KR20180046252A - Composition for prevention or treatment of oral disease comprising 1,2,4-Trihydroxyanthraquinone - Google Patents

Abstract

The present invention relates to a composition for preventing or treating oral diseases containing 1,2,4-trihydroxyanthraquinone, and more specifically, to a quasi-drug composition having an effect of preventing or alleviating dental caries, periodontal diseases, toothache, tooth smarting, and halitosis. The composition of the present invention has excellent antibacterial activity for bacteria inducing dental caries and periodontal diseases, inhibits PGEE2, which is a pain and inflammatory marker, in a concentration-dependent manner, and has excellent effects of inhibiting formation of gingivitis and tooth smarting, and removing halitosis. Accordingly, the composition of the present invention is highly applicable as a quasi-drug composition for preventing or alleviating one or more oral diseases selected from the group consisting of dental caries, periodontal diseases, toothache, tooth smarting, and halitosis. In addition, the composition of the present invention can be used as a pharmaceutical composition and a food composition.

Description

TECHNICAL FIELD The present invention relates to a composition for preventing or treating oral diseases including 1,2,4-trihydroxyanthraquinone,

The present invention relates to a composition for preventing or treating oral diseases comprising purpurin (1,2,4-trihydroxyanthraquinone), and more particularly, to a composition for preventing or treating oral diseases, The present invention also relates to a quasi-drug composition having an effect of treating The present invention also relates to pharmaceutical compositions, food compositions and oral compositions comprising furfurin.

Healthy teeth are one of the most important factors that determine the quality of life. Among oral diseases, dental cavities and periodontal diseases are diseases with high incidence worldwide and they have various clinical symptoms such as pain, chewing dysfunction, destruction of periodontal tissue, bad breath, And is known to be the main cause of tooth loss. The causes of oral diseases are increasing due to dietary changes.

It is known that about 600 to 800 or more microorganisms exist in human oral cavity, and these microorganisms are controlled by enzymes such as lysozyme secreted by saliva. However, nutrients and water-rich oral environments are good conditions for microbial growth, and dental plaques provide excellent microbial habits. Some of these microorganisms are opportunistic pathogens, causing diseases such as dental caries, periodontal disease, and acin (dentin hypersensitivity) and bad breath.

There are antimicrobial agents that inhibit the growth of oral pathogens that induce dental caries, periodontal disease, bad breath, and acinar infestation, and various kinds of antimicrobial agents including antibiotics that have a sterilizing and bacteriostatic action against oral pathogens, Have been developed as inhibitors and remedies for periodontal disease, dental and periapical infections.

However, since antibiotics can cause systemic adverse effects on our bodies and induce resistance to oral bacteria and superinfection, they are difficult to use for a long time and can only be used as therapeutic agents. The antimicrobial agents used in mouthwash are Sangquinarine, Listerine, Peroxide, and Chlorhexidine. The effect of bacteria on oral bacteria is unclear in the oral cavity The treatment effect of periodontal disease is more unclear, and the price is also high. Listerine is a major ingredient of alcohol and has a slight bacteriostatic effect. However, it has a temporary effect only in the oral cavity. There are drawbacks that can appear. In addition, the recently added pyridoxine for the whitening effect is toxic to bacteria but at the same time toxic to human tissues, which is not only problematic in safety but also resistant to bacterial fungi in bacteria. In addition, chlorhexidine is known to be one of the best known agents for the prevention and treatment of periodontal disease as well as suppression of plaque formation. However, chlorhexidine induces irritation of tissues, pigmentation and degeneration of tissues, and especially stimulant taste and odor In addition, there is a disadvantage in that it can not be used for a long time for the purpose of treatment or especially prevention, such as the occurrence of bacterial diabetes, carcinogenicity and limited use in pregnant women.

On the other hand, purpurin (1,2,4-trihydroxyanthraquinone) has the molecular formula C ₁₄ H ₈ O ₅ , molecular weight of 256.21, and is the main extract of the ruby (Rubia akane NAKAI). The furfurin is a red needle-shaped crystal and easily dissolves in ethanol and ether, and the color changes depending on the reagent. It changes to red in alcohol, aluminum solution (150 ℃, high pressure 2mmHg), it becomes dark yellow by benzene, toluene, xylene, and becomes yellow which becomes fluorescent by ether.

Under these circumstances, the present inventors have conducted studies to derive natural materials excellent in prevention and improvement of oral diseases such as dental caries, periodontal disease, toothache, syringe and bad breath without fear of side effects as described above . As a result, as a naturally-occurring composition which can be safely used safely in the body, purpurin exhibits antimicrobial effect, PGE2 inhibitory effect, gingivitis formation inhibitory effect, siline inhibitory effect and bad breath removal effect on dental caries and periodontal disease-causing bacteria The present invention has been accomplished on the basis of these findings. The present invention relates to a quasi-drug composition, a pharmaceutical composition, a food composition, and an oral composition containing furfurin.

