JP2003119117A - Anticariogenic agent and composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a naturally based safe anticariogenic agent having high anticarious activity, and to provide a composition for oral cavity containing the anticariogenic agent. SOLUTION: This anticariogenic agent comprises as the active ingredient at least one kind of extract from plant(s) selected from those belonging to Euphorbiaceae, Fagaceae, Umbelliferae and Lythraceae families, or comprises as the active ingredient a glucosyltransferase inhibitory substance extracted from at least one kind of plant selected from the group consisting of Phyllanthus niruri var. amarus Leamdri, Quercus phillyraeoides A. Gray, Glehnia littoralis F. Schrmidt ex Miq., Peucedanum japonicum Thunb. and Lagerstroemia speciosal. The other objective composition for oral cavity contains the above anticariogenic agent.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a novel anticaries agent and an oral composition containing the anticaries agent. In addition,
In the present invention, the oral composition means a broad concept including food and drink, which is held in the oral cavity for a certain period of time.

[0002]

2. Description of the Related Art In the development of dental caries, microorganisms in the oral cavity, especially Streptococcus mutans (hereinafter referred to as "S. muta")
abbreviated as "ns") and Streptococcus sobrinus (hereinafter abbreviated as "S. sobrinus").

That is, a part of sucrose in food and drink left in the oral cavity is changed into glucan which is water-insoluble and has strong adhesiveness by the action of glucosyltransferase, which is attached to the tooth surface together with the oral microorganisms. Form plaque. Then, it is caries that microorganisms in the plaque metabolize sugars to make acid, and this acid decalcifies and erodes tooth enamel. In addition to dental caries, plaque may cause bad breath, and its progression may lead to periodontal disease, gingivitis, and even alveolar pyorrhea.

Therefore, in order to prevent dental caries, the plaque attached to the tooth surface is not only removed by brushing the teeth, but also S. mutans and S. sobrinus
It is most effective to prevent the formation of glucans by inhibiting the growth of Escherichia coli and the action of glucosyltransferase and thus prevent plaque formation.

From such a viewpoint, in recent years, an oral composition having a caries preventive action by containing a substance having a glucosyltransferase inhibitory action has been provided.

Examples of the glucosyl transferase inhibitor suitable for such use include, for example, turmeric, fennel, peony, gentian, senso, dragon gall, yellow ream, cembly (Japanese Patent Laid-Open No. 58-112218), ellagic acid and Genoshoko, eucalyptus (JP-A 64-10985), peony, Biwayo, Jouinchin, Chiyu (JP-A-4-95020), mutastine, herbal medicine tannins, ellagic acid, green tea polyphenols containing ellagic acid, Although oolong tea extract and the like have been proposed, it is desired to provide a further safe and inexpensive anti-caries agent having a high anti-cariogenic effect.

[0007]

SUMMARY OF THE INVENTION It is an object of the present invention to solve the various problems in the prior art and achieve the following objects. That is, an object of the present invention is to provide a natural anti-caries agent having a safe and excellent anti-cariogenic effect and an oral composition containing the anti-carious agent.

[0008]

Means for Solving the Problems As a result of intensive studies to achieve the above-mentioned object, the present inventor has found that at least one member selected from the group consisting of Pleurotus cornucopsis, Ubamegashi, Hamaboufu, Buttonbofu and Banaba The plant extract has a glucosyltransferase inhibitory effect, is effective as a safe natural anti-cathartic agent, and
The present invention has been completed based on the finding that it can be used for a wide range of oral compositions, since it has little adverse effect on flavor and feeling of use.

That is, the present invention provides the following anti-caries agent and oral composition in order to solve the above problems.

The invention of claim 1 is the extraction of at least one plant selected from the plants of the genus Firantus of the Euphorbiaceae, the Quercus genus of the family Beech, the plant of the family Hamabofufu of the family Seriaceae, the plant of the family Seriaceae Kawalaboufu, and the plant of the genus Sarsbergi of the family Liliaceae. It is an anticaries agent containing a substance as an active ingredient.

[0012] The invention of claim 2 comprises as an active ingredient a glucosyltransferase inhibitory substance extracted from at least one plant selected from the group consisting of Pleurotus cornucopiae, Pleurotus cornucopiae, Pleurotus cornucopiae, Pleurotus cornucopsis, and Banaba. It is a characteristic anti-caries agent.

