Composition for enhancing effect of body fat reduction caused by exercise
By incorporating quercetin or its glycoside into a composition for use with low-to-moderate intensity exercise, the body fat reduction effects are significantly enhanced, addressing the challenge of insufficient physical activity and promoting improved health.
Patent Information
- Application Number
- JP2025036422
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2025-03-07
- Publication Date
- 2025-05-30
AI Technical Summary
Current levels of physical activity, particularly in terms of step count, fall short of the recommended 10,000 steps a day, which can contribute to lifestyle-related diseases. Enhancing the health promotion effects of low-to-moderate intensity exercise could increase motivation and overall health benefits.
A composition containing quercetin or its glycoside is used in conjunction with low-to-moderate intensity exercise (2.5 to 6.5 METs) to enhance body fat reduction effects. This composition can be in the form of food or drink and includes 30 to 250 mg of quercetin or its glycoside per day.
The use of quercetin or its glycoside with low-to-moderate intensity exercise significantly enhances body fat reduction, particularly in reducing total and subcutaneous abdominal fat areas, thereby promoting better health outcomes.
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Figure 2025083424000001_ABST
Abstract
Description
Technical Field
[0001] To reduce the risk of lifestyle-related diseases, in addition to a balanced diet, it is effective to engage in appropriate physical activity. As the amount of physical activity necessary for maintaining and improving health, the "National Health Promotion Movement in the 21st Century (Healthy Japan 21)" formulated based on the Health Promotion Act states that "it is considered ideal to ensure a step count of '10,000 steps a day' from the results of epidemiological studies on the relationship between the amount of physical activity and mortality, etc." However, according to the "Report on the National Health and Nutrition Survey in Reiwa 1" (Non-Patent Document 1), the average number of steps per day for men and women aged 20 - 64 is 7,226 steps, and on average, it is currently about 3,000 steps short.
[0002] Quercetin is a type of flavonoid and is contained in many plants such as onions, either as it is or as a glycoside. Also, the physiological activities of quercetin that have been known so far include antioxidant activity, anti-inflammatory activity, antitumor activity, vasodilatory activity, inhibition of muscle fibrosis (Patent Document 1), inhibition of the differentiation of muscle satellite cells from myoblasts to adipocyte-like cells (Patent Document 2), and inhibition of muscle fibrosis activity (Patent Document 3), etc.
[0003] Also, according to Non-Patent Document 2, when a test beverage containing 275 mg of enju polyphenol (enzymatically treated isoquercitrin) (the amount of quercetin or its glycoside is 71.6 mg in terms of quercetin conversion described later) was continuously ingested one bottle per day for 7 days and a transient exercise was performed using a bicycle ergometer on the 7th day, the lipid combustion amount was significantly increased during high-intensity exercise of 70 - 90 watts compared to the subjects who ingested a control beverage not containing enju polyphenol, while there was no significant difference in the lipid combustion amount at an exercise load of less than 70 watts. According to the homepage of the manufacturer of the bicycle ergometer, exercise of 70 watts on the same bicycle corresponds to approximately 6.5 mets in terms of the exercise intensity described later (Non-Patent Document 3).
Prior Art Documents
Patent Documents
[0004] [Patent Document 1] International Publication No. 2015 / 166887 [Patent Document 2] International Publication No. 2016 / 175136 [Patent Document 3] International Publication No. 2018 / 164221 [Non-Patent Document]
[0005] [Non-Patent Document 1] "Report on the National Health and Nutrition Survey in Reiwa 1", Ministry of Health, Labour and Welfare, December 2020 [Non-Patent Document 2] Pharmacology and Therapy, 2008, Vol. 36, No. 10, pp. 919 - 930 [Non-Patent Document 3] KONAMI SPORTS CLUB Online Store, "About the Exercise Effect of the Aerobike R", [online], [searched on July 8, Reiwa 4], Internet <URL:https: / / online.konamisportsclub.jp / page / ksc / aboutaerobike / about_aerobike.html> [Summary of the Invention] [Problems to be Solved by the Invention]
[0006] If the health promotion effect of exercise can be enhanced by performing exercise in combination with the intake of specific foods, more people can feel the benefits of exercise, which will increase their motivation for exercise and ultimately lead to better health promotion. In particular, if the effects of low - to - moderate intensity exercise that can be continued daily can be enhanced, it is ideal in terms of contributing to the health of a wide range of people regardless of age or exercise experience.
[0007] Therefore, the present invention contains, as an active ingredient, a component that can be safely ingested over a long period of time, An object of the present invention is to provide a composition (an agent for promoting body fat reduction during exercise) that enhances the effect of reducing body fat by low to moderate-intensity exercise that can be continued daily.
Means for Solving the Problems
[0008] The present inventors have found that quercetin or its glycoside functions as an active ingredient that enhances the effect of reducing body fat by low to moderate-intensity exercise (for example, exercise with an exercise intensity of 2.5 to 6.5 METs) that can be continued daily. In other words, the present inventors have found that quercetin or its glycoside is suitable for reducing body fat in combination with low to moderate-intensity exercise (for example, exercise with an exercise intensity of 3 to 6.5 METs) that can be continued daily, and thus completed the present invention.
