢｕＯＨ可用分画２．５４ｇのうち１．４０ｇに対し溶出溶媒３５％ ＭｅＯＨでＲＰ ＭＰＬＣを実施した。そのうちＢ４小分画に対し溶出溶媒ＣＭＩＷ＝９：６：１：４（＋０．２％ ａｃｅｔｉｃ ａｃｉｄ）条件でＨＰＣＣＣを実施した。このようにして得た小分画Ｂ４１、Ｂ４２、Ｂ４３、及びＢ４４をそれぞれのＨＰＬＣ条件で精製した結果、Ｂ４１ｐ１（１．６ｍｇ）、Ｂ４１ｐ２（Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、３．９ｍｇ）、Ｂ４２ｐ１（Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、１２．８ｍｇ）、Ｂ４２ｐ２（Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、５．６ｍｇ）、Ｂ４３ｐ２（Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、２．２ｍｇ）、Ｂ４３ｐ３（Ｃａｍｅｌｌｉａｓａｐｏｎｉｎ Ｂ１、１．６ｍｇ）、Ｂ４４ｐ１（Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、３ｍｇ）、Ｂ４４ｐ２（Ｔｈｅａｓａｐｏｎｉｎ Ｃ１、１．６ｍｇ）の総８種の物質を収得した（下記の図式参照）。 Next, 7.37 g of the obtained camellia seed extract was suspended in water and fractionated with n-BuOH, and 1.40 g of the 2.54 g of the available BuOH usable fraction was dissolved in 35% MeOH as an elution solvent. RP MPLC was performed at. Among them, HPCCC was performed on the B4 small fraction under the condition of elution solvent CMIW = 9: 6: 1: 4 (+ 0.2% acetic acid). The small fractions B41, B42, B43, and B44 thus obtained were purified under the respective HPLC conditions, and as a result, B41p1 (1.6 mg), B41p2 (Assamsaponin B, 3.9 mg), B42p1 (Theasaponin E1, 12). .8 mg), B42p2 (Theasaponin E2, 5.6 mg), B43p2 (Assamsaponin H, 2.2 mg), B43p3 (Camelliasasaponin B1, 1.6 mg), B44p1 (Assamsaponin D, 3 mg), B44p2 (B44p1). ) Were obtained (see the diagram below).
試験例１．毛乳頭細胞における毛髪成長因子ＶＥＧＦの発現増加
Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１が、血管形成に必要な成長因子であって毛髪の成長期に移動するのに必要な成長因子である血管内皮増殖因子（Ｖａｓｃｕｌａｒ ｅｎｄｏｔｈｅｌｉａｌ ｇｒｏｗｔｈ ｆａｃｔｏｒ；ＶＥＧＦ）を発現させる程度を評価するために、生体外（ｉｎ ｖｉｔｒｏ）システムを適用して、椿種子サポニン由来のＡｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１の効能を評価した。
Test Example 1. Increased expression of hair growth factor VEGF in hair papilla cells Assamaponin B, Theasaponin E1, Theasaponin E2, Assamasponin H, Assasaponin D, Thesasaponin C1 are growth factors necessary for the hair growth required for angiogenesis, which is a growth factor necessary for the migration of hair. In vitro system was applied to evaluate the degree of expression of various growth factors such as Vascular endothelium growth factor (VEGF), and camellia seed saponin-derived Assamsponin B, Theasaponin E1, The efficacy of Theasaponin E2, Assamaponin H, Assamaponin D, Theasaponin C1 was evaluated.
