KR102121048B1 - Antioxidant and anti-inflammatory composition comprising mixed extracts of ecklonia cava extract and scoria - Google Patents

Abstract

The present invention relates to an antioxidant and anti-inflammatory composition comprising a composite extract of persimmon and volcanic pine as an active ingredient and a method for manufacturing the same. The complex extract of persimmon and volcanic pine according to the present invention is not only toxic, but also weakens inducible nitric oxide synthase (iNOS) and NO production and prevents or treats inflammation by inhibiting microglia cell activity in microglia. , Inflammatory neurological disease prevention or treatment, inflammatory neurodegenerative disease prevention or treatment, or inflammatory skin disease relief pharmaceuticals and detergents, may be usefully used as cosmetics.

Description

Antioxidant and anti-inflammatory composition comprising mixed extracts of ecklonia cava extract and scoria}

The present invention relates to an antioxidant and anti-inflammatory composition comprising a composite extract of persimmon and volcanic pine as an active ingredient and a method for manufacturing the same.

Skin is a body part that is directly exposed to the external environment. When exposed to excessive ultraviolet rays or pollutants, skin irritation and inflammatory reactions such as erythema, edema, and itching are caused. It is known that such skin troubles are not only an aesthetic problem, but also substances that are generated in the inflammatory reaction process, incidentally cause pigmentation, and promote the collapse of skin elastic fibers to increase skin wrinkles. It is also known to be associated with free radicals for skin damage.

Free radicals cause various problems such as wrinkle formation, skin cancer, cell death, rheumatoid arthritis, atopic dermatitis, and acne, because free radicals destroy cells, cut the connective tissue of the dermis of the skin, or cause cross-linking.

The causes of free radicals are known to be the expression of leukocytes, the electron transport system during the production of ATP in mitochondria, the action of myeloperoxide (MPO), ultraviolet rays, tobacco, normal metabolic processes, stress, pollutants, and bacteria. .

Increased free radicals destroy collagen (Collagen), elastin and hyaluronic acid, which are the connective tissues of the dermis, causing subsidence (wrinkle) of the skin. Destructive phenomena occur, which causes diseases of dermatitis, acne, and skin cancer.

Inflammation is a physiological response that protects the body from harmful invasion, foreign organisms such as bacteria and mechanical damage. This inflammatory phenomenon leads to a large increase in several types of polynuclear leukocytes (PMNs) and immune substances, and these cells are able to treat and defend by secreting various types of proteolytic enzymes and cytokines, which are inflammatory cell products. Enable. Enzymes such as elastase, hyalurinidase, and lipoxygenase are well known proteins and lipid-degrading enzymes produced during inflammation.

Over-inflammation damages cells and connective tissue by proteolytic enzymes, and damage to connective tissue reduces elasticity of the skin, causing wrinkles, and adversely affecting cell regeneration and proliferation. It causes aging and local erythema and swelling of the skin. If the connective tissue is severely damaged and the inflammatory response persists, restoring normal tissue structure and function becomes much more difficult.

In order to reduce skin irritation and inflammation caused by various stress sources and reduce side effects caused by the use of cosmetics, it is urgently required to develop substances that have anti-inflammatory, antioxidant, and skin irritation-reducing effects. There is a need for a method that can effectively extract useful components of.

Eckloina cava is an edible seaweed and is a plant of the brown seaweed Laminariales and Alariaceae. It is mainly found in the south coast of Korea, the coast of Jeju, and Japan. It is mainly used for food such as abalone and conch, and is used as the main raw material for making alginic acid or potassium iodine.

Persimmon extract is also referred to as sinol, which is a compound of SEA + Polyphenol, a type of polyphenol that is a bioactive component extracted from persimmon found in the deep sea of Jeju Island.

Seanole was born through research for about 20 years using the sensation of senol, a component of Cinol, which protects from UV rays and activates cells so that life in the sea can inhabit.

The main difference between polyphenols extracted from terrestrial plants and polyphenols extracted from sea plant persimmons is that polyphenols extracted from sea plant persimmons are more potent in antioxidants and absorbed into the body because they are insoluble in water, unlike the water-soluble properties of terrestrial polyphenols. After being melted, it is not dissolved and decomposed and remains in the body for at least 12 hours, so it can pass the barriers of the brain and blood vessels better, so it can effectively deliver antioxidant components to the brain and nerve cells.

In addition to polysaccharides such as alginic acid and fucoidan, physiologically active substances present in persimmon are phlorotannin, and their physiological activities are HIV-1 reverse transcriptase inhibitory activity, xanthin oxidase inhibitory activity, tyrosinase activity inhibitory effect, elastase activity inhibitory effect, and thrombogenic inhibitory activity , Antioxidant activity, cardiovascular protective effect, antiviral activity, etc. have been reported.