[0009] That is, but not limited thereto, the present invention includes a composition for enhancing the effect of reducing body fat by the following exercise, a method for enhancing the reduction of body fat by the target exercise, and the like. [1] A composition for enhancing the effect of reducing body fat by exercise with an exercise intensity of 2.5 to 6.5 METs, containing quercetin or its glycoside as an active ingredient. [2] A composition for reducing the body fat of a subject in combination with exercise, containing quercetin or its glycoside, wherein the intensity of the exercise is 2.5 to 6.5 METs. [3] The composition according to [1] or [2], containing quercetin or its glycoside in an amount such that the total intake of quercetin or its glycoside in adult humans is 30 to 250 mg per day in terms of quercetin equivalent. [4] The composition according to [1] or [2], which is a food or drink. [5] A step of causing a subject to perform exercise with an exercise intensity of 2.5 to 6.5 METs, and A step of causing the subject to ingest a composition containing quercetin or its glycoside A method for enhancing the reduction of body fat by exercise with an exercise intensity of 2.5 to 6.5 METs in a subject (however, excluding medical acts on humans). [6]For a subject who performs exercise of 2.5 to 6.5 METs for 3 or more days a week, including having the subject ingest a composition containing quercetin or its glycoside for 3 or more days a week, wherein the composition contains quercetin or its glycoside in an amount such that the intake amount is 30 to 250 mg per day in terms of quercetin, a method for enhancing the reduction of body fat in the subject by the exercise (however, excluding medical practices for humans). [7]For a subject who performs exercise of 2.5 to 6.5 METs for 3 or more days a week, including having the subject ingest a composition containing quercetin or its glycoside for 3 or more days a week, wherein the intake amount of quercetin or its glycoside in the subject is 30 to 250 mg per day in terms of quercetin, a method for enhancing the reduction of body fat in the subject by the exercise (however, excluding medical practices for humans). [8]For a subject who walks 8,500 steps or more per day, including having the subject ingest a composition containing quercetin or its glycoside, wherein the intake amount of quercetin or its glycoside in the subject is 30 to 250 mg per day in terms of quercetin, a method for enhancing the reduction of body fat in the subject by the walking (however, excluding medical practices for humans). [9]For a subject who continues to walk 8,500 steps or more per day for 3 or more days a week and for 2 or more weeks, including having the subject continuously ingest a composition containing quercetin or its glycoside for 3 or more days a week for a period of 2 or more weeks, wherein the intake amount of quercetin or its glycoside in the subject is 30 to 250 mg per day in terms of quercetin, a method for enhancing the reduction of body fat in the subject by the walking (however, excluding medical practices for humans).
[10] An agent for promoting body fat reduction during exercise, containing quercetin or its glycoside as an active ingredient, wherein the exercise is exercise of 2.5 to 4.0 METs with an intensity of 30 minutes or more per day, and is continuously performed for 3 or more days a week and for 8 or more weeks, an agent for promoting body fat reduction during exercise.
[11] The exercise is performed consciously separately from daily activities. The agent for promoting body fat reduction during exercise according to
[10] .
[12] The exercise is walking. The agent for promoting body fat reduction during exercise according to
[10] or
[11] .
[13] The fat-reducing agent during exercise according to
[12] , wherein the exercise is walking of 3,000 steps or more consciously performed separately from daily activities.
[14] A food or drink for promoting fat reduction during exercise, containing the fat-reducing agent according to any one of
[10] to
[13] .
Advantages of the Invention
[0010] According to the composition of the present invention, it contains, as an active ingredient, a component that can be safely ingested over a long period of time, and can enhance the effect of reducing body fat by low to moderate-intensity exercise. According to the present invention, in addition to daily activities, it promotes the reduction of body fat in subjects who perform low to moderate-intensity exercise, and can contribute to the improvement of the exercise motivation of the subjects and the promotion of health.
Brief Description of the Drawings
[0011]
Figure 1
Figure 2
Modes for Carrying Out the Invention
[0012] [Composition for enhancing the effect of reducing body fat by low to moderate-intensity exercise (fat-reducing agent during exercise)] The present invention includes a composition (fat-reducing agent during exercise) for enhancing the effect of reducing body fat by low to moderate-intensity exercise, containing quercetin or its glycoside as an active ingredient.
[0013] (Quercetin or its glycoside) As used herein, "quercetin" refers to quercetin, which is also known as vitamin P and belongs to the flavonol class of polyphenols. Quercetin is a compound represented by the following formula (I).
[0014] [Chemical formula]
[0015] In the present invention, "quercetin glycoside" means a glycoside of the above quercetin. A quercetin glycoside is a compound represented by the following general formula (II). However, (X) in the following general formula (II) n represents a sugar chain, and n is an integer of 1 or more.
[0016] [Chemical formula]
[0017] The sugars constituting the sugar chain represented by X that is glycosidically bonded to quercetin are, for example, glucose, rhamnose, galactose, glucuronic acid, etc., preferably glucose or rhamnose. Also, if n is 1 or more, it is not particularly limited, but preferably 1 to 16, more preferably 1 to 8. When n is 2 or more, the X moiety may consist of one type of sugar or a plurality of types of sugars. In other words, when n is 2 or more, (X) n may be a sugar chain consisting of one type of sugar or a sugar chain consisting of a plurality of types of sugars.
[0018] The above quercetin glycosides include those obtained by treating existing quercetin glycosides with an enzyme or the like to effect glycosyl transfer. Specifically, the quercetin glycosides referred to in the present invention include rutin, enzyme-treated rutin, quercitrin, isoquercitrin, enzyme-treated isoquercitrin, etc.