前記実験のために、４７歳の男性の毛乳頭真皮細胞（Ｄｅｒｍａｌ Ｐａｐｉｌｌａ Ｃｅｌｌ；ＤＰＣ）（Ｐ．１１）４×１０５ｃｅｌｌを、１２ウェルプレートにシーディング（ｓｅｅｄｉｎｇ）し、１０％ＦＢＳ（ｆｅｔａｌ ｂｏｖｉｎｅ ｓｅｒｕｍ）を含有するＤＭＥＭ（Ｄｕｌｂｅｃｃｏ'ｓ ｍｏｄｉｆｉｅｄ Ｅａｇｌｅ'ｓ ｍｅｄｉｕｍ）培地において一晩培養した。培養後、椿種子サポニン由来のＡｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１をそれぞれ２０ｐｐｍで処理した。比較例としてＴｈｅａｓａｐｏｎｉｎを使用し、陰性対照群としてはＤＭＳＯを使用した。 For the experiment, 4 × 10 5 cells of a 47-year-old male dermal papilla cell (DPC) (P.11) were seeded in a 12-well plate and 10% FBS (fetal). The cells were cultured overnight in DMEM (Dulbecco's modified Eagle's medium) medium containing bovine serum. After culturing, the camellia seed saponin-derived Assamsaponin B, Theasasponin E1, Theasaponin E2, Assassaponin H, Assassaponin D, and Thesasaponin C1 were each treated with 20 ppm. Theasaponin was used as a comparative example, and DMSO was used as a negative control group.
２４時間後、椿種子サポニン由来のＡｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１が処理された混合液を収集（ｓｏｕｐ ｃｏｌｌｅｃｔ）し、ＶＥＧＦ ＥＬＩＳＡ（Ｖａｓｃｕｌａｒ ｅｎｄｏｔｈｅｌｉａｌ ｇｒｏｗｔｈ ｆａｃｔｏｒ Ｅｎｚｙｍｅ−Ｌｉｎｋｅｄ Ｉｍｍｕｎｏｓｏｒｂｅｎｔ Ａｓｓａｙ；Ｒ＆Ｄ ｂｉｏｓｙｓｔｅｍｓ）を使用して、ＶＥＧＦ発現程度を確認した。その結果を下記の表１に表した。 After 24 hours, Assamsaponin B from Tane Tsubaki saponin, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, collecting mixture Theasaponin C1 is processed (soup collect), VEGF ELISA (Vascular endothelial growth factor Enzyme-Linked The degree of VEGF expression was confirmed using an Immunosorbent Assay; R & D biosystems). The results are shown in Table 1 below.
表１から見られるように、Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１は、比較例及び対照群と比較して、顕著な効果の差があることが分かり、具体的に、毛乳頭細胞における毛髪成長因子ＶＥＧＦの発現を約３倍以上増加させた。したがって、Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１は、優れた毛髪生成促進能を有することが分かる。 As can be seen from Table 1, it is clear that the Assamsponnin B, Theasaponin E1, Theasaponin E2, Assemsaponin H, Assamsaponin D, Theasaponin C1 have a significant difference in effect as compared with the comparative example and the control group. In addition, the expression of hair growth factor VEGF in hair papilla cells was increased by about 3-fold or more. Therefore, it can be seen that Assamaponin B, Theasaponin E1, Theasaponin E2, Assamaponin H, Assamsaponin D, and Theasaponin C1 have excellent hair formation promoting ability.
試験例２．毛嚢毛乳頭細胞増殖
毛髪を構成するケラチン蛋白質は、毛根部ケラチン形成細胞（ｋｅｒａｔｉｎｏｃｙｔｅ）で生成され、このケラチン形成細胞は毛乳頭細胞から分化する。したがって、Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１が毛乳頭細胞の活性を促進するのであれば、それから分化するケラチン形成細胞の活性を促進させることができ、ひいては毛髪生成を促進させることができる。そこで、Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１の毛乳頭細胞活性促進効果を、下記のように評価した。
Test example 2. Proliferation of hair follicle papilla cells The keratin protein that constitutes hair is produced by hair root keratinocytes, and the keratinocytes differentiate from the papilla cells. Therefore, if Assemsaponin B, Theasaponin E1, Theasaponin E2, Assemsaponin H, Assemsaponin D, Theasaponin C1 promotes the activity of hair papilla cells, the keratinocyte that differentiates from them can stimulate the activity of keratinocytes, Can be promoted. Therefore, the hair papilla cell activity-promoting effect of Assemsaponin B, Theasaponin E1, Theasaponin E2, Assemsaponin H, Assemsaponin D, and Theasaponin C1 was evaluated as follows.
