WO2022216107A1 - Composition anticancéreuse comprenant un extrait d'elaeocarpus sylvestris ou un produit purifié de celui-ci en tant que principe actif - Google Patents

Composition anticancéreuse comprenant un extrait d'elaeocarpus sylvestris ou un produit purifié de celui-ci en tant que principe actif Download PDF

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WO2022216107A1
WO2022216107A1 PCT/KR2022/005120 KR2022005120W WO2022216107A1 WO 2022216107 A1 WO2022216107 A1 WO 2022216107A1 KR 2022005120 W KR2022005120 W KR 2022005120W WO 2022216107 A1 WO2022216107 A1 WO 2022216107A1
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dampalsu
cancer
extract
purified product
minutes
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PCT/KR2022/005120
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English (en)
Korean (ko)
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엄성운
오영지
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주식회사 더퓨쳐
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Priority claimed from KR1020220043755A external-priority patent/KR102455690B1/ko
Publication of WO2022216107A1 publication Critical patent/WO2022216107A1/fr

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    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105—Plant extracts, their artificial duplicates or their derivatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Definitions

  • the present invention relates to an anticancer composition
  • an anticancer composition comprising an extract of Dampalsu ( Elaeocarpus sylvestris ) or a purified product thereof as an active ingredient.
  • Cancer is currently one of the diseases that cause the highest number of deaths worldwide, and the cancer incidence rate is expected to further increase as the age of cancer onset is gradually decreasing while the average lifespan is gradually increasing.
  • a typical cancer treatment method is chemotherapy, but it can damage not only cancer cells but also rapidly dividing and proliferating normal cells, so the target for cancer cells is low. , nausea, and diarrhea may occur.
  • colorectal cancer is a major cause of cancer incidence and mortality in adult males and females worldwide, and the incidence of colorectal cancer is rapidly increasing in Korea due to the westernization of diet.
  • Colorectal cancer is known to occur mainly in the elderly, and as the population of Korea gradually ages and food culture becomes westernized, there is a growing interest in research to find ways to prevent and treat it. have.
  • Renal cell carcinoma refers to renal cell cancer that occurs mostly in the parenchyma (composed of the medulla and cortex), which is the part of the kidney where urine-producing cells are gathered. Although there are genetic factors as risk factors for kidney cancer, Common examples include smoking and excessive fat intake. In addition, it is known that the incidence of tumors is high in patients undergoing dialysis for a long time. Kidney cancer has almost no symptoms when the size of the tumor is small, and symptoms appear only when the tumor grows to a certain extent and pushes the organs away.
  • kidney cancer For the treatment of kidney cancer, a surgical operation in which the kidney and surrounding normal tissues are extensively removed is common. If the tumor is not large, laparoscopic resection is performed. Other treatment methods include immunotherapy, hormone therapy, chemotherapy, radiation therapy, etc., but the therapeutic effect is not known to be large, so there is no treatment with a definite effect other than surgical operation.
  • another object of the present invention is to provide a food composition for preventing or improving cancer containing an extract or a purified product thereof as an active ingredient.
  • Dampalsu Elaeocarpus sylvestris It is to provide a method for preventing or treating cancer, comprising administering to an individual an extract or a purified product thereof.
  • another object of the present invention is to provide a use of a dampalsu ( Elaeocarpus sylvestris ) extract or a purified product thereof for the manufacture of a pharmaceutical or food for the prevention, improvement or treatment of cancer.
  • the Dampalsu extract of the present invention or a purified product thereof has an apoptosis effect on cancer cells, it is used as an anticancer composition.
  • FIG. 2 is a chromatogram obtained by performing Prep HPLC on the filtrate of the undiluted dampalsu leaf extract of Example 3.
  • FIG. 2 is a chromatogram obtained by performing Prep HPLC on the filtrate of the undiluted dampalsu leaf extract of Example 3.
  • Figure 3 shows the cytotoxicity to the renal cancer cell line for the samples of Example 1 and Example 3 Dampalsu.
  • Figure 4 shows the cytotoxicity to the renal cancer cell line targeting the dampalsu samples of Examples 2-3 and 4-3.
  • Example 6 shows the cytotoxicity of the dampalsu sample of Example 5-2 to colon cancer cell lines and normal intestinal system cell lines.
  • FIG. 8 shows cytotoxicity to breast cancer cell lines in Dampalsu samples of Examples 5-1 and 5-2.
