JP6050572B2 - Elastic fiber formation promoter - Google Patents
Elastic fiber formation promoter Download PDFInfo
- Publication number
- JP6050572B2 JP6050572B2 JP2011175134A JP2011175134A JP6050572B2 JP 6050572 B2 JP6050572 B2 JP 6050572B2 JP 2011175134 A JP2011175134 A JP 2011175134A JP 2011175134 A JP2011175134 A JP 2011175134A JP 6050572 B2 JP6050572 B2 JP 6050572B2
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- Prior art keywords
- extract
- elastic fiber
- fiber formation
- algae
- acid
- Prior art date
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Description
本発明は、藻類または植物の抽出物を有効成分とする弾性線維形成促進剤に関する。 The present invention relates to an elastic fiber formation promoter comprising an algal or plant extract as an active ingredient.
藻類や植物を抽出したエキスの使用は、最近の天然志向の高まりにより、石油系合成成分に代わるとして好まれる傾向にある。そして、天然物の抽出物は、その様々な生理活性が研究され、応用されている。 The use of extracts extracted from algae and plants tends to be preferred as an alternative to petroleum-based synthetic components due to the recent increase in natural orientation. Natural extracts have been studied and applied for various physiological activities.
褐藻類、紅藻類、緑藻類などの藻類の抽出成分には、藻類特有の有効成分である、粘質多糖類、ミネラル、ビタミン等が豊富に含まれている。粘質多糖には、アルギン酸、カラギーナン、寒天などがあり、食物繊維としての作用や特定の生理活性があることが知られている。 The extracted components of algae such as brown algae, red algae, and green algae are rich in viscous polysaccharides, minerals, vitamins and the like, which are active ingredients unique to algae. The viscous polysaccharides include alginic acid, carrageenan, agar, etc., and are known to have action as dietary fiber and specific physiological activity.
例えば、紅藻類のマクリに、エラスターゼ阻害作用が見出されたことが報告されている他(特許文献1)、褐藻類および紅藻類由来の多糖類に、組織・細胞の障害を予防し及び/又は修復する機能があることが示されている(特許文献2)。 For example, it has been reported that an elastase inhibitory action has been found in red algae macri (Patent Document 1), and brown and algae-derived polysaccharides are used to prevent tissue / cell damage and / or Or it is shown that there exists a function to repair (patent document 2).
さらには、褐藻類、紅藻類、および緑藻類などから得られる海藻抽出物が、美白効果を有し、肌に対してシミ、ソバカスを軽減し、乾燥肌や湿疹・肌荒れの改善、更に、肌にツヤ・張りも与えることができることも示されている(特許文献3)。 Furthermore, seaweed extracts obtained from brown algae, red algae, green algae, etc. have a whitening effect, reduce spots and freckles on the skin, improve dry skin, eczema and rough skin, It is also shown that gloss and tension can be given (Patent Document 3).
また、特に紅藻類のカギケノリ科のアスパラゴプシス アルマタの抽出物は、細胞賦活、抗炎症作用、抗菌作用の3種の機能を有すること(特許文献4)、真皮線維芽細胞におけるコラーゲン産生促進作用があることが知られている(特許文献5および6)。 In particular, the extract of Asparagopsis arumata of the red alga Calyxaceae has three functions of cell activation, anti-inflammatory action and antibacterial action (Patent Document 4), and collagen production promoting action in dermal fibroblasts. (Patent Documents 5 and 6).
一方、植物エキスにも、各種ビタミン類、ミネラル類、糖類、油脂成分等が含まれ、各種の生理活性が知られている。その例としては、センブリ抽出物、チンピ抽出物、アーモンド抽出物、ニンジン抽出物、エンドウ抽出物、ユキノシタ抽出物、クワ抽出物等に含まれる、メラニン産生抑制作用、抗炎症作用、抗アレルギー作用、抗酸化作用等の生理活性(特許文献7)、ハマウツボ科の植物から抽出されたエラスターゼ阻害剤(特許文献8)などが挙げられる。 On the other hand, plant extracts also contain various vitamins, minerals, sugars, fats and oils, etc., and various physiological activities are known. Examples include the extract of chimpanzee extract, chimpi extract, almond extract, carrot extract, pea extract, yukinoshita extract, mulberry extract, etc., melanin production inhibitory action, anti-inflammatory action, anti-allergic action, Physiological activities such as antioxidant activity (Patent Document 7), elastase inhibitors extracted from plants of the genus Oleaceae (Patent Document 8), and the like.
これまで解明されていない藻類または植物の抽出物の新たな生理活性を見出し、適合する用途を提供することを目的とする。 It is an object of the present invention to discover new physiological activities of algal or plant extracts that have not been elucidated so far and to provide suitable applications.
本発明者らは前記課題を解決すべく鋭意検討を重ねた結果、藻類または植物の抽出物に弾性線維形成促進能があることを見出し、本発明を完成するに至った。 As a result of intensive studies to solve the above-mentioned problems, the present inventors have found that an algae or plant extract has an ability to promote elastic fiber formation and have completed the present invention.
即ち本発明は、藻類または植物の抽出物を有効成分として含有する弾性線維形成促進剤、に関する。 That is, the present invention relates to an elastic fiber formation promoter containing an algae or plant extract as an active ingredient.
上記藻類は、紅藻類および/または緑藻類であることが好ましい。 The algae are preferably red algae and / or green algae.
上記弾性線維形成促進剤において、上記紅藻類は、アクロカエティウム目、チノリモ目 、ウシケノリ目、ウミゾウメン目、エリスロペルティス目、オオイシソウ目、カクレイト目、サンゴモ目、ダルス目、テングサ目、ロドゴルゴン目、ベニマダラ目、カギノリ目、カギケノリ目、カワモズク目、 スギノリ目、オゴノリ目、マサゴシバリ目、イタニグサ目 およびイギス目に属する藻類からなる群より選択される少なくとも1種であり得る。 In the above-mentioned elastic fiber formation promoter, the red algae are acrocaetium, chinolimo, oxenaceae, sea urchins, erythropertis, euphorbiaceae, kakuraito, coralopidae, dalsu, proboscis, rhodogonon, It may be at least one selected from the group consisting of algae belonging to the order of Benimara, Clariformes, Clariformes, Duckweeds, Cyprinids, Pterodactyles, Pterodactyles, Caterpillars, and Cryptera.
上記弾性線維形成促進剤において、上記紅藻類は、ミリン科、スギノリ科、ムカデノリ科、テングサ科、カギケノリ科、およびカギノリ科からなる群より選択される少なくとも1種であり得る。 In the elastic fiber formation promoter, the red algae may be at least one selected from the group consisting of the family Milinaceae, Sugioriaceae, Muchadenoriaceae, Proboscisaceae, Kagikenoriaceae, and Kaginoriaceae.
上記弾性線維形成促進剤において、上記紅藻類は、キリンサイ、スギノリ、コトジツノマタ、ヒヂリメン、テングサ、およびアスパラゴプシスからなる群より選択される少なくとも1種であり得る。 In the elastic fiber formation promoter, the red algae may be at least one selected from the group consisting of giraffe, cedar, Kotojitsu no mata, hiridimen, proboscis, and asparagosis.
上記弾性線維形成促進剤において、上記緑藻類が、オオヒゲマワリ目、ヨコワミドロ目、サヤミドロ目、ケトフォラ目、ケトペルティス目、ヒビミドロ目、アオサ目、シオグサ目、モツレグサ目、クロレラ目、ミクロタムニオン目、トレボウクシア目、カワノリ目、マミエラ目、モノマスティクス目、ドリコマスティクス目、ミドリゲ目、イワヅタ目、スミレモ目、ウミイカダモ目、ミル目、ハネモ目、クロロデンドロン目、ドリコマスティクス目、ネフロセルミス目およびカサノリ目からなる群より選択される少なくとも1種であり得る。 In the above-mentioned elastic fiber formation promoter, the green algae may be: beige, sunflower, ketophora, ketopertis, hibimido, blue-eyed, cicada, moths, chlorella, microtamnion, trevoxia, The group consisting of Cloverfish, Mamiera, Monomastics, Doricostics, Midorigidae, Iwadata, Sumiremo, Umiikadamo, Milla, Hanemo, Chlorodendron, Doricomatica, Negrocermis It may be at least one selected from more.
上記弾性線維形成促進剤において、上記緑藻類が、アオサ目アオサ科のヒメアオノリ、ホソヒメアオノリからなる群より選択される少なくとも1種であり得る。 In the elastic fiber formation promoting agent, the green algae may be at least one selected from the group consisting of Hyacinthidae and Hyosohimeonori.
上記弾性線維形成促進剤において、植物エキスに見出されるが、特には、マツ科、ミカン科、タデ科、アカネ科、ノウゼンカズラ科、シソ科、マメ科およびクロウメモドキ科からなる群に属する植物からなる群より選択される少なくとも1種であり得る。 A group consisting of plants belonging to the group consisting of Pinaceae, Citrusaceae, Rubiaceae, Rubiaceae, Cranaceae, Lamiaceae, Leguminosae and Chromaceae It may be at least one selected from more.
本発明はまた、上記いずれかの弾性線維形成促進剤を含有する、弾性線維形成促進用組成物、に関する。 The present invention also relates to a composition for promoting elastic fiber formation, which contains any of the above-described elastic fiber formation promoters.
上記弾性線維形成促進用組成物は、化粧料であり得る。 The elastic fiber formation promoting composition may be a cosmetic.
上記弾性線維形成促進用組成物は、食品であり得る。 The elastic fiber formation promoting composition may be a food.
本発明により、藻類または植物の抽出物を有効成分とする弾性線維形成促進剤が提供される。さらには、このような弾性線維形成促進剤を含有する弾性線維形成用組成物であって、化粧料あるいは食品が提供される。 According to the present invention, there is provided an elastic fiber formation promoter comprising an algal or plant extract as an active ingredient. Furthermore, it is a composition for elastic fiber formation containing such an agent for promoting the formation of elastic fibers, and a cosmetic or food is provided.
肌、血管、肺などの特定の臓器、靱帯などにおける弾力向上又は維持は、細胞だけでなく、細胞外マトリクスを合わせた組織構成によって保たれている。細胞は、伸縮など外部強度に弱いため、細胞の回りに細胞外マトリックスを形成して、組織の形状を保っている。細胞外マトリクスとしては、コラーゲン線維、グリコサミノグリカン(ヒアルロン酸、ケラタン硫酸、へパラン硫酸、コンドロイチン、コンドロイチン硫酸、デルマタン硫酸など)、弾性線維(エラスチン線維)などがある。コラーゲン線維やグリコサミノグリカンは外部強度に対して伸び縮みができないが、弾性線維は引き延ばしても元に戻る特性、すなわち弾性を有しており、伸び縮みの機能が必須である動脈,肺、皮膚の組織には弾性線維は重要な因子である。弾性線維は、ミクロフィブリルという線維の周りにエラスチンが沈着・架橋してできると考えられている。 Elasticity improvement or maintenance in specific organs such as skin, blood vessels, and lungs, and ligaments is maintained not only by cells but also by a tissue configuration that combines extracellular matrices. Since cells are weak against external strength such as expansion and contraction, an extracellular matrix is formed around the cells to maintain the shape of the tissue. Examples of the extracellular matrix include collagen fibers, glycosaminoglycans (hyaluronic acid, keratan sulfate, heparan sulfate, chondroitin, chondroitin sulfate, dermatan sulfate, etc.), elastic fibers (elastin fibers), and the like. Collagen fibers and glycosaminoglycans cannot stretch or shrink with respect to external strength, but elastic fibers have the property of returning to their original state even when stretched, that is, have elasticity, and the function of stretching and contracting is essential. Elastic fibers are an important factor in skin tissue. Elastic fibers are thought to be formed by depositing and crosslinking elastin around microfibrils.
