Kaempferol analogue-containing composition
A kemperol-containing composition addresses the challenge of improving exercise efficiency and reducing fatigue by enhancing oxygen utilization efficiency, effectively supporting exercise performance and dynamic visual acuity even in hypoxic conditions.
Patent Information
- Application Number
- JP2025028982
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2017-08-30
- Filing Date
- 2025-02-26
- Publication Date
- 2025-05-27
AI Technical Summary
Existing compositions fail to effectively improve exercise efficiency, reduce fatigue, and enhance dynamic visual acuity, particularly when oxygen utilization efficiency is decreased due to factors like intense exercise, aging, or hypoxic conditions.
A composition containing a kemperol analog or its glycoside, which is orally administered to increase oxygen utilization efficiency, thereby improving exercise efficiency, reducing fatigue, and enhancing dynamic visual acuity across various exercise intensities.
The composition significantly enhances oxygen utilization efficiency, leading to improved exercise performance, reduced fatigue, and increased dynamic visual acuity, even under reduced oxygen states.
Smart Images

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Abstract
Description
Technical Field
[0001] The present application relates to a composition for improving exercise efficiency, a composition for reducing fatigue, and a composition for improving dynamic visual acuity.
Background Art
[0002] Improving exercise efficiency, reducing fatigue, and improving dynamic visual acuity are very important not only for athletes who perform intense training but also in the daily work of ordinary people (for example, housework, carrying luggage, ascending and descending stairs). Oxygen utilization is an indicator of energy production, and in sports and daily life, improving oxygen utilization efficiency is the key to being able to continuously "exercise" without feeling tired or out of breath. Generally, an arterial blood oxygen saturation of 96% or more at rest is considered normal, but it decreases to 93 - 88% during intense exercise (Non-Patent Document 1). Also, although the arterial blood oxygen saturation (at rest) is about 97% in the 20s, this value decreases with aging and becomes about 93% in the 60s (Non-Patent Document 2). That is, in addition to the rapid decrease in the oxygen state during intense sports, a decrease in the oxygen state can occur in the daily life of ordinary people due to aging, labor, bad weather (low pressure), apnea syndrome, etc. Since a decrease in the oxygen state can occur not only during sports but also in the daily life of ordinary people, even when the oxygen state is decreased in addition to the normal oxygen state, it is desirable to have a preparation that can improve oxygen utilization efficiency, improve exercise efficiency, relieve fatigue, or improve dynamic visual acuity and can be continuously and safely ingested daily.
[0003] Kempferol is a type of natural flavonoid contained in many edible plants such as tea, broccoli, grapefruit, cabbage, kale, beans, kudzu, scallions, tomatoes, strawberries, grapes, mizuna, apples, quinoa, and wasabi.
[0004] Regarding natural flavonoids containing quercetin, studies have been conducted focusing on their various physiological effects. For example, the involvement of quercetin in mitochondrial function (Patent Document 1, Patent Document 2, and Non-Patent Document 3), and the effects of quercetin on cellular energy consumption and thyroid hormones (Non-Patent Document 4) can be cited, but all of these are related to in vitro studies. Patent Document 3 discloses the effect of quercetin on lactic acid concentration, but there is no specific description using other flavonoids.
Prior Art Documents
Patent Documents
[0005]
Patent Document 1
Patent Document 2
Patent Document 3
Non-Patent Documents
[0006]
Non-Patent Document 1
Non-Patent Document 2
Non-Patent Document 3
Non-Patent Document 4
Non-Patent Document 5
[0007] The disclosures of all prior art documents cited in this specification are hereby incorporated by reference into this specification.
Summary of the Invention
Problems to be Solved by the Invention
[0008] The problem of the present application is to provide a composition that can suppress a decrease in exercise efficiency or improve exercise efficiency or reduce fatigue by improving oxygen utilization efficiency (that is, enhancing the ability to utilize oxygen), or can suppress a decrease in dynamic visual acuity or improve dynamic visual acuity, and can exhibit these effects even when the oxygen state is reduced in addition to the normal oxygen state.
Means for Solving the Problems
[0009] The inventors of the present invention conducted intensive studies to solve the above problems, and as a result, they found that by orally administering a kemperol-containing composition to humans, in a wide range of exercise intensities from mild exercise of daily life level to intense exercise equivalent to intense sports, oxygen utilization efficiency increases, exercise efficiency improves, fatigue is reduced, and dynamic visual acuity is improved, leading to the present invention.
