JP3749978B2 - Bone formation enhancing composition exhibiting anti-osteoporosis effect - Google Patents

Description

[0001]
BACKGROUND OF THE INVENTION
The present invention relates to a bone formation-promoting composition that exhibits an anti-osteoporosis effect by using a dried product or a water-extracted component of red mock (Honda Walla) as an active ingredient.
[0002]
[Prior art]
Osteoporosis is a condition in which bones become brittle, caused by a decrease in bone mass. Osteoporosis not only causes fractures and severe pain, but also causes bedridden elderly people, so effective treatment is required from the viewpoint of improving the quality of life in an aging society. ing. Active vitamin D ₃ , female hormone (estrogen), calcitonin, ipriflavone, and bisphosphonates have been used clinically as therapeutic agents for osteoporosis. Recently, polyisoprenoid derivatives represented by vitamin K ₂ have been broken. An anti-osteoporosis agent (Japanese Patent Application Laid-Open No. 7-215849) based on an inhibitory effect on bone cell formation has also been developed.
[0003]
On the other hand, recently, since osteoporosis is difficult to treat after onset, efforts to prevent it have been emphasized. To that end, it is essential to increase bone mass from a young age, and it is deeply recognized that nutritional components necessary for bone formation and foods that promote bone formation must be actively consumed on a daily basis. It became so. Currently, calcium, magnesium and vitamin D are mainly used as foods for strengthening bones. Casein phosphopeptides that promote absorption of calcium from the intestinal tract have also been used. Furthermore, it is also considered to utilize vitamin K ₂ of foods known as menaquinone (MK) -1~14 by the side chain length difference.
[0004]
[Problems to be solved by the invention]
However, active vitamin D ₃ , female hormone (estrogen), and calcitonin used as therapeutic agents for osteoporosis are known to have side effects and excess disease, and are problematic. Recently, vitamin K ₂ has been used as a highly safe treatment for osteoporosis, but the amount of vitamin K ₂ used for treatment must be ingested as much as 45 mg per day. In this case, side effects such as abdominal pain, nausea, vomiting, rash, and headache may appear in some cases. In addition, ipriflavone and bisphosphonate are unclear in terms of effectiveness and safety when used for a long period of time. In spite of the development of various osteoporosis therapeutic agents as described above, since the medication is performed over a long period of time, the burden on the patient due to side effects and the like is great, and a satisfactory therapeutic effect is not necessarily exhibited.
[0005]
On the other hand, the method of reinforcing the bone composition with foods such as calcium is not sufficient for increasing the bone mass or increasing the bone strength. Further, foods containing vitamin K ₂ or more 1ppm also vitamin K ₂ is Zongai less, slightly natto (vitamin K ₂ concentration, several to several tens of ppm) in a familiar food only find its examples. When trying to take vitamin K ₂ effective for osteoporosis treatment with natto, natto must be eaten several hundred g or more per day, which causes a problem in taste. Therefore, attempts have been made to the development of food products with enhanced vitamin K _2. However, when taking 45 mg a day as a therapeutic agent, side effects such as abdominal pain and rash may appear as described above, so only a smaller amount can be used. However, reducing the amount reduces the effect. Resulting in.
[0006]
In addition to nutritional guidance, exercise is recommended to load bones and promote bone formation, but in reality, there is a tendency to become underexercised due to a decline in physical fitness and a decrease in energy. . Of course, exercise alone cannot sufficiently maintain or increase bone mass and bone strength.
Thus, despite the desire for the development of safe functional foods that are effective in preventing or treating osteoporosis, no products that have both efficacy and safety have been developed at present.
[0007]
[Means for Solving the Problems]
An object of the present invention is to provide an effective bone mass enhancing composition capable of solving the above-mentioned problems.
The present inventors have intensively studied to solve the above-mentioned object. As a result, it was discovered that by giving the seaweed Akamoku (Honda Walla spp.) Or its water extract as an active ingredient, an excellent bone mass promoting effect was exerted on the rat femur. It has been found that a bone mass promoting composition that exhibits an effective anti-osteoporosis effect can be provided when a functional food or composition for treatment is made.
That is, the present invention provides a bone mass enhancing composition that exhibits an anti-osteoporosis effect, using a dried red mockup or its water extract as an active ingredient. Although it is not certain what mechanism the dried red mushroom and its water extract act on the bone tissue, it is considered that the dried red mokumoku or its aqueous extract has a bone formation promoting action. So far, no bone-enhancing effect is known for dried red mock-up or its water extract.
[0008]
DETAILED DESCRIPTION OF THE INVENTION
The dried red mushroom used in the present invention can be obtained by freeze-drying the whole red mushroom (Sargassum horneri) and then pulverizing it. A water extract of Sargassum horneri can be obtained by adding distilled water to akamoku and pulverizing it, and then separating the water-soluble component.
[0009]
