JP2916925B2 - Superoxide scavenger, food and drink and cosmetics - Google Patents

Description

Description: TECHNICAL FIELD The present invention relates to a superoxide scavenger that can be used in the fields of medicine, food, cosmetics, and the like, and to a superoxide scavenging food, beverage, and cosmetic. .

Radical O ₂ occurring at one-electron reduction of [Prior Art] superoxide i.e. oxygen molecules ^- are known to act as an important protective factor in vivo. For example, bacteria,
Neutrophils, monocytes,
Phagocytic cells such as macrophages are activated to develop dynamic functions such as migratory ability and phagocytosis, and as a result, lysosomal enzymes and superoxide are produced and secreted, which are directly or thorough in the melting and sterilization of poor foods. Involve indirectly and protect the body from external enemies.

On the other hand, superoxide causes various tissue disorders when present in an excessive amount in a living body. Normally, the amount of superoxide generated in a living body is about 1% or less of oxygen absorbed by respiration, and this is sequentially eliminated by the catalytic action of superoxide dismutase (SOD) contained in cells. In cases where the enzymatic action is reduced, such as in the elderly, the elimination is inadequate and the concentration of superoxide increases, which can lead to tissue disorders such as rheumatoid arthritis and Behcet's disease, and the superoxide or the resulting superoxide. Myocardial infarction, stroke, cataract, spots, freckles, wrinkles, diabetes,
Causes arteriosclerosis, stiff shoulders, and coldness. Even if you are not an old man, skin is an organ that is particularly easy to produce superoxide because it is directly stimulated by environmental factors such as ultraviolet rays,
An increase in the concentration of superoxide and the production of lipid peroxide accompanying the superoxide concentration are apt to occur, which is liable to cause melanin pigment formation, spots, fine wrinkles and the like.

Attempts to use superoxide dismutase as a pharmaceutical or in cosmetics or foods to prevent or treat the above-mentioned various disorders caused by excess superoxide have been made because the enzyme is unstable to heat and inactivated. It has been unsuccessful because of its simplicity and its significant cost.

Attempts to find substances other than superoxide dismutase for substances having a superoxide-eliminating action (hereinafter referred to as SOD-like substances) in the same manner as superoxide dismutase are described in JP-A-64-50877. Baikarain in Huangfen is used. However, baicalein is contained only a little in Huangfen, and its extraction is extremely expensive.

[Problems to be solved by the invention]

An object of the present invention is to provide a superoxide scavenger comprising a stable SOD-like substance, which is not unstable like superoxide dismutase and can be easily incorporated into pharmaceuticals, cosmetics, foods and the like.

Another object of the present invention is to provide a food and drink and a cosmetic that are effective in healthy growth and beauty by containing a stable SOD-like substance.

[Means for solving the problem]

The present invention provides a superoxide eliminator comprising, as an active ingredient, a pear juice or a synthetic resin adsorption part thereof.

The present invention also provides superoxide-eliminating foods and drinks and cosmetics to which the superoxide-eliminating agent according to the present invention is added.

Pears (Rosa roxburghii Tratt.f.normalis Rehd.et W
ils.) is a plant of the family Rosaceae, which is native or cultivated in Jiangsu, Hubei, Sichuan, Guizhou, Yunnan and Guangdong provinces of China. The fruit is said to have a stomachic effect and has been eaten raw or decocted since ancient times. In addition, a large amount of vitamin C
It has been found that fruit juice is used as a beverage in recent years.

The present invention is based on the discovery of a remarkable superoxide scavenging effect on the juice of the above-mentioned pears as a result of extensively searching for SOD-like substances that are stable to heat and to a large extent pH fluctuation.