まず、本試験例においては、ヒト毛乳頭細胞（Ｈｕｍａｎ ｄｅｒｍａｌ ｐａｐｉｌｌａ ｃｅｌｌ；ｈＤＰｃ、ソウル大学校のグォン・オサン教授から入手）細胞株を使用して実験を行った。前記細胞株は、１０％ウシ胎児血清（ＦＢＳ）が含有されたＤｕｌｂｅｃｃｏ'ｓ ｍｏｄｉｆｉｅｄ Ｅａｇｌｅ'ｓ ｍｅｄｉｕｍ（ＤＭＥＭ；Ｇｉｂｃｏ ＢＲＬ、Ｇａｉｔｈｅｒｓｂｕｒｇ、ＭＤ、ＵＳＡ）において、５％ＣＯ２、３７℃で維持されるインキュベータで２４時間培養した後、椿種子サポニン由来のＡｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１を２０ｐｐｍでそれぞれ処理した。比較例としてＴｈｅａｓａｐｏｎｉｎを使用し、陰性対照群としてはＤＭＳＯを使用した。 First, in this test example, an experiment was performed using a human dermal papilla cell (hDPc, obtained from Professor Gwon Ossan of Seoul National University) cell line. The cell line is maintained at 37 ° C. in 5% CO 2 in Dulbecco's modified Eagle's medium (DMEM; Gibco BRL, Gaithersburg, MD, USA) containing 10% fetal bovine serum (FBS). After culturing for 24 hours in an incubator, camellia seed saponin-derived Assassaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, and Theasaponin C1 were treated with 20 ppm, respectively. Theasaponin was used as a comparative example, and DMSO was used as a negative control group.
試験物質を処理してから２４時間経過後、ＷＳＴ−１キット（Ｒｏｃｈｅ）を使用して、細胞増殖能（％）を測定し、その結果を表２に表した。 After 24 hours from the treatment with the test substance, the cell growth ability (%) was measured using the WST-1 kit (Roche), and the results are shown in Table 2.
表２から見られるように、Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１は、比較例及び対照群と比較して、約１．５倍以上高い毛乳頭細胞増殖増加率を示した。これは、Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１が、毛乳頭細胞の増殖を促進させることができ、且つケラチン形成細胞の活性及び毛髪の生成もより効果的に促進することができることを意味する。 As can be seen from Table 2, the hair papilla cells having a proliferation rate of about 1.5 times higher than those of the comparative example and the control group, the hair papilla cells were higher than those of the comparative example and the control group by about 1.5 times as much as those of the comparison group and the control group. showed that. This is because Assamaponin B, Theasaponin E1, Theasaponin E2, Assamaponin H, Assamaponin D, Theasaponin C1 can promote the growth of hair papilla cells, and also the activity of keratinogenic cells and the effect of hair-forming cells on keratin formation. Means that you can do it.
試験例３．人体毛嚢器官における毛髪成長促進
本試験例においては、実際の人体毛嚢器官における毛髪成長促進能を確認した。
５５歳の男性の後頭部頭皮組織から毛嚢器官を一つずつ分離して、Ｗｉｌｌｉａｍ'ｓ Ｅ培地（Ｌ−グルタミン（２ｍＭ）、インスリン（１０μｇ／ｍｌ）、ヒドロコルチゾン（４０ｎｇ／ｍｌ）、抗生剤（１％）、抗真菌剤（１％）含有）で培養した。培養後３日目に成長が起こった毛嚢を選別して３ｍｍに切り、選別した毛嚢組織に対して、薬品処理を施していない場合を対照群とし、椿種子サポニン由来のＡｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１ ５ｐｐｍ、比較例としてＴｈｅａｓａｐｏｎｉｎをそれぞれ処理した。そして、処理して８日後、それぞれの長さの測定及び写真撮影を行った。その結果を表３に表した。
Test example 3. Promotion of Hair Growth in Human Hair Follicle Organ In this test example, the ability to promote hair growth in an actual human hair follicle organ was confirmed.