Korean Patent Publication No. 10-2015-0050239 Korean Patent Publication No. 10-2015-0128334

It is an object of the present invention to provide a quasi-drug composition for preventing or improving oral diseases, which comprises furfurin or a pharmaceutically acceptable salt thereof as an active ingredient.

Another object of the present invention is to provide a pharmaceutical composition for preventing or treating oral diseases comprising furfurin or a pharmaceutically acceptable salt thereof as an active ingredient.

It is still another object of the present invention to provide a food composition for preventing or improving oral diseases comprising furfurin or a pharmaceutically acceptable salt thereof as an active ingredient.

Another object of the present invention is to provide an oral composition comprising furfurin or an acceptable salt thereof as an active ingredient.

The present invention provides a quasi-drug composition for preventing or treating oral diseases, which comprises furfurin or a pharmaceutically acceptable salt thereof as an active ingredient to solve the above problems and to achieve the object of the present invention.

As another aspect of the present invention, there is provided a pharmaceutical composition for preventing or treating oral diseases comprising furfurin or a pharmaceutically acceptable salt thereof as an active ingredient.

As another embodiment of the present invention, there is provided a food composition for preventing or improving oral diseases, which comprises furfurin or a pharmaceutically acceptable salt thereof as an active ingredient.

As another embodiment of the present invention, there is provided an oral composition comprising furfurin or an acceptable salt thereof as an active ingredient.

The present invention provides a quasi-drug composition comprising furfurin or a pharmaceutically acceptable salt thereof as an active ingredient.

In the present invention, "greener purine (1, 2, 4-trihydroxyanthraquinone , purpurin)" is represented by the formula (1), the molecular formula C ₁₄ H ₈ O _5, as a natural coloring matter having a molecular weight of 256.21, madder (Rubia akane NAKAI) Is the most prominent extract.

Rubia akane NAKAI is a perennial herbaceous perennial herbaceous plant that contains purple purine and alizarin (C ₁₄ H ₈ 0 ₂ ) and its glycoside, ruberitric acid (C ₂₅ H ₂₆ 0 ₁₃ ) there are false positives _{(C 15 H 8 0 7)} , xanthosine greener purine _{(C 14 H 8 0 4)} , furfuryl lock Santin, ruby andin glycosides and the like. It is used for the treatment of endometritis when there is no menstruation, when there is no menstruation, when swelling is fever, when the fever is fever, especially when there is heat in the lungs and liver, swine flu and pneumonia , Sore throat, and blood circulation. The ingredients and use of herbal medicine, science, encyclopedia publishing company / January, Seokgak / Choi, Okja / 1994].

The present invention is not particularly limited to the method for obtaining furfurin, and may be chemically synthesized by a method known in the art, or a commercially available substance may be used.

The purin purines of the present invention may exist in solvated as well as unsolvated forms. The furfurin of the present invention may exist in crystalline or amorphous form, and all such physical forms are included within the scope of the present invention.

The present invention provides a quasi-drug composition for preventing or ameliorating oral diseases comprising the above purpurin or a pharmaceutically acceptable salt thereof as an active ingredient.

More specifically, the present invention relates to a pharmaceutical composition comprising at least one oral cavity selected from the group consisting of dental caries, periodontal disease (periodontitis or gingivitis), toothache, syringitis and bad breath comprising the above purpurin or a pharmaceutically acceptable salt thereof as an active ingredient A quasi-product composition for preventing or ameliorating a disease can be provided.

In the present invention, " oral disease " refers to various diseases occurring in the oral cavity region, and the oral cavity region refers to a space in the mouth which is connected to the pharynx from the front lip to the rear mouth. In the present invention, the oral disease refers to a disease that occurs in the oral cavity, regardless of its pathology. Examples of the oral disease include dental caries, periodontal disease (periodontitis or gingivitis), toothache, And the like.

In the present invention, " dental cavities " is an infectious disease caused by bacteria in the tooth surface, which is also called tooth decay. Specifically, a milky translucent and hard material that covers the surface of the head of a tooth and protects the tooth dentin is called tooth enamel or enamel. By the acid generated by decomposition of sugar and starch by the oral pathogenic bacteria in the mouth It means that tooth enamel is damaged and tooth decay occurs. A major cause of dental caries is dental plaque (plaque), which is a bacterial membrane formed on the surface of a tooth. The saliva forms a thin and sticky film on teeth, and on top of that, Streptococcus sobrinus A dental plaque is formed by the adhesion of oral microorganisms such as Streptococcus sobrinus and Streptococcus mutans to form biofilm and thicker by Fusobacterium Loses. Dental caries of the present invention if the organisms that cause dental caries but includes, regardless of their kinds, specifically Streptococcus mutans (Streptococcus mutans), Streptococcus Sangu yiniseu (Streptococcus sanguinis), Streptococcus small debris Taunus (Streptococcus sobrinus), Streptococcus Lahti (Streptococcus ratti), Streptococcus Cri Shetty (Streptococcus criceti), Streptococcus not Gino suspension (Streptococcus anginosus) and are from the group consisting of lactic acid bacteria can be at least one selected uniform, more specifically, Streptococcus It can be Mutans.

