KR20130077128A - Antibacterial composition containing aster incisus fisch extract - Google Patents

Abstract

PURPOSE: An antibacterial composition containing Aster incisus Fisch extract is provided to facilitate the prevention and treatment of disease caused by pathogenic microorganism. CONSTITUTION: An antibacterial pharmaceutical composition consists of Aster incisus Fisch extract as an active ingredient. Alcohol with one to four carbons or the mixture thereof is used for the extraction of the Aster incisus Fisch extract. A pharmaceutical composition for the prevention and treatment of gastric and duodenal disease consists of the Aster incisus Fisch extract as an active ingredient. The gastric and duodenal disease is selected from the group of gastritis, duodenitis, gastric ulcer, duodenal ulcer, gastric adenocarcinoma, gastric lymphoma, and gastric cancer. The group of disease is caused by Helicobacter pylori. Health functional food for preventing and improving gastric and duodenal disease consists of the Aster incisus Fisch extract as an active ingredient. Antibiotics consists of the Aster incisus Fisch extract as an active ingredient.

Description

Antibacterial Composition Containing Sproutweed Extract {Antibacterial Composition Containing Aster incisus Fisch Extract}

The present invention relates to an antimicrobial composition comprising Aster incisus Fisch extract as an active ingredient.

Direct or indirect damage by pathogenic microorganisms causes many economic, environmental and medical problems. Many problems throughout society, including losses due to corruption during the food distribution process in the food industry, human health and environmental pollution from the use of excessive chemical pesticides on crops in the agricultural industry, and the emergence of antibiotic resistant strains due to misuse of antibiotics. Is causing them.

Vancomycin-resistant staphylococcus aureus (VRSA), a highly resistant to vancomycin, known as the last cure for staphylococcus aureus, the most common cause of human infection, was reported for the first time in the world by the Centers for Disease Control in 2002. As a result, the possibility of the spread of so-called super bacteria is very high. This was the first time in Europe that vancomycin resistant enterococcus (VRE) was resistant to vancomycin in 1988, after the problem of methicillin-resistant s. Aureus (MRSA), which is treated only by vancomycin, from the 1970s. Was discovered, and in the late 1990s a new example of antibiotic resistance emerged as a global crisis with the development of vancomycin intermediate-resistant s. Aureus (VISA), reported in Japan, the United States, France and Korea. The development of new antibiotics is urgently needed, showing how severe the resistance problem is (Pfeltz, RF and Wilkinson, BJ 2004. The escalating challenge of vancomycin resistance in Staphylococcus aureus.Drug targets-infect. Disord. 4: 273-294. Levy, SB and Marshall, B. 2004.Antibacterial resistance worldwide: causes, challenges and responses.Nature Med. 10: 122-129.).

Most of the currently used antibiotics are manufactured through chemical synthesis, which is costly and has many limitations such as causing side effects. Therefore, in recent years, research to separate new antimicrobial substances from natural products has been actively conducted. The separation of new antimicrobial substances from natural products should take into account that the antimicrobial spectrum is broad and safe for long term administration without side effects.

In addition, Helicobacter pylori isolated from Marshall's, Warren and Goodwin's gastric mucosa in Australia in 1982 caused hepatitis B, gastric ulcer and duodenal ulcer. It is known as the primary determinant of occurrence. Among the pathogenesis of gastrointestinal and duodenal diseases caused by Helicobacter pylori infection, urease, a urease, is particularly important in inducing inflammation of the stomach. Helicobacter pylori produces urease, which is 6% of the total protein. The urease breaks down urea into ammonia and carbon dioxide, neutralizes the bacterial environment, and protects against gastric mucosa attack. Ammonia itself accumulates directly in the gastric mucosal epithelial cells, causing gastric mucosal damage (Sidebotham RL, et al., J. Clin. Pathol., 44, pp 52-57, 1991). Due to the action of this urease, gastric acid in the gastric lumens flows back down the mucosal layer, which causes gastric inflammation and gastric ulceration. In addition, ammonia itself inhibits the oxygen consumption of the gastric mucosal layer and the ATP production of mitochondria (Tsujii M., et al., Gastroenterology, 102, pp 1881-1888, 1992) and ultimately forms monochloroamine (Hahm KB, et al., Am. J. Gastroenterol). In addition, it has been reported that ROS produce reactive oxygen species, which cause cellular damage and cause chronic inflammation, , 92, pp 1853-1857, 1997).