[0012] The invention of claim 3 is the leaf part of at least one plant selected from the group consisting of Pleurotus cornucopiae, Pleurotus cornucopiae, Pleurotus cornucopiae, Pleurotus cornucopiae and Banaba,
The anticaries agent according to claim 2, which comprises, as an active ingredient, a glucosyltransferase-inhibiting substance obtained by extracting the stem portion, the root portion, or a mixed portion thereof with water, a hydrophilic solvent, or a mixed solvent thereof.

A fourth aspect of the present invention is an oral composition containing the anticaries agent according to any one of the first to third aspects.

[0014]

BEST MODE FOR CARRYING OUT THE INVENTION The present invention will be described in more detail below. The anti-caries agent of the present invention, as the first aspect, at least one species selected from the plant of the genus Phyllantus of the Euphorbiaceae, the plant of the genus Quercus genus, the plant of the family Seriaceae, the plant of the family Seriidae, the plant of the family Seriaceae, Kawalaboufu, and the plant of the genus Cercisaceae. The plant extract of the above is contained as an active ingredient.

The anti-caries agent of the present invention, in a second aspect, is citrus cypress, Ubamegashi, Hamaboufu,
It contains as an active ingredient a glucosyltransferase-inhibiting substance that is extracted from at least one plant selected from the group consisting of Botanbofu and Banaba.

[0016] The genus Phyllanthus (Eu)
Phorbiaceae) plants include Phylanthus niruri var.
amarus Leamdri), Yucan (Phyll)
anthus emblica) and the like, and of these, Pleurotus chinensis is preferable. Red citrus is a plant widely distributed in tropical to warm zones and is commonly found in cultivated areas and alleys, and its stems and leaves (whole grass) can be used.

The above-mentioned beech family Quercus genus (Fagaceae)
As a plant, Ubamegashi (Quercus phil)
lyraeoides A. Gray), Mizunara (Q
uercus mongolica var. gros
serratata (Bl.) Rehd. et Wil
s. ), White oak, oak, and the like, and of these, Ubamegashi is preferable. Ubamegashi is a tree that is often planted as a hedge or garden tree, with small, shiny, evergreen leaves densely attached. It is widely distributed in the west of Kanagawa prefecture in Honshu, Shikoku, Kyushu, Okinawa, and mainland China, and its leaves can be used.

Umbellif (Umbellif)
erae) plants include Glehni
a littoralis F. Schmidt ex
Miq. ) And the like. Hamabofu is a perennial plant that grows on the coast, and is widely distributed throughout Japan, Korea, mainland China, and the leaves or roots can be used.

Umbellii genus
ferae) plants include Peuce (Peuc)
edanum japonicum Thunb. ), Nodake, Inondo, Kawarabofu, and the like, and among these, Buttonbohuu is preferable. Button Bow Fuu is a perennial plant that grows on the coast and is distributed in the west of Kanto, Shikoku, Kyushu, Okinawa, Korea, Mainland China, the Philippines, etc.
The leaves or roots can be used.

Lythrac (Lythrac)
Eae plants include banaba (Lagerstroe)
mia speciosal. ), And clams, etc., and of these, banaba is preferable. Banaba, which is also referred to as Spodoptera litura, is native to Southeast Asia and its leaves can be used.

The above-mentioned plant as the extraction raw material may be used alone or in combination of two or more kinds. For example, it may be mixed with all of the citrus citrus fruit, Ubamegashi, Hamaboufu, Buttonbofu and Banaba, or the combination of Kidachikansu and Ubamegashi, the combination of Kidachikanso and Hamaboufu, the combination of Kidachikanso and Buttonbofuu. A combination, a combination of citrus cane and banaba, a combination of Hamabofu and Buttonbofu, and the like are preferable.

The plant used as a raw material for extracting the anticaries agent of the present invention has a large amount of each plant in nature and can be stably supplied, and has been used for food and medicinal purposes since ancient times. There is a high degree of safety. Incidentally, it has not been confirmed what compound in the extract has the glucosyltransferase inhibitory effect which is the active ingredient of the anti-catalyst of the present invention, but it is presumed that the effects of a plurality of compounds are combined. To be done.