[0010] The present invention provides the following: [1] Formula I:
Chemical formula
Chemical formula
[0011] [4] Formula I:
Chemical formula
[0012] [5] Formula I: [Chemical formula] (Formula I) [wherein, R 1 is -OH, or -OCH 3 ; R 2 is H, or -OH; R 3 is H, -OH, or -OCH 3 ; R 4 is -OH, or -OCH 3 ; R 5 is H, or -OH; and R 6 is H, -OH, or -OCH 3 ; provided that [Chemical formula] is excluded] A composition for improving dynamic visual acuity, containing a kemperol analog having the following or its glycoside.
[0013] [6] In the formula I, the glycoside of the kemperol analog R 1 , R 2 , R 4 , and R 6 At least one of is selected independently from -OR 7 , -OR 7 R 8 , or -OR 7 R 8 R 9 ; R 7 is a glucose residue; and R 8 and R 9 are selected independently from a glucose residue, a mannose residue, a galactose residue, a fucose residue, a rhamnose residue, an arabinose residue, a xylose residue, a fructose residue, a glucuronic acid residue, or an apiose residue; The composition according to any one of [1] to [5].
[0014] [7] The composition according to any one of [1] to [6], wherein the kemperol analog or its glycoside is selected from the group consisting of the following:
Chemical formula
Chemical formula
Chemical formula
Chemical formula
Chemical formula
Chemical formula
Chemical formula
[0015] [8] The composition according to any one of [1] to [7], wherein the kempferol analog or its glycoside is kempferol or kempferol 3-O-glucoside.
[0016] [9] The composition according to any one of [1] to [8], characterized in that it contains 0.1 mg to 200 mg of the kempferol analog or its glycoside in terms of the kempferol analog value.
[0017]
[10] The composition according to any one of [1] to [9], characterized in that it contains 0.5 mg to 100 mg of the kempferol analog or its glycoside in terms of the kempferol analog value.
[0018]
[11] The composition according to any one of [1] to
[10] , characterized in that the kempferol analog or its glycoside is administered at 0.1 mg to 200 mg per dose in terms of the kempferol analog value.
[0019]
[12] The composition according to any one of [1] to
[11] , characterized in that the kempferol analog or its glycoside is administered at 0.5 mg to 100 mg per dose in terms of the kempferol analog value.
[0020]
[13] The composition according to any one of [1] to
[12] , characterized in that the kempferol analog or its glycoside is administered at 0.1 mg to 600 mg per day in terms of the kempferol analog value.
[0021]
[14] The composition according to any one of [1] to
[13] , wherein the kempferol analog or its glycoside is administered at a dose of 0.5 mg to 200 mg in terms of kempferol analog per day.
[0022]
[15] The composition according to any one of [1] to
[14] , which is administered to a subject in a hypoxic state.
[0023]
[16] The composition according to any one of [1] to
[15] , which is a food or drink.
[0024]
[17] The composition according to any one of [1] to
[15] , which is a pharmaceutical composition.
[0025] Furthermore, the present invention provides the use of a kempferol analog or its glycoside in the manufacture of a composition for improving exercise efficiency, a composition for reducing fatigue, or a composition for improving dynamic visual acuity.
[0026] Furthermore, the present invention provides a method for improving exercise efficiency, a method for reducing fatigue, or a method for improving dynamic visual acuity, which comprises administering a kempferol analog or its glycoside.
[0027] In addition, the present invention provides a kempferol analog or its glycoside for use in improving exercise efficiency, reducing fatigue, or improving dynamic visual acuity.
Advantages of the Invention
[0028] The composition of the present invention can increase oxygen utilization efficiency (the ability to utilize oxygen), thereby improving its efficiency in any "exercise" including daily operations and sports, for example, enabling exercise in a state where shortness of breath is reduced or endurance is improved. The composition of the present invention can also be used as a shortness-of-breath reducing composition or an endurance improving composition. In addition, the composition of the present invention can reduce fatigue, making it possible to perform sports, daily housework, etc. without feeling tired. Furthermore, the composition of the present invention can improve dynamic visual acuity, for example, contributing to improved performance in sports.
Brief Description of the Drawings
[0029]
Figure 1
Figure 2
Figure 3
Figure 4
Figure 5
Figure 6-1
Figure 6-2
Figure 7
Figure 8
Figure 9-1
Figure 9-2
Figure 10
Figure 11
Figure 12
Figure 13
Figure 14
Mode for Carrying Out the Invention
[0030] The present invention relates to a composition for improving exercise efficiency, a composition for reducing fatigue, or a composition for improving dynamic visual acuity, and these compositions are characterized by containing kemperol analogs or their glycosides.
