WO2016080666A2 - Composition for preventing or treating dental caries and periodontal disease, containing extract of ambrosia trifida l. or fraction thereof as active ingredient - Google Patents

Abstract

The present invention relates to: an antimicrobial composition for Streptococcus mutans or periodontitis bacteria, containing an extract of Ambrosia trifida L. or fractions thereof as an active ingredient; a pharmaceutical composition for preventing or treating dental caries or periodontal disease, containing an extract of Ambrosia trifida L. or fractions thereof as an active ingredient; and a health functional food composition for preventing or ameliorating dental caries or periodontal disease, containing an extract of Ambrosia trifida L. or fractions thereof as an active ingredient.

Description

A composition for preventing or treating tooth decay and periodontal disease, which comprises maple leaf extract or fractions thereof as an active ingredient

The present invention relates to a composition for preventing or treating tooth decay and periodontal disease containing maple leaf ragweed extract or fractions thereof as an active ingredient, and more specifically, cavities or periodontitis bacterium containing maple leaf ragweed extract or fractions thereof as an active ingredient. Pharmaceutical composition for the prevention or treatment of tooth decay or periodontal disease containing as an active ingredient antimicrobial composition, maple leaf ragweed extract or fractions thereof Or to a health functional food composition for improvement.

Tooth decay means that the tooth eats insects and the hard tissue of the tooth is eroded and is a symptom of deficiency, also known as caries. Tooth decay is an infectious bacterial disease that causes pain that dissolves and destroys some of the hard calcified tissue of the tooth and eventually loses it, the most common periodontal disease.

Periodontitis is an inflammation of the supporting tissues surrounding the teeth and is a chronic inflammatory disease caused by bacteria and toxins in the microbial plaque, and the periodontal tissue supporting the teeth is gradually destroyed, which causes the teeth to shake and finally fall out. Periodontitis is an idiom and is often referred to as flavor, and it is also called periodontal disease or periodontal disease. When periodontitis occurs, the gums settle down and the roots of the teeth appear, causing the symptom.

Various oral diseases, including dental caries, gingivitis and periodontitis, can be caused by a variety of causes. The causes can be broadly divided into systemic causes and local causes, more important of which are known to be local causes. The most important local cause is bacteria that reside in the oral cavity, ie pathogenic microorganisms.

In the human oral cavity, up to now, about 300 kinds of microorganisms are known to reside on the tooth surface, between the teeth and gums of the root portion, the surface of the tongue, and the presence of these microorganisms is normal when proper oral hygiene activities are performed. It can be called a phenomenon. However, when proper oral hygiene activity is not performed, various oral diseases such as caries, bad breath, gingivitis or periodontal disease may be caused by pathogenic microorganisms among the above-mentioned microorganisms, and severe teeth may be lost.

More specifically, the pathogenic microorganisms resident in the oral cavity attach to the tooth surface, and after a few hours, they form a bacterial community called plaque and multiply, and initially the pathogenic microorganisms adhere to the surface of the upper teeth. By forming plaque, but gradually progressing, plaque is also formed on the tooth surface under the gingiva. When the plaque is formed on the tooth surface, the pathogenic microorganisms produce an acid by using sugars in the oral cavity, and the acid can cause tooth decay by demineralizing the mineral that is the main component of the tooth.

Microorganisms that play the most important role in inducing oral diseases as described above include Streptococcus mutans and Porphyromonas gingivalis . In particular, Streptococcus mutans is a causative agent of caries, and causes various oral diseases.

Conventionally, various kinds of antimicrobial agents including antibiotics having bactericidal and bacteriostatic effects on the microorganisms have been developed as inhibitors and treatments for tooth decay, periodontal disease or gingivitis. Conventionally used materials include compounds containing fluorine and chlorine, such as sodium copper chlorophyllin, sodium fluoride or benzethonium chloride, benzoic aicd, and the like. Aromatic carboxylic acid, allantoin, tocopherol acetate, antiplasmin or antibiotic, and the like. However, in the case of the composite containing fluorine and chlorine components, the safety of the human body is a problem, and in the case of antibiotics, it may cause systemic side effects on the whole body including diarrhea and vomiting, and the appearance of resistant bacteria in the oral cavity and Long-term use is difficult because it can cause the myoclosis has the disadvantage that can be used only as a therapeutic agent. In addition, in the case of treatment by surgery or mechanical therapy, there is a disadvantage that the treatment is not easy.

Therefore, compared to surgery or mechanical therapy, the prevention or treatment is easier, and even after long-term use, there are no problems of resistance and stability like antibiotics, and no side effects like fluorine and chlorine-containing compounds. It is urgent to develop a composition for preventing or treating oral diseases derived from natural materials, and there is an increasing demand to develop compositions capable of preventing or treating oral diseases from natural materials.