弾性線維のターンオーバーは非常に遅いため、加齢等によって弾性線維が劣化・断裂した結果、または炎症細胞から分泌されるプロテアーゼ等の外的要因によって弾性線維が劣化・断裂した結果、皮膚のたるみ、動脈硬化、肺が無理に引き延ばされたことに起因する肺気腫などが発生する。動脈においては、弾性線維は太い動脈の質量の半分程度を占めており、脈圧(収縮期圧−拡張期圧)を吸収している。弾性線維の機能が低下すると、動脈は硬い管となって脈圧が上昇する。脈圧の上昇は心疾患の予後を悪化させることがわかっている。 Elastic fiber turnover is very slow. As a result of elastic fiber deterioration and rupture due to aging, etc., or as a result of elastic fiber deterioration and rupture by external factors such as protease secreted from inflammatory cells, skin sagging , Arteriosclerosis, emphysema, etc. caused by the lungs being forcibly stretched. In arteries, elastic fibers occupy about half of the mass of thick arteries and absorb pulse pressure (systolic pressure-diastolic pressure). When the function of the elastic fiber decreases, the artery becomes a hard tube and the pulse pressure increases. An increase in pulse pressure has been shown to exacerbate the prognosis of heart disease.
弾性線維の再生が所望される状態又は疾患は、肺気腫、血管損傷、皮膚弛緩症、創傷、弾性線維劣化(例えば、加齢又は紫外線により引き起こされるもの、皮膚のたるみ)、肌荒れ、動脈硬化、大動脈瘤、加齢黄斑変性症、会陰ヘルニア、肛門ヘルニア、脳底動脈瘤、消化管運動障害、褥瘡などがあり、本願発明の弾性線維形成促進剤によって、弾性線維の伸び縮みの機能が必須である疾患または状態の改善や予防が可能となる。 Conditions or diseases for which elastic fiber regeneration is desired include emphysema, vascular injury, skin laxity, wounds, elastic fiber degradation (eg, caused by aging or UV rays, skin sagging), rough skin, arteriosclerosis, aorta There are aneurysms, age-related macular degeneration, perineal hernia, anal hernia, basilar artery aneurysm, gastrointestinal motility disorder, pressure ulcer, etc., and the elastic fiber formation promoter of the present invention requires the function of elastic fiber expansion and contraction. An amelioration or prevention of a disease or condition is possible.
本発明でいう弾性線維形成促進能とは、ミクロフィブリルの周りにエラスチンが沈着・架橋する工程が促進される能力をいい、その程度は問わず、処置を施さない場合と比較して、エラスチンの沈着がある程度でも促進されている状況であればよい。 The ability to promote elastic fiber formation in the present invention refers to the ability to promote the process of depositing and crosslinking elastin around microfibrils, regardless of the degree, compared to the case where elastin is not applied. Any situation where deposition is promoted to some extent is acceptable.
本発明においては、このような弾性線維を形成することを促進する作用が、藻類または植物の抽出物に見出された。藻類または植物からの抽出物は、1種を単独または2種以上を組み合わせて使用しても良い。このような藻類または植物としては、限定されず、また、抽出物とは、有効成分の弾性線維形成促進作用が損なわれない限り、藻類または植物からの水可溶性成分、酸可溶性成分、アルカリ可溶性成分、有機溶媒可溶性成分などをいう。 In the present invention, the action of promoting the formation of such elastic fibers has been found in algae or plant extracts. Extracts from algae or plants may be used singly or in combination of two or more. Such an algae or plant is not limited, and an extract is a water-soluble component, an acid-soluble component, an alkali-soluble component from an algae or a plant as long as the active fiber formation promoting action of the active ingredient is not impaired. And organic solvent soluble components.
本発明においては、このような弾性線維を形成することを促進する作用を有する成分としては、藻類の抽出物から抽出されるのもあれば特に限定はない。例えば、紅藻類の抽出物中に含まれるカラギーナン、ケイ素が含まれていてもよい。 In the present invention, the component having the action of promoting the formation of such elastic fibers is not particularly limited as long as it can be extracted from an algae extract. For example, carrageenan and silicon contained in the red algae extract may be contained.
カラギーナンは、カラギナン、カラゲナン、カラゲニンとも呼ばれ、主としてイバラノリ科、ミリン科、スギノリ科の紅藻類の海藻から抽出して得られる多糖類で、イオタ、カッパならびにラムダの三種類に大別される。イオタタイプカラギーナンは流動性のある粘性を持ち、弾力のある弱いゲルを形成し、カッパタイプカラギーナンは硬く脆いゲルを形成し、ラムダタイプカラギーナンは冷水可溶にて粘調な水溶液となり、ゲル化能力はない。本発明で用いるカラギーナンは、イオタタイプ、ラムダタイプ、あるいはカッパタイプのいずれのカラギーナンでも好適に使用できる。本発明において、カラギーナンを用いる場合には、紅藻類等から抽出した粗抽出物そのままでも、更にそれを精製処理したものでも良く、合成によって得られたものでも良い。ここでカラギーナンの抽出法も前記海藻類抽出物の調製方法と同様でよい。カラギーナンの主な成分は、直鎖含硫黄多糖類の一種で、D-ガラクトース(もしくは 3,6-アンヒドロ-D-ガラクトース)と硫酸から構成される陰イオン性高分子化合物である。 Carrageenan, also called carrageenan, carrageenan, and carrageenan, is a polysaccharide obtained by extraction from seaweeds of the red alga belonging to the family Ibarnori, Myrinaceae, and Sugiori, and is roughly classified into three types: iota, kappa and lambda. Iota-type carrageenan has fluid viscosity and forms a weak and elastic gel, kappa-type carrageenan forms a hard and brittle gel, and lambda-type carrageenan is soluble in cold water and becomes a viscous aqueous solution. There is no. As the carrageenan used in the present invention, any carrageenan of iota type, lambda type or kappa type can be suitably used. In the present invention, when carrageenan is used, the crude extract extracted from red algae or the like may be used as it is, further purified, or obtained by synthesis. Here, the extraction method of carrageenan may be the same as the preparation method of the seaweed extract. The main component of carrageenan is a kind of linear sulfur-containing polysaccharide, which is an anionic polymer compound composed of D-galactose (or 3,6-anhydro-D-galactose) and sulfuric acid.
ある態様においては、本発明の弾性線維形成促進剤は、例えば藻類に豊富に含まれるケイ素などのミネラルを有効成分の1つとして含有する。ケイ素は、骨、関節、血管、皮膚、毛髪、歯、爪などに多く含まれ、生命維持に不可欠な必須微量元素である。人体の組織内に存在するコラーゲンを強くする役割も有し、さらに、骨の形成の初期段階で、カルシウムのコラーゲン沈着を助け、骨を強くする作用も有する。ケイ素が減少すると、骨や爪がもろくなったり、血管に脂肪がつきやすくなるとの報告もある。 In a certain aspect, the elastic fiber formation promoter of this invention contains minerals, such as a silicon | silicone abundantly contained in algae, for example as one of the active ingredients. Silicon is an essential trace element that is abundant in bones, joints, blood vessels, skin, hair, teeth, nails and the like and is essential for life support. It also has the role of strengthening the collagen present in human tissues, and also has the effect of helping calcium collagen deposition and strengthening the bone at the initial stage of bone formation. There are reports that if silicon is reduced, bones and nails become brittle and blood vessels are more likely to have fat.
本発明でいう藻類は、特には、紅藻類または緑藻類をいい、これらの紅藻類または緑藻類の抽出物は、紅藻類または緑藻類から、通常の方法で抽出されるエキスをいう。ここで、紅藻類とは、例えば、アクロカエティウム目、チノリモ目、エリスロペルティス目、オオイシソウ目、ダルス目、ロドゴルゴン目、カギノリ目、カワモズク目、イタニグサ目、ウシケノリ目(ウシケノリ、フノリノウシゲ)、ウミゾウメン目(カモガシラノリ、ヒラガラガラ、フサノリ、ヒラフサノリ、ニセフサノリ、ガラガラ、ベニモヅク、ウミゾウメン)、カクレイト目(ムカデノリ)、サンゴモ目(エゾシコロ、モカサ、オオシコロ)、テングサ目(ユイキリ、シマテングサ、マクサ、オニクサ、オオブサ、オバクサ、ヒラクサ)、ベニマダラ目(ベニマダラ)、カギケノリ目(カギケノリ、タマイタダキ)、スギノリ目(イソダンツウ、ナミイワタケ、アカバ、ミチガエソウ、ハナフノリ、フクロフノリ、カイノリ、シキンノリ、スギノリ、コトジツノマタ、オオバツノマタ、ツノマタ、イボツノマタ、アカバギンナンソウ、イトフノリ、ヒロハノカクレイト、キントキ、フシキントキ、ムカデノリ、ニクムカデ、ウツロムカデ、ヒトツマツ、カタノリ、ナガキントキ、タンバノリ、フダラク、ヒラムカデ、ヒラキントキ、スジムカデ、オオバキントキ、ヒヂリメン、ツルツル、マツノリ、キョウノヒモ、マタボウ、コメノリ、ツノムカデ、トサカマツ、イバラノリ、コヒモイバラ、ホシガタイバラ、スジイバラノリ、カヅノイバラ、カギイバラノリ、サイダイバラ、タチイバラ、ヒロハノトサカモドキ、ホソバノトサカモドキ、ウスギヌ、イカノアシ、エツキイワノカワ、キジノオ、サイミ、オキツノリ、ハリガネ、ハスジグサ、マキユカリ、ユカリ、ホソバナミノハナ、ナミノハナ、アツバノリ、ベニスナゴ、トサカノリ、ミリン)、オゴノリ目(シラモ、ミゾオゴノリ、ベニオゴノリ、フシクレノリ、カバノリ、オゴノリ、マサゴシバリ目(ワツナギソウ、イソマツ、カイメンソウ、タオヤギソウ、フシツナギ、コスジフシツナギ、フクロツナギ 、ニセイバラノリ、マサゴシバリ)、イギス目(フトイギス、エゴノリ、トゲイギス、ハネイギス、イギス、ハリイギス、ケイギス、カザシグサ、キヌイトカザシグサ、ニクサエダ、サエダ、ベニヒバ、ナガウブゲグサ、ランゲリア、ヤレウスバノリ、スジウスバノリ、カギウスバノリ、タチウスベニ、ハスジギヌ、トゲノリ、ツクシホウズキ、ベンテンモ、ユナ、ヤナギノリ、マクリ、ケハネグサ、クロソゾ、ニッポンソゾ、ウラソゾ、ミツデソゾ、パピラソゾ、ハネソゾ、マギレソゾ、コブソゾ、ジャバラノリ、フジマツモ、ショウジョウケノリ、イソムラサキ、コザネモ)に属する藻類をいう。 The algae referred to in the present invention particularly refers to red algae or green algae, and these red algae or green algae extracts refer to extracts extracted from red algae or green algae by a usual method. Here, the red algae includes, for example, Acrocaetium, Chinolemo, Erythropertis, Olysamoptera, Dulce, Rhodogorgon, Ganoderma, Dermatophagoidea, Itagususa, Ganoderma (Boskenori, Funorinobosuge), and Cyprinus Eyes (Antirrhinus terrestris, Roughly Rattle, Fusanori, Hirafusanori, Nisefusanori, Rattlegar, Benimosuku, Sea Elephant), Kakuraito (Erythymidae), Coralidae (Ezosikoro, Mochasa, Oshikori), Proboscis, Osamu, Osamu Hiraksa, Benimara (Benimadara), Kachinokeri (Kagikenori, Tamaitaka), Sugiori (Isodantsu, Namiiwatake, Aqaba, Michigaesou, Hanafonori, Fukurofunori, Kainori, Shikin Li, Suginori, Kototsutsu no Mata, Oobatsu No Mata, Tsuno Mata, Ibotsu No Mata, Akabaginanso, Itofunori, Hirono Kakrate, Kintoki, Ashiki Toki, Mukadenori, Nikumukade, Utomumukade, Hitsuma Toki Kintoki, Hijirimen, Tsurutsuru, Matsunori, Kyonohimo, Matabou, Rice-necked, Tsunomukade, Tosakamatsu, Ibaranori, Kohimobara, Hoshigataibara, Sugibaranori, Kano-no-Ibara, Kagii-bara-no-ri, Aki-no-no-hito Kizino-o, Saimi, Otsunori, Harigane, Lotus Jigsas, Maki Yukari, Yukari, Hosobana Nohana, Naminohana, Atsubanori, Venetianago, Tosakanori, Mirin), Ogonori (Shiramo, Mizoogonori, Beniogonori, Fusukuri nori, Birch, Ogonori) Physalis (Futus terrestris, Egonori, Togegis, Haneigis, Igis, Harigis, Keigis, Kazasigusa, Kinuitsakasagusa, Nikusaeda, Saeda, Benihiba, Nagabuguegusa, Langeria, Jaleusbanori, Sugeusbanori, Sugeusbanori , Yuna, Yanagiri, Makri, Kenyagusa, Kurosozo, Nipponsozo, Urazoso, Mitsudezozo, Pirasozo refers Hanesozo, Magiresozo, Kobusozo, Jabaranori, Fujimatsumo, Sho Zhou Ke glue, iso purple, algae belonging to Kozanemo).