The transmission of Helicobacter occurs through animals or humans, or through various channels such as carelessness or food in medical practice (Dunn, BE, Cohen, H., and Blaser, MJ (1997).) Clinical Microbiology Reviews, 10 (4 ), 720-7; Kodaira, MS, Escobar, AMU, & Grisi, S. (2002) Revista de Sade Pade Pblica. 36: 356-369), once infected, are not easily eradicated.

Helicobacter pylori is specific to humans and is found mainly in certain places within the stomach, including diseases of the digestive tract such as peptic ulcers (e.g. gastric ulcer or duodenal ulcer), inflammation (e.g. gastritis) (Mucosa-associated lymphoid tissue) is a pathogenic factor in the pathogenesis of a lymphoma or chronic heart disease. At present, studies on the treatment of Helicobacter pylori infection have been actively conducted, and as a treatment method thereof, many reports for the purpose of removal and prevention of recurrence have been reported.

As described above, Helicobacter pylori is a very dangerous microorganism in gastrointestinal diseases, but there is a lack of development of appropriate antibacterial materials using natural materials. Currently, Helicobacter pylori therapies include bismuth, metronidazole, tetracycline or amoxicillin, bismuth, omeparazole, tetracycline or amoxicillin, And metronidazole have been reported. However, it has been pointed out that the appearance of resistant strains by the administration of antibiotics, the permeability of the drug in the stomach, and the reproductive growth of the bacteria whose growth has been suppressed after treatment are pointed out. For this reason, numerous efforts have been made to search for antibacterial substances specific to Helicobacter pylori. In recent years, there has been a growing interest in physiologically active ingredients in plants and their potential for regulating or preventing diseases Has come. Recently, the antimicrobial activity of Helicobacter pylori of various natural products, such as thyme, Chinese tea, Cashew apple, joiner and rhubarb, has been reported, but the research is still insufficient.

In order to solve the problems described above, the present inventors, while continuing to research to separate new antimicrobial substances from natural products, by discovering that the extract Aster incisus Fisch has an excellent antimicrobial effect against pathogenic microorganisms The present invention has been completed.

An object of the present invention is to provide an antimicrobial composition comprising the extract Aster incisus Fisch as an active ingredient.

In order to achieve the above object, the present invention provides a pharmaceutical composition for antimicrobial comprising a wormwood extract as an active ingredient.

In another aspect, the present invention provides an antimicrobial preparation comprising the extract of the wormwood as an active ingredient.

The wormwood extract of the present invention exhibits strong antimicrobial activity against pathogenic microorganisms, and thus can be usefully used for the prevention or treatment of diseases caused by pathogenic bacteria.

Hereinafter, the present invention will be described in more detail.

In one embodiment, the present invention provides a pharmaceutical composition for antimicrobial comprising the extract of the wormwood as an active ingredient.

The wormwood perennial plant is a perennial plant of the flowering plant, the dicotyledon plant, the Asteraceae family, and it is also called the wormwood worm, Korea mugwort worm, buds sprouts, wormwood worm, and wormwood worm. It grows in the humid place of the field, the stem stands straight about 1 to 1.5m and has light and short hairs all over the grass. Root leaves disappear when flowering. Stem leaves alternate, long oval or lanceolate, pointed at the end, narrowed at the bottom, like petiole, split into feathers. Young leaves are eaten, and the whole grass is dried and used as a diuretic.

The term "extract " as used herein refers to an active ingredient isolated from a natural product, that is, a substance exhibiting the desired activity. The extract may be obtained by an extraction process using water, an organic solvent or a mixed solvent thereof, and includes the dry powder thereof or any form formulated using the extract. In addition, the extract also includes a fraction obtained by the extraction through the extraction process.