As a specific example of the preferable drying method of red scallop, red squirrel is washed with distilled water, freeze-dried and dried with a mixer to obtain a dry powder. Moreover, as a specific example of a preferable method for extracting water from red peach, extraction is carried out by adding 3 times the amount of distilled water to red peach. This is centrifuged to obtain an extract. The above extract can be used as it is as an active ingredient of a bone augmenting agent, but the extract is further activated by an appropriate means such as silica gel column chromatography, reverse phase column chromatography, gel filtration chromatography, etc. It is also possible to fractionate and use a high fraction.
The dried red mock-up and red water extract obtained in this way have a bone mass promoting action. Therefore, a preparation containing dried dried red mushroom or red dried red mushroom as an active ingredient is useful for promoting bone mass.
When ingesting the composition made according to the present invention, the intake varies depending on symptoms, age, etc., but is not particularly limited. In general, it is recommended that dried red mockup be used in a range of 1 to 5 g / Kg body weight, preferably 10 to 1000 mg / Kg body weight per day. Moreover, it is recommended that the red mushroom water extract (dry weight) be used in the range of 0.1 to 1000 mg / Kg body weight, preferably 1 to 100 mg / Kg body weight per day.
[0010]
It is important that the composition according to the present invention contains dried red mushroom or red water extract as an active ingredient, and minerals such as calcium, magnesium, iron, manganese, copper, vitamin D, vitamin E, It does not matter if vitamins such as ubiquinone, polyphenols, isoflavonoids and flavonoids, peptides such as casein calcium phosphonate, and other normal food ingredients and food additives such as proteins and lipids are included. In addition, pharmaceutical preparations can be made into powders, granules, tablets, powders, etc. using pharmaceutically acceptable carriers, auxiliaries and the like.
Next, in order to demonstrate this invention concretely, although an example is hung up below, this invention is not limited by these.
[0011]
【Example】
Example 1 Powder material [prescription]
Ingredients 1) Akamoku dried product 15g
2) Corn starch 500g
The above raw materials were mixed with a high-speed mixer to obtain a uniform powder. This powder can be mixed into various foods.
[0012]
Example 2 A cocoa-flavored milk drink is obtained by adding 0.2 g of akamoku water extract, 0.5 g of cocoa powder, 30 g of sugar, and 0.5 g of sucrose fatty acid ester to 1 liter of drink milk and stirring vigorously. It was. Since the obtained beverage has a good taste and is easy to drink, it can be eaten and consumed on a daily basis.
[0013]
Example 3 Tablet [Prescription]
Ingredients Blending amount Akamoku water extract 80mg
Drinking beef bone meal 100mg
Lactose 150mg
Palatinose 30mg
Reduced maltose 10mg
Corn starch 10mg
Cellulose powder 10mg
Vitamin D ₃ 201U (international units)
Each raw material was mixed and tableted at the above blending ratio to obtain a tablet. The obtained tablet has a good taste and excellent portability, and can be easily carried and taken.
[0014]
[Performance test of the invention]
Test example Bone mass enhancement effect test [A. Performance test of dried red mockup
In order to examine the bone mass-enhancing effect of dried red mock-up, a freeze-dried powder of red mock-up was orally administered to rats, and bone calcium content and bone alkaline phosphatase activity were measured.
[0015]
[A. 1 Explanation of experimental method]
Akamoku (Sargassum horneri) was washed with distilled water, freeze-dried, and pulverized with a mixer to obtain a dried product (sample 1).
[0016]
The bone mass enhancement effect test of Sample 1 was carried out by orally administering to juvenile male rats (4 weeks old) and reared for 7 days. After 24 hours from the last administration, the femur was removed and the amount of calcium in bone tissue and This was done by measuring alkaline phosphatase activity in bone tissue. Bone alkaline phosphatase is present in osteoblasts (osteoblasts) and is deeply involved in bone formation. As described above, a method for measuring the amount of bone calcium in the femur of a reared rat and a method for measuring the bone alkaline phosphatase activity have been studied as one of methods for evaluating the effect of improving osteoporosis. For breeding, rats are allowed to freely take solid feed (containing 1.1% calcium, 1.1% phosphorus, 0.012% zinc) and distilled purified water, and orally administer sample 1 once a day for 7 days. I went.
[0017]
3 g of sample 1 was orally administered to young rats once a day, and after feeding for 7 days, the bone calcium content and bone alkaline phosphatase activity of the femur were compared with the control (control). The amount of calcium was expressed as the amount of calcium per dry weight of the femur. The amount of calcium was measured by decomposing a dried femur with 2 ml of nitric acid solution at 120 ° C. for 5 hours and using a calcium C test (manufactured by Wako Pure Chemical Industries, Ltd.). Bone alkaline phosphatase activity was measured using the supernatant obtained by crushing and centrifuging the femur as an enzyme solution and using disodium p-nitrophenol phosphate as a substrate. The enzyme reaction was performed by keeping the reaction solution in which the enzyme solution and the substrate were added at 30 ° C. for 30 minutes, and the reaction was stopped by adding 10 ml of 0.05N sodium hydroxide. Bone alkaline phosphatase activity was expressed as the amount of p-nitrophenol (nmol) released by the enzymatic reaction for 1 minute per 1 mg of bone protein.
