KR20130082250A - Composition for preventing or improving the hypertension containing parthenocissus tricuspidata extract - Google Patents

Abstract

PURPOSE: A composition for cardiovascular disease treatment or prevention including Parthenocissus Tricuspidata as an active ingredient is provided to have an effective treatment or prevention of cardiovascular disease by suppressing the transformation of angiotensin conversing enzyme to angiotensin II of the angiotensin. CONSTITUTION: A composition for treating or preventing a cardiovascular disease comprises Parthenocissus Tricuspidata as an active ingredient. The cardiovascular disease is hypertension or the hypertensive heart disease. The Parthenocissus Tricuspidata extract is extracted from water, 50-100% carbon number 1-4 of alcohol, ethyl acetate, hexane, chloroform, methylene chloride, and dichloromethane. A food composition for prevention and improvement of cardiovascular disease comprise Parthenocissus Tricuspidata extract as the active ingredient.

Description

COMPOSITION FOR PREVENTING OR IMPROVING THE HYPERTENSION CONTAINING PARTHENOCISSUS TRICUSPIDATA EXTRACT}

The present invention relates to a composition for treating or preventing hypertension.

With the rapid economic development, the disease pattern has changed greatly, and the importance of circulatory diseases such as hypertension, ischemic heart disease and cerebrovascular disease is increasing. According to the latest statistics released by the National Statistical Office, the proportion of elderly people aged 65 or older accounted for 9.1% of the total population in 2005, and the share of the under-14 age group is gradually decreasing. And 7.2%, indicating that our society has already entered an aging society. Also, as of 2003, the average age of Koreans is 77.5, and the elderly population is rapidly increasing. Meanwhile, Korea's GNI per capita announced by the National Statistical Office was $ 14,162 in 2004, and it is increasing by more than 10% every year.

Due to these social changes, death toll from infectious diseases, the leading cause of death in the past, is shrinking rapidly, while the number of deaths from degenerative diseases such as cancer, hypertension, cerebrovascular disease, and diabetes is steadily increasing.

Hypertension is the most common cause of chronic cardiovascular diseases. Although it is relatively uncomplicated, it may lead to fatal complications such as stroke, heart failure, and coronary artery disease. Therefore, more active management and treatment are required. In particular, essential hypertension accounts for 80% of hypertension and is a complex product of genetic factors and environmental factors, including family history of hypertension, race, salt intake, insulin resistance, obesity, excessive drinking and aging I think. The general physiological activity of the renin-angiotensin system (RAS), an important mechanism of blood pressure increase, is as follows.

First, the renin-angiotensin system is activated by the decrease of blood flow, sodium, and sympathetic nervous system in the kidney, and the renin secreted from the juxtaglomerular cell of the renal artery decomposes angiotensin into angiotensin I, Is converted to angiotensin II by an angiotensin converting enzyme (ACE). The angiotensin II regulates blood pressure through neuromodulation and increased synthesis of aldosterone.

Therefore, an inhibitor of angiotensin converting enzyme or an angiotensin converting enzyme inhibitor (ACE inhibitor) has been reported to treat or prevent cardiovascular diseases or nephropathy such as hypertension, heart disease, arteriosclerosis or cerebral hemorrhage. It is progressing. Specifically, the results of various clinical studies and clinical tests confirming that it is possible to effectively reduce chronic kidney disease, arteriosclerosis, heart attack, and mortality thereof are reported.

Currently, based on these results, it has been found that chemically synthesized compounds such as ramipril, captopril, enarapil, risinopril, fosinoril, spirapril, Many angiotensin converting enzyme inhibitors have been used as antihypertensive agents. However, these compounds are easily degraded in pharmaceutical dosage forms, which means they are not only stable, but also act on other cells, causing loss of systemic strength, reduced white blood cells, angioedema, liver failure, vomiting, dry cough, headache, and anorexia. It has been reported that there are problems related to side effects, such as causing abnormalities in taste and taste.

In order to solve this problem, there is an urgent need to develop an angiotensin converting enzyme inhibitor derived from a natural substance which does not cause side effects and ensures safety. In particular, in the case of an angiotensin converting enzyme inhibitor derived from a natural product used as a food, it is easy to ensure safety, the need for research on this is increasing.

KR 20090030831 A KR 0587179 B KR 20040072193 A

In order to solve the problems of the prior art as described above, the present invention effectively inhibits angiotensin converting enzyme, has an ability to lower blood pressure, is useful for the treatment, prevention or improvement of hypertension and does not cause side effects such as natural products, and stability An object of the present invention is to provide an effective ingredient for treating or preventing high blood pressure.

The present invention provides a composition for treating or preventing cardiovascular diseases comprising ivy extract as an active ingredient to achieve the above object.

In addition, in order to achieve the above object, the present invention provides a food composition for improving or preventing cardiovascular disease comprising ivy extract as an active ingredient. Examples of the food composition of the present invention include food, food additives, beverages or beverage additives.

