JPS5913721A - Agent for suppressing formation of bacterial plaque on tooth - Google Patents

Abstract

PURPOSE:To provide an agent for oral cavity application, containing flavonoid as an active component, suppressing the adhesion of cariogenic bacteria to the flat surface of the teeth, and effective to prevent or inhibit the progress of dental caries. CONSTITUTION:Flavonoid such as rhamnocitrin, kaempferol, etc. is used as a pure substance, or in the form of a vegetable extract containing the same, if necessary in combination with other plaque-formation inhibiting agent or conventional agent for oral cavity application. Flavonoid exhibits the activity to suppress the adhesion of Streptococcus mutans to flat glass surface by in vitro test, and the inhibiting activity to the synthesis of glucan from sucrose by crude glucosyltransferase originated from Streptococcus mutans.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a dental calculus formation inhibitor, and more specifically, as described in the claims, relates to a dental calculus formation inhibitor comprising flavonoids, The purpose is to provide an oral agent that is effective in inhibiting the formation of tartar on tooth surface pressure, thereby preventing erosion or inhibiting its progression.

It is a disease that causes localized and progressive destruction of the teeth, and is considered an extremely serious problem in current public health. .

This phenomenon is caused by the fact that oral streptococci, especially Streptococcus mutan, use sucrose in food as a substrate to produce a sticky polysaccharide (C-glucan), which allows the bacterial cells to adhere to the smooth surfaces of teeth. The first step is to take root.

This aggregate of bacteria that aggregates and colonizes on the south side is called dental calculus (Plp).
−que 1 . In order to prevent dental caries, it is good to suppress the formation of tartar mentioned above. The following various methods can be considered to suppress the formation of such tartar.

The first thing that comes to mind is 8. This method involves administering a drug that exhibits bactericidal or bacteriostatic activity to eradicating cariogenic Me from the oral cavity, and this method has actually been attempted in some cases. However, these drugs have the risk of disturbing the bacterial flora in the oral cavity and intestines, causing an imbalance of bacteria in the natural world, and are accompanied by other side effects, so they are far from being widely used.

Next, there is a mechanical method for removing tartar from IC, and it is routinely done using Habten, but this is a physical cleaning using the hands and does not completely remove tartar ((tartar). It is difficult to remove the tartar.0 The present inventors have conducted various studies on methods for appropriately and accurately inhibiting the formation of tartar, and have extensively examined means for preventing the adhesion of caryogenic bacteria to the smooth surfaces of teeth. As a result of their research, they discovered that flavonoids had such an effect, which was completely unexpected, and as a result of further deep research into Vc, they finally completed the present invention.The following describes the effects of the present invention. The experimental method and results will be explained in detail.

The inhibitory activity of flavonoids against the smooth surface adhesion of -J-t7, S, mutFLns was assayed for the following two points.8 These are also in vitro tests.

(1) In the presence of sucrose, S. mutans
Akira IJ on glass smooth surface adhesion by R, mutanθ-derived crude glucosyltransferase of heat-treated bacterial cells
-9 action by f21 S , mutanq-derived crude glucosyltransferase Next, each will be explained in more detail.

The effect of Zuzu (1) on preventing bacterial cell adhesion will be explained first. The assay method was similar to the method described in the applicant's previous application (Japanese Patent Application No. 156,963/1983), and for the heat-killed bacteria and crude glucosyltransferase, S, mutan, and OMZ+76 strains were used. It was prepared in the same manner as in the previous application. Flavonoids ↑
It was dissolved in methanol to prepare a test solution. However, to judge the adhesion inhibition activity, after the incubation is completed, the airborne bacterial bodies are removed and the adhered bacterial bodies are suspended in 3 ml of FFL ice.
Measure the turbidity at 50 nm + VC and compare it with that of a control with only solvent added at 1C with attached bacterial cells.
1 bottle 11. Activity was determined. The result is the first fi.
[show.

Table 1 shows the flavonoids according to the present invention.
In particular, kaempferol, quercetin, and myricetin exhibit excellent antiadhesion activity.

Next, explain the glucan synthesis inhibitory activity in (2).

Glucan synthesis and its quantification were carried out as follows.
, abbreviated as) 350 μe, 1. R% sucrose containing P
, B, 200/I/? , and 30 μe of the test solution were mixed well, and while cooling in ice water, 20 μe of glucosyltransferase (75 μm/ml) was added, mixed well, and incubated at 37°C for 2 hours. Immediately after incubation, remove γ in ice water and add cold methanol 2.
．． 4 Add II+7 and stir, then leave at 5°C overnight.

-Blank shall not be incubated in the same reaction. After cooling and sufficiently precipitating the glucan with methanol, centrifugation (20p00g, 20 minutes, 5°C) is performed to collect the residue, which is washed twice with 2ml of cold methanol at 80°C to obtain the produced glucan. This is 1. N NFLOH50
Dissolve at 0 treK to obtain a produced glucan solution. The amount of sugar is determined by the Phen91-Ht130 method. That is, the produced glucan solution 500tte VC vs. 17.5
Add 500μe of Typhen01 aqueous solution and mix.Concentrate +1y 80m 2.5117 is quickly added directly to the liquid surface, stirred thoroughly, left at room temperature for 10 minutes, and then kept at 27°CVC for another 20 minutes to complete color development. . 49
The absorbance at 0 nr+t17 was measured 7 and converted into sugar content using sucrose as a standard substance. The influence of the extract on color development, etc. was taken into consideration by using the sample that had been incubated in the same reaction system for a while as a blank. The control was a loaf in which only the solvent methanol (purified water for the glycoside) was added.

As shown in Table 2, flavonoids according to the present invention,
In particular, rhamnocitrin and kaempferol exhibit strong inhibitory activity, which is superior to chlorhexidine gluconate, which has been reported to have significant glucan synthesis inhibitory activity.

The flavonoids used in the present invention are also called flavonoid pigments or anthoxanthins, and include various flavones, flavonols, isoflavones, flavanones, flavanonols, chalcones,
It encompasses penzalkuraranones, andonanes, etc. These flavonoids may be used alone or in combination.

It may be a pure product, or it may be in the form of a plant extract containing these flavonoids. For example @I
An example of this is the use of a methanol extract, which contains a high amount of rhamnosium IJ. If necessary, in addition to these, other tartar formation inhibitors, general oral preparations, and even VCV! iS
, a drug that exhibits bactericidal or bacteriostatic activity against mutane Ic may be used in combination.

The tartar formation inhibitor according to the present invention may be applied directly to intraoral pressure in its form, or may be mixed with other oral preparations such as toothpaste, or may be used as an intraoral spray.
It may also be used in the form of a softener. Troches, sublingual tablets, buccal tablets, chewing tablets, and other dosage forms may be used as required.

It is best to use an appropriate dose based on the above experimental data, but considering the loss during use, for example, a considerable amount may be washed away when rinsing the mouth when mixed with toothpaste, It is advisable to use an excess amount of water.

that's all

Claims (1)

[Claims] 1 Tartar formation inhibitor consisting of flavonoids