Composition for improving blood cholesterol levels

Abstract

The purpose of the present invention is to provide: a composition for improving a blood cholesterol level; and a method for improving a blood cholesterol level. The present invention relates to a composition for improving a blood cholesterol level in a human body, the composition containing L-ergothioneine or a salt thereof as an active ingredient.

Description

[Technical Field]

[0001] The present invention relates to a composition for improving blood cholesterol levels in humans. The present invention also relates to a method for improving blood cholesterol levels. [Background technology]

[0002] LDL (low-density lipoprotein) cholesterol and HDL (high-density lipoprotein) cholesterol are lipids present in the human body. Excessive LDL cholesterol is known to cause arteriosclerosis. On the other hand, HDL cholesterol is thought to have the effect of recovering excess cholesterol and preventing arteriosclerosis. To prevent or improve arteriosclerosis, it is recommended to reduce the ratio of LDL cholesterol to HDL cholesterol in the blood (LDL / HDL ratio) and to increase HDL cholesterol in the blood.

[0003] Ergothioneine is an amino acid found in mushrooms and the like, and naturally exists in the L-form. Patent Document 1 describes that mice orally administered with ergothioneine showed a decrease in plasma triglyceride (neutral fat) levels compared to mice not orally administered with ergothioneine. [Prior art documents] [Patent documents]

[0004] [Patent Document 1] Japanese Patent Application Laid-Open No. 2011-102286 Summary of the Invention [Problem to be solved by the invention]

[0005] However, Patent Document 1 does not consider any substance that reduces the ratio of LDL cholesterol to HDL cholesterol in the blood (LDL / HDL ratio), nor does Patent Document 1 describe any substance that has the effect of increasing HDL cholesterol in the blood.

[0006] An object of the present invention is to provide a composition for improving blood cholesterol levels, and a method for improving blood cholesterol levels. [Means for solving the problem]

[0007] As a result of intensive research to solve the above-mentioned problems, the present inventors have found that L-ergothioneine or a salt thereof has the effect of improving cholesterol levels in humans, such as by reducing the LDL / HDL ratio in the blood.

[0008] That is, although not limited thereto, the present invention relates to the following compositions for improving blood cholesterol levels, methods for improving blood cholesterol levels, etc. [1] A composition for improving blood cholesterol levels in humans, comprising L-ergothioneine or a salt thereof as an active ingredient. [2] The composition according to [1] above, which is used to reduce the ratio of LDL cholesterol to HDL cholesterol (LDL / HDL ratio) in the blood. [3] The composition described in [1] or [2] above, which is used to increase HDL cholesterol levels in the blood. [4] The composition according to any one of [1] to [3] above, which is used for preventing arteriosclerosis. [5] The composition according to any one of [1] to [4] above, which is an oral composition. [6] The composition according to any one of [1] to [5] above, which is a food or drink. [7] The composition according to any one of [1] to [6] above, wherein the content of L-ergothioneine or a salt thereof is 2 to 50 mg in terms of L-ergothioneine per daily intake for an adult. [8] A method for improving blood cholesterol levels in a human, comprising administering L-ergothioneine or a salt thereof. [9] Use of L-ergothioneine or a salt thereof for improving blood cholesterol levels in humans. [Effects of the Invention]

[0009] According to the present invention, a composition for improving blood cholesterol levels in humans can be provided. According to the present invention, a method for improving blood cholesterol levels can be provided. [Brief explanation of the drawings]

[0010] [Figure 1] FIG. 1 is a graph showing the change in blood LDL / HDL ratio (ΔLDL / HDL) in the test food group and the control food group. [Figure 2] FIG. 2 is a graph showing the change in blood HDL cholesterol levels (ΔHDL cholesterol) in the test food group and the control food group. DETAILED DESCRIPTION OF THE INVENTION

[0011] The composition for improving blood cholesterol levels of the present invention is a composition for improving blood cholesterol levels in humans. The composition for improving blood cholesterol levels of the present invention contains L-ergothioneine or a salt thereof as an active ingredient. Hereinafter, the composition for improving blood cholesterol levels of the present invention may also be simply referred to as the composition of the present invention.