Further, the anti-caries agent of the present invention is obtained by pulverizing the leaves, stems, roots or a mixed portion thereof of the plant which is the above-mentioned extraction raw material as it is or after pulverizing it as it is or by using a pulverizer. It can be obtained by subjecting to solvent extraction.
As the solvent used for the extraction, it is preferable to use water, a hydrophilic solvent or a mixed solvent thereof at a temperature from room temperature to the boiling point of the solvent.

The water that can be used as the extraction solvent includes pure water, tap water, well water, mineral water, mineral water, hot spring water, spring water, fresh water and the like, as well as those that have been subjected to various treatments. Examples of the treatment applied to water include purification, heating, sterilization, sterilization, filtration, ion exchange, adjustment of osmotic pressure, buffering, and the like. Therefore, the water that can be used as the extraction solvent in the present invention also includes purified water, hot water, ion-exchanged water, physiological saline, phosphate buffer, phosphate buffered saline and the like.

Examples of the hydrophilic organic solvent include lower alcohols having 1 to 5 carbon atoms such as methanol, ethanol, propylene alcohol and isopropyl alcohol;
Lower aliphatic ketones such as acetone and methyl ethyl ketone;
1,3-butylene glycol, propylene glycol,
Examples thereof include polyhydric alcohols having 2 to 5 carbon atoms such as glycerin, and mixed solvents of these hydrophilic organic solvents and water can be used. When a mixed solvent of water and a hydrophilic organic solvent is used, 1 to 990 parts by mass is used for 10 parts by mass of water in the case of lower alcohol, and 10 parts by mass of water is used in the case of lower aliphatic ketone. 1 to 990 parts by mass,
In the case of polyhydric alcohol, 1 to 99 per 10 parts by mass of water
It is preferable to add 0 part by mass.

In the present invention, it is not necessary to employ a special extraction method for extracting the active ingredient of the anticaries agent,
It can be extracted using any device at room temperature to under reflux heating. Specifically, the extraction raw material is put into a treatment tank filled with an extraction solvent, and occasionally stirred to elute the soluble component. Then, the extraction residue is removed by filtration, and the obtained extract is concentrated and dried to obtain an extract containing the active ingredient.

The extraction conditions are usually 40 to 90 ° C. and about 30 minutes to 2 hours when water is used as the extraction solvent.
When a mixed solvent of water and ethanol is used as the extraction solvent, it is usually at 40 to 80 ° C for about 30 minutes to 2 hours. The extract obtained by extraction with a solvent can be blended as it is and used as the anti-cariogenic agent of the present invention if the extraction solvent is highly safe.

Further, the obtained extract can be purified for the purpose of decolorizing, deodorizing, improving activity and the like. The purification means is not particularly limited, activated carbon treatment, resin adsorption treatment,
Examples of the method include ion exchange resin treatment and liquid-liquid countercurrent distribution. For example, a resin adsorption purification method in which a porous resin such as SepaBeads SP-207 and Diaion HP-20 (both manufactured by Mitsubishi Chemical Corporation) and a concentrated solution are brought into contact with each other can be employed. The active ingredient adsorbed on the resin is water,
It can be eluted with ethanol or the like.

The extract or extract of these plants obtained as described above can be used as it is as an anticaries agent, but if necessary, it may be used in combination with other active substances and molding aids. It can be an anti-caries agent in the dosage form.

The anticaries of the present invention can be added to various oral compositions to contribute to the prevention of glucan formation in the oral cavity. As the oral composition, various toothpaste, mouthwash, troche, oral pasta, gum massage cream, mouthwash, mouth freshener, confectionery, bread, candy, chewing gum, gummies, jellies, chocolates, tablets, pets Examples include food. In this case, the amount of the anti-fouling agent to be added to the oral composition varies depending on the strength of activity and the object to be added and cannot be unconditionally specified, but it is about 0.001 as an extract of the plant.
To 5.0% by mass, especially about 0.05 to 1.0% by mass
Is preferred.