In the present invention, the cardiovascular disease is a disease including heart disease and vascular disease, and in a crowd consisting of hypertension, hypertensive heart disease, heart disease, arrhythmia, stroke, thrombosis, angina pectoris, heart failure, myocardial infarction, atherosclerosis and arteriosclerosis It may be any one selected, preferably hypertension or hypertensive heart disease.

Reported data show that angiotensin II acts on four AT receptors in the adrenal glands, vascular smooth muscle cells, kidneys, heart, etc., and they release vasoconstriction, aldosterone and vasopressin release. In addition, by causing the absorption of sodium in the tubules and decreased blood flow to the kidney, various lesions can be caused in the cardiovascular, renal and central nervous areas.

In addition, angiotensin converting enzyme is one of the dicarboxyl peptides found in the proximal tubules of the blood vessels and kidneys, endothelial, heart, lung, activated macrophages, brain tissue, etc., by converting angiotensin to angiotensin II, thereby vascular contraction. In addition, aldosterone and vasopressin release, the absorption of sodium in the tubules and decreased blood flow to the kidneys have been reported to cause various lesions in the cardiovascular, renal and central nervous areas.

Therefore, angiotensin converting enzyme inhibitors or angiotensin converting enzyme inhibitors (ACE inhibitors) are reported to be able to treat or prevent cardiovascular diseases such as hypertension, heart disease, arteriosclerosis, or cerebral hemorrhage or kidney disease, and specifically, clinical studies and Clinical trials have shown that angiotensin converting enzyme inhibitors can effectively reduce hypertension, chronic kidney disease, atherosclerosis, heart attack and death.

In the present invention, blood pressure refers to the force that blood exerts on the vessel wall. When reading blood pressure, it is divided into systolic blood pressure (highest blood pressure) and diastolic blood pressure (lowest blood pressure). Systolic blood pressure is the pressure exerted on blood vessels as the heart contracts and releases blood, while diastolic blood pressure is the pressure the blood vessel receives when the heart receives blood as it expands (relaxes).

In the present invention, hypertension is a disease in which the systolic blood pressure is 140 mmHg or more or the diastolic blood pressure is 90 mmHg or more in adults 18 years or older, and the cause is not found. Cases occur, and about 95% of all hypertension patients are essential hypertension. Diseases caused by the hypertension include hypertensive heart disease (hypertensive heart disease).

In the present invention, atherosclerosis refers to a disease in which the walls of the arteries become thick and the elasticity of the arteries is reduced. When the arteriosclerosis is caused, blood supply to organs that have been supplied with blood from the hardened artery is decreased, and further diseases may be caused. An example of a related disease is coronary artery disease, where atherosclerosis changes in the heart arteries supplying blood to the heart muscle.

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

The inventors of the present invention study the anti-hypertensive substance derived from natural substance or the substance for the treatment or prevention of cardiovascular disease, which is much less likely to be related to the chemically synthesized drug and the possibility of safety related problems such as side effects or resistance is easy. In order to confirm the angiotensin converting enzyme inhibitory ability on various natural-derived components, the ivy extract has excellent angiotensin converting enzyme inhibitory activity, and when the ivy extract and pine needle extract are used together, the angiotensin converting enzyme inhibiting activity is increased. Through experiments that confirmed that the improvement was further confirmed that the cardiovascular disease, more specifically, the treatment, improvement or prevention effect of hypertension was excellent, to complete the present invention based on this.

The present invention relates to a composition for treating or preventing cardiovascular diseases comprising ivy extract as an active ingredient. The cardiovascular disease may preferably be hypertension.

In addition, the present invention relates to a food composition for improving or preventing cardiovascular diseases comprising ivy extract as an active ingredient. The food composition may be a functional food composition.

The ivy vine ( Parthenocissus tricuspidata ) is a deciduous broad-leaved vine plant belonging to the dicotyledon buckthorn vine family, also called ivy, ivy vine or now, sangchun and the like. The ivy grows up to 10m in length and branches off a lot. The vines of the ivy vines face and split to form a round adsorbent root at the end, and the adsorbent root does not fall well when attached. The leaves of the ivy are shifted into broad ovate, reddish in autumn, and petioles are longer than the leaves. The flower of the ivy is yellow-green in June-July, the fruit is covered with white powder with berries, and ripens black in August-October.

The ivy is inhabited in Korea, China, Japan or Taiwan, and grows in all over the country in Korea, grows attached to stone walls or rocks or tree trunks. The roots and stems of the ivy vine is used as a medicinal herb in herbal medicine now, it is used for the analgesic effect to loosen the blood, and to reduce pain in joints and muscles.

The ivy vine may be any one selected from the group consisting of ivy vine leaves, ivy vine stem, ivy vine flower, ivy vine root, ivy vine fruit and mixtures thereof, preferably ivy vine leaf, ivy vine stem and these It may be a mixture of.