このうち、本発明で特に好適に用いることができるのは、ミリン科、スギノリ科、ムカデノリ科、テングサ科、カギケノリ科、カギノリ科に属するものであり、代表的には、ミリン科はミリン、キリンサイ、オオキリンサイ、オカムラキリンサイ、カタメンキリンサイ、トゲキリンサイ、ビャクシンキリンサイ、スギノリ科はスギノリ、コトジツノマタ、ムカデノリ科はヒヂリメン、テングサ科はテングサ、カギケノリ科はアスパラゴプシスアルマタが挙げられる。 Among these, those that can be particularly preferably used in the present invention belong to the family Milinaceae, Sugioriaceae, Muchadenoriaceae, Proboscisaceae, Kagikenoriaceae, Kaginoriaceae. , Giant rhinoceros, Okaramirin rhinoceros, Catamen giraffe rhinoceros, Rhinoceros giraffe rhinoceros, Gypsum giraffe rhinoceros, Sugiori family, Sugiori, Kotojitsu no Mata, Hydrameniaceae, Amanitaceae, Aegusa, Asparagopsis almata.
緑藻類とは、オオヒゲマワリ目、ヨコワミドロ目、サヤミドロ目、ケトフォラ目、ケトペルティス目、クロレラ目、ミクロタムニオン目、トレボウクシア目、カワノリ目、マミエラ目、モノマスティクス目、ドリコマスティクス目、スミレモ目、ウミイカダモ目、クロロデンドロン目、ドリコマスティクス目、ネフロセルミス目、ヒビミドロ目 (シワランソウモドキ、ランソウモドキ)、アオサ目(ナガアオサ、ボタンアオサ、リボンアオサ、ボウアオノリ、ウスバアオノリ、アナアオサ、アミアオサ、ヤブレグサ)、シオグサ目(ウキオリソウ、タルガタジュズモ、ホソジュズモ、ウスイロジュズモ、フトジュズモ、カイゴロモ、オオシオグサ、カタシオグサ、アサミドリシオグサ、チャシオグサ)、モツレグサ目(シリオミドロ)、ミドリゲ目(アオモグサ、マガタマモ、キッコウグサ、タマバロニア、タマゴバロニア、オオバロニア)、イワヅタ目(ヘライワヅタ、フジノハヅタ、フサイワヅタ、クサビガタハウチワ、イトゲノマユハキ、マユハキモ、ヒメイチョウ)、ミル目(ナンバンハイミル、ヒゲミル、ネザシミル、サキブトミル、ナガミル、ミル、モツレミル、ヒラミル、タマミル、コブシミル、クロミル)、ハネモ目(カタハノハネモ、オオハネモ、ナンカイハネモ)、カサノリ目(ミズタマ、フデノホ、リュウキュウガサ、カサノリ、イソスギナ)などに属する藻類をいう。特に限定はされないが、アオサ目アオサ科ヒメアオノリ属のヒメアオノリ、ホソヒメアオノリ、が代表的に示される。 Green algae are: beige, yellow, yellow, ketophora, ketopertis, chlorella, microtamnion, trevoxia, winged eyes, mamyera, monomastics, dolomatics, violets , Chlorodendrone, Doricomatics, Nephrosomis, Himidoromi (Siwaransokidoki, Ransomodoki), Aosa (Nagaaosa, Button Aosa, Ribbon Aosa, Bowuaonori, Usbaaoonori, Anaaoosa, Amiaosa, Ambrosusa) , Targata juzumo, Hosojuzumo, Ushirojuzumo, Futojuzumo, Kaigoromo, Oshiogusa, Katashiogususa, Asamidurishigususa, Chashiogusa), Odonata (Shiromidoro), Mid Ligue order (Aomogusa, Magatamamo, Akiyokugusa, Tamabalonia, Tamagobaronia, Ovalonia), Iwauta (Heraiwata, Fujinohata, Fusaiwata), Kusabigatahachiwa, Itohumayuhaki, Mayuhachimo, Himebanane, Miramibanha Sakibutomiru, Nagamiru, Mill, Motsuremil, Hiramil, Tamamiru, Kobushimiru, Kuromil), Anemone belonging to the order of Anemone (Katahanohanemo, Ohananemo, Nankaihanemo), Kasanoori (Mizuta, Fudenoho, Ryukyusa, Casanori, Isosugina), etc. Although not particularly limited, representatives of the genus Aeosidae are those belonging to the genus Aoaceae Himeonori, and Hosohimeonori.
本発明における弾性線維形成促進作用は、植物エキスに見出されるが、特には、マツ科、ミカン科、タデ科、アカネ科、ノウゼンカズラ科、シソ科、マメ科およびクロウメモドキ科からなる群に属する植物より選択される少なくとも1種の植物のエキスであることが好ましい。また、特に、マツ科トウヒ属のトウヒ、ミカン科ミカン属のビターオレンジ、タデ科のアイ、アカネ科のアセンヤク、ノウゼンカズラ科のタベブイアインペチギノサ、シソ科のオウゴン、マメ科のカンゾウ、およびクロウメモドキ科のナツメからなる群より選択される少なくとも1種の植物のエキスであることが好ましい。ここで、これらの植物の部位は特に限定はされないが、例えば、ビターオレンジは果皮、アイは葉、カンゾウは根およびナツメは果実の部位からの抽出物が特に好ましく用いられる。 The elastic fiber formation-promoting action in the present invention is found in plant extracts, particularly from plants belonging to the group consisting of Pinaceae, Citrusaceae, Rapaceae, Rubiaceae, Cranaceae, Lamiaceae, Leguminosae and Chrysomelidae It is preferably an extract of at least one selected plant. Also, in particular, Spruce spruce, Bitter orange of Citrus, Citrus eye, Acaciaceae, Acanthaceae, Papaveraceae, Rubiaceae, Leguminosae, and Chrysanthemum It is preferably an extract of at least one plant selected from the group consisting of jujube. Here, the parts of these plants are not particularly limited. For example, extracts from the fruit skin of bitter orange, leaves of eye, leaves of roots of licorice and fruit parts of jujube are particularly preferably used.
本発明の藻類または植物の抽出物が有している、優れた弾性線維形成促進能とは、ミクロフィブリルの周りにエラスチンが沈着・架橋する工程が促進される能力をいい、その程度は問わず、なんらの処置を施さない場合と比較して、エラスチンの沈着が促進されている状況であればよい。 The excellent ability to promote elastic fiber formation possessed by the algae or plant extract of the present invention refers to the ability to promote the process of depositing and crosslinking elastin around microfibrils, regardless of the degree. It is sufficient that the deposition of elastin is promoted as compared with the case where no treatment is performed.
以下に、本発明の内容を詳細に説明する。 The contents of the present invention will be described in detail below.
藻類または植物の抽出物は、天然物からの粗抽出液として用いても、また、粗抽出液から分離精製したものを用いてもよい。 The algae or plant extract may be used as a crude extract from a natural product, or a product extracted and purified from a crude extract.
藻類または植物の抽出物を得る方法としては、特に限定されず、通常の抽出法が採用される。粗抽出液は、例えば全藻または植物の全体あるいはそれらの特定の部位を裁断機・スライサー・カッター・ピーラーなどで細断したものを、水、熱水あるいは有機溶媒を単独あるいは組み合わせて得られる溶媒を用いて抽出することにより得ることができる。有機溶媒としては、メタノール、エタノール、1−プロパノール、2−プロパノール、1−ブタノール、2−ブタノール等のアルコール類、酢酸メチル、酢酸エチル等のエステル類、アセトン等のケトン類、ホルムアルデヒド、ジメチルスルホキシドなどを挙げることができる。 The method for obtaining the algae or plant extract is not particularly limited, and a normal extraction method is employed. The crude extract is a solvent obtained by, for example, water, hot water or an organic solvent alone or in combination obtained by chopping whole algae or whole plants or specific parts thereof with a cutting machine, slicer, cutter, peeler, etc. It can obtain by extracting using. Examples of the organic solvent include alcohols such as methanol, ethanol, 1-propanol, 2-propanol, 1-butanol and 2-butanol, esters such as methyl acetate and ethyl acetate, ketones such as acetone, formaldehyde, dimethyl sulfoxide and the like. Can be mentioned.
また、溶媒は、室温又は常温の溶媒を用いることもできるが、加熱溶媒や熱溶媒(溶媒を沸点付近に加熱したもの)を用いることもできる。 In addition, a solvent at room temperature or room temperature can be used as the solvent, but a heating solvent or a thermal solvent (a solvent heated near the boiling point) can also be used.
さらに、酸、アルカリの条件下で抽出する事もできる。酸としては、塩酸、硫酸、硝酸、リン酸などの無機酸、又は、酢酸、クエン酸、シュウ酸、コハク酸、ギ酸、プロピオン酸などの有機酸が挙げられる。アルカリとしては、アルカリ無機塩が好ましく用いられ、水酸化カリウム、水酸化ナトリウム等を例示できる。 Furthermore, extraction can be performed under acid and alkali conditions. Examples of the acid include inorganic acids such as hydrochloric acid, sulfuric acid, nitric acid, and phosphoric acid, and organic acids such as acetic acid, citric acid, oxalic acid, succinic acid, formic acid, and propionic acid. As the alkali, an alkali inorganic salt is preferably used, and examples thereof include potassium hydroxide and sodium hydroxide.
また、凍結乾燥粉末化法、高圧法や超高圧法を利用する事も可能である。 It is also possible to use a freeze-drying powdering method, a high pressure method or an ultrahigh pressure method.
粗抽出物の抽出条件の一例を挙げる。抽出溶媒が有機溶媒の場合、溶媒の沸点以下であればよく抽出温度は特に制限はないが、好ましくは1〜100℃、より好ましくは20〜100℃の範囲で、1〜24時間、好ましくは1時間〜10時間撹拌しながら行う。また、抽出溶媒が水の場合、抽出時の温度は特に限定されないが、加圧熱水による抽出方法を利用する場合もあるため、約0〜200℃が好ましく、約20〜130℃がより好ましい。また、反応時間も特に限定するものではないが、好ましくは数秒間〜数日間に設定すれば良く、更に好ましくはい30分〜6時間に設定すれば良い。 An example of the extraction conditions for the crude extract is given. When the extraction solvent is an organic solvent, the extraction temperature is not particularly limited as long as it is not higher than the boiling point of the solvent, but it is preferably 1 to 100 ° C., more preferably 20 to 100 ° C., preferably 1 to 24 hours, preferably 1 to 10 hours with stirring. In addition, when the extraction solvent is water, the temperature at the time of extraction is not particularly limited, but is preferably about 0 to 200 ° C, more preferably about 20 to 130 ° C, because an extraction method using pressurized hot water may be used. . Also, the reaction time is not particularly limited, but it may be set to several seconds to several days, more preferably 30 minutes to 6 hours.
反応温度及び反応時間は、溶媒の種類と濃度により適宜選択すれば良い。 The reaction temperature and reaction time may be appropriately selected depending on the type and concentration of the solvent.
このように抽出されたものであれば、弾性線維形成能を有する成分を十分に抽出することができる。 As long as it is extracted in this way, it is possible to sufficiently extract components having the ability to form elastic fibers.
得られた抽出物を遠心分離してその上清を、抽出液として得る。かかる抽出液に水可溶性、酸性可溶性、アルカリ可溶性、あるいは有機溶媒可溶性の多糖画分が含まれる。 The obtained extract is centrifuged to obtain the supernatant as an extract. Such an extract contains a water-soluble, acidic-soluble, alkali-soluble, or organic solvent-soluble polysaccharide fraction.
