KR20080088925A - Compositions for protecting eyesight - Google Patents

Abstract

A composition comprising the extract of Rubus coreanus Miq is provided to protect oxidative stresses, inhibit cataract caused by diabetes, treat and prevent disease or disorder of crystalline lens, and inhibit side effects by using natural products, so that the composition is useful to protect eyesight. A composition for protecting eyesight comprises the extract of Rubus coreanus Miq which is prepared by extracting Rubus coreanus Miq with a solvent selected from water, C1-C4 anhydrous or hydrous lower alcohol, a mixed solvent of water and lower alcohol, acetone, ethyl acetate, chloroform, 1,3-butylene glycol, hexane, diethylether and butylacetate; and optionally bilberry extract and vitamin A, or optionally at least one component selected from vitamin B6 hydrochloride, taurine, zinc, soy lecithine, tocopherol, Cassia tora L., marigold, Lysimachia vulgaris var. davurica extract, grape seed oil, palm oil, yellow wax, and combinations thereof.

Description

Composition for Eye Protection {Compositions for Protecting Eyesight}

The present invention relates to a composition for protecting a sample, and more particularly, to a composition for protecting eyesight comprising a bokbunja extract as an active ingredient.

As the frequency of use of electronic devices such as computers, TVs, and mobile phones increases, the population of eyeglasses is increasing day by day due to deterioration in vision of infants, adolescents, and middle-aged people, as well as deterioration in vision due to adult diseases of the elderly. Vitamins and drugs have been developed and distributed to prevent vision loss, but it is classified as a medicine and is difficult to purchase without a doctor or pharmacist's prescription.

On the other hand, there have been various studies for protecting and strengthening eyesight. For example, Korean Patent No. 539633 discloses about 420 mg to about 600 mg of vitamin C on a daily dose basis; About 400 IU to about 540 IU of vitamin E; about 17.2 mg to about 28 mg of vitamin A in beta-carotene form; about 60 mg to about 100 mg of zinc; And about 1.6 mg to about 2.4 mg of copper for retinal health enhancing compositions. Korean Patent No. 622045 discloses a method for preparing a diglyceride fat and oil composition having an eye protection effect. Specifically, A) monoglyceride, fatty acid, and DHA (DOCOSAHEXAENOIC ACID) are mixed and stirred, and the temperature is 200 to 250. Reacting for 1 to 4 hours at a temperature of 0.001 TORR to 0.5 TORR under reduced pressure; And B) molecular distillation of the stirred reaction mixture of step A) at 200 to 250 ° C. under reduced pressure of 0.001 TORR to 0.5 TORR, to disclose a method for preparing a diglyceride fat or oil composition comprising DHA. .

Korean Patent Application Publication No. 2002-0087834 is a neuroprotective and retinal ophthalmic drug capable of retarding and reversing the process of deterioration of visual function, and as an inhibitor of enzyme conversion angiotensin 1 to angiotensin 2 whose active ingredient is highly stable. Disclosed is a drug characterized by being configured.

Korean Patent Application No. 2005-0008702 discloses a composition for protecting eyesight having a bilberry extract containing a large amount of anthocyanin as a main component and a method for producing the same.

Throughout this specification, many papers and patent documents are referenced and their citations are indicated. The disclosures of cited papers and patent documents are incorporated herein by reference in their entirety, and the level of the technical field to which the present invention belongs and the contents of the present invention are more clearly explained.

The inventors have sought to develop substances that can protect or prevent vision, in particular the diseases or disorders of the lens, and seek to obtain such substances from natural products as possible. As a result, the present inventors have completed the present invention by discovering that bokbunja extract effectively defends against oxidative stress and effectively inhibits cataract induced by diabetes.

Accordingly, an object of the present invention is to provide a composition for protecting eyesight.

Other objects and advantages of the present invention will become apparent from the following detailed description, claims and drawings.