  • the present invention provides a pharmaceutical composition for treating or preventing cancer containing an extract or a purified product thereof as an active ingredient.
  • the term "dampalsu ( Elaeocarpus sylvestris )" of the present invention is an evergreen tree growing at the southern foot of Jeju Island, about 20 m in height, and also inhabits subtropical regions including southern China and Japan. Since its efficacy is hardly known, it can be said that it is a material with very high R&D rarity.
  • the composition may be applied to extraction of dried and crushed dampalsu, and may include leaves, stems, roots, flowers, or both of dampalsu. Specifically, the leaves or stems of dampalsu may be used.
  • extract refers to an extract obtained by extraction treatment, a dilution or filtrate of the extract, or a concentrate of the filtrate of the extract, re-filtrate of the concentrate, the extract, dilution, filtrate, concentrate, Or the extract obtained by drying the re-filtrate, the extract, the diluent, the filtrate, the concentrate, the adjusted or purified product of the re-filtrate, or a mixture thereof, and the extract of all formulations that can be formed using the extract itself and the extract.
  • Drying of the extract in the present invention may be carried out by a known method in the range in which useful components from the harvested plant are not destroyed, for example, it may be carried out by a method of natural drying in the shade.
  • crushing or pulverization can be pulverized by crushing or pulverizing to an extent that useful components of plants can be sufficiently extracted in the subsequent extraction process.
  • the drying, crushing, or pulverizing processes may be performed in reverse order or repeated if necessary.
  • the extraction method is not particularly limited, and extraction may be performed according to a method commonly used in the art.
  • the Dampalsu ( Elaeocarpus sylvestris ) extract can be obtained by extraction with water, C 1 to C 4 lower alcohol or a mixed solvent thereof, specifically, Dampalsu leaves or stems with water, C 1 to C 4 alcohol or It may be extracted with these mixed solvents. More specifically, the leaves or stems of Dampalsu may be extracted with water or methanol.
  • the lower alcohol may be ethanol or methanol, and the methanol may be 50 to 70% methanol.
  • the "dampalsu extract” may be a concentrate obtained by concentrating the filtrate of the extract of Dampalsu, and the "purified Dampalsu” may be obtained by purifying the re-filtrate obtained by filtering the concentrate.
  • the purified product of the Dampalsu extract may be a purified product of the Dampalsu stem extract, specifically, the purified water of the methanol extract of the Dampalsu stem.
  • the retention time may be one or more fractions selected from the group consisting of 2-8 minutes, 16-22 minutes, 22-28 minutes, 27-35 minutes, and 34-40 minutes, specifically, the retention time of the sample This may be a fraction that is 22 to 28 minutes.
  • the purified product of the Dampalsu extract may be the purified product of the Dampalsu leaf extract, and specifically, it is a purified product of the methanol extract of Dampalsu leaf until a sample is added and a chromatogram peak appears in the process of performing HPLC.
  • the retention time of the sample may be one or more fractions selected from the group consisting of 2-5 minutes, 18-26 minutes, 26-33 minutes, and 33-40 minutes, and specifically, the retention time of the sample is 26- It may be a fraction that is 33 minutes.
  • composition of the present invention may further include a fraction of the dampalsu extract in addition to the dampalsu extract or a purified product thereof.
  • fraction refers to a result obtained by performing fractionation in order to separate a specific component or a specific component group from a mixture including various components.
  • the fractionation method for obtaining the fraction in the present invention is not particularly limited, and may be performed according to a method commonly used in the art.
  • Non-limiting examples of the fractionation method include a method of obtaining a fraction from the extract by treating the extract with a predetermined solvent ( Elaeocarpus sylvestris ).
  • the kind of solvent used to obtain the fraction in the present invention is not particularly limited, and any solvent known in the art may be used.
  • Non-limiting examples of the fractionation solvent include water, alcohol having 1 to 4 carbon atoms, hexane, ethyl acetate, chloroform, butanol, or a mixed solvent thereof.
  • active ingredient means a component that can exhibit the desired activity alone or can exhibit activity together with a carrier that is not active by itself.
  • cancer refers to or describes a physiological condition in a mammal that is generally characterized by unregulated cell growth.
  • “Cancer” refers to a condition in which a problem occurs in the control function of normal division, differentiation and death of cells, so that it proliferates abnormally, invades surrounding tissues and organs, forms a mass, and destroys or deforms the existing structure.
