KR20040057103A - Composition for a degenerative arthritis comprising a seaweed extract - Google Patents

Abstract

PURPOSE: Provided is therapeutic composition for degenerative joint disease containing seaweed extract. The composition has strong antioxidation effect to inhibit the activity of elastase, therefore, it inhibits the decomposition of elastin and collagen, and improves degenerative joint disease without adverse effects. CONSTITUTION: A therapeutic composition for degenerative joint disease is characterized by containing seaweed extract which contains 10% or more polyphloroglucinol complex(PPC). The seaweed includes Porphyra tenera KJELLMAN, Costaria costata (TURNER)SAUNDERS, Hizikia fusiforme (HARVEY) OKAMURA, Undaria pinnatifida (harvey) SURINGAR, Meristotheca papulosa, Enteromorpha, Porphyra tenera, Laminaria japonica , Rheum coreanum Nakai., Acanthogobius hasta (Temminck et Schlegel), Gigartina tenella, Gallicrex cinerea cineria, G. furcata, Campylaephora hypnaeoides, Spirulina, Gelidium amansii, Chondrus ocellatus Holmes, Codium Fragile, Chlorella and the like.

Description

Composition for a degenerative arthritis comprising a seaweed extract}

The present invention relates to a degenerative arthritis composition comprising a seaweed extract having an effect of improving degenerative arthritis, and more particularly, a degenerative disease such as degenerative arthritis caused by degenerative changes in cartilage and bones around the joint. For the prevention and improvement of the degenerative arthritis composition comprising seaweed extract containing 10% or more of the polyphloroglucinol complex (hereinafter referred to as "PCC") consisting of 15 polyphenols extracted from seaweed It is about.

The seaweed extract has a strong antioxidant effect of inhibiting the activity of elastase, which is one of the components of matrix-metallo-proteinases (MMPs) consisting of 14 or more degrading enzymes. It has the effect of inhibiting the breakdown of elastin and collagen in tissues due to the inflammatory response.

On the other hand, in general, degenerative arthritis is one of chronic arthritis, a degenerative change occurs in the articular cartilage that receives a lot of weight, resulting in overgrowth of the joint bone, and is often seen in middle-aged adults. The disease is first depleted due to aging of the cartilage cells that make up the cartilage composition, the cartilage loses its elasticity, over time, the surface of the cartilage becomes rough, and the various kinds of substances inside the joint cavity wrapped in the joint membrane This influx causes inflammation. Clinically, recurrent pain, joint stiffness, and gradual dyskinesia of the joints are present. This disease is the most common inflammatory disease of the joints, it is known that about 80% of people over 55 years of age, almost all over 75 years old have this disease. Only about 25% of these symptoms are clinical. The older they are, the more severe the clinical symptoms are in women than in men.

Since such degenerative arthritis is due to the degeneration of articular cartilage, there is no sure way to completely stop this degeneration, and the general method of treating degenerative arthritis is to temporarily reduce pain only by using an anti-inflammatory or analgesic agent. However, the use of such anti-inflammatory agents and analgesics interferes with cartilage regeneration ability, accelerates cartilage destruction of joints, worsens the patient's condition, and causes side effects such as stomach, liver, and kidneys.

Therefore, there is an urgent need for the development of new degenerative arthritis improving agents that have sufficient effects without side effects.

Therefore, the present inventors conducted a study to solve the problems such as side effects, lack of efficacy and safety of the conventional degenerative arthritis improvers, containing a polyfluoroglucinol complex consisting of 15 polyphenol compounds extracted from marine plants The seaweed extract was developed as a degenerative arthritis improving agent. According to clinical trials, the degenerative arthritis improving seaweed extract exhibited a strong antioxidant effect and an inhibitory activity of elastase to inhibit the degradation of elastin and collagen in the tissues. It is not merely a pain relief or anti-inflammatory effect, but showed an excellent effect on the improvement of degenerative arthritis, and the present invention was completed based thereon.

Accordingly, an object of the present invention is to prevent and improve degenerative diseases such as degenerative arthritis caused by physical and biochemical degeneration of tissues due to destruction and degeneration of cells by depleted oxygen and deterioration of blood vessel and blood function. Seaweeds that inhibit the activity of elastase, one of the components of matrix-metallo-proteinases (MMPs) consisting of 14 or more degrading enzymes that cause elastin and collagen breakdown and joint breakdown To provide a degenerative arthritis composition comprising a seaweed extract containing a polyfluoroglucinol complex consisting of 15 polyphenols extracted from.