[0012] L-ergothioneine is a type of amino acid. The salt of L-ergothioneine is not particularly limited as long as it is a pharmacologically acceptable salt or a salt acceptable for use in foods and beverages, and may be either an acidic salt or a basic salt. Examples of acidic salts include inorganic acid salts such as hydrochloride, sulfate, nitrate, and phosphate; and organic acid salts such as acetate, citrate, maleate, malate, oxalate, lactate, succinate, fumarate, and propionate. Examples of basic salts include alkali metal salts such as sodium salt and potassium salt; and alkaline earth metal salts such as calcium salt and magnesium salt.

[0013] L-ergothioneine or its salts may be chemically synthesized or extracted and purified from natural sources. L-ergothioneine is found in large amounts in the Golden / Yellow Oyster mushroom (scientific name: Pleurotus cornucopiae var. citrinopileatus), a mushroom of the Pleurotus genus in the family Pleurocystis. L-ergothioneine is also found in mushrooms such as white button mushrooms, crimini mushrooms, and portabella mushrooms (Agaricus bisporus), grey oyster mushrooms (Pleurotus ostreatus), shiitake mushrooms (Lentinula edodes), maitake mushrooms (Grifola Frondosa), reishi mushrooms (Ganoderma lucidum), Yamabushitake mushrooms (Hericium erinaceus), willow matsutake mushrooms (Agrocybe aegerita), chanterelles (Cantharellus cibarius), porcini mushrooms (Boletus edulis), and morels (Morchella esculenta). When obtaining L-ergothioneine from a natural product, it is preferable to extract it from Pleurotus cornucopiae. L-ergothioneine or a salt thereof can also be produced by microbial fermentation. An extract containing L-ergothioneine or a salt thereof produced by microbial fermentation, or a product purified from such an extract, may be used. Extraction and purification from natural products can be carried out by known methods. L-ergothioneine or a salt thereof may be isolated.

[0014] L-ergothioneine or its salts are compounds that are found in natural products and foods and beverages and are consumed as food. Therefore, from a safety perspective, L-ergothioneine or its salts are thought to pose few problems, even when taken over a long period of time.

[0015] The composition of the present invention is used to improve blood cholesterol levels in humans. In the present invention, improvement of blood cholesterol levels preferably refers to a reduction in the ratio of LDL cholesterol to HDL cholesterol (cholesterol concentration) in the blood (LDL / HDL ratio) and / or an increase in the HDL cholesterol level in the blood.

[0016] As shown in the Examples below, taking L-ergothioneine increased blood HDL cholesterol levels compared to not taking it, and taking L-ergothioneine also reduced the ratio of LDL cholesterol to HDL cholesterol levels (LDL / HDL ratio) in blood compared to not taking it. Therefore, L-ergothioneine or a salt thereof has the effect of improving blood cholesterol levels in humans and can be used as an active ingredient for improving blood cholesterol levels.

[0017] In one embodiment, the composition of the present invention can be used to reduce the ratio of LDL cholesterol to HDL cholesterol in the blood (LDL / HDL ratio) and / or to increase the HDL cholesterol level in the blood. In a preferred embodiment, the composition of the present invention can be used to reduce the ratio of LDL cholesterol to HDL cholesterol in the blood (LDL / HDL ratio) and to increase the HDL cholesterol level in the blood.

[0018] In one aspect, the composition of the present invention is useful for preventing or ameliorating conditions or diseases for which improving blood cholesterol levels is effective in preventing or ameliorating them. Improving blood cholesterol levels can result in the prevention or amelioration of conditions or diseases such as arteriosclerosis, myocardial infarction, angina pectoris, cerebral infarction, fatty liver, etc. In one aspect, the composition of the present invention can be used to prevent or ameliorate conditions or diseases such as arteriosclerosis, myocardial infarction, angina pectoris, cerebral infarction, fatty liver, etc. In one aspect, the composition of the present invention is suitable for use in preventing arteriosclerosis. Preventing a condition or disease includes preventing the onset, delaying the onset, reducing the incidence, reducing the risk of onset, etc. Ameliorating a condition or disease includes recovering a subject from the condition or disease, alleviating the symptoms of the condition or disease, ameliorating the symptoms of the condition or disease, delaying or preventing the progression of the condition or disease, etc.