According to an aspect of the present invention, the present invention provides a composition for protecting eyesight comprising bokbunja extract as an active ingredient.

The inventors have sought to develop substances that can protect or prevent vision, in particular the diseases or disorders of the lens, and seek to obtain such substances from natural products as possible. As a result, the inventors have found that the bokbunja extract effectively protects against oxidative stress and effectively inhibits cataract induced by diabetes.

The bokbunja extract used as an active ingredient in the present invention is obtained from bokbunja (ie, bokbunja strawberry). Bokbunja strawberry is a deciduous shrub of the family Rosaceae, and the term “bokbunja” as used herein means the fruit of the bokbunja strawberry tree.

Bokbunja extract of the present invention is a conventional extraction solvent known in the art, preferably, (a) water, (b) anhydrous or hydrous lower alcohol having 1 to 4 carbon atoms (e.g. methanol, ethanol, propanol, butanol, normal -Propanol, iso-propanol and normal-butanol, etc.), (c) mixed solvent of the lower alcohol with water, (d) acetone, (e) ethyl acetate, (f) chloroform, (g) 1,3-butyl It can be obtained using ethylene glycol, (h) hexane, (i) diethyl ether, or (j) butyl acetate.

Bokbunja extract of the present invention includes not only those obtained by using the above-described solvent, but also those obtained by additionally applying a purification process thereto. For example, fractions obtained by passing the extract through an ultrafiltration membrane having a constant molecular weight cut-off value, separation by various chromatography (manufactured for separation according to size, charge, hydrophobicity or affinity), etc. The fraction obtained through the purification method is also included in the extract of the present invention.

Bokbunja extract of the present invention may be prepared in powder form by an additional process such as distillation under reduced pressure and freeze drying or spray drying.

According to a preferred embodiment of the present invention, the composition of the present invention further comprises a bilberry extract and vitamin A. More preferably, the composition of the present invention is at least one member selected from the group consisting of vitamin B6 hydrochloride, taurine, zinc, soy lecithin, tocopherol, deficiency, marigold, millet extract, grapeseed oil, palm oil, wax and combinations thereof It further comprises a component of. Most preferably, the composition of the present invention comprises all of bokbunja extract, bilberry extract, vitamin A, vitamin B6 hydrochloride, taurine, zinc, soy lecithin, tocopherol, deficiency, marigold, millet extract, grapeseed oil, palm oil, and halves .

According to a preferred embodiment of the present invention, the composition of the present invention may be provided as a pharmaceutical composition, cosmetic composition or food composition.

When the composition of the present invention is made into a pharmaceutical composition, the pharmaceutical composition of the present invention includes a pharmaceutically acceptable carrier. Pharmaceutically acceptable carriers included in the pharmaceutical compositions of the present invention are those commonly used in the preparation, such as lactose, dextrose, sucrose, sorbitol, mannitol, starch, acacia rubber, calcium phosphate, alginate, gelatin, Calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrup, methyl cellulose, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil, and the like It doesn't happen. In addition to the above components, the pharmaceutical composition of the present invention may further include a lubricant, a humectant, a sweetener, a flavoring agent, an emulsifier, a suspending agent, a preservative, and the like. Suitable pharmaceutically acceptable carriers and formulations are described in detail in Remington's Pharmaceutical Sciences (19th ed., 1995).

The pharmaceutical composition of the present invention may be administered orally or parenterally, and preferably applied by oral administration.

Suitable dosages of the pharmaceutical compositions of the present invention may vary depending on factors such as the formulation method, mode of administration, age, weight, sex, morbidity, condition of food, time of administration, route of administration, rate of excretion and response to response of the patient. Can be. The dosage of the pharmaceutical composition of the present invention is 0.001-100 mg / kg on an adult basis.

