JP2009209088A - Muscle-enhancing agent containing asperuloside or its analog - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a muscle-enhancing agent and a basal metabolism-enhancing agent which use a natural material, reduce side effects, and are safe when taken in over a long period, and furthermore an oral intake composition for muscle enhancement or basal metabolism enhancement, a pharmaceutical composition, a food composition, a drug, and a food. <P>SOLUTION: The muscle-enhancing agent or a basal metabolism-enhancing agent and the oral intake composition for muscle enhancement or basal metabolism enhancement comprise asperuloside or its analog. <P>COPYRIGHT: (C)2009,JPO&INPIT

Description

  The present invention relates to a muscle potentiator comprising asperroside or an analog thereof, compositions for ingestion and pharmaceutical compositions used for muscle augmentation, food compositions containing the muscle potentiators, pharmaceuticals, foods and beverages. The present invention also provides a basal metabolism enhancer comprising asperroside or an analog thereof, a composition for ingestion and a pharmaceutical composition used for enhancing basal metabolism, a food composition containing the basal metabolism enhancer, a pharmaceutical, a food And relating to beverages.

  It is widely recognized that regular exercise is important for maintaining health. However, the proportion of the sports population who regularly exercise is still low compared to the nationwide population, and in adults who tend to lack exercise, coupled with the effects of aging, There is a marked decrease in quantity. Muscle attenuation reduces energy metabolism in daily life and can cause lifestyle-related diseases as well as unexpected injury in daily life. In addition, restriction of nutrition intake for the purpose of reducing body weight and body fat percentage may cause a decrease in muscle mass.

  When long-term rest is required after surgery or medical treatment, muscle atrophy or muscle mass loss may occur, preventing early return to daily life after healing. In addition, elderly people generally have little muscle mass, and there are cases where suppression of muscle mass decline is desired in order to live safely. In addition, athletes may use effective supplements and supplements to build the necessary muscles.

  The use of steroids and growth hormones as muscle building agents is known, but these have the problem of side effects. In addition, compositions having a muscle enhancing action have been reported (Patent Documents 1 to 4, etc.).

  At the time of awakening, the minimum energy consumed to maintain life by performing physiological functions such as breathing, circulation, excretion, and maintaining body temperature is called basic metabolism. Basal metabolism varies depending on age, sex, physique, etc., but most basal metabolism is devoted to supplementing body heat dissipated from the body surface. Become higher. Since energy in the body is produced by the oxidation of nutrients, the magnitude of basal metabolism is expressed by the consumption of oxygen taken up by respiration. The basal metabolic rate is an index obtained by converting the basal metabolic rate per body size, and several methods for calculating the basal metabolic rate are known. Is considered high. The basal metabolic rate is the highest in children who are active in all life activities, and the peak is 2 years old. It remains almost constant between the ages of 20 and 45, but gradually decreases after that. This is thought to be due to muscle attenuation, which is the main tissue that performs basal metabolism.

  Body temperature also decreases in proportion to the decrease in basal metabolic rate. Recently, it is said that the number of people with so-called hypothermia whose body temperature is in the 35 degree range is increasing. Enzymes in the body are generally said to increase in activity at 36.5 ° C or higher. When body temperature is low, enzyme activity decreases, cell activity decreases, and the body's original ability cannot be exerted, resulting in decreased QOL. When it is easy to be caused, it becomes a state.

Asperoside is a kind of iridoid glycoside compound contained in Noni leaves, Tochu Naka leaves, etc., for example, it has the effect of reducing visceral fat and blood neutral fat in the Tochu Nakaba water extract fraction containing Asperloside Has been reported (Patent Document 5).
JP 2004-168704 A JP 2004-292325 A JP 2004-256513 A International Publication No. WO2004 / 075905 JP 2007-238449 A

  There is a need for a muscle enhancer that exerts an effect without requiring exercise, and in particular, from the viewpoint of improving QOL, a muscle enhancer that can be safely applied to elderly people and patients being treated is valuable. It can be said that the invention. Similarly, from the viewpoint of improving QOL, a basal metabolism enhancer that can be safely applied is also a valuable invention. An object of the present invention is to provide a safe muscle enhancer and a basal metabolism enhancer that are derived from natural products and have no side effects.

  The inventor has conducted extensive studies to solve the above problems, and as a result, found an asperidoside, which is an iridoid glycoside, or an analog thereof to find a muscle enhancing action and a basal metabolic enhancing action, thereby completing the present invention.