Another object of the present invention is to provide a degenerative arthritis composition comprising the seaweed extract added as an additive to medicines, dietary supplements, special nutritional products, beverages and liquors, food additives, sweets or bread.

The degenerative arthritis composition of the present invention for achieving the above and other objects includes a seaweed extract containing more than 10% of the polyphloroglucinol complex (PPC, Polyphloroglucinol complex).

1 is a bar graph comparing the antioxidant activity of the seaweed extract according to the present invention and the antioxidant activity of the chemically synthesized BHT and BHA, and the natural antioxidant tocopherol.

Figure 2 is a graph showing the elastase inhibitory activity of seaweed extract according to the present invention.

Figure 3 is a bar graph showing the therapeutic distribution when the composition according to the present invention in male and female patients with degenerative arthritis.

Figure 4 is a bar graph showing the results of treatment according to clinical symptoms when taking the composition according to the present invention to male and female patients with degenerative arthritis.

Hereinafter, the present invention will be described in more detail.

As described above, the present invention relates to a degenerative arthritis composition comprising algae extracts having an effect of improving degenerative arthritis, and more particularly, tissues may be deteriorated by degeneration and degeneration of cells and deterioration of blood vessels and blood function by free radicals. Matrix-metallo-pro is made up of 14 or more degrading enzymes that cause degradation of elastin and collagen and joint degradation in tissues for the prevention and amelioration of degenerative diseases such as degenerative arthritis caused by physical and biochemical degeneration. Algae containing more than 10% of polyfluoroglucinol complex consisting of 15 polyphenols extracted from seaweeds that inhibit the activity of elastase, one of the components of matrix-metallo-proteinases (MMPs) It relates to a degenerative arthritis composition comprising an extract.

Seaweed extract used for the improvement of degenerative arthritis according to the present invention is a material extracted from edible seaweed, and contains 15 antioxidant polyfluoroglucinol complexes which have a strong antioxidant function and inhibit the activity of elastase. The polyfluoroglucinol complex inhibits the activity of the aldose reductase enzyme, an enzyme that is involved in the formation of advanced glycation end-products (AGEs) by binding glucose to proteins in the blood, thereby reducing sugars in the blood to AGEs. Not only does it effectively block the conversion, it also has a powerful antioxidant that removes excess free radicals to protect the vascular endothelium and has an excellent anti-inflammatory effect.

The seaweed extract is brown seaweed, mabanban, forked bear, green, Ecklonia, sesame, kelp, rhubarb, seaweed, bratwurst, stone starfish, boulder, moss, falconus, independence starfish, stone, spirulina, wood starfish, jindubal, hearing, chlorella And one or more selected seaweeds selected from the group consisting of gompi.

The polyfluoroglucinol complex is a polyphenol-based compound including ecol, dieckol, phlorotannin A, phlorofucopurocol, 7,7'-bieckol, 9,9'-bieckol and glycosides thereof.

The seaweed extract can be obtained in the present invention that the polyfluoroglucinol complex containing at least 10% by weight.

The composition of the present invention may include vitamins or various other ingredients depending on the method of ingestion, the form of addition and the form of the formulation. In addition, the composition may be added to medicines, dietary supplements, special nutrition, beverages and alcohol, food additives, sweets or bread. In addition, the formulation of the composition of the present invention may be tablets, capsules, pills and granules. .

The composition of the present invention is preferably taken at least 100mg per day seaweed extract containing more than 10% polyfluoroglucinol complex, there is no side effect because it is a product obtained from natural foods in excess.

Hereinafter, the present invention will be described in more detail with reference to the following examples, but the scope of the present invention is not limited to the following examples.

Example 1

Preparation of Seaweed Extract

By the seaweed in Ecklonia cava taken from water (Ecklonia cava), fusiformis (Hizikia fusiformis), Sargassum (Sargassum fulvellum), rhubarb (Eisenia bicyclis), gompi (Eisenia stolonifera), kelp (Laminaria japonica), first washed with distilled water to remove foreign material After drying in the back shade, crush it. 500 g of algae consisting of the algae (e.g., 300 g of Ecklonia cava, 30 g, Mabban 40 g, Dashima 40 g, rhubarb 50 g, Gompi 40 g) is extracted under reflux for 2 hours to elute the active substance using a 20-fold 85% alcoholic solvent. . This process was repeated twice. Then, the residue was filtered off and the solvent extract was concentrated under reduced pressure using a rotary evaporator. The concentrated solution is suspended in 20 times distilled water, and the aqueous layer is concentrated under reduced pressure, followed by a lyophilization process to obtain a powder form. The lyophilized powder is extracted at room temperature for 2 hours to elute the active substance using 95% alcohol of 5 times the content. The residue contained in the extract solution is filtered off and the solvent extract is concentrated under reduced pressure to obtain a concentrate. After loading this concentrate on 20-50 times of silica gel, the polyphenol concentrate is obtained using the mixed solvent of ethyl acetate / methanol (volume ratio 10/1). This was lyophilized to obtain 192 g of seaweed extract having 10% by weight of polyfluoroglucinol complex.