[0018]
[Explanation of experimental results]
FIG. 1 shows the results of measuring the bone calcium content of the femur extracted from young rats, which were obtained by oral administration of dried dried red mock-up for 7 days, and the bone calcium phosphatase activity is shown in FIG. As shown in FIG. 1, the effect of increasing bone calcium (statistically significant difference, risk rate of 1% or less; p <0.01) was observed in red spider, seaweed, arame, and buckwheat. As shown in FIG. 2, the effect of increasing bone alkaline phosphatase activity (p <0.01) was observed in akamoku and maca. Among the seaweeds tested, only the dry powder of Akamoku showed both bone calcium increasing effect and bone alkaline phosphatase activity increasing effect.
[0019]
[B. Akamoku water extract performance test]
In order to examine the bone mass-promoting effect of the water extract of Sargassum horneri, the water extract of akamoku was added to the medium, the femur of the rat was cultured, and the bone calcium content and bone alkali of the femur after the culture were cultured. The phosphatase activity was measured.
[0020]
[B. 1 Explanation of experimental method]
After adding 3 times the amount of purified distilled water and homogenizing it, it was centrifuged (8000 / rpm for 20 minutes) and divided into supernatant and precipitate. The supernatant was freeze-dried to obtain a freeze-dried sample (sample 2) of the red spider mushroom extract.
[0021]
The bone mass enhancement effect test of Sample 2 was performed by cutting out the femur of a male rat (4 weeks old), transferring it to a 35 mm culture dish containing a culture medium, and measuring the calcium content in the bone tissue after culturing. Thus, the method of measuring the amount of calcium in the cultured tissue of rat femur and the bone tissue alkaline phosphatase activity has been studied as one of the evaluation tests for the effect of improving osteoporosis. The medium used was 2.0 ml Dulbecco's modified Eagle medium (glucose concentration 4.5 g / dl) containing 0.25% bovine serum albumin and antibiotics (100 units penicillin and 100 μg streptomycin / ml medium). Tissue culture was performed using a carbon dioxide incubator for 48 hours at 37 ° C. in a water saturated atmosphere under conditions of 5% carbon dioxide and 95% air.
[0022]
A freeze-dried sample of the akamoku water extract was added to the medium, and the amount of calcium and bone alkaline phosphatase activity in the bone tissue after the culture were compared with the control (control). The amount of calcium was expressed as the amount of calcium per bone tissue dry weight. The dry weight was measured by drying the bone tissue at 100 ° C. for 5 hours. The amount of calcium was measured with a calcium C test (manufactured by Wako Pure Chemical Industries, Ltd.) by decomposing the dried bone tissue with a 2 ml nitric acid solution at 120 ° C. for 5 hours. Bone alkaline phosphatase activity was performed using the supernatant obtained by crushing and centrifuging the femoral tissue as an enzyme solution and using disodium p-nitrophenol phosphate as a substrate. The enzyme reaction was performed by keeping the reaction solution in which the enzyme solution and the substrate were added at 30 ° C. for 30 minutes, and the reaction was stopped by adding 10 ml of 0.05N hydroxide. Bone alkaline phosphatase activity was expressed as p-nitrophenol (nmol) released by the enzymatic reaction for 1 minute per bone protein amount (mg).
[0023]
[B. 2 Explanation of experimental results]
Using the femur tissue of young male rats, the akamoku water extract was added to the culture and the calcium content after 48 hours was measured. The results of measuring the bone alkaline phosphatase activity are shown in FIG. Shown in As shown in FIG. 3, compared with the control, the amount of calcium in the bone tissue is significantly increased (p <0.01) by adding the akamoku water extract to the medium at 25 μg / ml and 50 μg / ml. did. As shown in FIG. 4, the bone alkaline phosphatase activity was also significantly increased (p <0.01) by adding to the medium at 25 μg / ml and 50 μg / ml. Thus, the water extract of akamoku showed bone calcium increasing effect and bone alkaline phosphatase activity increasing effect in tissue culture system of rat femur.
[0024]
【The invention's effect】
As described above, the anti-osteoporosis composition of the present invention is safe because it is a dry matter and water extract prepared from red seaweed, a seaweed with a long dietary history, and is taken daily for preventive purposes from an early age. As well as protecting the quality of life of individuals after retirement, it can be expected to contribute to reducing medical costs in an aging society.
[0025]
[Brief description of the drawings]
BRIEF DESCRIPTION OF DRAWINGS FIG. 1 is a graph showing the effect of oral administration of dried akamoku on the amount of calcium in the femur of young rats.
FIG. 2 is a graph showing the effect of oral administration of dried red swordfish on bone alkaline phosphatase activity in the femurs of young rats.
[Fig. 3] Fig. 3 is a graph showing the effect of adding a red seamoku water extract on the amount of calcium in rat femur.
[Fig. 4] Fig. 4 is a graph showing the effect of adding an aqueous extract of akamoku on bone alkaline phosphatase activity in rat femur.

Claims (2)

Bone formation enhancing composition that exhibits anti-osteoporosis effect, using dried dried red moss (Honda Walla) as an active ingredient Bone formation enhancing composition that exhibits an anti-osteoporosis effect by using the water extract component of Akamoku (Honda Walla) as an active ingredient

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