According to one aspect of the present invention, a muscle enhancer comprising asperroside, or an analog thereof, is provided.
According to another aspect of the present invention, a basal metabolism enhancer comprising asperroside or an analog thereof is provided.

According to another aspect of the present invention, there is provided a basal metabolic rate enhancer comprising asperroside or an analog thereof.
The asperoside used here may be a synthetic product or an extract from a natural product. The asperoside may be, for example, a powder of dried Nakanaka leaves or Noni leaves, or an aqueous extract of Junnaka leaves or Noni leaves, or a fraction thereof. As the asperoside of the present invention, for example, the dried Nakanaka leaf is dried without roasting into a fine powder (for example, the Nakanaka leaf powder described in Example 5 of JP-A-2005-287469), What was extracted with water, concentrated and dried to a powder (for example, powder of the extract of Tochu Nakaba water extract described in Example 1 of JP-A-2005-289950) and the like can be used.

As analogs of asperoside, for example, asperoside acid, deacetylasperroside acid, geniposide acid and the like can be mentioned.
According to another aspect of the present invention, there is provided a composition having an muscle enhancing action, a basal metabolic enhancing action, or a basal metabolic rate improving action comprising asperroside or an analog thereof. In one embodiment of the aspect, the composition is an orally ingested composition used for muscle augmentation, basal metabolism enhancement, or basal metabolic rate improvement, including, for example, an oral ingestion pharmaceutical composition or beverage It is a food composition.

  Furthermore, according to another aspect of the present invention, there is provided a medicament and a food or beverage comprising a muscle enhancer, a basal metabolism enhancer, or a basal metabolic rate improver that has already been defined as the present invention. The food is not particularly limited, and may be, for example, a functional food, a health food, a health supplement, a nutritional supplement, a health function food, a specific health food, a special purpose food, or a nutrition function food.

  As used herein, “muscle augmentation” means increasing muscle mass or muscle tension, and includes, for example, increasing muscle weight. “Muscle decay” means a decrease in muscle mass or muscle tension, and includes muscle atrophy, muscle weight loss, muscle fatigue, and the like.

  The “basal metabolism” as used herein is a “resting metabolic rate” obtained by quantifying the consumption of oxygen taken in by breathing as a metabolic amount when resting and awakening. “Enhancement of basal metabolism” means increasing basal metabolism.

As used herein, “basal metabolic rate (BMR)” means oxygen consumption per body surface area. Since basal metabolism increases in proportion to the size of the body surface area, the basal oxygen consumption (V0 ₂ (ml / min)) increases in proportion to the increase in body weight and the body surface. However, the oxygen consumption per body surface area, that is, in terms of BMR, often decreases. That is, an increase in BMR is an increase in basal metabolism taking into account body size.

The muscle enhancer, basal metabolism enhancer, or basal metabolic rate improver of the present invention can be used, for example, for prevention or treatment of hypothermia or coldness.
The muscle enhancing agent, basal metabolism enhancing agent, or basal metabolic rate improving agent of the present invention is not particularly limited, but other drugs that can be used for muscle augmentation (eg, growth hormone), hypothermia, etc. Or other agents that can be used for the prevention or treatment of coldness, or other agents that can be used for the prevention or treatment of lifestyle-related diseases (eg, prophylactic and therapeutic agents for hyperlipidemia, prophylactic agents for diabetes and As well as therapeutic agents, as well as therapeutic or prophylactic agents such as hypertension). Further, the muscle building agent of the present invention may be used together with other foods (functional foods, supplements, etc.) used for muscle building.

  The muscle enhancer, basal metabolism enhancer, or basal metabolic rate improver of the present invention can be used as an active ingredient of a pharmaceutical composition. The pharmaceutical composition can be used in various dosage forms such as tablets, capsules, powders, granules, pills, solutions, emulsions, suspensions, solutions, spirits, syrups, for oral administration. For example, it can be a cream, jelly, gel, paste, ointment and the like for topical administration, but is not limited thereto. The pharmaceutical composition may contain various commonly used components, such as one or more pharmaceutically acceptable excipients, disintegrants, diluents, lubricants, flavoring agents, Coloring agents, sweetening agents, flavoring agents, suspending agents, wetting agents, emulsifying agents, dispersing agents, adjuvants, preservatives, buffering agents, binders, stabilizers, coating agents and the like can be included. The pharmaceutical composition of the present invention may be in a sustained or sustained release dosage form.