The wormwood extract according to the present invention can be obtained through the following process. The wormwood is extracted with an organic solvent containing alcohol, ethyl acetate, methylene chloride, methyl ethyl ketone, acetone, methylene chloride or ether and concentrated under reduced pressure. The alcohol may be a lower or higher alcohol and may be a mixture with water.

The wormwood extract of the present invention shows strong antibacterial activity against pathogenic strains including Staphylococcus aureus and Escherichia coli, and shows antibacterial activity against Helicobacter bacteria. The Helicobacter bacteria is not particularly limited and may include all bacteria included in Helicobacter spp., But preferably Helicobacter pylori, Helicobacter canis, Helicobacter cinaedi, Helicobacter cinaedi Helicobacter Helicobacter Helicobacter Helicobacter Helicobacter Helicobacter Helicobacter Helicobacter Helicobacter Helicobacter Helicobacter heilmannii , Helicobacter bilis, Helicobacter pullorum (Helicobacter pullorum) may be selected from.

In another aspect, the present invention provides a pharmaceutical composition for the prevention and treatment of gastrointestinal and duodenal diseases, including the extract of wormwood as an active ingredient.

Since the wormwood extract according to the present invention shows an antimicrobial activity against Helicobacter pylori, it can be usefully used for the prevention and treatment of gastric and duodenal diseases caused by Helicobacter pylori. The gastric and duodenal diseases may include peptic ulcer and gastric cancer, and preferably one or more selected from the group consisting of gastritis, duodenal ulcer, gastric ulcer, duodenal ulcer, gastric cancer, gastric lymphoma and gastric cancer, May be preferably chronic atrophic gastritis. Since the discovery of Helicobacter pylori, it has been reported that Helicobacter pylori is the main cause of gastric and duodenal diseases, and Helicobacter pylori is known to live mainly in the gastric mucosa, specifically epithelial cells and mucosal layer. Accordingly, it is possible to prescribe an excellent substance having excellent antimicrobial activity against Helicobacter pylori which is a causative organism for treating gastric and duodenal diseases.

The pharmaceutical compositions of the present invention can be used in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, oral dosage forms, sterile injectable solutions, suppositories, and transdermal formulations according to conventional methods. have. Carriers, excipients and diluents that may be included in the composition include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, Microcrystalline cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil. If necessary, it is formulated with diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrants, surfactants and the like.

In one embodiment, the pharmaceutical compositions of the present invention may be formulated as a solid preparation for oral administration. Solid form preparations for oral administration include tablets, pills, powders, granules, capsules and the like, which include at least one excipient such as starch, calcium carbonate, sucrose or lactose, gelatin and the like. It is formulated by mixing. In addition to simple excipients, lubricants such as magnesium stearate and talc may also be used.

In another embodiment, the pharmaceutical compositions of the present invention may be formulated into liquid preparations for oral administration. Liquid preparations for oral administration include suspensions, solutions, emulsions, syrups, and the like. In addition to conventional inert diluents (e.g., purified water, ethanol, liquid paraffin), various excipients may be used. Wetting agents, sweetening agents, fragrances, preservatives and the like can be included.

In another embodiment, the pharmaceutical compositions of the present invention may be formulated into preparations for parenteral, preferably intraperitoneal administration. Formulations for parenteral administration include sterilized aqueous solutions, non-aqueous solutions, suspensions, emulsions, freeze-dried preparations, and suppositories. As a sterile aqueous solution, suitable buffer solutions such as Hanks' solution, Ringer's solution, or physically buffered saline can be used.For non-aqueous solvents, suspensions include propylene glycol, polyethylene glycol, olive oil, Same vegetable oils, injectable esters such as ethyloleate, and the like can be used. If desired, preservatives, stabilizers, wetting or emulsifying agents, salts for controlling osmotic pressure and / or buffers may be used. On the other hand, suppositories, such as witepsol, macrogol, tween 61, cacao butter, laurin butter, glycerogelatin, and the like may be used.

