KR20160059605A - Composition for preventing or treating cavity and periodontal disease comprising kaempferol as effective component - Google Patents

Abstract

The present invention relates to: an antimicrobial composition with respect to Streptococcus mutans or Porphyromonas gingivalis, comprising kaempferol or a salt thereof as an active ingredient; a pharmaceutical composition for preventing or treating a cavity or periodontal diseases, comprising kaempferol or a salt thereof as an active ingredient; and a health functional food composition for preventing or alleviating a cavity or periodontal diseases, comprising kaempferol or a salt thereof as an active ingredient.

Description

Technical Field [0001] The present invention relates to a composition for preventing or treating periodontal disease and cavities containing camphorol as an active ingredient,

The present invention relates to a composition for preventing or treating periodontal disease and cavities comprising camphorol as an active ingredient, and more particularly to a composition for preventing or treating periodontal disease or antimicrobial activity against cavities or periodontal bacteria containing kaempferol or a salt thereof as an active ingredient. Composition for preventing or treating periodontal disease, comprising a pharmaceutical composition for preventing or treating periodontal disease or periodontal disease comprising camerol or its salt as an active ingredient and a health functional food composition for preventing or ameliorating tooth decay or periodontal disease comprising camerol or its salt as an active ingredient .

A tooth is a tooth that is worm-wormed. The tooth's hard tissue is eroded and it is called a dental caries. Tooth decay is an infectious bacterial disease that causes part of the hard calcified tissue of the tooth to dissolve and break down and ultimately lose teeth. It is the most common periodontal disease.

Periodontitis is a chronic inflammatory disease caused by bacteria and toxins in the microbial plaque, which is caused by inflammation of the surrounding tissues of the teeth. Periodontal tissue that supports the teeth is gradually destroyed, causing the tooth to shake and eventually fall out. Periodontitis is an idiom and is often referred to as a periodontal disease. It is also called periodontal disease or periodontal disease. When periodontal disease occurs, the gingiva falls and the tooth root appears and the symptoms of syenin appear.

Dental medicine Various oral diseases including tooth decay, gingivitis and periodontal disease can be caused by various causes. The cause is divided into systemic cause and local cause, and the most important cause is local cause. The most important local cause is bacteria that reside in the mouth, that is, pathogenic microorganisms.

It is known in the human oral cavity that about 300 kinds of microorganisms are resident on the surface of the teeth, between the teeth and gums of the root portion, and on the surface of the tongue, and the presence of such microorganisms, Phenomenon. However, if proper oral hygiene activities are not performed, various oral diseases such as tooth decay, halitosis, gingivitis and periodontal disease may be caused by pathogenic microorganisms among the above-mentioned microorganisms, and in severe cases, teeth may be lost.

More specifically, a pathogenic microorganism resident in the oral cavity attaches to the surface of the tooth and forms a bacterial population called a plaque after a few hours. At first, a pathogenic microorganism attaches However, as progressive progression occurs, plaque is formed on the surface of the tooth under the gingiva. When the plaque is formed on the tooth surface, the pathogenic microorganism produces an acid by using the sugar introduced into the oral cavity, and this acid may cause tooth decay by demineralizing the main ingredient of the tooth.

Examples of the microorganisms that play the most important role in inducing oral diseases include Streptococcus mutans , Porphyromonas gingivalis , and the like. In particular, Streptococcus mutans is a causative organ of tooth decay and causes various oral diseases.

Conventionally, various kinds of antimicrobial agents including antibiotics having sterilization and bacteriostatic action against the microorganisms have been developed as inhibitors and remedies for cavity, periodontal disease or gingivitis. Conventional materials include fluorine and chlorine-containing compounds such as sodium copper chlorophyllin, sodium fluoride or benzethonium chloride, benzoic acid, , Allantoin, tocopheryl acetate, antiplasmic agents or antibiotics, and the like. However, in the case of the fluorine-chlorine-containing compound, safety of the human body is problematic. Antibiotics can cause systemic side effects, including diarrhea and vomiting, in the whole body, It is difficult to use it for a long period of time because it can induce homozygosity, so that it can be used only as a therapeutic agent. In addition, in the case of treatment by surgical treatment or mechanical therapy, there is a disadvantage that treatment is not easy.