Example 2

Antioxidant Activity of Seaweed Extracts

In order to measure antioxidant activity, 15 ml of ethanol was added to 2 mg of DPPH to dissolve. Then, 600 µl of DPPH solution was taken and mixed with 250 µl of DMSO and 1500 µl of ethanol to finally prepare DPPH solution for initial absorbance (B). 900 μl of the prepared DPPH solution is placed in a cuvette and the initial absorbance (B) is measured at 518 nm. At this time, the initial absorbance is measured so as to be in the range of 0.94 to 0.97. When the initial absorbance is 0.97 or more, the ethanol is further added and diluted, and if it is too low, a solution made by adding 15 ml of ethanol to 2 mg of DPPH is added to measure the initial absorbance. When the initial absorbance is properly adjusted, 100 μl of seaweed extract powder, tocopherol, BHT and BHA samples dissolved in methanol are placed in a cuvette and measured at 518 nm for 10 minutes at 10 second intervals. The antioxidant activity at this time is represented by A.

Antioxidant activity (A) = B (initial absorbance)-C (absorbance after measurement)

Where B is the initial absorbance, 0.94-0.97, and C is the lowest absorbance measured over 10 minutes. The antioxidant activity thus measured is shown in FIG. 1. As shown in FIG. 1, the seaweed extract containing the polyfluoroglucinol complex composed of 15 polyphenol compounds showed 5 to 10 times antioxidant activity compared to chemically synthesized BHT and BHA, and a natural antioxidant tocopherol. It also showed about twice the antioxidant activity.

Example 3

Determination of Elastase Inhibitory Activity of Seaweed Extracts

To measure the elastase inhibitory activity, first, 1 mg of enzyme (PPE) was added to 2.8 ml of 0.4 M HEPES buffer (pH 6.8) to prepare an enzyme solution in 0.5 unit. 275 μl of HEPES buffer (pH 6.8), 100 μl of sample (MeOH), 100 μl of Suc- (Ala) 3-PNA, 5 μm of substrate, and 5 μl of DMSO were mixed in a cuvette and incubated for 25 to 3 minutes 40 seconds. 20 μl of 0.5 unit enzyme (PPE) solution is added and measured at 410 nm for 60 seconds. At this time, the reference value should be in the range of 1.5 × 10 ^-3-2.5 × 10 ^-3 Au / sec. Measurement of the sample is performed in the same volume of the sample prepared in place of MeOH, the rest using the solutions that were used as a reference value above. The inhibition rate is expressed in percent, and the percent value is calculated in the same manner as in Equation 1 below.

Inhibition (%) = 100-(sample / control × 100)

The result of comparing the elastase inhibitory activity according to the concentration is shown in FIG. As shown in Figure 2, seaweed extract showed excellent elastase inhibitory activity (IC ₅₀ = 10 g / ㎖). Therefore, by inhibiting the activity of the elastase, one of the MMP components, it was possible to suppress the degradation of elastin and collagen in the tissue and to prevent arthritis.

Example 4

Manufacture of Seaweed Extract Capsule

In order to satisfy the nutritional supplement standard prescribed in the Food Code, 398 mg of seaweed extract of Example 1 were mixed with 0.6 mg of vitamin B1, 0.6 mg of B2 and 0.8 mg of B6 uniformly for 15 minutes using a stirrer, and then placed into a hard capsule. Filling was prepared.

Comparative Examples 1 and 2

In order to compare the efficacy of the composition of Example 1, instead of the seaweed extract was performed in the same manner using glucosamine and kelp powder.

