JP5892716B2 - Oral composition - Google Patents
Oral composition Download PDFInfo
- Publication number
- JP5892716B2 JP5892716B2 JP2006084849A JP2006084849A JP5892716B2 JP 5892716 B2 JP5892716 B2 JP 5892716B2 JP 2006084849 A JP2006084849 A JP 2006084849A JP 2006084849 A JP2006084849 A JP 2006084849A JP 5892716 B2 JP5892716 B2 JP 5892716B2
- Authority
- JP
- Japan
- Prior art keywords
- extract
- plant
- gtase
- genus
- plaque
- 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 34
- 108010043797 4-alpha-glucanotransferase Proteins 0.000 claims description 60
- 102100039604 mRNA guanylyltransferase Human genes 0.000 claims description 60
- 108010026228 mRNA guanylyltransferase Proteins 0.000 claims description 60
- 239000000284 extract Substances 0.000 claims description 57
- 241000219925 Oenothera Species 0.000 claims description 40
- 241000196324 Embryophyta Species 0.000 claims description 32
- 239000003112 inhibitor Substances 0.000 claims description 28
- 210000000214 mouth Anatomy 0.000 claims description 24
- 238000004519 manufacturing process Methods 0.000 claims description 22
- 239000002798 polar solvent Substances 0.000 claims description 18
- 235000004496 Oenothera biennis Nutrition 0.000 claims description 15
- 208000002925 dental caries Diseases 0.000 claims description 14
- 238000002156 mixing Methods 0.000 claims description 8
- 241001107098 Rubiaceae Species 0.000 claims description 6
- 241000207834 Oleaceae Species 0.000 claims description 3
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- 240000006055 Dacrydium cupressinum Species 0.000 claims 2
- 235000013697 Pinus resinosa Nutrition 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 description 42
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 41
- 239000000419 plant extract Substances 0.000 description 36
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 28
- 239000002324 mouth wash Substances 0.000 description 26
- 230000007505 plaque formation Effects 0.000 description 26
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- 238000012360 testing method Methods 0.000 description 20
- 238000000605 extraction Methods 0.000 description 19
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- VZSRBBMJRBPUNF-UHFFFAOYSA-N 2-(2,3-dihydro-1H-inden-2-ylamino)-N-[3-oxo-3-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)propyl]pyrimidine-5-carboxamide Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C(=O)NCCC(N1CC2=C(CC1)NN=N2)=O VZSRBBMJRBPUNF-UHFFFAOYSA-N 0.000 description 9
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- WJLVQTJZDCGNJN-UHFFFAOYSA-N Chlorhexidine hydrochloride Chemical compound Cl.Cl.C=1C=C(Cl)C=CC=1NC(N)=NC(N)=NCCCCCCN=C(N)N=C(N)NC1=CC=C(Cl)C=C1 WJLVQTJZDCGNJN-UHFFFAOYSA-N 0.000 description 2
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- 239000002202 Polyethylene glycol Substances 0.000 description 2
- PXIPVTKHYLBLMZ-UHFFFAOYSA-N Sodium azide Chemical compound [Na+].[N-]=[N+]=[N-] PXIPVTKHYLBLMZ-UHFFFAOYSA-N 0.000 description 2
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- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
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Classifications
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- 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)
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- 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
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9728—Fungi, e.g. yeasts
-
- 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
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/74—Biological properties of particular ingredients
- A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
- A61K2800/782—Enzyme inhibitors; Enzyme antagonists
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Epidemiology (AREA)
- Botany (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Birds (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Alternative & Traditional Medicine (AREA)
- Medical Informatics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Oral & Maxillofacial Surgery (AREA)
- Cosmetics (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Medicines Containing Plant Substances (AREA)
Description
本発明は、優れたGTase阻害作用を有し、歯垢の形成を抑制してう蝕を効果的に予防できる口腔用組成物に関する。 The present invention relates to an oral composition that has an excellent GTase inhibitory action and can effectively prevent dental caries by suppressing the formation of dental plaque.
口腔内の疾患の1つとして、う蝕(虫歯)が知られている。このう蝕の発生機序は、次のように考えられている。歯表面には、だ液中の成分である糖タンパク質によってペリクル層が形成されており、このペリクル層にミュータンス菌等の細菌が付着する。この細菌は、菌体外に分泌する酵素であるグルコシルトランスフェラーゼ(以下、「GTase」と表記する)の作用により、食物由来のショ糖を粘着性多糖類に変性させ、更に増殖しながら強固に歯面に付着する。これを一般に歯垢(プラーク)と呼ぶが、付着した細菌は、歯垢中で糖類を代謝し、その代謝産物として酸を生成する。そしてこの酸が歯のエナメル表面を脱灰することにより、う蝕が引き起こされる。また歯垢は、う蝕の他、口臭、歯周病、歯肉炎、歯槽膿漏の原因になるとも言われている。 As one of the diseases in the oral cavity, caries (tooth decay) is known. The occurrence mechanism of this caries is considered as follows. On the tooth surface, a pellicle layer is formed by glycoprotein which is a component in saliva, and bacteria such as mutans bacteria adhere to the pellicle layer. This bacterium is modified by the action of glucosyltransferase (hereinafter referred to as “GTase”), an enzyme that is secreted outside the cell body, to denature food-derived sucrose into an adhesive polysaccharide, and further grows firmly in the teeth. Adhere to the surface. This is generally called plaque, but the attached bacteria metabolize saccharides in plaque and produce acid as a metabolite. This acid then decalcifies the tooth enamel surface, causing caries. In addition to dental caries, plaque is said to cause halitosis, periodontal disease, gingivitis, and alveolar pus leakage.
今日では、う蝕を予防する1つの方策として、GTaseの作用を阻害して、歯垢の形成を抑制することが有効であると考えられている。このような観点から、近年、GTase阻害作用を有する物質の開発が精力的に行われており、GTase阻害作用を有する植物抽出物が種々報告されている(例えば、特許文献1参照)。しかしながら、これまで報告されている植物抽出物では、GTase阻害作用が十分でない等の理由で実用に供し得ないものも多く、更なるGTase阻害成分及びそれを用いた口腔用組成物の開発、提供が望まれている。
そこで本発明は、優れたGTase阻害作用を有し、歯垢の形成を抑制することにより、う蝕を効果的に予防できる口腔用組成物を提供することを目的とする。 Therefore, an object of the present invention is to provide an oral composition that has an excellent GTase inhibitory action and can effectively prevent dental caries by suppressing the formation of plaque.
本発明者は、上記課題を解決すべく鋭意検討したところ、アカバナ科マツヨイグサ属植物の極性溶媒抽出物には、優れたGTase阻害作用があり、該抽出物を含有する口腔用組成物は、う蝕の予防に有用であることを見出した。本発明は、かかる知見に基づいて、更に改良を重ねることにより完成したものである。 The present inventor has intensively studied to solve the above-mentioned problems. As a result, the polar solvent extract of the plant of the genus Ranaaceae has an excellent GTase inhibitory action. It was found that it is useful for prevention of pitting. The present invention has been completed by making further improvements based on such findings.
即ち、本発明は、下記に掲げる態様の発明を包含する:
項1. アカバナ科マツヨイグサ属植物の極性溶媒抽出物を含有することを特徴とする、抗う蝕用口腔用組成物。
項2. アカバナ科マツヨイグサ属植物の極性溶媒抽出物を0.00001〜20重量%含有する項1に記載の抗う蝕用口腔用組成物。
項3. 前記抽出物が、アカバナ科マツヨイグサ属植物の種子の抽出物である、項1又は2に記載の抗う蝕用口腔用組成物。
項4. アカバナ科マツヨイグサ属植物が、メマツヨイグサである、項1乃至3のいずれか1項に記載の抗う蝕用口腔用組成物。
That is, this invention includes the invention of the aspect hung up below:
Item 1. A composition for oral cavity for anti-caries , comprising a polar solvent extract of a plant of the genus Rubiaceae.