In addition to the plant extract, other glucosyltransferase inhibitors and plaque formation inhibitors may be used in combination with the oral composition of the present invention. m
utans and S. An antibacterial agent effective against sobrinus may be added. Furthermore, by adding any anti-inflammatory agent, antibacterial agent, deodorant, etc., a more excellent oral preparation can be provided.

Examples of the above-mentioned anti-inflammatory agents include acacia, liquorice, oak sumac, ogon, kouki, psycho, hawthorn, schizophrenia, peony, sour apricot, kyounin, taiso, clove, tounin, nutmeg, button pie, mulberry leaf and the like. Extract; azulene, allantoin,
Ursolic acid, oleanolic acid, glycyrrhizic acid, glycyrrhetinic acid or derivatives thereof; tocopherol, tranexamic acid and the like can be mentioned.

Examples of the antibacterial agent include Gobayashi,
Saishin, salmon, ginger, dill, thyme,
Extracts such as rosemary and oil-soluble licorice extract; ascorbic acid, mutastine, humic acid, linoleic acid, linolenic acid and the like can be mentioned.

As the deodorant, for example, armature,
Extracts such as fennel, veiled roach, cinnamon, pepper, mace, sage, perilla, ginkgo, oyster leaf, green tea, oolong tea, capsicum, tamarind husk, rosin, oyster astringent, actizol, chlorophyllin derivative, ellagic acid, chlorhexidine, maillard reaction product And so on.

In addition to the above-mentioned components, the oral composition of the present invention contains abrasives, surfactants, adhesives, thickeners, sweeteners, preservatives, and fragrances which are commonly used in oral compositions. Various dyes and the like can be appropriately selected and blended according to the purpose. For example, polishing agents such as calcium hydrogen phosphate, calcium carbonate, insoluble sodium metaphosphate, aluminosilicate, silicic acid anhydride, and resin; long-chain sodium alkyl sulfate, sodium lauryl sulfoacetate, lauryl diethanolamide, sucrose fatty acid ester, etc. Active agent; CMC, hydroxyethyl cellulose, alginate, carrageenan, gum arabic, polyvinyl alcohol, etc. adhesive agent; polyethylene glycol, sorbitol, glycerin, propylene glycol, etc. viscous agent; saccharin, stevioside, glycyrrhizinic acid, thaumatin, aspartame, etc. Sweeteners for dehydroacetic acid; preservatives such as dehydroacetic acid and sodium dehydroacetate; menthol, carvone, eugenol, anethole, peppermint oil, spearmint oil, peppermint oil, youth May be incorporated with various dye; Li oil, ginger oil, perfume anise oil.

[0036]

EXAMPLES Hereinafter, the present invention will be specifically described by showing production examples and examples, but the present invention is not limited to the following examples.

[Manufacturing Example 1] Goldenrod extract The 50% ethanol (1000 mL) was added to the whole grass root (100 g), and a reflux condenser was used.
Extraction was performed at 80 ° C. for 2 hours and then filtered through filter paper to obtain an extract. The obtained extract was concentrated and dried under reduced pressure to give 26.0 g (powder) of Pleurotus cornucopia extract (yield 26.0%).

Production Example 2 Ubamegashi Extract Water (1000 mL) was added to Ubamegashi leaf parts (100 g), and the mixture was extracted with a reflux condenser at 80 ° C. for 2 hours and then filtered with filter paper. An extract was obtained. The resulting extract was concentrated and dried under reduced pressure to obtain Ubamegashi extract 29.
1 g (powder) was obtained (yield 29.1%).

[Production Example 3] Hamabofu leaf extract 50% by mass acetone (1000 mL) was added to Hamabofu leaf part (100 g), and the mixture was heated at 80 ° C. using a reflux condenser.
After being extracted for 2 hours with a filter paper, it was filtered with a filter paper to obtain an extract. The obtained extract was concentrated and dried under reduced pressure to obtain 23.4 g (powder) of Hamabofufu leaf extract (yield 2
3.4%).

[Production Example 4] Hamabofufu root extract Hamabofufu root (100 g) was treated with ethanol (1000 g).
mL) was added, and the mixture was extracted with a reflux condenser at 80 ° C. for 2 hours and then filtered with filter paper to obtain an extract. The obtained extract was concentrated and dried under reduced pressure to obtain 15.8 g (powder) of Hamabofufu root extract (yield 15.8).
%).