The extract of the present invention can be prepared by extracting with an extraction solvent or by adding a fractional solvent to the crude extract prepared by extraction with an extraction solvent.

The extraction solvent may be at least one selected from the group consisting of water and an organic solvent. The organic solvent may be a polar solvent such as methanol, ethanol or the like, an alcohol having 1 to 5 carbon atoms, ethyl acetate or acetone, or a nonpolar solvent such as ether, chloroform, benzene, hexane or dichloromethane or a mixture thereof.

The extraction solvent of the present invention may preferably be one or more solvents selected from the group consisting of water and alcohols having 1 to 4 carbon atoms, more preferably alcohols having 1 to 4 carbon atoms such as water and 50 to 99% ethanol It may be any one selected from the group consisting of an aqueous solution, even more preferably may be water.

The extract of the present invention may be prepared according to a conventional land plant, for example, a method of preparing an extract for extracting leaves, stems, roots or fruits, and specifically, may be cold extraction, hot extraction or heat extraction. A conventional extraction device, an ultrasonic grinding extractor or a fractionator may be used.

In addition, the extract of the present invention may be a fraction further subjected to the fractionation process after adding a fractional solvent to the crude extract extracted with the solvent. The fractional solvent is selected from the group consisting of ethyl acetate, ether, chloroform, benzene, hexane, methylene chloride, butanol, water and mixed solvents thereof, preferably hexane, butanol, water and mixtures thereof. Can be.

The thus-prepared extract or the fraction obtained by performing the fractionation process may be filtered, concentrated or dried to remove the solvent, and may be subjected to both filtration, concentration and drying. Specifically, the filtration can be performed using a filter paper or a vacuum filter, and the concentration can be reduced by using a vacuum concentrator, for example, a rotary evaporator. The drying can be performed by, for example, freeze drying.

In one embodiment of the present invention, the ivy extract may be obtained by the following method.

Specifically, the ivy extract is added distilled water to the mixture of ivy vine leaves and ivy vine stem, extracted for 1 hour to 48 hours or 5 hours to 24 hours at 50 ℃ to 150 ℃, preferably 75 ℃ to 120 ℃ And filtration and concentration under reduced pressure, followed by lyophilization. The ivy vine fraction may be prepared by sequentially adding hexane and butanol to the ivy vine extract, and then separating each solvent fraction.

The ivy hot water extract is not only excellent in the inhibitory ability of angiotensin converting enzyme, but also less likely to cause problems such as side effects or resistance as a substance derived from natural products, and excellent in safety, the ivy hot water extract is a cardiovascular system including high blood pressure It can be used as an active ingredient of a pharmaceutical or pharmaceutical composition for the treatment or prevention of a related disease or an active ingredient of a food composition for improving or preventing a cardiovascular disease.

In this aspect, the present invention relates to a cardiovascular disease treatment or prevention composition comprising ivy extract as an active ingredient.

The cardiovascular disease is a disease including heart disease and vascular disease, any one selected from the group consisting of hypertension, hypertensive heart disease, heart disease, arrhythmia, stroke, thrombosis, angina pectoris, heart failure, myocardial infarction, atherosclerosis and arteriosclerosis And preferably hypertension or hypertensive heart disease.

The hypertension is a blood vessel-related disease, and may be arterial hypertension with high arterial blood pressure. The hypertension may cause arteriosclerosis or hypertensive heart disease.

From the results that the ivy extract can effectively inhibit angiotensin converting enzyme, the blood pressure lowering ability of the ivy extract was confirmed, the ivy extract extract is used to treat cardiovascular diseases such as hypertension and heart disease, arteriosclerosis or cerebral hemorrhage, It is thought to have a prophylactic or improvement effect.

The cardiovascular disease treatment or prevention composition comprising the ivy extract of the present invention as an active ingredient may comprise 0.001 to 99.99% by weight, preferably 0.1 to 99% by weight of the ivy extract based on the total weight of the composition. .

The cardiovascular disease treatment or prevention composition comprising the ivy extract as an active ingredient is an extract of a natural substance does not cause a problem of side effects, and has an excellent effect in that it has an improvement or prevention effect of cardiovascular disease. .

Cardiovascular disease treatment or prevention composition comprising the ivy extract of the present invention as an active ingredient can be applied directly to humans.

The cardiovascular disease treatment or prevention composition comprising the ivy extract as an active ingredient may include the ivy extract as an active ingredient alone, other ingredients, depending on the formulation and the purpose of use, that is pharmaceutical Or further nutritionally acceptable carriers, excipients, diluents or accessory ingredients.

More specifically, the composition for treating or preventing cardiovascular diseases comprising the ivy extract as an active ingredient is a nutrient, vitamins, electrolytes, flavors, coloring agents, neutralizing agents, pectic acid and salts thereof, alginic acid in addition to the active ingredient. And salts thereof, organic acids, protective colloidal thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohols, carbonation agents used in carbonated drinks, and the like. In addition, the carrier, excipient or diluent may be lactose, dextrose, sucrose, sorbitol, mannitol, ziitol, erythritol, maltitol, starch, acycia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, microcrystalline In the group consisting of cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil, dextrin, calcium carbonate, propylene glycol, liquid paraffin, saline It may be one or more selected, but is not limited to any conventional carrier, excipient or diluent can be used. The ingredients may be added independently or in combination to the ivy extract, the active ingredient.

