JPS63198616A - Anticariogenic substance - Google Patents

Anticariogenic substance

Info

Publication number
JPS63198616A
JPS63198616A JP3120687A JP3120687A JPS63198616A JP S63198616 A JPS63198616 A JP S63198616A JP 3120687 A JP3120687 A JP 3120687A JP 3120687 A JP3120687 A JP 3120687A JP S63198616 A JPS63198616 A JP S63198616A
Authority
JP
Japan
Prior art keywords
glycyrrhizin
anticariogenic
formation
gymnemic acid
substance
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.)
Granted
Application number
JP3120687A
Other languages
Japanese (ja)
Other versions
JPH0322847B2 (en
Inventor
Yasutake Hichi
日地 康武
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Priority to JP3120687A priority Critical patent/JPS63198616A/en
Publication of JPS63198616A publication Critical patent/JPS63198616A/en
Publication of JPH0322847B2 publication Critical patent/JPH0322847B2/ja
Granted legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63Steroids; Derivatives thereof

Abstract

PURPOSE:To provide an anticariogenic substance composed of glycyrrhizin extracted from KANZO (root of Glycyrrhiza glabra), suppressing the formation of glucan by cariogenic bacteria, surely inhibiting the formation of bacterial plaque and having excellent effect to prevent dental caries. CONSTITUTION:An anticariogenic substance having excellent effect to inhibit the formation of bacterial plaque can be produced by compounding preferably >=1mM of glycyrrhizin which is a kind of glucoside extracted from the root of KANZO as an essential component and preferably further compounding gymnemic acid. The anticariogenic substance surely prevents the formation of dental caries by the anticariogenic effect of glycyrrhizin even by taking conventional foods and drinks containing sucrose and starch. Gymnemic acid suppresses with sweet taste of glycyrrhizin and refreshes the oral cavity. Glycyrrhizin is a known agent having steroidal action, anti-inflammatory action, antiarteriosclerotic action, etc., and gymnemic acid is a known agent for suppressing sweet taste. Both are harmless to human body.

Description

【発明の詳細な説明】 A0発明の目的 (1)産業上の利用分野 本発明は、虫歯の予防に用いられる抗齲蝕性物質に関す
る。
DETAILED DESCRIPTION OF THE INVENTION A0 Object of the Invention (1) Field of Industrial Application The present invention relates to an anti-caries substance used for preventing dental caries.

(2)従来の技術 虫歯(6M歯)は古くから人類を悩ませ、特に、「砂糖
の消費は文明のバロメータ」と称される頃から砂糖と關
蝕との関係は注目され、その予防法については多くの研
究実績が積み重ねられている。
(2) Conventional technology Tooth decay (6M teeth) has plagued humanity since ancient times, and in particular, the relationship between sugar and tooth decay has been attracting attention since the time when sugar consumption was called the barometer of civilization, and ways to prevent it. Many research results have been accumulated regarding this.

従来、鶴蝕予防法の基本的な考え方は、殺菌剤や抗生物
質の投与により連鎖球菌の一種である鯖蝕原生細菌(ス
トレプトコッカス ムタンス、5treptococc
us mutans)を口腔内から排除する翫抗麟蝕性
人工甘味物質を用いるようにして砂糖を摂取しない、歯
質を強化して鵬蝕原生細菌の侵襲に抗する等である。
Traditionally, the basic idea of crane erosion prevention methods has been to eliminate Streptococcus mutans, a type of streptococcus, by administering bactericides and antibiotics.
For example, the use of artificial sweeteners with anti-erosive properties that eliminate S. mutans) from the oral cavity prevents the ingestion of sugar, and strengthens the tooth structure to resist invasion by proto-erosive bacteria.

ところが近年になって、麟蝕は口腔内の献蝕原生細菌が
砂糖を分解して粘り気の強いグルカン(多糖体)を生成
し、それが歯のエナメル質表面に粘着して歯垢(プラー
ク)を形成することから始まると提唱され、この歯垢形
成が鵬蝕の根源であることは、今や学界の定説とされて
いる。
However, in recent years, dental caries is caused by progenitor bacteria in the oral cavity decomposing sugar and producing sticky glucan (polysaccharide), which adheres to the tooth enamel surface and forms dental plaque. It has been proposed that plaque formation begins with the formation of dental plaque, and it is now an established theory in academic circles that this plaque formation is the root cause of dental caries.

