KR20120055482A - Antibacterial composition containing anthriscus sylvestris extract - Google Patents

Abstract

PURPOSE: An antimicrobial composition including Anthriscus sylvestris extracts is provided to improve antibacterial activity against Helicobacter pylori, Escherichia coli, and staphylococcus aureus, thereby being used for prevention and treatment of diseases caused by pathogenic bacteria. CONSTITUTION: An antimicrobial composition including Anthriscus sylvestris extracts includes Anthriscus sylvestris extracts as active ingredients. The extract from Anthriscus sylvestris is extracted as alcohol having 1-4 carbons or a mixed solvent thereof. The extract from Anthriscus sylvestris has antibacterial activity against Helicobacter pylori, Escherichia coli, and staphylococcus aureus. A pharmaceutical composition for antibiotic includes falcarindiol or deoxypodophyllotoxin as an active ingredient. Falcarindiol or dioxy podophyllotoxin is obtained from the Anthriscus sylvestris. A pharmaceutical composition for duodenal disease prevention and treating includes extract from Anthriscus sylvestris as an active ingredient.

Description

Antibacterial Composition Containing Whole Lake Extract {Antibacterial Composition Containing Anthriscus sylvestris Extract}

The present invention relates to an antimicrobial composition comprising an anthriscus sylvestris extract and falcarindiol or deoxypodophyllotoxin isolated therefrom 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 first discovered in Europe in 1988, after methicillin-resistant Staphylococcus aureus (MRSA), which was treated only by vancomycin, was questioned since the 1970s. In the late 1990s, the resistance issue of vancomycin intermediate-resistants.aureus (VISA), reported in Japan, the United States, France, and Korea, emerged as a new example of antibiotic resistance that emerged as a global crisis. Is an urgent need for new antibiotic development (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 antibiotics currently used are manufactured through chemical synthesis, which is expensive 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 oxygen consumption of gastric mucosa cells and ATP production in mitochondria (Tsujii M., et al., Gastroenterology, 102, pp 1881-1888, 1992), ultimately forming monochloroamine It has been reported to produce reactive oxygen pecies, causing cell damage, causing chronic inflammation, and further DNA damage, thereby promoting the cancer development process (Hahm KB, et al., Am. J. Gastroenterol). , 92, pp 1853-1857, 1997).

The transmission of Helicobacter is 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 primarily found in certain places in the stomach, such as peptic ulcers (e.g. gastric or duodenal ulcers), inflammation (e.g. gastritis, etc.), diseases of the upper digestive tract such as gastric cancer, MALT (Mucosaassociated lymphoid tissue) Background of pathogenesis of 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. Current Helicobacter pylori treatments include general triple therapy, bismuth preparations, bismuth preparations, omeparazole and tetracycline in combination with bismuth preparations, metronidazole, and tetracycline or amoxicillin. And quadruple therapy with metronidazole. However, it has been pointed out that the emergence of resistant strains by antibiotic administration, the penetration of drugs in the stomach, and the regrowth of bacteria whose growth has been inhibited after treatment. For this reason, numerous efforts have been made to search for antimicrobial substances specific to Helicobacter pylori, and recently, interest in bioactive components in plants has increased, suggesting the possibility of their bioregulatory function and recovery or prevention of diseases. Has been. 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 isolate a new antibacterial substance from natural products, Jeonho extract and Falcarindiol or deoxypodophyllotoxin isolated from it The present invention has been completed by finding that it has an excellent antimicrobial effect against this pathogenic microorganism.

It is an object of the present invention to provide an antimicrobial composition comprising anthraccus sylvestris extract and falcarindiol or deoxypodophyllotoxin isolated therefrom as an active ingredient.

In order to achieve the above object, the present invention provides an antimicrobial pharmaceutical composition comprising an extract of Anthriscus sylvestris as an active ingredient.

The present invention also provides a pharmaceutical composition for antimicrobial comprising falcarindiol or deoxypodophyllotoxin as an active ingredient.