On the other hand, Korean Patent No. 1280868 discloses a pharmaceutical composition and food composition for preventing or treating dental caries and periodontal disease containing yacon extract as an active ingredient, and Korean Patent Publication No. 2011-0103267 discloses 'gold leaf extract' Oral composition for the prevention and treatment of tooth decay or periodontitis as an active ingredient 'is disclosed, but there is no description about the composition for caries and periodontal disease prevention or treatment containing the maple leaf extract or fractions thereof of the present invention as an active ingredient. .

The present invention was derived by the above-mentioned demands, and the present inventors confirmed that the methanol extract and its fractions of the maple leaf ragweed showed antimicrobial activity against Streptococcus mutans and the periodontal bacterium Porphyromonas gingivalis The present invention has been completed.

In order to solve the above problems, the present invention provides an antimicrobial composition against cavities or periodontitis bacteria containing maple leaf ragweed extract or fractions thereof as an active ingredient.

In addition, the present invention provides a pharmaceutical composition for the prevention or treatment of caries or periodontal disease containing maple leaf botanical extract or fractions thereof as an active ingredient.

In another aspect, the present invention provides a health functional food composition for the prevention or improvement of tooth decay or periodontal disease containing maple leaf botanical extract or fractions thereof as an active ingredient.

The composition containing the extract of the maple leaf ragweed extract or the extract of the maple leaf ragweed extract according to the present invention shows excellent antimicrobial activity against Streptococcus mutans bacteria and periodontitis Porphyromonas gingivalis bacteria It can be used as a pharmaceutical composition for caries and periodontal disease prevention or treatment such as disease prevention, removal of tartar and sterilization of caries, and health functional food composition for preventing or improving caries and periodontal disease.

In addition, the maple leaf pigweed extract or fractions thereof of the present invention is to utilize the discarded plants, it is possible to increase the utilization of plant resources.

1 is a result showing the growth inhibition rate of the Streptococcus mutans bacteria of the methanol extract of the maple leaf ragweed and its fractions. MeOH ex, methanol extract; BuOH fr, butanol fraction of methanol extract; CHCl ₃ fr, chloroform fraction of methanol extract; EtOAc fr, ethyl acetate fraction of methanol extract; Hexane fr, hexane fraction of methanol extract.

Figure 2 is a result showing the growth inhibition rate for Porphyromonas gingivalis bacteria of methanol extract and its fractions of maple leaf ragweed. MeOH ex, methanol extract; BuOH fr, butanol fraction of methanol extract; CHCl ₃ fr, chloroform fraction of methanol extract; EtOAc fr, ethyl acetate fraction of methanol extract; Hexane fr, hexane fraction of methanol extract.

In order to achieve the object of the present invention, the present invention provides an antimicrobial composition against cavities or periodontitis bacteria containing maple leaf ragweed extract or fractions thereof as an active ingredient.

In the antimicrobial composition according to the embodiment of the present invention, the caries may be Streptococcus mutans , Streptococcus sobrinus , Lactobacillus salivarius , etc. Streptococcus mutans ( Streptococcus mutans ) may be, but not limited to, the periodontal bacterium is Porphyromonas gingivalis , Tannerella forsythia , Fusobacterium nucleotum nucleatum ) and Actinobacillus actinomycetemcomitans , and the like, and preferably Porphyromonas gingivalis , but is not limited thereto.

In the antimicrobial composition according to the embodiment of the present invention, the maple leaf pigweed extract may be an extract such as a leaf, stem or inflorescence which is the ground portion of the plant, and preferably may be an extract using a leaf or inflorescence region, It is not limited.

In addition, the maple leaf ragweed extract may be water, methanol, ethanol, propanol, butanol or a mixed solvent extract of dried maple leaf ragweed, preferably the methanol extract of dried maple leaf ragweed, specifically After using dried soybeans, dried 2 ~ 3cm of maple leaf, dried at 2 ~ 4 days at a temperature of 30 ~ 50 ℃, 75 ~ 85% of methanol is added to 400 ~ 600g dry weight, and extracted using an ultrasonic device. It may be prepared by.

In the antimicrobial composition according to the embodiment of the present invention, the fraction of the maple leaf ragweed extract is mixed with 400 to 600 g of dried maple leaf ragweed, 75-85% methanol, extracted using an ultrasonic device, filtered and then vacuumed. Methanol extract from which the solvent is removed in the state is dissolved in water, and then obtained by adding chloroform or hexane (n-hexane).