The pharmaceutical compositions of the present invention may be prepared in unit dose form by formulating with a pharmaceutically acceptable carrier and / or excipient according to methods which can be easily carried out by those skilled in the art. Or may be prepared by incorporation into a multi-dose container. The formulation may be in the form of solutions, suspensions, syrups or emulsions in oils or aqueous media, or in the form of extracts, powders, powders, granules, tablets or capsules, and may further comprise dispersants or stabilizers.

When the composition of the present invention is made into a food composition, it includes ingredients which are commonly added in the preparation of food, and include, for example, proteins, carbohydrates, fats, nutrients, seasonings and flavoring agents. Examples of the above carbohydrates include monosaccharides such as glucose, fructose and the like; Disaccharides such as maltose, sucrose, oligosaccharides and the like; And sugars such as conventional sugars such as polysaccharides such as dextrin, cyclodextrin and the like and xylitol, sorbitol, erythritol. As the flavoring agent, natural flavoring agents (tauumatin, stevia extract (for example rebaudioside A, glycyrrhizin, etc.) and synthetic flavoring agents (saccharin, aspartame, etc.) can be used.

 For example, when the food composition of the present invention is prepared with a drink, in addition to the above-mentioned active ingredient, citric acid, liquid fructose, sugar, glucose, acetic acid, malic acid, fruit juice, tofu extract, jujube extract, licorice extract, and the like may be further included. have.

According to a preferred embodiment of the present invention, the composition of the present invention has the effect of preventing or treating cataracts. The cataract is preferably diabetic cataract. Therefore, the present invention can be expressed as a "cataract prevention or treatment composition" in addition to "eye protection composition".

The composition of the present invention effectively defends against oxidative stress and exerts very good efficacy in protecting eyesight. In particular, it exhibits very good efficacy in the treatment or prevention of cataracts (eg, diabetic cataracts), and is safe for the human body because it uses natural-derived materials as active ingredients.

Hereinafter, the present invention will be described in more detail with reference to Examples. These examples are only for illustrating the present invention in more detail, it will be apparent to those skilled in the art that the scope of the present invention is not limited by these examples in accordance with the gist of the present invention. .

Example

Example  One: Bilberry  And Preparation of Bokbunja Extract

The purchased bilberry was stored by rapid freezing at -10 ° C, and then frozen bilberry was crushed while thawing in hot water at 30 ° C. Subsequently, 400 ppm of pectinase was added to the ground solution and treated for 90 minutes, and 50% (v / v) of ethanol was extracted for 120 minutes. The extract was filtered and spray dried bilberry extract to obtain bilberry extract powder.

In addition, the bokbunja extract was prepared as follows: The purchased bokbunja strawberry was stored by rapid freezing at -10 ℃, and the frozen bokbunja was crushed while thawing in 30 ℃ hot water. Subsequently, 400 ppm of pectinase was added to the ground solution and treated for 90 minutes, and 50% (v / v) of ethanol was extracted for 120 minutes. The extract was filtered to spray dry the bokbunja extract to obtain a bokbunja extract powder.

Example  2: Preparation of Composition I

Bilberry extract 17% (w / v) obtained in Example 1, 17% (w / v) bokbunja extract, 0.01% (w / v) of vitamin A and a residual amount of water was prepared for the composition for protecting eyes .

Example  3: Preparation of Composition II

17% (w / v) bilberry extract obtained in Example 1, 17% (w / v) of bokbunja extract, 0.01% (w / w) of vitamin A, 5% (w / w) of deficiency, 1% (w) of marigold / w), millet 9% (w / w), halves 1.5% (w / w), tocopherol 5% (w / w), grapeseed oil 56.29% (w / v), taurine 0.2% (w / w), Vitamin B6 hydrochloride 0.2% (w / w), zinc oxide 0.3% (w / w), soy lecithin 3% (w / w), refined palm oil 1.5% (w / w), lead 1.5% (w / w) ) And the remaining amount of water was added to the mixer, mixed, and filled into soft capsules to prepare health functional foods for vision protection.