As for the pear juice, a concentrate with an extract content of about 50% is commercially available, and the superoxide scavenger of the present invention may be used as it is, but the SOD-like substance in the juice is non-polar or intermediate polar. Is selectively adsorbed on the synthetic adsorption resin, and the active ingredient may be concentrated before using the synthetic adsorption resin before use. As the synthetic adsorption resin used for concentration, a non-polar or intermediate-polar resin is preferable, and specific examples thereof include Diaion HP-10, HP-20, HP-30, and HP-
Styrene divinyl such as 40, HP-50 (all products of Mitsubishi Kasei Co., Ltd.), Amberlite XAD-2, XAD-4 (all products of Rohm and Haas), Levatit OC-1031 (product of Bayer) A resin based on a benzene-based copolymer, or Amberlite XAD-7, X
AD-8 (both products manufactured by Rohm and Haas Co., Ltd.) such as those using a polyacrylate as a resin matrix.
When concentrating the active ingredient using these resins, the pear juice having a solid content of about 5 to 30% is brought into contact with these resins, and the resin separated from the juices is then subjected to methanol, ethanol, acetone or the like. The desorption treatment may be carried out with a hydrophilic organic solvent or a mixture of these and water. The SOD-like substance concentrated and present in the desorbate is stable in a weakly acidic and high-temperature region.

It is considered that the superoxide scavenger of the present invention scavenges superoxide by a reaction of O ₂ ⁻ + 2H ⁺ → H ₂ O ₂ + O _2. Whether the component eliminates superoxide has not yet been elucidated. However, it is clear that this SOD-like substance is not an enzyme or vitamin C because it is adsorbed by a synthetic adsorption resin that does not adsorb sugar or protein, and vitamin C has no superoxide scavenging action.

The superoxide scavenger of the present invention can be used in a wide range of applications, such as being used as a pharmaceutical product, and blended into cosmetics (including quasi-drugs), foods, and the like. Since it is excellent in stability and safety, it can be used with almost no limitation on the addition target and the amount added. A preferable addition amount is 0.01 to 3% as a synthetic adsorbed resin adsorbed product of the pear juice.

〔The invention's effect〕

As described above, the superoxide eliminator of the present invention can be easily produced using pears as a raw material, so that it is inexpensive, and there is no concern about safety. More wide
Shows stable superoxide scavenging action in the pH range,
Its effect is not impaired by heating, so it is used as a drug for the prevention or treatment of the above-mentioned diseases caused by excess superoxide, and added to foods, cosmetics, etc. to help promote health and beauty It can be very useful.

〔Example〕

Hereinafter, the present invention will be described with reference to examples. In each of the following examples, the superoxide erasing activity was measured by the following NBT method.

NBT method: A superoxide anion radical is generated by a xanthine-xanthine oxidase system under a certain condition. This superoxide anion radical reduces nitro blue tetrazolium (NBT) to form formazan. Formazan production is SOD
SOD-like activity can be determined by colorimetrically determining the degree of inhibition. The inhibition rate shown as a measurement result is the above-mentioned inhibition rate of formazan formation, and ID ₅₀ is a value obtained by interpolation of the amount of fruit juice added corresponding to a 50% inhibition rate.

Example 1 Japanese pear concentrated juice (extract content 50.6%, vitamin C content 6.
2%) was examined for SOD-like activity by the NBT method. Table 1 shows the results.

Table 1. Inhibition rate (%) of added amount of concentrated pear juice (μ / g) 260 91.3 85 79.1 54 46.6 32 35.6 16 24.9 60 (ID ₅₀ ) 50 Under the same conditions, the ID ₅₀ of superoxide dismutase by the NBT method was 0.035 μg. Therefore, the SOD-like activity of the concentrated pear juice is recognized as about 0.06% of that of superoxide dismutase.

Example 2 The concentrated juice of pears used in Example 1 was treated using a synthetic adsorption resin (Diaion HP-20), and the adsorbed part (hydrophobic fraction) and non-adsorbed part (hydrophilic fraction; saccharide) , Proteins, etc.). The adsorbed portion was desorbed with 80% ethanol and then subjected to gel filtration using Sephadex G-75. As a result, no protein was found in the fraction having a molecular weight of 10,000 or more. Therefore, it was confirmed that superoxide dismutase itself did not exist in the adsorption part.