The present invention also provides a pharmaceutical composition for the prevention or treatment of caries or periodontal disease, containing the maple leaf ragweed extract or a fraction thereof as an active ingredient.

The term 'periodontal disease' is often referred to as flavour, and is divided into gingivitis and periodontitis depending on the severity of the disease. It is a relatively light and fast-recovering form of periodontal disease that is limited to the gums, ie soft tissues, is called gingivitis, and when this inflammation progresses to the gums and around the gum bone, it is called periodontitis.

Extracts or fractions of the invention may comprise suitable carriers, excipients and diluents conventionally used in the manufacture of pharmaceutical compositions.

Pharmaceutical dosage forms of the extracts or fractions 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 collection.

The extracts or fractions according to the invention are each formulated in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, oral formulations, external preparations, suppositories, and sterile injectable solutions according to conventional methods. Can be used. Carriers, excipients and diluents that may be included in the extract or fraction include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose And various compounds or mixtures including methyl cellulose, microcrystalline cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, mineral oil and the like. When formulated, diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrating agents, and surfactants are usually used. Solid preparations for oral administration include tablets, pills, powders, granules, capsules and the like, and such solid preparations may contain at least one excipient such as starch, calcium carbonate and sucrose in the extract or fraction. (sucrose), lactose (lactose), gelatin, etc. are mixed and prepared. In addition to simple excipients, lubricants such as magnesium stearate and talc are also used. Oral liquid preparations include suspensions, solvents, emulsions, and syrups, and may include various excipients, such as wetting agents, sweeteners, fragrances, and preservatives, in addition to commonly used simple diluents such as water and liquid paraffin. . Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized preparations, suppositories. As the non-aqueous solvent and suspending agent, propylene glycol, polyethylene glycol, vegetable oil such as olive oil, injectable ester such as ethyl oleate and the like can be used. As the base of the suppository, witepsol, macrogol, tween 60, cacao butter, laurin butter, glycerogelatin and the like can be used.

Preferred dosages of the extracts or fractions of the present invention vary depending on the condition and weight of the patient, the extent of the disease, the form of the drug, the route of administration and the duration, and may be appropriately selected by those skilled in the art. However, for the desired effect, the extract or fraction of the present invention is preferably administered at 0.0001 to 100 mg / kg, preferably at 0.001 to 100 mg / kg. Administration may be administered once a day or may be divided several times. The dosage does not limit the scope of the invention in any aspect.

Extracts or fractions of the invention can be administered to a variety of routes to mammals, such as mice, mice, livestock, humans. All modes of administration can be expected, for example oral, by injection.

In another aspect, the present invention provides a health functional food composition for the prevention or improvement of tooth decay or periodontal disease containing maple leaf botanical extract or fractions thereof as an active ingredient.

The extract of the maple leaf ragweed or the fractions thereof of the present invention shows excellent antimicrobial activity against the cavities Streptococcus mutans and periodontitis Porphyromonas gingivalis, so it is useful for the prevention or improvement of periodontal diseases such as caries or gingivitis. Can be used.

When the extract or fraction of the present invention is used as a food additive, the extract or fraction may be added as it is or used with other food or food ingredients, and may be appropriately used according to a conventional method. The mixed amount of the active ingredient can be suitably determined according to the purpose of use (prevention, health or therapeutic treatment). Generally, in the preparation of foods or beverages, the extracts or fractions of the invention are added in an amount of up to 15 parts by weight, preferably up to 10 parts by weight relative to the raw materials. However, in the case of long-term intake for health and hygiene or health control, the amount may be below the above range, and the active ingredient may be used in an amount above the above range because there is no problem in terms of safety. .

There is no particular limitation on the kind of food. Examples of the food to which the extract or fraction may be added include meat, sausage, bread, chocolate, candy, snacks, confectionary, pizza, ramen, other noodles, gums, dairy products including ice cream, various soups, drinks, teas, Drinks, alcoholic beverages and vitamin complexes, and the like includes all of the dietary supplements in the conventional sense.

Hereinafter, the present invention will be described in detail by way of examples. However, the following examples are merely to illustrate the invention, but the content of the present invention is not limited to the following examples.

Experiment method

Preparation Example 1 Preparation of Maple Leaf Pigweed Extract

Extracts of Ambrosia trifida were used above the ground of maple leaf, using leaves, stems and inflorescences. The leaves and inflorescences of the maple leaf, identified by the plant taxonomy, were cut evenly to 2.54 cm using small green beans, and dried in a drying oven at 40 ° C. for 3 days. Using a plant dry weight of about 500 g, the resultant was extracted with an ultrasonic device in 80% methanol, and these liquids were filtered through a membrane filter (0.2 µm), and then the solvent was removed under vacuum to leave a methanol extract. Through this process, the cellulose and the like of the components of the maple leaf ragweed are filtered through the purification process, the maple leaf vinegar extract is a methanol extract mainly containing a trace component of the maple leaf ragweed. All solvents used were analytical grade, purchased from Sigma-Aldrich (USA) or Merck (USA).