[0031] In the composition of the present invention, the kemperol analog is Formula I:
Chemical formula
Chemical formula
[0032] The composition of the present invention may contain glycosides of quercetin analogs. Since the glycosides of quercetin analogs can be converted into their aglycones in vivo, they may have the same activity as the aglycones.
[0033] In the composition of the present invention, the glycoside of quercetin analog means a compound in which a sugar chain having one or more (preferably 1 to 3, more preferably 1) sugar residues is glycosidically bonded at one or more (preferably 1 to 2, more preferably 1) hydroxy groups of the quercetin analog. Preferred examples of the sugar residue include a glucose residue, a mannose residue, a galactose residue, a fucose residue, a rhamnose residue, an arabinose residue, a xylose residue, a fructose residue, a glucuronic acid residue, or an apiose residue.
[0034] As a more preferred example of the glycoside of quercetin analog, in formula I, R 1 、R 2 、R 4 、and R 6 at least one of which is independently selected from -OR 7 、-OR 7 R 8 、or -OR 7 R 8 R 9 ; R 7 is a glucose residue; and R 8 and R 9 are independently selected from a glucose residue, a mannose residue, a galactose residue, a fucose residue, a rhamnose residue, an arabinose residue, a xylose residue, a fructose residue, a glucuronic acid residue, or an apiose residue; Compounds are included.
[0035] Examples of preferred quercetin analogs and their glycosides include the following quercetin analogs and their glycosides: TIFF2025081665000020.tif94157.
[0036] An example of a more preferable kempferol analog is kempferol, and an example of its glycoside is kempferol 3 - O - glucoside.
[0037] In the composition of the present invention, the kempferol analog or its glycoside may be included in a combination of a kempferol analog and a glycoside of a kempferol analog. In the composition of the present invention, the kempferol analog may be a single kempferol analog or a combination of multiple types of kempferol analogs. In the composition of the present invention, the glycoside of the kempferol analog may be a glycoside of a single kempferol analog or a combination of glycosides of multiple types of kempferol analogs.
[0038] The kempferol analog or its glycoside used in the composition of the present invention is not limited by its form, production method, etc. For example, when kempferol is selected, it is possible to directly use an extract obtained by a known method from a plant known to contain a large amount of kempferol, or a synthetic product can also be used. The glycoside of the kempferol analog derived from the plant may be used as it is, or may be converted to the kempferol analog as its aglycone by a known method (for example, by enzymatic treatment). When making food and drink products or pharmaceutical compositions, in order to formulate an effective amount, it is preferable to use a product with an increased content by operations such as concentration and purification. Known concentration methods and purification methods can be used in this case.
[0039] In this specification, the "kempferol analog equivalent value" means a value obtained by converting the amount of the glycoside of the kempferol analog to the amount of the kempferol analog as its aglycone. Specifically, it can be calculated by multiplying the number of moles of the glycoside obtained by dividing the amount of the glycoside by its molecular weight by the molecular weight of the aglycone.
[0040] The amount of the kempferol analog or its glycoside contained in the composition of the present invention (in food and drink, pharmaceutical composition, etc.), the amount of the kempferol analog or its glycoside administered per administration, and the amount of the kempferol analog or its glycoside administered per day are not particularly limited as long as the intended effect is exhibited, and can be appropriately selected according to the form of the composition, the number of administrations, the health condition of the subject, etc. The administration period of the composition of the present invention is not particularly limited as long as the intended effect is exhibited, and it may be administered once or continuously. In order to continuously obtain the effects of improving exercise efficiency, reducing fatigue, or improving dynamic visual acuity, it is desirable that the composition of the present invention be continuously administered over a long period, for example, it can be administered for 2 days, 3 days, 1 week, 10 days, 1 month, 3 months or more.
[0041] In the composition of the present invention, depending on the total weight of the composition, the kempferol analog or its glycoside is contained in an amount of, for example, 0.1 mg to 200 mg, preferably 0.5 mg to 100 mg, more preferably 1 mg to 30 mg, and most preferably 2 mg to 10 mg in terms of kempferol equivalent. Examples of the lower limit value of the kempferol equivalent include 0.1 mg, 0.5 mg, 1 mg, 2 mg, and 2.5 mg, and examples of the upper limit value include 200 mg, 150 mg, 100 mg, 50 mg, 30 mg, 25 mg, 15 mg, 10 mg, 5 mg, 3 mg, and 2.5 mg. The preferred range of the kempferol equivalent can be shown by the combination of the upper limit value and the lower limit value.