[0019] The compositions of the present invention can be used for either therapeutic (medical) or non-therapeutic (non-medical) purposes, the latter being a concept that does not include medical procedures, i.e., human surgery, treatment, or diagnosis. The blood cholesterol level-improving composition of the present invention can be provided in the form of a drug, for example, but is not limited to this form. The drug can be provided as a composition as is, or as a composition containing the drug. In one aspect, the blood cholesterol level-improving composition of the present invention can also be referred to as a blood cholesterol level-improving drug. From the viewpoint of fully achieving the effects of the present invention, the composition of the present invention is preferably an oral composition. Examples of oral compositions include foods and beverages, oral medicines, and quasi-drugs, and are preferably foods and beverages or oral medicines, and more preferably foods and beverages.

[0020] The composition of the present invention may contain any additives and any components in addition to L-ergothioneine or a salt thereof, as long as the effects of the present invention are not impaired. These additives and components can be selected depending on the form of the composition, and those that can generally be used for foods and beverages, pharmaceuticals, quasi-drugs, etc. can be used. When the composition of the present invention is made into a food or beverage, pharmaceutical, quasi-drug, etc., the production method thereof is not particularly limited, and it can be produced by a general method.

[0021] For example, when the composition of the present invention is made into a food or beverage, various foods and beverages can be prepared by blending L-ergothioneine or a salt thereof with ingredients that can be used in foods and beverages (e.g., food ingredients, food additives used as needed, etc.). The foods and beverages are not particularly limited, and examples include general foods and beverages, health foods, health drinks, functional foods, foods for specified health uses, health supplements, foods and beverages for patients, etc. The health foods, functional foods, foods for specified health uses, health supplements, etc. can be made into various dosage forms, such as fine granules, tablets, granules, powders, capsules, chewable tablets, syrups, liquids, and liquid diets.

[0022] When the composition of the present invention is used as a pharmaceutical or quasi-drug, for example, L-ergothioneine or a salt thereof can be blended with a pharmacologically acceptable carrier and, if necessary, additives to produce a pharmaceutical or quasi-drug in various dosage forms. Such carriers, additives, etc. may be any pharmacologically acceptable carriers that can be used in pharmaceuticals or quasi-drugs, and may include, for example, one or more of excipients, binders, disintegrants, lubricants, antioxidants, colorants, etc. The pharmaceutical or quasi-drug may be administered orally or parenterally, with oral administration being preferred from the viewpoint of more fully achieving the effects of the present invention. When the composition of the present invention is used as a pharmaceutical or quasi-drug, it is preferably an oral pharmaceutical or quasi-drug. Dosage forms for oral administration include liquids, tablets, powders, fine granules, granules, sugar-coated tablets, capsules, suspensions, emulsions, chewable tablets, etc. Dosage forms for parenteral administration include injections and infusions.

[0023] The content of L-ergothioneine or a salt thereof in the composition of the present invention is not particularly limited and can be set depending on the form, etc. The content of L-ergothioneine or a salt thereof in the composition of the present invention is, for example, preferably 0.0001% by weight or more, more preferably 0.001% by weight or more, and preferably 90% by weight or less, more preferably 50% by weight or less, calculated as L-ergothioneine. In one aspect, the content of L-ergothioneine or a salt thereof in the composition is preferably 0.0001 to 90% by weight, more preferably 0.001 to 50% by weight, calculated as L-ergothioneine. In one aspect, when the composition of the present invention is used as a food or drink, a pharmaceutical product, a quasi-drug, or the like, the content of L-ergothioneine or a salt thereof is preferably within the above-mentioned range. The amount converted to L-ergothioneine or similar expressions means the amount of L-ergothioneine, or in the case of a salt of L-ergothioneine, the value obtained by multiplying the number of moles of the salt by the molecular weight of L-ergothioneine.