Component Contents of Example 4 and Comparative Examples 1 and 2 Furtherance Example 4 Comparative group 1 Comparative Group 2 chief ingredient Seaweed Extract 398mg Glucosamine 398mg Kelp powder 398mg Vitamin B1 0.6mg 0.6mg 0.6mg Vitamin B2 0.6mg 0.6mg 0.6mg Vitamin B6 0.8mg 0.8mg 0.8mg

Example 5

Efficacy Cognitive Experiment of Seaweed Extract

Thirty female patients with degenerative arthritis were divided into three groups of 10 patients, each of which contained 400 mg of the composition of Example 4, Comparative Example 1 and Comparative Example 2 into hard capsules, two daily. Weekly intake. Two weeks later, a sensory test was conducted to evaluate the degenerative arthritis effect. The test results are shown in Table 2 below.

The score at the time of examination was given as follows.

1: No effect at all

2: Not very effective

3: Normal.

4: It works a bit.

5: Very effective.

Sensory Effects on the Improvement of Degenerative Arthritis sample Finger joint joint pain Swelling of the back of the hand Changes in Knee Joint Pain Fifty dogs Example 4 5 4 5 5 Comparative Example 1 4 3 4 3 Comparative Example 2 One One 2 One

As shown in Table 2, the degenerative arthritis composition comprising the seaweed extract of the present invention, compared to glucosamine and kelp powder generally known to be effective for degenerative arthritis, joint pain in the knuckle, swelling of the hand, knee joint pain, pain in the shoulder Significantly improved the general symptoms of degenerative arthritis.

Example 6

Clinical trial in patients with degenerative arthritis

The trial included 100 patients with degenerative arthritis (men: 17, women: 83, children under 30: 2, 40: 8, 50: 40, 60: 27, 70: 18, More than 80s: 5 people) was administered 400mg twice each of the composition of Example 4 for 8 weeks, and then clinically observed and analyzed. In order to observe the progress of treatment, the patients were divided into starting pain box (degrees II), load pain (degrees III), active active pain (degrees IV), and rest pain (degrees V). This is shown in Table 3 below.

Pain degree comparison Pain Severe pain at first visit I degree Because of other symptoms of the knee, I come to the hospital and have no pain in my daily life, and I feel tired, heavy, or not fit. 0 Ⅱ degree There is a bit of pain and patience at the start of various movements, no disruption to life and work, and pain after a long day of work or after a long walk. 0 Ⅲ degrees It hurts when walking and is reduced or lost after a short break. Pain may attract the patient's attention or disturb the emotions, but activity or life is possible and persevering. Interfering with exercise and severely affects your work. 63 IV degree Intense pain during loads or movements can interfere with activity, affect life and always take painkillers. It is reduced after a break, but soon becomes ill or spontaneous. 28 Ⅴ degree Not only at rest, but also at any activity, there is intense pain, so you can't do it, you can't live your life, you can't stand it without taking painkillers, and even if you take medicine, you have pain and rest and sleep. . 9

The evaluation criteria of treatment grade were as follows.

Excellent: When you can do enough of your daily activities and activities without pain.

Good: Sometimes you have discomfort in the affected area

Fair: If you can't exercise severely with some restrictions

Poor: Continued pain and no improvement or worsening of symptoms

1) Distribution according to therapeutic result

There were 68 good patients, 13 excellent, 10 good and 9 poor. This was shown in Table 4 below.

Distribution of personnel according to treatment result male female sum Great 3 10 13 Good 8 60 68 Improvement 5 5 10 Bad One 8 9 sum 17 83 100

2) Treatment result by clinical symptom grade

In case of pain degree Ⅲ, there were 8 excellent, 44 good, 6 good and 5 poor. For pain Ⅳ, 5 good, 18 good, 2 good, 3 poor. In the degree of pain V, 6 patients were good, 2 patients improved, and 1 patient was poor. This was shown in Table 5 below.

Therapeutic Distribution by Clinical Symptom Grade Pain Bad Improvement Good Great sum Ⅲ 5 6 44 (69.8%) 8 63 Ⅳ 3 2 18 (64.2%) 5 28 Ⅴ One 2 6 (66.6%) 0 9 sum 9 10 68 (68%) 13 100

3) Treatment Result by Age

In patients under 30 years of age, 1 patient each was excellent and good. In the 40s, 2 patients were poor, 4 patients were improved, 1 patient was good, 1 patient was excellent. There were 30 good, 5 good, 3 poor, 2 good, 19 good, 3 good, 60 good, 1 poor, 15 good, 2 good, and 80 poor. One person, one improvement, two good, and two good showed relatively even distribution. This was shown in Table 6 below.