このような観点より、前記話蝕予防法に加え、グルカン
の生成を抑制して歯のエナメル質表面における歯垢の形
成を阻止するようにすれば、虫歯を確実に予防すること
ができることになる。
From this perspective, in addition to the above-mentioned dental caries prevention method, it is possible to reliably prevent tooth decay by suppressing glucan production and preventing plaque formation on the tooth enamel surface. .

(3)発明が解決しようとする問題点 そこで、抗門蝕性物質を求めて多くの研究者が鋭意硬鋼
に励んでいるが、現在のところ効果的な抗鶴蝕性物質は
得られていない。
(3) Problems to be solved by the invention Therefore, many researchers are working diligently on hard steel in search of anti-corrosion substances, but so far no effective anti-corrosion substances have been obtained. do not have.

本発明は前記に鑑み、歯垢の形成阻止効果の高い前記抗
門蝕性物質を提供することを目的とする。
In view of the above, an object of the present invention is to provide the above-mentioned anti-portal caries substance which is highly effective in inhibiting the formation of dental plaque.

B0発明の構成 (1)問題点を解決するための手段 本発明に係る抗齲蝕性物質は、甘草から得られるグリチ
ルリチンよりなることを特徴とする。
B0 Structure of the Invention (1) Means for Solving Problems The anti-caries substance according to the present invention is characterized by comprising glycyrrhizin obtained from licorice.

また本発明に係る抗鯖蝕性物質は、甘草から得られるグ
リチルリチンにギムネマ酸を配合したことを特徴とする
Furthermore, the anti-cariogenic substance according to the present invention is characterized in that gymnemic acid is blended with glycyrrhizin obtained from licorice.

(2)作 用 前記グリチルリチンは甘草の根から抽出される配糖体の
一種であり、前記話蝕原生細菌によるグルカンの生成を
抑制し、歯垢形成を確実に阻止する作用を有する。
(2) Effect Glycyrrhizin is a type of glycoside extracted from licorice root, and has the effect of suppressing the production of glucan by the cariogenic bacteria and reliably inhibiting the formation of dental plaque.

グリチルリチンの薬剤としての歴史は古く、それは紀元
前から用いられており、現在知られているグリチルリチ
ンの薬理作用はステロイド様作用、抗炎症作用、抗動脈
硬化作用等であり、したがってグリチルリチンは人体に
対して無害である。
Glycyrrhizin has a long history as a drug, having been used since B.C. The currently known pharmacological effects of glycyrrhizin include steroid-like effects, anti-inflammatory effects, and anti-arteriosclerotic effects. It is harmless.

グリチルリチンは、砂糖(サッカロース)の100倍の
甘味を有し、また砂糖とは異なった後味を呈するが、こ
のグリチルリチンにギムネマ酸を配合すると、そのギム
ネマ酸の甘味抑制作用によってグリチルリチンの甘味を
和らげることができる。
Glycyrrhizin is 100 times sweeter than sugar (sucrose) and has a different aftertaste from sugar; however, when gymnemic acid is added to glycyrrhizin, the sweetness of glycyrrhizin is softened by the sweetness suppressing action of the gymnemic acid. Can be done.

前記ギムネマ酸は、インド、アフリカおよび中国に自生
する植物である匙關藤(シコウトウ、Gymnema 
5ylvestre )の葉または茎から抽出されるも
ので、経口投与後1〜2時間はグリチルリチンの甘味を
抑制する等飲食物の味を変える作用を有する。
The gymnemic acid is derived from Gymnema, a plant native to India, Africa, and China.
It is extracted from the leaves or stems of Glycyrrhizin and has the effect of changing the taste of foods and drinks, such as suppressing the sweetness of glycyrrhizin, for 1 to 2 hours after oral administration.