The present invention also provides a pharmaceutical composition for the prevention and treatment of gastrointestinal and duodenal diseases, including the extract of Jeonho as an active ingredient.

In another aspect, the present invention provides a pharmaceutical composition for the prevention and treatment of gastric and duodenal diseases, including falcarindiol or deoxypodophyllotoxin as an active ingredient.

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

In another aspect, the present invention provides a dietary supplement for preventing and improving gastrointestinal and duodenal diseases, including falcarindiol or deoxypodophyllotoxin as an active ingredient.

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

In another aspect, the present invention provides an antimicrobial formulation comprising falcarindiol or deoxypodophyllotoxin as an active ingredient.

The extract of the present invention and falcarindiol or deoxypodophyllotoxin isolated therefrom exhibit strong antimicrobial activity against Helicobacter pylori, Staphylococcus aureus and Escherichia coli, which are caused by pathogenic bacteria. It can be usefully used for the prevention or treatment of diseases.

1 is a schematic diagram of the fraction of Jeonho extract.
Figure 2 is the antimicrobial activity of Helicobacter pylori bacteria of methanol extract of Jeonho.
Figure 3 is the antimicrobial activity of Staphylococcus aureus and Escherichia coli of the jeonho fraction.
4 shows the antimicrobial activity of falcarindiol or deoxypodophyllotoxin isolated from Jeonho extract.

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

In one embodiment, the present invention provides an antimicrobial pharmaceutical composition comprising an extract of Anthriscus sylvestris as an active ingredient.

Jeonho (Anthriscus sylvestris) is a perennial herb that is common in mountain valleys throughout the country and is distributed in Japan, Manchuria, and China. It is 30-70cm high, long brown hairs, and the rhizome is thick and short. Flowers bloom in July-August, reddish purple, many flowers hang on the conical inflorescences at the end of stems, brown hairs on flower shaft, calyxes are divided into 5 pieces, the fragments are egg-shaped, and 5 petals. Dried and dried horses are also called horse riding horses or red horses, which improve blood circulation, release blood, reduce heat, release poison, and convulsions. It is known to be effective in relieving pain and relieving pain. It is also used to relieve overworked diseases, sore muscles and bone nodes, sore symptoms, bruises, joint pain, postoperative pain, and snake bites (Bae Gi-hwan, Korean medicinal plants, Kyohaksa, p204, 2000).

As used herein, the term "extract" refers to an active ingredient isolated from natural products, that is, a material that exhibits 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.

Jeonho extract according to the present invention can be obtained through the following process.

The precursor is extracted with one or more solvents selected from the group consisting of alcohol, ethyl acetate, methyl chloride, methyl ethyl ketone, acetone and ether and concentrated under reduced pressure. The alcohol may be a lower or higher alcohol, preferably a lower alcohol selected from the group consisting of methanol, ethanol, isopropanol and butanol, more preferably methanol. The alcohol may be a mixture with water. In addition to the concentrate, hexane, methyl chloride, ethyl acetate, butanol or water may be fractionated and concentrated under reduced pressure again. The fractional concentrate may be further purified by chromatography (paper, TLC, column, etc.) using silica or paper as a carrier, and a mixed solution of chloroform: acetone: formic acid as a developing solvent. have. Here, the distribution of the substances in the extract between the water contained in the carrier and the developing solvent occurs, and the substances are separated according to the difference in distribution ratio. Chloroform: acetone: formic acid in the developing solvent may be mixed in a ratio of 50-100: 10-20: 5-10, most preferably 75: 16.5: 8.5. The chromatography may be thin layer chromatography (TLC) or column chromatography using silica as a carrier. The TLC is a method of applying a thin coating of silica gel to a support such as a glass plate or plastic, dropping the extract thereon and then developing with a developing solvent to purify. In the column chromatography, silica is packed into a column, an extract is loaded thereon, and then purified by developing with a developing solvent. It is preferable to use column chromatography for mass production of the extract.

