JPH08310931A - Inhibitor of glucosyltransferase and cleaning agent for oral cavity - Google Patents

Abstract

PURPOSE: To obtain a new readily usable inhibitor of glucosyltransferases, containing an essential oil of a plant body and having high safety and a cleaning agent for the oral cavity and a food and drink having preventing actions on carious teeth imparted thereto by adding the inhibitor thereto. CONSTITUTION: This inhibitor of glucosyltransferases contains about 0.001-5wt.% an essential oil obtained by carrying out the steam distillation of a plant body selected from the pericarp of an orange, a leaf of a eucalyptus or a mugwort and a flower of a lavender or a rose as an active ingredient (the essential oil of the eucalyptus is blended in a dentifrice, etc.) and prepared into a formulation by further suitably blending optional adjuvants, excipients, water or organic solvents, etc., therewith. The resultant formulation is capable of inhibiting activities of glucosyltransferases which are enzymes capable of synthesizing glucan causing dental caries and effective in prevention of the dental caries. The inhibitor can be added to a cleaning agent for the oral cavity to use its inhibiting actions on the glucosyltransferases for preventing the glucan from being produced in the oral cavity. The inhibitor can be added to a food and drink containing sucrose for preventing the glucan from being produced and the dental caries from causing.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a glucosyltransferase inhibitor having an action of inhibiting the activity of glucosyltransferase, an enzyme that synthesizes glucan causing caries, to prevent the occurrence of caries teeth, and the glucosyltransferase inhibitor. The present invention relates to a mouth cleansing agent and food and drink which are provided with a caries preventive action by adding an agent.

[0002] In this specification, food and drink are meant to include not only foods and drinks eaten by humans, but also feeds and baits of livestock and pet animals that may cause caries.

[0003]

BACKGROUND OF THE INVENTION To develop dental caries, microorganisms in the oral cavity, especially Streptococcus mutans
The enzyme glucosyltransferase produced by mutans) is involved. That is, among the sucrose in the food and drink, what remains in the oral cavity is changed to glucan which is water-insoluble and has strong adhesiveness by the action of glucosyltransferase,
It adheres to the surface of the teeth together with the microorganisms in the oral cavity to form plaque. Then, the microorganisms in the dental plaque metabolize sugar in food to produce acid, and this acid decalcifies and erodes tooth enamel is caries.

Therefore, in order to prevent dental caries, not only is plaque attached to the surface of the tooth removed by brushing the teeth, but also the production of glucan is suppressed by inhibiting the action of glucosyltransferase in the oral cavity. It is most effective to prevent the generation of dirt.

From these points of view, in recent years, oral cleansing agents such as toothpaste and foods and drinks have been provided which have a caries preventive action by containing a substance having a glucosyltransferase inhibitory action. Glucosyltransferase inhibitors conventionally known as suitable for such applications are mutasteine, herbal medicine tannins, ellagic acid, green tea polyphenols, oolong tea extract and the like.

[0006]

DISCLOSURE OF THE INVENTION An object of the present invention is to provide a novel glucosyltransferase inhibitor made of a highly safe natural product as a raw material, and an oral cleansing agent added with it to prevent caries. To provide food and drink.

[0007]

The novel glucosyltransferase inhibitors successfully provided by the present invention are:
Orange (Citrus aurantium L.) peel, eucalyptus (E
ucalyptus globulus L.) leaves, mugwort (Artemisia pr)
inceps P. And Artemisia mongolia F.) leaves, lavender (Lavandula vera DC) flowers, and roses (R
(Osa centifolia L.) flowers are essential oils obtained by steam distillation from plants selected from the group consisting of flowers.

The present invention also provides an oral cleansing agent and a caries-preventive food or drink, which comprises the glucosyltransferase inhibitor according to the present invention.

The present invention was completed based on the novel finding by the present inventors that the essential oil obtained by steam distillation from the above-mentioned specific plant body exhibits an excellent glucosyltransferase inhibitory action.

All of the above-mentioned essential oils are commercially available and can be used as they are in the present invention, but they can also be produced from a raw material plant by a conventional method of steam distillation. That is, the raw plant is charged into a steam distillation apparatus,
Steam is continuously supplied to the sedimentary layer to heat the plant, and the steam after passing the heated plant sedimentary layer is cooled by a cooler to collect a condensate, which is separated when left standing. Collect the oil layer. Since a part of the essential oil is also dispersed or dissolved in the aqueous layer, it may be recovered by organic solvent extraction and used. Since the obtained essential oil exhibits a strong glucosyltransferase activity inhibitory action, it can be used as it is as the glucosyltransferase inhibitor of the present invention.

In addition to the plant essential oil, the glucosyltransferase inhibitor of the present invention may optionally contain any auxiliary agent, excipient, water or organic solvent for use as a solution.