Item 2. Item 2. The oral cavity composition for caries according to Item 1, which contains 0.00001 to 20% by weight of a polar solvent extract of the plant of the genus Rubiaceae.
Item 3. Item 3. The oral cavity composition for caries according to Item 1 or 2 , wherein the extract is an extract of a seed of the genus Oleaceae.
Item 4. Item 4. The oral cavity composition for anti-carious disease according to any one of Items 1 to 3 , wherein the plant of the genus Rabbitaceae is an evening primrose.
本発明の口腔用組成物は、アカバナ科マツヨイグサ属(Oenothera)植物の極性溶媒抽出物を含有することを特徴とする。 The composition for oral cavity of the present invention is characterized by containing a polar solvent extract of a plant of the genus Oenothera .
本発明で使用されるアカバナ科マツヨイグサ属植物としては、特に制限されず、例えば、メマツヨイグサ(Oenothera biennis)、マツヨイグサ(Oenothera striata)、オオマツヨイグサ(Oenothera erythrosepala)、コマツヨイグサ(Oenotheralaciniata)等が例示される。これらの中で、好ましくはメマツヨイグサである。 The onagraceae evening primrose genus plants used in the present invention is not particularly limited, for example, evening primrose (Oenothera biennis), evening primrose (O enothera striata), evening primrose (Oenothera erythrosepala), Oenothera laciniata (Oenotheralaciniata) and the like . Of these, the evening primrose is preferable.
当該アカバナ科マツヨイグサ属植物の抽出物は、該植物体の全草、又は種子、根、茎、葉、花蕾等の該植物体の一部から抽出されたものであればよいが、好ましくは該植物の種子から抽出されたものである。 The extract of the genus Oenothera spp. Is not limited as long as it is extracted from the whole plant of the plant or a part of the plant such as seeds, roots, stems, leaves, and florets. Extracted from plant seeds.
また、アカバナ科マツヨイグサ属植物の抽出物の抽出に使用される溶媒としては、極性溶媒である限り、特に制限されない。このような極性溶媒としては、例えば、水;メタノール、エタノール、プロパノール、イソプロピルアルコール、ブタノール等の炭素数1〜5の低級アルコール;、1,3−ブチレングリコール、グリセリン、ポリエチレングリコール等の多価アルコール;アセトン;エチルエーテル;酢酸エチル;酢酸メチル等が例示される。これらの極性溶媒は、1種単独で用いてもよく、2種以上を組み合わせて用いてもよい。当該抽出溶媒として、好ましくは水、炭素数1〜5の低級アルコール、及び炭素数1〜5の低級アルコールと水の混合液;更に好ましくは水、エタノール、及びエタノールと水の混合液;特に好ましくはエタノールと水の混合液が挙げられる。抽出溶媒として、炭素数1〜5の低級アルコールと水の混合液を使用する場合、該混合液の総重量に対する該低級アルコールの含有割合としては、例えば0.0001〜99.9重量%、好ましくは40〜99.9重量%、更に好ましくは50〜90重量%となる割合が挙げられる。 Moreover, as a solvent used for the extraction of the extract of the genus Ranunculaceae, there is no particular limitation as long as it is a polar solvent. Examples of such polar solvents include water; lower alcohols having 1 to 5 carbon atoms such as methanol, ethanol, propanol, isopropyl alcohol, and butanol; polyhydric alcohols such as 1,3-butylene glycol, glycerin, and polyethylene glycol. Acetone; ethyl ether; ethyl acetate; methyl acetate and the like. These polar solvents may be used alone or in combination of two or more. The extraction solvent is preferably water, a lower alcohol having 1 to 5 carbon atoms, and a mixed liquid of water having a lower alcohol having 1 to 5 carbon atoms and water; more preferably water, ethanol, and a mixed liquid of ethanol and water; Is a mixture of ethanol and water. When a mixed solution of lower alcohol having 1 to 5 carbon atoms and water is used as the extraction solvent, the content ratio of the lower alcohol to the total weight of the mixed solution is, for example, 0.0001 to 99.9% by weight, preferably Is a ratio of 40 to 99.9% by weight, more preferably 50 to 90% by weight.
アカバナ科マツヨイグサ属植物の抽出物は、上記抽出対象植物部位をそのまま、或いは必要に応じて、乾燥、細切、破砕、圧搾、煮沸或いは発酵処理したものを、上記抽出溶媒により抽出することによって得られる。抽出方法としては、通常用いられている植物抽出物の抽出方法を採用することができ、具体的には、冷浸、温浸等の浸漬法;加温下で攪拌する方法;又はパーコレーション法等が例示される。 The extract of the genus Rhizophoraceae is obtained by extracting the plant part to be extracted as it is or after drying, shredded, crushed, pressed, boiled or fermented with the above extraction solvent. It is done. As the extraction method, a commonly used extraction method for plant extracts can be employed, and specifically, immersion methods such as cold immersion and digestion; a method of stirring under heating; or a percolation method, etc. Is exemplified.
なお、アカバナ科マツヨイグサ属植物を極性溶媒で抽出するのに先立って、前処理として、圧搾法又はヘキサン等の非極性有機溶媒を使用することにより予め脱脂処理を行い、抽出処理時に該植物から余分な脂質が抽出されるのを防止しておくことが望ましい。 In addition, prior to the extraction of the genus Avenidae with a polar solvent, as a pretreatment, a degreasing treatment is performed in advance by using a non-polar organic solvent such as a pressing method or hexane, and an extra portion is removed from the plant during the extraction treatment. It is desirable to prevent the extraction of fresh lipids.
上記方法で得られるアカバナ科マツヨイグサ属植物の抽出物は液状であり、本発明では、該抽出物を液状のまま使用してもよく、また必要に応じて濃縮、乾燥等の処理に供して濃縮物や乾燥物として使用してもよい。また濃縮又は乾燥後、該濃縮又は乾燥物を非溶解性溶媒で洗浄して精製して用いてもよく、またこれを更に適当な溶剤に溶解もしくは懸濁して用いることもできる。また、得られた抽出物を、慣用されている精製法、例えば向流分配法や液体クロマトグラフィー等を用いて、GTase阻害活性を有する画分を取得、精製して使用することも可能である。 The extract of the plant of the genus Rubiaceae obtained by the above method is in a liquid state, and in the present invention, the extract may be used in a liquid state, and it is concentrated by subjecting it to a treatment such as concentration and drying as necessary. You may use as a thing or a dry thing. Further, after concentration or drying, the concentrated or dried product may be used after being purified by washing with an insoluble solvent, or may be used by further dissolving or suspending it in an appropriate solvent. It is also possible to obtain and purify a fraction having GTase inhibitory activity using the obtained extract using a conventional purification method such as a countercurrent distribution method or liquid chromatography. .
また、簡便には、アカバナ科マツヨイグサ属植物の抽出物としては、商業的に入手できるものを使用することもできる。 In addition, for convenience, a commercially available extract can be used as the extract of the plant of the genus Ranunculaceae.
本発明の口腔用組成物において、上記アカバナ科マツヨイグサ属植物の抽出物の配合割合は、口腔用組成物の形態、抽出物の濃縮率等に応じて異なり、一律に規定することができないが、一例として、口腔用組成物の総量に対して、該抽出物(乾燥重量換算)が、通常0.00001〜20重量%、好ましくは0.0001〜10重量%、更に好ましくは0.001〜5重量%となる割合が例示される。 In the composition for oral cavity of the present invention, the blending ratio of the extract of the genus Acanthaceae, which depends on the form of the composition for oral cavity, the concentration rate of the extract, etc., cannot be defined uniformly. As an example, the extract (in terms of dry weight) is usually 0.00001 to 20% by weight, preferably 0.0001 to 10% by weight, more preferably 0.001 to 5%, based on the total amount of the composition for oral cavity. The ratio which becomes weight% is illustrated.