  The muscle enhancer, basal metabolism enhancer, or basal metabolic rate improver of the present invention may be administered together with other supplements. Supplements include, for example, amino acids (eg, arginine, ornithine, lysine, glutamine, methionine, valine, leucine, isoleucine, cysteine, alanine, aspartic acid and histidine, especially arginine, lysine and ornithine) and minerals (eg. Zinc, selenium, iron, manganese, molybdenum, magnesium, potassium, chromium, calcium, phosphorus, etc., in particular zinc).

  The dose of asperloside or its analog in the muscle enhancer, basal metabolism enhancer, or basal metabolic rate improver of the present invention can be appropriately selected depending on the patient's body type, age, physical condition, severity, etc. The pharmaceutical composition of the present invention may comprise a therapeutically effective amount and / or a prophylactically effective amount of asperroside or an analog thereof. For example, the present invention is generally used as asperoside or geniposide acid at a dose of 10 to 1000 mg / day / adult, preferably 30 to 200 mg / day / adult, more preferably 50 to 100 mg / day / adult. The administration of the pharmaceutical composition may be a single dose or multiple doses, and may be used in combination with other drugs such as other muscle enhancing agents.

  Further, for example, as a crushed mash of the present invention or a water extract thereof, it is generally used at a dose of 100 to 50000 mg / day / adult, preferably 500 to 3000 mg / day / adult, more preferably 1000 to 2000 mg / day / adult. Is done. Used at doses of Administration of the pharmaceutical composition may be single dose or multiple doses, and may be used in combination with other drugs such as other muscle building agents.

  The food according to the present invention includes liquid beverages, solid and semi-solid foods. The food can be used as a quasi-drug, other ingredients such as food and drink, food additives and the like. In addition, the composition for oral consumption in the present specification can be used as a functional food as it is, and can be used as a component of a pharmaceutical product, quasi-drug, food and drink, a food additive, and the like. The use enables daily and continuous ingestion of the food or composition for oral intake containing the muscle enhancer, basal metabolism enhancer, or basal metabolic rate improver of the present invention, and is effective in muscular attenuation. Prevention or amelioration, effective prevention or amelioration of hypothermia or coldness, and effective prevention of lifestyle diseases (eg, obesity, hypertension, hyperlipidemia, diabetes, etc.) are possible.

  Examples of foods or beverages containing the muscle enhancer, basal metabolism enhancer, or basal metabolic rate improver of the present invention include functional foods having a muscle enhancing effect, basal metabolic enhancing effect, or basal metabolic rate improving effect, health Foods, health supplements, nutritional supplements (nutrition drinks, etc.), health functional foods, foods for specified health use, nutritional functional foods, special purpose foods, general foods (juices, confectionery, processed foods, etc.) are included. The food or beverage herein includes, as optional additives, inorganic components such as iron and calcium, various vitamins, dietary fibers such as oligosaccharides and chitosan, proteins such as soy extract, lipids such as lecithin, salt Sugars and sugars such as lactose, sweeteners such as aspartame, acesulfame potassium, stevia, saumatine, saccharin, sodium saccharin and the like can be included.

  The muscle enhancer, basal metabolism enhancer, or basal metabolic rate improver according to the present invention uses a natural material as a raw material and can be safely ingested over a long period of time. A basal metabolism enhancing effect can be obtained.

  EXAMPLES Hereinafter, although the preferable Example of this invention is described in detail, this invention is not limited to these Examples. In addition, the percentage shown in this specification means weight% unless there is particular mention.

[Example 1] Confirmation test of muscle enhancement effect and basal metabolism enhancement effect SD male rats were ingested with a diet formulated with processed licorice leaves, and the effect on respiratory metabolism was examined. Randomly selected SD male rats (4 weeks old, body weight approximately 75 g) were grouped into 4 animals in each group. Asperuloside to be added to the bait and its analogues, dried Nakachu leaves were dried and finely divided without roasting (hereinafter referred to as EGLP; manufactured in Example 5 of JP 2005-287469 A); Extracted with hot water and concentrated to dryness (hereinafter referred to as ELE, manufactured in Example 1 of JP-A-2005-289950); separated and purified from the hot water extract of EGLP (hereinafter referred to as ASP) , ASP purity 97% or higher); and geniposide (purchased from Sichuan Twin Leaf Biotechnology Co., Ltd.), then separated and purified (hereinafter GEA, GEA purity 99.5% or higher) EGLP and ELE are added to the diet so that each is 1% or 5%, and ASP and GEA are each added to 0.05% or 0.1% for 30 days. And education. A high-fat bait (HFD) obtained by adding 30% lard to MF powder feed (manufactured by Oriental Yeast Co., Ltd.) was used as the base bait. During the breeding period, rats were allowed to freely consume food and water.

