JPH0434968B2 - - Google Patents

Description

[Detailed description of the invention]

(Field of Industrial Application) The present invention is a dental carcinogen that exhibits excellent antibacterial activity against oral bacteria represented by Streptococcus mutans, which is greatly involved in the formation of dental caries. Concerning a cariogenic fungus growth inhibitor. (Prior Art) Chlorhexidine, antibiotics, and the like have been known to be used as drugs that inhibit the growth of oral bacteria, and many synthetic and natural products have been reported. (Problems to be Solved by the Invention) However, these known oral bacteria growth inhibitors may have safety issues for the human body depending on the administration method and dosage, and their stability has not been confirmed. However, it has drawbacks such as low antibacterial properties and an unpleasant odor when administered. An object of the present invention is to provide a cariogenic bacteria growth inhibitor that has been confirmed to be safe for the human body, has high antibacterial properties, and has a pleasant aroma. (Means for Solving the Problems) According to the present invention, there is provided a cariogenic fungus growth inhibitor characterized by containing maltol and/or ethyl maltol as an active ingredient. The present invention will be explained in more detail below. In general, the causes of dental caries (cavities) formation include tooth substance, substrate, and St. mutans, and when these three factors exist at the same time, caries (caries) occurs. ) is said to occur. The mechanism of caries formation is, for example, when sugar is used as a substrate among sugars, this sugar is hydrated by glucoxytransferase (enzyme) produced by St. mutans. It changes into insoluble and sticky dextran (glucan) and forms plaque on the surface of teeth. This dental plaque becomes anaerobic and fermentation progresses due to lactic acid bacteria, etc., producing lactic acid and lowering the pH. This lactic acid is said to demineralize tooth enamel and form caries (cavities). Therefore, suppressing the growth of oral bacteria such as St. mutans and inhibiting the formation of dental plaque is an effective method for preventing the formation of dental caries. The present inventors are actively searching for a substance that is compatible with the conditions of inhibiting the growth of St. mutans, which has already been confirmed to be safe for the human body and is significantly involved in caries formation. As a result of research, it was discovered that maltol and/or ethyl maltol are very effective, leading to the completion of the present invention. Maltol and ethylmaltol used in the present invention are already known substances, and the different chemical structural formulas and chemical names are shown below. 3-Hydroxy-2-methyl-4-pyrone (maltol) 3-Hydroxy-2-ethyl-4-pyrone (ethyl maltol) The maltol used in the present invention is a commercially available product, such as pyromatol (Otsuka Chemical Co., Ltd., trade name) and bertol (Phizer Co., Ltd., trade name) and ethyl maltol. Maltol is a commercially available product, such as pyromatol E (Otsuka Chemical Co., Ltd.).
Co., Ltd., product name) and Bertol Plus (Phaseiser
Co., Ltd., commercially available products) can be used. Maltol and ethyl maltol used in the present invention are listed in the GRAS list (No. 2656, No. 3487) and
It is a flavoring substance whose safety has already been confirmed and is listed on the FDA list (〓121・1164,〓121・1164), and it is a flavoring agent or flavor improvement enhancer (Flavor
enhancer), such as Chiyocolate products,
It is widely used in breads, sugar confections, alcoholic beverages, meat products, dairy products, ice cream, canned foods, tobacco, toothpaste, lipstick, health products, animal feed, etc. [Overview of Fragrance Chemistry (), Osamu Okuda, 940 pages,
Published by Hirokawa Shoten]. It is surprising that a flavoring substance that gives off a pleasant aroma in the oral cavity exhibits excellent effects as a cariogenic bacteria growth inhibitor. The maltol and ethyl maltol of the present invention may be used together, or one of them may be used alone. The cariogenic bacteria growth inhibitor of the present invention can be expected to be effective when incorporated into tablets, chewing gum, candy, troches, etc., which have a relatively long residence time in the oral cavity. Since growth inhibitors have almost no antibacterial activity due to surfactants, they can also be used in combination with oral cleansers such as toothpastes and mouthwashes. The blending amount is not necessarily uniform depending on the form and type of the target product, but it is 0.005%/10% by weight of the oral composition, preferably 0.01%.
Generally, it is blended in an amount of ~5% by weight. Examples of formulations containing the caries growth inhibitor of the present invention are shown below. Formulation Example 1 Chewing gum of the composition shown below was manufactured according to a conventional method. Ingredient weight% Gum base 20 Powder sugar 35 Maltose 10 Fructose 10 Starch syrup 15 Flavor 1 Maltol 0.4 Water Balance 100% Formulation example 2 A mouthwash of the composition shown below was produced according to a conventional method. Ingredient weight % Ethanol 20 Saccharin 0.5 Glycerin 50 Sucrose laurylate 2 Turolhexidine 0.5 Flavor 1 Ethyl maltol 0.5 Water Balance 100% Formulation Example 3 A troche of the composition shown below was produced according to a conventional method. Ingredients Weight% Gum Arabic 8 Maltose 30 Fructose 20 Glucose 20 Flavor 0.2 Maltol 0.2 Water Balance 100% (Example) Next, the antibacterial activity of maltol and ethyl maltol of the present invention will be explained in more detail by Examples. do. Example 1) Peptone 1%, yeast extract 0.5%, sucrose 2%,
Prepare an agar medium with a pH of 7.0, sterilize it, cool it, and add it to it.
0.5% of the culture solution of Streptococcus mutans RIMD-3125001 strain cultured for 24 hours was added, and 12 ml of each was immediately poured into a sterilized jar with a diameter of 80 mm. Next, a pepper disc with a diameter of 8 mm was impregnated with the sample compound, placed on the center of the above-mentioned Schare's agar medium, and cultured upside down at 37°C for 72 hours. The antibacterial activity test (preliminary test) was evaluated as follows. A transparent agar medium becomes cloudy when bacteria proliferate, but if the sample has antibacterial activity, the area around the pepper disc will remain transparent, so this clear zone (hereinafter referred to as the inhibition circle diameter) will be measured to determine the inhibition. A circle diameter of 40 mm or more was evaluated as having an effective growth inhibition effect.