When the SOD-like activity was measured for the adsorption part and the non-adsorption part, almost no activity was recognized in the non-adsorption part, and most of the activity was in the adsorption part. The activity of the adsorption section is as shown in Table 2, and the activity of the superoxide dismutase was about 0.5%.
It showed 6% activity.

Table 2 Addition amount of adsorption part (μ / g) Inhibition rate (%) 27.5 78.2 13.8 56.3 6.9 58.5 3.4 40.2 1.7 23.66 (ID ₅₀ ) 50 Example 3 The following was prepared by mixing the concentrated pear juice used in Example 1 Made acidic foods.

Vinegar 95 Pear pear concentrated juice 5 kg Salt 85 kg Sodium glutamate 1 kg Sugar 36 kg Stevioside preparation 41 kg Complex seasoning 100 g Cuensan 20 g Leave this food at 40 ° C, 75% RH for one month, then separate SOD-like active ingredients with synthetic adsorption resin When the activity was measured by the NBT method, the SOD-like activity was recovered in 95% of the blended amount and was confirmed to be stable in acidic foods.

Example 4 1 kg of concentrated pear pear juice used in Example 1 was passed through a column of Diaion HP-20 1000 ml with SV 0.5 / Hr, the column was washed with 2000 ml of water, and then 60 v / v% ethanol. Desorption was performed with 5000 ml. The obtained desorbed solution is concentrated under reduced pressure, and
The residue was dried under reduced pressure to obtain 94 g of a dried product. 50 g of the dried product was blended with the following juice drink, and sterilized by heating at 130 ° C. for 15 seconds. The SOD-like activity was measured in the same manner as in Example 1. As a result, 98% of the blended activity was recovered. No decomposition by sterilization was observed.

Juice beverage formulation Granulated sugar 9.2 kg Stevioside preparation 12 g Citric acid 150 g Malic acid 70 g 1/5 concentrated grapefruit juice 2.1 kg Grapefruit essence 100 ml Add water to make the total amount 100 Example 5 Dried product obtained in Example 4 Pear juice fraction) 5% of the following lotion was blended to prepare a lotion, and then 6% at 40 ° C and 75% RH.
After storage for months, the SOD-like activity was measured in the same manner as in Example 1. As a result, 94% of the combined activity was recovered, and almost no degradation was observed.

Lotion formulation Glycerin 3.0% Propylene glycol 4.0 Ethanol 3.0 POE (20 mol%) Oleyl alcohol 0.5 Allantoin 0.1 Methyl paraben 0.1 Citric acid 0.01 Sodium citrate 0.1 Perfume 0.1 Purified water

Continuation of the front page (51) Int.Cl. ⁶ Identification code FI A61K 35/78 ABX A61K 35/78 ABX ADA ADA ADN ADN ADP ADP AED AED (56) References Chemical Abstracts, Vol. 110 Abstract No. 132172 Chemical Abstracts, Vol. 107 Abstract No. 93526 Chemical Abstracts, Vol. 107 Abstract No. 4276 Chemical Abstracts, Vol. 106 Abstract No. 107794 Chemical Abstracts, Vol. 102 Abstract No. 44438 Chemical Abstracts, Vol. 100 Abstract No. 31820 (58) Fields investigated (Int.Cl. ⁶ , DB name) A61K 35/78 A61K 7/00 A23L 1/015

Claims (3)

(57) [Claims] 1. A superoxide scavenger comprising, as an active ingredient, a pear juice or a synthetic adsorption resin adsorption part thereof. 2. A superoxide-eliminating food or drink comprising the superoxide-eliminating agent according to claim 1. 3. A superoxide-eliminating cosmetic comprising the superoxide-eliminating agent according to claim 1.