The cardiovascular disease treatment or preventive composition comprising the ivy extract as an active ingredient is 0.001% to 99.9% by weight, preferably 0.1% to 99% by weight, and more preferably 0.001% to 99.9% by weight of the total weight of the composition. It may include 1% to 50% by weight. In addition, the content of the additional component is preferably 0.1 to 200 parts by weight or 0.5 to 100 parts by weight or 1 to 50 parts by weight or 5 parts by weight per 100 parts by weight of the composition for treating or preventing the cardiovascular disease. It may be added in the range from 20 parts by weight to parts.

In addition, the cardiovascular disease treatment or prevention composition comprising the ivy extract as an active ingredient, when formulated, conventional fillers, extenders, binders, disintegrants, surfactants, anticoagulants, lubricants, wetting agents, fragrances, emulsifiers Or may further include preservatives, and can be used orally or parenterally.

Specifically, solid preparations for oral administration include tablets, pills, powders, granules, capsules, and the like, and the solid preparations include at least one excipient such as starch, calcium carbonate, It is prepared by mixing sucrose or lactose, gelatin and the like. In addition to simple excipients, lubricants such as magnesium stearate and talc may also be used. Liquid preparations for oral use include suspensions, solutions, emulsions, and syrups. In addition to water and liquid paraffin, which are commonly used simple diluents, various excipients such as wetting agents, sweetening agents, have.

In addition, the formulation of the composition for the treatment or prevention of cardiovascular diseases comprising the ivy extract of the present invention as an active ingredient may be in a preferred form according to the method of use, in particular the rapid, sustained or delayed action of the active ingredient after administration to a mammal Methods known in the art can be employed and formulated to provide release. Examples of the specific formulations include granules, powders, syrups, liquids, suspensions, tablets, injections, main tablets, cataplasma, capsules, soft or hard gelatin capsules and the like.

Furthermore, the composition for treating or preventing cardiovascular diseases comprising the ivy extract of the present invention as an active ingredient may be prepared using any suitable method known in the art or by Remington's Pharmaceutical Science (Recent Edition), Mack Publishing Company. , Easton PA).

The dosage of the composition for treating or preventing cardiovascular diseases including the ivy extract according to the present invention as an active ingredient is appropriately determined by those skilled in the art in consideration of the method of administration, the age, sex and weight of the recipient, and the severity of the disease. Can be selected. For example, the cardiovascular disease treatment or preventive composition comprising the ivy extract of the present invention as an active ingredient, based on the ivy extract, 0.0001 mg / kg to 1000 mg / kg, to be more effective 0.01 It may be administered at mg / kg to 100 mg / kg. The administration may be carried out once a day or divided into several times. The dose is not intended to limit the scope of the invention in any way.

In addition, the cardiovascular disease treatment or prevention composition comprising the ivy vine extract of the present invention as an active ingredient, in addition to the ivy vine extract may further include an extract for a compound or natural product having a known cardiovascular disease treatment or prophylactic effect. And, it can be included in 5 parts by weight to 200 parts by weight with respect to 100 parts by weight of the ivy extract.

Specifically, the cardiovascular disease treatment or prevention composition comprising the ivy extract as an active ingredient may further comprise a pine extract.

Pinus pine densiflora ) is an evergreen coniferous tree that grows widely in forests in Korea, China, Japan and all Asian regions. The pine is an example of pine ( Pinus densiflora Sieb & Zucc.), Pinus thumbergii Parlatore, Pinus densiflora Sieb & Zucc. For. erecta Uyeki, Old Tree ( Pinus) sylvestris L. or Pine tree ( Pinus) pinea Cupressus Sempervirens), and the pine may be pine bark or pine leaf, preferably pine leaf. The pine bark or pine leaves may be in powder form to increase the extraction area to the maximum with the extraction solvent to increase the extraction yield.

The pine extract may be prepared by adding a fractional solvent to the crude extract prepared by extracting or extracting with an extraction solvent.

The extraction solvent may be at least one selected from the group consisting of water and an organic solvent. The organic solvent may be a polar solvent such as methanol, ethanol or the like, an alcohol having 1 to 5 carbon atoms, ethyl acetate or acetone, or a nonpolar solvent such as ether, chloroform, benzene, hexane or dichloromethane or a mixture thereof.

In addition, the pine extract may be prepared according to a method of preparing an extract for extracting a conventional land plant, for example, leaves, stems, roots or flowers, and specifically, cold extraction, hot extraction or heat extraction. It may be used, a conventional extraction device, ultrasonic grinding extractor or fractionator.