[Production Example 5] Botanus fusifolia leaf extract 70 mass% ethanol (1000 mL) was added to Botanus fusifolia leaf portion (100 g), and the mixture was heated to 80 by using a reflux condenser.
After performing extraction for 2 hours at ℃, it was filtered through a filter paper to obtain an extract. The obtained extract is concentrated under reduced pressure and dried,
22.3 g (powder) of the leaf extract of Botania graminata were obtained (yield 22.3%).

[Production Example 6] Botanus fusaria root extract Botanus fusaria roots (100 g) with water (1000 mL)
Was added, and the mixture was extracted with a reflux condenser at 80 ° C. for 2 hours, and then filtered with filter paper to obtain an extract. The obtained extract was concentrated and dried under reduced pressure to obtain 30.2 g (powder) of Boletus fusaria root extract (yield 30.2%).

[Production Example 7] Banaba extract 70% by mass of acetone (100 g) was added to banaba leaves (100 g).
(0 mL) was added, and the mixture was extracted with a reflux condenser at 80 ° C. for 2 hours and then filtered with filter paper to obtain an extract. The obtained extract was concentrated and dried under reduced pressure to obtain 23.5 g of banaba extract (powder) (yield 23.5%).

[Examples 1 to 7] Glucosyl transfer
Jerase Inhibition Test Ceratophyllum japonicum extract of Production Example 1 (Example 1), Ubamegashi extract of Production Example 2 (Example 2), Hamabofufu Leaf Extract of Production Example 3 (Example 3), Hamabofufu of Production Example 4 Root extract (Example 4), Botanus japonicus leaf extract of Production Example 5 (Example 5), Botanus botanus root extract of Example 6 (Example 6), Banaba extract of Production Example 7 (Example 7) )
Were dissolved and diluted with 50% by mass of ethanol to give sample concentrations of 3.125 μg / mL to 40 mg, respectively.
/ ML of sample solution was prepared.

50 μL of each obtained sample solution, 1000 μ of 2% sucrose aqueous solution containing 0.1% of sodium azide
L, crude glucosyltransferase solution (S. mut
(prepared from ans) 50 μL and distilled water 900 μ
L was added to the test tube and mixed. After reacting at 37 ° C. for 5 hours, the produced glucan was dispersed in water with a stirrer and the absorbance at 550 nm was measured as an index of turbidity.
Separately, as a control, the same operation was performed when the solvent of the sample solution was added instead of each sample solution.
Furthermore, in each case, the same operation and measurement were performed without adding the crude glucosyltransferase solution.

From the obtained measurement results, the inhibition rate of glucosyltransferase activity was calculated by the following formula. <Formula 1> Inhibition rate (%) = [1- (AB) / (CD)] × 100 where A: absorbance of sample solution after enzyme reaction B: absorbance of sample solution without addition of enzyme C: Absorbance after control enzyme reaction D: Absorbance without control enzyme addition

The sample concentration of each reaction solution was 0.078 to 10
The above-mentioned glucosyltransferase activity inhibition rate was measured by gradually changing it to 00 μg / mL.
The sample concentration (IC ₅₀ ) of each reaction solution which becomes 0% (μg /
mL) was calculated. The results are shown in Table 1. In addition, when IC ₅₀ is 1000 μg / mL or less, it can be judged that the glucosyltransferase inhibitory action is sufficient.

[0048]

[Table 1]

From the results shown in Table 1, sufficient glucosyltransferase was obtained for the extract of Phytolacca communis, the extract of Pleurotus cornucopiae, the extract of Hamabofufu leaf, the extract of Hamabofufu root, the extract of Botanbofu leaf, the extract of Botanbofu root and the extract of Banaba. It was confirmed to have an inhibitory effect.