Therefore, it is easy to prevent or treat as compared with surgical therapy or mechanical therapy, and there is no problem of tolerance or stability such as antibiotics even when used for a long time, and there is no problem of side effects such as a compound containing fluorine and chlorine components There is an urgent need to develop a composition for the prevention or treatment of oral diseases derived from natural materials, and there is an increasing demand for developing a composition capable of preventing or treating oral diseases from natural materials.

Kaempferol is one of the representative components of flavonol, one of the flavonoids, and is widely distributed in flowers or leaves of plants. More than 100 flavonols are already known and three of the most abundant are known: camphorol, quercetin and myricetin. In particular, camphorol has excellent physiological activities such as antioxidant and anti-inflammation, and various effects have been studied and applied to various fields.

On the other hand, Korean Patent No. 1149686 discloses a cosmetic composition for inhibiting sebum containing catechins and camphor components, and Korean Patent No. 1154616 discloses a composition for promoting the production of hyaluronic acid containing camphor and quercetin A composition for preventing or treating periodontal disease or a periodontal disease containing the camphorol of the present invention as an active ingredient has not been disclosed.

SUMMARY OF THE INVENTION The present invention has been made in view of the above-mentioned needs, and the present inventors have found that camphorol is isolated from an extract of American perennial plant and treated with Streptococcus mutans, a carrot, and Porphyromonas gingivalis, Confirming that it exhibits antimicrobial activity against pathogenic bacteria, thus completing the present invention.

In order to solve the above problems, the present invention provides an antimicrobial composition for a decubitus or periodontal bacteria containing kaempferol or a salt thereof as an active ingredient.

In addition, the present invention provides a pharmaceutical composition for preventing or treating cavities or periodontal disease containing camphorol or a salt thereof as an active ingredient.

The present invention also provides a health functional food composition for preventing or ameliorating tooth decay or periodontal disease comprising camphorol or a salt thereof as an active ingredient.

The composition containing the camphorol as an active ingredient according to the present invention exhibits excellent antibacterial activity against Streptococcus mutans bacteria, which are carrot bacteria and Porphyromonas gingivalis bacteria, which are periodontal bacteria, so that they can prevent gum disease, remove gums and sterilize cavities A pharmaceutical composition for the prevention or treatment of periodontal disease and a functional food composition for preventing or ameliorating tooth decay and periodontal disease.

FIG. 1 shows the growth inhibition rates of Streptococcus mutans strains of natural ingredients including camphor, which are present in the United States of America.
FIG. 2 shows the growth inhibition rates of Porphyromonas gingivalis bacteria including natural camphor and other natural ingredients in the United States.

In order to accomplish the object of the present invention, the present invention provides a composition for antimicrobial activity against cavities or periodontitis bacteria containing kaempferol or a salt thereof as an active ingredient.

The camphorol of the present invention can be used as it is or in the form of a pharmaceutically acceptable salt. The salt used in the present invention is not particularly limited as long as it is a pharmaceutically acceptable non-toxic salt. For example, a salt form such as hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid, hydrofluoric acid, hydrobromic acid, acetic acid, tartaric acid, lactic acid, citric acid, fumaric acid, maleic acid, succinic acid, metal sulfonic acid, benzenesulfonic acid, toluenesulfonic acid or naphthalenesulfonic acid .

In the antimicrobial composition according to an embodiment of the present invention, the camphor can be produced by using water and various organic solvents including C1 to C4 lower alcohol such as methanol, ethanol, butanol and the like, ( Phytolacca americana extract and the solvent extract can be isolated from fractions using water and various non-polar solvents including butanol, ethyl acetate, hexane, or chloroform, and most preferably from the ethyl acetate fraction But is not limited thereto.

The US peritoneal extract may be, but is not limited to, an extract using leaves or stem parts of the plant.

In the antimicrobial composition according to an embodiment of the present invention, the above-mentioned cavities may be Streptococcus mutans mutans , Streptococcus sobrinus , and Lactobacillus < RTI ID = 0.0 > salivarius , and the like, preferably Streptococcus mutans , but not limited thereto, the periodontal bacteria may be selected from the group consisting of Porphyromonas gingivalis , Tannerella < RTI ID = 0.0 > forsythia , Fusobacterium nucleatum , Actinobacillus actinomycetemcomitans and the like, preferably Porphyromonas gingivalis . However, it is also possible to use the above- It is not limited.