The present invention also provides a pharmaceutical composition for antimicrobial comprising falcarindiol or deoxypodophyllotoxin as an active ingredient. The falcarindiol or deoxypodophyllotoxin has a structure of Formula 1 or Formula 2. The falcarindiol or deoxypodophyllotoxin can be obtained from jeonho extract and can be used synthetically or purchased from the manufacturer.

The extract of Jehoho according to the present invention and falcarindiol or deoxypodophyllotoxin isolated therefrom exhibit strong antimicrobial activity against Staphylococcus aureus and Escherichia coli. Therefore, Jehoho extract and falcarindiol or deoxypodophyllotoxin isolated therefrom according to the present invention can be usefully used for the prevention or treatment of the bacteria.

In still another aspect, the present invention provides a pharmaceutical composition for preventing and treating gastrointestinal and duodenal diseases, which comprises Jehoho extract as an active ingredient. In another aspect, the present invention provides a pharmaceutical composition for the prevention and treatment of gastric and duodenal diseases, including falcarindiol or deoxypodophyllotoxin as an active ingredient.

Since the jeonho extract according to the present invention and falcarindiol or deoxypodophyllotoxin isolated therefrom exhibits antimicrobial activity against Helicobacter pylori bacteria, prevention of gastric and duodenal diseases caused by Helicobacter pylori And therapeutically useful. The gastric and duodenal diseases may include peptic ulcer and gastric cancer, and preferably at least one selected from the group consisting of gastritis, duodenitis, gastric ulcer, duodenal ulcer, gastric cancer, gastric lymphoma and gastric cancer, the gastritis May preferably be chronic atrophic gastritis. Since the discovery of Helicobacter pylori, the main causative agents of gastric and duodenal diseases have been reported as Helicobacter pylori, and Helicobacter pylori is known to inhabit mainly in the gastric mucosa, specifically epithelial cells and mucosal layers. Therefore, it is possible to prescribe an excellent antimicrobial activity against the causative bacterium Helicobacter pylori to treat the 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 sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized preparations, 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 necessary, preservatives, stabilizers, wetting or emulsifying agents, salts for controlling osmotic pressure and / or buffers may also 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 depending on the degree of disease, preferably 0.1 to 10000 mg / kg / day, more preferably 10 ~ 1000 mg / kg / day It may be administered in an effective amount of.

In another aspect, the present invention provides a dietary supplement for the prevention and improvement of gastric and duodenal diseases, including the extract of Anthriscus sylvestris as an active ingredient. In another aspect, the present invention provides a dietary supplement for the prevention and improvement of gastric and duodenal diseases, including falcarindiol or deoxypodophyllotoxin as an active ingredient.

When the composition of the present invention is used as a food or beverage additive, the extract or falcarindiol or deoxypodophyllotoxin may be added as it is, or used together with other food or food ingredients, and used in a conventional method. Can be used accordingly. The mixed amount of the extract or falcarindiol or deoxypodophyllotoxin may be appropriately determined depending on the purpose of use (prevention, health or therapeutic treatment).

In the case of long-term intake for health purposes or health control purposes, the whole extract can be taken for a long time since 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 may be added include meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gums, dairy products including ice cream, various soups, beverages, teas, and drinks. Alcoholic beverages and vitamin complexes.

The liquid component added in addition to the Jeho 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 proportion of said natural carbohydrates 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.

As another aspect, the present invention provides an antimicrobial agent comprising an extract of Anthriscus sylvestris as an active ingredient. In another aspect, the present invention provides an antimicrobial formulation comprising falcarindiol or deoxypodophyllotoxin as an active ingredient.