In addition, the pine extract may be a fraction further subjected to the fractionation process after adding a fractional solvent to the crude extract extracted with the solvent. The fractional solvent may be a solvent selected from the group consisting of ethyl acetate, ether, chloroform, benzene, hexane, methylene chloride and mixed solvents thereof.

The prepared pine extract or fractions obtained by performing the fractionation process may be filtered or concentrated or dried to remove the solvent, it is possible to perform both filtration, concentration and drying. Specifically, the filtration can be performed using a filter paper or a vacuum filter, and the concentration can be reduced by using a vacuum concentrator, for example, a rotary evaporator. The drying can be performed by, for example, freeze drying.

In addition, to achieve the above object, the present invention provides a food composition for preventing or improving cardiovascular disease comprising the ivy extract as an active ingredient.

The cardiovascular disease may be any one selected from the group consisting of hypertension, hypertensive heart disease, heart disease, arrhythmia, stroke, thrombosis, angina pectoris, heart failure, myocardial infarction, atherosclerosis and arteriosclerosis, preferably hypertension or It may be a hypertensive heart disease.

The hypertension is a blood vessel-related disease, and may be arterial hypertension with high arterial blood pressure. The hypertension may cause arteriosclerosis or hypertensive heart disease.

As used herein, the term " food " means a natural product or a processed product containing one or more nutrients. Preferably, it means that the food can be directly eaten through a certain degree of processing. Health functional foods, beverages, food additives, and beverage additives.

The food of the present invention includes, for example, various foods, beverages, gums, tea, a vitamin complex, a health functional food, and the like. In addition, the food in the present invention includes special nutritional products (e.g., prepared oils, infants, baby food, etc.), processed meat products, fish products, tofu, jelly, noodles (e.g. ramen, noodles, etc.), health supplements, seasoned foods ( For example, soy sauce, miso, red pepper paste, mixed soy sauce), sauces, confectionery (e.g. snacks), dairy products (e.g. fermented milk, cheese, etc.), other processed foods, kimchi, pickles (various kimchi, pickles, etc.), beverages ( Examples include, but are not limited to, fruits, vegetable drinks, soy milk, fermented beverages, and the like, and natural seasonings (eg, ramen soup). The food, the health functional food, the beverage, the food additive and the beverage additive can be produced by a usual production method.

In the present invention, a health functional food is a biological defense rhythm control, disease prevention and the like having a food group or a food composition which has added value to the food by using physical, biochemical, biotechnological techniques, etc. It means a food that is designed and processed to fully express the gymnastics function on recovery.

The health functional food may include a food-acceptable food-aid additive, and may further comprise suitable carriers, excipients and diluents conventionally used in the production of health functional foods.

In the present invention, beverage is a generic term for drinking or enjoying a taste, and is intended to include a health functional beverage. The beverage is not particularly limited in addition to including the ivy vine extract as an active ingredient in the indicated ratio as an active ingredient, and may contain various flavors or natural carbohydrates, etc. as additional ingredients, as in ordinary drinks. have.

Examples of such natural carbohydrates include monosaccharides such as disaccharides such as glucose and fructose such as maltose, sucrose and the like and polysaccharides such as dextrins, cyclodextrins and the like, and Xylitol, sorbitol, and erythritol. Natural flavors (tau martin, stevia extract (e.g., rebaudioside A, glycyrrhizin, etc.) and synthetic flavors (saccharin, aspartame, etc.) can be advantageously used as flavors other than those described above The ratio of the natural carbohydrate may be generally about 1 to 20 g, preferably 5 to 12 g per 100 ml of the food composition of the present invention. In addition, the composition of the present invention can be used for the production of natural fruit juice, fruit juice drink, Can also be added.

In addition to the above, the food composition of the present invention can be used as a flavoring agent such as a variety of nutrients, vitamins, minerals (electrolytes), synthetic flavors and natural flavors, coloring agents and thickening agents (cheese, chocolate etc.), pectic acid and its salts, Salts thereof, organic acids, protective colloid thickeners, pH adjusting agents, stabilizers, preservatives, glycerin, alcohols, carbonating agents used in carbonated drinks, and the like. These components can be used independently or in combination. The proportion of such additives is not so critical, but may be selected in the range of 0 to 2,000 parts by weight per 100 parts by weight of the ivy extract of the present invention.

In the present invention, the health functional beverage includes a beverage group to which added value is imparted so that the function of the beverage functions to a specific purpose using physical, biochemical, biotechnological techniques, etc., Means a beverage which is processed by being designed so that the body control function related to recovery and the like is sufficiently expressed to a living body.

The health functional beverage is not particularly limited in addition to the ivy vine extract of the present invention as an essential ingredient in the indicated ratio, and may contain various flavors or natural carbohydrates as additional ingredients, such as ordinary drinks. .