Treatment Outcome by Age Bad Improvement Good Great sum Under 30 0 0 One One 2 40 spaces 2 4 One One 8 50 spaces 2 3 30 5 10 60 spaces 3 2 19 3 27 70 spaces One 0 15 2 18 80 spaces One One 2 One 5 sum 9 10 68 13 100

4) Treatment result according to medical history

In the case of less than 1 month, there were 2 defects, and less than 3 months and less than 6 months each had 1 defect and improvement. In the case of medical history of, 6 patients were good and 6 were excellent. In the history of 10 to 10 years, there was 1 poor, 1 improved, 10 good, 2 excellent, and 2 years better than 20, 2 good, 3 good, excellent. There were one patient, and more than 20 years of history showed improvement in 2 patients, good in 4, and good in 1. In patients with a short history of less than 6 months, patients with a long history of more than 6 months showed more improvement of treatment. This was shown in Table 7 below.

Therapeutic distribution according to medical history Bad Improvement Good Great sum 1 month or less 2 0 0 0 2 3 months or less One One 0 0 2 6 months or less One One 0 0 2 Less than 1 year One 0 11 0 2 1 year-3 years 0 0 6 6 12 3 to 5 years 3 3 34 3 43 5 to 10 years One One 10 2 14 10-20 years 0 2 3 One 6 More than 20 years 0 2 4 One 7 sum 9 10 68 13 100

5) Treatment result analysis by treatment period

Fourteen patients showed improvement after treatment at week 1, and 44 patients showed improvement after treatment at week 2, and 26 patients showed improvement after treatment at week 3. There were 5 patients who showed improvement after 4 weeks of treatment, and 2 patients who showed improvement after 5 weeks to 8 weeks of treatment. This was shown in Table 8 below.

Therapeutic distribution by treatment period Improvement Good Great sum <1 week 2 8 4 14 <2 weeks One 40 3 44 <3 weeks 3 18 5 26 <4 weeks 3 One One 5 <5 weeks One One 0 2 <6 weeks 0 0 0 0 <7 weeks 0 0 0 0 <8 weeks 0 0 0 0 sum 10 68 13 91

As described above, as a result of ingesting the composition of the present invention in a patient with degenerative arthritis, the treatment of chronic degenerative arthritis, such as significantly improving the general symptoms of degenerative arthritis such as arthralgia of the knuckle, swelling of the hand, knee joint pain, pain of the shoulder and shoulder, etc. The results showed a significant effect, and were more meaningful because it was a clinical trial involving 100 patients who did not improve significantly with the existing treatments except for arthroplasty. Indicated.

In the above clinical trials, the results of improvement or improvement showed 91% of the total and 81% of good and excellent treatment results. In particular, there were many cases of more than good results in patients with a relatively long history of more than 6 months. In the 8-week clinic, most patients showed improvement after 2 weeks of treatment, and improved within 3 weeks. In view of the 92.3% of patients who showed the above treatment results, the composition of the present invention was found to be a suitable material for significantly improving degenerative arthritis.

As described above, the efficacy of the degenerative arthritis composition comprising the seaweed extract of the present invention is superior to glucosamine used as an important component of articular cartilage, and high pain relief and improvement were obtained. Therefore, it inhibits the activity of elastase that causes collagen breakdown and joint breakdown due to inflammatory reactions, thereby reducing the breakdown of elastin and collagen in tissues, and has a strong antioxidant ability to inhibit free radicals. Degenerative arthritis compositions comprising seaweed extracts containing phloroglucinol complexes can prevent or ameliorate degenerative arthritis.

Claims (5)

A degenerative arthritis composition comprising seaweed extract containing more than 10% of the polyfluorologusinol complex (PPC, Polyphloroglucinol complex). According to claim 1, wherein the seaweed extract is seaweed, mabanban, forked bear, green, Ecklonia cava, 톳, kelp, rhubarb, seaweed, stalk, dolphin, round stone, squirting, falconus, light starfish, stone, spirulina, wood starfish, A composition characterized in that it is obtained from one or more selected seaweeds selected from the group consisting of auspidia, auditory, chlorella and gompi. The method of claim 1, wherein the polyfluoroglucinol complex comprises exocol, dieckol, fluorotannin A, fluorofucofuro exocol, 7,7'-bieckol, 9,9'-bieckol and glycosides thereof A composition comprising a polyphenol type. The composition of claim 1, wherein the composition is added to medicines, dietary supplements, special nutritional supplements, beverages and liquors, food additives, confectionery or bread. The composition of claim 1 wherein the formulation of the composition is a tablet, capsule, pill or granule.