The Streptococcus mutans is a type of streptococcus, Gram-positive bacteria, and is also referred to as carnivorous. Streptococcus mutans proliferate only on the surface of the teeth, but not until 30 months after birth. Therefore, it is difficult for Mythans to multiply until after this period. When other oral bacteria in the mouth are not infected by the mutans bacteria from the mouths of adults during infancy, it is difficult for the mutans bacteria to enter the already balanced ecosystem in the oral cavity. . If you are already infected with causative organisms through adults' mouths, brush your teeth frequently and keep your mouth clean to help prevent tooth decay. However, once mutans bacteria are in the oral cavity, it is impossible to eradicate mutans.

In one embodiment of the present invention, the size of growth inhibition rings was measured after inoculating a disk containing purpurin in a medium coated with Streptococcus mutans, and as a result, in the experimental group containing purpurin, , And it was confirmed that a composition containing furfurin can be used for prevention or improvement of dental caries (Table 2).

In the present invention, " periodontal disease " refers to a disease in which gingiva, periodontal ligament, and bone tissue injure the teeth, and is often referred to as a style. Depending on the severity of the disease, gingivitis and periodontitis, . It is a relatively light and fast-acting periodontal disease called gingivitis that is limited to gingiva or soft tissue, and it is called periodontitis when the inflammation progresses to the gums and the gums. There is a V-shaped gap between the gum (gums) and the teeth, where oral pathogens attack the area under the gum line of the sulcus to release the inflammatory stimulant Lipopolysaccharide (LPS) Inflammation occurs, such as swelling of the gums and bleeding, which can damage the periodontal ligament and adjacent tissue. If periodontal disease progresses, the periodontal ligament, and even the alveolar bone, will be damaged and eventually the teeth will be lost. Malnutrition such as protein and vitamins, hormonal disorders such as pregnancy and diabetes, smoking, AIDS and the like can aggravate the disease. Other causes of periodontal disease include plaque and calculus. The periodontal disease of the present invention includes all kinds of causative bacteria causing periodontal disease regardless of the type thereof, but specifically, Actinobacillus Actinomycetemcomitans , Porphyromonas gingivalis , Tannerella forsythia , Treponema ( Treponema spp.), denticola , and Fusobacterium nucleatum . More specifically, it may be Poppyromonas japonica varis.

The Poppyromonas jinx valis is a kind of Bacteroide-type bacteria and is gram-negative bacteria and anaerobic bacteria. The Poppyromonas jinx valis is found in the oral cavity with periodontal disease, as well as in the upper gastrointestinal tract, respiratory tract and colon. In patients with chronic periodontal disease, collagen is degraded by the collagenase enzyme of the bacterium, and the bacterium can enter the gingival fibroblast, and can survive even at a considerable concentration of antibiotics. In addition, the bacterium can enter the gingival epithelial cells and survive for a long time.

In one embodiment of the present invention, the size of the growth inhibition ring was measured after inoculating a disk containing purpurin in a medium coated with poppy mongoose juniperis, and as a result, in the experimental group containing purpurin, And showed that the composition containing furfurin can be used for prevention or improvement of periodontal disease (Table 2).

In addition, in one embodiment of the present invention, the subjects who had gingival inflammation were selected and subjected to clinical tests. As a result, in the experimental group using the furfurin-containing dentifrice, the gingival inflammation-suppressing effect was excellent and the effect was sustained Thus, it was confirmed that a composition containing furfurin can be used for prevention or improvement of periodontal disease including gingivitis (Table 4).

In the present invention, " toothache " refers to a pain in a tooth when eating a sweet food or a very cold or hot food. In general, not only the pain of the tooth itself, but also the periodontal tissue supporting the tooth on the jaw Pain is also included. It usually causes pain when chewing, and the gums are swollen and emit a strong odor. Toothache is slightly different according to the cause disease. Specifically, pain caused by dental caries is not pain at first, but gradually progresses to pain in the deep tooth nerve. When there is impacted tooth, If the tooth is broken or cracked, when it touches cold food or when it bites strongly, the tooth is split and the nerve is stimulated to cause pain. In the case of dental infection, it is painful when cold food is initially exposed, and pain is felt in hot food when it is advanced. When inflammation progresses and dental tissue is dying, there is no cold reaction, no reaction to hot, Of the pain caused by inflammation.