Hair follicle organs were separated from the occipital scalp tissue of a 55-year-old man one by one, and William's E medium (L-glutamine (2 mM), insulin (10 μg / ml), hydrocortisone (40 ng / ml), antibiotic ( 1%), containing antifungal agent (1%)). Hair follicles that had grown on the 3rd day after culture were selected and cut into 3 mm, and the selected hair follicle tissues were not subjected to chemical treatment as a control group, and camellia seed saponin-derived Assamsaponin B and Theasaponin were used. E1, Theasaponin E2, Assamaponin H, Assamaponin D, Theasaponin C1 5ppm, and Theasaponin as a comparative example were each processed. Then, 8 days after the treatment, each length was measured and photographed. The results are shown in Table 3.
その結果、表３から見られるように、毛嚢器官における毛髪の長さの増加において、Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１を処理した場合、比較例及び対照群よりも優れた毛髪成長促進効果が示された。したがって、Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１は、毛嚢において毛髪の長さの成長を促進する効果に優れることが分かる。 As a result, as can be seen from Table 3, in the increase of the hair length in the hair follicle organ, Assamaponin B, Theasaponin E1, Theasaponin E2, Assasaponin H, Assasaponin D, Theasaponin C1 and the control group were compared, and the control group was compared. A superior hair growth promoting effect was shown. Therefore, it can be seen that Assemsaponin B, Theasaponin E1, Theasaponin E2, Assemsaponin H, Assemsaponin D, Theasaponin C1 are excellent in the effect of promoting the growth of hair length in hair follicles.
試験例４．ＰＧＥ２、ＩＬ−６及びＩＬ−８生成抑制
ヒト線維芽細胞を６−ウェル培養プレートに１×１０５の細胞濃度で接種し、２４時間の間、３７℃、５％ＣＯ２インキュベータで培養した。Ｈ２Ｏ２ ５００μＭをウェルに処理して２４時間刺激を与えた後、椿種子サポニン由来のＡｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１、比較例としてＴｈｅａｓａｐｏｎｉｎをそれぞれ処理して４８時間反応させた。反応完了後、培養液を回収してＥＬＩＳＡ分析を行った。このとき、抗炎及び刺激緩和剤として多く使用される物質であるα−ビサボロール（α−ｂｉｓａｂｏｌｏｌ）を対照群として使用した。
Test example 4. Inhibition of PGE2, IL-6 and IL-8 production Human fibroblasts were inoculated into 6-well culture plates at a cell concentration of 1 × 10 5 and cultured for 24 hours at 37 ° C., 5% CO 2 incubator. The wells were treated with H 2 O 2 500 μM and stimulated for 24 hours, and then camellia seed saponin-derived Assamaponin B, Theasaponin E1, Theasaponin E2, Assamsaponin H, Assamsaponin D, Theasaponin D, Theasapon were compared, respectively. And reacted for 48 hours. After completion of the reaction, the culture solution was collected and subjected to ELISA analysis. At this time, α-bisabolol, which is a substance often used as an anti-inflammatory and stimulant alleviation agent, was used as a control group.
ＰＧＥ２はアッセイデザイン（Ａｓｓａｙ Ｄｅｓｉｇｎ）社製のキット、ＩＬ−６、ＩＬ−８はエンドゲン（Ｅｎｄｏｇｅｎ）社製のキットを使用し、各会社のマニュアルに明記された方法に従って実験を行った。抑制効果は、下記数式１に基づいて計算し、測定結果は下記の表４に表した。 For PGE2, a kit manufactured by Assay Design was used, and for IL-6 and IL-8, a kit manufactured by Endogen was used, and an experiment was performed according to the method specified in the manual of each company. The suppression effect was calculated based on the following formula 1, and the measurement results are shown in Table 4 below.