[0042] In the composition of the present invention, the kempferol analog or its glycoside can be administered at a dose of, for example, 0.1 mg to 200 mg, preferably 0.5 mg to 100 mg, more preferably 1 mg to 30 mg, and most preferably 2 mg to 10 mg in terms of the kempferol analog value per administration. Examples of the lower limit value of the kempferol analog value include 0.1 mg, 0.5 mg, 1 mg, 2 mg, and 2.5 mg, and examples of the upper limit value include 200 mg, 150 mg, 100 mg, 50 mg, 30 mg, 25 mg, 15 mg, 10 mg, 5 mg, 3 mg, and 2.5 mg. The preferred range of the kempferol analog value can be shown by the combination of the upper limit value and the lower limit value.
[0043] In the composition of the present invention, the kempferol analog or its glycoside can be administered at a dose of, for example, 0.1 mg to 600 mg, preferably 0.5 mg to 200 mg, more preferably 1 mg to 100 mg in terms of the kempferol analog value per day. Examples of the lower limit value of the kempferol analog value include 0.1 mg, 0.5 mg, 1 mg, 2 mg, and 2.5 mg, and examples of the upper limit value include 600, 300, 200 mg, 150 mg, 100 mg, 50 mg, 30 mg, 25 mg, 15 mg, 10 mg, 5 mg, 3 mg, and 2.5 mg. The preferred range of the kempferol analog value can be shown by the combination of the upper limit value and the lower limit value. The kempferol analog or its glycoside that can be administered per day may be administered in a single dose or divided into multiple doses (for example, 2, 3, 4, and 5 times).
[0044] The composition of the present invention is preferably formulated as an oral administration preparation, and the formulation type is not particularly limited. For example, it can be in the form of ordinary food such as tablets, granules, capsules, powders, chewable tablets, confectioneries (cookies, biscuits, chocolate confectioneries, chips, cakes, gums, candies, gummies, steamed buns, yokan, puddings, jellies, yogurts, ice creams, sherbets, etc.), bread, noodles, cooked rice, cereal foods, beverages (liquid preparations, soft drinks, carbonated drinks, nutritional drinks, powdered drinks, fruit drinks, milk drinks, jelly drinks, etc.), soups (powdered, freeze-dried), miso soup (powdered, freeze-dried), etc.
[0045] The composition of the present invention can be a food or drink product or a pharmaceutical composition, and can be used as a food or drink product such as a food with functional claims, a food for specified health use, a health food, a dietary supplement, a medical food, etc.
[0046] In addition to the kempferol analogs or their glycosides, the composition of the present invention can be formulated into an oral administration preparation by adding pharmaceutically acceptable bases, carriers, additives that can be used in foods, etc. Materials other than the kempferol analogs or their glycosides used in the composition of the present invention are preferably those that do not impair the stability of the kempferol analogs, and further preferably those that do not impair the intended effects of the composition of the present invention (for example, improvement of oxygen utilization efficiency, improvement of exercise efficiency, reduction of fatigue, or improvement of dynamic visual acuity).
[0047] In the present invention, "improvement of oxygen utilization efficiency" means an increase in the ability to utilize oxygen. As specific examples, in addition to the increase in oxygen consumption efficiency (VO 2 / VE) described in the examples of the present application, an increase in oxygen utilization amount (VO 2 ) under a predetermined exercise intensity, an increase in oxygen uptake efficiency gradient (increase in OUES), and an increase in maximum oxygen utilization amount (VO 2peak ) are included.
[0048] In this specification, "exercise" means moving the body and includes all aspects such as daily housework, carrying luggage, ascending and descending stairs, sports, etc.
[0049] In the present invention, "improvement of exercise efficiency" means that the body can be moved more easily in any exercise situation. For example, the endurance is improved and it is possible to continue exercising for a long time in a more comfortable state, or it is possible to exercise more easily in a state where shortness of breath is reduced. Examples of indices for improvement of exercise efficiency include an increase in oxygen uptake (VO 2 ) under a predetermined exercise intensity, an increase in oxygen consumption efficiency (VO 2 / VE), an increase in the oxygen uptake efficiency gradient (increase in OUES), an increase in the maximum oxygen uptake (VO 2peak ), an increase in the maximum exercise load, a decrease in the exercise intensity under a predetermined oxygen uptake (VO 2 ), or a decrease in the perceived exercise intensity (these terms are explained in the examples of the present application). When the composition of the present invention is administered for improving exercise efficiency, its dosage and frequency of administration are not particularly limited, and it can be administered, for example, at the dosages, frequencies of administration, and administration periods exemplified above.