The present invention also provides a pharmaceutical composition for preventing or treating cavities or periodontal diseases containing camphorol or a pharmaceutically acceptable salt thereof as an active ingredient.

The camphorol of the present invention can be used as it is or in the form of a pharmaceutically acceptable salt. The form of the salt which can be used is as described above.

The term 'periodontal disease' is often referred to as a style, depending on the degree of disease gingivitis (gingivitis) and periodontitis (periodontitis) is divided into. 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.

Compositions comprising the active ingredient of the present invention may comprise suitable carriers, excipients and diluents conventionally used in the manufacture of pharmaceutical compositions.

The pharmaceutical dosage form of the composition containing the active ingredient of the present invention may be used in the form of their pharmaceutically acceptable salts, and may be used alone or in combination with other pharmaceutically active compounds as well as in a suitable combination.

The pharmaceutical composition containing the active ingredient according to the present invention can be administered orally or parenterally in the form of powders, granules, tablets, capsules, oral preparations such as suspensions, emulsions, syrups and aerosols, external preparations, suppositories, Can be used. Examples of carriers, excipients and diluents that may be contained in the composition containing the active ingredient of the present invention include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium A variety of compounds or mixtures including phosphate, calcium silicate, cellulose, methylcellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, . In the case of formulation, a diluent or excipient such as a filler, an extender, a binder, a wetting agent, a disintegrant, or a surfactant is usually used. Solid form preparations for oral administration include tablets, pills, powders, granules, capsules and the like, which may contain at least one excipient such as starch, calcium carbonate, Sucrose, lactose, gelatin and the like. In addition to simple excipients, lubricants such as magnesium stearate and talc are also used. Examples of the liquid preparation for oral use include suspensions, solutions, emulsions, and syrups. In addition to water and liquid paraffin, simple diluents commonly used, various excipients such as wetting agents, sweeteners, fragrances, preservatives and the like may be included . Formulations for parenteral administration include sterilized aqueous solutions, non-aqueous solutions, suspensions, emulsions, freeze-dried preparations, and suppositories. Examples of the suspending agent include propylene glycol, polyethylene glycol, vegetable oil such as olive oil, injectable ester such as ethyl oleate, and the like. As a suppository base, witepsol, macrogol, tween 60, cacao paper, laurin, glycerogelatin and the like can be used.

The preferable dosage of the pharmaceutical composition containing the active ingredient of the present invention varies depending on the condition and body weight of the patient, the degree of disease, the drug form, the administration route and the period, but can be appropriately selected by those skilled in the art. However, for the desired effect, the pharmaceutical composition containing the active ingredient of the present invention is preferably administered at a daily dose of 0.0001 to 100 mg / kg, preferably 0.001 to 100 mg / kg. The administration may be carried out once a day or divided into several times. The dose is not intended to limit the scope of the invention in any way.

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

The present invention also provides a health functional food composition for preventing or ameliorating tooth decay or periodontal disease containing camphorol or a salt thereof as an active ingredient.

The camphorol of the present invention can be used as it is or in the form of a pharmaceutically acceptable salt. The form of the salt which can be used is as described above.

Since the composition containing the active ingredient of the present invention exhibits excellent antimicrobial activity against Streptococcus mutans bacteria, which are carrot bacteria and Porphyromonas gingivalis bacteria, which are periodontal bacteria, it is useful for preventing or improving periodontal diseases such as tooth decay or periodontal disease .

When a health functional food composition comprising the active ingredient of the present invention is used as a food additive, the composition may be added as it is, or may be used together with other food or food ingredients, and may be suitably used according to a conventional method. The amount of the active ingredient to be mixed can be suitably determined according to its intended use (prevention, health or therapeutic treatment). Generally, the composition of the present invention is added in an amount of not more than 15 parts by weight, preferably not more than 10 parts by weight, based on the raw material, when the food or beverage is produced. However, in the case of long-term consumption intended for health and hygiene purposes or for health control purposes, the amount may be less than the above range, and since there is no problem in terms of safety, the active ingredient may be used in an amount exceeding the above range .