  • the cancer is not particularly limited thereto, as long as the symptoms can be alleviated, alleviated, improved or treated by the dampalsu extract or a purified product thereof provided in the present invention, but specifically, gastric cancer, colon cancer, small intestine cancer, breast cancer, liver cancer, And it may be one or more diseases selected from the group consisting of kidney cancer, more specifically, it may be selected from the group consisting of kidney cancer, colorectal cancer and breast cancer.
  • the composition exhibits cytotoxicity to the cancer cells and has an anticancer effect, but has no or weak toxicity to normal cells. In particular, there is little or no toxicity to normal intestinal system cells, specifically human intestinal epithelial cells. In addition, it is not toxic to normal human skin cells, specifically human dermal fibroblasts.
  • prevention refers to any act of inhibiting or delaying cancer by administering a composition comprising the dampalsu extract or a purified product thereof.
  • treatment refers to any action in which the symptoms of cancer are improved or beneficially changed by administering the composition of the dampalsu extract or a purified product thereof.
  • composition of the present invention is administered in a pharmaceutically effective amount.
  • pharmaceutically effective amount means an amount sufficient to treat a disease at a reasonable benefit/risk ratio applicable to medical treatment, and the effective dose level is determined by the type and severity of the subject, age, sex, drug activity, sensitivity to drugs, administration time, administration route and excretion rate, duration of treatment, factors including concomitant drugs, and other factors well known in the medical field.
  • the extract or fraction may be administered as an active ingredient at a dose of 0.001 to 500 mg/kg per day, specifically 0.1 to 100 mg/kg, and the administration may be administered once or several times a day.
  • the pharmaceutical composition of the present invention may include the extract or fraction in an amount of 0.001 to 50% by weight based on the total weight of the composition.
  • composition of the present invention may be administered as an individual therapeutic agent or in combination with other therapeutic agents, and may be administered sequentially or simultaneously with conventional therapeutic agents. and may be administered single or multiple. Taking all of the above factors into consideration, it is important to administer an amount that can obtain the maximum effect with a minimum amount without side effects, and can be easily determined by those skilled in the art.
  • the pharmaceutical composition for preventing or treating cancer of the present invention may include a pharmaceutically acceptable carrier, excipient or diluent in addition to the active ingredients described above.
  • the carrier, excipient and diluent include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, gum acacia, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, microcrystalline cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil.
  • the pharmaceutical composition of the present invention can be formulated in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, etc., external preparations, suppositories, or sterile injection solutions according to conventional methods, respectively. have. Specifically, in the case of formulation, it can be prepared using a diluent or excipient such as a filler, a weight agent, a binder, a wetting agent, a disintegrant, and a surfactant commonly used.
  • Solid preparations for oral administration include, but are not limited to, tablets, pills, powders, granules, capsules, and the like.
  • Such a solid preparation may be prepared by mixing at least one or more excipients, for example, starch, calcium carbonate, sucrose, lactose, gelatin, and the like.
  • excipients for example, starch, calcium carbonate, sucrose, lactose, gelatin, and the like.
  • lubricants such as magnesium stearate and talc may also be used.
  • It can be prepared by adding various excipients, for example, wetting agents, sweetening agents, fragrances, preservatives, and the like, in addition to liquids for oral use and liquid paraffin.
  • Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solutions, suspensions, emulsions, lyophilized formulations and suppositories.
  • Non-aqueous solvents and suspending agents include propylene glycol, polyethylene glycol, vegetable oils such as olive oil, injectable esters such as ethyl oleate, and the like.
  • As the base of the suppository Witepsol, Macrogol, Tween 61, cacao butter, laurin fat, glycerogelatin, etc. may be used.
  • the pharmaceutical composition of the present invention may be administered orally or parenterally (eg, intravenously, subcutaneously, intraperitoneally or topically) according to a desired method, and the dosage may vary depending on the condition and weight of the patient, and the disease. Although it varies depending on the degree, drug form, administration route and time, it may be appropriately selected by those skilled in the art.
  • the Dampalsu ( Elaeocarpus sylvestris ) extract has an anticancer effect by killing kidney cancer or colon cancer cells. Therefore, the dampalsu extract or a purified product thereof of the present invention can be very usefully used in a pharmaceutical composition for treating or preventing cancer.
  • the present invention provides a food composition for preventing or improving cancer containing an extract or a purified product thereof as an active ingredient.
  • Dampalsu Elaeocarpus sylvestris
  • a purified product thereof, cancer, and prevention are the same as described above.