Examples of such natural carbohydrates include monosaccharides such as disaccharides such as glucose and fructose such as maltose, sucrose and the like and polysaccharides such as dextrins, cyclodextrins and the like, and xylitol , Sorbitol, and erythritol. As flavoring agents other than those mentioned above, natural flavoring agents (tauumatin, stevia extract (for example, rebaudioside A, glycyrrhizin, etc.) and synthetic flavoring agents (saccharin, aspartame, etc.) can be advantageously used. The proportion of natural carbohydrates is generally about 1 to 20 g, preferably 5 to 12 g per 100 ml of the composition of the present invention.

In addition, in the food composition for preventing or improving cardiovascular disease comprising ivy extract as an active ingredient, the amount of the ivy extract may include 0.01 to 15% by weight of the total food weight, the beverage composition is 100 ml It may be included in a ratio of 0.02 to 5 g, preferably 0.3 to 1 g as a reference.

In addition, the food composition for preventing or improving cardiovascular disease comprising the ivy extract as an active ingredient may further comprise a pine extract.

The ivy extract of the present invention inhibits angiotensin converting enzyme, and thus, may be useful in patients with cardiovascular diseases, specifically hypertension or hypertensive heart disease, or when there is such a risk.

As described above, ingestion of the composition for treating or preventing cardiovascular diseases comprising the ivy extract of the present invention as an active ingredient may inhibit the conversion of angiotensin to angiotensin II by inhibiting angiotensin converting enzyme, thereby preventing cardiovascular disease. As well as effective in the treatment or prevention of the ivy extract, the active ingredient is a natural plant-derived substance, unlike the conventional drug treatment for cardiovascular diseases, artificial side effects, such as side effects are not a problem. Since it is economically advantageous to use the ivy growing on the ivy, the composition for treating or preventing cardiovascular diseases including the ivy extract as an active ingredient will be very effective industrially.

1 is a graph confirming the inhibitory effect of Angiotensin I converting enzyme (Angiotensin I converting enzyme) of the ivy according to an embodiment of the present invention, the horizontal axis shows the content of the ivy hot water extract, the vertical axis is angiotensin I conversion compared to the control It shows the inhibitory activity (%) of the enzyme.
Figure 2 is a graph confirming the angiotensin I converting enzyme inhibitory effect of the ivy extract and pine needle extract according to an embodiment of the present invention, the horizontal axis shows the content of the extract of the ivy and pine needles mixture, the vertical axis is angiotensin I compared to the control It shows the inhibitory activity (%) of the conversion enzyme.
Figure 3 is a graph confirming the antioxidant activity of the ivy vine extract according to an embodiment of the present invention, the horizontal axis shows the content of the ivy vine extract, the vertical axis shows the DPPH free radical scavenging ability (%).
4 is a graph confirming the antioxidant activity of the extract of the ivy and pine needles mixture according to an embodiment of the present invention, the horizontal axis shows the content of the extract of the ivy and pine needles mixture, the vertical axis is DPPH free radical scavenging ability (%) It is shown.

Hereinafter, preferred embodiments of the present invention will be described. The following examples are for illustrative purposes only and are not intended to limit the scope of the invention.

[ Example ]

Example 1: Preparation of ivy vine extract

Ivy ivy ( Parthenocissus tricuspidata ) was collected near Mabongsan, Gadeok-do, Busan, Korea, near Baegunsan and Geomunsan, Gijang-gun, Busan, and Sobaeksan, Yeongju, Gyeongsangbuk-do. After adding 300 ml of distilled water to 150 g of the dried ivy vine, and extracting hot water at 95 ° C. for 10 hours, the extract was filtered with Whatman No. 2 filter paper and filtered under a rotary evaporator. , EYELA N-1000, Rikakikai Co., Japan). The extract was lyophilized at -70 ° C and the extract was used as a sample. The obtained extract sample was stored at −20 ° C. using a freezer until use in experiments.

Extracts of ivy and pine needles mixtures were collected in the vicinity of Busan, South Korea, 300 g of distilled water was added to a mixture of 4.5 g of washed pine needles and 150 g of the dried ivy vines, and the extraction was carried out in the same manner as described above. .

Example 2: Determination of Cardiovascular Disease Therapeutic Effect of Ivy Extracts

In order to confirm the cardiovascular disease treatment effect or antihypertensive effect of the ivy extract extracted in Example 1, angiotensin I converting enzyme (ACE) inhibitory activity was analyzed.

Angiotensin convertase hydrolyzes C-terminal dipeptides (His-Leu) from angiotensin I produced by renin to produce angiotensin II, which exhibits potent vasoconstriction. Therefore, angiotensin II acts to constrict blood vessels, promote the release of aldosterone from the adrenal glands, increase the amount of water in the body, and consequently increase blood pressure. If the action of the angiotensin converting enzyme is continued, blood pressure is continuously increased, the blood vessel wall is weakened and burst, or may cause various diseases such as stroke. Therefore, low molecular weight peptides (peptides) and derivatives thereof, which are the inhibitors of angiotensin converting enzymes, and polyphenols such as catechin or rumine of buckwheat in green tea are associated with cardiovascular diseases such as hypertension. Since it is known to be able to treat, prevent or improve, the cardiovascular disease treatment ability or antihypertensive activity of the ivy extract was analyzed by confirming the inhibitory ability of angiotensin converting enzyme.