なお、ギムネマ酸は、低カロリー飲食物に用いられて砂
糖等の腸管からの吸収を抑制する作用を有するもので、
この点については本出願人が既に提案しており(特開昭
61−5023号公報参照)、シたがってギムネマ酸は
人体に対して無害である。
Gymnemic acid is used in low-calorie foods and drinks and has the effect of suppressing the absorption of sugar and other substances from the intestinal tract.
The present applicant has already proposed this point (see Japanese Patent Laid-Open No. 61-5023), and therefore gymnemic acid is harmless to the human body.

(3)実施例 〔検定例■〕 被検試料として、甘草の根から得られた市販のグリチル
リチンを用い、その濃度が0.1.1.10mMの溶液
を調製する。
(3) Example [Test Example ■] Using commercially available glycyrrhizin obtained from licorice root as a test sample, a solution having a concentration of 0.1.1.10 mM is prepared.

液体培地(TTY基礎培地)として、砂糖(サッカロー
ス)を含有してない培地、30mMの砂糖を含有する培
地、および30mMの砂糖に前記各溶液を個別に含有さ
せた培地を調製し、各液体培地に醋蝕原生細菌(Str
eptococcus mutans、 IID 97
3株)を100.cuff/4m/植菌し、37℃にて
48時間の試験管培養を行う。
As a liquid medium (TTY basal medium), a medium containing no sugar (sucrose), a medium containing 30mM sugar, and a medium containing each of the above solutions individually in 30mM sugar were prepared, and each liquid medium was Streptococcus protobacteria (Str
Eptococcus mutans, IID 97
3 stocks) to 100. Cuff/4m/inoculated and cultured in a test tube at 37°C for 48 hours.

前記各液体培地において、生成されたグルカンに伴う歯
垢形成の程度は、その歯垢を粉砕した後、波長660n
mの濁度計を用いてクレット単位(Klett uni
t)を測定することにより行われる。
In each of the above-mentioned liquid media, the degree of plaque formation accompanying the generated glucans was determined by the wavelength of 660 nm after the plaque was pulverized.
Klett unit (Klett uni
t).

図面は前記測定結果を示す。砂糖を含有していない液体
培地(No Sue )ではグルカンの生成、したがっ
て歯垢の形成はなく、測定値は2クレット単位以下であ
るが、30mMの砂糖を含有する液体培地(30mM 
 5uc)では約100クレツト単位となる。
The drawings show the measurement results. In the liquid medium containing no sugar (No Sue), there is no glucan production and therefore no plaque formation, and the measured value is less than 2 Cret units, whereas in the liquid medium containing 30mM sugar (30mM
5uc), it becomes about 100 cret units.

30mMの砂糖およびグリチルリチンを含有する液体培
地(Glyr)において、グリチルリチンを1mM以上
含有すると、測定値は前記No  Sueの場合と同じ
2クレット単位であり、歯垢の形成が阻止されている。
In a liquid medium (Glyr) containing 30mM sugar and glycyrrhizin, when glycyrrhizin is contained at 1mM or more, the measured value is 2 Cret units, which is the same as in the case of No Sue, and plaque formation is inhibited.

ただし、グリチルリチンの含有量が0.1mM以下では
、前記歯垢形成阻止効果は得られない。
However, if the content of glycyrrhizin is 0.1 mM or less, the above-mentioned plaque formation inhibiting effect cannot be obtained.

以上の結果より、歯垢形成阻止のためにはグリチルリチ
ンを1mM以上含有するのが望ましい。
From the above results, it is desirable to contain glycyrrhizin at 1 mM or more in order to inhibit plaque formation.

〔検定例■〕[Examination example■]

先ず、ギムネマ酸の抽出および精製について説明する。 First, extraction and purification of gymnemic acid will be explained.

匙菱藤の乾燥葉200gを60℃の温水中に約5時間浸
し、これを4〜5回繰返して粗製ギムネマ酸を含む温水
抽出液を得る。この温水抽出操作は、最初からアルコー
ルを用いて抽出すると、葉緑素、脂質類が溶出されてく
るので、これを避けるために行われる。
200 g of dried leaves of Sobishi Wisteria are immersed in warm water at 60° C. for about 5 hours, and this is repeated 4 to 5 times to obtain a hot water extract containing crude gymnemic acid. This hot water extraction operation is performed to avoid chlorophyll and lipids from being eluted if alcohol is used for extraction from the beginning.