本発明の口腔用組成物には、上記アカバナ科マツヨイグサ属植物の抽出物に加えて、う蝕性細菌に対する抗菌剤や他のGTase阻害物質を組み合わせて配合することにより、抗う蝕効果を相加的若しくは相乗的に増強しておくこともできる。このような抗菌剤としては、例えば、塩酸クロルヘキシジン、塩化セチルピリジニウム、ソルビン酸、ヒノキチオール、イソプロピルメチルフェノール、塩化デカリニウム、トリクロサン、塩酸クロルヘキシジン、ヨウ化カリウム等が挙げられる。また、他のGTase阻害物質としては、例えば、ブドウ科ブドウ属(Vitis)植物の抽出物、デキストラナーゼ、ムタナーゼ、モノフルオロリン酸ナトリウム、フッ化ナトリウム、フッ化第一錫、タステイン、タンニン類、エラグ酸、ポリフェノール、ウーロン茶抽出物、緑茶抽出物、センブリ、タイソウ、ウイキョウ、芍薬、ゲンチアナ、センソ、龍胆、黄連等が挙げられる。 The composition for oral cavity of the present invention has an anti-cariogenic effect by combining it with an antibacterial agent against carious bacteria and other GTase inhibitors in addition to the above-mentioned extract of the genus Rhizopus. It can also be strengthened synergistically or synergistically. Examples of such antibacterial agents include chlorhexidine hydrochloride, cetylpyridinium chloride, sorbic acid, hinokitiol, isopropylmethylphenol, decalinium chloride, triclosan, chlorhexidine hydrochloride, potassium iodide and the like. Other GTase inhibitors include, for example, Vitis plant extracts, dextranase, mutanase, sodium monofluorophosphate, sodium fluoride, stannous fluoride, tastein, tannins , Ellagic acid, polyphenol, oolong tea extract, green tea extract, assembly, Taiso, fennel, glaze, gentian, senso, rye gall, yellow ream and the like.
本発明の口腔用組成物の好適な一実施態様として、上記アカバナ科マツヨイグサ属植物の極性溶媒抽出物に加えて、更にGTase阻害物質としてブドウ科ブドウ属植物の抽出物を含有するものが例示される。 As a preferred embodiment of the composition for oral cavity of the present invention, in addition to the polar solvent extract of the above-mentioned Aceraceae Oenothera genus plant, a composition further containing an extract of a Grapeaceae genus plant as a GTase inhibitor is exemplified. The
当該ブドウ科ブドウ属植物としては、特に制限されず、ヨーロッパブドウ(Vitis viniferaL.)やアメリカブドウ(Vitis labruscaL.)等を使用することができる。好ましくは、ヨーロッパブドウである。 The grapevine genus plant is not particularly limited, and European grape ( Vitis vinifera L.), American grape ( Vitis labrusca L.) and the like can be used. Preferred is European grape.
当該ブドウ科ブドウ属植物の抽出物は、該植物体の葉部、茎部、根部又はこれらの混合物から抽出されたものであればよいが、好ましくは葉部から抽出されたものである。 Although the extract of the grape genus Grapes plant should just be extracted from the leaf part, stem part, root part, or these mixture of this plant body, Preferably it is extracted from the leaf part.
また、ブドウ科ブドウ属植物の抽出物の抽出に使用される溶媒としては、特に制限されないが、例えば、水;メタノール、エタノール、プロパノール、イソプロピルアルコール、ブタノール等の炭素数1〜5の低級アルコール;、1,3−ブチレングリコール、グリセリン、ポリエチレングリコール等の多価アルコール;アセトン;エチルエーテル;酢酸エチル;酢酸メチル等の極性溶媒が例示される。これらの溶媒は、1種単独で用いてもよく、2種以上を組み合わせて用いてもよい。当該抽出溶媒として、好ましくは水、炭素数1〜5の低級アルコール、及び炭素数1〜5の低級アルコールと水の混合液;更に好ましくは水、エタノール、及びエタノールと水の混合液;特に好ましくは水が挙げられる。抽出溶媒として、炭素数1〜5の低級アルコールと水の混合液を使用する場合、該混合液の総重量に対する該低級アルコールの含有割合としては、例えば0.1〜99.9重量%、好ましくは0.1〜70重量%、更に好ましくは0.1〜50重量%となる割合が挙げられる。 In addition, the solvent used for the extraction of the extract of the genus Grapeaceae is not particularly limited. For example, water; lower alcohols having 1 to 5 carbon atoms such as methanol, ethanol, propanol, isopropyl alcohol, butanol; Examples include polyhydric alcohols such as 1,3-butylene glycol, glycerin and polyethylene glycol; polar solvents such as acetone; ethyl ether; ethyl acetate; These solvent may be used individually by 1 type, and may be used in combination of 2 or more type. The extraction solvent is preferably water, a lower alcohol having 1 to 5 carbon atoms, and a mixed liquid of water having a lower alcohol having 1 to 5 carbon atoms and water; more preferably water, ethanol, and a mixed liquid of ethanol and water; Is water. When a mixed liquid of a lower alcohol having 1 to 5 carbon atoms and water is used as the extraction solvent, the content ratio of the lower alcohol to the total weight of the mixed liquid is, for example, 0.1 to 99.9% by weight, preferably Is 0.1 to 70% by weight, more preferably 0.1 to 50% by weight.
ブドウ科ブドウ属植物の抽出物の抽出は、上記アカバナ科マツヨイグサ属植物の抽出物の場合と同様の方法で行うことができる。なお、ブドウ科ブドウ属植物の溶媒抽出に先立って、前処理として、圧搾法又はヘキサン等の非極性有機溶媒を使用することにより予め該植物に対して脱脂処理を行ってもよい。 Extraction of an extract of a vine belonging to the genus Grapeaceae can be performed by a method similar to the case of the extract of the genus Acanthaceae. Prior to solvent extraction of Grapeaceae plants, as a pretreatment, the plant may be preliminarily degreased by using a pressing method or a nonpolar organic solvent such as hexane.
ブドウ科ブドウ属植物の抽出物は、上記アカバナ科マツヨイグサ属植物の抽出物の場合と同様、液状であってもよく、濃縮物や乾燥物の状態であってもよい。 As in the case of the above-mentioned extract of the genus Aceraceae, the extract of the grape genus grape genus plant may be liquid, or may be in the form of a concentrate or a dried product.
本発明の口腔用組成物に上記ブドウ科ブドウ属植物の抽出物を配合する場合、該抽出物の配合割合としては、特に制限されないが、例えば、0.00001〜20重量%、好ましくは0.0001〜10重量%、更に好ましくは0.001〜5重量%となる割合が挙げられる。 When blending the above-mentioned grapevine plant extract in the oral composition of the present invention, the blending ratio of the extract is not particularly limited, but is, for example, 0.00001 to 20% by weight, preferably 0.8. A ratio of 0001 to 10% by weight, more preferably 0.001 to 5% by weight, is mentioned.
本発明の口腔用組成物には、その形態に応じて、口腔用組成物に通常使用される成分を含有していてもよい。このような成分としては、制限されないが、例えば、研磨剤、粘結剤、粘稠剤、発泡剤、香料、矯味剤、甘味剤、防腐剤、消炎剤、殺菌剤、抗菌剤、色素、増粘剤、界面活性剤、pH調整剤、酸化防止剤等が挙げられる。 The composition for oral cavity of the present invention may contain components usually used in the composition for oral cavity depending on its form. Examples of such components include, but are not limited to, abrasives, binders, thickeners, foaming agents, fragrances, flavoring agents, sweeteners, preservatives, anti-inflammatory agents, disinfectants, antibacterial agents, dyes, Examples thereof include a viscosity agent, a surfactant, a pH adjuster, and an antioxidant.