前記表４に表されたように、炎症媒介物質であるＰＧＥ２、ＩＬ−６、ＩＬ−８の生成量が、Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１の添加によって、比較例及び対照群と比較して顕著に低減し、優れた抗炎効果があることを確認することができた。 As shown in Table 4, the production amount of PGE2, IL-6, and IL-8, which are inflammation mediators, was increased by the addition of Assemsaponin B, Theasaponin E1, Theasaponin E2, Assemsaponin H, Assemsaponin D, Theinasapon. It was confirmed that the anti-inflammatory effect was significantly reduced as compared with the comparative example and the control group.
以下、本発明の一側面に係る組成物の剤形例について説明するが、他の種々の剤形へも応用可能であり、これは本発明を限定するためのものではなく、単に本発明を具体的に説明するためのものであるに過ぎない。 Hereinafter, an example of a dosage form of the composition according to one aspect of the present invention will be described, but it can be applied to various other dosage forms, and this is not intended to limit the present invention, and the present invention is simply It is only for the purpose of concrete description.
［剤形例１］シャンプー
下記表５に記載された組成に従い通常の方法にてシャンプーを製造した。
[Formulation Example 1] Shampoo A shampoo was produced by a conventional method according to the composition shown in Table 5 below.
［剤形例２］リンス
下記の表６に記載された組成に従い通常の方法にてリンスを製造した。
[Formulation Example 2] Rinse A rinse was manufactured by a usual method according to the composition shown in Table 6 below.
［剤形例３］軟膏
下記の表７に記載された組成に従い通常の方法にて軟膏を製造した。
[Formulation Example 3] Ointment An ointment was produced by a usual method according to the composition shown in Table 7 below.
［剤形例４］ヘアトニック
下記の表８に記載された組成に従い通常の方法にてヘアトニックを製造した。
[Formulation Example 4] Hair tonic A hair tonic was produced by a usual method according to the composition shown in Table 8 below.
［剤形例５］ヘアーローション
下記の表９に記載された組成に従い通常の方法にてヘアーローションを製造した。
[Formulation Example 5] Hair lotion A hair lotion was produced by a usual method according to the composition shown in Table 9 below.
［剤形例６］石鹸
下記の表１０に記載された組成に従い通常の方法にて石鹸を製造した。
[Formulation Example 6] Soap A soap was produced by a usual method according to the composition shown in Table 10 below.
［剤形例７］ローション
下記の表１１に記載された組成に従い通常の方法にてローションを製造した。
[Formulation Example 7] Lotion A lotion was produced by a usual method according to the composition shown in Table 11 below.
［剤形例８］クリーム
下記の表１２に記載された組成に従い通常の方法にてクリームを製造した。
[Formulation Example 8] Cream A cream was produced by a conventional method according to the composition shown in Table 12 below.
［剤形例９］パック
下記の表１３に記載された組成に従い通常の方法にてパックを製造した。
[Formulation Example 9] Pack A pack was produced by a usual method according to the composition shown in Table 13 below.
［剤形例１０］美容液型製剤
下記の表１４に記載された組成に従い通常の方法にて美容液型製剤を製造した。
[Dosage form example 10] Beauty essence type preparation According to the composition shown in Table 14 below, a beauty essence type preparation was produced by a usual method.
［剤形例１１］軟質カプセル剤
Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１からなる群より選択される一つ以上の化合物５０ｍｇ、Ｌ−カルニチン８０〜１４０ｍｇ、大豆油１８０ｍｇ、パーム油２ｍｇ、植物性硬化油８ｍｇ、黄蝋４ｍｇ及びレシチン６ｍｇを混合し、通常の方法に従って、１カプセル当たり４００ｍｇずつ充填して軟質カプセル剤を製造した。
[Formulation Example 11] Soft capsules One or more compounds selected from the group consisting of Assemsaponin B, Theasaponin E1, Theasaponin E2, Assemsaponin H, Assemsaponin D, Theasaponin C50mg-140mg soybean 80mg, L-carnitine, 140mg. , 2 mg of palm oil, 8 mg of hydrogenated vegetable oil, 4 mg of yellow wax, and 6 mg of lecithin were mixed, and 400 mg per capsule was filled according to a usual method to produce a soft capsule.
