JPH10114669A - Antiinflamatory agent - Google Patents

Abstract

PROBLEM TO BE SOLVED: To extract an antiinflammatory agent with a solvent from a plant extract having antiinflammatory effect. SOLUTION: Fresh leaf or dried leaf of prune is extracted with a hydrophilic solvent such as water, cold water, hot water, ethanol or glycerol and the extract is directly used or used as an antiinflammatory agent a diluted or concentrated state or in the form of concentrated and dried or freeze-dried powder or granule or tablet.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to anti-inflammatory agents and compositions thereof.

[0002]

2. Description of the Related Art Generally, inflammation is a defense reaction of a living body that attempts to repair and regenerate the damaged site when an invasion that causes some organic change to cells and tissues of the living body is caused and damage occurs. It is considered that the reaction involves local body fluids, blood vessels, various tissue cells, phagocytes, immune cells, and the like. Since the body suppresses the spread of damage to tissues and cells by this defense reaction, and tries to eliminate the cause of the damage and repair the tissue, it is not preferable to suppress inflammation unnecessarily. However, at this time, the inflammation itself includes factors unfavorable for the living body, such as excessive pain, swelling, itching and fever caused by the inflammation, and the tissue damage may be amplified in reverse. Therefore, it is necessary to suppress excessive inflammation in order to reduce the pain of the patient, and an anti-inflammatory agent is administered as a means of suppressing inflammation.

[0003] Drugs developed and used for the treatment of inflammation have excellent anti-inflammatory effects, but most drugs have a prostaglandin biosynthesis inhibition mechanism as their anti-inflammatory action. It is well known that it has a strong physiological action other than the anti-inflammatory action. For example, non-steroidal compounds represented by aspirin, indomethacin and the like are known to exhibit anti-inflammatory effects by inhibiting the synthesis of arachidonic acid endoperoxide.

[0004] Methods for evaluating the efficacy of anti-inflammatory drugs include:
It is common to examine the healing effect on various inflammation models. As a model to reproduce the pathology of inflammation, the behavior exhibited when a physical or chemical stimulus is applied to the local area of the animal is regarded as a pain response, a pain model that examines the effect on this, a vascular permeability at the inflammatory site, There is a model that reproduces edema associated with the leakage of plasma components due to hypertension, and a model of ultraviolet irradiation-induced erythema that reproduces inflammatory redness due to an increase in blood flow due to vasodilation of the inflammatory site.

[0005] Among them, an edema model induced by inoculating carrageenan, a kind of polysaccharide, into rat footpads is an inflammation caused by non-specific stimulation involving various chemical mediators over time, and various anti-inflammatory It is known that it is well controlled by the agent.

The prunes (Prunus dome) used in the present invention
stica L.) is a kind of western plum belonging to the genus Sakura, Rosaceae, is a deciduous fruit tree of 3-8 m in height of middle and high trees, the leaves are smaller than the fruits, thicker and shiny, the fruits are oval or It is egg-shaped. And the color of the peel (epidermis)
It is blue-black or yellow with indistinct speckles and the flesh (mesocarp) is yellow, hard, sweet and sour, and aromatic.

[0007]

However, most of the conventional anti-inflammatory agents are chemically synthesized products, and considering the side effects thereof, studies on natural plant extracts have been scarce and their appearance has been desired. The present inventors have conducted intensive studies on plant extracts having an anti-inflammatory effect, and found that pruned leaf extracts have an excellent anti-inflammatory effect. It is an object to extract and provide by using

[0008]

SUMMARY OF THE INVENTION The present invention has been accomplished to solve the above-mentioned problems. The present invention provides a method for producing fresh or dried leaves of prunes using a hydrophilic solvent such as water, cold water, hot water, ethanol or glycerin. The extract is used as an anti-inflammatory agent as it is, or in a diluted or concentrated state, or in the form of a concentrated dried, lyophilized powder, granules, tablets or the like.

