KR101503503B1 - Antibacterial Composition Containing Ixeris polycephala Cassini Extract and active ingredient isolated from the same - Google Patents

Abstract

The present invention relates to an antimicrobial composition comprising an extract of Ixeris polycephala Cassini and an active substance isolated therefrom as an active ingredient. The honeycomb extract and the urs-12-ene and olean-12-en-3-ol isolated therefrom according to the present invention are effective against Gram- Gram-positive bacteria or Helicobacter pylori, and thus can be usefully used as an antimicrobial composition or as a therapeutic agent for diseases caused by the strain.

Description

[0001] The present invention relates to an antimicrobial composition comprising an extract from Bee Silva and an active substance isolated therefrom,

The present invention relates to an antimicrobial composition comprising an extract of Ixeris polycephala Cassini and an active substance isolated therefrom as an active ingredient.

Direct or indirect damages caused by pathogenic microorganisms are causing economic, environmental and medical problems. The loss of food in the food industry due to corruption, the harmfulness and environmental pollution of the human body due to the use of excessive chemical pesticides in the agricultural industry, and the emergence of antibiotic resistant strains due to abuse of antibiotics. .

Vancomycin-resistant staphylococcus aureus (VRSA), a highly resistant strain of vancomycin, is known to be the world's first treatment for Staphylococcus aureus, the most common cause of human infection. It was first reported by the Centers for Disease Control in 2002 The possibility of so-called super-bacteria spreading is becoming very high. This is the first time in Europe that vancomycin resistant enterococcus (VRE) resistant to vancomycin has been reported since the 1970s, when methicillin-resistant S. aureus (MRSA), which is only treated by vancomycin, And vancomycin intermediate-resistant S. aureus (VISA), a vancomycin resistant strain reported in Japan, the United States, France and Korea in late 1990, is a new example of antibiotic resistance that has emerged as a global crisis (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. : 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, studies for separating new antimicrobial substances from natural products have been actively conducted. In order to isolate new antimicrobial substances from natural products, it should be considered that the antimicrobial spectrum is wide and safe even without long-term administration without adverse effects.

In 1982, Helicobacter pylori isolated from gastric mucosa of patients with type B gastritis by Marshall, Warren and Goodwin in Australia induced chronic gastritis type B, gastric ulcer and duodenal ulcer, It is known as a primary determinant of development. A major factor in the pathogenesis of stomach and duodenal diseases caused by Helicobacter pylori infection is urease, an urease, in the induction of gastric inflammation. Helicobacter pylori produces urea, which is equivalent to 6% of the total protein. The resulting urease breaks down the urea into ammonia and carbon dioxide to neutralize the environment surrounding the bacteria to prevent attack by hydrochloric acid in the gastric lumen, (Sidebotham RL, et al., J. Clin. Pathol., 44, pp. 52-57, 1991), which causes cytotoxicity directly to gastric epithelial cells. Due to the action of urease, stomach acid in the gastric lumen is regressed below the mucosal layer, and gastric acid causes gastric mucosal epithelial cells to be extensively damaged, resulting in gastritis and gastric ulcer. 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 induce chronic inflammation due to the generation of reactive oxygen species (ROS) , 92, pp 1853-1857, 1997).

Helicobacter infections are transmitted through animals or humans, or through carelessness or through various routes of food (Dunn, BE, Cohen, H., and Blaser, MJ (1997). Clinical Microbiology Reviews, 10 ), 720-7, Kodaira, MS, Escobar, AMU, & Grisi, S. (2002) Revista de Sade Pade Pblica.36: 356-369).

It is also known that Helicobacter pylori, Helicobacter canis, Helicobacter cinaedi, Helicobacter heilmannii, Helicobacter pylori (Helicobacter pylori), Helicobacter pylori Helicobacter species such as Helicobacter felis, Helicobacter mustelae, Helicobacter fenelliae, Helicobacter rappini, Helicobacter hepaticus, Helicobacter bilis, (Helicobacter pullorum) have been known.

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. Currently, studies on the treatment of Helicobacter pylori infection have been actively conducted, and many therapies for the purpose of elimination and prevention of recurrence have been reported.