Volcanic cluster (scientific name: Scoria) is a volcanic clast formed by burning high-temperature clay by volcanic activity and is known as a kind of natural ceramic. When the volcano erupts, the first erupted lava solidifies and is produced. At this time, the lava mixed with the gas is first ejected, and in this process, a volcanic cluster of porous structures including numerous fine holes is born.

It is found in Jeju Island in Korea, and is called Songi or Songi Seok in the dialect of Jeju Island. The physical properties of volcanic clusters are porous, with a pH of about 7.2 to 7.8, and are porous, and generally have red, yellow, brown, black, and gray colors depending on the minerals they contain.

Therefore, in order to improve the skin trouble caused by these free radicals and inflammation, it has excellent antioxidant and anti-inflammatory effects, develops natural extracts without side effects, develops functional materials containing the extracts, develops industrial materials, and extracts cosmetic methods. This is required.

The present inventors have solved the problems of the prior art as described above, and during earnest research to develop a material having excellent anti-oxidant properties and anti-inflammatory properties, as described below, the complex extract of persimmon and volcanic pine has no toxicity but has anti-oxidant properties and anti-inflammatory properties. It has been found that it is possible to satisfy the above requirements due to its excellent properties, and the present invention has been completed.

Accordingly, an object of the present invention is to provide a composition that improves the problems of the prior art as described above and eliminates free radicals, thereby exhibiting antioxidant and anti-inflammatory efficacy. Antioxidant and anti-inflammatory composition according to the present invention contains a composite extract of persimmon and volcanic pine as an active ingredient, after mixing the persimmon and volcanic pine in a weight ratio of 9:1, room temperature using an alcohol extraction solvent of 5 to 20 multiples It is characterized in that it is alcohol extract of persimmon and volcanic pine extract extracted for 72 hours.

The object of the present invention as described above can be achieved by a pharmaceutical composition or detergent or cosmetic composition for the prevention or treatment of antioxidant, inflammation, characterized in that it comprises a composite extract of persimmon and volcanic pine as an active ingredient.

The complex extract of persimmon and volcanic pine according to the present invention is not only toxic, but also weakens inducible nitric oxide synthase (iNOS) and NO production and prevents or treats inflammation by inhibiting microglia cell activity in microglia. , Inflammatory neurological disease prevention or treatment, inflammatory neurodegenerative disease prevention or treatment, or inflammatory skin disease relief pharmaceuticals and detergents, may be usefully used as cosmetics.

1 is a graph showing the DPPH radical inhibitory ability of persimmon and volcanic cluster extract.
Figure 2 is a graph showing the cell viability (BV-2 cells) of persimmon and volcanic cluster extract.
Figure 3 is a graph showing the inhibition of NO production of persimmon and volcanic cluster extract.

The present invention, in one aspect, provides an antioxidant and anti-inflammatory composition, characterized in that it comprises a composite extract of persimmon and volcanic pine as an active ingredient.

The present invention, in a further aspect, provides a pharmaceutical composition for the prevention or treatment of inflammatory diseases, characterized in that it comprises a composite extract of persimmon and volcanic pine as an active ingredient.

The present invention, in another aspect, provides a functional cosmetic composition for alleviating and improving inflammation characterized in that the complex extract of persimmon and volcanic pine as an active ingredient.

The composition according to the present invention can be used as an active ingredient that is extracted for 72 hours at room temperature using an extraction solvent of 5 to 20 times after mixing the persimmon and volcanic clusters in a suitable ratio, preferably 9:1 by weight. .

Here, at least one selected from water, lower alcohol having 1 to 4 carbon atoms, polyhydric alcohol, or a mixture thereof can be used as the extraction solvent. As a lower alcohol having 1 to 4 carbons, methanol, ethanol, or the like can be used, and as the polyhydric alcohol, butylene glycol, propylene glycol, pentylene glycol, and the like can be used. And as the mixture, a mixture of water and lower alcohol, a mixture of water and polyhydric alcohol, a mixture of lower alcohol and polyhydric alcohol, or a mixture of water and lower alcohol and polyhydric alcohol may be used.

The composite extract of persimmon and volcanic matsutake according to the present invention is not only toxic as confirmed from the results of Examples and Test Examples described below, but also weakens inducible nitrogen oxide synthase (iNOS) and NO production, and microglia By inhibiting microglia activity in the prevention or treatment of inflammation, inflammatory neurological disease prevention or treatment, inflammatory neurodegenerative disease prevention or treatment, or can be usefully used as pharmaceuticals and cosmetics for inflammatory skin disease alleviation.