The angiotensin converting enzyme inhibitory effect, that is, the activity measurement of angiotensin converting enzyme was measured according to the method of Cushman et al. More specifically, it was performed in the following manner.

Coenzyme solution for confirming the angiotensin converting enzyme inhibitory effect was prepared by the following method. First, rabbit lung acetone powder (Sigma, USA) was extracted in 0.1 M sodium borate buffer (pH 8.3) containing 0.3 M NaCl at a concentration of 1 g / ml (w / v) for 24 hours at 4 ℃, 4 ℃ After centrifugation for 40 minutes under the condition of 4,000 rpm, a supernatant was obtained, and the supernatant was used as a crude enzyme solution. The substrate was prepared by dissolving HHL (hippuryl-histidyl-leucine, Sigma, USA) in 0.1 M sodium borate buffer (pH 8.3) containing 0.3 M NaCl at a concentration of 5 mg / ml (w / v).

The angiotensin converting enzyme inhibitory activity was prepared by the following method. Samples were prepared by dissolving 1 mg, 2 mg, 5 mg, and 10 mg of the ivy extract and the extract of the ivy extract and pine needle mixture prepared in Example 1, respectively, in 1 ml of distilled water. Distilled water was used instead of the sample as a negative control, and captopril was dissolved at a concentration of 0.1 mg / ml as a positive control. The sample used ivy vine extract or extracts of ivy vine and pine needle mixture prepared in Example 1.

50 μl of the angiotensin converting enzyme coenzyme solution prepared above was added to each 50 μl of the prepared katopril solution used as the sample, distilled water and positive control, and then pre-reacted at 37 ° C. for 5 minutes, and then 50 μl of the substrate was added again, and 37 It was made to react at 1 degreeC. The reaction was stopped with 1N HCl in the 150 μl reaction solution. 750 μl of ethyl acetate was added to the reaction solution to stop the reaction, followed by stirring for 1 minute, and centrifuged for 10 minutes at 4 ° C. and 5000 rpm. After the centrifugation, 500 μl of the supernatant was obtained.

The supernatant was completely dried at 120 ° C. for 30 minutes to add 2 ml of methanol, and then absorbance was measured at 228 nm using a spectrophotometer (Ultrospec 3000 pro UV / Visible, Amersham Pharmacia Biotech UK Ltd., UK). . The absorbance results measured above were substituted in the following Formula 1 to determine the angiotensin converting enzyme inhibitory activity effect of the extract. In the following formula 1, S represents the sample absorbance, C represents the control absorbance, and B represents the absorbance of the sample-free sphere. The results measured by the above formulas are shown in FIGS. 1 and 2.

[Equation 1]

As shown in FIG. 1, it was confirmed that an inhibitory effect of 88.9% was observed in the addition of 0.1 mg / ml of captopril, which is a currently available anticardiovascular disease agent. On the other hand, ivy hot water extract was confirmed that the inhibitory effect of about 45.7% and 66.0% at 5 mg / ml and 10 mg / ml concentration, respectively. Considering that the positive control catopril is a compound currently being used as a therapeutic agent, according to the above experimental results, the ivy extract, which is a hydrothermal extract, showed almost similar activity at a concentration of 10 times, the ivy extract was antihypertensive It can be expected to have a function of treating or ameliorating cardiovascular diseases, including activity, which activity has been found to increase in a concentration dependent manner.

In addition, as shown in Figure 2, the hot water extract of the ivy and pine needles mixture was found to be markedly excellent angiotensin converting enzyme inhibitory activity of 56.7% even when using 1 mg / ml, 2 mg / ml, 5 mg / Inhibition effects of about 75.8%, 88.1% and 100% at ml and 10 mg / ml concentrations, respectively, showed a remarkably improved effect compared to ivy extract alone. In particular, when the ivy extract was used alone extracts excellent activity was also confirmed in 1 mg / ml and 2 mg / ml concentration did not appear. The hydrothermal extracts of the ivy and pine needle mixtures were also found to increase angiotensin converting enzyme inhibitory activity, that is, antihypertensive activity in a concentration-dependent manner.

Example  3: ivy Vine  Extract Antioxidant ability  Measure

In order to confirm the antioxidant effect of the ivy vine extract prepared in Example 1, the antioxidant activity was analyzed using DPPH.

More specifically, the antioxidant capacity of the extract was measured by the hydrogen donating effect on DPPH (1,1-Diphenyl-2-picrylhydrazyl, Sigma Chemical Co., USA).