[0024] The composition of the present invention can be ingested or administered by an appropriate method depending on its form. From the viewpoint of more fully obtaining the effects of the present invention, the composition of the present invention is preferably taken orally (administered orally). The intake amount (which can also be called the administration amount) of the composition of the present invention is not particularly limited, and may be an amount that can obtain the effect of improving blood cholesterol levels, and may be appropriately set depending on the administration form, administration method, subject weight, etc.

[0025] In one embodiment, when the composition of the present invention is orally ingested or administered to a human (adult) subject, the daily intake of L-ergothioneine or a salt thereof is preferably 2 mg or more, more preferably 5 mg or more, even more preferably 10 mg or more, and preferably 50 mg or less, more preferably 25 mg or less, and even more preferably 20 mg or less, in terms of L-ergothioneine. In one embodiment, when the composition of the present invention is orally ingested or administered to a human (adult) subject, the daily intake of L-ergothioneine or a salt thereof is preferably 2 to 50 mg, more preferably 5 to 25 mg, even more preferably 5 to 20 mg, and particularly preferably 10 to 20 mg, in terms of L-ergothioneine. The above amount is preferably ingested or administered once or more times a day, for example, once a day or in divided doses (e.g., 2 to 3 times a day). In one embodiment of the present invention, the composition of the present invention may be an oral composition for ingesting or administering the above amount of L-ergothioneine or a salt thereof per 60 kg body weight per day to a human. In one aspect, when the composition of the present invention is parenterally administered to a human (adult), the dosage of L-ergothioneine or a salt thereof is, for example, preferably 2 to 50 mg, more preferably 5 to 25 mg, even more preferably 5 to 20 mg, and particularly preferably 10 to 20 mg, per day in terms of L-ergothioneine. In one embodiment, it is preferable to have a human (adult) ingest or administer the above amount of L-ergothioneine or a salt thereof per 60 kg of body weight per day.

[0026] In one aspect, the composition of the present invention preferably contains 2 to 50 mg of L-ergothioneine or a salt thereof per daily intake for an adult, more preferably 5 to 25 mg, even more preferably 5 to 20 mg, and particularly preferably 10 to 20 mg of L-ergothioneine per daily intake for an adult.

[0027] It is expected that continuous ingestion or administration of L-ergothioneine or a salt thereof will exhibit a more excellent effect of improving blood cholesterol levels. Therefore, in a preferred embodiment, the composition of the present invention is continuously ingested or administered. In one embodiment of the present invention, the composition of the present invention is preferably continuously ingested or administered for one week or more, more preferably two weeks or more.

[0028] The subject to which the composition of the present invention is ingested or administered (which may also be referred to as the administration subject) is a human. Subjects to whom the composition of the present invention is administered or taken include those who need or desire improved blood cholesterol levels. Examples of subjects include those who need or desire a reduction in the ratio of LDL cholesterol to HDL cholesterol in the blood (LDL / HDL ratio), and those who need or desire an increase in blood HDL cholesterol levels. Further, subjects of the present invention include those who need or desire the prevention or amelioration of conditions or diseases such as arteriosclerosis, myocardial infarction, angina pectoris, cerebral infarction, and fatty liver. In one embodiment, the composition of the present invention can be suitably used for those who need or desire the prevention or amelioration of arteriosclerosis (particularly, the prevention of arteriosclerosis). In one embodiment, examples of subjects include humans with the above-mentioned conditions or diseases. In one embodiment, the subject to whom the composition of the present invention is administered may be a healthy individual. The composition of the present invention can also be used in healthy individuals, for example, for the prevention of conditions or diseases for which improving blood cholesterol levels is effective in preventing or ameliorating them.