There is no particular limitation on the kind of the food. Examples of the foods to which camphorol or its salt can be added include dairy products including meat, sausage, bread, chocolate, candy, snack, confectionery, pizza, ramen and other noodles, gums, ice cream, Tea, a drink, an alcoholic beverage, and a vitamin complex, all of which include health functional foods in a conventional sense.

Hereinafter, the present invention will be described in detail with reference to examples. However, the following examples are illustrative of the present invention, and the present invention is not limited to the following examples.

Experimental Method

Production of American Perilla Extracts and Fractions

The extract of Phytolacca americana used the top part of the American periosteum, and the leaves and stem parts were used. The leaves and stems of the American periosteal plants identified by the plant taxonomist were evenly cut to 2.54 cm by using a cutting blade and then dried in a drying oven at 40 ° C for 3 days. Using a plant weight of about 500 g, 80% methanol was extracted using an ultrasonic apparatus. The liquid was filtered through a membrane filter (0.2 μm), and the solvent was removed in a vacuum to leave a methanol extract. Through this process, the cellulose in the United States of America is filtered through the purification process, and the American artichoke extract becomes a methanol extract mainly containing the trace elements of the United States digit.

The US peritoneal fraction was fractionated by dissolving the US spot methanol extract in water and then using butanol, chloroform (CHCl ₃ ), ethyl acetate or hexane (n-hexane). The fractionated sample was passed through a membrane filter (0.2 μm) before lyophilization and the solvent was removed under vacuum to leave only each fraction. These fractions were stored in a -20 ° C freezer until used. All solvents used were analytical grade, purchased from Sigma-Aldrich (USA) or Merck (USA).

Camphor Roll  Separation and purification

After separating from the ethyl acetate fraction of the U.S.A. and obtaining a specific material obtained from the separated materials by silica gel thin layer chromatography and then drying, pure camelol was obtained by ¹ H-NMR I could confirm.

Inhibition of growth of oral pathogens

The antimicrobial activity of camperol against oral pathogens was examined. First, 1 × 10 ⁶ cfu / ml of Streptococcus mutans UA159 (ATCC 700610) or Porphyromonas gingivalis W83 (ATCC BAA-1703) were prepared on a 96-well plate, respectively . Thereafter, camperol, quercetin, quercetin 3-glucoside, isoqueritrin and ferulic acid were treated at 1, 2, 4 and 8 μg / ml, respectively, and incubated at 37 ° C. After incubation for 24 hours, growth inhibition rates of oral pathogens were analyzed.

Example 1. Measurement of antimicrobial activity of camphorol against periodontitis bacteria and bacillus subtilis

As a result of the test for antimicrobial activity against periodontal bacteria and decidua bacteria of natural ingredients derived from US pertussis, a component having antimicrobial activity against Porphyromonas sp. In addition, growth inhibition against streptococcus mutans, which is a deciduous germ, was confirmed in two components of camphor and quercetin (Fig. 1). In particular, at the concentration of 8 ㎍ / ㎖, camphorol and quercetin showed similar growth inhibition rates, but camphorol showed better antimicrobial activity than quercetin at the concentration of 4 ㎍ / ㎖.

Oral pathogen growth inhibition rate of camphor Growth inhibition rate (%) Camphor concentration S.mutans UA159 P.gingivalis W83 8 mu g / ml 97 ± 4.75 84 ± 5.7 4 / / ml 45 ± 9.47 38 ± 12.94 2 쨉 g / ml 0 0 1 mu g / ml 0 0

Claims (6)

A composition for antimicrobial treatment against decaying bacteria or periodontal bacteria containing kaempferol or a salt thereof as an active ingredient. 2. The method of claim 1, wherein the camphor is a phytolacca americana ). < / RTI > The antimicrobial composition according to claim 1, wherein the decidua is Streptococcus mutans . The antimicrobial composition according to claim 1, wherein the periodontal bacteria is Porphyromonas gingivalis . A pharmaceutical composition for preventing or treating cavities or periodontal diseases containing kaempferol or a salt thereof as an active ingredient. A health functional food composition for preventing or ameliorating tooth decay or periodontal disease containing kaempferol or a salt thereof as an active ingredient.

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