本発明において、口腔用組成物とは、例えば経口的に摂取される組成物、及び歯磨きやマウスウォッシュのように口腔内で用いられる組成物の双方を含むものである。 In the present invention, the oral composition, is intended to include both compositions that are used in the oral cavity as through the mouth to ingested composition, and toothpaste and mouthwash, for example.
本発明の口腔用組成物の具体例としては、可食性フィルム、トローチ、タブレット、顆粒、カプセル;ドリンク剤;歯磨剤(練り状、液体状、粉末固形状),口中清涼剤(マウススプレー等)、咀嚼剤、トローチ剤、口腔用パスタ剤、うがい剤、シロップ剤、歯肉マッサージクリーム等の医薬品又は医薬部外品;歯磨剤、マウスウォッシュ、マウスリンスなどの口腔内化粧品を挙げることができる。これらの中で好ましくは、可食性フィルム、歯磨剤、口中清涼剤、洗口剤(マウスウォッシュ)、マウスリンス等を挙げることができる。これらの形態並びに剤形は、特に制限されず、種類に応じて任意に定めることができる。 Specific examples of the oral composition of the present invention, edible films, lozenges, the tablet, granule, capsule Le; drinks; dentifrices (kneaded-like, liquid, powder solid), breath fresheners (mouth spray Etc.), chewing agents, lozenges, oral pastes, gargles, syrups, gingival massage creams and other drugs or quasi-drugs; oral cosmetics such as dentifrices, mouthwashes, mouth rinses, etc. . Preferably Among these may be mentioned edible films, dental Migakuzai, breath fresheners, mouthwash (mouth wash), a mouthrinse or the like. These forms and dosage forms are not particularly limited, and can be arbitrarily determined according to the type.
また、本発明の口腔用組成物は、含有するアカバナ科マツヨイグサ属植物の極性溶媒抽出物の作用により、GTase阻害効果、歯垢形成阻害効果、抗う蝕効果等の効果を奏することができる。即ち、本発明の口腔用組成物は、GTase阻害剤、歯垢形成阻害剤、又は抗う蝕剤として有用である。更に、本発明は、他の観点から、下記態様の発明を提供する:
(1) アカバナ科マツヨイグサ属植物の極性溶媒抽出物を含有することを特徴とする、GTase阻害剤、歯垢形成阻害剤又は抗う蝕剤。
(2) 前記抽出物が、アカバナ科マツヨイグサ属植物の種子の抽出物である、(1)に記載のGTase阻害剤、歯垢形成阻害剤又は抗う蝕剤。
(3) アカバナ科マツヨイグサ属植物がメマツヨイグサである、(1)又は(2)に記載のGTase阻害剤、歯垢形成阻害剤又は抗う蝕剤。
(4) アカバナ科マツヨイグサ属植物の前記抽出物が、該剤の総量に対して、0.00001〜20重量%、好ましくは0.0001〜10重量%、更に好ましくは0.001〜5重量%の割合で含有されている、(1)乃至(3)のいずれかに記載のGTase阻害剤、歯垢形成阻害剤又は抗う蝕剤。
(5) 更に、ブドウ科ブドウ属植物の葉部、茎部、根部又はこれらの混合物の抽出物を含有する、(1)乃至(4)のいずれかに記載のGTase阻害剤、歯垢形成阻害剤又は抗う蝕剤。
(6) ブドウ科ブドウ属植物の抽出物が、極性溶媒を使用して得られるものである、(5)に記載のGTase阻害剤、歯垢形成阻害剤又は抗う蝕剤。
(7) ブドウ科ブドウ属植物がヨーロッパブドウである、(5)又は(6)に記載のGTase阻害剤、歯垢形成阻害剤又は抗う蝕剤。
(8) ブドウ科ブドウ属植物の前記抽出物が、該剤の総量に対して、0.00001〜20重量%、好ましくは0.0001〜10重量%、更に好ましくは0.001〜5重量%の割合で含有されている、(5)乃至(7)のいずれかに記載のGTase阻害剤、歯垢形成阻害剤又は抗う蝕剤。
(9) 口腔組成物である、(1)乃至(8)のいずれかに記載のGTase阻害剤、歯垢形成阻害剤又は抗う蝕剤。
(10)医薬品、医薬部外品又は口腔内化粧品である、(9)に記載のGTase阻害剤、歯垢形成阻害剤又は抗う蝕剤。
Moreover, the composition for oral cavity of this invention can show effects, such as a GTase inhibitory effect, a plaque formation inhibitory effect, an anti-caries effect, by the effect | action of the polar-solvent extract of the Acrobaceae evening primrose plant to contain. That is, the oral composition of the present invention is useful as a GTase inhibitor, a plaque formation inhibitor, or an anti-cariogenic agent. Furthermore, the present invention provides the following aspects of the invention from another viewpoint:
(1) A GTase inhibitor, a plaque formation inhibitor or an anti-cariogenic agent, characterized by containing a polar solvent extract of a plant belonging to the genus Rubiaceae.
(2) The GTase inhibitor, plaque formation inhibitor or anti-cariogenic agent according to (1), wherein the extract is an extract of the seeds of the genus Oenothera spp.
(3) The GTase inhibitor, plaque formation inhibitor, or anti-cariogenic agent according to (1) or (2), wherein the plant of the genus Ranunculaceae is the evening primrose.
(4) The above-mentioned extract of the genus Ranaaceae is 0.00001 to 20% by weight, preferably 0.0001 to 10% by weight, more preferably 0.001 to 5% by weight, based on the total amount of the agent. The GTase inhibitor, plaque formation inhibitor or anti-cariogenic agent according to any one of (1) to (3), which is contained in a proportion of
(5) In addition, the GTase inhibitor according to any one of (1) to (4), further comprising an extract of a leaf part, a stem part, a root part, or a mixture thereof, of a Grapeaceae genus plant, plaque formation inhibition Or anti-cariogenic agent.
(6) The GTase inhibitor, plaque formation inhibitor or anti-cariogenic agent according to (5), wherein the extract of the Grapeaceae genus plant is obtained using a polar solvent.
(7) The GTase inhibitor, plaque formation inhibitor or anti-cariogenic agent according to (5) or (6), wherein the Grapeaceae genus plant is European grape.
(8) The extract of the Grapeaceae genus plant is 0.00001 to 20% by weight, preferably 0.0001 to 10% by weight, more preferably 0.001 to 5% by weight, based on the total amount of the agent. The GTase inhibitor, plaque formation inhibitor or anti-cariogenic agent according to any one of (5) to (7), which is contained in a proportion of
(9) The GTase inhibitor, plaque formation inhibitor or anti-cariogenic agent according to any one of (1) to (8), which is an oral composition.
(10) and Drug, a quasi drug or oral cosmetics, GTase inhibitors, plaque formation inhibitor or anti-dental caries agent according to (9).
なお、上記GTase阻害剤、歯垢形成阻害剤及び抗う蝕剤において、使用するアカバナ科マツヨイグサ属植物の極性溶媒抽出物、当該抽出物の配合割合、該阻害剤に配合可能な成分、使用形態等については、前述する口腔用組成物の場合を援用することができる。 In addition, in the above GTase inhibitor, plaque formation inhibitor, and anti-cariogenic agent, the polar solvent extract of the plant of the genus Aceraceae that is used, the blending ratio of the extract, the components that can be blended in the inhibitor, the form of use, etc. About the case of the composition for oral cavity mentioned above can be used.
本発明の口腔組成物によれば、アカバナ科マツヨイグサ属植物の極性溶媒抽出物の作用に基づいて、口腔内で優れたGTase阻害効果を奏することができ、これによって、歯垢形成を阻害してう蝕を効果的に予防することができる。 According to the oral composition of the present invention, an excellent GTase inhibitory effect can be achieved in the oral cavity based on the action of the polar solvent extract of the genus Oenothera spp., Thereby inhibiting plaque formation. Caries can be effectively prevented.