Such formulations include, but are not limited to, cosmetics, disinfectants, sterile detergents and food preservatives. In the above cosmetics is a sugar containing one or more excipients and additives commonly used in the field of manufacturing cosmetic compositions with the extract of the present invention or falcarindiol or deoxypodophyllotoxin isolated therefrom It can be manufactured easily according to a method known in the art. 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 jeoncar extract of the present invention or falcarindiol or deoxypodophyllotoxin isolated therefrom 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 used as it is or by dilution with a dermatologically and pharmacologically acceptable diluent or solvent so as to use the extract or Falcarindiol or deoxypodophyllotoxin isolated from the present invention. It can manufacture. 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 cleaning agent, in addition to the extract of jeonho according to the present invention or falcarindiol or deoxypodophyllotoxin isolated therefrom, it includes one or more excipients and additives generally used in the field of preparation of the cleaning agent. It can be easily prepared according to methods known in the art. The disinfectant cleaner may be used for kitchen or food, and the disinfectant detergent for kitchen may include anionic surfactants and nonionic surfactants in addition to falcarindiol or deoxypodophyllotoxin, which are isolated from whole leaf extract or falcarindiol or deoxypodophyllotoxin isolated therefrom. And amphoteric surfactants may be further included. 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 a food disinfectant detergent, a foodstuff acceptable solvent or diluent is added to the appropriate concentration by the addition of ethanol extract according to the present invention or falcarindiol or deoxypodophyllotoxin isolated therefrom. It can manufacture by diluting. The food sterilizing detergent may be used for sterilization and washing of fruits, fish and meat, for example.

Food preservatives are added food-acceptable solvents or diluents to the falcarindiol or deoxypodophyllotoxin isolated from the Jeho extract according to the present invention or separated therefrom for the purpose of enhancing the preservation of foods. It can be prepared by adding. 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 examples and preparation examples are provided to aid in understanding the present invention. However, the following examples and preparations are merely provided to more easily understand the present invention, and the contents of the present invention are not limited by the examples and preparations.

Example  One. War  Methanol and Fraction  purchase

After drying the whole lake, systematic extraction using methanol (methanol) was carried out three times or more, and then concentrated under reduced pressure (CCA-1100, EYELA) under reduced pressure at 40 ℃, to obtain a methanol extract of Jeonho.

The methanol extracts were fractionated with hexane, methylene chloride, ethyl acetate, butanol or water, respectively, to obtain a fraction of ethanol. Fractional schematics are shown in FIG. 1.

Example  2. Helicobacter Pylori  Antimicrobial effect on bacteria

Dispense 100 μL of the homogenous solution into a Helicobacter Pylori optimal medium plate, spread it with a sterile glass rod, place sterilized disc paper (8 mm in diameter), concentrate each extract sterilized with a 0.45 μm membrane filter, and dilute with sterile water. 30 μL of the extract was absorbed into the disc paper, and the control was absorbed in sterile water and then incubated for 24 hours at 37 ° C. in aerobic conditions, and then the presence of clear zones around the disc was confirmed.

As a result of examining the antimicrobial effect of Helicobacter pylori bacteria in methanol extract of Jehoho, as shown in Figure 2, the clear zone was 8 mm in sterile water showed no antimicrobial effect of Helicobacter pylori, but 10 μg / 30μL concentration In the case of 10 μg, the clear zone was 11 mm, indicating the antimicrobial effect against Helicobacter pylori.

Example  3. Antibacterial effect test for pathogenic bacteria

In the same manner as in Example 2, it was confirmed that the extract of Jeonho showed antimicrobial activity against Staphylococcus aureus and Escherichia coli which are representative pathogenic bacteria.

The precursors Hx, MC, EtOAc, BuOH fractions obtained in Example 1 were each treated for 24 hours at a concentration of 10 μg / 30 μL. As a result, as shown in FIG. 3, the Hx, Mc and EtOAc fractions of E. coli exhibited growth inhibition rings of 10 mm, respectively. In addition, the Hx and Mc fractions of S. aureus showed growth inhibition ring of 11 mm, confirming the antimicrobial effect.