[0019] Rutin is a compound represented by the following formula (III).
[0020] [Chemical formula]
[0021] In the present invention, it is particularly preferable to use an enzymatically treated product of rutin as the quercetin glycoside. Preferable examples of the enzymatically treated product of rutin include a rutin enzymatically decomposed product mainly composed of isoquercitrin obtained by enzymatically treating rutin to remove the rhamnose sugar chain portion, an enzymatically treated rutin mainly composed of α-glucosyl rutin obtained by enzymatically treating rutin and further adding one molecule of glucose to rutinoside of rutin, and an enzymatically treated isoquercitrin mainly composed of α-glucosyl isoquercitrin obtained by treating the rutin enzymatically decomposed product or isoquercitrin with a glycosyltransferase to bind a sugar chain composed of 1 to 7 glucose molecules. Among these, it is preferable to use enzymatically treated isoquercitrin, which is a mixture of α-glucosyl isoquercitrin having a sugar chain composed of 1 to 7 glucose molecules.
[0022] The ingested quercetin glycoside is absorbed into the body from the digestive tract and then becomes quercetin by the action of digestive enzymes or metabolic enzymes, and can exhibit the same effects as quercetin in the body. In the present invention, only one kind of quercetin or its glycoside may be used, or a plurality of kinds of compounds may be used. When using a plurality of kinds of compounds, for example, quercetin and one or more kinds of quercetin glycosides may be used, or two or more kinds of quercetin glycosides may be used.
[0023] There are no particular restrictions on the origin and production method for obtaining quercetin or its glycoside used in the present invention. For example, plants rich in quercetin or its glycoside such as buckwheat, adzuki bean, caper, apple, tea, onion, grape, broccoli, spinach, raspberry, loquat, cranberry, opuntia, leafy vegetables, citrus fruits, etc. are known, and quercetin or its glycoside can be obtained from these plants.
[0024] [Action and Use] As shown in the following examples, the composition of the present invention has an effect of enhancing the body fat reduction effect by exercise when used in combination with low to moderate intensity exercise, preferably low intensity exercise (hereinafter also simply referred to as "the above exercise"). And even in the case of exercise at an intensity where the effects of quercetin or its glycoside on muscle mass and basal metabolic rate are not yet significantly manifested, it is possible to significantly reduce body fat by ingesting quercetin or its glycoside. Although the details of the mechanism are unknown and do not limit the present invention, it is presumed that quercetin or its glycoside has an effect of increasing the amount of fat decomposition during the above exercise.
[0025] Therefore, quercetin or its glycoside can be used in combination with the above exercise and can be used to enhance the body fat reduction effect by the above exercise. In addition, it can be used to enhance the body fat reduction effect when performing the above exercise in addition to physical activities in daily life or work (collectively referred to as daily activities). Also, it can be used to enhance the body fat reduction effect when regularly continuing the above exercise in addition to daily activities. Here, the use for enhancing the body fat reduction effect by the above exercise includes, in addition to promoting or increasing the reduction of body fat by the above exercise, for example, promoting or increasing the decomposition or combustion of body fat by the above exercise, etc., which ultimately lead to an enhancement of the body fat reduction effect by the above exercise.
[0026] From the perspective of being able to enjoy the enhanced effect of body fat reduction of the present invention while being sustainable in daily life, the above exercise has a MET value of 6.5 or less, preferably 6.2 or less, more preferably 6.0 or less, still more preferably 5.5 or less, even more preferably 5.0 or less, even more preferably 4.5 or less, and particularly preferably 4.0 or less. Also, the above exercise can be, for example, 2.5 or more, preferably 3.0 or more, more preferably 3.2 or more, and more preferably 3.5 or more. Here, METs (Metabolic Equivalent of Task) is an index representing the intensity of various physical activities and represents the energy consumption of each physical activity when the energy consumption at rest is set to 1.0.
[0027] Low- to medium-intensity exercise (especially low-intensity exercise) is an exercise that can be continuously carried out in daily life, and the enhanced effect of body fat reduction of the present invention is further exerted by continuous performance. In particular, the composition of the present invention has the effect of significantly promoting the reduction of body fat in subjects who regularly and continuously perform low- to medium-intensity exercise (especially low-intensity exercise) in addition to daily activities.
[0028] In this specification, for the MET value of each physical activity related to the above exercise, for example, the numerical values described in the "Revised 'METs Table of Physical Activity'" (revised on April 11, 2012, URL: https: / / www.nibiohn.go.jp / files / 2011mets.pdf) prepared by the National Institute of Health and Nutrition can be used.
[0029] Examples of the above-mentioned exercise include walking (ordinary walking, brisk walking, hiking, etc.), running (jogging, running, etc.), gymnastics (aerobics, radio calisthenics, yoga, Pilates, tai chi, etc.), dancing, cycling, ascending and descending stairs, strength training, carrying luggage, ascending and descending stairs, strength training, various sports (soccer, baseball, golf, basketball, badminton, swimming, tennis, softball, volleyball, table tennis, rugby, surfing, skiing, etc.). These exercises are preferably carried out in addition to daily activities.