[0050] In the present invention, reduction of fatigue means that it is possible to exercise with less fatigue in any exercise situation. Examples of indices for reduction of fatigue include a decrease in the exercise intensity or the perceived exercise intensity (these terms are explained in the examples of the present application). When the composition of the present invention is administered for reducing fatigue, its dosage and frequency of administration are not particularly limited, and it can be administered, for example, at the dosages, frequencies of administration, and administration periods exemplified above.
[0051] In the present invention, improvement of dynamic visual acuity means preventing a decrease in dynamic visual acuity or improving dynamic visual acuity. When the composition of the present invention is administered for improving dynamic visual acuity, its dosage and frequency of administration are not particularly limited, and it can be administered, for example, at the dosages, frequencies of administration, and administration periods exemplified above.
[0052] The composition of the present invention may have an effect of improving oxygen utilization efficiency (that is, enhancing the ability to utilize oxygen). Therefore, the composition of the present invention can also be used as an oxygen utilization efficiency improver.
[0053] In the present invention, the hypoxic state means a state in which the body lacks oxygen, and for example, a state where the arterial blood oxygen saturation is less than 95% can be mentioned. Since the composition of the present invention can have the effect of improving oxygen utilization efficiency even in a subject in a hypoxic state, it can contribute to improving exercise efficiency, reducing fatigue, and improving dynamic visual acuity even in a subject in a hypoxic state.
[0054] The administration target of the composition of the present invention is not particularly limited, but is preferably a human. It is preferably administered before and after sports, before and after outdoor work, before and after daily labor (going up and down stairs, housework, etc.), when feeling unable to get rid of daily fatigue, when wanting to work efficiently, and when feeling that movement has become dull due to aging.
Examples
[0055] Hereinafter, the present invention will be described by way of formulation examples and test examples, but the present invention is not limited thereto. [Formulation Example 1] Cookie (Kempferol content 2.5 mg) Quinoa extract * 37% by weight Maple syrup 22% by weight Milk 22% by weight Butter (salted) 15% by weight Granulated sugar 4% by weight Total 100% by weight These were mixed and baked in an oven at a temperature of about 140°C for 20 minutes by a conventional method to produce cookies. The content of kempferol per cookie was 2.5 mg (by HPLC). Quinoa extract * : An extract obtained by converting kempferol glycoside to kempferol aglycone by enzymatic treatment.
[0056] [Formulation Example 2] Capsule-shaped food (Kempferol content 2.5 mg) Ethanol-extracted enzymatically-treated quinoa powder ** 48% by weight Gelatin capsule 52% by weight Total 100% by weight The ethanol-extracted enzyme-treated quinoa powder was filled into gelatin capsules. The content of kaempferol per capsule was 2.5 mg (by HPLC). Ethanol-extracted enzyme-treated quinoa powder ** : An extract obtained by extracting kaempferol glycoside from quinoa grains with 50% ethanol and then converting the kaempferol glycoside to kaempferol aglycone by enzyme treatment.
[0057] <Test Example 1: Incremental load exercise test on cycling Twenty-five healthy adult males were given three doses of kaempferol-containing cookie-like foods (containing 2.5 mg, 10 mg, and 25 mg of kaempferol) and placebo cookie-like foods (containing no kaempferol) as test foods, and continuous intake once a day for 8 days was repeated 4 sets by the crossover method. From 3 hours after the intake of the test foods on the first day of intake (single intake) and the eighth day of intake (continuous intake), cycling incremental load exercise was performed while collecting exhaled gas, and the oxygen uptake was calculated. During the exercise, the heart rate and the perceived exercise intensity were monitored. Also, the dynamic visual acuity was measured before and after the exercise. The details of each evaluation item are shown below.
[0058] <1: Evaluation of oxygen uptake (VO 2 ) The oxygen uptake (VO 2 )(mL / min / kg) was calculated from the difference between the amount of oxygen contained in the inhaled breath (atmosphere) and the amount of oxygen contained in the exhaled gas. In the cycling incremental load exercise, the heart rate (HR) reaches its maximum when the weight of the pedals approaches the limit of the subject. Taking the increase in heart rate from the resting heart rate to the maximum heart rate as 100% of the exercise intensity, the oxygen uptake (VO 2 ) at each exercise intensity was plotted. That is, for example, when the exercise intensity is 50% HR, the following formula: 100×(x - resting heart rate) / (maximum heart rate - resting heart rate)=50% HR When the heart rate of "x" in the formula indicates the oxygen uptake (VO 2 ), it becomes "oxygen uptake (VO 2 ) at exercise intensity 50% HR". The results are shown in Fig. 1. As shown in Fig. 1, after single-dose intake and after continuous intake, at all exercise intensities of 50%, 60%, 70%, 80%, 90%, and 100%, it was confirmed that the oxygen uptake increased when Kempower was ingested compared to when it was not ingested.