［剤形例１２］錠剤
Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１からなる群より選択される一つ以上の化合物５０ｍｇ、カラクトオリゴ糖２００ｍｇ、乳糖６０ｍｇ及び麦芽糖１４０ｍｇを混合し、流動層乾燥機を利用して顆粒状に造粒した後、糖エステル（ｓｕｇａｒ ｅｓｔｅｒ）を６ｍｇを添加し、打錠機で打錠して錠剤を製造した。
[Formulation Example 12] Tablets 50 mg of one or more compounds selected from the group consisting of Assemsaponin B, Theasaponin E1, Theasaponin E2, Assemsaponin H, Assemsaponin D, Theasaponin C1 and maltose sugar 60 mg, and 60 mg of lactose oligosaccharide, 200 mg of galacto-oligosaccharide, After granulating into granules using a fluid bed dryer, 6 mg of sugar ester was added and the mixture was tableted with a tableting machine to produce tablets.
［剤形例１３］顆粒剤
Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１からなる群より選択される一つ以上の化合物５０ｍｇ、無水結晶ブドウ糖２５０ｍｇ及び澱粉５５０ｍｇを混合し、流動層造粒機を使用して顆粒状に成形した後、包に充填して顆粒剤を製造した。
[Dosage form example 13] Granules 50 mg of one or more compounds selected from the group consisting of Assemsaponin B, Theasaponin E1, Theasaponin E2, Assemsaponin H, Assemsaponin D, Theasaponin C1, and 50 mg of anhydrous starch dextrose, and 50 mg of mixed crystalline glucose. After granulating using a fluidized bed granulator, the granules were manufactured by filling the granules.
［剤形例１４］ドリンク剤
Ａｓｓａｍｓａｐｏｎｉｎ Ｂ、Ｔｈｅａｓａｐｏｎｉｎ Ｅ１、Ｔｈｅａｓａｐｏｎｉｎ Ｅ２、Ａｓｓａｍｓａｐｏｎｉｎ Ｈ、Ａｓｓａｍｓａｐｏｎｉｎ Ｄ、Ｔｈｅａｓａｐｏｎｉｎ Ｃ１からなる群より選択される一つ以上の化合物５０ｍｇ、ブドウ糖１０ｇ、クエン酸０．６g、及び液状オリゴ糖２５ｇを混合した後、精製水３００ｍｌを加えて各瓶に２００ｍｌずつ充填した。瓶に充填した後、１３０℃で４〜５秒間殺菌して、ドリンク剤飲料を製造した。
[Formulation Example 14] Drink agent 50 mg of one or more compounds selected from the group consisting of Assemsaponin B, Theasaponin E1, Theasaponin E2, Assemsaponin H, Assemsaponin D, Theasaponin C1, 0.6 g of glucose, 10 g of glucose, and 10 g of glucose. After mixing 25 g of oligosaccharide, 300 ml of purified water was added and each bottle was filled with 200 ml. After filling the bottle, it was sterilized at 130 ° C. for 4 to 5 seconds to manufacture a drink beverage.
以上、本発明内容の特定の部分を詳細に記述したところ、当業者にとってこのような具体的な技術は単に好適な実施態様であるに過ぎず、これによって本発明の範囲が制限されるものではないことは明らかである。したがって、本発明の実質的な範囲は添付の請求項とそれらの等価物によって定義されるといえよう。 As described above, specific parts of the present invention have been described in detail. Such a specific technique is merely a preferred embodiment for those skilled in the art, and the scope of the present invention is not limited thereby. Clearly not. Accordingly, the substantial scope of the present invention may be defined by the appended claims and their equivalents.