また、本発明の口腔用組成物に配合されるアカバナ科マツヨイグサ属植物の極性溶媒抽出物は、天然由来成分で高い安全性を備えている。 Moreover, the polar solvent extract of the plant of the genus Rubiaceae that is blended in the composition for oral cavity of the present invention is a naturally derived component and has high safety .
以下、実施例を挙げて本発明を説明するが、本発明はこれらの実施例に限定されるものではない。 EXAMPLES Hereinafter, although an Example is given and this invention is demonstrated, this invention is not limited to these Examples.
製造例1
メマツヨイグサ(Oenothera biennis)植物の種子の粉砕物100gに対して、常法に従って脱脂処理した後、濾過により残渣を回収した。脱脂された脱脂種子粉砕物を乾燥させた後、抽出溶媒として水エタノール混合液(水30重量%、エタノール70重量%含有)を用いて、45〜55℃で2時間抽出を行った。次いで、濾過により残渣を除去して抽出液を得、これをエバポレーターにて濃縮、噴霧乾燥することにより、植物抽出物(以下、「マツヨイグサ属植物抽出物」と表記する)5gを得た。
Production Example 1
100 g of pulverized seeds of Oenothera biennis plant were degreased according to a conventional method, and the residue was collected by filtration. After the defatted defatted seed pulverized product was dried, extraction was performed at 45 to 55 ° C. for 2 hours using a water ethanol mixed solution (containing 30 wt% water and 70 wt% ethanol) as an extraction solvent. Next, the residue was removed by filtration to obtain an extract, which was concentrated with an evaporator and spray-dried to obtain 5 g of a plant extract (hereinafter referred to as “Oenothera plant extract”).
参考製造例1
ヨーロッパブドウ(Vitis vinifera L.)の葉の粉砕物を原料として、抽出溶媒として精製水を用いて、浸漬法により抽出処理を行った。抽出処理後、濾過により残渣を除去して抽出液を得、これをエバポレーターにて濃縮、噴霧乾燥することにより、植物抽出物(以下、「ブドウ属植物抽出物」と表記する)を得た。
Reference production example 1
Extraction processing was performed by a dipping method using a ground product of European grape ( Vitis vinifera L.) as a raw material and purified water as an extraction solvent. After the extraction treatment, the residue was removed by filtration to obtain an extract, which was concentrated and spray-dried with an evaporator to obtain a plant extract (hereinafter referred to as “Grape plant extract”).
試験例1 Streptococcus sobrinusが産生するGTaseに対する阻害作用の評価
Streptococcus sobrinus 6715株(大阪大学歯学部より分与)が産生するGTaseに対するマツヨイグサ属植物抽出物の阻害作用を評価するために、以下の試験を行った。
1.Streptococcus sobrinus 6715株産生GTaseの調製
(1)培地の調製
Trypticase 15g、Tryptose 4g、yeast extract 4g、K2HPO42g、KH2PO4 5g、Na2CO32g、及びNaCl 2gに水を添加して合計900mlにメスアップした。また、別途、glucose 10gに水を添加して合計100mlにメスアップした。これらを別々の加熱滅菌した後、培養前に、これらを混合することによって、培地を調製した。
(2)Streptococcus sobrinus6715株の培養
前培養しておいたStreptococcussobrinus 6715株を上記培地 1000mlに植菌し、37℃で18時間、静置培養を行った。
(3)GTaseの精製
上記(2)で得られた培養液を遠心分離し、上清を回収した。得られた上清に終濃度50重量%となるように硫酸アンモニウムを添加した後、再度遠心分離を行い、沈殿を回収した。回収した沈殿をリン酸緩衝液(pH6.5)で洗浄した後、再度遠心分離を行い、沈殿を回収した。得られた沈殿に、リン酸緩衝液(pH6.5)を適量加えて、これと同緩衝液を用いて透析を行った。透析後に、GTaseを含む溶液を回収し、これをGTase液とした。得られたGTase液は、−80℃で保存した。
Test Example 1 Evaluation of inhibitory effect on GTase produced by Streptococcus sobrinus
In order to evaluate the inhibitory action of Oenothera genus plant extracts on GTase produced by Streptococcus sobrinus 6715 (distributed from Osaka University School of Dentistry), the following test was conducted.
1. Preparation of Streptococcus sobrinus 6715 production GTase
(1) Preparation of medium
Water was added to 15 g of Trypticase, 4 g of Tryptose, 4 g of yeast extract, 2 g of K 2 HPO 4 , 5 g of KH 2 PO 4 , 2 g of Na 2 CO 3 , and NaCl 2 g to make a total of 900 ml. Separately, water was added to 10 g of glucose to make a total of 100 ml. After these were heat sterilized separately and before culturing, the medium was prepared by mixing them.
(2) a Streptococcus sobrinus 6715 strain Streptococcussobrinus 6715 strain that had been pre-cultured culture was inoculated into the above medium 1000 ml, 18 hours at 37 ° C., was stationary culture.
(3) Purification of GTase The culture solution obtained in (2) above was centrifuged, and the supernatant was recovered. Ammonium sulfate was added to the obtained supernatant to a final concentration of 50% by weight, and then centrifuged again to collect the precipitate. The collected precipitate was washed with a phosphate buffer (pH 6.5) and then centrifuged again to collect the precipitate. An appropriate amount of phosphate buffer (pH 6.5) was added to the resulting precipitate, and dialysis was performed using the same buffer. After dialysis, a solution containing GTase was collected and used as a GTase solution. The obtained GTase solution was stored at −80 ° C.
2.Streptococcus sobrinus 6715株産生GTaseに対する阻害作用の評価試験
96穴プレートの各穴に、基質液(0.1M リン酸緩衝液(pH6.5)、2重量%スクロース、0.1重量%アジ化ナトリウム、40μM デキストラン10(分子量1万)含有)260μl、GTase液20μl、及びマツヨイグサ属植物抽出物溶液(穴中のマツヨイグサ属植物抽出物の終濃度が0.063〜2mg/mlとなるように調整)20μlを添加し、37℃で18時間インキュベートした。その後、合成されたグルカンの量を求めるために、550nmの吸光度を測定した。また、コントロールとして、マツヨイグサ属植物抽出物を添加しなかった穴についても同様に測定を行った。コントロールの550nmの吸光度をGTase活性値100%として、各濃度のマツヨイグサ属植物抽出物共存下でのGTase活性値(%)を算出した。また、比較として、GTase阻害活性が公知であるウーロン茶抽出物(商品名「サンウーロン」サントリー(株)製)を用いて、上記と同様に試験を行った。また、参考として、ブドウ属植物抽出物を用いて、上記と同様に試験を行った。
2. Evaluation test of inhibitory action against Streptococcus sobrinus 6715 production GTase In each hole of 96-well plate, substrate solution (0.1 M phosphate buffer (pH 6.5), 2 wt% sucrose, 0.1 wt% sodium azide, 40 μM dextran 10 (Molecular weight 10,000) included) 260 μl, GTase solution 20 μl, and Oenothera plant extract solution (adjusted so that the final concentration of Oenothera plant extract in the hole is 0.063-2 mg / ml) are added, 37 Incubated for 18 hours at ° C. Thereafter, the absorbance at 550 nm was measured in order to determine the amount of synthesized glucan. Further, as a control, the same measurement was performed on a hole to which no extract of the genus Oenothera was added. Taking the absorbance at 550 nm of the control as the GTase activity value of 100%, the GTase activity value (%) in the presence of the extract of the genus Oenothera plant at each concentration was calculated. For comparison, a test was performed in the same manner as described above, using a oolong tea extract (trade name “San Oolong” manufactured by Suntory Ltd.) with a known GTase inhibitory activity. For reference, a test was carried out in the same manner as described above using a grape plant extract.