[0030] The duration of the above-mentioned exercise can be appropriately set according to the physique, age and physical condition of the subject, the type of exercise, intensity, target amount of body fat reduction, etc. For example, it can be 3 minutes or more, 5 minutes or more, 10 minutes or more, 30 minutes or more, 60 minutes or more, or 2 hours or more, and can be, for example, 10 hours or less or 5 hours or less.
[0031] The total time of the above-mentioned exercise per day can be appropriately set according to the physique, age and physical condition of the subject, the type of exercise, intensity, target amount of body fat reduction, etc. For example, it can be 10 minutes or more, 30 minutes or more, 60 minutes or more, 2 hours or more, or 5 hours or more, and is, for example, 10 hours or less.
[0032] From the viewpoint of more significantly demonstrating the effects of the present invention, the above-mentioned exercise is preferably performed repeatedly (for example, regularly). The frequency can be appropriately set according to the type of exercise, intensity, target amount of body fat reduction, etc. For example, it can be daily, 1 to 6 times a week, or 1 to 3 times a week. Alternatively, the frequency of exercise is 1 day or more per week, preferably 2 days or more per week, more preferably 3 days or more per week, even more preferably 4 days or more per week, even more preferably 5 days or more per week, even more preferably 6 days or more per week, and most preferably daily. Also, from the viewpoint of more significantly demonstrating the effects of the present invention, the period during which the above-mentioned exercise is repeatedly performed is preferably 2 weeks or more, more preferably 4 weeks or more, even more preferably 8 weeks or more, and even more preferably 12 weeks or more.
[0033] When the above-mentioned exercise is walking, the preferred amount of exercise per day is, in terms of the total number of steps, preferably 8,500 steps or more, more preferably 9,000 steps or more, and even more preferably 10,000 steps or more. Considering that according to the "Report on the National Health and Nutrition Survey in Reiwa 1" by the Ministry of Health, Labour and Welfare, the average number of steps per day for men and women aged 20 - 64 is 7,226 steps, when the above-mentioned exercise is walking consciously separately from daily activities, the amount of exercise per day is preferably 1,000 steps or more, more preferably 2,000 steps or more, and even more preferably 3,000 steps or more. The exercise intensity of normal walking varies depending on the walking speed and walking environment, but is approximately about 2.5 - 4.0 METs.
[0034] The exercise combined with the composition of the present invention, when expressed in "exercise (Ex)" (MET·hour), which is a unit obtained by multiplying the exercise time (hour) by the MET which is the exercise intensity, is preferably about 1.0 - 3.0 exercise per day, more preferably 1.0 - 2.5 exercise, and even more preferably 1.0 - 2.0 exercise. These exercises may be carried out in addition to daily activities.
[0035] Specific examples of the low - to - medium - intensity exercise combined with the composition of the present invention are given below, but are not limited thereto: · Walking 1,000 steps or more, more preferably 2,000 steps or more, and even more preferably 3,000 steps or more, consciously in addition to daily activities. · Walking for 10 minutes or more, more preferably 15 minutes or more, more preferably 20 minutes or more, more preferably 25 minutes or more, and even more preferably 30 minutes or more, consciously in addition to daily activities. · Bicycle riding for 5 minutes or more, more preferably 10 minutes or more, and even more preferably 15 minutes or more.
[0036] The timing of ingestion of the composition of the present invention is not particularly limited in relation to the timing of the above - mentioned exercise, and it may be ingested when not doing the above - mentioned exercise, or before, after, or during the above - mentioned exercise.
[0037] Specific examples of body fat reduced by using the composition of the present invention in combination with the above exercise include, for example, total fat, subcutaneous fat, or visceral fat. In particular, the reduction effects on total fat and subcutaneous fat are remarkable. As the measurement site of body fat, for example, the abdomen can be mentioned. The confirmation of these body fat reduction effects can be carried out by, for example, the method for measuring the abdominal fat area described in the examples.
[0038] (Form of the composition) As an example, the composition of the present invention can be provided in the form of an agent, but is not limited to this form. The agent can be provided as the composition itself, or as a composition containing the agent.
[0039] The composition of the present invention can be provided, for example, in the form of food and drink products, pharmaceuticals, quasi-drugs, feeds, etc., but is not limited thereto. The composition of the present invention may itself be a food and drink product, a pharmaceutical, a quasi-drug, a feed, etc., or may be a formulation or material such as an additive used therein. In one aspect, the composition of the present invention is preferably an oral composition.
[0040] In one aspect, the composition of the present invention is preferably a food and drink product, a medicine (preferably an oral medicine) or a quasi-drug, more preferably a food and drink product or an oral medicine, still more preferably a food and drink product, and even more preferably a beverage.
[0041] The above food and drink products are not particularly limited, and examples include general food and drink products, health foods, foods with function claims, foods for specified health use, foods with nutritional functions, health foods, health supplements, supplements, foods for patients or food additives, or raw materials thereof. The form of the above food and drink products is also not particularly limited, and in addition to the form of ordinary beverages or foods, various formulation forms of oral solid preparations such as powders, tablets, coated tablets, fine granules, granules, powders, pills, capsules, dry syrups, chewable agents, etc.; oral liquid preparations such as oral solutions, syrups, etc. can also be used.