Example 8 Toothpaste Toothpaste having a caries-preventing action was produced by mixing the following ingredients. Yellow citrus extract of Production Example 1 1 part by mass Dibasic calcium phosphate 45 parts by mass CMC / sodium salt 1 part by mass Glycerin 20 parts by mass Sodium lauryl sulfate 2 parts by mass 1-menthol 1 part by mass Water 30 parts by mass

Example 9 Toothpaste The following ingredients were mixed to prepare a toothpaste having a caries-preventing action. Hamaboufuu root extract of Production Example 4 3 parts by mass Dicalcium phosphate 45 parts by mass CMC / sodium salt 1 part by mass Glycerin 20 parts by mass Sodium lauryl sulfate 2 parts by mass 1-Menthol 1 part by mass Water 30 parts by mass

Example 10 Mouthwash A mouthwash having a caries-preventing action was produced by mixing the following ingredients. Ubamegashi extract of Production Example 1 1 part by mass Ethanol 20 parts by mass Glycerin 0.2 parts by mass Chlorhexidine 5 parts by mass 1-Carvone 0.005 parts by mass Water 74 parts by mass

Example 11 Mouthwash A mouthwash having a caries-preventing action was prepared by mixing the following ingredients. Buttonweed leaf extract of Production Example 5 3 parts by mass Ethanol 20 parts by mass Glycerin 0.2 parts by mass Chlorhexidine 5 parts by mass 1-Carvone 0.005 parts by mass Water 74 parts by mass

[Example 12] Chewing gum The following raw materials were processed by a conventional method for producing chewing gum to produce chewing gum having a caries preventive action. Hamaboufuu leaf extract of Production Example 3 5 parts by mass Chewing gum base 20 parts by mass Sucrose 50 parts by mass starch syrup 20 parts by mass Softener 4 parts by mass Fragrance 1 part by mass

[Example 13] Chewing gum The following raw materials were processed by a conventional method for producing chewing gum to produce chewing gum having a caries preventive action. Peony root extract of Production Example 5 5 parts by mass Chewing gum base 20 parts by mass Sucrose 50 parts by mass Syrup 20 parts by mass Softener 4 parts by mass Fragrance 1 part by mass

Example 14 Candy A candy having a caries-preventing action was produced by mixing, concentrating and molding the following raw materials by a conventional method for producing candy. Banaba extract of Production Example 7 3 parts by mass Sucrose 70 parts by mass Starch 30 parts by mass Citric acid 1 part by mass Perfume 0.1 parts by mass Water 15 parts by mass

[0057]

INDUSTRIAL APPLICABILITY The anti-caries agent of the present invention has little adverse effect on the flavor and feeling of use of the oral composition to be added, and therefore can be used for a wide range of oral compositions. Further, each plant serving as a raw material for extracting the active ingredient of the anticaries agent of the present invention is present in a large amount in nature and can be stably supplied, so that the anticaries agent of the present invention can be produced safely and inexpensively. be able to.

   ─────────────────────────────────────────────────── ─── Continued front page    F term (reference) 4B018 LB01 LE03 MD48 MD61 ME09                       MF01 MF06                 4C083 AA111 AA112 AB282 AC101                       AC122 AC742 AC782 AD272                       AD532 CC41 DD22 DD23                       EE32

Claims (4)

[Claims] 1. An extract of at least one plant selected from plants of the genus Phyllanthus of the Euphorbiaceae, the Quercus genus of the family Beech, the plants of the genus Hamaboufuu, the plants of the Umbelliferae, the plants of the genus Kawarabouhu and the plant of the genus Sarsbergi of the Lamiaceae, as an active ingredient. An anticaries agent characterized by containing. 2. An anticaries agent comprising as an active ingredient a glucosyltransferase inhibitory substance extracted from at least one plant selected from the group consisting of Prickly rust, Pleurotus cornucopiae, Pleurotus cornucopiae, Pleurotus cornucopiae, Pentaphyllum arvense and Banaba. Agent. 3. The leaves, stems, roots or at least one plant of at least one plant selected from the group consisting of Pleurotus cornucopiae, Pleurotus cornucopiae, Pleurotus cornucopiae, Pleurotus cornucopiae, Pleurotus cornucopiae and Banaba, or a mixed site thereof is treated with water or a hydrophilic solvent or The anti-caries agent according to claim 2, which comprises a glucosyltransferase inhibitory substance obtained by extraction with a mixed solvent of these as an active ingredient. 4. An oral composition containing the anticaries agent according to any one of claims 1 to 3.