KR102068469B1 - Composition comprising Boehmeria platanifolia extract for treating or preventing cancer - Google Patents

Abstract

The present invention relates to a composition for the prevention or treatment of cancer containing the extract of C. defoliation, the pharmaceutical composition or functional food containing the extract of C. persimmon is very excellent in killing effect of lung cancer cells of various cancer-related diseases including lung cancer. It can be easily used for prevention, improvement and treatment.

Description

Composition comprising Boehmeria platanifolia extract for treating or preventing cancer

The present invention relates to a composition for the prevention or treatment of cancer containing the extract of C. aureus.

Malignant tumor, the worst disease that threatens human health, is the most common cause of death in Western society after cardiovascular disease. In modern society, lung cancer due to the aging smoking population and air pollution has increased significantly, and the consumption of high-fat diets and the increase of environmental pollutants due to the westernization of diet have increased lung cancer, colon cancer, breast cancer and prostate cancer. The back is continuously increasing. Therefore, there is an urgent need for the creation of anti-cancer substances that can contribute to the promotion of human health, the improvement of healthy quality of life and the promotion of human health by enabling early prevention and treatment of cancer. Drugs developed for the treatment of cancer have low specificity for cancer cells due to the nonspecificity acting systemically along the bloodstream following systemic injection or oral administration. Therefore, there are many systemic side effects due to the administration of the drug, and there are disadvantages that many side effects appear compared to surgery or radiation therapy. The cancer treatment period using the existing anticancer drugs is a lot of cases to stop the treatment by causing various anticancer drug side effects by administering 3-5 days a week for 6 months to a year at 3-4 weeks intervals.

Existing chemical therapies that directly attack cancer cells to exert their effects are not only very strong side effects, but despite the non-specificity of the drawbacks, there is a limited clinical use. Many inventors are actively researching for a natural material having anticancer activity.

Boehmeria platanifolia Franch. & Sav. Is a perennial herb that grows at the edges of forests or in moist areas. The stem reaches 1m in height and dense short hairs. The leaves are opposite and broad ovate or ovate oblong, the tip is pointed like a tail and regular serrate at the edge. Flowers bloom pale green in July-August. The inflorescence runs under the stem and the female inflorescence runs above the stem. Fruits are achene, obovate, winged at the edges, hairy throughout. It grows in south of Hwanghaedo in Korea, and is distributed in Japan and China.

The inventors of the present invention, while studying the various physiological activities of hazelnut grass, completed the present invention by confirming that the leaf extract of hazelnut grass has an excellent killing effect on lung cancer cells.

Republic of Korea Registered Patent No. 10-0873372 (Invention name: Wang Moshi pool extract and anticancer agent containing the same, Applicant: BC World Pharmaceutical Co., Ltd. registered date: December 04, 2008) Republic of Korea Patent Publication No. 10-2014-0043263 (Invention: Composition for inhibiting angiogenesis, containing the extract of ramie grass as an active ingredient, Applicant: Korea Food Research Institute, Publication Date: April 09, 2014) Republic of Korea Patent Application Publication No. 10-2012-0000250 (Invention: Anti-cancer composition comprising the extract of Sesame leaf tree (Ｂｏｅｈｍｅｒｉａ ｓｐｉｃａｔａ Ｔｈｕｎｂ) Anticancer composition comprising the flower, Applicant: Hallym University Industry-University Cooperation, Publication Date: January 02, 2012)

Paramasivan Poornima (2014). Doxorubicin induced apoptosis was potentiated by neferine in human lung adenocarcima, A549 cells, Food and Chemical Toxicology, 68, 87-98. Maria Davoren (2007). In vitro toxicity evaluation of single walled carbon nanotubes on human A549 lung cells, Toxicology in Vitro, 21, 438-448.

An object of the present invention is to provide a composition for the prevention or treatment of cancer containing the extract of C. aureus.

The present invention relates to a composition for preventing or treating cancer containing Boehmeria platanifolia Franch. & Sav.

The Cannabis extract may be extracted by using C. C. C. alcohol or a mixed solution thereof as a solvent. The solvent may preferably be methanol.

The herbaceous extract may be a leaf extract of herbaceous herb.

The cancer may be a disease selected from lung cancer, colon cancer, cervical cancer, pituitary selection, brain tumor, gastric cancer, liver cancer, breast cancer, pancreatic cancer, uterine cancer, leukemia, esophageal cancer, prostate cancer, bladder cancer and ovarian cancer, preferably lung cancer Can be.