[0042] Examples of the above beverage include tea-based beverages (such as green tea, oolong tea, roasted green tea, jasmine tea, barley tea, brown rice tea, buckwheat tea, rooibos tea, mate tea, etc.), coffee beverages, flavored water-based beverages, sports beverages, carbonated beverages, vegetable and fruit-based beverages (such as green juice, vegetable juice, fruit juice, etc.), alcoholic beverages (beverages with an alcohol content of 1 degree or more), etc. Preferably, it is a tea-based beverage, a flavored water-based beverage, a sports beverage or a carbonated beverage, and more preferably a tea-based beverage.
[0043] The above beverage is not particularly limited in terms of the form when it is circulated in the market or the blending ratio of each component contained therein as long as it is something that can be consumed by the target. Therefore, the above beverage may be a concentrate such as powder or syrup, and also includes those that are diluted, dissolved, or leached (such as tea leaves or tea bags) with water, alcohols, carbonated water, etc. for drinking at the time of consumption.
[0044] For beverage products in the form that are diluted, etc. and then consumed, the concentration or amount of each component of the beverage described in this specification represents the concentration or amount at the time of consumption. The dosage form of the above medicine or quasi-drug may be a dosage form suitable for the administration form, and it may be for human use or for non-human animals. The administration form of the medicine or quasi-drug may be oral administration or may be administered in a parenteral form, but oral administration is preferred.
[0045] Examples of the dosage form of oral medicine include solid oral preparations such as tablets, coated tablets, fine granules, granules, powders, pills, capsules, dry syrups, chewable tablets, etc.; and liquid oral preparations such as oral solutions, syrups, etc. Examples of the dosage form of parenteral medicine include injections, infusions, external preparations, suppositories, transdermal absorbents, etc.
[0046] Examples of the above feed include livestock feed for use in cattle, pigs, chickens, sheep, horses, etc.; small animal feed for use in rabbits, rats, mice, etc.; pet food for use in dogs, cats, birds, etc.
[0047] The composition of the present invention can contain, in addition to quercetin or its glycosides as the active ingredient, any additives and any components as long as the effects of the present invention are not impaired. As these additives and components, those generally usable in food and drink products, pharmaceuticals, quasi-drugs, feeds, cosmetics, etc. can be used. As an example of an arbitrary additive or component, in addition to vitamins such as vitamin E and vitamin C, minerals, physiologically active components such as nutritional components, excipients, binders, emulsifiers, tonicity agents (isotonic agents), buffers, solubilizing agents, preservatives, stabilizers, antioxidants, coloring agents, coagulants, coating agents, fragrances, etc. formulated in pharmaceutical preparations can be mentioned. These may be used singly or in combination of two or more.
[0048] In addition to the above, depending on the use, components such as materials used in food and drink products, pharmaceuticals, quasi-drugs, feeds, cosmetics, etc. can be appropriately blended. The composition of the present invention may display one or more of the use, the type of active ingredient, the above-described effects, the method of use (for example, the method of ingestion, the method of administration), etc. on the package, container, or instruction manual.
[0049] As such a display, the present invention may, for example, be provided with at least one display selected from (1) a statement that it has an effect of enhancing the body fat reduction effect by the above exercise, promoting or increasing the reduction of body fat by the above exercise, promoting or increasing the decomposition of body fat by the above exercise, or promoting or increasing the combustion of body fat by the above exercise, (2) a display indicating that it is used to obtain the effect (for example, a display recommending the combined use of the composition of the present invention and the above exercise such as "Drink and walk", "In combination with low to moderate-intensity exercise", "Add to daily exercise habits"), and (3) a display of the target for which the effect is necessary or desired (for example, "For those who want to reduce body fat while exercising daily", "For those who want to reduce body fat with light exercise", "For those who want to reduce body fat by walking").
[0050] The content of quercetin or its glycoside in the composition of the present invention is not particularly limited and can be appropriately set according to its form and the like. For example, the total content of quercetin or its glycoside (the total content of quercetin and its glycoside) in the composition of the present invention is, in terms of the amount of quercetin converted, for example, 0.001% by weight or more, preferably 0.002% by mass or more, more preferably 0.003% by mass or more, and also, for example, 99.9% by weight or less, preferably 95% by weight or less, more preferably 80% by weight or less, and still more preferably 45% by weight or less, based on the total amount of the composition.
[0051] When the composition of the present invention is a beverage, the total content of quercetin or its glycoside in the composition is, in terms of the amount of quercetin converted, preferably 0.002 to 0.5% by mass, preferably 0.003 to 0.1% by mass, more preferably 0.005 to 0.05% by mass, and still more preferably 0.01 to 0.02% by mass, based on the total amount of the composition.
[0052] When referring to the concentration or amount of a component of a beverage in this specification, unless otherwise specified, it refers to the concentration or amount in the final product. Due to processes such as sterilization, the components may be somewhat decomposed, and the amount of decomposition can be taken into account to determine the amount to be added to the beverage, but usually, the concentration or amount at the time of formulation and that in the final product are substantially the same.
[0053] When the composition of the present invention is a supplement, the total content of quercetin or its glycoside in the composition is, in terms of the amount of quercetin converted, preferably 0.1 to 50% by mass, more preferably 0.2 to 20% by mass, and still more preferably 0.3 to 10% by mass, based on the total amount of the composition.