Compositions formulated in such a manner can be administered in various amounts, including parenteral or oral (dermal, subcutaneous, intravenous, intramuscular, intraperitoneal) in an effective amount. As used herein, an "effective amount" refers to an amount exhibiting a prophylactic or therapeutic effect when administered to a patient. The dosage of the composition according to the present invention may be appropriately selected depending on the route of administration, subject of administration, age, sex, weight, individual difference and disease state. Preferably, the composition of the present invention may vary the content of the active ingredient according to the degree of disease, preferably 0.1 to 10000 mg / kg / day, more preferably 10 ~ 1000 mg / kg / day of weight It may be administered in an effective amount.

In another aspect, the present invention provides a health functional food for the prevention and improvement of gastric and duodenal diseases, including the extract of the wormwood as an active ingredient.

When the composition of the present invention is used as a food or beverage additive, the wormwood extract may be added as it is, or used together with other food or food ingredients, and may be appropriately used according to a conventional method. The mixed amount of the wormwood extract may be suitably determined according to the purpose of use (prevention, health or therapeutic treatment). In the case of prolonged ingestion for health or health control, the wormwood extract can be taken for a long time because there is no problem in terms of safety.

There is no particular limitation on the kind of the food. Examples of the food to which the substance can be added include meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen, dairy products including other noodles, gum, ice cream, various soups, drinks, tea, and drinks. Alcoholic beverages and vitamin complexes.

The liquid component added in addition to the wormwood extract when formulated into a beverage is not limited to the above, but may contain various flavors or natural carbohydrates, etc. as additional ingredients, as in conventional beverages. Examples of the above-mentioned natural carbohydrates include monosaccharides (e.g. glucose, fructose and the like), disaccharides (e.g. maltose, sucrose and the like) and polysaccharides (e.g. conventional sugars such as dextrin, cyclodextrin and the like), and xylitol Sugar alcohols such as sorbitol and erythritol. The ratio of the natural carbohydrate is generally about 1 to 20 g, preferably about 5 to 12 g per 100 ml of the composition of the present invention. As flavoring agents other than those mentioned above, natural flavoring agents (for example, taumarin, stevia extracts (e.g., rebaudioside A, glycyrrhizin, etc.)) and synthetic flavoring agents (e.g., saccharin, aspartame, etc.) can be used. .

In another embodiment, the food composition of the present invention comprises various nutrients, vitamins, minerals (electrolytes), flavoring agents such as synthetic and natural flavoring agents, colorants and enhancers (cheese, chocolate, etc.), pectic acid and salts thereof, organic acids , Protective colloid thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohols, carbonation agents used in carbonated beverages, and the like. The food composition of the present invention may also contain pulp for the production of fruit and vegetable drinks. These ingredients may be used alone or in combination, and the proportion of such additives may be selected in the range of 10 to 20% by weight, based on the total weight of the composition.

In still another aspect, the present invention provides an antimicrobial preparation comprising the extract of the wormwood as an active ingredient.

Such formulations include, but are not limited to, cosmetics, disinfectants, sterile detergents and food preservatives. In the above cosmetics can be easily prepared according to known methods in the art, including one or more excipients and additives commonly used in the field of manufacturing cosmetic compositions with the extract of the wormwood of the present invention. More specifically, the cosmetics, such as face lotion, cream, essence, cleansing foam and cleansing water, basic cosmetics such as packs, body oil, etc., color cosmetics such as foundation, lipstick, mascara and makeup base, shampoo, rinse, hair conditioner And hair products such as hair gels, soaps, and the like. Preferably, the cosmetic composition comprising the wormwood extract of the present invention can be used to treat or prevent acne. Therefore, the cosmetic composition of the present invention further comprises a skin exfoliating agent such as plant-derived protease and microorganism-derived protease, such as papain and bromelain, which can improve the therapeutic effect of acne. Can be added. In particular, substances, such as salicylic acid and triclosan, can be added further.

The disinfectant may be prepared by using the extract of the wormwood of the present invention as it is or by diluting with a dermatologically and pharmacologically acceptable diluent or solvent to an appropriate concentration. The disinfectant may be used on the surface of the organism, preferably on the skin of mammals and most preferably on human skin. The disinfectant may also be used on inanimate surfaces, such as wood, metal, glass, ceramics, plastics, paper and cloth. The disinfectant may be treated on the surface of the living or non-living object using a method including dipping, swab, spraying and brushing. Preferably, the disinfectant may be used in hospitals and homes for the purpose of wound surface, pre-surgical skin disinfection, surgical instrument disinfection, conduit disinfection and the like.