粗抽出物から藻類または植物の抽出物を分離精製する方法としては、例えば、塩化セチルピリジニウムなどの4級アンモニウム塩を添加し、藻類または植物の抽出物を沈殿させ、アルコール溶液で洗浄する方法やDEAEセルロースなどの陰イオン交換樹脂などを用いたクロマトグラフィーを用いる方法もある。 Examples of the method for separating and purifying the algae or plant extract from the crude extract include, for example, a method of adding a quaternary ammonium salt such as cetylpyridinium chloride to precipitate the algae or plant extract and washing with an alcohol solution. There is also a method using chromatography using an anion exchange resin such as DEAE cellulose.
このように抽出、精製した藻類または植物の抽出物溶液は、そのまま用いることもできる他、稀釈液で希釈したり、濃縮してエキスとして用いることもでき、さらには、凍結乾燥などにより乾燥粉末物としたり、ペースト状に調製して用いることもできる。 The algae or plant extract solution thus extracted and purified can be used as it is, or can be diluted with a diluting solution, concentrated, and used as an extract. Or prepared as a paste and used.
本発明では、このように抽出、精製した藻類または植物の抽出物として、そのままの状態で用いることもできるが、有機溶媒が含まれている場合には減圧蒸留等により有機溶媒を除去することが好ましい。また、本発明において、この抽出液は、液状のものを使用してもよいが、必要に応じて、減圧乾燥、凍結乾燥、噴霧乾燥等の乾燥処理を行って液体分を低減又は除去することにより、濃縮液状、半固形状、固形状、又は粉末状にしたものを使用してもよい。 In the present invention, the extracted and purified algae or plant extract can be used as it is, but when an organic solvent is contained, the organic solvent can be removed by vacuum distillation or the like. preferable. In the present invention, this extract may be used in a liquid form, and if necessary, the liquid content may be reduced or removed by performing a drying process such as reduced pressure drying, freeze drying, spray drying or the like. May be used in the form of a concentrated liquid, semi-solid, solid, or powder.
本発明における藻類または植物の抽出物としては、市販品を用いることもできる。例えば、紅藻類の抽出物としては、アスパラゴプシスアルマタ(Asparagopsis armata)の若芽からの細胞抽出物であるPHYKOSIL 2000(EXSYMOL MONAKO製)、アスパラゴプシスアルマタ(Asparagopsis armata)の抽出物であるAsparcid P(EXSYMOL MONAKO製)、トチャカの抽出物であるGELALG(Biotech Marine社製)、ゲリジウムカーチラギネウム(Gelidium cartilagineum)の抽出物であるRHODYSTEROL S/B DICAPRILAT(Biotech Marine社製)、スサビノリの抽出物であるIPF-100K、アルゲフィルター(いづれも一丸ファルコス社製)、緑藻類の抽出物としては、アオサ科のヒメアオノリ(Blidingia minima)からの抽出物であるSAVE MARINE(Biotech Marine社)、植物エキスとしては、ビターオレンジ果皮エキスとマツ科のトウヒエキスを配合したトウヒリキッドB(一丸ファルコス株式会社)、タデ科ののアイ葉エキスである藍ルーロス(株式会社林原生物化学研究所)、アカネ科のアセンヤク抽出物であるファルコレックスアセンヤクB(一丸ファルコス株式会社)、シソ科のオウゴン、マメ科のカンゾウ根、およびクロウメモドキ科のナツメ果実エキスを配合したプランテージ(ホワイト)(丸善株式会社)などが例示されるがこれに限定はされない。 Commercially available products can also be used as the algae or plant extract in the present invention. For example, as an extract of red algae, PHYKOSIL 2000 (manufactured by EXSYMOL MONAKO) which is a cell extract from a young shoot of Asparagopsis armata, an extract of Asparagopsis armata (Asparagopsis armata) Asparcid P (manufactured by EXSYMOL MONAKO), GELALG (manufactured by Biotech Marine), which is an extract of Tochaka, RHODYSTEROL S / B DICAPRILAT (manufactured by Biotech Marine), which is an extract of gelidium cartilagineum, Extracts IPF-100K, Arge filter (Izumaru Ichimaru Falcos), green algae extracts, SAVE MARINE (Biotech Marine), an extract from the heronaceae (Blidingia minima), plant extract As Spruce Liquid B (Ichimaru Falcos Co., Ltd.) containing bitter orange peel extract and pine family spruce extract, Kiso Aro Luros (Hayashibara Biochemical Laboratories Co., Ltd.), Rubiaceae Ayenak Extract Falcolex Asenyaku B (Ichimaru Falcos Co., Ltd.), Lamiaceae Ogon, Leguminosae Roots, and Chrysanthemum Plantage (white) (Maruzen Co., Ltd.) containing a jujube fruit extract is exemplified, but not limited thereto.
本発明の藻類または植物の抽出物を有効成分とする弾性線維形成促進剤は、弾性線維の再生が所望される状態又は疾患、例えば、肺気腫、肺線維症、血管損傷、皮膚弛緩症、創傷、弾性線維劣化(例えば、加齢又は紫外線により引き起こされるもの)、皮膚硬化症、肌荒れ、動脈硬化、大動脈瘤、加齢黄斑変性症、会陰ヘルニア、肛門ヘルニア、脳底動脈瘤、消化管運動障害、褥瘡などの予防、治療又は改善に有用である他、皮膚のたるみやしわの予防や改善といった美容目的のためにも有用である。また、本発明の弾性線維形成促進剤は、弾性線維の再生能を有する細胞の培養用試薬などとしても有用である。さらに、人工皮膚、皮膚モデル、人工血管などの人工組織の作製に役立つ。さらに、十分解明されているとはいえない弾性線維自体の研究への応用も考えられ、非常に広い範囲で有用である。 The elastic fiber formation promoter comprising the algal or plant extract of the present invention as an active ingredient is a state or disease in which regeneration of elastic fibers is desired, such as emphysema, pulmonary fibrosis, vascular injury, skin laxity, wound, Degradation of elastic fibers (eg caused by aging or ultraviolet rays), skin sclerosis, rough skin, arteriosclerosis, aortic aneurysm, age-related macular degeneration, perineal hernia, anal hernia, basilar aneurysm, gastrointestinal motility disorder In addition to being useful for the prevention, treatment or improvement of pressure ulcers, etc., it is also useful for cosmetic purposes such as prevention and improvement of skin sagging and wrinkles. The elastic fiber formation promoter of the present invention is also useful as a cell culture reagent having the ability to regenerate elastic fibers. Furthermore, it is useful for producing artificial tissues such as artificial skin, skin models, and artificial blood vessels. Furthermore, it can be applied to the study of elastic fibers that have not been fully elucidated, and is useful in a very wide range.
本発明の弾性線維形成剤は、医薬品、医薬部外品、食品、化粧品などとして幅広く利用可能な任意の製剤または組成物の形態で提供され得るが、好ましくは、機能性食品または化粧品として利用可能な製剤または組成物である。 The elastic fiber-forming agent of the present invention can be provided in the form of any preparation or composition that can be widely used as pharmaceuticals, quasi drugs, foods, cosmetics, etc., but preferably can be used as functional foods or cosmetics. Preparation or composition.
本発明の弾性線維活性促進剤を含む組成物が、医薬品、医薬部外品、食品、化粧品のいずれの形態を取る場合でも、藻類または植物の抽出物の含有量は、乾燥重量に換算して、例えば約0.000001〜99重量%とすればよく、より好ましくは約0.00001〜30重量%、更に好ましくは約0.0001〜10重量%、特に好ましくは0.001〜5重量%である。上記範囲であれば、医薬品、医薬部外品、食品、化粧品の使用で十分な弾性線維形成作用がみられ皮膚の伸縮性の改善または予防効果が得られる。 Even if the composition containing the elastic fiber activity promoter of the present invention takes any form of pharmaceuticals, quasi drugs, foods, and cosmetics, the content of the algae or plant extract is converted to dry weight. For example, it may be about 0.000001 to 99% by weight, more preferably about 0.00001 to 30% by weight, still more preferably about 0.0001 to 10% by weight, particularly preferably 0.001 to 5% by weight. is there. If it is the said range, sufficient elastic fiber formation effect | action is seen by use of a pharmaceutical, a quasi-drug, foodstuffs, and cosmetics, and the elasticity improvement or prevention effect of skin is acquired.
本発明を医薬品または健康食品の用途に用いる場合の藻類または植物の抽出物の投与量は、成人1日当り、乾燥重量にして、0.0001〜10g/kg、より好ましくは、0.001〜5000mg/kgとすることができる。上記範囲であれば、弾性線維の伸び縮みの機能を必須とする疾患または状態の改善や予防が可能となる。 The dose of the algal or plant extract when the present invention is used for pharmaceuticals or health foods is 0.0001 to 10 g / kg, more preferably 0.001 to 5000 mg, as a dry weight per day for an adult. / Kg. If it is the said range, the improvement or prevention of the disease or condition which requires the function of elastic fiber expansion and contraction is attained.
内服用形態 Internal form
本発明の有効成分である藻類または植物の抽出物は、薬学的に許容される担体と配合し、錠剤、カプセル剤、顆粒剤、散剤などの固形製剤;またはシロップ剤、注射剤などの液状製剤として経口または非経口的に投与することもできる。これらの製剤は、常法の添加剤を含んでいても良い。薬学的に許容される担体としては、製剤素材として慣用の各種有機あるいは無機担体物質が用いられ、固形製剤における賦形剤、滑沢剤、結合剤、崩壊剤;液状製剤における溶剤、溶解補助剤、懸濁化剤、等張化剤、緩衝剤、無痛化剤などとして配合される。また必要に応じて、防腐剤、抗酸化剤、着色剤、甘味剤などの製剤添加物を用いることもできる。 The algae or plant extract, which is an active ingredient of the present invention, is mixed with a pharmaceutically acceptable carrier, and is a solid preparation such as a tablet, capsule, granule or powder; or a liquid preparation such as a syrup or injection. Can also be administered orally or parenterally. These preparations may contain conventional additives. As the pharmaceutically acceptable carrier, various organic or inorganic carrier substances commonly used as pharmaceutical materials are used. Excipients, lubricants, binders, disintegrants in solid preparations; solvents, dissolution aids in liquid preparations , Suspending agents, isotonic agents, buffers, soothing agents and the like. Further, if necessary, preparation additives such as preservatives, antioxidants, colorants, sweeteners and the like can be used.
賦形剤の好適な例としては、例えばD−ソルビトール、マンニトール、キシリトールなどの糖アルコール、ブドウ糖、白糖、乳糖、果糖などの糖類、結晶セルロース、カルメロースナトリウム、クロスカルメロースナトリウム、リン酸水素カルシウム、コムギデンプン、コメデンプン、トウモロコシデンプン、バレイショデンプン、デキストリン、β−シクロデキストリン、軽質無水ケイ酸、酸化チタン、メタケイ酸アルミン酸マグネシウム、タルク、カオリンなどが挙げられる。 Preferable examples of the excipient include sugar alcohols such as D-sorbitol, mannitol and xylitol, sugars such as glucose, sucrose, lactose and fructose, crystalline cellulose, carmellose sodium, croscarmellose sodium, calcium hydrogen phosphate , Wheat starch, rice starch, corn starch, potato starch, dextrin, β-cyclodextrin, light silicic acid anhydride, titanium oxide, magnesium aluminate metasilicate, talc, kaolin and the like.
結合剤の好適な例としては、例えばメチルセルロース、エチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロースなどのセルロース誘導体、ポリビニルピロリドン、ポリビニルアルコール、アクリル酸系高分子、ゼラチン、アラビアゴム、プルラン、アルファー化デンプン、カンテン、トラガント、アルギン酸ナトリウム、アルギン酸プロピレングリコールエステルなどが挙げられる。 Preferable examples of the binder include cellulose derivatives such as methyl cellulose, ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, polyvinyl pyrrolidone, polyvinyl alcohol, acrylic polymer, gelatin, gum arabic, pullulan, pregelatinized starch, agar , Tragacanth, sodium alginate, propylene glycol alginate, and the like.
崩壊剤の好適な例としては、例えばデンプン、低置換度ヒドロキシプロピルセルロース、カルボキシメチルセルロースカルシウム、クロスカルメロースナトリウム、ヒドロキシプロピルスターチ、部分アルファー化デンプンなどが挙げられる。溶剤の好適な例としては、例えば注射用水、アルコール、プロピレングリコール、マクロゴール、ゴマ油、トウモロコシ油などが挙げられる。 Preferable examples of the disintegrant include starch, low-substituted hydroxypropylcellulose, carboxymethylcellulose calcium, croscarmellose sodium, hydroxypropyl starch, and partially pregelatinized starch. Preferable examples of the solvent include water for injection, alcohol, propylene glycol, macrogol, sesame oil, corn oil and the like.