[0054] Unless otherwise specified, the measurement of the amount of quercetin glycoside is determined by the following method using QG1 to QG7 as involved components: That is, Quercetin 3 - O - glucoside (QG1) is used as a standard substance, and a calibration curve is created by high - performance liquid chromatography (HPLC) based on the area at an ultraviolet absorbance of 350 nm and the standard substance concentration. Since quercetin glycosides are hydrolyzed to quercetin in the small intestine, QG1 to QG7 are considered to be physiologically equivalent. Also, regardless of the length of the sugar chain, all 3-position glycosides of quercetin have a maximum absorption at 350 nm, and the absorbance depends on quercetin, the aglycone part. Therefore, although the molecular weights are different, it is considered that QG1 to QG7 have equal molar absorbances, and the components involved are quantified in terms of QG1. Specifically, the analysis sample is subjected to HPLC under the same conditions as the standard substance, and in the obtained chart, a peak that coincides with the elution retention time of the standard substance is identified. Then, if there are peaks of quercetin glycosides QG2 to QG7 detected before the peak of QG1, the content of quercetin glycosides in the analysis sample is calculated using the calibration curve prepared with the standard substance from the total of the peak areas of each.
[0055] From another perspective, when the composition is a container-packed beverage with a volume of 350 to 500 ml, quercetin or its glycoside can be in an amount, in terms of QG1 converted as follows, of 10 to 1800 mg, preferably 50 to 900 mg, more preferably 100 to 500 mg, and even more preferably 100 to 250 mg per bottle of the beverage.
[0056] In addition, when referring to the amount of quercetin blended in the beverage in this specification, unless otherwise specified, the total amount of quercetin glycosides blended is converted to QG1 (for example, isoquercitrin), and it refers to the amount of quercetin generated by the hydrolysis of QG1. The amount of quercetin generated by the hydrolysis of QG1 can be determined by (amount of quercetin glycoside / 464) × 302 using the molecular weight of quercetin of 302 and the molecular weight of QG1 of 464.
[0057] (Dosage and Administration) The composition of the present invention can be ingested or administered by an appropriate method according to its form. The composition of the present invention may be administered or ingested orally, or may be administered parenterally in the form of an injection or the like, but is preferably administered or ingested orally.
[0058] The intake amount (which can also be referred to as the dosage) of the composition of the present invention is not particularly limited and may be appropriately set according to the dosage form, administration method, etc. As one aspect, for example, when orally or parenterally administering or causing to ingest to a human (adult), the intake amount of the composition of the present invention, as the total intake amount of quercetin or its glycoside (the total intake amount of quercetin and its glycoside), is preferably 0.1 mg to 8000 mg per day in terms of quercetin equivalent, more preferably 0.3 mg to 4000 mg, still more preferably 1.0 mg to 1000 mg, even more preferably 10 mg to 500 mg, and particularly preferably 30 mg to 250 mg. It is preferable to orally administer or cause to ingest the above amount, for example, divided into 1 to 3 times a day.
[0059] The intake period and the number of intakes of the composition of the present invention are not particularly limited. For example, on the day of performing low to moderate-intensity exercise, the above amount may be ingested, for example, divided into 1 to 3 times a day, or it may be ingested before or after the day of exercise, such as the day before or the day after the day of exercise. From the viewpoint of more significantly demonstrating the effects of the present invention, the composition of the present invention is preferably ingested daily, for example, every day, 1 to 6 times a week, or 1 to 3 times a week, regardless of the presence or absence of exercise. Further, from the viewpoint of more significantly demonstrating the effects of the present invention, the intake period is preferably 2 weeks or more, 4 weeks or more, 8 weeks or more, or 12 weeks or more. For example, during such a period, the composition of the present invention is ingested in the above amount at a frequency of every day, 1 to 6 days a week, or 1 to 3 days a week, and during the same period, the above-mentioned low to moderate-intensity exercise is preferably repeated (for example, regularly).
[0060] (Subject) The subject to which the composition of the present invention is administered or caused to ingest (hereinafter, also simply referred to as the administration subject) is preferably an animal, more preferably a mammal (human and non-human mammals), and even more preferably a human. Examples of non-human mammals include cows, horses, goats, dogs, cats, rabbits, mice, rats, guinea pigs, monkeys, etc. Further, as the administration subject in the present invention, low to Subjects who need or desire to enhance the effect of reducing body fat by moderate-intensity exercise are preferred. For example, subjects with insufficient daily exercise or limited exercise time, or subjects with reduced exercise function due to weight gain, aging, etc. are preferred subjects.
[0061] Also, those with a BMI (Body Mass Index) of 22 or more (preferably 25 or more, for example, 25 or more and less than 30 (grade I obesity)) are also suitable subjects for the composition of the present invention. In these subjects, the composition of the present invention is preferred in that low- to moderate-intensity exercise is preferred for suppressing the burden on the body, and the effect of the present invention is more remarkable compared to normal-weight subjects with a BMI of 18.5 to less than 25.
[0062] [Method for enhancing reduction of body fat by low- to moderate-intensity exercise] The present invention includes a method for enhancing the reduction of body fat by low- to moderate-intensity exercise in a subject, the method including a step of causing the subject to perform low- to moderate-intensity exercise (for example, exercise with an exercise intensity of 2.5 to 6.5 METs), and a step of causing the subject to ingest a composition containing quercetin or a glycoside thereof.