[0059] <2: Evaluation of oxygen consumption efficiency (VO 2 / VE)> The oxygen consumption efficiency was calculated by the following formula. Oxygen consumption efficiency (VO 2 / VE) = oxygen uptake / ventilation volume As shown in Fig. 2, after single-dose intake and after continuous intake, an increase in oxygen consumption efficiency (VO 2 / VE) was observed when Kempower was ingested compared to when it was not ingested.
[0060] <3: Evaluation of oxygen uptake efficiency slope (OUES)> Using the ventilation volume and VO 2 per minute starting from the start of incremental load exercise, the oxygen uptake efficiency slope (OUES) was calculated. Specifically, a linear graph with the "log value of ventilation volume (VE)" on the horizontal axis and "VO 2 " on the vertical axis was obtained, and the slope of the linear function graph was taken as OUES. For details, refer to Non-Patent Document 5. As shown in Fig. 3, after single-dose intake and after continuous intake, the oxygen uptake efficiency slope (OUES) increased when Kempower was ingested compared to when it was not ingested, and it was confirmed that oxygen was efficiently utilized throughout the incremental load exercise.
[0061] <4: Evaluation of maximum oxygen uptake (VO 2peak )> As shown in Fig. 4, after single-dose intake and after continuous intake, the maximum oxygen uptake (VO 2peak )(mL / min / kg) increased when Kempower was ingested compared to when it was not ingested.
[0062] <5: Evaluation of maximum exercise load> As shown in Fig. 5, the maximum exercise load (weight of the pedal (watt)) increased when Kemperol was ingested both after single ingestion and after continuous ingestion, compared to the case where Kemperol was not ingested.
[0063] <6: Influence on exercise intensity in daily life> Oxygen uptake (VO 2 ) is generally reported to be 14 mL / min / kg and 24.5 mL / min / kg respectively when climbing stairs and jogging. In incremental exercise, the exercise intensity (%HR) and the rating of perceived exertion (RPE) were evaluated when the oxygen uptake (VO 2 ) corresponded to 14 mL / min / kg and 24.5 mL / min / kg for climbing stairs and jogging respectively. The calculation methods of oxygen uptake (VO 2 ) and exercise intensity (%HR) are the same as above. The rating of perceived exertion (RPE) was evaluated by the subjects at 1-minute intervals from the start of incremental exercise according to the following table, and the response values of each subject were averaged and calculated. As shown in Figs. 6-1 and 6-2, in both cases of oxygen uptake (VO 2 ) corresponding to climbing stairs and jogging, the exercise intensity and the rating of perceived exertion decreased when Kemperol was ingested both after single ingestion and after continuous ingestion, compared to the case where Kemperol was not ingested. TIFF2025081665000021.tif39105
[0064] As shown in the evaluation results of 1 to 6 above, by ingesting the kemperol-containing food, the oxygen consumption and oxygen utilization efficiency increased under the same exercise intensity. Furthermore, the maximum exercise load increased. Also, when assuming the exercise intensity under the same oxygen consumption, the heart rate decreased, suggesting that the subjects' endurance improved and they could exercise more easily without shortness of breath. Since the exercise efficiency improved in this way, it is considered that the fatigue feeling of the subjects was also reduced. In fact, by ingesting the kemperol-containing food, the exercise intensity perceived by the subjects decreased, and shortness of breath and fatigue were reduced. Therefore, it was suggested that this composition can be used as a composition for reducing shortness of breath and / or a composition for improving endurance and / or a composition for improving oxygen utilization.
[0065] <7:Effect on dynamic visual acuity> Before and after the incremental load exercise (within about 1 minute after exercise), the horizontal dynamic visual acuity (DVA) and the depth dynamic visual acuity (KVA) were measured to examine the effect on dynamic visual acuity.