滑沢剤の好適な例としては、ステアリン酸、ステアリン酸マグネシウム、ステアリン酸カルシウム、ステアリン酸ポリオキシル、セタノール、タルク、硬化油、ショ糖脂肪酸エステル、ジメチルポリシロキサン、ミツロウ、サラシミツロウなどが挙げられる。 Preferable examples of the lubricant include stearic acid, magnesium stearate, calcium stearate, polyoxyl stearate, cetanol, talc, hydrogenated oil, sucrose fatty acid ester, dimethylpolysiloxane, beeswax, and white beeswax.
溶解補助剤の好適な例としては、例えばポリエチレングリコール、プロピレングリコール、D−マンニトール、安息香酸ベンジル、エタノール、トリスアミノメタン、コレステロール、トリエタノールアミン、炭酸ナトリウム、クエン酸ナトリウムなどが挙げられる。懸濁化剤の好適な例としては、例えばステアリルトリエタノールアミン、ラウリル硫酸ナトリウム、ラウリルアミノプロピオン酸、レシチン、塩化ベンザルコニウム、塩化ベンゼトニウム、モノステアリン酸グリセリンなどの界面活性剤;例えばポリビニルアルコール、ポリビニルピロリドン、カルボキシメチルセルロースナトリウム、メチルセルロース、ヒドロキシメチルセルロース、ヒドロキシエチルセルロース、ヒドロキシプロピルセルロースなどの親水性高分子などが挙げられる。 Preferable examples of the solubilizer include polyethylene glycol, propylene glycol, D-mannitol, benzyl benzoate, ethanol, trisaminomethane, cholesterol, triethanolamine, sodium carbonate, sodium citrate and the like. Suitable examples of the suspending agent include surfactants such as stearyltriethanolamine, sodium lauryl sulfate, laurylaminopropionic acid, lecithin, benzalkonium chloride, benzethonium chloride, glyceryl monostearate; for example, polyvinyl alcohol, Examples thereof include hydrophilic polymers such as polyvinylpyrrolidone, sodium carboxymethylcellulose, methylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, and hydroxypropylcellulose.
等張化剤の好適な例としては、例えば塩化ナトリウム、グリセリン、D−マンニトールなどが挙げられる。緩衝剤の好適な例としては、例えばリン酸塩、酢酸塩、炭酸塩、クエン酸塩などの緩衝液などが挙げられる。無痛化剤の好適な例としては、例えばベンジルアルコールなどが挙げられる。防腐剤の好適な例としては、例えばパラオキシ安息香酸エステル類、クロロブタノール、ベンジルアルコール、フェネチルアルコール、デヒドロ酢酸、ソルビン酸などが挙げられる。抗酸化剤の好適な例としては、例えば亜硫酸塩、アスコルビン酸などが挙げられる。 Preferable examples of the isotonic agent include sodium chloride, glycerin, D-mannitol and the like. Preferable examples of the buffer include buffer solutions such as phosphate, acetate, carbonate, citrate and the like. Preferable examples of the soothing agent include benzyl alcohol. Preferable examples of the preservative include paraoxybenzoates, chlorobutanol, benzyl alcohol, phenethyl alcohol, dehydroacetic acid, sorbic acid and the like. Preferable examples of the antioxidant include sulfite and ascorbic acid.
本発明の液状製剤または固形製剤を製造する方法としては、藻類または植物の抽出物を製剤原料と混合して液状製剤または固形製剤を製造する工程を含むものであれば特に限定はなく、公知の方法を使用することができる。 The method for producing the liquid preparation or solid preparation of the present invention is not particularly limited as long as it includes a step of producing a liquid preparation or solid preparation by mixing an algae or plant extract with a preparation raw material. The method can be used.
固形製剤調製例:
例えば、藻類または植物の抽出物と製剤原料を含む製剤組成物を練合し、スクリーンを通過させることで成型する押出造粒物を、粉砕し、整粒する方法、前記製剤組成物に練合水を加えバーチカルグラニュレーターによって成型する攪拌造粒の後に、コーミルを用いて粉砕・篩過する方法、及び前記製剤組成物をローラーコンパクターで圧縮した後、ロールグラニュレーターで粉砕し篩過する方法、撹拌造粒の後に、流動層乾燥する方法が例示される。
Example of solid preparation:
For example, a method of kneading a formulation composition containing an algae or plant extract and a formulation raw material, and pulverizing and sizing the extruded granulated product by passing through a screen, kneading the formulation composition After stirring and granulating by adding water and molding with a vertical granulator, pulverizing and sieving using a comil, and after compressing the formulation composition with a roller compactor, pulverizing and sieving with a roll granulator, A method of fluidized bed drying after stirring granulation is exemplified.
また、例えば、直打により製造する場合には、藻類または植物の抽出物と製剤原料を含む製剤組成物を混合した後、直接、打錠機に投入して打錠すればよい。 In addition, for example, in the case of producing by direct compression, after mixing an algae or plant extract and a pharmaceutical composition containing a pharmaceutical raw material, it may be directly put into a tableting machine for tableting.
皮膚外用剤形態 Skin topical form
本発明の藻類または植物の抽出物を有効成分とする弾性線維形成促進剤は、化粧料又は医薬部外品の外用剤形態として公知の形態を採ることができる。このような形態として、例えば、液剤、懸濁剤、乳剤、クリーム剤、軟膏剤、ゲル剤、リニメント剤、ローション剤、エアゾール剤、パウダー剤、パップ剤、不織布等のシートに薬液を含浸させたシート剤、リップスティックのようなスティック剤などが挙げられる。中でも、好ましくは、液剤、懸濁剤、乳剤、クリーム剤、軟膏剤、ゲル剤、ローション剤、ゲル剤の形態で用いられる。かかる形態とすることにより、弾性線維形成効果を十分に発揮することができる。皮膚外用剤には、藻類または植物の抽出物に加えて、本発明の効果を損なわない範囲で、外皮用剤(化粧料、医薬部外品、医薬品)に添加される公知の添加剤、例えば、界面活性剤、油分、アルコール類、保湿剤、増粘剤、保存剤(防腐剤)、酸化防止剤、キレート剤、pH調整剤、安定化剤、分散剤、香料、着色剤、色素、パール光沢付与剤、血行促進成分、保湿成分、紫外線吸収成分、紫外線散乱成分、洗浄成分、抗菌成分、収斂成分、ビタミン類、アミノ酸類、老化防止成分、抗炎症成分、美白成分、角質柔軟成分、細胞賦活化成分、水等を配合することができる。添加剤は、1種を単独で、又は2種以上を組み合わせて使用できる。 The elastic fiber formation promoter containing the algal or plant extract of the present invention as an active ingredient can take a known form as an external preparation form of cosmetics or quasi drugs. As such forms, for example, liquids, suspensions, emulsions, creams, ointments, gels, liniments, lotions, aerosols, powders, poultices, nonwoven fabrics and the like were impregnated with chemicals. Examples thereof include a sheet agent and a stick agent such as a lipstick. Among these, the liquid, suspension, emulsion, cream, ointment, gel, lotion, and gel are preferably used. By setting it as this form, the elastic fiber formation effect can fully be exhibited. For skin external preparations, in addition to algal or plant extracts, known additives that are added to skin external preparations (cosmetics, quasi-drugs, pharmaceuticals) within a range that does not impair the effects of the present invention, for example, , Surfactants, oils, alcohols, humectants, thickeners, preservatives (preservatives), antioxidants, chelating agents, pH adjusters, stabilizers, dispersants, fragrances, colorants, pigments, pearls Gloss imparting agent, blood circulation promoting component, moisturizing component, UV absorbing component, UV scattering component, cleaning component, antibacterial component, astringent component, vitamins, amino acids, anti-aging component, anti-inflammatory component, whitening component, keratin softening component, cell An activation component, water, etc. can be mix | blended. An additive can be used individually by 1 type or in combination of 2 or more types.
また、化粧料組成物の具体的な用途は特に限定されず、化粧水、乳液、クリーム、美容液、日焼け止め用化粧料、パック、ハンドクリーム、ボディローション、ボディークリームのような基礎化粧料;洗顔料、メイク落とし、ボディーシャンプー、シャンプー、リンスのような洗浄用化粧料;ファンデーション、化粧下地、リップクリーム、口紅、チークカラーのようなメークアップ化粧料;入浴剤などが挙げられる。 In addition, the specific use of the cosmetic composition is not particularly limited, and basic cosmetics such as lotion, milky lotion, cream, cosmetic liquid, sunscreen cosmetics, packs, hand creams, body lotions, body creams; Cosmetics for cleaning such as face wash, makeup remover, body shampoo, shampoo, rinse; makeup cosmetics such as foundation, makeup base, lip balm, lipstick, teak color;
基剤又は担体としては、流動パラフィン、スクワラン、ゲル化炭化水素(プラスチベースなど)、オゾケライト、α−オレフィンオリゴマー、軽質流動パラフィンのような炭化水素;メチルポリシロキサン、架橋型メチルポリシロキサン、高重合メチルポリシロキサン、環状シリコーン、アルキル変性シリコーン、架橋型アルキル変性シリコーン、アミノ変性シリコーン、ポリエーテル変性シリコーン、ポリグリセリン変性シリコーン、架橋型ポリエーテル変性シリコーン、架橋型アルキルポリエーテル変性シリコーン、シリコーン・アルキル鎖共変性ポリエーテル変性シリコーン、シリコーン・アルキル鎖共変性ポリグリセリン変性シリコーン、ポリエーテル変性分岐シリコーン、ポリグリセリン変性分岐シリコーン、アクリルシリコン、フェニル変性シリコーン、シリコーンレジンのようなシリコーン油;エチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロースのようなセルロース誘導体;ポリビニルピロリドン;カラギーナン;ポリビニルブチラート;ポリエチレングリコール;ジオキサン;ブチレングリコールアジピン酸ポリエステル;ミリスチン酸イソプロピル、ミリスチン酸オクチルドデシル、パルミチン酸イソプロピル、パルミチン酸セチル、イソノナン酸イソノニル、テトラ2−エチルヘキサン酸ペンタエリスリットのようなエステル類;デキストリン、マルトデキストリンのような多糖類;エタノール、イソプロパノールのような低級アルコール;エチレングリコールモノメチルエーテル、エチレングリコールモノエチルエーテル、エチレングリコールモノプロピルエーテル、ジエチレングリコールモノメチルエーテル、ジエチレングリコールモノエチルエーテル、ジエチレングリコールモノプロピルエーテル、ジエチレングリコールモノブチルエーテル、プロピレングリコールモノエチルエーテル、プロピレングリコールモノプロピルエーテル、ジプロピレングリコールモノエチルエーテル、ジプロピレングリコールモノプロピルエーテルのようなグリコールエーテル;ポリエチレングリコール、プロピレングリコール、1,3-ブチレングリコール、グリセリン、イソプレングリコールなどの多価アルコール;水などの水系基剤などが挙げられる。 Bases or carriers include liquid paraffin, squalane, gelled hydrocarbons (such as plastibase), ozokerite, α-olefin oligomers, hydrocarbons such as light liquid paraffin; methyl polysiloxane, cross-linked methyl polysiloxane, highly polymerized methyl Polysiloxane, Cyclic silicone, Alkyl-modified silicone, Cross-linked alkyl-modified silicone, Amino-modified silicone, Polyether-modified silicone, Polyglycerin-modified silicone, Cross-linked polyether-modified silicone, Cross-linked alkyl polyether-modified silicone, Silicone / alkyl chain copolymer Modified polyether-modified silicone, silicone / alkyl chain co-modified polyglycerin-modified silicone, polyether-modified branched silicone, polyglycerin-modified branched silicone, acrylic silicone, Silicone oils such as phenyl-modified silicones and silicone resins; cellulose derivatives such as ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose; polyvinylpyrrolidone; carrageenan; polyvinyl butyrate; polyethylene glycol; dioxane; butylene glycol adipate polyester; isopropyl myristate , Esters such as octyldodecyl myristate, isopropyl palmitate, cetyl palmitate, isononyl isononanoate, pentaerythritol tetra-2-ethylhexanoate; polysaccharides such as dextrin and maltodextrin; lower levels such as ethanol and isopropanol Alcohol; ethylene glycol monomethyl ether, ethylene glycol monoethyl ether , Ethylene glycol monopropyl ether, diethylene glycol monomethyl ether, diethylene glycol monoethyl ether, diethylene glycol monopropyl ether, diethylene glycol monobutyl ether, propylene glycol monoethyl ether, propylene glycol monopropyl ether, dipropylene glycol monoethyl ether, dipropylene glycol monopropyl Examples include glycol ethers such as ethers; polyhydric alcohols such as polyethylene glycol, propylene glycol, 1,3-butylene glycol, glycerin, and isoprene glycol; and aqueous bases such as water.