得られた結果を図1に示す。この結果から、マツヨイグサ属植物抽出物には、ウーロン茶抽出物に比して、顕著に優れたGTase阻害作用があることが確認され、該抽出物は、有効な抗う蝕作用を発揮できることが明らかとなった。また、参考のため評価したブドウ属植物抽出物についても、優れたGTase阻害作用があることが確認された。 The obtained results are shown in FIG. From this result, it was confirmed that the Oenothera genus plant extract has a significantly superior GTase inhibitory action compared to the oolong tea extract, and it is clear that the extract can exhibit an effective anti-cariogenic action. became. In addition, it was confirmed that the grape plant extract evaluated for reference has an excellent GTase inhibitory action.
試験例2 Streptococcus sobrinusが産生するGTaseに対する阻害作用の評価
更に、Streptococcus sobrinus 6715株(大阪大学歯学部より分与)が産生するGTaseに対するマツヨイグサ属植物抽出物の阻害作用を評価するために、上記試験例1と同様の方法で(但し、該抽出物の穴中の終濃度は0.5〜2mg/mlとした)、マツヨイグサ属植物抽出物のGTaseに対する阻害作用を評価した。なお、ここでは、比較として、緑茶抽出物(商品名「緑茶乾燥エキス」、アスク薬品(株))を使用して、同様に試験を行った。また、参考として、ブドウ属植物抽出物についても、同様に試験を行った。
Test Example 2 Streptococcus sobrinus further assessment of inhibitory effect against GTase produced, for Streptococcus sobrinus 6715 strain (dispensing from Osaka Dental) to evaluate the inhibitory effect of evening primrose genus plant extract on GTase produced, in Test Example In the same manner as in Example 1 (however, the final concentration in the well of the extract was 0.5 to 2 mg / ml), the inhibitory effect of the evening primrose plant extract on GTase was evaluated. Here, for comparison, a green tea extract (trade name “Green Tea Dried Extract”, Ask Chemical Co., Ltd.) was used for the same test. For reference, a grape plant extract was similarly tested.
得られた結果を図2に示す。この結果から、GTase阻害活性が公知である緑茶抽出物に比して、マツヨイグサ属植物抽出物は、顕著に優れたGTase阻害作用があることが明らかとなり、口腔内で、歯垢形成抑制作用や抗う蝕作用を有効に発揮し得ることが確認された。 The obtained results are shown in FIG. From this result, it is clear that the Oenothera plant extract has a significantly superior GTase inhibitory action compared to the green tea extract with known GTase inhibitory activity, It was confirmed that the caries action can be effectively exhibited.
試験例3 Streptococcus mutansが産生するGTaseに対する阻害作用の評価
Streptococcus mutans MT8148株(大阪大学歯学部より分与)が産生するGTaseに対するマツヨイグサ属植物抽出物の阻害作用を評価した。具体的には、以下に記載の方法で、Streptococcusmutans MT8148株産生GTaseの調製を行い、前記試験例1と同様の方法で、該GTaseに対するマツヨイグサ属植物抽出物の阻害作用の評価試験を行った。
<Streptococcus mutans MT8148株産生GTaseの調製>
(1)培地の調製
Trypticase 15g、Tryptose 4g、yeast extract 4g、K2HPO42g、KH2PO4 5g、Na2CO32g、及びNaCl 2gに水を添加して合計900mlにメスアップした。また、別途、glucose 10gに水を添加して合計100mlにメスアップした。これらを別々の加熱滅菌した後、培養前に、これらを混合することによって、培地を調製した。
(2)Streptococcus mutansMT8148株の培養
前培養しておいたStreptococcusmutans MT8148株を上記培地1000mlに植菌し、37℃で18時間、静置培養を行った。
(3)GTaseの精製
上記(2)で得られた培養液を遠心分離し、沈殿を回収した。得られた沈殿をリン酸緩衝液(pH6.5)で洗浄した後、再度遠心分離を行い、沈殿を回収した。次いで、回収した沈殿に、8M尿素を加え抽出した。得られた抽出上清を、リン酸緩衝液(pH6.5)で透析後、限外濾過を行い得られた溶液をGTase液とした。得られたGTase液は、−80℃で保存した。
Test Example 3 Evaluation of inhibitory action on GTase produced by Streptococcus mutans
The inhibitory action of evening primrose extract on GTase produced by Streptococcus mutans MT8148 strain (distributed from Osaka University Dental School) was evaluated. Specifically, Streptococcusmutans MT8148 strain-produced GTase was prepared by the method described below, and an evaluation test of the inhibitory effect of evening primrose plant extract on the GTase was performed by the same method as in Test Example 1.
<Preparation of Streptococcus mutans MT8148 strain production GTase>
(1) Preparation of medium
Water was added to 15 g of Trypticase, 4 g of Tryptose, 4 g of yeast extract, 2 g of K 2 HPO 4 , 5 g of KH 2 PO 4 , 2 g of Na 2 CO 3 , and NaCl 2 g to make a total of 900 ml. Separately, water was added to 10 g of glucose to make a total of 100 ml. After these were heat sterilized separately and before culturing, the medium was prepared by mixing them.
(2) the Streptococcus mutans MT8148 strain Streptococcusmutans MT8148 strain which had been precultured culture was inoculated into the above medium 1000 ml, 18 hours at 37 ° C., was stationary culture.
(3) Purification of GTase The culture solution obtained in (2) above was centrifuged, and the precipitate was collected. The obtained precipitate was washed with a phosphate buffer (pH 6.5) and then centrifuged again to collect the precipitate. Next, 8M urea was added to the collected precipitate for extraction. The obtained supernatant was dialyzed with a phosphate buffer (pH 6.5) and subjected to ultrafiltration to obtain a GTase solution. The obtained GTase solution was stored at −80 ° C.
得られた結果を図3に示す。この結果から、試験例1の場合と同様に、マツヨイグサ属植物抽出物には優れたGTase阻害作用があることが確認された。また、参考のため評価したブドウ属植物抽出物についても、同様に、優れたGTase阻害作用があることが確認された。 The obtained results are shown in FIG. From this result, as in Test Example 1, it was confirmed that the evening primrose plant extract has an excellent GTase inhibitory action. In addition, it was confirmed that the grape plant extract evaluated for reference also has an excellent GTase inhibitory action.
試験例4 歯垢形成阻害作用の評価
マツヨイグサ属植物抽出物の歯垢形成阻害作用を評価するために、12名の被験者(歯周病疾患がない25〜30歳の男性)により、表1に示す洗口剤(実施例1及び比較例1)を用いて、以下の試験を行った。
Test Example 4 Evaluation of Plaque Formation Inhibitory Action In order to evaluate the plaque formation inhibitory action of an extract of the genus Oenothera plant, 12 subjects (25-30 year old men without periodontal disease) The following tests were conducted using the mouthwashes shown (Example 1 and Comparative Example 1).
まず、電動歯ブラシやデンタルフロスを用いて、口腔内の歯垢を完全に除去した。口腔内の歯垢が完全に除去されていることについては、歯垢染色液(商品名「DENT リキッドプラークテスター」;ライオン株式会社製)を用いて確認した。その後の2日間、実施例1の洗口剤を用いて洗口させた。なお、洗口は、食前、食後、就寝前、間食前、間食後に、実施例1の洗口剤10mlで20秒間実施した。当該期間中は、被験者には、実施例1の洗口剤以外での物理的又は化学的口腔清掃を禁止させた。また、日本茶、紅茶、コーヒー及びワインの摂取も禁止したが、他の食品、甘味料、喫煙については制限しなかった。実施例1の洗口剤の使用開始から2日後に、歯垢の付着状況を確認した。実施例1の洗口剤を用いた試験期間が終了した後、5日間の間隔を空けて、比較例1の洗口剤を用いて同様の条件で洗口を行い、歯垢の付着状況を確認した。 First, dental plaque in the oral cavity was completely removed using an electric toothbrush or dental floss. It was confirmed that plaque in the oral cavity was completely removed using a plaque staining solution (trade name “DENT Liquid Plaque Tester”; manufactured by Lion Corporation). The mouthwash was carried out for 2 days using the mouthwash of Example 1. The mouthwash was performed with 10 ml of the mouthwash of Example 1 for 20 seconds before eating, after eating, before going to bed, before snacking, and after snacking. During the period, the subject was prohibited from physical or chemical oral cleaning except for the mouthwash of Example 1. Japanese tea, tea, coffee and wine were also prohibited, but other foods, sweeteners and smoking were not restricted. Two days after the start of use of the mouthwash of Example 1, the state of adhesion of plaque was confirmed. After the test period using the mouthwash of Example 1 was completed, the mouthwash was performed under the same conditions using the mouthwash of Comparative Example 1 with an interval of 5 days, and the adhesion status of plaque was determined. confirmed.