[0063] The above method may be a therapeutic method or a non-therapeutic method. "Non-therapeutic" is a concept that does not include medical acts, that is, surgery, treatment or diagnosis. The dosage of quercetin or its glycoside may be any amount that enhances the reduction of body fat by exercise in the subject, i.e., an effective amount, and is not particularly limited. For example, it is preferable to administer or ingest the dosage described in the section of [Composition for enhancing the body fat reduction effect by low to moderate-intensity exercise] above. Quercetin or its glycoside may be administered or ingested as it is, or may be administered or ingested as a composition containing quercetin or its glycoside. For example, the composition of the present invention described above can be administered or ingested. Quercetin or its glycoside, low to moderate-intensity exercise, administration subject, administration method, dosage, and their preferred embodiments, etc. are the same as those in the composition of the present invention described above. According to the method of the present invention, side effects are not caused, and the body fat reduction effect by low to moderate-intensity exercise can be enhanced safely.
Example
[0064] Hereinafter, the present invention will be described in more detail with reference to examples, but this does not limit the scope of the present invention. [Example 1 Human test on the effect of combined use of quercetin glycoside and low to moderate-intensity exercise] (Overview of the test) (1) Test beverage As the test beverage, 500 mL of green tea beverage containing 110 mg of quercetin glycoside as isoquercitrin (71.6 mg in terms of quercetin) was used. As the control beverage, 500 mL of green tea beverage without quercetin glycoside was used, and a beverage prepared so that it could not be distinguished from the test beverage in terms of shape, color, flavor, etc. was used. The nutritional component analysis values of the test beverage and the control beverage were all 0 kcal of energy, 0 g of protein, lipid, and carbohydrate respectively.
[0065] (2) Test subjects Persons aged 20 or above and under 65 years old, with grade I obesity (BMI of 25 kg / m 2 or more and 30 kg / m 2Healthy men and women (under a certain age) were recruited as subjects. Also excluded were those who regularly engaged in intense exercise (such as jogging, aerobics, strength training, swimming, etc.), heavy drinkers, excessive smokers, those who were continuously taking medications, those who were pregnant or planning to become pregnant during the test period and lactating women, those with allergies to the test beverage, and others whom the responsible test physician determined to be unsuitable as subjects.
[0066] (3) Test method This test example was conducted as a randomized double-blind placebo-controlled parallel-group comparison test with a 12-week intake period. The subjects were randomly assigned to the test beverage group (n = 74) and the control beverage group (n = 74) to ensure randomness. The subjects were instructed to continuously consume one test beverage or control beverage per day according to the assignment from the time of the examination at the start of test beverage intake until the day before the 12-week post-intake examination. In addition, they were guided to walk approximately 3,000 steps more per day (target range: 3,000 ± 500 steps) than the average number of steps per week measured for each subject before the test. Also, during the test period, they were instructed to keep the exercise other than diet and walking unchanged from before the start of the test and maintain it as constant as possible. Note that the exercise intensity of walking is generally about 2.5 - 4.0 METs. Also, 3,000 steps generally correspond to approximately 30 minutes of walking.
[0067] (4) Examination items The following items were examined for the subjects. The collection of each examination data was conducted at the start of intake (0 week), 8 weeks after intake, and at the 12-week examination.
[0068] <Abdominal fat area> The measurement of the abdominal fat area was performed using the method of Tokunaga et al. (Tokunaga K et al. Int. J. Obes., 1983, Vol.7, pp.437 - 45) with a computerized tomography (CT) scanner at the umbilicus. Measured by the system (Hitachi full-body X-ray device ROBUSTO Ei, Hitachi Medical Corporation, Tokyo). The measurement site was the umbilical region (re-photographed with the fourth lumbar vertebra as the center if the image at the time of umbilical region positioning included the kidneys and ilium), and the photograph was taken at the end-expiratory phase. The CT imaging conditions were tube voltage: 120 kVp, tube current: AEC function, slice thickness: 5 mm, and the film processing was window level "0" and window width "1000". The obtained images were analyzed using visceral fat measurement PC software (Fat Scan Premium, East Japan Technical Research Institute Co., Ltd., Ibaraki Prefecture).
[0069] <Number of steps> Using a pedometer, the test subjects were asked to record their daily number of steps in a daily log, and the average number of steps per day was calculated for each period from the start of intake (0 weeks) to the 12-week post-intake examination.
[0070] (5) Statistical analysis From all the assigned test subjects, a group excluding the test subjects who did not consume any test beverage and the test subjects for whom all the data after assignment were missing was defined as the Full Analysis Set (FAS), and among the FAS, the group that complied with the test protocol was defined as the Per Protocol Set (PPS). The analysis was performed on the PPS.
[0071] Regarding the abdominal fat area, it was evaluated using a linear mixed-effects model with group, examination time, and the interaction between group and examination time as fixed effects and the test subjects as variable effects. Comparisons were made between the intake groups of each test beverage at each examination time and with the start of intake (0 weeks). For the comparison between intake groups, a test for equal variance was performed by F-test, and in the case of equal variance, Student's t-test was performed, and in the case of unequal variance, Welch's t-test was performed for evaluation. The comparison with the start of intake (0 weeks) was evaluated by paired t-test. The statistical significance level was 5%, and the test was two-sided. SAS software (R9.4, SAS Institute Japan), SPSS (SPSS Statistics ver. 27, IBM), etc. were used for tabulation and analysis.