As described above, although Helicobacter pylori is a very dangerous microorganism in gastrointestinal diseases, development of an appropriate antibacterial substance using natural materials is lacking. Currently, Helicobacter pylori therapies include bismuth, metronidazole, tetracycline or amoxicillin as well as conventional triple therapy with bismuth, omeprazole, tetracycline and metronidazole, And a combination of these drugs has 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, antimicrobial activity against Helicobacter pylori of various natural products such as Thyme, Chinese tea, Cashew apple, Caboose and Chrysanthemum has been reported, but the research has not been done yet. Therefore, finding antimicrobial materials for Helicobacter pylori from an abundant and easily available food source is an important substitute for antibiotics such as tetracycline. In particular, the most ideal antibiotic against Helicobacter pylori is that it does not stimulate the stomach epithelium as well as its antibacterial role.

In order to solve the above-mentioned problems, the inventor of the present invention has been studying to separate new antimicrobial substances from natural products, and found that an extract of Ixeris polycephala Cassini and an active substance isolated therefrom are excellent antimicrobial against pathogenic microorganisms The present invention has been completed.

It is an object of the present invention to provide a method for the production of bee parapertum extract or oleum-12-en-3-ol by separating urs-12-ene or olean- And to provide a pharmaceutical composition for antimicrobial use.

It is still another object of the present invention to provide a pharmaceutical composition for preventing and treating gastric or duodenal diseases, which comprises an extract from bee venom extract or woll-12-ene or olean-12-en-3-ol isolated therefrom as an active ingredient .

Another object of the present invention is to provide a food composition for preventing or ameliorating gastric or duodenal diseases, which comprises a bee parrots extract or wool-12-ene or olean-12-en-3-ol isolated therefrom as an active ingredient .

It is still another object of the present invention to provide an antimicrobial agent comprising an actinomycetes extract or wool-12-ene or oleene-12-en-3-ol separated therefrom as an active ingredient.

In order to accomplish the above object, the present invention relates to a method for the treatment and / ) As an active ingredient.

The present invention also provides a pharmaceutical composition for the prevention and treatment of stomach or duodenal diseases, which comprises as an active ingredient woolenberry extract or wool-12-ene or olean-12-en-3-ol isolated therefrom.

The present invention also provides a food composition for preventing or ameliorating stomach or duodenal diseases, which comprises as an active ingredient woolenberry extract or wool-12-ene or olean-12-en-3-ol isolated therefrom.

The present invention also provides an antimicrobial preparation comprising a bee saprol extract or woll-12-ene or olean-12-en-3-ol isolated therefrom as an active ingredient.

The honeycomb extract and the urs-12-ene and olean-12-en-3-ol isolated therefrom according to the present invention are effective against Gram- Gram-positive bacteria or Helicobacter pylori, and thus can be usefully used as an antimicrobial composition or as a therapeutic agent for diseases caused by the strain.

Fig. 1 shows mass spectrometry results of wool-12-ene isolated from bee venom extract.
Fig. 2 is a diagram showing mass spectrometry results of olean-12-en-3-ol isolated from bee venom extract.

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

The present invention provides a pharmaceutical composition for antimicrobial use which comprises an extract of Bee Silva as an active ingredient.

The present invention also relates to a pharmaceutical composition for antimicrobial use comprising urs-12-ene or olean-12-en-3-ol as an active ingredient to provide.

The wool-12-ene or olean-12-en-3-ol can be isolated from bee pruritus extract.

The Ixeris polycephala Cassini of the present invention is a kind of scumbag belonging to Asteraceae. It is a perennial weed in mountains, fields, and fields of southern central part of Korea. It grows about 25 ~ 50cm in size, and when it cuts stem or leaves, white juice comes out. Flowers bloom in May to July, about 1.5cm in size.

The honeycomb extract according to the present invention can be obtained by the following process.

First, the bees are washed with water to remove foreign matter, dried and crushed in the shade. The bees can be used without restrictions, such as cultivated or marketed. An appropriate amount of solvent is added to the pulverized beehive so that it is completely immersed. The extraction solvent is not limited thereto, but at least one solvent selected from water, alcohols having 1 to 4 carbon atoms, and a mixed solvent thereof may be used, and methanol is preferably used. The extract is filtered and concentrated under reduced pressure to obtain a final bee parrot extract.

In addition, the bee guinea pig extract is sequentially fractionated with hexane, dimethyl chloride, ethyl acetate, butanol and water to obtain each bee scarlet fraction.

The honeycomb extract and the urs-12-ene and olean-12-en-3-ol isolated therefrom according to the present invention are effective against Gram- Gram-positive bacteria or Helicobacter pylori, and thus can be usefully used as an antimicrobial composition or as a therapeutic agent for diseases caused by the strain.