The glucosyltransferase inhibitor of the present invention can be added to an oral cleansing agent and its glucosyltransferase inhibitory effect can be utilized to prevent glucan production in the oral cavity. Examples of mouth cleansing agents suitable for addition include various toothpastes, mouthwashes, troches, chewing gums, oral pasta, gum massage creams, mouthwashes, mouthwashes and the like.

The addition of the glucosyltransferase inhibitor of the present invention does not limit other components of the oral cleansing agent or the method for producing the oral cleansing agent. For example, calcium hydrogen phosphate, calcium carbonate, insoluble sodium metaphosphate, Abrasives such as aluminosilicate, silicic anhydride, and resin; surfactants such as long-chain sodium alkylsulfate, sodium laurylsulfoacetate, lauryldiethanolamide, sucrose fatty acid ester; CMC, hydroxyethylcellulose, alginate, carrageenan, gum arabic , A binder such as polyvinyl alcohol; a thickener such as polyethylene glycol, sorbitol, glycerin, propylene glycol; a sweetener such as saccharin, stevioside, glycyrrhizic acid, thaumatin; dehydroacetic acid, dehydroacetic acid Preservatives such as sodium; menthol, carvone, eugenol, anethole, peppermint oil,
Fragrances such as spearmint oil, peppermint oil, eucalyptus oil, ginger oil, anise oil; various pigments and other ingredients commonly used in the manufacture of mouth cleansing agents are arbitrarily selected according to the product type and application It can be manufactured.

When the mouth cleansing agent is produced by adding the glucosyltransferase inhibitor of the present invention, other glucosyltransferase inhibitors may be used in combination, and an antibacterial agent effective against Streptococcus mutans may be used. You may use together. Furthermore, by adding any anti-inflammatory agent, antibacterial agent, deodorant, etc., it is possible to provide a more excellent oral cleansing agent. Examples of anti-inflammatory agents that can be added include Acacia yak, liquorice, oak, oak, ginger, psychosis, hawthorn, hawthorn, perilla,
Extracts such as peony, sowakuhi, kyounin, tannin, clove, tonin, nutmeg, button pie; azulene, allantoin, ursolic acid, oleanolic acid,
Glycyrrhizic acid, glycyrrhetinic acid or derivatives thereof; tocopherol, tranexamic acid, etc. can be mentioned, and examples of antibacterial agents that can be added include Gobaishi, Cycin, salmon, ginger, dill, thyme, rosemary, oil-soluble Extracts such as licorice extract; ascorbic acid, muustine, humic acid, linoleic acid, linolenic acid and the like can be mentioned. Furthermore, examples of deodorants that can be used in combination include extracts of amacha, fennel, veiled oak, keihi, pepper, mace, sage, perilla, ginkgo, oyster leaf, green tea, oolong tea, capsicum, tamarind husk; rosin, oyster. Shibu, actizol,
Chlorophyllin derivative, ellagic acid, chlorhexidine,
Examples include Maillard reaction products.

The effectiveness of the glucosyltransferase inhibitor of the present invention varies slightly depending on the type of raw material plant, the place of origin, the time of collection, and the like. Therefore, it is difficult to uniformly show a suitable addition amount of the glucosyltransferase inhibitor of the present invention to the oral cleansing agent, but when describing an example in which a standard eucalyptus essential oil is directly blended in toothpaste or the like, it will be about 0.001. .About.5.0% by weight is a suitable amount, and a particularly preferable blending ratio is about 0.005 to 1.0% by weight.

The glucosyltransferase inhibitor of the present invention can also be added to foods and drinks containing sucrose to prevent the production of glucan in the oral cavity and thus prevent caries. Examples of suitable substances to be added include soft drinks, confectioneries, breads, candies, chewing gums, gummi, jellies, chocolates and pet foods.

[0017]

The present invention will be described below with reference to examples. In addition, in each example of Examples 2-7, "part" means a weight part.

Example 1 100 kg of fresh rose flowers were put in a steam distillation apparatus, steam was passed through the steam, and the distillate obtained by cooling the passing steam with a cooler was allowed to stand at 5 ° C., and the separated oil layer was collected. 300 g of essential oil was obtained.

By the same operation, essential oils were also obtained from orange peel, eucalyptus leaves, mugwort leaves and lavender flowers (yields 1.8 kg, 1 kg, 200 g and 800, respectively).
g).

The glucosyltransferase activity inhibition rate of each of the obtained essential oils was examined by the following method.