[0009]

EXAMPLES Hereinafter, the present invention will be described in more detail with reference to Examples and Experimental Examples. However, the present invention is not particularly limited as long as it is a means and a solvent that can effectively extract the active ingredient of the present invention. It is not limited at all by the following production examples, preparation examples, and pharmacological test results.

Example 1 Production of Prune Leaf Extract (Example 1) 100 g of fresh leaves collected from prunes cultivated for harvesting fruits are cut into small pieces, and 10 times the amount of about 90
The obtained extract was decompressed and concentrated at about 60 ° C. and freeze-dried to obtain 1.93 g of dry powder.

(Example 2) 100 g of fresh leaves collected from prunes cultivated for harvesting fruits were shredded, and 10
It was immersed in twice the amount of normal temperature 30% ethanol for 4 days, and filtered to obtain 917 g of 30% ethanol extract.

Example 3 92 g of fresh leaves collected from prunes cultivated for harvesting fruits were shredded, immersed in a 10-fold amount of room temperature reagent primary grade ethanol for 4 days, filtered, and subjected to ethanol extraction. 724 g were obtained.

Test Example (Rat Carrageenin Edema Inhibitory Effect) Preparation of Test Substance An ointment in which 5% of prune leaf extract (Example 1) was uniformly dispersed in Macrogol ointment of the Japanese Pharmacopoeia was prepared. Macrogol ointment as a base material was used for a control group.

Test Method Five rats (wister / SPF, male, 6 weeks old, weighing about 150 g) were grouped into one group, and a 5% ointment containing a test substance was administered to the right hind paw with administration of a proinflammatory agent (carrageenin) 2 and 50m one hour ago
g each, and film (manufactured by American National Can)
Covered lightly. Next, a 1% solution of carrageenin (manufactured by Wako Pure Chemical Industries, Ltd.) prepared using physiological saline in advance was added. l m
was injected subcutaneously into the right hind footpad of the rat, the volume of the paw was measured 1, 2, 3 and 4 hours after administration of the proinflammatory agent, and the edema rate was calculated according to the following equation (1). . In addition, the suppression rate was calculated according to the formula shown in Expression 2 by comparison with a control group (placebo).

[0015]

(Equation 1)

[0016]

(Equation 2)

Test Results The edema rate of each group is shown in Table 1 as mean ± standard deviation, and the inhibition rate at 4 hours after carrageenin administration calculated based on the edema rate of the control group is also shown in the table. As is clear from Table 1, the prune leaf extract showed an excellent carrageenan edema inhibitory action.

[0018]

[Table 1] Edema rate (%) Mean ± standard deviation Test group 1 hour 2 hours 3 hours 4 hours After inhibition rate (%) Control group 89.6 ± 3.6 81.2 ± 14.6 85.0 ± 24.8 81.9 ± 15.4-Test substance 71.0 ± 11.3 72.0 ± 20.5 75.0 ± 20.6 60.2 ± 17.4 26.5

Example 4 Hard Candy A hard candy having the composition shown in Table 2 was evaluated by comparing an example with a comparative example. The manufacturing method followed the manufacturing method of the usual hard candy.

[0020]

Table 2 Composition Example 4 Comparative Example 1 Granulated sugar 54.0% by weight 55.0% by weight Water candy 45.0 45.0 Prune leaf extract 1.0 --- (Example 1) Total 100 100

Evaluation Method A paneler having rhinitis (sneezing, nasal discharge), sore throat and cough was ingested 4 g of the hard candy of Comparative Example 1 three times a day for three consecutive days in the morning, noon, and night. 8 panelists (6 males and 2 females) who did not see the hard candy of Example 4 were similarly ingested for 5 consecutive days and evaluated. Table 3 shows the results.

[0022]

Table 3 Evaluation Example 4 Comparative Example 1 Significantly improved 0 0 Slightly improved 60 0 No effect 2 8 Deteriorated 0 0

As is clear from Table 3, Example 4 showed an improvement in symptoms as compared with Comparative Example 1, and had no problems such as side effects.