In one embodiment of the present invention, the PGE2 inhibitory effect, known as pain and inflammation markers, was examined. As a result, the test group containing purpurin showed a concentration-dependent inhibitory effect on PGE2, It can be used for improvement purposes (FIG. 1).

In the present invention, " syringe " refers to dentin hypersensitive dentine, and silent refers to dentine hyperesthesia. This symptom is felt when the dentin part of the exposed tooth touches cold air or irritating food or the like, and it shows symptoms in 60 ~ 98% of adults with periodontal disease. This symptom may be caused by incorrect brushing habits, excessive occlusal force, dissolution of the tooth due to acid dissolution, gum breakage, poor oral hygiene, periodontal treatment, restorative treatment, . As the root cause of the symptoms is acne, many tubules present in the dentin of the teeth are exposed to the outside. By exposure, all the stimuli are transmitted to the nerve in the dentine as they are, and they react more sensitively to the same stimuli than usual. have. Symptoms can range from mild symptoms to intense and persistent pain, and due to the nature of teeth, the use of painkillers and anti-inflammatory agents is not a fundamental solution to the symptoms. Symptoms may occur throughout the tooth, either in the maxilla or mandible, or even in certain areas, such as the right or left side. The most common site is the canine, the small molar area, and the most severe pain area is the cervical area where more than 90% is the boundary between the gum and the tooth.

In one embodiment of the present invention, a test subject having a dentin hypersensitive tooth was selected and subjected to clinical tests. As a result, in the case of the test group using the toothpaste containing the purpurin, (Table 6). ≪ tb > < TABLE >

In the present invention, " bad breath " refers to the odor derived from the oral cavity and adjacent organs, and 85 to 90% of the bad breath is derived from the oral cavity, in particular from the back of the tongue. The major component of halitosis is volatile sulfur compounds, in which 90% of total volatile sulfur compounds are methyl mercaptan and dimethyl sulfide produced from hydrogen sulfide and methionine produced from cysteine. These components are produced mainly by protein enzymes secreted by anaerobic bacteria, and the back of the tongue is the most important habitat. This area is not well cleansed by saliva, and there are many small depressions, making it a place where bacteria live on. The formation of volatile sulfur compounds by anaerobic bacteria is the most important cause of halitosis, but it is also caused by oral diseases such as dental caries, periodontitis and dry mouth. Many types of anaerobic bacteria are involved in generating bad breath, and a non-limiting example of causative organisms of halitosis is Porphyromonas gingivalis , which secretes many species and large amounts of enzymes.

In one embodiment of the present invention, clinical trials were conducted on subjects who did not have dental caries, and as a result, the test group using the dentifrice containing the furfurin showed excellent odor removal effect and the composition containing furfurin Can be used for preventing or improving bad breath (Table 7).

The quasi-drug composition of the present invention may include quasi-drugs for oral use. The components contained in the quasi-drug composition of the present invention may contain, as an active ingredient, the components commonly used in oral quasi-drug compositions in addition to the above-mentioned effective ingredients, and examples thereof include abrasives, wetting agents, binders, foaming agents, sweeteners, preservatives, A coloring agent, a solvent, a brightener, a solubilizing agent or a pH adjusting agent.

The oral quasi-drug composition of the present invention may be prepared in any form conventionally produced in the art, and examples thereof include toothpaste, mouthwash, mouthwash, gum, candy, oral spray, oral ointment, , Mouthwash and gum massage cream, but are not limited thereto.

As one example, when the quasi-drug composition for oral use of the present invention is a toothpaste formulation, it may contain a wetting agent, an abrasive, a binder, a foaming agent, a flavoring agent, a sweetening agent, a coloring agent, a preservative, a pharmaceutical composition, a solvent and a pH adjusting agent.

The wetting agent is used to prevent the toothpaste from hardening in the air and to make the powder of the toothpaste composition paste-like and prevent the toothpaste from hardening in the air. The wetting agent may be used alone or in combination of two or more kinds of glycerin, sorbitol, propylene glycol, polyethylene glycol, %, Specifically 10 to 50% by weight.

The foaming agent is a surfactant which diffuses the toothpaste into the oral cavity to enhance the cleaning effect and acts as a surfactant to clean the oral contamination. It is also possible to use a surfactant such as sodium lauryl sulfate, sodium lauryl sarcosinate, sodium alkylsulfosuccinate, Or 0.5 to 10% by weight, specifically 0.5 to 5% by weight, based on the total weight of the composition.