In the case of the sterile detergent, it may be easily prepared according to a method known in the art, including one or more excipients and additives generally used in the field of preparation of detergents in addition to the extract of the wormwood according to the present invention. The disinfectant detergent may be used for kitchen or food, and the disinfectant detergent for kitchen may further include anionic surfactants, nonionic surfactants, amphoteric surfactants, and the like, in addition to the wormwood extract. Examples of anionic surfactants include alkylbenzene sulfonates, alpha olefin sulfates, sodium or ammonium lauryl ether sulfates, and examples of nonionic surfactants include fatty acid amides, alkyl polyglucosides, ethoxylated fatty alcohols, and ethoxylates. And cylated nonylphenol. Examples of amphoteric surfactants include betaine-based surfactants, amine oxides, and the like. In addition to the above surfactants, diluents such as flavors, pigments and water may be optionally added.

In the case of the food disinfectant detergent, it may be prepared by further adding a food acceptable solvent or diluent to the extract of the wormwood according to the present invention to dilute to an appropriate concentration. The food sterilizing detergent may be used for sterilization and washing of fruits, fish and meat, for example.

Food preservatives may be prepared by additionally adding a food or acceptable solvent or diluent to the wormwood extract according to the present invention for the purpose of enhancing the preservation of foods. The food preservative of the present invention may be added together with the raw materials in the manufacturing process of the food or prepared into a separate water-soluble suspension. In addition, the food preservative according to the present invention may be used to immerse the target food or spray the food preservative of the present invention onto the target food.

Hereinafter, preferred embodiments and production examples are provided to facilitate understanding of the present invention. However, the following Examples and Preparation Examples are provided only for the purpose of easier understanding of the present invention, and the present invention is not limited by the Examples and Production Examples.

Example  One. Worm  Obtaining Extracts

After drying the mugwort worms, the extracts were systematically extracted with methanol and extracted three times or more, and then concentrated under reduced pressure with a vacuum concentrator (CCA-1100, EYELA) at 40 ° C. to obtain a wormwood methanol extract. The methanol extracts were fractionated with hexane, methylene chloride, ethyl acetate, butanol or water, respectively, to obtain a wormwood fraction.

Example  2. Antimicrobial Effect Experiment

Helicobacter pylori, the causative agent of stomach and duodenal ulcers, is a Helicobacter pylori strain 26695, which is available from Helicobacter pylori isolated strain banks for optimal culture of bacteria (Brucella Broth 0.56g <Pancreatic digest of casein 0.2g, dextrose 0.2g, Yeast) extract 0.04 g, sodium chloride 0.1 g, sodium bisulfate 0.002 g>, agar 0.24 g, Horse serum 2 mL). In order to maintain the aerobic condition, the cells were maintained at 95% or higher in a 10% CO2 incubator. The agar plate was incubated at 37 ° C for 48 to 72 hours.

100 μL of the fungus dispersion was dispensed on a Helicobacter pylori optimal plate, sterilized by a glass rod, and sterilized disc paper (diameter 8 mm) was raised. Each extract was sterilized with 0.45 μm membrane filter and concentrated with a vacuum evaporator. 30 μL of each extract at various concentrations was absorbed into disc paper. After the sterilized water was absorbed into the control, the cells were incubated at 37 ° C under aerobic condition for 24 hours.

The antibacterial effect of Helicobacter pylori bacteria on the extract of P. locust extract showed that the clear zone was 8 mm in sterile water and there was no antimicrobial effect of Helicobacter pylori. The antimicrobial effect against pylori was confirmed.

Hereinafter will be described a pharmaceutical composition comprising the composition of the present invention and a preparation example of a health functional food, the present invention is not intended to limit this but only to be described in detail.

Formulation example  One. Sanje  Produce

2 g extract

Lactose 100 mg

Talc 10 mg

The above components are mixed and filled in airtight bags to prepare powders.