Preparation Example 2 Preparation of Fractions of Maple Leaf Pigweed Extract

The fractions of the maple leaf ragweed extract were dissolved in the methanol leaf ragweed methanol extract, and then fractionated using butanol, chloroform (CHCl ₃ ), ethyl acetate or hexane (n-hexane). The fractionated sample was passed through a membrane filter (0.2 μm) before freeze drying and the solvent was removed in vacuo leaving only each fraction. These fractions were stored until use in a -20 ° C. freezer. All solvents used were analytical grade, purchased from Sigma-Aldrich (USA) or Merck (USA).

Oral Pathogen Growth Inhibition Assay

The antifungal activity of the extracts and the fractions of Maple Leaf Pigweed extract and fractions were investigated.

Briefly, 1 × 10 ⁶ cfu / ml of Streptococcus mutans UA159 (ATCC 700610) or Porphyromonas gingivalis W83 (ATCC BAA-1703), which are the decay causative organisms, were prepared in 96-well plates, respectively. Methanol extract of maple leaf was treated at concentrations of 0.2 and 0.6 mg / ml, and maple leaf fractions were treated to final concentrations of 0.008, 0.04 and 0.2 mg / ml, respectively. Then, after maintaining the anaerobic state for 24 hours at 37 ℃, the growth inhibition rate of oral pathogens was analyzed.

Example 1 Determination of Antimicrobial Activity against Caries Bacteria of Maple Leaf Porcine Extract and Fractions

The antimicrobial activity of the methanol extract of maple leaf and extracts of the fraction against caries was confirmed in the methanol extract of maple leaf and hexane fraction (FIG. 1). Butanol, chloroform and ethyl acetate fractions showed no antimicrobial activity against caries, while the hexane fraction showed 50% growth inhibition at 0.04 mg / ml. The growth inhibition was 50% at the concentration of.

Example 2 Determination of Antimicrobial Activity against Periodontitis Bacteria of Maple Leaf Pigweed Extract and Fractions

The antimicrobial activity of methanol extract and fractions of maple leaf on the periodontal bacterium was confirmed in the methanol extract of maple leaf and chloroform, ethyl acetate and hexane fraction (Fig. 2). Butanol fractions showed no antimicrobial activity against periodontitis, while chloroform fractions showed growth inhibition of 100% at a concentration of 0.2 mg / ml, and hexane fractions of about 100 at a concentration of 0.04 mg / ml. Showed percent growth inhibition. The ethyl acetate fraction showed growth inhibition of 50% or more at the concentration of 0.2 mg / ml, and the methanol extract also showed antimicrobial activity against periodontitis although higher concentration than that of the fraction.

Through the above results, it was confirmed that methanol extract and hexane fraction of maple leaf ragweed had antimicrobial activity to both cavities and periodontal bacteria, and chloroform fraction to periodontal bacteria. Through this, it was confirmed that the maple leaf ragweed extract or fractions thereof may be used for the prevention or treatment of caries or periodontal disease.

Claims (7)

1. Antimicrobial composition against cavities or periodontitis which contains maple leaf ( Ambrosia trifida ) extract or fractions thereof as an active ingredient.
2. According to claim 1, wherein the decay bacteria Streptococcus mutans ( Streptococcus mutans ) characterized in that the antimicrobial composition against caries or periodontitis bacteria.
3. According to claim 1, wherein the periodontal bacteria is Porphyromonas gingivalis ( Porphyromonas gingivalis ) antimicrobial composition against caries or periodontitis, characterized in that.
4. The antimicrobial composition of claim 1, wherein the maple leaf ragweed extract is water, methanol, ethanol, propanol, butanol, or a mixed solvent extract of dried maple leaf ragweed.
5. The antimicrobial composition of claim 1, wherein the fraction of the maple leaf ragweed extract is a chloroform or hexane fraction obtained by adding chloroform or hexane (n-hexane) to the maple leaf ragweed methanol extract.
6. Pharmaceutical composition for the prevention or treatment of tooth decay or periodontal disease containing maple leaf botanical extract or fractions thereof as an active ingredient.
7. Health functional food composition for the prevention or improvement of tooth decay or periodontal disease containing maple leaf botanical extract or fractions thereof as an active ingredient.

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