The binder is to prevent the separation of the powder and the liquid component in the dentifrice, and may be a combination of a cellulose derivative such as sodium carboxymethylcellulose, methylcellulose or hydroxypropylcellulose, sodium alginate, carrageenan or xanthan gum alone or in combination 0.1 to 5% by weight, specifically 0.3 to 2% by weight, of the total weight of the composition may be used.

The abrasive is used to remove calcium oxide (CaCO ₃ ), dicalcium phosphate (CaHPO ₄ , CaHPO ₄ 2H ₂ O), silicic anhydride (SiO ₂ ) ₂ H ₂ O), aluminum hydroxide (Al (OH) ₃ ), potassium pyrophosphate, magnesium carbonate, etc., in an amount of 1 to 60% by weight, specifically 10 to 50% by weight, Can be used.

The flavor agent is used for imparting an exhilarating feeling and smell to the toothpaste to improve the sensation of use. The flavor agent is selected from the group consisting of peppermint oil, spearmint oil, menthol, etc. in an amount of 1 to 60% by weight, 5% by weight can be used.

The sweetener is used to remove an unpleasant taste or raw material from a toothpaste raw material and to improve a cooling sensation. The sweetener is used in an amount of 1 to 60% by weight of the total composition of saccharin acid, aspartame, xylitol, licorice acid, 0.01 to 5% by weight can be used.

The active ingredient is for the prevention of periodontal disease, prevention of periodontal disease, prevention of toothache, prevention of acne, removal of bad breath, and the like, and it can be used as fluoride, zinc chloride, chlorhexidine, aminocaproic acid, tranexamic acid, cetylpyridinium chloride, Triclosanic acid, tocopherol acetate, sodium fluorophosphate, and the like, or a mixture of two or more thereof. In the present invention, furfurin can be used as an additional active ingredient.

The oral quasi-drug composition of the present invention may be used singly or in combination, or may be used in combination with other oral quasi drug compositions other than the present invention.

In another aspect of the present invention, there is provided a pharmaceutical composition comprising the above purpurin or a pharmaceutically acceptable salt thereof as an active ingredient. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating at least one oral disease selected from the group consisting of dental caries, periodontal disease (periodontitis or gingivitis), toothache, syrinite and bad breath comprising the above purpurin as an active ingredient Can be provided. Furfurin, oral disease, dental caries, periodontal disease, toothache, syringitis and bad breath are as described above.

The pharmaceutical composition of the present invention may be in the form of tablets, pills, powders, granules, capsules, suspensions, solutions, emulsions, syrups, aerosols, sterilized injection solutions or the like in accordance with a conventional method for preventing and treating oral diseases Formulation is possible.

Solid formulations for oral administration include tablets, pills, powders, granules, capsules, etc. These solid preparations are prepared by mixing at least one excipient, for example, starch, calcium carbonate, sucrose, lactose, . In addition to simple excipients, lubricants such as magnesium stearate and talc may also be used. Liquid preparations for oral administration include suspensions, solutions, emulsions, syrups and the like. In addition to water and liquid paraffin which are commonly used simple diluents, various excipients such as wetting agents, sweeteners, fragrances, Can be used.

Formulations for parenteral administration may include sterilized aqueous solutions, non-aqueous solutions, suspensions, emulsions, freeze-dried preparations, suppositories, and the like. Examples of the non-aqueous solvent and the suspending agent include vegetable oils such as propylene glycol, polyethylene glycol and olive oil, injectable esters such as ethyl oleate, and the like.

In addition, the pharmaceutical composition of the present invention may further comprise a carrier, an excipient or a diluent. Examples of the carrier, excipient or diluent include lactose, textol, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose, Mineral oil such as propyl methylcellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and silicon dioxide can be used have.

The specific dosage of the pharmaceutical composition according to the present invention depends on factors such as the formulation method, the patient's condition and body weight, the patient's sex, age, degree of disease, drug type, administration route and period, excretion rate, May be variously selected by those skilled in the art, and the dosage and the number of times do not limit the scope of the present invention in any way.

The pharmaceutical composition of the present invention can be administered to mammals such as rats, mice, livestock, humans, and the like through various routes. All modes of administration may be expected and may be administered, for example, by oral, intravenous, intramuscular or subcutaneous injection.

In another aspect of the present invention, the present invention provides a food composition comprising the furfurin or a pharmaceutically acceptable salt thereof as an active ingredient. More specifically, the present invention relates to a food composition for preventing or improving oral diseases selected from the group consisting of dental caries, periodontal disease (periodontitis or gingivitis), toothache, syringitis and bad breath containing the purpurin as an active ingredient . Furfurin, oral disease, dental caries, periodontal disease, toothache, syringitis and bad breath are as described above. The food composition may be used in the form of a health functional food, but is not limited thereto.