Claims (9)
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| KR10-2015-0045134 | 2015-03-31 | ||
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| PCT/KR2016/002976 WO2016159567A2 (en) | 2015-03-31 | 2016-03-24 | Composition for promoting hair growth or hair restoration and for anti-inflammation |
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| JP2018511600A JP2018511600A (en) | 2018-04-26 |
| JP6697479B2 true JP6697479B2 (en) | 2020-05-20 |
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| KR (1) | KR101957849B1 (en) |
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| PH (1) | PH12017501722A1 (en) |
| SG (1) | SG11201707761WA (en) |
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| CN110531057B (en) * | 2019-07-01 | 2020-11-20 | 启迪禾美生物科技(嘉兴)有限公司 | Method for high-throughput screening of active composition for skin care products |
| KR20210131598A (en) * | 2020-04-24 | 2021-11-03 | 바이오스펙트럼 주식회사 | Composition for preventing hair loss or promoting hair growth, comprising Camellia japonica pericarp extract as an active ingredient |
| KR102480528B1 (en) * | 2020-12-30 | 2022-12-23 | 코스맥스 주식회사 | Streptococcus pneumoniae strain and its use for improving hair or scalp condition |
| KR102480529B1 (en) * | 2020-12-30 | 2022-12-23 | 코스맥스 주식회사 | Cutibacterium granulosum strain and its use for improving hair or scalp condition |
| KR102495405B1 (en) * | 2020-12-30 | 2023-02-06 | 코스맥스 주식회사 | Micrococcus luteus strain and its use for improving hair or scalp condition |
| KR102495404B1 (en) * | 2020-12-30 | 2023-02-06 | 코스맥스 주식회사 | Brevundimonas vesicularis strain and its use for improving hair or scalp condition |
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| JPS6396116A (en) * | 1986-10-11 | 1988-04-27 | Shiseido Co Ltd | Hair cosmetic |
| CN101392015B (en) * | 2008-07-22 | 2013-05-15 | 沈阳药科大学 | Triterpene saponin in camellia seeds, preparation method and medical use thereof |
| JP5685752B2 (en) * | 2009-05-13 | 2015-03-18 | ビーエイチエヌ株式会社 | Blood flow promoting agent |
| KR101274029B1 (en) | 2011-01-06 | 2013-06-12 | (주)대덕바이오 | Composition for enhancing hair growth containing saponin Rd and Re as active ingredients |
| CN103251636B (en) * | 2012-02-16 | 2015-06-10 | 浙江大学宁波理工学院 | Medicament for treating Candida infections and diseases caused by Candida, and preparation method thereof |
| KR20130122070A (en) * | 2012-04-30 | 2013-11-07 | (주)아모레퍼시픽 | Hair cosmetic composition containing extract of camellia japonica l. seed |
| CN103266154A (en) * | 2013-05-29 | 2013-08-28 | 大连工业大学 | Biological transformation method for preparing high-activity theasaponin |
| CN103385831A (en) * | 2013-07-19 | 2013-11-13 | 泉州市新益日用化妆品有限公司 | Novel oil tea shampoo and preparation method thereof |
| KR102061716B1 (en) * | 2013-08-30 | 2020-01-02 | (주)아모레퍼시픽 | Composition for promoting hair growth or restoration containing 21-o-angeloyltheasapogenol e3 |
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| MY182581A (en) | 2021-01-25 |
| CN107530258A (en) | 2018-01-02 |
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| KR101957849B1 (en) | 2019-03-15 |
| WO2016159567A2 (en) | 2016-10-06 |
| SG11201707761WA (en) | 2017-10-30 |
| CN107530258B (en) | 2021-03-16 |
| JP2018511600A (en) | 2018-04-26 |
| PH12017501722A1 (en) | 2018-03-12 |
| KR20160116834A (en) | 2016-10-10 |
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