Example  4. Identification of antimicrobial and antimicrobial effects of active ingredients

In order to confirm the active ingredient showing antimicrobial activity, Falcarindiol or deoxypodophyllotoxin showing antimicrobial activity was identified from TMC by the active fraction, and its structure was identified through NMR. It was.

Falcarindiol; ¹ H-NMR (500 MHz, CDCl ₃ ): δ 5.94 (H-2), 5.61 (H-10), 5.50 (H-9), 5.45 (H-1a), 5.27 (H-1b), 5.21 ( H-8), 4.94 (H-3), 0.87 (CH ₃ )

[Formula 1]

Deoxypodophyllotoxin; ¹ H-NMR (400 MHz, CDCl ₃ ): δ 6.67 (1H, s, H-2), 6.52 (1H, s, H-5), 6.34 (2H, s, H-2 ′, 6 ′), 5.95 (2H, d, J = 1.0 Hz, OCH ₂ O), 5.93 (2H, d, J = 1.0 Hz, OCH ₂ O), 4.60 (1H, d, J = 2.8 Hz, H-7 ′), 4.45 (1H, td, H-9), 3.91 (1H, td, H-9), 3.80 (3H, s, 4′-OCH ₃ ), 3.75 (6H, s, 3 ′ & 4′-OCH ₃ ), 3.08 (1H, d, J = 11.2 Hz, H-7), 2.77 (1H, m, H-7), 2.74 (2H, m, H-8, 8 ′)

[Formula 2]

The antimicrobial activity of falcarindiol or deoxypodophyllotoxin, an active substance obtained through the above procedure, was confirmed. As a result, the inhibitory ring against Staphylococcus aureus, Escherichia coli and Helicobacter pylori was confirmed (FIG. 4). .

Therefore, it was confirmed that the extracts and fractions of Korean native plants Jeonho showed excellent antimicrobial activity against Helicobacter pylori, Staphylococcus aureus and Escherichia coli, and Falcarindiol or dioxy isolated from active fractions. Grape phytotoxin (deoxypodophyllotoxin) was also confirmed to show antimicrobial activity.

Hereinafter, the preparation of pharmaceutical compositions, health functional foods, and antimicrobial preparations including the composition of the present invention will be described, but the present invention is not intended to limit the present invention.

Formulation example  One. Powder  Produce

Jehoho extract or Falcarindiol or dioxypodophyllotoxin 2g

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

Whole Lake Extract or Falcarindiol or Dioxypodophyllotoxin 100 mg

Corn starch 100 mg

Lactose 100 mg

Magnesium stearate 2 mg

After mixing the above components, tablets are prepared by tableting according to a conventional method for preparing tablets.

Formulation example  3. Preparation of capsules

Whole Lake Extract or Falcarindiol or Dioxypodophyllotoxin 100 mg

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

Whole Lake Extract or Falcarindiol or Dioxypodophyllotoxin 100 mg

180 mg mannitol

Sterile sterilized water for injection 2974 mg

Na ₂ HPO ₄ 2H ₂ O 26 mg

According to the conventional method for preparing an injection, the amount of the above ingredient is prepared per ampoule (2 ml).

Formulation example  5. Liquid  Produce

Whole Lake Extract or Falcarindiol or Dioxypodophyllotoxin 100 mg

10 g per isomer

5 g mannitol

Purified water quantity

After dissolving each component in purified water according to the usual method of preparing a liquid solution, adding a proper amount of lemon aroma, and then mixing the above components, adding purified water and adjusting the whole to 100 ml by adding purified water and filling into a brown bottle. The solution is prepared by sterilization.