The furfurin or a phytopathologically acceptable salt thereof contained in the food composition of the present invention may be in the form of an animal or plant including furfurin, an extract thereof, a fraction thereof or a processed product thereof. The composition may also include a food-acceptable food-aid additive in addition to the active ingredient.

In the present invention, the term "food-aid additive " means a component that can be added to foods in a supplementary manner, and is appropriately selected and used by those skilled in the art as added to produce health functional foods of each formulation. Examples of food-aid additives include flavors such as various nutrients, vitamins, minerals (electrolytes), synthetic flavors and natural flavors, colorants and fillers, pectic acid and its salts, alginic acid and its salts, organic acids, , a pH adjusting agent, a stabilizer, a preservative, a glycerin, an alcohol, and a carbonating agent used in a carbonated drink. However, the types of the food auxiliary additives of the present invention are not limited by these examples.

A health functional food may be included in the food composition of the present invention. In the present invention, the term "health functional food" refers to a food prepared and processed in the form of tablets, capsules, powders, granules, liquids and rings using raw materials and components having useful functions in the human body. The term "functional" as used herein means that the structure and function of the human body have a beneficial effect on health uses such as controlling nutrients or physiological actions. The health functional food of the present invention can be prepared by a method commonly used in the art and can be prepared by adding raw materials and ingredients that are conventionally added in the art. In addition, the formulations of the above health functional foods may also be manufactured without limitations as long as they are acceptable as health functional foods. The food composition of the present invention can be manufactured in various formulations, and unlike general pharmaceuticals, it has an advantage of being free from side effects that may occur when a food is used as a raw material for a long period of time, and is excellent in portability. Health functional foods can be ingested as an adjunct to prevent or improve oral diseases.

The form of the health functional food of the present invention is not limited, and may include all foods in the conventional meaning, and may be used in combination with terms known in the art such as functional foods. In addition, the health functional food of the present invention can be prepared by mixing other suitable auxiliary ingredients, which may be included in food, according to the selection of a person skilled in the art, and known additives. Examples of foods that can be added include dairy products, such as meat, sausage, bread, chocolates, candies, snacks, confectionery, pizza, ramen, other noodles, gums, ice cream, various soups, drinks, tea, Vitamin complex, and the like, and can be prepared by adding to the juice, tea, jelly, juice and the like prepared by using purpurin as a main component according to the present invention. It also includes foods used as feed for animals.

The quasi-drug composition comprising the purpurin of the present invention or a pharmaceutically acceptable salt thereof as an active ingredient is excellent in preventing or improving oral diseases. Specifically, the composition of the present invention is excellent in antimicrobial activity against dental caries and periodontal disease-causing bacteria, and inhibits the pain and inflammation marker PGE2 in a concentration-dependent manner, and has a gingivitis formation inhibitory effect, And is highly utilized as a quasi-drug composition for preventing or ameliorating at least one oral disease selected from the group consisting of dental caries, periodontal diseases, toothache, syringitis and bad breath. In addition, the composition comprising the purpurin of the present invention can be used as a pharmaceutical composition and a food composition.

BRIEF DESCRIPTION OF THE DRAWINGS The accompanying drawings, which are incorporated in and constitute a part of the specification, illustrate exemplary embodiments of the invention and, together with the description of the invention, It should not be construed as limited.
FIG. 1 shows the results of confirming the inhibitory effect of PGE2 by treating LPS (control group), LPS and purpurin (experimental group), which are inflammatory stimuli, respectively, in macrophages.

Hereinafter, the constitution and effects of the present invention will be described in more detail with reference to Examples and Experimental Examples. These Examples and Experimental Examples are only for illustrating the present invention, and the scope of the present invention is not limited by these Examples and Experimental Examples.

Experimental Example  One : Dental caries  And antimicrobial effect against periodontitis causing bacteria

Antimicrobial activity tests were conducted to confirm the preventive or therapeutic effect of the furfurin on dental caries and periodontitis. Streptococcus mutans , a representative dental caries-inducing bacterium, and Porphyromonas , a representative bacterium for periodontal disease, gingivalis ) was used for the test of antimicrobial activity.

Each of the oral pathogens was cultivated for 4 to 6 hours in an optimal medium after increasing the activity under the optimal culture conditions shown in Table 1 below. The turbidity of the culture was determined by Macfarland turbidity No. 1. 0.5 (1.5 x 10 ⁸ ), and 0.1 ml of each of the oral pathogens was evenly plated on a plate medium. Then, the paper was inoculated on a sterilized paper disk (Whatman no. 5 paper, 8 mm diameter) with a concentration of 10 mg / disc of furfurin and absorbed and dried for 1 hour. Then, after culturing at the optimal temperature of each of the oral pathogens for 24 to 48 hours, the size (diameter mm) of the growth inhibition rings was measured. The results are shown in Table 2 below.