The Gram-negative bacteria are not limited thereto, but preferably Escherichia coli.

The Gram-positive bacteria are not limited thereto, but are preferably Staphylococcus aureus.

The present invention also provides a composition for the prevention and treatment of stomach or duodenal diseases, which comprises as an active ingredient wolfram extract or wool-12-ene or olegan-12-en-3-ol isolated therefrom.

The composition may be a pharmaceutical composition or a food composition.

The gastric and duodenal disease refers to a disease caused by Helicobacter pylori and occurring in the stomach or duodenum. It may include peptic ulcer and gastric cancer, preferably gastritis, duodenal ulcer, gastric ulcer, duodenal ulcer, , Gastric lymphoma, and gastric cancer, and the gastritis may preferably be 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. Therefore, in order to treat the stomach and duodenal diseases, it is possible to prescribe an excellent substance having excellent antimicrobial activity against Helicobacter pylori causing causative bacteria.

The pharmaceutical composition of the present invention may be formulated into oral dosage forms, sterile injectable solutions, suppositories, and transdermal dosage forms such as powders, granules, tablets, capsules, suspensions, emulsions, syrups and aerosols according to a conventional method have. Examples of carriers, excipients and diluents that can be included in the composition include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose, Microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil. If necessary, it is formulated using a diluent such as a filler, an extender, a binder, a wetting agent, a disintegrant, a surfactant, or an excipient.

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

In another embodiment, the pharmaceutical composition of the present invention may be formulated into a liquid preparation for oral administration. Liquid preparations for oral administration include suspensions, solutions, emulsions and syrups. These liquid preparations may contain various excipients in addition to commonly used inert diluents (for example, purified water, ethanol, liquid paraffin) For example, wetting agents, sweeteners, fragrances, preservatives and the like may be included.

In another embodiment, the pharmaceutical composition of the present invention may be formulated into a preparation for parenteral, preferably intraperitoneal administration. Formulations for parenteral administration include sterilized aqueous solutions, non-aqueous solutions, suspensions, emulsions, freeze-dried preparations, and suppositories. As the sterilized aqueous solution, a suitable buffer solution such as Hank's solution, Ringer's solution or physically buffered saline can be used. As the non-aqueous solvent, propylene glycol, polyethylene glycol, olive oil, The same vegetable oil, an injectable ester such as ethyl oleate, or 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, in the case of suppositories, witepsol, macrogol, tween 61, cacao paper, laurin, glyceroglatin and the like may be used.

The composition formulated in the above manner may be administered through various routes including parenteral or oral (transdermal, subcutaneous, intravenous, muscular, abdominal, etc.) in an effective amount. The "effective amount" as used herein refers to an amount that shows a preventive or therapeutic effect when administered to a patient. The dose of the composition according to the present invention can be appropriately selected depending on the route of administration, subject to be administered, age, sex, weight, individual difference, and disease state. Preferably, the composition of the present invention may contain the active ingredient in an amount of 0.1 to 10000 mg / kg body weight / day, more preferably 10 to 1000 mg / kg body weight / day, Can be administered in an effective amount.

When the composition of the present invention is used as a food or beverage additive, the honeycomb extract or wool-12-ene or olean-12-en-3-ol separated therefrom may be added intact, And can be suitably used according to a conventional method. The mixing amount of the honeycomb extract can suitably be determined according to its use purpose (prevention, health or therapeutic treatment). In the case of long-term ingestion for health or for the purpose of controlling health, the above-mentioned honeycomb extract or wool-12-ene or olean-12-en-3-ol separated therefrom has no problem in terms of safety Because there is no, it can be taken for a long time.

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

When formulated as a beverage, the liquid ingredients added to the bee extract or other than wool-12-ene or olean-12-en-3-ol isolated therefrom include, but are not limited to, A flavoring agent or a natural carbohydrate as an additional ingredient. Examples of such natural carbohydrates include monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose and polysaccharides such as those commonly used in dextrin and cyclodextrins, , 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. Natural flavors (taumarin, stevia extract (e.g., rebaudioside A, glycyrrhizin, etc.)) and synthetic flavors (e. G., Saccharin, aspartame, etc.) can be used as flavors other than those described above .