歯垢の付着状況の評価は、上顎右側第一大臼歯、上顎左側中切歯、上顎左側第一小臼歯、下顎左側第一大臼歯、下顎右側中切歯及び下顎右側第一小臼歯の各歯について、歯垢染色液(商品名「DENT リキッドプラークテスター」;ライオン株式会社製)を用いて染色した後に、頬側及び口蓋側の両面をミラーホルダー等を用いて観察し、以下の判定基準に従ってスコア化することにより行った。
<歯垢の付着状況の判定基準>
プラークスコア
0 :染色された領域なし
1 :僅かに染色されている領域がある
2 :表面積の1/3以下の領域が染色されている
3 :表面積の1/3より大きく2/3以下の領域が染色されている
4 :表面積の2/3より大きい領域が染色されている
参考のために、図4に、各プラークスコアと歯垢の付着状況(染色領域)の関係についての代表例を示す。
Evaluation of plaque adhesion was performed on the maxillary right first molar, maxillary left central incisor, maxillary left first premolar, mandibular left first premolar, mandibular right central incisor, and mandibular right first premolar. After staining with dental plaque staining solution (trade name “DENT Liquid Plaque Tester”; manufactured by Lion Corporation), both cheek and palate sides are observed using a mirror holder and the following criteria are used: Was scored according to
<Criteria for determining plaque adhesion>
Plaque score 0: No stained area 1: Slightly stained area 2: Area of 1/3 or less of the surface area is stained 3: Area greater than 1/3 of the surface area and 2/3 or less 4: Area larger than 2/3 of the surface area is stained For reference, Fig. 4 shows a representative example of the relationship between plaque score and plaque adhesion (stained area). .
また、上記試験終了後、被験者に、実施例1及び比較例1の洗口剤の使用感について、「歯垢形成阻害効果の実感」及び「呈味」を下記基準に従ってスコア化して評価した。
<洗口剤の使用感の判定基準>
・歯垢形成阻害効果の実感
5:実施例1の方が比較例1よりも歯垢形成阻害効果が優れていると感じる
4:実施例1の方が比較例1よりも歯垢形成阻害効果がやや優れていると感じる
3:実施例1と比較例1とでは、歯垢形成阻害効果は同等であると感じる
2:実施例1の方が比較例1よりも歯垢形成阻害効果がやや劣っていると感じる
1:実施例1の方が比較例1よりも歯垢形成阻害効果が劣っていると感じる
・呈味
In addition, after the above test was completed, the subjects were evaluated for the feeling of use of the mouth washes of Example 1 and Comparative Example 1 by scoring “actual feeling of plaque formation inhibiting effect” and “taste” according to the following criteria.
<Judgment criteria for feeling of mouthwash>
・ Real feeling of plaque formation inhibitory effect 5: Example 1 feels that plaque formation inhibitory effect is superior to Comparative Example 1. 4: Example 1 has better plaque formation inhibitory effect than Comparative Example 1. 3: I feel that the plaque formation inhibitory effect is the same between Example 1 and Comparative Example 2. 2: The plaque formation inhibitory effect of Example 1 is slightly higher than that of Comparative Example 1. I feel that it is inferior 1: I feel that Example 1 is inferior in plaque formation inhibition effect compared with Comparative Example 1
・ Taste
5:実施例1の方が比較例1よりも呈味が良好であると感じる
4:実施例1の方が比較例1よりも呈味がやや良好であると感じる
3:実施例1と比較例1とでは、呈味は同等であると感じる
2:実施例1の方が比較例1よりも呈味がやや劣っていると感じる
1:実施例1の方が比較例1よりも呈味が劣っていると感じる。
5: Example 1 feels better in taste than Comparative Example 1 4: Example 1 feels slightly better in taste than Comparative Example 3: Compared with Example 1 It feels that taste is the same as in Example 1: 2: Feels that Example 1 is slightly inferior in taste compared to Comparative Example 1: 1: Example 1 is more tasteful than Comparative Example 1 I feel inferior.
得られた結果を表2及び3に示す。この結果から、実施例1の洗口剤で洗口した場合には、比較例1の洗口剤の場合に比して明らかに歯垢の付着が低減されており、マツヨイグサ属植物抽出物には、歯垢の形成を阻害する作用があることが確認された。また、実施例1の洗口剤は、使用者にとって、歯垢形成阻害効果が実感でき、しかも呈味も良好であることが明らかとなり、使用感の点でも優れていることが分かった。 The obtained results are shown in Tables 2 and 3. From this result, when the mouthwash was washed with the mouthwash of Example 1, plaque adhesion was clearly reduced as compared with the mouthwash of Comparative Example 1, and it was found that Was confirmed to have an effect of inhibiting the formation of plaque. In addition, it was found that the mouthwash of Example 1 was able to realize a plaque formation inhibitory effect for the user, and also had good taste, and was also excellent in terms of usability.
実施例3 タブレット
(重量%)
製造例1で得られたマツヨイグサ属植物抽出物 1
ポリデキストロース 7
シュガーエステル 2
香料 1
キシリトール 15
パラチノース 残部
合計 100
Example 3 Tablet
(weight%)
Oenothera plant extract obtained in Production Example 1 1
Polydextrose 7
Sugar ester 2
Fragrance 1
Xylitol 15
Palatinose remaining
Total 100
実施例4 糖衣タブレット
下記組成の錠剤と糖衣を用いて、糖衣タブレットを調製した。
錠剤 (重量%)
製造例1で得られたマツヨイグサ属植物抽出物 1.5
シュガーエステル 1
グアガム 0.2
アスパルテーム 0.01
パラチノース 残部
香料 適量
合計 100
糖衣 (重量%)
リン酸カルシウム 1
アスパルテーム 0.01
アラビアガム 0.5
カルバナワックス 0.1
シェラック 0.2
マルチトース 残量
香料 0.4
合計 100
Example 4 Sugar-coated tablets Sugar-coated tablets were prepared using tablets and sugar-coated tablets having the following composition.