Strain Optimum condition Gram stain
(Gram staining) Strain name Temperature badge characteristics Gram (+) Streptococcus mutans 37 BHI Flowable anaerobic Gram (-) Porphyromonas  gingivalis 37 TSA Hemin Menadione Badge Anaerobic

Antifungal Activity of Furfurin against Oral Pathogens Growth inhibition diameter (mm) Streptococcus mutans Porphyromonas gingivalis No treatment - (Growth is not inhibited) - (Growth is not inhibited) Purine purine treatment 10.5 10.0

As shown in Table 2, the groups treated with furfurin had a growth inhibition diameter of not less than 10.0 mm for the two oral pathogens, compared to the non-furfurin-treated group, and the streptococcus mutans And < RTI ID = 0.0 > Porphyromonas jinx valis. ≪ / RTI > Therefore, it has been found that furfurin can be used for preventing or treating dental caries or periodontal disease.

Experimental Example  2: Gingivitis formation inhibitory effect

In order to confirm the preventive or therapeutic effect of furfurin on gingivitis, experimental groups were selected and clinical experiments were conducted.

First, there are used carboxymethylcellulose sodium, sodium lauryl sulfate, glycerin, colloidal silicon dioxide, silica, sodium cocoyl sulfate, sodium dodecanoate, sweetener, flavoring agent, coloring agent, To prepare a control toothpaste, and the test toothpaste was prepared so that the control toothpaste contained 0.01% by weight of the purpurin.

In order to select the subjects, a thorough oral examination was performed on 30 patients of gingival inflammation without dentition and between 30 and 50 years of age at 10-year intervals according to gender. After the screening, 60 patients were divided into two groups.

Specifically, the test subjects were divided into a control group and an experimental group, and the control group was instructed to use the prepared control toothpaste three times a day before sleeping 2 hours after the meal, and the experimental group was used three times a day . Thereafter, the initial gingival index was scored and the oral gingivitis was scored at 1 week, 1 month, 3 months and 6 months after the control toothpaste was prepared and the experimental toothpaste was used in the experimental group. Gingivitis index was examined. The method of measuring the gingival index was performed by inserting a periodontal probe into the gingival fissure, burning the circumference of each tooth without applying any force, measuring the bleeding state after 30 seconds, The scores were recorded according to the results, and the results are shown in Table 4.

Gingivitis index standard score Contents 0 point No bleeding state 1 point Normal bleeding state 2 points Hemorrhage 3 points Triangle Bleeding 4 points Gingival hemorrhage

Gingival inflammation inhibitory effect time
Control group Experimental group 0 weeks 1.06 1.05 1 week 1.58 1.05 1 month 2.64 1.07 3 months 2.73 1.08 6 months 2.85 1.09

As shown in Table 4, when compared to the control group, the experimental group using the furfurin-containing toothpaste maintained the normal bleeding state even after 6 months, and the gingival inflammation suppression effect was maintained. Therefore, it has been found that furfurin can be used for preventing or treating gingivitis.

Experimental Example  3: Pain and inflammation Marker Inn PGE2  Inhibitory effect

In order to confirm the preventive or therapeutic effect of furfurin on toothache, PGE2 inhibitory effect, known as pain and inflammation marker, was confirmed.

First, macrophages were inoculated in DMEM medium containing 10% FBS at a concentration of 1.5 × 10 ⁵ cells / ml and cultured in a 24-well plate at 37 ° C and 5% CO ₂ for 24 hours. The PGE2 ELISA assay kit (Thermo SCIENTIFIC) was purchased for 24 h after treatment with 1 μg / ml LPS and furfurin for the induction of inflammation induction stimuli. The supernatant was used for the PGE2 inhibition (Fig. 1).

As shown in FIG. 1, when the concentration of 0.2 ppm of furfurin was about 45% and that of 2 ppm of furfurin was about 62%, PGE 2 was inhibited as compared with the group treated with LPS alone as shown in FIG. Thus, it has been found that furfurin can be used for preventing or treating toothache.

Experimental Example  4 : Cyrin  Inhibitory effect

In order to confirm the preventive or therapeutic effect of the purine purine, the subjects were selected and the clinical tests were conducted. The control toothpaste and the experimental toothpaste used in the clinical experiment were prepared in the same manner as the toothpaste of Experimental Example 2, respectively.

The subjects were 40 volunteers who agreed to participate in this experiment as dentin hypersensitive teeth, and 80 teeth were used for the total test. Of the subjects, 20 were male and 20 were female and the ages ranged from 20 to 50 years. The subjects were not allowed to know the contents of toothpaste, and the total duration of the experiment was 2 weeks.