  • the term “improvement” refers to any action that at least reduces the parameters related to the condition to be treated, for example, the severity of symptoms by administration of a composition comprising the dampalsu extract or a purified product thereof of the present invention.
  • the composition of the present invention When used as a food additive, the composition may be added as it is or used with other foods or food ingredients, and may be appropriately used according to a conventional method.
  • the food composition of the present invention may include the form of pills, powders, granules , needles, tablets, capsules or liquids, etc. There are no restrictions. Examples of foods to which the above substances can be added include meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gums, dairy products including ice cream, various soups, beverages, tea, drinks, Alcoholic beverages and vitamin complexes are available.
  • ingredients may be added to the food composition in addition to the dampalsu ( Elaeocarpus sylvestris ) extract or a purified product thereof, and the type thereof is not particularly limited.
  • the type thereof may contain, as an additional ingredient, various herbal extracts, food-logically acceptable food supplements or natural carbohydrates, such as conventional food, but is not limited thereto.
  • food supplement additive refers to a component that can be supplementally added to food, and is added to prepare food of each formulation, and those skilled in the art can appropriately select and use it.
  • food supplement additives include various nutrients, vitamins, minerals (electrolytes), synthetic flavoring agents and flavoring agents such as natural flavoring agents, coloring agents and fillers, pectic acid and salts thereof, alginic acid and salts thereof, organic acids, protective colloidal thickeners , pH adjusters, stabilizers, preservatives, glycerin, alcohol, carbonation agents used in carbonated beverages, etc., but the above examples are not limited to the types of food supplement additives of the present invention.
  • Examples of the natural carbohydrate include monosaccharides such as glucose and fructose; disaccharides such as maltose and sucrose; and polysaccharides such as dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol, and erythritol. hygin, etc.) and synthetic flavoring agents (saccharin, aspartame, etc.) may be advantageously used.
  • the food composition of the present invention may include a health functional food.
  • health functional food refers to food manufactured and processed in the form of tablets, capsules, powders, granules, liquids, pills, etc. using raw materials or ingredients useful for the human body.
  • functionality refers to obtaining useful effects for health purposes, such as regulating nutrients or physiological effects on the structure and function of the human body.
  • the health functional food of the present invention can be prepared by a method commonly used in the art, and during the manufacture, it can be prepared by adding raw materials and components commonly added in the art. In addition, unlike general drugs, there are no side effects that may occur when taking the drug for a long period of time by using food as a raw material, and it can be excellent in portability.
  • the mixed amount of the active ingredient may be appropriately determined according to the purpose of use (prevention, health or therapeutic treatment).
  • the active ingredient of the present invention may be added in an amount of 0.01 to 50% by weight, preferably 0.1 to 10% by weight of the raw material composition, but is not limited thereto.
  • the above amount may be used below the above range.
  • the present invention provides a method for preventing or treating cancer , comprising administering an extract or a purified product thereof to a subject.
  • the term "individual” refers to all animals, including humans, who have developed cancer. Including cattle, pigs, sheep, chickens, dogs, mammals including humans, birds, etc., the growth of cancer is inhibited by the Elaeocarpus sylvestris extract of the present invention or a purified product thereof, thereby preventing cancer
  • Subjects to be treated include without limitation.
  • the present invention provides the use of a dampalsu ( Elaeocarpus sylvestris ) extract or a purified product thereof for the manufacture of a pharmaceutical or food for the prevention, improvement or treatment of cancer.
  • the methanol extract stock solution of Dampalsu stem obtained in Example 1 was filtered with a PTFE (Polytetrafluoroethylene) Syringe Filter (0.45 ⁇ m pore size, 25 mm diameter).
  • PTFE Polytetrafluoroethylene
  • Solvent Solvent A; DI Water, solvent B; Methanol
  • the methanol extract stock solution of Dampalsu leaf obtained in Example 3 was filtered with a PTFE (Polytetrafluoroethylene) Syringe Filter (0.45 ⁇ m pore size, 25 mm diameter).
  • PTFE Polytetrafluoroethylene
  • Injection volume 0.8mL (filtrate of dampalsu leaf extract stock solution)
  • Solvent Solvent A; DI Water, solvent B; Methanol
  • FIG. 2 is a chromatogram obtained by performing Prep HPLC on the filtrate of the undiluted dampalsu leaf extract of Example 3.