温水抽出液を2N硫酸でpH3に調整して、粗製ギムネ
マ酸を含む沈澱物を得る。
The warm water extract is adjusted to pH 3 with 2N sulfuric acid to obtain a precipitate containing crude gymnemic acid.

沈澱物を、15000rpm、15分間の条件の下で遠
心沈降を行うことにより集め、その集合物を水で洗浄後
、エタノールにより4〜5回抽出してエタノール抽出液
を得る。このエタノール抽出操作は、沈澱物からタンパ
ク質、多糖類等を除くために行われる。
The precipitate is collected by performing centrifugal sedimentation at 15,000 rpm for 15 minutes, and the aggregate is washed with water and then extracted with ethanol 4 to 5 times to obtain an ethanol extract. This ethanol extraction operation is performed to remove proteins, polysaccharides, etc. from the precipitate.

エタノール抽出液を減圧下で濃縮し、その濃縮物に、容
量でそれの2倍量のアセトンを加えた後、遠心沈降を行
う。
The ethanol extract is concentrated under reduced pressure, and twice its volume of acetone is added to the concentrate, followed by centrifugation.

粗製ギムネマ酸を含む、遠心沈降後の上澄液を減圧下で
濃縮乾固し、これに溶媒として炭酸ジエチルを加えて沸
点下で数回抽出を繰返す。
The supernatant containing crude gymnemic acid after centrifugal sedimentation is concentrated to dryness under reduced pressure, diethyl carbonate is added as a solvent, and extraction is repeated several times at boiling point.

前記溶媒から析出したものを集め、これを蒸発乾固して
高速液体クロマトグラフィに通す。大型カラムに逆相系
担体(Cue)を充填し、移動相が水:メタノール=1
:1の割合からメタノール100%となるように緩徐に
溶出すると、メタノール濃度70〜80%の部分に、精
製されたギムネマ酸が溶出する。これを蒸発乾固してp
H7に調整すると、ギムネマ酸はNa塩、K塩またはN
H4塩として得られる。この精製ギムネマ酸は一種のサ
ポニン(配糖体)である。精製ギムネマ酸の収量は、前
記乾燥葉100g当り0.1〜0.5重量%である。
The precipitate from the solvent is collected, evaporated to dryness and passed through high performance liquid chromatography. A large column is packed with a reverse phase carrier (Cue), and the mobile phase is water:methanol = 1
When slowly eluting from a ratio of 1:1 to 100% methanol, purified gymnemic acid is eluted in a portion where the methanol concentration is 70 to 80%. Evaporate this to dryness and p
When adjusted to H7, gymnemic acid is converted into Na salt, K salt or N
Obtained as H4 salt. This purified gymnemic acid is a type of saponin (glycoside). The yield of purified gymnemic acid is 0.1 to 0.5% by weight per 100 g of the dried leaves.

次いで 被検試料として、前記市販グリチルリチンと前
記精製ギムネマ酸とを容量比で75対25.50対50
.25対75の割合に配合して合計1mM(両物質の分
子量は約1000として計算する)となるように調整し
たものを得る。
Next, as a test sample, the commercially available glycyrrhizin and the purified gymnemic acid were mixed in a volume ratio of 75:25.50:50.
.. A mixture prepared in a ratio of 25:75 to give a total of 1 mM (calculated assuming that the molecular weight of both substances is about 1000) is obtained.

前記三種の被検試料を用いて、前記検定例■と同様の方
法で試験管培養を行い、次いで測定を行ったところ何れ
の被検試料についても測定値は、前記No sucの場
合と同様に2クレット単位以下であり、歯垢の形成が阻
止されていることが確認されている。
Using the three types of test samples, test tube culture was carried out in the same manner as in the test example ① above, and then measurement was performed.The measured values for all test samples were the same as in the case of No suc. It has been confirmed that the amount is 2 Clets or less, and that plaque formation is inhibited.