[0029] The composition of the present invention may be labeled with a function that is exerted by improving blood cholesterol levels. For example, the composition of the present invention may be labeled with a function such as "prevention of arteriosclerosis." In one aspect of the present invention, the composition of the present invention is preferably a food or drink to which the above-mentioned label is attached. The above-mentioned label may also be a label indicating that the composition is used to obtain the above-mentioned function. The above-mentioned label may be attached to the composition itself, or to a container or packaging of the composition.

[0030] The present invention also encompasses the following methods and uses. A method for improving blood cholesterol levels by administering or having a human ingest L-ergothioneine or a salt thereof. Use of L-ergothioneine or a salt thereof for improving blood cholesterol levels in humans. The above method is a method for improving blood cholesterol levels in humans. Blood cholesterol levels can be improved by having a subject ingest or administering L-ergothioneine or a salt thereof. Preferably, L-ergothioneine or a salt thereof is orally ingested or administered. The method may be a therapeutic method or a non-therapeutic method. The use may be a therapeutic use or a non-therapeutic use.

[0031] The above method may be a method for reducing the ratio of LDL cholesterol to HDL cholesterol (LDL / HDL ratio) in the blood and / or for increasing the HDL cholesterol level in the blood. The above use may be use of L-ergothioneine or a salt thereof for reducing the ratio of LDL cholesterol to HDL cholesterol (LDL / HDL ratio) in the blood and / or for increasing the HDL cholesterol level in the blood.

[0032] In the above-mentioned methods and uses, L-ergothioneine or a salt thereof, and preferred embodiments thereof, are the same as those of the above-mentioned composition for improving blood cholesterol levels of the present invention. In the above-mentioned methods and uses, it is preferable to have a subject ingest or administer L-ergothioneine or a salt thereof at least once a day, for example, once to several times (e.g., 2 to 3 times) a day. In one aspect, L-ergothioneine or a salt thereof can be used to prevent or ameliorate conditions or diseases such as arteriosclerosis, myocardial infarction, angina pectoris, cerebral infarction, and fatty liver by improving blood cholesterol levels.

[0033] In the above-mentioned methods and uses, L-ergothioneine or a salt thereof may be used in an amount (which may also be referred to as an effective amount) that provides a blood cholesterol level-improving effect. The preferred dosage and administration targets of L-ergothioneine or a salt thereof are the same as those for the above-mentioned composition for improving blood cholesterol levels of the present invention. L-ergothioneine or a salt thereof may be ingested or administered as is, or as a composition containing it. For example, the composition of the present invention may be ingested or administered.

[0034] L-ergothioneine or a salt thereof can be used to produce foods and drinks, pharmaceuticals, quasi-drugs, etc. that are used to improve blood cholesterol levels. In one aspect, the present invention also encompasses the use of L-ergothioneine or a salt thereof to produce a composition for improving blood cholesterol levels. The present invention also encompasses L-ergothioneine or a salt thereof for use in improving blood cholesterol levels in humans. [Example]

[0035] The present invention will be described in more detail below with reference to examples, but the scope of the present invention is not limited to these examples.

[0036] Example 1 (Human blood cholesterol evaluation test) To evaluate the effect of an ergothioneine-containing supplement on human blood cholesterol levels, a placebo-controlled, randomized, double-blind, parallel-group comparative study was conducted on adult men and women (46 in the test food group, 46 in the control food group, a total of 92 people) who took one capsule per day for four weeks containing 20 mg of ergothioneine (test food) or one capsule without ergothioneine (control food). Prior to the start of the study (before starting to take the test food or control food), subjects' blood cholesterol levels were measured as a pre-test. After taking the test food or control food for four weeks, subjects' blood cholesterol levels were measured again (week 4 test). The cholesterol measured was HDL cholesterol and LDL cholesterol.