  • FIG. The red (low) peak is the result of analysis at 254 nm
  • the blue (high) peak is the result of the analysis at 280 nm.
  • 1, 2 by retention time , 3, 4 Peaks corresponding to four fractions were obtained, and these were fractionated to obtain four purified samples.
  • the retention times for the four fractions are shown in Table 4.
  • Human kidney cancer cell line A489 and human dermal fibroblast Detroit 551 were purchased from Korean Cell Line Bank (Seoul, Korea).
  • A489 and Detroit 551 cells were cultured in MEM medium at 37° C. and 5% CO 2 condition. 10% fetal bovine serum (FBS) and antibiotics (100 U/mL penicillin, 0.1 mg/mL streptomycin) were added to each medium, and 1% non-essential amino acid was added to the MEM medium for Detroit 551 cells. was injected.
  • FBS fetal bovine serum
  • antibiotics 100 U/mL penicillin, 0.1 mg/mL streptomycin
  • the number of cells per well was aliquoted in a 96-well plate to 1.5 ⁇ 10 4 , and cultured for 24 to 48 hours. Then, the treatment medium was removed, and 100 ⁇ L of 0.5 mg/mL MTT solution was added to each well, followed by reaction at 37° C. for about 1 to 2 hours. The resulting MTT formazan was dissolved in 100 ⁇ L DMSO and absorbance was measured at 550 nm with a microplate reader (SpectraMax i3x, Molecular Devices, CA, USA) to evaluate cell viability.
  • Example 3 The methanol extract of dampalsu stem extract of Example 1, the methanol extract of dampalsu leaf of Example 3, and the purified product of the dampalsu stem extract of Example 2-3 (stem 3), Example The purified product (leaf 3) of the dampalsu leaf extract of 4-3 was treated with the renal cancer cell line A489 and cytotoxicity was evaluated.
  • Figure 3 shows the cytotoxicity to the renal cancer cell line for the samples of Example 1 and Example 3 Dampalsu.
  • the dampalsu leaf extract stock solution of Example 3 inhibited the viability of the renal cancer cell line by about 35% at 62.5 ⁇ g/mL, but the stock solution of Dampalsu leaf extract of Example 1 showed 10% inhibition of cell line growth at 62.5 ⁇ g/mL. , and inhibited the survival rate of renal cancer cell lines from 125 ⁇ g/mL to about 37%. Therefore, at the same concentration, the undiluted dampalsu leaf extract showed higher cytotoxicity to kidney cancer cell lines than the undiluted stem extract.
  • Figure 4 shows the cytotoxicity to the renal cancer cell line targeting the dampalsu samples of Examples 2-3 and 4-3.
  • the purified product of the dampalsu leaf extract stock solution of Example 3 and the dampalsu leaf extract of Example 4-3 showed high cytotoxicity against kidney cancer cell lines compared to the purified product of the dampalsu stem extract stock solution and the dampalsu stem extract, thereby increasing the anticancer effect. was found to be high.
  • Detroit 551 cells were treated with the methanol extracts of the stem extracts of Dampalsu stem of Example 1 and the methanol extracts of the leaves of Dampalsu leaves of Example 3, and cytotoxicity was evaluated.
  • the undiluted dampalsu leaf extract of Example 3 had no toxicity to human dermal fibroblasts, and rather induced the proliferation of human dermal fibroblasts at 500 ⁇ g/mL.
  • the undiluted dampalsu stem extract of Example 1 induced cell proliferation at a low concentration, and inhibited the survival rate of human dermal fibroblasts at 125 ⁇ g/mL.
  • HT-29 and normal intestinal system cell line INT-407 were purchased from the American Type Culture Collection (Manassas, VA, USA).
  • HT-29 and INT-407 cells were cultured in DMEM and MEM media, respectively, at 37°C and 5% CO 2 conditions.
  • 10% fetal bovine serum (FBS) and antibiotics 100 U/mL penicillin, 0.1 mg/mL streptomycin
  • FBS fetal bovine serum
  • antibiotics 100 U/mL penicillin, 0.1 mg/mL streptomycin
  • 1% non-essential amino acid non-essential amino acid
  • HT-29 and INT-407 cells were aliquoted in a 96-well plate at a volume of 1.5 ⁇ 104 per well, incubated for 24 to 48 hours, and then exchanged with a serum-free medium containing the sample for 24 hours. further processed. After that, the treatment medium was removed, and 100 ⁇ L of 0.5 mg/mL MTT solution was added to each well, followed by reaction at 37° C. for about 1 to 2 hours. Cell viability was evaluated by dissolving the generated MTT formazan in 100 ⁇ L DMSO and measuring the absorbance at 550 nm with a microplate reader.