グリチルリチンとギムネマ酸の配合割合は、抗門蝕性物
質の甘味を考慮した場合、50対50が適当である。そ
の理由は、例えばグリチルリチンおよびギムネマ酸の配
合量をそれぞれ0.5 m Mに設定すると、グリチル
リチンの0.5mMは砂糖の甘味度に換算すると、砂糖
の0.05Mに相当する淡い甘さであり、一方、ギムネ
マ酸0.5 m、 Mはグリチルリチンの甘味をさらに
和らげて口腔内を清凍にするからである。
The appropriate blending ratio of glycyrrhizin and gymnemic acid is 50:50, considering the sweet taste of the anti-portal caries substance. The reason is that, for example, if the blending amounts of glycyrrhizin and gymnemic acid are each set to 0.5 mM, 0.5mM of glycyrrhizin has a light sweetness equivalent to 0.05M of sugar when converted to the sweetness of sugar. On the other hand, 0.5 m, M of gymnemic acid further softens the sweetness of glycyrrhizin and makes the oral cavity refreshing.

前記グリチルリチン単独またはそれにギムネマ酸を配合
した抗鯖蝕性物賞の具体的使用例としては、その物質を
含有する歯磨、チューインガム、キャンディ、テーブル
シュガー、口腔内用スプレー等を挙げることができる。
Specific examples of the use of the anti-cariogenic substance containing glycyrrhizin alone or gymnemic acid include toothpaste, chewing gum, candy, table sugar, oral spray, etc. containing the substance.

C8発明の効果 本発明によれば、グリチルリチンの抗門蝕効果によって
砂糖、デンプン賞を含む通常の飲食物を摂取しても、虫
歯の発生を確実に回避することができる。
C8 Effects of the Invention According to the present invention, the occurrence of dental caries can be reliably avoided even if ordinary foods and drinks containing sugar and starch are ingested due to the anti-portal caries effect of glycyrrhizin.

またグリチルリチンにギムネマ酸を配合することによっ
て、グリチルリチンの甘味を抑制して口腔内を清涼にす
ることができる。
Further, by blending gymnemic acid with glycyrrhizin, the sweet taste of glycyrrhizin can be suppressed and the inside of the oral cavity can be refreshed.

【図面の簡単な説明】[Brief explanation of the drawing]

図面は各種液体培地の、波長660nmにおけるクレッ
ト単位を示すグラフである。
The figure is a graph showing Klett units at a wavelength of 660 nm for various liquid media.

Claims (2)

【特許請求の範囲】[Claims] (1)甘草から得られるグリチルリチンよりなることを
特徴とする抗齲蝕性物質。
(1) An anti-caries substance characterized by comprising glycyrrhizin obtained from licorice.
(2)甘草から得られるグリチルリチンにギムネマ酸を
配合したことを特徴とする抗齲蝕性物質。
(2) An anti-caries substance characterized by blending gymnemic acid with glycyrrhizin obtained from licorice.
JP3120687A 1987-02-13 1987-02-13 Anticariogenic substance Granted JPS63198616A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP3120687A JPS63198616A (en) 1987-02-13 1987-02-13 Anticariogenic substance

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP3120687A JPS63198616A (en) 1987-02-13 1987-02-13 Anticariogenic substance

Publications (2)

Publication Number Publication Date
JPS63198616A true JPS63198616A (en) 1988-08-17
JPH0322847B2 JPH0322847B2 (en) 1991-03-27

Family

ID=12324944

Family Applications (1)

Application Number Title Priority Date Filing Date
JP3120687A Granted JPS63198616A (en) 1987-02-13 1987-02-13 Anticariogenic substance

Country Status (1)

Country Link
JP (1) JPS63198616A (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998044901A1 (en) * 1997-04-04 1998-10-15 Optiva Corp. Antimicrobial agents for oral hygiene products
US6248309B1 (en) 1997-04-04 2001-06-19 Optiva Corporation Gums containing antimicrobial agents

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59134729A (en) * 1983-01-24 1984-08-02 Takasago Corp Inhibitor against growth of decay bacteria

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59134729A (en) * 1983-01-24 1984-08-02 Takasago Corp Inhibitor against growth of decay bacteria

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998044901A1 (en) * 1997-04-04 1998-10-15 Optiva Corp. Antimicrobial agents for oral hygiene products
US6248309B1 (en) 1997-04-04 2001-06-19 Optiva Corporation Gums containing antimicrobial agents

Also Published As

Publication number Publication date
JPH0322847B2 (en) 1991-03-27

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