[Table] From the results shown in Table 1, maltol showed an excellent bacterial growth effect, and ethyl maltol in particular showed a very remarkable inhibiting effect. Example 2) The same method was used as in Example 1, except that a heart infusion agar medium (pH 7.0) containing 2% sucrose was used, and the results were as shown in Table 2 below. The results obtained were as follows.

[Table] From the results shown in Table 2, maltol showed an excellent growth-inhibiting effect, and ethyl maltol in particular showed a very remarkable inhibiting effect. Example 3) Streptococcus mutans RIMD-3125002 (E49)
As a result of using the same medium and the same method as in Example 1 except for using the different strains, the results shown in Table 3 below were obtained.

[Table] From the results shown in Table 3, both maltol and ethylmaltol showed extremely remarkable effects in inhibiting bacterial growth. Example 4) 0.02% maltol in a heart infusion broth liquid medium (pH 7.0) supplemented with 2% sucrose
(1/5000 concentration), precultured, and cultured with Streptococcus mutans strain 3125001.
After adding 0.5% and culturing at 37℃ for 24 hours in a nitrogen desiccator, we checked the growth status of the bacteria. As a result, there was no decrease in the pH of the culture medium and no glucan formation was observed, so the bacteria were completely destroyed. was able to prevent the growth of. In addition, for the purpose of practical use of this sample, the antibacterial activity was measured in the presence of 0.5% sodium lauryl sulfate, and no decrease in activity was observed compared to when no additive was added. Example 5) The test sample was mixed with ethyl maltol 0.02% (1/5000
As a result of carrying out the experiment using the same medium (pH 7.0), bacteria, and method as in Example 4, except that the concentration of
Since there was no decrease in pH and no glucan formation was observed, bacterial growth was completely inhibited.

Claims (1)

[Claims] 1. A caries growth inhibitor characterized by containing maltol and/or ethyl maltol as an active ingredient.