[0037] (Food for evaluation) Two types of food were used for evaluation, and they were indistinguishable in appearance, flavor, etc. Test food: Capsules containing the test substance (L-ergothioneine 20 mg) Control food: Capsules containing no test substance In addition to the test substance, the ingredients of each evaluation food product included dextrin, hydroxypropyl cellulose, carrageenan, potassium chloride, and titanium oxide. The control food was manufactured using the same ingredients as the test foods, except that it did not contain the test substance (L-ergothioneine).

[0038] The ratio of LDL cholesterol to HDL cholesterol in the blood (LDL / HDL ratio) was calculated for each subject from the measured values ​​of HDL cholesterol and LDL cholesterol (mg / dL). The mean LDL / HDL ratio of the subjects in the test food group was used as the LDL / HDL ratio for the test food group. The mean LDL / HDL ratio of the subjects in the control food group was used as the LDL / HDL ratio for the control food group. In addition, for each group, the change in LDL / HDL ratio from the pre-test (ΔLDL / HDL ratio) was calculated by subtracting the LDL / HDL ratio at the pre-test from the LDL / HDL ratio at the 4-week test (LDL / HDL ratio at the 4-week test - LDL / HDL ratio at the pre-test). The change in LDL / HDL ratio at the pre-test (ΔLDL / HDL ratio) was set to 0. The results are shown in Figure 1.

[0039] Figure 1 is a graph showing the change in blood LDL / HDL ratio (ΔLDL / HDL ratio) for the test food group and the control food group. In Figures 1 and 2, ■ (black square) represents the test food group, and □ (white square) represents the control food group. "Pre" on the horizontal axis represents the time of the pre-test, and "Week 4" represents the time of the 4-week test. As a result, the blood LDL / HDL ratio was reduced more in the test food group than in the control food group.

[0040] Additionally, for each subject, the HDL cholesterol measurement value at the pre-test was subtracted from the HDL cholesterol measurement value at the 4-week test (measurement value at the 4-week test - measurement value at the pre-test) to calculate the delta value (change in HDL cholesterol level) (mg / dL). The average of the above delta values ​​for the subjects in the test food group was used as the change in HDL cholesterol level (ΔHDL cholesterol) for the test food group. The average of the above delta values ​​for the subjects in the control food group was used as the change in HDL cholesterol level (ΔHDL cholesterol) for the control food group. The change in HDL cholesterol level at the pre-test was set to 0. The results are shown in Figure 2.

[0041] FIG. 2 is a graph showing the change in blood HDL cholesterol levels (ΔHDL cholesterol) (mg / dL) in the test food group and the control food group. As a result, blood HDL cholesterol levels increased in the test food group compared to the control food group.

[0042] The above results demonstrate that L-ergothioneine or a salt thereof has the effect of improving blood cholesterol levels in humans.

Claims

1. A composition for improving blood cholesterol levels in humans, which contains L-ergothioneine or a salt thereof as an active ingredient, the content of L-ergothioneine or a salt thereof being 2 to 50 mg in terms of L-ergothioneine per daily intake for an adult, and which is used to reduce the ratio of LDL cholesterol levels to HDL cholesterol levels in the blood (LDL / HDL ratio).

2. The composition according to claim 1, which is used to increase HDL cholesterol levels in the blood.

3. The composition according to claim 1 or 2, which is an oral composition.

4. The composition according to any one of claims 1 to 3, which is a food or drink.

5. The composition according to any one of claims 1 to 4, which is to be taken or administered continuously for two weeks or more.

6. A method for reducing the ratio of LDL cholesterol to HDL cholesterol in the blood (LDL / HDL ratio) by administering L-ergothioneine or a salt thereof to a human, wherein 2 to 50 mg of L-ergothioneine or a salt thereof is administered to an adult per day (however, this does not include medical procedures performed on humans).

7. Use of L-ergothioneine or a salt thereof to reduce the ratio of LDL cholesterol to HDL cholesterol in the blood (LDL / HDL ratio) in humans, wherein 2 to 50 mg of L-ergothioneine or a salt thereof is administered to an adult daily in terms of L-ergothioneine (however, medical procedures on humans are excluded).

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