In addition, the used asperoside (ASP) was prepared by the following method.
EGPL was dissolved in water and injected into a column packed with Diaion HP20 (manufactured by Mitsubishi Chemical Corporation), and then water was further injected to remove components eluted by water. Thereafter, a 30% by volume aqueous methanol solution was injected to obtain an eluted fraction, which was then concentrated to a solid. The 30% methanol eluate was dissolved in methanol / water = 1/2 (volume ratio) and introduced into an ODS column (filler: YMC S-15 / 30 120A ODS). Methanol / water = 1/2 (volume ratio) was fed as a moving bed at a flow rate of 500 mL / min, and fractionated using UV215 nm as an index. From the fraction, methanol was distilled off under reduced pressure to obtain a crude aqueous asperoside solution. The crude aqueous asperoside solution was further subjected to ODS treatment in the same manner, and only fractions having a purity of 97% or more were collected, and methanol was distilled off under reduced pressure to obtain highly pure asperroside.

The geniposide acid (GEA) used was prepared by the following method.
48% NaOH was added to purified water and the temperature was raised to 50 ° C. Geniposide was added over 6 minutes and stirred at 50 ° C. for 2 hours. After confirming the disappearance of the raw materials, it was cooled to around 25 ° C. and neutralized with 4N HCl to obtain a crude geniposide acid solution. The crude geniposide acid solution was adjusted to pH 3.5 with dilute hydrochloric acid, adsorbed to ODS (Daigel SP-120-40 / 60 ODS-B, manufactured by Daiso Corporation) equilibrated with H ₂ O, and purified water for desalting. And eluted with 50% by volume methanol aqueous solution to obtain highly pure geniposide acid.

After the breeding, the basal metabolism at rest for 20 hours was measured using a metabolic measurement system for small animals (MK-5000RQ, manufactured by Muromachi Kikai Co., Ltd.). However, data for 2 hours from the start were excluded because of the influence of animal exploration behavior. After measuring the basal metabolism, it was dissected and the soleus weight was measured. For the test results, the soleus muscle weight per body weight (soleus muscle weight (g) / rat body weight (g) × 100) is shown in FIG. 1, and the oxygen consumption per body surface area (basal metabolic rate) (VO ₂ (ml / min) / BW (kg) ^0.75 ) is shown in FIG.

  Regarding muscle weight (FIG. 1), an increasing trend was confirmed in all administration groups compared to the control (Cont.), EGLP 1% and 5%, ELE 1%, ASP 0.1%, and GEA 0.05% and A significant increase in muscle weight was observed in the 0.1% administration group. In addition, when 0.1% of purified asperroside (ASP; purity 97% or higher) or geniposide acid (GEA; 99.5% or higher) is added, powder of dried bamboo leaf (EGLP) or powder of bamboo leaf water extract It was also confirmed that with the addition amount of 1/50 of (ELE), a muscle strengthening effect exceeding that of EGLP and ELE was obtained.

  Regarding oxygen consumption per body surface area (basal metabolic rate) (FIG. 2), an increasing trend was confirmed in all administration groups as compared to the control (Cont.), And EGLP 5%, ELE 5% and ASP 0.1% In the administration group, a significant increase in oxygen consumption (basal metabolic rate) per body surface area was observed.

It is a graph which shows an example of the test result about the effect of the muscle strengthening agent of this invention. It is a graph which shows an example of the test result about the effect of the basal metabolism enhancer of this invention.

Claims (8)

  A muscle strengthening agent containing asperoside or an analog thereof.   The muscle strengthening agent according to claim 1, which is used for prevention or treatment of muscle wasting.   The muscle strengthening agent according to claim 1 or 2, wherein the asperoside is a Tochu Nakaba extract.   The foodstuff or drink containing the muscle strengthening agent of any one of Claims 1-3.   A pharmaceutical composition used for the prevention or treatment of muscle augmentation or muscle wasting comprising asperroside, or an analog thereof.   A basal metabolism enhancer comprising asperoside or an analog thereof.   The basal metabolism-enhancing agent according to claim 6, wherein the asperoside is a Tochu Nakaba extract.   A food or beverage comprising the basal metabolism enhancer according to claim 6 or 7.

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