[0072] (Results) (1) Subjects to be analyzed There were 148 subjects at the time of allocation, and 143 subjects (73 in the test beverage group and 70 in the control beverage group) started ingestion (FAS). Table 1 shows the background data of the subjects at the time of allocation. The number of subjects related to PPS is described in each table of the results.
[0073]
Table 1
[0074] (2) Total abdominal fat area The results are shown in Tables 2 and 3. Continuous ingestion of the test beverage for 12 weeks resulted in a significant decrease in the change in total abdominal fat area compared to the ingestion of the control beverage (interaction between group and examination time by linear mixed effect model: p < 0.05, main effect of group: p < 0.05). Also, in the test beverage group, a significant decrease in the change in total abdominal fat area was observed at the 8-week and 12-week examinations after ingestion compared to the control beverage group (p < 0.05). Moreover, in the test beverage group, a significant decrease in the total abdominal fat area was observed at the 8-week and 12-week examinations after ingestion compared to the start of ingestion (0 week) (p < 0.05).
[0075] (3) Subcutaneous abdominal fat area The results are shown in Tables 2 and 3. Continuous ingestion of the test beverage for 12 weeks resulted in a significant decrease in the change in subcutaneous abdominal fat area compared to the ingestion of the control beverage (interaction between group and examination time by linear mixed effect model: p < 0.05, main effect of group: p < 0.05). In the test beverage group, a significant decrease in the change in subcutaneous abdominal fat area was shown at the 8-week and 12-week examinations after ingestion compared to the control beverage group (p < 0.05). Also, in the test beverage group, a significant decrease in the subcutaneous abdominal fat area was observed at the 8-week and 12-week examinations after ingestion compared to the start of ingestion (0 week) (p < 0.05).
[0076]
Table 2
[0077]
Table 3
[0078] (4) Number of steps The average number of steps per day before the start of intake was 6,890.2 steps / day in the test beverage group and 7,000.4 steps / day in the control beverage group. The average number of steps per day during the intake period (from the start of intake to the 12-week examination after intake) was 9,813.0 steps / day in the test beverage group and 10,000.0 steps / day in the control beverage group, showing almost the same trend in both groups.
[0079] [Comparative Example 1: Human test on the effect of quercetin glycoside without combined exercise] (Test overview) A randomized double-blind placebo-controlled trial was conducted on test subjects aged 20 to 65 years with a BMI of 25 or more and less than 30 (81 males and 119 females). They were randomly divided into two groups and made to ingest a beverage containing 0 mg or 110 mg of quercetin for 12 weeks (89 subjects in the control beverage group (36 males and 53 females), 83 subjects in the test beverage group (33 males and 50 females)). The details of the method and results of this test are as described in the paper by Egawa et al. (Egawa et al., Pharmacology and Therapy, 2012, Vol. 40, No. 6, pp. 495 - 503) as described.
[0080] That is, the test in Comparative Example 1 differed from the test in Example 1 above in that there was no instruction for exercise, but was conducted under the same conditions with respect to the beverage, subjects (adult men and women with grade I obesity), region, and season.
[0081] (Results) The total abdominal fat area at the 12-week time point after the start of the test, compared with that at the start of the test, was -5.32 ± 2.42 cm 2 in the test beverage group and +4.97 ± 2.34 cm 2 (both with errors being standard errors) in the control beverage group. The change in the total abdominal fat area of the test beverage group compared to the control beverage group (12-week examination after intake) was -10.30 cm 2
[0082] The subcutaneous abdominal fat area at the 12-week time point after the start of the test, compared with that at the start of the test, was -2.31 ± 1.73 cm in the test beverage group2 、In the control beverage group, it was +0.64 ± 1.56 cm 2 . The change in abdominal subcutaneous fat area (12-week examination after ingestion) of the test beverage group compared to the control beverage group was -2.94 cm 2 .
[0083] [Discussion by comparison between Example 1 and Comparative Example 1] Graphs comparing the changes in total abdominal fat area and abdominal subcutaneous fat area at 12 weeks after the start of the test with respect to the start of the test in each test are shown in FIGS. 1 and 2. By combining the intake of quercetin glycosides with low to moderate-intensity exercise such as walking about 3,000 steps, the total abdominal fat area and abdominal subcutaneous fat area were significantly reduced compared to the case without combined exercise. Such a combined effect with low to moderate-intensity exercise was not observed in the group that ingested the control beverage containing no quercetin glycosides.
[0084] From the above, it was shown that quercetin glycosides significantly enhanced the body fat reduction effect by low to moderate-intensity exercise.
Claims
1. An agent for promoting body fat reduction during exercise, comprising: Contains quercetin or its glycoside as an active ingredient, The exercise is performed for 30 minutes or more per day at an intensity of 2.5 to 4.0 METs, and is performed continuously for 8 weeks or more on 3 or more days per week.
2. Exercise is something you do consciously apart from your daily activities. The agent for promoting body fat reduction during exercise according to claim 1.
3. 3. The agent for promoting body fat reduction during exercise according to claim 1 or 2, wherein the exercise is walking.
4. 4. The agent for promoting body fat reduction during exercise according to claim 3, wherein the exercise is walking of 3,000 steps or more consciously performed in addition to daily activities.
5. A food or drink for promoting body fat reduction during exercise, comprising the body fat reduction promoter according to claim 1 or 2.
Citation Information
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