Formulation example  2. Preparation of tablets

100 mg of wormwood extract

Corn starch 100 mg

Lactose 100 mg

Magnesium stearate 2 mg

After mixing the above components, tablets are prepared by tableting according to the usual preparation method of tablets.

Formulation example  3. Preparation of capsules

100 mg of wormwood extract

Crystalline cellulose 3 mg

Lactose 14.8 mg

Magnesium stearate 0.2 mg

The above components are mixed according to a conventional capsule preparation method and filled in gelatin capsules to prepare capsules.

Formulation example  4. Preparation of injections

100 mg of wormwood extract

180 mg mannitol

Sterile sterilized water for injection 2974 mg

Na ₂ HPO _{4 ?} 2H ₂ O 26 mg

(2 ml) per 1 ampoule in accordance with the usual injection preparation method.

Formulation example  5. Liquid  Produce

100 mg of wormwood extract

10 g per isomer

5 g mannitol

Purified water quantity

Each component was added and dissolved in purified water according to the usual liquid preparation method, and the lemon flavor was added in an appropriate amount. Then, the above components were mixed, and purified water was added thereto. The whole was added with purified water to adjust the total volume to 100 ml, And sterilized to prepare a liquid preparation.

Formulation example  6. Manufacture of health food

1 g of wormwood extract

Vitamin mixture quantity

Vitamin A acetate 70 μg

Vitamin E 1.0 mg

Vitamin B1 0.13 mg

0.15 mg of vitamin B2

Vitamin B6 0.5 mg

Vitamin B12 0.2 μg

Vitamin C 10 mg

Biotin 10 μg

Nicotinic acid amide 1.7 mg

Folic acid 50 μg

Calcium pantothenate 0.5 mg

Mineral mixture quantity

1.75 mg of ferrous sulfate

0.82 mg of zinc oxide

Magnesium carbonate 25.3 mg

Potassium monophosphate 15 mg

Secondary calcium phosphate 55 mg

Potassium citrate 90 mg

Calcium carbonate 100 mg

Magnesium chloride 24.8 mg

Although the composition ratio of the above-mentioned vitamin and mineral mixture is comparatively mixed with a composition suitable for health food as a preferred embodiment, the compounding ratio may be arbitrarily modified, and the above ingredients are mixed according to a conventional method for producing healthy foods , Granules can be prepared and used in the manufacture of health food compositions according to conventional methods.

Formulation example  7. Health drink  Produce

1 g of wormwood extract

Vitamin C 15 g

Vitamin E (powder) 100 g

19.75 g of ferrous lactate

3.5 g of zinc oxide

Nicotinic acid amide 3.5 g

Vitamin A 0.2 g

Vitamin B1 0.25 g

Vitamin B2 0.3g

Water quantification

The above components were mixed according to a conventional health drink manufacturing method, and the mixture was stirred and heated at 85 DEG C for about 1 hour. The solution thus prepared was filtered and sterilized in a sterilized 2 liter container, It is used in the production of the health beverage composition of the invention.

Although the compositional ratio is relatively mixed with a component suitable for a favorite drink, it is also possible to arbitrarily modify the compounding ratio according to the regional or national preference such as the demand class, the demanding country, and the use purpose.

Claims (6)

Antimicrobial pharmaceutical composition comprising the extract of the wormwood as an active ingredient.
The method of claim 1, wherein the extract of the wormwood extract, characterized in that the extract is extracted with an alcohol having 1 to 4 carbon atoms or a mixed solvent thereof.
A pharmaceutical composition for preventing and treating gastrointestinal and duodenal diseases, comprising the extract of Pleurotus eryngii as an active ingredient.
According to claim 3, wherein the stomach and duodenal disease is a composition characterized in that the disease selected from the group consisting of gastritis, duodenitis, gastric ulcer, duodenal ulcer, gastric adenocarcinoma, gastric lymphoma and gastric cancer caused by Helicobacter pylori.
Health functional food for the prevention and improvement of stomach and duodenal diseases, including the extract of P. locust.
Antimicrobial preparations containing the extract of the wormwood as an active ingredient.