基剤又は担体は、1種を単独で、又は2種以上を組み合わせて使用できる。 A base or a support | carrier can be used individually by 1 type or in combination of 2 or more types.
酸化防止剤としては、ジブチルヒドロキシトルエン、ブチルヒドロキシアニソール、ソルビン酸、亜硫酸ナトリウム、アスコルビン酸、エリソルビン酸、L−システイン塩酸塩などが挙げられる。 Examples of the antioxidant include dibutylhydroxytoluene, butylhydroxyanisole, sorbic acid, sodium sulfite, ascorbic acid, erythorbic acid, L-cysteine hydrochloride and the like.
界面活性剤としては、例えば、ソルビタンモノイソステアレート、ソルビタンモノラウレート、ソルビタンモノパルミテート、ソルビタンモノステアレート、ペンタ−2−エチルヘキシル酸ジグリセロールソルビタン、テトラ−2−エチルヘキシル酸ジグリセロールソルビタンのようなソルビタン脂肪酸エステル類;モノステアリン酸プロピレングリコールのようなプロピレングリコール脂肪酸エステル類;ポリオキシエチレン硬化ヒマシ油40(HCO−40)、ポリオキシエチレン硬化ヒマシ油50(HCO−50)、ポリオキシエチレン硬化ヒマシ油60(HCO−60)、ポリオキシエチレン硬化ヒマシ油80などの硬化ヒマシ油誘導体;モノラウリル酸ポリオキシエチレン(20)ソルビタン(ポリソルベート20)、モノステアリン酸ポリオキシエチレン(20)ソルビタン(ポリソルベート60)、モノオレイン酸ポリオキシエチレン(20)ソルビタン(ポリソルベート80)、イソステアリン酸ポリオキシエチレン(20)ソルビタンのようなポリオキシエチレンソルビタン脂肪酸エステル類;ポリオキシエチレンモノヤシ油脂肪酸グリセリル;グリセリンアルキルエーテル;アルキルグルコシド;ポリオキシエチレンセチルエーテルのようなポリオキシアルキレンアルキルエーテル;ステアリルアミン、オレイルアミンのようなアミン類;ポリオキシエチレン・メチルポリシロキサン共重合体、ラウリルPEG−9ポリジメチルシロキシエチルジメチコン、PEG−9ポリジメチルシロキシエチルジメチコンのようなシリコーン系界面活性剤などが挙げられる。 Examples of the surfactant include sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, diglycerol sorbitan penta-2-ethylhexylate, and diglycerol sorbitan tetra-2-ethylhexylate. Sorbitan fatty acid esters; propylene glycol fatty acid esters such as propylene glycol monostearate; polyoxyethylene hydrogenated castor oil 40 (HCO-40), polyoxyethylene hydrogenated castor oil 50 (HCO-50), polyoxyethylene hardened Hardened castor oil derivatives such as castor oil 60 (HCO-60), polyoxyethylene hydrogenated castor oil 80; polyoxyethylene (20) sorbitan (polysorbate 20) monolaurate, monostearate Polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene (20) sorbitan (polysorbate 60), polyoxyethylene monooleate (20) sorbitan (polysorbate 80), polyoxyethylene (20) sorbitan isostearate; Glyceryl alkyl ether; alkyl glucoside; polyoxyalkylene alkyl ether such as polyoxyethylene cetyl ether; amines such as stearylamine and oleylamine; polyoxyethylene / methylpolysiloxane copolymer; And silicone surfactants such as lauryl PEG-9 polydimethylsiloxyethyl dimethicone and PEG-9 polydimethylsiloxyethyl dimethicone.
増粘剤としては、例えば、グアーガム、ローカストビーンガム、カラギーナン、キサンタンガム、カルボキシメチルセルロース、ヒドロキシメチルセルロース、ヒドロキシエチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、ポリビニルアルコール、ポリビニルピロリドン、カルボキシビニルポリマー、アクリル酸メタクリル酸アルキル共重合体、ポリエチレングリコール、ベントナイト、(アクリル酸ヒドロキシエチル/アクリロイルジメチルタウリンNa)コポリマー、(アクリロイルジメチルタウリンアンモニウム/ビニルピロリドン)コポリマーなどが挙げられる。 Examples of the thickener include guar gum, locust bean gum, carrageenan, xanthan gum, carboxymethylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinyl alcohol, polyvinylpyrrolidone, carboxyvinyl polymer, alkyl methacrylate methacrylate. Copolymers, polyethylene glycol, bentonite, (hydroxyethyl acrylate / acryloyldimethyltaurine Na) copolymer, (acryloyldimethyltaurine ammonium / vinylpyrrolidone) copolymer, and the like.
保存剤としては、安息香酸、安息香酸ナトリウム、デヒドロ酢酸、デヒドロ酢酸ナトリウム、パラオキシ安息香酸イソブチル、パラオキシ安息香酸イソプロピル、パラオキシ安息香酸ブチル、パラオキシ安息香酸エチル、パラオキシ安息香酸プロピル、パラオキシ安息香酸ベンジル、パラオキシ安息香酸メチル、フェノキシエタノールなどが挙げられる。 Preservatives include benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl paraoxybenzoate, isopropyl paraoxybenzoate, butyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, benzyl paraoxybenzoate, paraoxybenzoate Examples include methyl benzoate and phenoxyethanol.
pH調整剤としては、無機酸(塩酸、硫酸など)、有機酸(乳酸、乳酸ナトリウム、クエン酸、クエン酸ナトリウム、コハク酸、コハク酸ナトリウムなど)、無機塩基(水酸化カリウム、水酸化ナトリウムなど)、有機塩基(トリエタノールアミン、ジイソプロパノールアミン、トリイソプロパノールアミンなど)などが挙げられる。
キレート剤としては、EDTA・2ナトリウム塩、EDTA・カルシウム・2ナトリウム塩などが挙げられる。
Examples of pH adjusters include inorganic acids (hydrochloric acid, sulfuric acid, etc.), organic acids (lactic acid, sodium lactate, citric acid, sodium citrate, succinic acid, sodium succinate, etc.), inorganic bases (potassium hydroxide, sodium hydroxide, etc.) ) And organic bases (such as triethanolamine, diisopropanolamine, and triisopropanolamine).
Examples of the chelating agent include EDTA / disodium salt, EDTA / calcium disodium salt, and the like.
安定化剤としては、ポリアクリル酸ナトリウム、ジブチルヒドロキシトルエン、ブチルヒドロキシアニソールなどが挙げられる。 Examples of the stabilizer include sodium polyacrylate, dibutylhydroxytoluene, butylhydroxyanisole and the like.
添加剤は1種を単独で又は2種以上を組み合わせて使用できる。 An additive can be used individually by 1 type or in combination of 2 or more types.
本発明の外用組成物は、本発明の効果を損なわない範囲で、その他の有効成分を含むことができる。有効成分の具体例としては、例えば、保湿成分、抗炎症成分、抗菌成分、ビタミン類、ペプチド又はその誘導体、アミノ酸又はその誘導体、細胞賦活化成分、老化防止成分、血行促進成分などが挙げられる。 The composition for external use of this invention can contain another active ingredient in the range which does not impair the effect of this invention. Specific examples of active ingredients include moisturizing ingredients, anti-inflammatory ingredients, antibacterial ingredients, vitamins, peptides or derivatives thereof, amino acids or derivatives thereof, cell activation ingredients, anti-aging ingredients, blood circulation promoting ingredients, and the like.
保湿成分としては、グリセリン、1,3−ブチレングリコール、プロピレングリコール、ポリエチレングリコール、ジグリセリントレハロースのような多価アルコール;ヒアルロン酸ナトリウム、ヘパリン類似物質、コンドロイチン硫酸ナトリウム、コラーゲン、エラスチン、ケラチン、キチン、キトサンのような高分子化合物;グリシン、アスパラギン酸、アルギニンのようなアミノ酸;乳酸ナトリウム、尿素、ピロリドンカルボン酸ナトリウムのような天然保湿因子;セラミド、コレステロール、リン脂質のような脂質;カミツレエキス、ハマメリスエキス、チャエキス、シソエキスのような植物抽出エキスなどが挙げられる。 As moisturizing ingredients, polyhydric alcohols such as glycerin, 1,3-butylene glycol, propylene glycol, polyethylene glycol, diglycerin trehalose; sodium hyaluronate, heparin-like substance, sodium chondroitin sulfate, collagen, elastin, keratin, chitin, Macromolecular compounds such as chitosan; amino acids such as glycine, aspartic acid, arginine; natural moisturizing factors such as sodium lactate, urea, sodium pyrrolidonecarboxylate; lipids such as ceramide, cholesterol, phospholipid; chamomile extract, hamamelis Plant extract such as extract, tea extract, perilla extract and the like can be mentioned.
抗菌成分としては、クロルヘキシジン、サリチル酸、塩化ベンザルコニウム、アクリノール、エタノール、塩化ベンゼトニウム、クレゾール、グルコン酸及びその誘導体、ポピドンヨード、ヨウ化カリウム、ヨウ素、イソプロピルメチルフェノール、トリクロカルバン、トリクロサン、感光素101号、感光素201号、パラベン、フェノキシエタノール、1,2-ペンタンジオール、塩酸アルキルジアミノグリシン等が挙げられる。 Antibacterial components include chlorhexidine, salicylic acid, benzalkonium chloride, acrinol, ethanol, benzethonium chloride, cresol, gluconic acid and its derivatives, popidone iodine, potassium iodide, iodine, isopropylmethylphenol, triclocarban, triclosan, photosensitizer No. 101 Photosensitive element 201, paraben, phenoxyethanol, 1,2-pentanediol, alkyldiaminoglycine hydrochloride and the like.