Formulation example  6. Manufacture of health food

Whole Lake Extract or Falcarindiol or Dioxypodophyllotoxin 1 g

Vitamin mixture quantity

Vitamin A acetate 70 μg

Vitamin E 1.0 mg

Vitamin B1 0.13 mg

Vitamin B2 0.15 mg

Vitamin B6 0.5 mg

Vitamin B12 0.2 μg

Vitamin C 10 mg

Biotin 10 μg

Nicotinamide 1.7 mg

Folic acid 50 μg

Calcium pantothenate 0.5 mg

Mineral mixture

Ferrous Sulfate 1.75 mg

Zinc Oxide 0.82 mg

Magnesium carbonate 25.3 mg

15 mg potassium monophosphate

Dicalcium 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 mixtures is mixed with a component suitable for a health food in a preferred embodiment, the compounding ratio may be arbitrarily modified. The granules may be prepared and used for preparing a health food composition according to a conventional method.

Formulation example  7. Health drink  Produce

Whole Lake Extract or Falcarindiol or Dioxypodophyllotoxin 1 g

15 g of vitamin C

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

After mixing the above components according to the conventional healthy beverage production method, and stirred and heated at 85 ℃ for about 1 hour, the resulting solution is filtered and obtained in a sterilized 2 l container, sealed sterilization and refrigerated and then Used to prepare the healthy 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.

Formulation example  8. Preparation of Skin Cleanser

0.5% by weight of Jehoho extract or Falcarinediol or deoxypodophyllotoxin

Glycerin 6g

2.0 g of monoalkyl phosphates

0.5 g sodium hydroxide solution

1.5g of myristic acid, 12g of face wash base containing trace amount of fragrance

The components are stirred in a homo mixer, heated at 60 ° C. for 3 minutes, then degassed and cooled to 37 ° C. to prepare a face wash composition.

Formulation example  9. Manufacture of soap

0.5% by weight of Jehoho extract or Falcarinediol or deoxypodophyllotoxin

Soap base 99.5% by weight (including moisture)

The components are well mixed with a mixer and then extruded, cut and molded in a soap maker to prepare a solid soap composition.

Formulation example  10. Preparation of kitchen cleaners

0.5% by weight of Jehoho extract or Falcarinediol or deoxypodophyllotoxin

20% by weight of alkylethersulfonate

4% by weight of alkylpolyglucoside

4% by weight of lauryldimethylamine oxide

Cocamidopropyl Betaine 7% by weight

5% by weight of ethoxylated lauryl alcohol

EDTA 0.3 wt%

Small amount of pigment

Incense 0.5% by weight

Purified water quantity

The above components are mixed to prepare a cleaning agent.

Claims (12)

Antimicrobial pharmaceutical composition comprising an extract of Jeonho (Anthriscus sylvestris) as an active ingredient.
The composition of claim 1, wherein the extract is extracted with an alcohol having 1 to 4 carbon atoms or a mixed solvent thereof.
The composition of claim 1, wherein the extract of the jeonho exhibits antimicrobial activity against at least one microorganism selected from the group consisting of Helicobacter pylori, Staphylococcus aureus and Escherichia coli.
Pharmaceutical composition for antibacterial comprising falcarindiol or deoxypodophyllotoxin as an active ingredient.
The composition according to claim 4, wherein the falcarindiol or deoxypodophyllotoxin is obtained from Jeonho.
A pharmaceutical composition for preventing and treating gastrointestinal and duodenal diseases, comprising Jehoho extract as an active ingredient.
The composition of claim 6, wherein the gastric and duodenal diseases are diseases selected from the group consisting of gastritis, duodenitis, gastric ulcer, duodenal ulcer, gastric adenocarcinoma, gastric lymphoma and gastric cancer caused by Helicobacter pylori.
Pharmaceutical composition for the prevention and treatment of gastric and duodenal diseases, including falcarindiol or deoxypodophyllotoxin as an active ingredient.
Health functional food for preventing and improving gastrointestinal and duodenal diseases, including Jeonho extract as an active ingredient.
Health functional food for the prevention and improvement of gastric and duodenal diseases, including falcarindiol or deoxypodophyllotoxin as an active ingredient.
Antimicrobial preparation comprising the extract of Anthriscus sylvestris as an active ingredient.
Antibacterial agent comprising falcarindiol or deoxypodophyllotoxin as an active ingredient.

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