Glucosyltransferase activity inhibition rate measurement method: 2% sucrose solution (using a pH 6.5 50 mM potassium phosphate buffer) 1.0 ml 1% sodium azide 0.1 ml crude glucosyltransferase solution 50 μl essential oil solution (concentration 10 mg / ml DMSO) 50 μl 50 mM potassium phosphate buffer (pH 6.5) 0.1 ml

The enzyme reaction solution (the essential oil concentration is 400 μg / ml) obtained by mixing the above-mentioned solutions is put into a test tube, the test tube is tilted at 30 degrees, and the mixture is allowed to stand at 37 ° C. for 20 hours. Then, the test tube is slowly tilted to remove the reaction supernatant, and the glucan produced by the enzymatic reaction and attached to the test tube is washed three times with water. Then, 2 ml of water is added and the glucan is dispersed in water by ultrasonic treatment. The absorbance at a wavelength of 550 nm is measured for the glucan dispersion and the above-mentioned enzyme reaction solution immediately after preparation. As a control, the same operation is performed when water is added instead of the essential oil aqueous solution.
From the measurement results, the inhibition rate of glucosyltransferase activity is calculated by the following calculation formula.

Inhibition rate (%) = [1− (A ₁ −A ₀ ) / (A ₃ −A ₂ )] × 100 where A ₀ : Absorbance when essential oil is added; before initiation of enzymatic reaction A ₁ : Absorbance when essential oil was added; glucan dispersion liquid A ₂ : control (before starting enzyme reaction) A ₃ : control (glucan dispersion liquid) The results are shown in Table 1.

[0024]

[Table 1]

The following are examples of foods and drinks and mouth cleansing agents containing these essential oils as glucosyltransferase inhibitors.

Example 2 The following raw materials were mixed by a conventional method for producing candy, and further boiled and molded to produce a candy for preventing caries. Sucrose 70 parts starch syrup 30 parts citric acid 1 part fragrance 0.1 parts orange essential oil 0.01 parts water 20 parts

Example 3 A caries-preventive chewing gum was produced by treating the following raw materials by a conventional method for producing chewing gum. Chewing gum base 20 parts Sucrose 55 parts Syrup 20 parts Softener 4 parts Perfume (mint oil) 0.8 parts Rose essential oil 0.05 parts

Example 4 The following raw materials were processed by a conventional method for chocolate production,
A caries-preventive chocolate was produced. Chocolate 45 parts Sucrose 15 parts Cocoa butter 20 parts Whole milk powder 25 parts Lavender essential oil 0.1 parts

Example 5 Dicalcium phosphate 45 parts CMC / sodium salt 1 part Glycerin 20 parts Sodium lauryl sulfate 2 parts l-Menthol 1 part Glycyrrhizin 0.1 parts Eucalyptus essential oil 0.1 parts Water 30 parts Mixing the above raw materials , A dental caries preventive toothpaste was produced.

Example 6 Ethanol 20 parts Glycyrrhizin 0.2 parts Glycerin 5 parts Chlorhexidine 0.005 parts l-Carvone 1 part Artemisia essential oil 0.5 parts Water 70 parts The above ingredients are mixed to prepare a caries preventive mouthwash. Manufactured.

Example 7 Wheat flour 30 parts Cornflower 15 parts Soybean flour 15 parts Meat meal 20 parts Sucrose 5 parts Beef tallow 5 parts Salt 1 part Calcium phosphate 2 parts Potassium sorbate 0.5 parts Perfume 0.5 parts Propylene glycol 7 parts Lavender essential oil 0.1 part The above raw materials were mixed, 40 parts of water was added to 100 parts of the obtained mixture, and the mixture was molded into pellets while heating with an extruder to produce a dog food.

[0032]

INDUSTRIAL APPLICABILITY According to the present invention, there is provided a novel glucosyltransferase inhibitor which is safe and easy to use, which contains plant essential oils which have been used as crude drugs for a long time. Since this inhibitor does not cause any concern even if it is ingested into the body, it becomes possible to provide an oral cleansing agent or a caries-preventive food or drink to which a caries-preventing action is added by incorporating the inhibitor.

Continuation of the front page (51) Int.Cl. ⁶ Identification code Office reference number FI Technical display area A61K 35/78 ACK A61K 35/78 ACKW C12N 9/99 C12N 9/99

Claims (3)

[Claims] 1. A peel of orange (Citrus aurantium L.), a leaf of eucalyptus (Euca-lyptus globulus L.), a mugwort (Artemisia princeps P. and Artemisia mongolia).
F.) leaves, lavender (Lavandula vera DC.) Flowers, and rose (Rosa centifolia L.) flowers, as an active ingredient, an essential oil obtained by steam distillation from a plant selected from the group consisting of A glucosyltransferase inhibitor characterized by: 2. An oral cleansing agent comprising the glucosyltransferase inhibitor according to claim 1. 3. A caries-preventive food or drink, which comprises the glucosyltransferase inhibitor according to claim 1.