ビタミン類としては、dl−α−トコフェロール、酢酸dl−α−トコフェロール、コハク酸dl−α−トコフェロール、コハク酸dl−α−トコフェロールカルシウム等のビタミンE類;リボフラビン、フラビンモノヌクレオチド、フラビンアデニンジヌクレオチド、リボフラビン酪酸エステル、リボフラビンテトラ酪酸エステル、リボフラビン5’−リン酸エステルナトリウム、リボフラビンテトラニコチン酸エステル等のビタミンB2類;ニコチン酸dl−α−トコフェロール、ニコチン酸ベンジル、ニコチン酸メチル、ニコチン酸β−ブトキシエチル、ニコチン酸1−(4−メチルフェニル)エチル等のニコチン酸類;アスコルビゲン−A、アスコルビン酸ステアリン酸エステル、アスコルビン酸パルミチン酸エステル、ジパルミチン酸L−アスコルビルなどのビタミンC類;メチルヘスペリジン、エルゴカルシフェロール、コレカルシフェロールなどのビタミンD類;フィロキノン、ファルノキノン等のビタミンK類、γ−オリザノール、ジベンゾイルチアミン、ジベンゾイルチアミン塩酸塩;チアミン塩酸塩、チアミンセチル塩酸塩、チアミンチオシアン酸塩、チアミンラウリル塩酸塩、チアミン硝酸塩、チアミンモノリン酸塩、チアミンリジン塩、チアミントリリン酸塩、チアミンモノリン酸エステルリン酸塩、チアミンモノリン酸エステル、チアミンジリン酸エステル、チアミンジリン酸エステル塩酸塩、チアミントリリン酸エステル、チアミントリリン酸エステルモノリン酸塩等のビタミンB1類;塩酸ピリドキシン、酢酸ピリドキシン、塩酸ピリドキサール、5’−リン酸ピリドキサール、塩酸ピリドキサミン等のビタミンB6類;シアノコバラミン、ヒドロキソコバラミン、デオキシアデノシルコバラミン等のビタミンB12類;葉酸、プテロイルグルタミン酸等の葉酸類;ニコチン酸、ニコチン酸アミドなどのニコチン酸類;パントテン酸、パントテン酸カルシウム、パントテニルアルコール(パンテノール)、D−パンテサイン、D−パンテチン、補酵素A、パントテニルエチルエーテル等のパントテン酸類;ビオチン、ビオチシン等のビオチン類;アスコルビン酸、アスコルビン酸ナトリウム、デヒドロアスコルビン酸、アスコルビン酸リン酸エステルナトリウム、アスコルビン酸リン酸エステルマグネシウム等のアスコルビン酸誘導体であるビタミンC類;カルニチン、フェルラ酸、α−リポ酸、オロット酸等のビタミン様作用因子などが挙げられる。 Vitamins such as dl-α-tocopherol, dl-α-tocopherol acetate, dl-α-tocopherol succinate, dl-α-tocopherol calcium succinate; riboflavin, flavin mononucleotide, flavin adenine dinucleotide Vitamin B2 such as riboflavin butyrate, riboflavin tetrabutyrate, sodium riboflavin 5′-phosphate, riboflavin tetranicotinate; nicotinic acid dl-α-tocopherol, benzyl nicotinate, methyl nicotinate, β-nicotinic acid β- Nicotinic acids such as butoxyethyl and 1- (4-methylphenyl) ethyl nicotinate; ascorbigen-A, ascorbyl stearate, ascorbyl palmitate, dipalmitate -Vitamin Cs such as ascorbyl; Vitamin Ds such as methyl hesperidin, ergocalciferol and cholecalciferol; Vitamin Ks such as phylloquinone and farnoquinone, γ-oryzanol, dibenzoylthiamine, dibenzoylthiamine hydrochloride; thiamine hydrochloride , Thiamine cetyl hydrochloride, thiamine thiocyanate, thiamine lauryl hydrochloride, thiamine nitrate, thiamine monophosphate, thiamine lysine salt, thiamine triphosphate, thiamine monophosphate phosphate, thiamine monophosphate, thiamine diphosphate Vitamin B1 such as thiamine diphosphate hydrochloride, thiamine triphosphate, thiamine triphosphate monophosphate; pyridoxine hydrochloride, pyridoxine acetate, pyridoxal hydrochloride, 5'- Vitamin B6 such as pyridoxal phosphate and pyridoxamine hydrochloride; Vitamin B12 such as cyanocobalamin, hydroxocobalamin and deoxyadenosylcobalamin; Folic acid such as folic acid and pteroylglutamic acid; Nicotinic acids such as nicotinic acid and nicotinamide; Pantothenic acids such as calcium pantothenate, pantothenyl alcohol (panthenol), D-panthecine, D-panthetin, coenzyme A, pantothenyl ethyl ether; biotins such as biotin and bioticin; ascorbic acid, sodium ascorbate, Vitamin C which is an ascorbic acid derivative such as dehydroascorbic acid, sodium ascorbate phosphate, magnesium ascorbate phosphate; carnitine, ferulic acid, α-lipoic acid Such as vitamin-like effect factors such as orotic acid, and the like.
ペプチド又はその誘導体としては、ケラチン分解ペプチド、加水分解ケラチン、コラーゲン、魚由来コラーゲン、アテロコラーゲン、ゼラチン、エラスチン、エラスチン分解ペプチド、コラーゲン分解ペプチド、加水分解コラーゲン、塩化ヒドロキシプロピルアンモニウム加水分解コラーゲン、エラスチン分解ペプチド、コンキオリン分解ペプチド、加水分解コンキオリン、シルク蛋白分解ペプチド、加水分解シルク、ラウロイル加水分解シルクナトリウム、大豆蛋白分解ペプチド、加水分解大豆蛋白、小麦蛋白、小麦蛋白分解ペプチド、加水分解小麦蛋白、カゼイン分解ペプチド、アシル化ペプチド(パルミトイルオリゴペプチド、パルミトイルペンタペプチド、パルミトイルテトラペプチド等)などが挙げられる。 Peptides or derivatives thereof include keratin-degrading peptide, hydrolyzed keratin, collagen, fish-derived collagen, atelocollagen, gelatin, elastin, elastin-degrading peptide, collagen-degrading peptide, hydrolyzed collagen, hydroxypropylammonium chloride hydrolyzed collagen, elastin-degrading peptide , Conchiolin degrading peptide, hydrolyzed conchiolin, silk proteolytic peptide, hydrolyzed silk, lauroyl hydrolyzed silk sodium, soy proteolytic peptide, hydrolyzed soy protein, wheat protein, wheat proteolytic peptide, hydrolyzed wheat protein, casein degrading peptide Acylated peptides (palmitoyl oligopeptide, palmitoyl pentapeptide, palmitoyl tetrapeptide, etc.).
アミノ酸又はその誘導体としては、ベタイン(トリメチルグリシン)、プロリン、ヒドロキシプロリン、アルギニン、リジン、セリン、グリシン、アラニン、フェニルアラニン、β−アラニン、スレオニン、グルタミン酸、グルタミン、アスパラギン、アスパラギン酸、システイン、シスチン、メチオニン、ロイシン、イソロイシン、バリン、ヒスチジン、タウリン、γ−アミノ酪酸、γ−アミノ−β−ヒドロキシ酪酸、カルニチン、カルノシン、クレアチン等が挙げられる。 As amino acids or their derivatives, betaine (trimethylglycine), proline, hydroxyproline, arginine, lysine, serine, glycine, alanine, phenylalanine, β-alanine, threonine, glutamic acid, glutamine, asparagine, aspartic acid, cysteine, cystine, methionine Leucine, isoleucine, valine, histidine, taurine, γ-aminobutyric acid, γ-amino-β-hydroxybutyric acid, carnitine, carnosine, creatine and the like.
本発明の弾性線維形成促進剤は、植込錠及びマイクロカプセルに封入された送達システムなどの徐放性製剤として用いることもできる。この徐放性製剤は、体内から速やかに除去されることを防止できるような、薬剤的に受容可能な公知の担体を用いて調製し得る。具体的には、例えば、エチレンビニル酢酸塩、ポリ酸無水物、ポリグリコール酸、コラーゲン、ポリオルトエステル、及びポリ乳酸などの生物分解性または生物適合性ポリマーを用いることができる。これらのポリマーは公知であり、常法に基づき、当業者によって容易に調製することができる。あるいは、薬剤的に受容可能な他の担体として、リポソームの懸濁液なども使用することができる。上記リポソームは特に限定されず、ホスファチジルコリン、コレステロール及びPEG誘導ホスファチジルエタノール(PEG−PE)を含む脂質組成物などが挙げられる。これは、使用に適したサイズになるように、適当なポアサイズのフィルターを通して調製した後、逆相蒸発法によって精製して得られる。 The elastic fiber formation promoter of the present invention can also be used as a sustained-release preparation such as a delivery system encapsulated in implantable tablets and microcapsules. This sustained-release preparation can be prepared using a known pharmaceutically acceptable carrier that can prevent rapid removal from the body. Specifically, biodegradable or biocompatible polymers such as ethylene vinyl acetate, polyanhydride, polyglycolic acid, collagen, polyorthoester, and polylactic acid can be used. These polymers are known and can be easily prepared by those skilled in the art based on conventional methods. Alternatively, liposome suspensions and the like can also be used as other pharmaceutically acceptable carriers. The liposome is not particularly limited, and examples thereof include a lipid composition containing phosphatidylcholine, cholesterol and PEG-derived phosphatidylethanol (PEG-PE). This is obtained by preparing through a filter having an appropriate pore size so as to have a size suitable for use and then purifying by a reverse phase evaporation method.
食品 Food
本発明の藻類または植物の抽出物を含有する弾性線維形成促進剤は、食品または機能性食品に含有させて提供され得る。このような食品または機能性食品としては、米飯;そば、うどん、はるさめ、中華麺、即席麺、カップ麺を含む各種の麺類;清涼飲料、炭酸飲料、栄養飲料、果実飲料、乳酸飲料、スポーツ飲料等の飲料;カレールー、シチュー、各種スープ類;アイスクリーム、アイスシャーベット、かき氷等の冷菓;飴、クッキー、キャンディー、ガム、チョコレート、錠菓、スナック菓子、ビスケット、ゼリー、ジャム、クリーム、その他の焼き菓子等の菓子類;かまぼこ、はんぺん、ハム、ソーセージ等の水産・畜産加工食品;加工乳、発酵乳等の乳製品;サラダ油、てんぷら油、マーガリン、マヨネーズ、ショートニング、ホイップクリーム、ドレッシング等の油脂及び油脂加工食品;ソース、ドレッシング、味噌、醤油、たれ等の調味料;スープ、シチュー、サラダ、惣菜、ふりかけ、漬物;その他種々の形態の健康・栄養補助食品などが例示される。 The elastic fiber formation promoter containing the algae or plant extract of the present invention can be provided by being contained in a food or functional food. Examples of such foods or functional foods include cooked rice; various kinds of noodles including soba, udon, harusame, Chinese noodles, instant noodles, cup noodles; soft drinks, carbonated drinks, nutrition drinks, fruit drinks, lactic acid drinks, sports drinks Beverages such as Carrero, stew, various soups; Ice cream, ice sorbet, shaved ice and other frozen desserts; Strawberries, cookies, candy, gum, chocolate, tablet confectionery, snacks, biscuits, jellies, jams, creams, and other baked goods Sweets such as kamaboko, hampen, processed food such as ham, sausage; dairy products such as processed milk and fermented milk; fats and oils such as salad oil, tempura oil, margarine, mayonnaise, shortening, whipped cream, dressing Processed foods; seasonings such as sauces, dressings, miso, soy sauce, sauces; soups Stew, salad, delicatessen, sprinkle, pickles; health and nutrition supplement other various forms is illustrated.
さらには、本発明の弾性線維形成剤を含有するサプリメント(散在、顆粒剤、ソフトカプセル、ハードカプセル、錠剤、チュアブル錠、速崩錠、シロップ、液剤等)を調製してもよい。 Furthermore, supplements (scattering, granules, soft capsules, hard capsules, tablets, chewable tablets, quick-disintegrating tablets, syrups, liquids, etc.) containing the elastic fiber-forming agent of the present invention may be prepared.
また、ペットなどの動物用の餌に対して本発明の弾性線維形成剤を含有させることもできる。 Moreover, the elastic fiber formation agent of this invention can also be contained with respect to animal foods, such as a pet.
食品には、必要に応じて、添加物が加えられる。このような添加物としては、例えばブドウ糖、果糖、ショ糖、マルトース、ソルビトール、ステビオサイド、ルブソサイド、コーンシロップ、乳糖、マンニット、デキストリン、クエン酸、クエン酸ソーダ、酒石酸、リンゴ酸、コハク酸、乳酸、L−アスコルビン酸、dl−α−トコフェロール、エリソルビン酸ナトリウム、グリセリン、プロピレングリコール、グリセリン脂肪酸エステル、ポリグリセリン脂肪酸エステル、ショ糖脂肪酸エステル、ソルビタン脂肪酸エステル、アラビアガム、カラギーナン、カゼイン、ゼラチン、ペクチン、寒天、ビタミンC、ビタミンB類、ビタミンE、ニコチン酸アミド、パントテン酸カルシウム、アミノ酸類、カルシウム塩類、界面活性剤、色素、香料、保存剤などが挙げられる。 Additives are added to the food as needed. Examples of such additives include glucose, fructose, sucrose, maltose, sorbitol, stevioside, rubusoside, corn syrup, lactose, mannitol, dextrin, citric acid, sodium citrate, tartaric acid, malic acid, succinic acid, lactic acid L-ascorbic acid, dl-α-tocopherol, sodium erythorbate, glycerol, propylene glycol, glycerol fatty acid ester, polyglycerol fatty acid ester, sucrose fatty acid ester, sorbitan fatty acid ester, gum arabic, carrageenan, casein, gelatin, pectin, Examples include agar, vitamin C, vitamin B, vitamin E, nicotinic acid amide, calcium pantothenate, amino acids, calcium salts, surfactants, pigments, fragrances, and preservatives.