In another aspect, the food composition of the present invention may be formulated into various flavors such as various nutrients, vitamins, minerals (electrolytes), synthetic flavors and natural flavors, colorants and enhancers (cheese, chocolate etc.), pectic acid and its salts, , Protective colloid thickening agents, pH adjusting agents, stabilizers, preservatives, glycerin, alcohols, carbonating agents used in carbonated drinks, and the like. In addition, the food composition of the present invention may contain pulp for the production of fruit and vegetable drinks. These components may be used singly 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 addition, the present invention provides an antimicrobial agent comprising an antibacterial extract or wool-12-ene or oleene-12-en-3-ol isolated therefrom as an active ingredient.

Such preparations include, for example, but are not limited to, cosmetics, disinfectants, sterilizing detergents, and food preservatives. The cosmetics may be selected from the group consisting of beeswax extract of the present invention or urs-12-ene or olean-12-en-3-ol isolated therefrom May be readily prepared according to methods known in the art, including one or more excipients and additives commonly used in the art of making cosmetic compositions. More specifically, the cosmetic may be at least one selected from the group consisting of basic cosmetics such as cleanser, pack, body oil and the like such as lotion, cream, essence, cleansing foam and cleansing water, color cosmetics such as foundation, lipstick, mascara and makeup base, shampoo, Hair products such as hair gel and soap, and the like. Preferably, the bee jug extract of the present invention or urs-12-ene or olean-12-en-3-ol isolated therefrom The included cosmetic composition can be used to treat or prevent acne. Therefore, the cosmetic composition of the present invention may further comprise a plant-derived proteolytic enzyme such as Papain and Bromelain which can improve the therapeutic effect of acne, and a skin exfoliating agent such as a protease derived from a microorganism Can be added. In particular, substances such as salicylic acid and triclosan can be further added.

The disinfectant may be selected from beeswax extract of the present invention or urs-12-ene or olean-12-en-3-ol isolated therefrom as it is May be prepared or diluted with a dermatologically and pharmacologically acceptable diluent or solvent to the appropriate concentration. The disinfectant may be used on the surface of the organism, preferably on the skin of mammals, most preferably on human skin. In addition, the disinfectant may be used on surfaces of non-living organisms such as wood, metal, glass, ceramic, plastic, paper and cloth. The disinfecting agent may be applied to the surface of the organism or organism using methods including immersion, swab, spray and brushing. Preferably, the disinfectant may be used in hospitals and general households for use on wound surfaces, pre-operative skin disinfection, surgical instrument disinfection, and catheter disinfection.

In the case of the sterilizing detergent described above, the bee parapet extract according to the present invention or urs-12-ene or olean-12-en-3- ol as well as one or more excipients and additives commonly used in the manufacture of detergents and can be readily prepared according to methods known in the art. The germicidal detergent may be used in the kitchen or food, and the sterilizing detergent for the kitchen may be selected from beeswax extract or urs-12-ene or olean-12-en- -12-en-3-ol), an anionic surfactant, a nonionic surfactant, an amphoteric surfactant, and the like. Examples of anionic surfactants include alkylbenzenesulfonates, alpha olefin sulfates, sodium or ammonium lauryl ether sulfates, and examples of nonionic surfactants include fatty acid amides, alkylpolyglucosides, ethoxylated fatty alcohols, And the like. Examples of amphoteric surfactants include betaine surfactants, amine oxides, and the like. In addition to the surfactant, a diluent such as fragrance, pigment and water may be optionally added.

In the case of a food sterilizing detergent, it is preferable to use the honeycomb extract according to the present invention or urs-12-ene or olean-12-en-3-ole -ol) with a pharmaceutically acceptable solvent or diluent to dilute it to an appropriate concentration. The food sterilizing detergent can be used for sterilizing and washing fruits, fish and meat, for example.

For the purpose of enhancing the preservability of foodstuffs, the food preservative may be selected from the group consisting of umbraculifera extract of the present invention or urs-12-ene or olean-12-en-3-ol -12-en-3-ol) with a pharmaceutically acceptable solvent or diluent. The food preservative of the present invention may be formulated together with the raw material in the process of producing food or may be added as a separate aqueous suspension. In addition, the food preservative according to the present invention can be used to immerse the target food or spray the food preservative of the present invention to the target food.

Hereinafter, preferred embodiments of the present invention will be described in order to facilitate understanding of the present invention. However, the following examples are provided only for the purpose of easier understanding of the present invention, and the present invention is not limited by the examples.