Example  4: In Vivo  Experiment

The effects of diabetic cataract production were investigated in order to examine the effects of eye protection on the composition comprising the extract of Bokbunja of the present invention as an active ingredient. Cataract is a disease in which the lens becomes cloudy and loses transparency, leading not only to vision loss, but also to being the most common cause of blindness. Various gastric factors causing cataracts such as oxidative stress, UV exposure, and aging are known, and diabetes is also an important risk factor. Other factors include mechanical changes, biochemical changes, and biological changes. It is thought that NO, a free radical, very unstable and highly reactive chemical, is involved in the cataract production process. As peroxynitrate is formed by reacting with superoxide generated when NO is produced, lipid peroxidation of lens protein occurs. It seems to have played an important role in cataract formation.

The incidence of cataracts has been reported to increase in proportion to the duration and extent of diabetes. In this study, the development and progression of cataracts in diabetic cataract-induced rats treated with bokbunja extract composition were examined in the following manner.

1. Diabetic Cataract Induction and Experimental Diet

Six-week-old Sprague-Daweley species rats were fed to a solid diet and water, kept at a temperature of 20-25 ° C and a humidity of 55 ± 1%, and reared for two weeks and adapted to the environment. Streptozotocin (STZ) is a chemical that induces diabetes by inducing insulin deficiency by selectively destroying beta cells in the pancreas.

The animals were fasted for 16 hours prior to administration of STZ, and then dissolved in 50 mM citrate buffer (pH 4.5) to 60 mg / kg of STZ (Sigma, chemical CO. USA) once in the abdominal cavity within 10 minutes. Diabetes was induced by injection. Three days after STZ injection, diabetes was induced, and venous blood was collected from the tail to confirm that the fasting blood glucose was 250 ± 10 mg / dl or more.

The experimental diet was administered orally, and in rats induced diabetes, group A (no treatment), group B (groups inducing diabetes with STZ) and group C (induction of diabetes with STZ). Group administered the Bokbunja extract), group D (group administered the composition of Example 2 after inducing diabetes with STZ) and group E (group administered with the composition of Example 3 after inducing diabetes with STZ) Each group consisted of 20 rats. The oral dose was 5 mg / kg.

2. Specimens collected and biochemical analysis of the experimental animals

Two, four and twelve weeks after administration of the composition of the present invention, five experimental animals included in each group were sacrificed to extract eyeballs and the lens was separated, followed by biochemical analysis. GSH content was measured using a GSH assay kit (Cayman chemical. Catalog No. 703002), and MDA content was measured using a lipid hydroperoxide assay kit (Cayman chemical. Catalog No. 705002). Quantification of total protein was carried out according to the Bradford method, at which time BSA (Bovine Serum Albumin) was used as a standard.

3. photodocumentation for observing lens clarity and changes

To investigate cataract incidence and progression in each control and experimental group, slit lamp microscope (Takagi, SM-50F) was observed at 3, 1, 2, 4, 8, and 12 weeks, respectively. Photographs were taken at magnification. The degree of cataract observed at this time was classified using the scoring system of Table 1.

Lens opacity Rating Lens opacity 0 No lens opacity One Faint visible Y suture 2 Obvious Visible Y Sutures 3 Obvious visible Y suture with surrounding front capsule opacity 4 Serious Front Capsule Opacity Invisible Y Suture

4. Cataract Development and Changes

Cataract progressed to grade 3 or more in 20 patients (100%) in group B, 8 eyes (40%) in group C, 5 eyes (25%) in group D, and 3 eyes in group E. (15%), even when the bokbunja extract was administered alone, the occurrence of cataract was statistically significantly suppressed, and the occurrence of cataract was also statistically significantly suppressed in group D and E to which other visually active ingredients were added. In the group induced diabetes with STZ (group B), the opacity of the opaque lens with an average opacity rating of 1.6 or more occurred from day 3, and the opacity rating increased to an average of 2.8 or more after 1 week. It became. On the other hand, in the group administered the bokbunja extract (Group C) increased to grade 2 or more only after 7 weeks on average. In groups D and E, opacity increased to grade 2 or higher only after an average of 9 and 11 weeks, respectively. In the control group that did not induce diabetes (Group A), no lens opacity was observed during the experiment.