The experiment was performed by measuring the response of the subject after applying the temperature stimulus. Before the experiment, the dentin hypersensitivity areas of dentin hypersensitivity teeth of each subject were checked in advance, and cold water of about 5 ° C was dropped on the syringe area of the teeth with a syringe. The teeth were rated according to the criteria shown in Table 5, The control toothpaste was used in the experimental group, and the toothpaste of the test group was used three times a day for two weeks. After about two weeks, cold water of about 5 ° C was dropped on the syringe and evaluated. Statistical analysis was performed using a paired Student's t-test before and two weeks after the experiment, and the response score after two weeks to the temperature stimulation is shown in Table 6 below.

Evaluation criteria of subjects after stimulation score Contents 0 point There is no sense of inconvenience. 1 point Somewhat uncomfortable or seiri. 2 points It is a lot. 3 points pain.

Degree of inhibition time
Control group Experimental group 0 weeks 2.14 ± 0.12 2.14 ± 0.17 2 weeks 2.14 ± 0.23 1.81 0.20 p > 0.05 * p < 0.05

※ p> 0.05: 95% reliability, no statistically significant difference. * p <0.05: 95% confidence, statistically significant difference.

As shown in Table 6, in the test group using the furfurin-containing toothpaste, the syringe phenomenon was suppressed after 2 weeks as compared with the control group. Therefore, it has been found that furfurin can be used for the purpose of preventing or treating syringitis.

Experimental Example  5: Bad breath removal effect

In order to confirm the effect of preventing or treating bad breath of purpurin, clinical subjects were selected and the control toothpaste and the experimental toothpaste used in the clinical experiment were prepared in the same manner as the toothpaste of Experimental Example 2, respectively.

Fifty men and women without dental caries were selected as subjects and cross-over tests were performed on the toothpaste of the control group and the toothpaste of the experimental group. The commercially available garlic powder was dispersed in water, allowed to stand for 24 hours, and diluted so that the measured value of halimeter was 700 ppb or more. The diluted solution was used as a source of bad breath. The subjects were gagged with 15 ml of garlic min diluted solution for 30 seconds and after 1 minute, the degree of halitosis was measured with a halimeter, then the control group was used the control toothpaste and the experimental group was used for the toothpaste for 30 seconds to 1 minute . After 1 minute, 5 minutes, and 30 minutes after brushing, the degree of halitosis was measured with a halimeter to measure the persistence of halitosis suppression. The results are shown in Table 7 below.

Bad breath removal effect time
Control group Experimental group 1 minute 53.9% 95.1% 5 minutes 44.1% 88.0% 30 minutes 39.9% 85.4%

As shown in Table 7, in the experimental group using toothpaste containing furfurin, about 95% of the odor was removed after the tooth brushing, and the odor removal rate was about 85% even after 30 minutes after the tooth brushing, The removal efficiency was much better than the control group. It has been found that furfurin can be used to prevent or treat halitosis.

Claims (14)

A quasi-drug composition for preventing or ameliorating oral diseases comprising, as an active ingredient, furfurin (1,2,4-trihydroxyanthraquinone, purpurin) or a pharmaceutically acceptable salt thereof.
The quasi-drug composition according to claim 1, wherein the oral disease is dental caries.
3. The quasi-drug composition according to claim 2, wherein the dental caries is caused by Streptococcus mutans .
The quasi-drug composition according to claim 1, wherein the oral disease is periodontal disease.
The quasi-drug composition according to claim 4, wherein the periodontal disease is periodontitis or gingivitis.
The quasi-drug composition according to claim 4, wherein the periodontal disease is caused by Porphyromonas gingivalis .
The quasi-drug composition according to claim 1, wherein the oral disease is toothache.
The quasi-drug composition according to claim 1, wherein the oral disease is psoriasis.
The quasi-drug composition according to claim 1, wherein the oral disease is halitosis.
The quasi-drug composition according to claim 1, wherein the quasi-drug is oral.
The composition according to claim 10, wherein the formulation of the quasi-drug composition is one or more formulations selected from the group consisting of toothpaste, mouthwash, mouthwash, gum, candy, oral spray, oral ointment, oral varnish, mouthwash, Lt; / RTI &gt; composition.
A pharmaceutical composition for preventing or treating oral diseases, which comprises 1, 2, 4-trihydroxyanthraquinone, purpurin or a pharmaceutically acceptable salt thereof as an active ingredient.
(1, 2, 4-trihydroxyanthraquinone, purpurin) or a pharmaceutically acceptable salt thereof as an active ingredient.
An oral composition comprising 1, 2, 4-trihydroxyanthraquinone, purpurin or an acceptable salt thereof as an active ingredient.

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