  • Example 6 shows the cytotoxicity to colon cancer cell lines and normal intestinal system cell lines for the hot water extract sample of Dampalsu leaf of Example 5-2.
  • the hot water extract of Dampalsu leaf of Example 5-2 inhibited the cell viability of the colon cancer cell line (HT-29) compared to the normal intestinal system cell line (INT-407). Therefore, it can be seen that the hot water extract of Dampalsu leaf of Example 5-2 has little toxicity to normal intestinal system cell lines (human intestinal epithelial cells, INT-407) and cytotoxicity to colorectal cancer cell lines, indicating that it has an anticancer effect. there was.
  • Cytotoxicity to colon cancer cell lines was evaluated using the hot water extract of Dampalsu stem of Example 5-1 and the hot water extract of Dampalsu leaf of Example 5-2.
  • FIG. 7 is a graph showing the cytotoxicity to colorectal cancer cell lines of the hot water extract samples of Examples 5-1 and 5-2.
  • the hot water extract of Dampalsu stem of Example 5-1 and the hot water extract of Dampalsu leaf of Example 5-2 inhibited the cell viability of the colon cancer cell line (HT-29) even at a low concentration of 3.125 to 12.5 ⁇ g/Ml. Therefore, both the hot water extract of Dampalsu stem of Example 5-1 and the hot water extract of Dampalsu leaf of Example 5-2 showed cytotoxicity to colon cancer cell lines, thereby confirming that they had anticancer effects.
  • the human breast cancer cell line MCF-7 was purchased from the American Type Culture Collection (Manassas, VA, USA). For cell culture and toxicity evaluation, MCF-7 cells were cultured in DMEM medium at 37° C. and 5% CO 2 condition. 10% fetal bovine serum (FBS) and antibiotics (100 U/mL penicillin, 0.1 mg/mL streptomycin) were added to each medium.
  • FBS fetal bovine serum
  • antibiotics 100 U/mL penicillin, 0.1 mg/mL streptomycin
  • the number of cells per well was aliquoted in a 96-well plate to 1.5 ⁇ 10 4 and cultured for 24 to 48 hours. Then, the treatment medium was removed, and 100 ⁇ L of 0.5 mg/mL MTT solution was added to each well, followed by reaction at 37° C. for about 1 to 2 hours. The resulting MTT formazan was dissolved in 100 ⁇ L DMSO and absorbance was measured at 550 nm with a microplate reader (SpectraMax i3x, Molecular Devices, CA, USA) to evaluate cell viability.
  • Cytotoxicity to breast cancer cell lines was evaluated using the hot water extract of Dampalsu stem of Example 5-1 and the hot water extract of Dampalsu leaf of Example 5-2.
  • FIG. 8 shows cytotoxicity to breast cancer cell lines in Dampalsu hot water extract samples of Examples 5-1 and 5-2.
  • the extract or the purified product derived from the leaf or stem of Dampalsu had little or no cytotoxicity to normal cells, or rather induces proliferation, and specifically induces apoptosis in kidney cancer, breast cancer, and colorectal cancer.

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Abstract

La présente invention concerne une composition pharmaceutique destinée à traiter ou prévenir un cancer, et une composition alimentaire destinée à prévenir ou soulager un cancer, dont chacune comprend un extrait d'Elaeocarpus sylvestris ou un produit purifié de celui-ci en tant que principe actif. L'extrait d'Elaeocarpus sylvestris ou un produit purifié de celui-ci possède un effet cytotoxique sur les cellules cancéreuses et peut donc être utilisé en tant que principe actif dans des compositions pharmaceutiques et des compositions alimentaires, anticancéreuses.
PCT/KR2022/005120 2021-04-09 2022-04-08 Composition anticancéreuse comprenant un extrait d'elaeocarpus sylvestris ou un produit purifié de celui-ci en tant que principe actif WO2022216107A1 (fr)

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KR20210046652 2021-04-09
KR10-2021-0046652 2021-04-09
KR1020220043755A KR102455690B1 (ko) 2021-04-09 2022-04-08 담팔수 추출물 또는 이의 정제물을 유효성분으로 함유하는 항암용 조성물
KR10-2022-0043755 2022-04-08

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