JPH0455164B2 - - Google Patents

Description

[Detailed description of the invention]

FIELD OF THE INVENTION The present invention relates to caries treatment materials. For more details,
The present invention relates to gallotannins such as trigalloylglucose, tetragalloylglucose, pentagalloylglucose, hexagalloylglucose, heptagalloylglucose, octagalloylglucose, thievlic acid, thiebradiic acid, granatin A, granatin B, punicalin, or The present invention relates to a cariogenic material containing one or more punicalagins as an active ingredient. Dental caries, generally referred to as dental caries, is a disease that causes localized and progressive destruction of teeth, has an extremely high morbidity rate, and has become an important public health problem in modern times. According to recent research results, dental caries is caused by the presence of sucrose in food, which is linked to certain oral streptococci, especially Streptococcus miutans.
This is thought to be due to the production of insoluble and sticky glucan (a polysaccharide consisting of D-glucose) through the action of glucosyltransferase derived from D-glucose (D-glucose). That is, due to the glucan produced as described above, bacterial cells adhere to the tooth surface and multiply to form dental moss, which is a nest of bacteria. This process is the first stage of dental caries, and then the bacteria in this dental plaque demineralize the tooth tissue with the acid produced by sugar fermentation, and caries progresses. Since the essence and cause of dental caries is an infectious disease, it is necessary to eradicate the oral streptococcus that causes dental caries in order to prevent it and prevent its progression. Oral streptococci include Streptococcus mutans and Streptococcus sanguis.
sunguis) and Streptococcus mitis, among which Streptococcus mutans has the strongest caries progeny. i.e., Storeptococcus mutans
It is known that the ability to adhere to tooth surfaces (requirement for sucrose), the bacterial agglutination reaction (induced by high molecular weight dextran), and the ability to produce lactic acid through sorbitol-mannite fermentation are key characteristics, and these properties are important for caries induction. extremely involved. Conventionally, many studies have been conducted to eradicate oral bacteria in order to prevent dental caries. For example, antibiotics such as penicillin, bacterial wall-lytic enzymes,
There are research results using fungicides such as chlorhexidine. However, all of these are associated with side effects resulting from disrupting the human bacterial balance by disrupting oral and intestinal bacteria. This side effect is particularly noticeable with antibiotics, but in any case they have not been widely put into practical use, and no caries prevention method superior to physical cleaning methods has been established. The present inventors previously disclosed the invention of an agent for preventing and inhibiting the progression of caries using Japanese and Chinese medicine in Japanese Patent Application Laid-open No. 57-85319 entitled "Caries Agent" etc., but as a result of further intensive research, The invention has been completed. Traditionally, tannins have been useful as a general term for substances that have the property of transforming hides into leather, but tannins have been fractionated and purified into their constituent components, and the ability of each component to inhibit enzyme activity has been studied. I haven't done anything yet. The present inventors focused on the individual components contained in tannins, and discovered
We fractionated and purified the individual components of tannins using a method such as saccharine, examined their ability to inhibit the enzyme activity of glucosyltransferase, and conducted research to find particularly effective components for use in dental caries agents. I found out. The present invention will be explained in detail below. The anti-caries agent according to the present invention is used as dentifrices such as toothpaste, toothpaste, water toothpaste, troches, mouthwashes, liniments, chewing gums, etc., and has active ingredients such as trigalloylglucose and tetragalloylglucose. , gallotannins such as pentagalloylglucose, hexagalloylglucose, heptagalloylglucose, octagalloylglucose, tubulic acid thiebradiic acid, granatin A, granatin B, punicalin or punicalagin. Become. Each of the above substances is
It may be fractionated and purified from medicinal plants such as uricum, gomae, orchid, or it may be obtained by other methods, such as chemical synthesis. The present invention will be specifically explained below with reference to test examples and formulation examples, but the present invention is not limited thereto. Test example Specimen: The medicinal plants Uwa sumac, Gobai, Azalea, and Pomegranate are finely powdered, extracted with water or ethanol, separated and purified by liquid chromatography, and each compound is determined by the standard specimen. Those that were identified were used as specimens. Test method: Enzyme titer method by Mukasa et al.
The ability of each sample to inhibit glucosyltransferase activity was measured by assay. Standard reaction solution 10μ
This includes: When the sample is an aqueous solution, add [ ^14C ]-labeled sucrose (1mM,
100μCi/ml), potassium phosphate buffer (0.1M, PH
6.8), glucosyltransferase 0.34mg/ml
and 5μ of sample aqueous solution. When the sample is an ^ethanol solution, add sucrose (1mM,
100μCi/ml), potassium phosphate buffer (0.1M, PH
6.8), glucosyltransferase 2.2mg/ml
and 1μ of sample ethanol solution. The above standard reaction solution was incubated at 37°C for 1 hour, cooled with ice water, and spotted on "Toyo 51A" filter paper. The filter paper is developed three times with a mixed solvent of pyridine/water/butanol (6:3:4), and radioactive spots are detected by autoradiography and quantified using a liquid scintillation counter. The reagents used in this test are as follows. Enzyme - A crude enzyme was obtained from Streptococcus miutans strain OMZ176 (serotype d) by modifying the method of Mukasa et al. [ ¹⁴ C] labeled sucrose-purchased from New England Nuclear. Control compound - chlorhexidine gluconate. Judgment of results: The ability of each sample to inhibit glucosyltransferase activity was determined from the relationship between the concentration of the sample and the amount of sticky glucan produced. The results are shown in Tables 1 and 2.

【table】

[Table] Formulation Example 1 Toothpaste A toothpaste is obtained according to the formulation shown below using a conventional method. Note that the numerical values indicate parts by weight. Dicalcium phosphate dihydrate…45 Carboxymethyl cellulose…1.0 Glycerin…20 Sodium lauryl sulfate…1.5 Flavoring…1.0 Artificial sweetener…0.1 Sodium fluoride…0.1 Sample…0.2 Water…100 remaining Combination example 2 Lozenge By the usual method, A troche is obtained according to the formulation shown below. Note that the numerical values indicate parts by weight. Gum arabic…6.0 Fructose…20 Glucose…20 Maltose…30 Flavor…0.1 Artificial sweetener…0.1 Sample…3.0 Water…Remaining 100 Compounding example 3 Tablets for loading Preparation of tablets for loading using the following recipe using the usual method obtain. Note that the numerical values indicate parts by weight. Sodium diphosphate…15 Sodium hydrogen carbonate…55 Polyethylene glycol…3.0 Sodium monofluorophosphate…0.5 Flavor…4.0 Chlorhexidine…0.05 Citric acid…15 Ethanol…6.0 Sample…1.0 100

Claims (1)

[Claims] 1 trigalloylglucose, tetragalloylglucose, pentagalloylglucose, hexagaloylglucose, heptagaloylglucose,
An agent for caries containing one or more of the following as active ingredients: gallotannins of octagalloylglucose, thiebric acid, thiebradiic acid, granatin A, granatin B, punicalin, or punicalacin.