5. Biochemical Analysis

   (1) Determination of Glutathione Content (GSH Content, μM)

 GSH is a non-enzymatic antioxidant defense system in the body is known to play an important role in inhibiting cell damage caused by oxidative stress. It is also known that excessive oxidative stress leads to a decrease in GSH content and oxidation of GSH, thereby impairing the defense mechanism against oxidative damage caused by GSH. It is reported that diabetes also induces oxidative damage and impairs the protective mechanism of oxidative damage caused by GSH in tissues. The GSH content measurement results after 12 weeks in this experiment are shown in Table 2 below.

division Group A B group Group C D group E group GSH content (μM) 252.7 158.2 196.9 231.2 242.5

As can be seen in Table 2, it was observed that the GSH content significantly decreased in the lens treated with STZ, compared with the group without any treatment. However, the GSH content of the bokbunja extract after treatment with STZ showed a significantly increased GSH content of 196.9 μM after 12 weeks, and the GSH content increased as the administration period increased. In addition, the GSH content was also significantly increased in Groups D and E which added other visually active ingredients.

Taken together with the results of the lens opacity, bokbunja extract is believed to prevent the increase of opacity of the lens by protecting the lens from oxidative stress by increasing the activity of antioxidant system such as GSH damaged by diabetes.

    (2) MDA (Malondialdehyde) measurement (hydroperoxide content, μM)

Oxidative cell damage induces modification of macromolecules such as proteins, nucleic acids, lipids, and the like, and exerts their effects. In particular, the oxidation of lipids in oxidative damage leads to a deformation of the cell membrane, which in turn causes an amplification process that produces ROS. Therefore, lipid peroxidation of cell membrane is measured as an important indicator of oxidative cell damage. Since the MDA is the same as the lipid peroxidation, MDA is used as an indicator of oxidative damage in the body. The MDA content measurement results after 12 weeks in this experiment are shown in Table 3 below.

division Group A B group Group C D group E group MDA content (μM) 82.1 154.2 110.8 106.2 90.3

As can be seen from Table 3, compared to the diabetic group B group, the group showed a relatively close to normal MDA value in the C group administered the bokbunja extract. In addition, the MDA content was significantly reduced in Groups D and E, which added other visually active ingredients. The results of this experiment indicate that bokbunja extract protects the lens by effectively inhibiting lipid peroxidation caused by oxidative citrus.

As described in detail above, the composition of the present invention effectively defends against oxidative stress, and exhibits very good efficacy in protecting eyesight. In particular, it exhibits very good efficacy in the treatment or prevention of cataracts (eg, diabetic cataracts), and is safe for the human body because it uses natural-derived materials as active ingredients.

As described above in detail certain parts of the present invention, it is apparent to those skilled in the art that these specific descriptions are merely preferred embodiments, and the scope of the present invention is not limited thereto. Thus, the substantial scope of the present invention will be defined by the appended claims and equivalents thereof.

Claims (5)

Eyesight protection composition comprising the bokbunja extract as an active ingredient. The composition of claim 1, wherein the composition further comprises bilberry extract and vitamin A. 3. The composition of claim 1, wherein the composition is at least one component selected from the group consisting of vitamin B6 hydrochloride, taurine, zinc, soy lecithin, tocopherol, deficiency, marigold, millet extract, grapeseed oil, palm oil, wax and combinations thereof Composition comprising a further. The composition of claim 1, wherein the composition has a prophylactic or therapeutic effect of cataracts. The composition of claim 4 wherein the cataract is diabetic cataract.