Tablet (% by weight)
Oenothera plant extract obtained in Production Example 1.5
Sugar ester 1
Guam gum 0.2
Aspartame 0.01
Palatinose remaining
Perfume
Total 100
Sugar coating (wt%)
Calcium phosphate 1
Aspartame 0.01
Gum arabic 0.5
Carbana wax 0.1
Shellac 0.2
Multi-tose remaining
Fragrance 0.4
Total 100
実施例6 練歯磨き
(重量%)
製造例1で得られたマツヨイグサ属植物抽出物 1
リン酸カルシウム 30
グリセリン 10
ソルビトール 20
カルボキシメチルセルロースナトリウム 1
ラウリル酸ナトリウム 1.5
カラギーナン 0.5
サッカリンナトリウム 0.1
安息香酸ナトリウム 0.3
香料 1
水 残部
合計 100
Example 6 Toothpaste
(weight%)
Oenothera plant extract obtained in Production Example 1 1
Calcium phosphate 30
Glycerin 10
Sorbitol 20
Sodium carboxymethylcellulose 1
Sodium laurate 1.5
Carrageenan 0.5
Saccharin sodium 0.1
Sodium benzoate 0.3
Fragrance 1
Water balance
Total 100
実施例7 練歯磨き
(重量%)
製造例1で得られたマツヨイグサ属植物抽出物 1
ラウリル酸ナトリウム 0.8
ラウリル酸ジエタノールアミド 1
プロピレングリコール 3
60重量%ソルビット液 35
メチルパラベン 0.2
ブチルパラベン 0.01
サッカリンナトリウム 0.15
ゼラチン 0.3
アルギン酸ナトリウム 0.9
水酸化アルミニウム 45
モノフルオリン酸ナトリウム 0.76
香料 残部
合計 100
Example 7 Toothpaste
(weight%)
Oenothera plant extract obtained in Production Example 1 1
Sodium laurate 0.8
Lauric acid diethanolamide 1
Propylene glycol 3
60% by weight sorbit solution 35
Methylparaben 0.2
Butylparaben 0.01
Saccharin sodium 0.15
Gelatin 0.3
Sodium alginate 0.9
Aluminum hydroxide 45
Sodium monofluorate 0.76
Fragrance remainder
Total 100
実施例8 洗口剤
(重量%)
製造例1で得られたマツヨイグサ属植物抽出物 1
エタノール 10
グリセリン 5
クエン酸 0.01
クエン酸ナトリウム 0.1
ポリオキシエチレン硬化ひまし油 0.5
パラオキシ安息香酸メチル 0.1
香料 0.2
水 残部
合計 100
Example 8 mouthwash
(weight%)
Oenothera plant extract obtained in Production Example 1 1
Ethanol 10
Glycerin 5
Citric acid 0.01
Sodium citrate 0.1
Polyoxyethylene hydrogenated castor oil 0.5
Methyl paraoxybenzoate 0.1
Fragrance 0.2
Water balance
Total 100
実施例9 洗口剤
(重量%)
製造例1で得られたマツヨイグサ属植物抽出物 1
ラウリル酸ナトリウム 0.8
ラウリル酸ジエタノールアミド 0.8
グリセリン 12
サッカリンナトリウム 0.2
ハッカ油 0.8
アルギニン 0.1
リン酸水素二ナトリウム 0.5
リン酸水素二カリウム 0.08
水 残部
合計 100
Example 9 mouthwash
(weight%)
Oenothera plant extract obtained in Production Example 1 1
Sodium laurate 0.8
Lauric acid diethanolamide 0.8
Glycerin 12
Saccharin sodium 0.2
Peppermint oil 0.8
Arginine 0.1
Disodium hydrogen phosphate 0.5
Dipotassium hydrogen phosphate 0.08
Water balance
Total 100
実施例10 トローチ
(重量%)
製造例1で得られたマツヨイグサ属植物抽出物 1
マルチトール 21
アラビアガム 1.5
ショ糖脂肪酸エステル 2.5
クエン酸 4
粉末香料 1
キシリトール 残部
合計 100
Example 10 Lozenges
(weight%)
Oenothera plant extract obtained in Production Example 1 1
Maltitol 21
Gum arabic 1.5
Sucrose fatty acid ester 2.5
Citric acid 4
Powder flavor 1
Xylitol balance
Total 100
実施例11 口腔用パスタ
(重量%)
製造例1で得られたマツヨイグサ属植物抽出物 1
流動パラフィン 13
セタノール 10
グリセリン 25
ソルビタンモノパルミテート 0.6
ポリオキシエチレンソルビタンモノステアレート 5
ラウリル硫酸ナトリウム 0.1
塩化ベンゾトニウム 0.1
サリチル酸メチル 0.1
サッカリン 0.2
香料 0.25
水 残部
合計 100
Example 11 Oral Pasta
(weight%)
Oenothera plant extract obtained in Production Example 1 1
Liquid paraffin 13
Cetanol 10
Glycerin 25
Sorbitan monopalmitate 0.6
Polyoxyethylene sorbitan monostearate 5
Sodium lauryl sulfate 0.1
Benzotonium chloride 0.1
Methyl salicylate 0.1
Saccharin 0.2
Fragrance 0.25
Water balance
Total 100
実施例12 洗口剤
(重量%)
製造例1で得られたマツヨイグサ属植物抽出物 1
参考製造例1で得られたブドウ属植物抽出物 1
エタノール 10
グリセリン 5
クエン酸 0.01
クエン酸ナトリウム 0.1
ポリオキシエチレン硬化ひまし油 0.5
パラオキシ安息香酸メチル 0.1
香料 0.2
水 残部
合計 100
Example 12 mouthwash
(weight%)
Oenothera plant extract obtained in Production Example 1 1
Grape genus plant extract obtained in Reference Production Example 1 1
Ethanol 10
Glycerin 5
Citric acid 0.01
Sodium citrate 0.1
Polyoxyethylene hydrogenated castor oil 0.5
Methyl paraoxybenzoate 0.1
Fragrance 0.2
Water balance
Total 100
実施例13 洗口剤
(重量%)
製造例1で得られたマツヨイグサ属植物抽出物 0.5
濃グリセリン 5
パラオキシ安息香酸プロピル 0.02
ポリオキシエチレン硬化ひまし油 2
香料 0.1
エタノール 5
精製水 残部
合計 100
Example 13 mouthwash
(weight%)
Oenothera plant extract obtained in Production Example 1 0.5
Concentrated glycerin 5
Propyl paraoxybenzoate 0.02
Polyoxyethylene hydrogenated castor oil 2
Fragrance 0.1
Ethanol 5
Purified water balance
Total 100
Claims (6)
Priority Applications (2)
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JP2006084849A JP5892716B2 (en) | 2005-03-31 | 2006-03-27 | Oral composition |
PCT/JP2006/306973 WO2006106990A1 (en) | 2005-03-31 | 2006-03-31 | Composition for oral use |
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JP2005100919 | 2005-03-31 | ||
JP2005100919 | 2005-03-31 | ||
JP2006084849A JP5892716B2 (en) | 2005-03-31 | 2006-03-27 | Oral composition |
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JP5892716B2 true JP5892716B2 (en) | 2016-03-23 |
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Country Status (2)
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WO (1) | WO2006106990A1 (en) |
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JP5665280B2 (en) * | 2009-03-31 | 2015-02-04 | 小林製薬株式会社 | Oral composition |
JP2020002042A (en) * | 2018-06-27 | 2020-01-09 | 小林製薬株式会社 | Oral composition |
Family Cites Families (9)
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JPS61268613A (en) * | 1985-05-22 | 1986-11-28 | Rooto Seiyaku Kk | Composition for oral cavity containing evening primrose seed oil |
DE3712803C2 (en) * | 1987-04-15 | 1996-06-13 | Elba Buerosysteme Erich Kraut | Device for storing data disks in registry media |
DE69838405T2 (en) * | 1997-05-02 | 2008-06-12 | Ciba Specialty Chemicals Holding Inc. | Microstructured, cosmetically acceptable compositions |
ES2134743B1 (en) * | 1998-02-06 | 2000-05-01 | Biocosmetics Sl | COMPOSITION FOR THE TREATMENT OF HALITOSIS. |
JP4109818B2 (en) * | 2000-06-08 | 2008-07-02 | 小川香料株式会社 | Flavor degradation inhibitor |
JP2003261435A (en) * | 2002-03-11 | 2003-09-16 | Ichimaru Pharcos Co Ltd | Energy modifying agent |
JP2003286182A (en) * | 2002-03-29 | 2003-10-07 | Kobayashi Pharmaceut Co Ltd | IgE PRODUCTION INHIBITOR |
JP2005171116A (en) * | 2003-12-12 | 2005-06-30 | Ogawa & Co Ltd | Deterioration inhibitor for flavor or fragrance |
JP2006199661A (en) * | 2005-01-24 | 2006-08-03 | Sunstar Inc | Coaggregation inhibitor |
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