In addition, the present invention relates to a dietary supplement for cancer prevention or improvement containing the extract of Hawthorn.

EMBODIMENT OF THE INVENTION Hereinafter, this invention is demonstrated in detail.

The present invention relates to a composition for the prevention or treatment of cancer containing the extract of C. defoliation, the extract of the C. persimmon extract can be extracted using C. C. C. alcohol or a mixed solution thereof as a solvent. The C4 alcohol may be selected from the group consisting of methanol, ethanol, propanol, isopropanol, butanol and isobutanol.

Water, C1 ~ C4 alcohol or a mixed solution thereof used in the preparation of the seedling grass extract may be used 1 to 50 times the volume (1 ~ 50L based on 1kg), and preferably 5 to 50 A fold volume can be used. Extraction conditions of the seedling grass extract may be 1 minute to 48 hours at 20 ~ 100 ℃, preferably 1 to 18 hours at 40 ~ 80 ℃. The process may be repeated 1 to 4 times.

In addition, as a conventional method in the art, after dissolving the water, C1 ~ C4 alcohol or a mixed solution extract of the hazelnut grass in water 1 selected from the group consisting of n-hexane, methylene chloride, ethyl acetate and n-butanol Fractions can be prepared by further fractionation using more than one solvent.

More specifically, the hazelnut extract obtained by extracting and concentrating the hazelnut extract obtained by extracting and concentrating water, C1 to C4 alcohol or a mixed solvent thereof, preferably 1 to 1000 times the weight of the hazelnut extract, more Suspended by preferably adding 5 to 500 times, most preferably 10 to 50 times of water, and then adding the solvent selected from the group consisting of hexane, methylene chloride, ethyl acetate and n-butanol to the suspension. It can be prepared from ramie pool fractions.

More preferably, the n-hexane layer is obtained by suspending the extract of hazelnut grass obtained by extracting and extracting the hazelnut grass with water, C1-C4 alcohol or a mixed solvent thereof in water and then mixing with n-hexane. Concentrate of the methylene chloride layer obtained by removing the n-hexane layer and methylene chloride remaining in the remaining water layer, or concentration of ethyl acetate layer obtained by mixing the ethyl acetate in the remaining water layer after removing the methylene chloride layer. It may be a concentrate of the n-butanol layer obtained by mixing n-butanol with water and the remaining ethyl acetate layer by removing the ethyl acetate layer, or a concentrate of the remaining water layer by removing the butanol layer.

As a device for extracting the extract or fractions thereof, a conventional extractor, an ultrasonic pulverizer or a fractionator may be used. The soybean grass extract or fraction thus prepared may be dried under reduced pressure or lyophilized to remove the solvent. In addition, the cultivars extract or fractions can be purified using column chromatography.

According to the conventional method, the extract of the seedling grass is a known method used for the separate extraction of plant components, such as extraction with an organic solvent (alcohol, ether, acetone, etc.), hexane and water distribution, column chromatography, or the like. It can be used by fractionation or purification using a method suitably combined.

The chromatography may include silica gel column chromatography, LH-20 column chromatography, ion exchange resin chromatography, and medium pressure liquid chromatography. chromatography, thin layer chromatography (TLC), silica gel vacuum liquid chromatography, and high performance liquid chromatography.

In addition, the present invention provides a pharmaceutical composition for preventing or treating cancer, containing the extract of C. aureus or its fraction. The Cannabis extract or fractions thereof may be added as 0.001 to 30% by weight to the pharmaceutical composition of the present invention.

The pharmaceutical compositions may be used in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols and the like, oral formulations, external preparations, suppositories, and sterile injectable solutions, respectively, according to a conventional method. Carriers, excipients and diluents that may be included in the pharmaceutical 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. When formulated, diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrating agents and surfactants are usually used. Solid form preparations for oral administration include tablets, pills, powders, granules, capsules and the like, and such solid form preparations may contain at least one excipient such as starch, calcium carbonate, sucrose or It is prepared by mixing lactose and gelatin. In addition to simple excipients, lubricants such as magnesium stearate and talc are also used. Oral liquid preparations include suspensions, solvents, emulsions, and syrups, and may include various excipients, such as wetting agents, sweeteners, fragrances, and preservatives, in addition to commonly used simple diluents such as water and liquid paraffin. . Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized preparations, suppositories. As the non-aqueous solvent and suspending agent, propylene glycol, polyethylene glycol, vegetable oil such as olive oil, injectable ester such as ethyl oleate, and the like can be used. As the base of the suppository, witepsol, macrogol, tween 61, cacao butter, laurin butter, glycerogelatin and the like can be used.