本発明の弾性線維形成促進剤を用いて、人工弾性線維をインビトロで作成すること、弾性線維の研究への応用に用いることも可能である。本発明の弾性線維形成促進剤を用いて、インビトロで弾性線維を形成させ、人工弾性線維の培養用試薬、人工皮膚、皮膚モデル、人工血管などの人工組織の作製に用いることもできる。このようなインビトロでの研究や実施への応用に用いる場合、藻類または植物の抽出物をそのままの形で用いることも好ましい。 Using the elastic fiber formation promoter of the present invention, artificial elastic fibers can be prepared in vitro, and can be used for application to elastic fiber research. Using the elastic fiber formation promoter of the present invention, elastic fibers can be formed in vitro and used for the production of artificial tissues such as artificial elastic fiber culture reagents, artificial skin, skin models, and artificial blood vessels. When used for such in vitro research and practical application, it is also preferable to use an algae or plant extract as it is.
本発明の弾性線維形成促進剤は、さらに、DANCE発現増強因子(DANCE誘導因子)を含んでいてもよい。DANCE発現増強因子を用いることができ、例えば、ナンテンカズラエキス、シカクマメエキス、フィチン酸及びその生理学的に許容される塩、並びにL−ヒドロキシプロリン及びその生理学的に許容される塩等のDANCE発現増強因子;DANCE発現ベクター、またはDANCE誘導因子発現ベクターなどが挙げられる。 The elastic fiber formation promoter of the present invention may further contain a DANCE expression enhancing factor (DANCE inducing factor). DANCE expression enhancing factor can be used, for example, DANCE expression enhancement such as Nanten quail extract, winged bean extract, phytic acid and physiologically acceptable salts thereof, and L-hydroxyproline and physiologically acceptable salts thereof Factor: DANCE expression vector, DANCE inducing factor expression vector and the like.
次に、試験例、実施例等により本発明を具体的に説明するが、本発明は以下の実施例に限定されるものではない。 Next, the present invention will be specifically described with reference to test examples and examples, but the present invention is not limited to the following examples.
〔製造例1〕(通常の紅藻類抽出物の抽出)
紅藻類の抽出物は、市販のPHYKOSIL 2000 (EXSYMOL MONAKO製、カギケノリ科紅藻の抽出物)をそのまま用いた。試験例1で示す培養液を利用して添加後の最終濃度が培養液全体の0.001重量%になるように調製した。
[Production Example 1] (Extraction of normal red algae extract)
As an extract of red algae, commercially available PHYKOSIL 2000 (manufactured by EXSYMOL MONAKO, an extract of red algae) was used as it was. Using the culture solution shown in Test Example 1, the final concentration after addition was 0.001% by weight of the whole culture solution.
〔製造例2〕(通常の紅藻類抽出物の抽出)
紅藻類の抽出物として、市販品Asparcid P(EXSYMOL MONAKO製、カギケノリ科紅藻の抽出物;アスパラゴシプシアルマタ(asparagopsis armata))をそのまま用いた。試験例1で示す培養液を利用して添加後の最終濃度が0.001重量%になるように調製した。
[Production Example 2] (Extraction of normal red algae extract)
As an extract of red algae, a commercially available product Asparcid P (manufactured by EXSYMOL MONAKO, an extract of red algae; asparagopsis armata) was used as it was. Using the culture solution shown in Test Example 1, the final concentration after addition was 0.001% by weight.
〔製造例3〕(通常の緑藻類抽出物の抽出)
緑藻類の抽出物として、市販品SAVE MARINE(Biotech Marine社、緑藻抽出物;アオサ目ヒメアオノリ属のヒメアオノリ)をそのまま用いた。試験例1で示す培養液を利用して添加後の最終濃度が0.001重量%になるように調製した。
[Production Example 3] (Extraction of normal green algae extract)
As an extract of green algae, a commercially available product, SAVE MARINE (Biotech Marine, green algae extract; Using the culture solution shown in Test Example 1, the final concentration after addition was 0.001% by weight.
〔製造例4〕(藻類および植物の抽出物)
表1に示す市販の製品を使って、同様に、弾性線維形成能を測定するために、各種の抽出物を調製した。
Similarly, various extracts were prepared using the commercially available products shown in Table 1 in order to measure the ability to form elastic fibers.
〔試験例1〕(弾性線維形成促進の評価試験)
無血清下での実験
24ウエルプレートの底にMicroscope Cover Glass(Fisherbrandから購入)を置き、その上に皮膚線維芽細胞を1ウエルあたり7.5×104個播種し、継代用培地(DMEM(Dulbecco’s Modified Eagle Medium、Invitrogenから購入)、10%ウシ胎仔血清(FBS、JRH Bioscienceから購入)、2mMのグルタミン、100units/mLのペニシリン、100g/mLのストレプトマイシン)にて37℃、5%CO2で培養した。さらに、血清を含まない弾性線維形成培地、すなわち、DMEM/F12、2mMのグルタミン、100units/mLのペニシリン、100g/mLのストレプトマイシンを用い、ヒト線維芽細胞を1ウエルあたり7.5×104個播種し、この無血清培地に、製造例1から4までの調製物をそれぞれ、培養物全体の0.001重量%になるように加えて、あるいは加えないで、37℃、5%CO2で4週間培養した。4週間の培養後、弾性線維の蛍光免疫染色を行なった。詳細には、1mLのPBSを用いて3回洗浄した後、100%メタノールを用い、−20℃で20分間固定した。更にPBSを用いて洗浄した後、2%BSAを含むPBSを用い、室温で1時間ブロッキングした後、1次抗体として抗エラスチンポリクローナル抗体(Elastin Products Companyから購入)を用い、2次抗体としてAlexa488−抗ウサギIgG抗体(Invitrogenから購入)を用いた。1次抗体と室温で1時間以上インキュベートした後、PBSで洗浄し、上記の2次抗体と室温で1時間インキュベートした。PBSで洗浄した後、4%パラホルムアルデヒドを用いて室温で10分間固定し、再びPBSで洗浄した後、Hoechst33258(Dojindoから購入)を用いて室温で5分間反応させ、再びPBSで洗浄した後、Aqua Poly/Mount(Poluscienceから購入)にてスライドガラス上にサンプルをマウントした。観察は蛍光顕微鏡IX71(Olympus)を用いて行った。その結果を図1〜図5に示す。
[Test Example 1] (Evaluation test for promotion of elastic fiber formation)
Serum-free experiment Place a Microscope Cover Glass (purchased from Fisherbrand) on the bottom of a 24-well plate, and inoculate 7.5 × 10 4 skin fibroblasts per well on the passage medium (DMEM (DMEM)). Dulbecco's Modified Eagle Medium, purchased from Invitrogen), 10% fetal calf serum (FBS, purchased from JRH Bioscience), 2 mM glutamine, 100 units / mL penicillin, 100 g / mL streptomycin) at 37 ° C., 5% CO Incubated in 2 . Furthermore, 7.5 × 10 4 human fibroblasts per well were prepared using serum-free elastic fibrosis medium, ie, DMEM / F12, 2 mM glutamine, 100 units / mL penicillin, 100 g / mL streptomycin. Seeded and added to the serum-free medium at 37 ° C., 5% CO 2 with or without the preparations of Production Examples 1 to 4 added to 0.001% by weight of the whole culture. Cultured for 4 weeks. After culturing for 4 weeks, fluorescent immunostaining of elastic fibers was performed. Specifically, after washing three times with 1 mL of PBS, the cells were fixed with -100C methanol at -20 ° C for 20 minutes. After washing with PBS and blocking with PBS containing 2% BSA for 1 hour at room temperature, anti-elastin polyclonal antibody (purchased from Elastin Products Company) was used as the primary antibody, and Alexa 488- was used as the secondary antibody. An anti-rabbit IgG antibody (purchased from Invitrogen) was used. After incubating with the primary antibody at room temperature for 1 hour or more, it was washed with PBS, and incubated with the above secondary antibody at room temperature for 1 hour. After washing with PBS, it was fixed with 4% paraformaldehyde at room temperature for 10 minutes, washed again with PBS, reacted with Hoechst33258 (purchased from Dojindo) for 5 minutes, washed again with PBS, Samples were mounted on glass slides with Aqua Poly / Mount (purchased from Poluscience). Observation was performed using a fluorescence microscope IX71 (Olympus). The results are shown in FIGS.
図1および図3は、弾性線維であるエラスチンを蛍光染色したものである。本蛍光染色法ではエラスチンに加えて細胞質も同時に染色されるためコントロールでは斑点状の蛍光発色が認められるが、これは細胞質を染色したものでありエラスチンを染色したものではない。一方、紅藻類の抽出または緑藻類の抽出物では、コントロール同様に細胞質は斑点状に染色されるが、写真全面に著明な線維状の蛍光染色が確認された。このことから紅藻類の抽出または緑藻類の抽出物には、著明な弾性線維、すなわちエラスチン線維形成促進効果が確認された。紅藻類の抽出、緑藻類の抽出物およびコントロールの細胞数に変化がないことは確認済みである。 FIG. 1 and FIG. 3 are fluorescent stains of elastin, an elastic fiber. In this fluorescent staining method, cytoplasm is also stained in addition to elastin, so that a spot-like fluorescent coloration is observed in the control. On the other hand, in the extract of red algae or green algae, the cytoplasm was stained in spots like the control, but a marked fibrous fluorescent staining was confirmed on the entire surface of the photograph. From this, it was confirmed that the extract of red algae or the extract of green algae has a remarkable elastic fiber, that is, elastin fiber formation promoting effect. It has been confirmed that there is no change in the number of red algae extract, green algae extract and control cells.
さらに、蛍光量を数値化する為に、Image J(数値化に用いた画像ソフト)を用いた。その結果を図2、図4、および図5に示す。 Furthermore, Image J (image software used for quantification) was used to quantify the amount of fluorescence. The results are shown in FIG. 2, FIG. 4, and FIG.
製造例1で得た抽出物および製造例2で得た抽出物は、優れた弾性線維形成促進作用を有していることが示された。また、製造例3で得た抽出物を用いた場合、製造例1および2ほどの線維形成は見られなかったものの、コントロールと比較して、明らかにエラスチン沈着が進んでいることが見られる。このことは弾性線維(エラスチン線維)形成が促進している事を示している。 It was shown that the extract obtained in Production Example 1 and the extract obtained in Production Example 2 have excellent elastic fiber formation promoting action. In addition, when the extract obtained in Production Example 3 was used, fiber formation as in Production Examples 1 and 2 was not observed, but it was clearly seen that elastin deposition was advanced as compared with the control. This indicates that the formation of elastic fibers (elastin fibers) is promoted.
〔組成物調製例1〕
化粧料組成物
以下の化粧料組成物の実施例中の数値の単位は「重量%」である。
[Composition Preparation Example 1]
Cosmetic composition The unit of the numerical value in the Example of the following cosmetic compositions is "weight%".
[組成物調製例2]
内服組成物
以下の食品組成物の処方例において、藻類または植物の抽出物の重量は乾燥重量である。
食品組成物の全処方において、藻類または植物の抽出物としては、エタノール抽出物が好ましい。
[Composition Preparation Example 2]
Oral Composition In the formulation examples of the following food compositions, the weight of the algae or plant extract is the dry weight.
In the whole formulation of the food composition, the algae or plant extract is preferably an ethanol extract.
この飲料は、1日3回の食事毎に1本摂取される。 This drink is taken once every three meals a day.
この錠剤は、1日3回の食事毎に3錠摂取される。 Three tablets of this tablet are taken every three meals a day.
Claims (9)
A method of forming elastic fibers in vitro using an eye leaf extract, a geridium curcilaineum extract, and / or an asparagopsis armata extract.
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JP6399545B2 (en) * | 2014-08-28 | 2018-10-03 | 株式会社コスモステクニカルセンター | Anti-oxidant derived from microalgae and cosmetic or skin external preparation containing the same |
FR3034780B1 (en) * | 2015-04-10 | 2018-10-19 | Societe D'exploitation De Produits Pour Les Industries Chimiques Seppic | PROCESS FOR OBTAINING CULTURE OF CELLS OF RED ALGAE ACROCHAETIUM MONILIFORM, METHOD FOR OBTAINING EXTRACT FROM BIOMASS AND USE THEREOF IN COSMETICS |
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