[0066] (1)Measurement of horizontal dynamic visual acuity (DVA:Dynamic Visual Acuity) Measuring instrument: Dynamic vision tester HI-10Dynamic Vision Tester (Kowa Co., Ltd.) Measurement method: The fastest speed at which the Landolt ring moving horizontally on the arc centered on the subject could be visually recognized was measured. The target object automatically and gradually decelerated each time it rotated. When the break of the Landolt ring was distinguishable, the subject pressed the switch at hand and was made to answer the direction (up, down, left, right) of the break. The rotation speed at that time displayed digitally was described on the recording paper and used as the test result. The results are shown in Figure 7.
[0067] <Test Example 2:Effect on ATP production in a hypoxic environment> C differentiated with horse serum 2 C 12 Skeletal muscle cells were obtained, various compounds (final concentration 20 μM) or dimethyl sulfoxide (DMSO) as a negative control were added, and a hypoxic incubator (3% O 2) After culturing for 24 hours, the ATP content in the cells was quantified using a kit (luciferase luminescence method) manufactured by Toyo B-net Co., Ltd. The activity values were expressed as % values when the ATP content of the DMSO-added sample was set to 100%. The results are shown in Fig. 8.
[0068] <Test Example 3: Effects of Quercetin or Quercetin 3-O-Glucoside in Rats> Nine-week-old male SD rats were orally administered quercetin (KMP; 1.0 mg / kg body weight) or quercetin 3-O-glucoside (K3G; 0.1, 0.2, or 1 mg / kg body weight in terms of the KMP aglycone value) once a day at 9:00 am for 8 consecutive days (bred in 21% oxygen). On the 8th day of administration, after the Cont group was exposed to 21% oxygen for 1 hour and the other groups were exposed to 12% oxygen for 1 hour, the soleus muscle (Sol) and whole brain were excised, and the ATP content in the tissues was measured. The results are shown in Figs. 9-1 to -2.
[0069] <Test Example 4: Effects on 400-m Run Performance> A single-dose, two-group, two-period crossover comparative study was conducted on 13 healthy adult men using a quercetin-containing capsule food: SNR14 (containing 10 mg of quercetin) and a placebo capsule food: Placebo (containing no quercetin) as test foods. Three hours after ingesting the test food, a 400-m all-out sprint was performed, and after a 90-minute interval, a 400-m all-out sprint was performed again. The respiratory rate and heart rate were monitored during the sprint. Using an electronic spirometer Auto Spirol (Minato Medical Science Co., Ltd.), the expiratory muscle strength was measured by the maximum oral pressure method before and after the 400-m sprint. The expiratory muscle strength was measured by having the subject take three deep breaths in the standing position, inhaling as much as possible, and then exhaling forcefully into the measurement mouthpiece while preventing air leakage from the nose.
[0070] Figure 10 shows a graph indicating the changes in the times of the first and second 400 - meter sprints. In the placebo food intake group, the average time for the second sprint was - 0.11 seconds compared to the first sprint, while in the group that consumed food containing Kempeol, the average time was - 0.77 seconds.
[0071] Figure 11 shows a graph indicating the breathing rate during the sprint. In the second sprint, compared to the placebo food intake group, the total breathing rate during the sprint in the group that consumed food containing Kempeol was significantly lower, and for each breathing rate (times / minute) every 50 meters, the group that consumed food containing Kempeol was also significantly lower.
[0072] Figure 12 shows a graph indicating the exercise intensity during the sprint. In the second sprint, compared to the placebo food intake group, the exercise intensity during the sprint in the group that consumed food containing Kempeol was significantly lower.
[0073] Figure 13 shows a graph indicating the change in expiratory muscle strength. As shown in Figure 13, compared to the placebo food intake group, the decrease in expiratory muscle strength in the group that consumed food containing Kempeol was significantly suppressed.
[0074] Figure 14 shows a graph indicating the change in heart rate. As shown in Figure 14, compared to the placebo food intake group, in the first run, the heart rate in the group that consumed food containing Kempeol showed a significantly lower value at 200 - 250 meters, and in the second run, it showed a significantly lower value at - 150 meters after the start.
[0075] As for the feelings after the sprint, compared to the placebo food intake group, there were more comments such as "easy", "quick recovery", and "the body can move" from the subjects in the group that consumed food containing Kempeol. Food containing Kempeol can improve exercise performance while being accompanied by feelings such as "easy" and "quick recovery".