Example 5 About 100 g of fresh leaves of tea prune were steamed in steam for about 40 minutes, and then dried at 60 ° C. for 3 hours to give a final moisture of 3.5.
% Of steamed prune leaf tea was prepared.

Evaluation Method For 12 panelists (9 males and 3 females) having rhinitis (sneezing, nasal discharge), sore throat and cough, 5 g of the pruned leaf tea of Example 5 was teased for 2 minutes. The tea was evaluated for four consecutive days of drinking instead of the usual tea.
Table 4 shows the results.

[0026]

[Table 4] Evaluation Example 5 Significant improvement 2 Slight improvement 5 No effect 5 Deterioration 0

As is evident from Table 4, an excellent improvement effect was observed in Example 5, and there were no problems such as side effects.

(Example 6) Lotion The lotion having the composition shown in Table 5 was evaluated by comparing Example 6 with Comparative Example 2. The production method was in accordance with the usual lotion production method.

[0029]

Table 5 Composition Example 6 Comparative Example 2 Ethanol 8.0% by weight 8.0% by weight Glycerin 2.0 2.0 Citric acid 0.2 0.2 Sodium citrate 0.1 0.1 Sorbitol -2.0 (methyl paraben) 0.02 0.02 Flavor 0.1 0.1 Pruned leaf extract (Example 2) 1.0---Purified water 86. 58 87.58 Total 100 100

(Example 7) Cream A cream having the composition shown in Table 6 was evaluated by comparing Example 7 with Comparative Example 3. In addition, the manufacturing method followed the normal cream manufacturing method.

[0031]

Table 6 Composition Example 7 Comparative Example 3 Stearic acid 9.0% by weight 9.0% by weight Cetanol 3.5 3.5 Lanolin 1.0 1.0 Octyldodecyl myristate 10.0 10.0 Polyoxy Ethylene 1.0 1.0 Sorpitan monooleate Polyoxyethylene 3.0 3.0 Sorpitan monostearate Methylparaben 0.2 0.2 Propylene glycol 3.0 3.0 Triethanolamine 0.5 0.5 Incense 0.5 0.5 Prune leaf extract (Example 2) 2.0 --- Purified water 66.3 68.3 Total 100 100

Evaluation method To 9 female panelers each having itching or sunburn pain, the lotion (Example 6) and cream (Example 7) shown in Tables 5 and 6 were applied to the right arm, and Examples 6 and 7 were applied to the right arm. Comparative Examples 2 and 3 were applied to the left arm twice a day in the morning and at night, and a usage test for three consecutive days was performed to evaluate the left arm. Table 7 shows the results.

[0033]

[Table 7] Evaluation Example 6 Comparative Example 2 Example 7 Comparative Example 3 Itching and pain are remarkably reduced 10 4 0 Slightly reduced 6 1 4 2 No effect 2 8 17 Deterioration 0 0 0 0

As is evident from Table 7, Examples 6 and 7 exhibited excellent improvement effects, and there was no problem with skin irritation.

[0035]

EFFECT OF THE INVENTION The pruned leaf extract of the present invention has an anti-inflammatory effect, contains a natural plant extract as an active ingredient, and has an excellent carrageenin edema inhibitory effect. In addition, these components can be added to foods and cosmetics to reduce various inflammations and to improve itching of the skin.

──────────────────────────────────────────────────の Continued on the front page (51) Int.Cl. ⁶ Identification code FI A61K 7/00 A61K 7/48 7/48 A23L 2/00 F

Claims (3)

[Claims] 1. An anti-inflammatory agent comprising, as an active ingredient, an extract obtained by extracting prune leaves using a hydrophilic solvent. 2. Cosmetics containing the anti-inflammatory agent according to claim 1. 3. A food containing the anti-inflammatory agent according to claim 1.