Example  One. Punishment  The extract and Fraction  Produce

The bees were shaken and then subjected to systematic extraction using methanol. The extracts were extracted three times or more, and then concentrated under reduced pressure at 40 ° C with a vacuum concentrator (CCA-1100, EYELA) to obtain a bee barrow methanol extract.

The methanol extract was fractionated with hexane, dimethyl chloride, ethyl acetate, butanol or water, respectively, to obtain a bee scarlet fraction.

Example  2. Punishment  The extract and Fraction  Antibacterial effect experiment

Antibacterial activity against Helicobacter pylori, causative bacteria such as Gram-negative bacteria, Gram-positive bacteria and stomach and duodenal ulcers, was confirmed in order to confirm the antimicrobial effect of extracts and fractions. E. coli was used as Gram-negative bacteria, S. aureus was used as Gram-positive bacteria, and strain 26695 obtained from Helicobacter pylori isolate strain bank was used as Helicobacter pylori. Helicobacter pylori strain 26695 was cultivated in the optimal medium (Brucella Broth 0.56 g, Pancreatic digest of casein 0.2 g, dextrose 0.2 g, yeast extract 0.04 g, sodium chloride 0.1 g, sodium bisulfate 0.002 g, agar 0.24 g, Horse serum 2 mL) To maintain the aerobic condition, 10% CO ₂ 95% or more was maintained in the incubator.

More specifically, 100 μL of the microdispersion was dispensed on an optimal culture plate of each strain and plated with a sterilizing glass rod. Then, sterilized disc paper (diameter: 8 mm) was raised and 30 μL of each bee extract and fraction was absorbed into the disc paper. After incubation at 37 ° C under aerobic conditions for 24 hours, it was confirmed whether a clear zone was formed around the disk. Sterile water was used as a control. The results are shown in Table 1.

sample
(50 μg / 30 μL) Growth inhibition ring (mm) E. coli S. aureus H. pylori Hexane fraction 27 11 11 Dimethyl chloride fraction 18 10 10 Ethyl acetate fraction 14 10 12 Butanol fraction 11 11 14 Methanol extract 18 12 12

As shown in Table 1, it was confirmed that the honeycomb extract and fractions had antimicrobial activity against Gram-negative bacteria such as Escherichia coli, Gram-positive bacteria, Staphylococcus aureus and Helicobacter pylori.

Example  3. Punishment  From the extract Active ingredient separation

Based on the results of Example 2, the active ingredient was isolated from the bee scarlet extract and fraction obtained in Example 1 by nuclear magnetic resonance analysis and mass spectrometry. As a result, urs-12-ene of Ursene series of the following formula (1) and olean-12-en-3-ol of Oleanene series of the following formula (2) were identified. These are all substances that are first separated and reported from punishment.

The results of nuclear magnetic resonance analysis and mass spectrometry of urs-12-ene and olean-12-en-3-ol are shown in Table 2, Fig. 1 and Fig.

location Formula 1 (2) 隆_H δ _C 隆_H δ _C One - 39.5 - 39.6 2 - 28.0 - 27.9 3 - - 80.8 4 - 39.0 4.5 (1H, s) 39.5 5 - 54.6 - 55.1 6 - 18.6 - 18.1 7 - 32.0 - 33.6 8 - 40.0 - 38.3 9 - 47.7 - 47.4 10 - 37.2 - 35.0 11 - 23.5 - 23.5 12 5.50 (1H, brs) 124.1 5.15 (1H, dt) 121.5 13 - 139.2 - 145.1 14 - 42.0 - 42.0 15 - 28.8 - 28.2 16 - 26.5 - 27.9 17 - 33.7 - 32.5 18 - 58.5 - 59.0 19 - 39.4 - 40.2 20 - 39.6 - 41.4 21 - 31.1 - 31.0 22 - 41.3 - 42.0 23 1.08 (3 H, s) 28.1 0.92 29.5 24 0.97 (3 H, s) 15.6 0.80 15.8 25 1.22 (3 H, s) 15.8 0.98 15.8 26 1.04 (3 H, s) 16.8 0.88 16.8 27 1.27 (3 H, s) 23.5 1.0 23.5 28 1.08 (3 H, s) 28.0 0.88 28.8 29 0.99 (3H, d) 17.5 0.80 17.6 30 1.02 (3H, d) 21.5 0.83 21.2 C OCH ₃ - 170.8 CO CH ₃ 2.05 (3 H, s) 21.2

Example  4. Punishment  The antibacterial effect of the active ingredient isolated from the extract