[0076] As shown in the results of Test Example 4, the intake of the kemperol-containing food decreased the exercise intensity. Furthermore, since the intake of the kemperol-containing food suppressed the decrease in respiratory muscle strength and the increase in heart rate, it is considered that the exercise efficiency was improved by the alleviation of shortness of breath and the fatigue feeling was reduced. In fact, from the subjective feelings of the subjects, the exercise intensity decreased and the exercise efficiency was improved and the fatigue feeling was reduced by the intake of the kemperol-containing food. Therefore, it was suggested that the present composition can be used as a composition for suppressing an increase in heart rate and / or a composition for alleviating shortness of breath and / or a composition for improving endurance.
Claims
1. Formula I: 【Chemical 1】 (Formula I) [wherein, R 1 is - OH, or - OCH 3 and; R 2 is H, or -OH; R 3 is H, -OH, or -OCH 3 ; R 4 is -OH, or -OCH 3 and; R 5 is H, or -OH; and R 6 is H, -OH, or -OCH 3 ; provided that, [Chemical Formula 2] excluding] A composition for improving exercise efficiency containing a kemperol analog or its glycoside having.
2. The composition for improving exercise efficiency according to Claim 1, wherein the improvement in exercise efficiency is an improvement in endurance.
3. The composition for improving exercise efficiency according to Claim 1, wherein the improvement in exercise efficiency is a reduction in shortness of breath.
4. Formula I: [Chemical Formula 3] (Formula I) [wherein, R 1 is -OH, or -OCH 3 and; R 2 is H, or -OH; R 3 is H, -OH, or -OCH 3 ; R 4 is -OH, or -OCH 3 and; R 5 is H, or -OH; and R 6 is H, -OH, or -OCH 3 ; provided that, 【Chemical Formula 4】 excluding] A composition for reducing fatigue containing a kemperol analog or its glycoside having.
5. Formula I: 【Chemical Formula 5】 (Formula I) [wherein, R 1 is -OH, or -OCH 3 and; R 2 is H, or -OH; R 3 is H, -OH, or -OCH 3 ; R 4 is -OH, or -OCH 3 and; R 5 is H, or -OH; and R 6 is H, -OH, or -OCH 3 ; provided that, 【Chemical Formula 6】 excluding] A composition for improving dynamic visual acuity containing a kemperol analog or its glycoside having.
6. The glycoside of the kemperol analog, in Formula I, R 1 、R 2 、R 4 、and R 6 at least one of which is -OR 7 、-OR 7 R 8 、or -OR 7 R 8 R 9 is independently selected from; R 7 is a glucose residue; and R 8 and R 9 is independently selected from a glucose residue, a mannose residue, a galactose residue, a fucose residue, a rhamnose residue, an arabinose residue, a xylose residue, a fructose residue, a glucuronic acid residue, or an apiose residue; The composition according to any one of Claims 1 to 5.
7. The composition according to any one of Claims 1 to 6, wherein the kemperol analog or its glycoside is selected from the group consisting of: 【Chemical Formula 7】 [Chemical Formula 8] 【Chemical Formula 9】 【Chemical Formula 10】 【Chemical 11】 【Chemical Formula 12】 【Chemical 13】 【Chemical 14】 【Chemical Formula 15】 【Chemical 16】 【Chemical 17】 and their glycosides.
8. The composition according to any one of Claims 1 to 7, wherein the kemperol analog or its glycoside is kemperol or kemperol 3 - O - glucoside.
9. The composition according to any one of Claims 1 to 8, characterized in that it contains 0.1 mg to 200 mg of the kemperol analog or its glycoside in terms of kemperol analog value.
10. The composition according to any one of Claims 1 to 9, characterized in that it contains 0.5 mg to 100 mg of the kemperol analog or its glycoside in terms of kemperol analog value.
11. The composition according to any one of Claims 1 to 10, characterized in that the kemperol analog or its glycoside is administered at 0.1 mg to 200 mg in terms of kemperol analog value per administration.
12. The composition according to any one of Claims 1 to 11, characterized in that the kemperol analog or its glycoside is administered at 0.5 mg to 100 mg in terms of kemperol analog value per administration.
13. The composition according to any one of Claims 1 to 12, characterized in that the kemperol analog or its glycoside is administered at 0.1 mg to 600 mg in terms of kemperol analog value per day.
14. The composition according to any one of claims 1 to 13, wherein the kempferol analog or its glycoside is administered at a kempferol analog equivalent value of 0.5 mg to 200 mg per day.
15. The composition according to any one of claims 1 to 14, which is administered to a subject in a hypoxic state.
16. The composition according to any one of claims 1 to 15, which is a food or drink.
17. The composition according to any one of claims 1 to 15, which is a pharmaceutical composition.
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