First, the DPPH solution was dissolved in 100 ml ethanol, 1.5 x 10 ^-4 M of DPPH, and then mixed with 100 ml of distilled water. Prepared by filtration with 2. After mixing the sample and DPPH solution in a 1: 4 ratio in a 96 well plate and reacting for 30 minutes at 37 ℃, the absorbance at 520 nm using an ELISA reader (Molecular Device, VersaMax Microplate Reader, Los Angeles, CA, USA) Measured. The sample was prepared by dissolving 0.1 mg, 0.5 mg, 1 mg and 2 mg of each of the extracts of the ivy vine extract or ivy vine and pine needle mixture prepared in Example 1 in 1 ml of distilled water, respectively. As a control, distilled water without any sample was used. As positive control, vitamin C, known as antioxidant, was used.

In order to compare the absorbance difference with the control group without adding the sample, the electron donating ability was expressed as a percentage of radical scavenging activity by the following formula 2, and the results are shown in FIGS. 3 and 4.

[Equation 2]

As shown in FIG. 3, the ivy extract showed an electron donating ability of 63.3% at 1 mg / ml concentration, that is, antioxidant activity, and at 1 mg / ml concentration, it showed 92.7% antioxidant activity as a positive control. The antioxidant activity was comparable to that of 0.1 mg / ml of vitamin C having good antioxidant activity (96.2%).

In addition, as shown in Figure 4, the extract of the ivy and pine needles mixture showed an antioxidant activity of about 75.7% improved by about 20% compared to the use of ivy vine alone even at 1 mg / ml concentration, 2 mg / ml At the concentration, 93.1% of the antioxidant activity was exhibited, which was remarkably excellent.

The antioxidant activity was increased in a concentration-dependent manner with the addition amount.

The results indicate that the ivy hot water extract has an angiotensin converting enzyme inhibitory effect, and has an excellent antioxidant activity, and from this result, it has the effect of treating, preventing or improving cardiovascular diseases including blood pressure lowering ability and antihypertensive activity. It seems to suggest.

Manufacturing example Ivy Vine  Formulation with Extract

Manufacturing example  One. Sanje  Produce

Ivy vine hot water extract powder 20 mg

Lactose 100 mg

Talc 10 mg

The above ingredients were mixed and filled in an airtight container to prepare powders.

Manufacturing example  2. Preparation of tablets

Ivy vine hot water extract powder 10 mg

Corn starch 100 mg

Lactose 100 mg

2 mg magnesium stearate

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

Manufacturing example  3. Preparation of Capsule

Ivy vine hot water extract powder 10 mg

3 mg of crystalline cellulose

Lactose 14.8 mg

Magnesium Stearate 0.2 mg

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

Manufacturing example  4. Liquid  Produce

Ivy vine hot water extract powder 20 mg

10 g of isomerized sugar

5 g of mannitol

Purified water quantity

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

Manufacturing example  5. Preparation of dietary supplements

Ivy vine hot water extract powder 1000mg

Vitamin mixture proper amount

70 [mu] g of vitamin A acetate

Vitamin E 1.0 mg

Vitamin B1 0.13 mg

Vitamin B2 0.15 mg

Vitamin B6 0.5 mg

0.2 μg of vitamin B12

Vitamin C 10 mg

10 μg biotin

Nicotinic Acid 1.7 mg

50 μg folic acid

Calcium Pantothenate 0.5mg

Mineral mixture quantity

Ferrous Sulfate 1.75 mg

Zinc Oxide 0.82 mg

Magnesium carbonate 25.3 mg

Potassium monophosphate 15 mg

Dibasic 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 mixtures is a composition that is relatively suitable for the health functional food, the composition is mixed in a preferred embodiment, but the compounding ratio may be arbitrarily modified, and the above ingredients are mixed according to a conventional health functional food manufacturing method. The granules can then be prepared and used in the manufacture of nutraceuticals in accordance with conventional methods.

Claims (6)

Ivy Vine ( Parthenocissus tricuspidata ) A composition for treating or preventing cardiovascular diseases, comprising the extract as an active ingredient. The method of claim 1,
The cardiovascular disease is a composition for treating or preventing cardiovascular disease, which is hypertension or hypertensive heart disease. The method of claim 1,
The ivy extract is a cardiovascular disease treatment, which is extracted with at least one extractant selected from the group consisting of water, alcohol having 1 to 4 carbon atoms of 50% to 100%, ethyl acetate, hexane, chloroform, methylene chloride and dichloromethane Or prophylactic composition. The method of claim 3,
The ivy extract is a composition for treating or preventing cardiovascular diseases, which is fractionated with one or more fractions selected from the group consisting of water, alcohol having 1 to 4 carbon atoms, ethyl acetate, hexane and dichloromethane extracted with the extraction solvent. . The method of claim 1,
The cardiovascular disease treatment or prevention composition is a cardiovascular disease treatment or prevention composition further comprising a pine extract as an active ingredient. Food composition for the prevention or improvement of cardiovascular diseases comprising ivy extract ( Parthenocissus tricuspidata ) as an active ingredient.

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