The dosage of the pharmaceutical composition of the present invention will vary depending on the age, sex, weight of the subject to be treated, the specific disease or pathology to be treated, the severity of the disease or pathology, the route of administration and the judgment of the prescriber. Dosage determination based on these factors is within the level of skill in the art and generally dosages range from 0.01 mg / kg / day to approximately 2000 mg / kg / day. More preferred dosage is 1 mg / kg / day to 500 mg / kg / day. Administration may be administered once a day or may be divided several times. The dosage does not limit the scope of the invention in any aspect.

The pharmaceutical composition of the present invention can be administered to mammals such as rats, livestock, humans, etc. by various routes. All modes of administration can be expected, for example, by oral, rectal or intravenous, intramuscular, subcutaneous, intrauterine dural or cerebrovascular injections. Extracts or fractions of the present invention is a drug that can be used safely in long-term administration for the purpose of prevention because there is little toxicity and side effects.

In addition, the present invention provides a functional food for cancer prevention or amelioration comprising the extract or fractions of Hawthorn grass and food supplements acceptable food. The hazelnut extract may be added as 0.001 to 100% by weight to the health functional food of the present invention. The health functional food of the present invention includes the form of tablets, capsules, pills or liquids, and the food to which the extract of the present invention can be added includes, for example, various drinks, meats, sausages, breads, candy, Snacks, noodles, ice cream, dairy products, soups, ionic drinks, beverages, alcoholic beverages, gums, teas and vitamin complexes.

The present invention relates to a composition for the prevention or treatment of cancer containing the extract of C. defoliation, the pharmaceutical composition or functional food containing the extract of C. persimmon is very excellent in killing effect of lung cancer cells of various cancer-related diseases including lung cancer. It can be easily used for prevention, improvement and treatment.

Republic of Korea Patent No. 10-0873372 discloses that Wang Mosiful extract can be used as an anti-renal cancer agent, and Republic of Korea Patent Publication No. 10-2014-0043263 shows that the extract of Moshi grass inhibits angiogenesis, Korean Patent Laid-Open Publication No. 10-2012-0000250 discloses that the sesame leaf tree flower extract has an anti-cancer effect because it kills neuroblastoma or fibroblasts, but as in the present invention, the death of lung cancer cells of the leaf extract of Hazelnut grass The effect has not been disclosed at all, and the leaf extract of Hawthorn is the best in killing effect of lung cancer cells.

1 is a process chart showing the manufacturing process of the extract and fractions of the seedling grass.
Figure 2 is a graph showing the killing effect on the lung cancer cells of Hawthorn extract.

Hereinafter, a preferred embodiment of the present invention will be described in detail. However, the present invention is not limited to the embodiments described herein and may be embodied in other forms. Rather, it is provided to fully convey the spirit of the present invention to those skilled in the art so that the contents introduced herein are thoroughly and completely.

<Example 1. Preparation of Hawthorn Leaf Extract and Fractions>

1.28 kg of leaves of Boehmeria platanifolia Franch. & Sav. Were added to 14 L of methanol (MeOH) and refluxed for 6 hours. This operation was repeated three times, and the extraction filtrates were combined, and then concentrated under reduced pressure using a rotary concentrator to obtain 99.78 g of methanol extract. The methanol extract was dispersed again in water and then fractionally extracted using n-hexane, CH ₂ Cl ₂ , EtOAc, n-BuOH according to polarity. As a result, 17.6 g of n-hexane fraction, 1.24 g of CH ₂ Cl ₂ fraction, 4.38 g of EtOAc fraction, and 11.1 g of n-BuOH fraction were obtained, and the final residue was collected as an Aqueous fraction (water residue fraction). This fractionation process is shown in FIG. 1.

<Example 2. Lung cancer cell killing effect of Hawthorn leaf extract>

Confirmation of the death effect of lung cancer cells was confirmed by MTT assay. 1 x 10 ⁴ cells / 100 μl of A549 cells (human lung carcinoma cell line, sold by the Korea Cell Line Bank) were added to a 6 well plate and incubated for 24 h in an incubator. After removing the media in the plate 2 times the sample, positive control (adriamycin) 100 ㎕ treated for 48h incubation in the incubator, remove the media in the plate, 0.2 mg / ml MTT treated with 100 ㎕ 3- Incubation in an incubator for 4 h. Next, the MTT solution was removed from the plate, and DMSO was added thereto, and then shaken at 1 mm amplitude for 5 seconds using a microplate reader (Tecan, Switzerland). At this time, the control group was a solvent control (Solvent control), the positive control was adriamycin 2 μM, each sample was treated with the concentration of the leaves extract of Hawthorn grass obtained in Example 1. Evaluation of cytotoxicity (anticancer activity) was expressed as a relative ratio when the survival rate of the control group was 100%.