The antimicrobial activity of the active ingredient (urs-12-ene and olean-12-en-3-ol) obtained in Example 3 was confirmed in the same manner as in Example 2. Penicillin was used as a positive control. The results are shown in Table 3.

compound density
(μg / μL) Growth inhibition ring (mm) E. coli S. aureus H. pylori urs-12-ene 15 10 13 8 30 10 13 12 oleate-12-en-3-ol 15 14 14 8 30 10 15 13 penicillin 15 25 23 17 30 25 28 17

As shown in Table 3, urs-12-ene and olean-12-en-3-ol isolated from bee guinea pig extract and fractions had antimicrobial activity against Gram-negative bacteria such as Escherichia coli, Gram-positive bacteria, Staphylococcus aureus and Helicobacter pylori .

Hereinafter, a pharmaceutical composition containing the composition of the present invention and an example of a preparation of a health functional food will be described, but the present invention is not intended to be limited thereto but is specifically described.

Formulation example  One. Sanje  Produce

Bee extract or wool-12-ene or olean-12-en-3-ol 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

Bee extract or wool-12-ene or olean-12-en-3-ol 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 the usual preparation method of tablets.

Formulation example  3. Preparation of capsules

Bee extract or wool-12-ene or olean-12-en-3-ol 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

Bee extract or wool-12-ene or olean-12-en-3-ol 100 mg

180 mg mannitol

Sterile sterilized water for injection 2974 mg

_{Na 2 HPO 4 · H 2 O} 26 mg

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

Formulation example  5. Liquid  Produce

Bee extract or wool-12-ene or olean-12-en-3-ol 100 mg

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

Bee supple or wool-12-yen or olean-12-en-3-ol 1 g

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

Bee supple or wool-12-yen or olean-12-en-3-ol 1 g

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.

Formulation example  8. Manufacture of skin cleanser

Bee extract or wool-12-ene or olean-12-en-3-ol 0.5%

Glycerin 6 g

2.0 g of monoalkyl phosphate

Aqueous solution of sodium hydroxide 0.5 g

1.5 g of myristic acid, 12 g of a cleanser base containing a small amount of fragrance

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

Formulation example  9. Manufacture of soap

Bee extract or wool-12-ene or olean-12-en-3-ol 0.5%

Soap base 99.5% by weight (including moisture)

The ingredients are mixed well in a mixer, extruded, cut and pressed in a soap maker to produce a solid soap composition.

Formulation example  10. Manufacture of kitchen cleaner

Bee extract or wool-12-ene or olean-12-en-3-ol 0.5%

20% by weight alkylethersulfonate (alkylethersulfonate)

4% by weight alkylpolyglucoside < RTI ID = 0.0 >

4% by weight of lauryldimethylamine oxide,

Cocamidopropyl betaine 7% by weight < RTI ID = 0.0 >

5% by weight of ethoxylated lauryl alcohol

EDTA 0.3 wt%

Small amount of pigment

Incense 0.5%

Purified water quantity

The above components are mixed to prepare a cleaning agent.

Claims (13)

delete delete delete delete delete At least one gastric or duodenal disease selected from the group consisting of gastritis, duodenal ulcer, gastric ulcer, duodenal ulcer, gastric cancer, gastric lymphoma and gastric cancer caused by Helicobacter pylori comprising an extract of Ixeris polycephala Cassini as an active ingredient A pharmaceutical composition for prevention and treatment. delete At least one selected from the group consisting of gastritis, duodenitis, gastric ulcer, duodenal ulcer, gastric cancer, gastric lymphoma and gastric cancer caused by Helicobacter pylori comprising at least one compound selected from the group consisting of: A pharmaceutical composition for the prevention and treatment of gastric or duodenal diseases.
[Chemical Formula 1]

(2)

Prevention of at least one gastric or duodenal disease selected from the group consisting of gastritis, duodenal ulcer, gastric ulcer, duodenal ulcer, gastric cancer, gastric lymphoma and stomach cancer caused by Helicobacter pylori containing the extract of Ixeris polycephala Cassini as an active ingredient ≪ / RTI > A gastric ulcer, a duodenal ulcer, a gastric cancer, a gastric lymphoma and a stomach cancer caused by Helicobacter pylori comprising at least one compound selected from the group consisting of the following formula 1 and 2 as an active ingredient: Or a food composition for preventing and improving duodenal diseases.
[Chemical Formula 1]

(2)

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