The results are shown in FIG. 2. Referring to the results of FIG. 2, it was confirmed that the extract of C. aphids kills A549 cells, which are lung cancer cell lines, in a concentration-dependent manner. In addition, the two fractions, one fraction ramie extract was found to CH ₂ Cl ₂ fractions is highest.

<Example 3. Boehmeria Comparison of Lung Cancer Cell Killing Effects of Plant Leaf Extracts

Next, Boehmeria platanifolia Franch. & Sav. Leaf extracts, and leaf extracts of other Boehmeria genus plants were checked by concentration in Example 2 to determine the concentration (IC ₅₀ ) that inhibits cell death by 50%. .

Target plant IC ₅₀ of leaf extract (μl / ml) Hawthorn ( Boehmeria platanifolia ) 16.4 ± 1.0 Royal Grasshopper ( Boehmeria pannosa ) 100.0 ± 2.5 Ramie ( Boehmeria nivea ) 40.8 ± 2.9

Referring to the results of Table 1, it was confirmed that the leaf extract of hazelnut grass repeatedly showed a similar good effect of the death of lung cancer cells as in Example 1, 3 to 4 compared to the leaf extract of other plants of the genus Boehmeria It can be seen that remarkably superior over two times, the leaf extract of the cultivars of the present invention can be confirmed that it is the best composition for the prevention / improvement / treatment of lung cancer.

Formulation Example 1 Pharmaceutical Formulation-Preparation of Tablet

200 g of the methanol extract of the leaves of the cultivars of the present invention was mixed with 175.9 g of lactose, 180 g of potato starch, and 32 g of colloidal silicic acid. 10% gelatin solution was added to the mixture, which was then ground and passed through a 14 mesh sieve. It was dried and the mixture obtained by adding 160 g of potato starch, 50 g of talc and 5 g of magnesium stearate was made into a tablet.

Preparation Example 2 Food Preparation

Formulation Example 2-1. Preparation of Cooking Seasonings

Methanol extract of the foliar leaves of the present invention was added to the cooking seasoning in 1% by weight to prepare a cooking seasoning for health promotion.

Formulation Example 2-2. Manufacture of Flour Food

Methanol extract of the foliar leaves of the present invention was added to the flour in 0.1% by weight, and using this mixture to prepare bread, cakes, cookies, crackers and noodles to produce health foods.

Formulation Example 2-3. Preparation of soups and gravy

Methanol extract of the leaves of the cultivars of the present invention was added to the soup and gravy 0.1% by weight to prepare a soup and gravy for health promotion.

Formulation Example 2-4. Manufacture of dairy products

Methanol extract of the foliar leaves of the present invention was added to the milk at 0.1% by weight, and the milk was used to prepare various dairy products such as butter and ice cream.

Formulation Example 2-5. Vegetable Juice Manufacturing

0.5 g of methanol extract of the leaves of the cultivars of the present invention was added to 1,000 ml of tomato juice or carrot juice to prepare vegetable juice for health promotion.

Formulation Example 2-6. Fruit juice manufacturing

0.1 g of methanol extract of the leaves of the cultivars of the present invention was added to 1,000 ml of apple juice or grape juice to prepare fruit juice for health promotion.

Claims (6)

A composition for the prevention or treatment of lung cancer, characterized in that it contains an extract of Boehmeria platanifolia Franch. & Sav. The method of claim 1,
The extract of C. falciparum is a composition for the prevention or treatment of lung cancer, characterized in that the extract of C. vulgaris in water, C 1 ~ C 4 alcohol or a mixed solution thereof as a solvent. delete Health functional food for the prevention or improvement of lung cancer, characterized in that it contains the extract of Boehmeria platanifolia Franch. & Sav. The method of claim 4, wherein
The hazelnut extract is a health functional food for preventing or improving lung cancer, characterized in that the extract of hazelnut grass, water, C1 ~ C4 alcohol or a mixture thereof as a solvent. delete

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