Accordingly, the composite extract of persimmon and volcanic pine according to the present invention can be usefully used as an anti-inflammatory and anti-inflammatory agent, and those skilled in the art can easily grasp individuals suspected of suffering from such diseases, conditions and abnormalities.

The pharmaceutical composition of the present invention can be formulated in combination with a known pharmaceutical carrier. In general, the active ingredient is combined with a pharmaceutically acceptable liquid or solid carrier, and if necessary, a solvent, dispersant, emulsifier, buffer, stabilizer, excipient, binder, disintegrant, lubricant, etc. are added and purified. , Granules, powders, solids such as powders, capsules and the like, and can be used as liquids such as ordinary liquids, suspensions and emulsions. Moreover, it can also be set as a dried product that can be made into a liquid by adding a suitable carrier before use.

The pharmaceutical composition of the present invention can be administered by any of parenteral agents such as oral preparations, injections, and drops.

The pharmaceutical carrier can be selected according to the above dosage form and dosage form. For oral preparations, for example, starch, lactose, white sugar, mannitol, carboxymethylcellulose, corn starch, inorganic salts, etc. are used. In addition, in the preparation of an oral preparation, a binder, a disintegrant, a surfactant, a luster, a fluidity accelerator, a mating agent, a colorant, and a fragrance may be further added.

On the other hand, in the case of a parenteral agent, distilled water for injection as a diluent, physiological saline, aqueous glucose solution, vegetable oil for injection, sesame oil, peanut oil, soybean oil, corn, etc. It is prepared by dissolving or suspending oil, propylene glycol, polyethylene glycol, and the like, and adding a sterilizing agent, a stabilizer, an isotonic agent, and a painless agent as necessary.

The pharmaceutical composition of the present invention is administered by a suitable route of administration according to the form of the formulation. The administration method is not particularly limited, and can be administered by content, external use, and injection. The injection can be administered, for example, intravenously, intramuscularly, subcutaneously, intradermally, and the like.

The dosage of the pharmaceutical composition of the present invention is appropriately set according to the formulation form, method of administration, purpose of use, and age, weight, and symptoms of the patient applied to the pharmaceutical composition. The amount is, for example, 10 μg to 10 mg/kg per adult per day. However, one of ordinary skill in the art will appreciate the pharmacokinetic properties of a particular reagent and its mode and route of administration; The recipient's age, health and weight; It will be understood that the dosage varies depending on known factors such as the nature and extent of symptoms, the type of concurrent treatment, the frequency of treatment and the desired effect.

The composition of the present invention is not particularly limited in the content of the main component, but can be used, for example, 0.1 to 99.9% based on the weight of the composition.

In addition, the complex extracts of persimmon and volcanic matsutake according to the present invention can be used as a main component of detergents or cosmetics that require this function.

(Example)

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

Example 1: Emotion And Volcanic cluster Extraction of complex

100 g of samples mixed with persimmon and volcanic cluster according to the respective ratios shown in Table 1 were extracted with 1 L of ethanol at room temperature for 72 hours.

Sample number Emotional content Volcanic cluster content One 10 0 2 9 One 3 8 2 4 7 3 5 6 4 6 5 5 7 4 6 8 3 7 9 2 8 10 One 9 11 0 10

Example 2: Emotion And Volcanic cluster Complex extract DPPH Radical scavenging activity

The free radical scavenging activity of the persimmon and volcanic cluster extract according to Example 1 was measured for reducing power against stable radical DPPH (Sigma Co.).

160 μL of the diluted solution diluted with 99% methanol and 40 μL of 0.15 mM DPPH solution dissolved in methanol were added and left at room temperature for 30 minutes, and absorbance was measured at 517 nm. The DPPH radical scavenging activity was calculated according to the following equation. At this time, the treatment concentration of the extract and Vit.C is 100 μg/mL.

DPPH radical scavenging activity (%) = (100-(S/Cㅧ100))

S: Absorbance after sample group reaction-Absorbance before sample group reaction

C: Absorbance after control reaction-Absorbance before control reaction

The results are shown in FIG. 1. Figure 1 is a graph showing the DPPH radical inhibitory ability of the persimmon and volcanic cluster extract. As a result of measuring DPPH radical scavenging activity, when the ratio of eclectic and volcanic clusters was extracted at a ratio of 9:1, it showed the best radical inhibitory activity of about 88.24% (FIG. 1).

Example 3: Cell viability of persimmon and volcanic cluster extract

To confirm the effect of LPS and persimmon extract on cell survival in LPS-stimulated BV-2 cells, cell biability was changed to 3-[4,5-Dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide (MTT ) It was measured by analytical method.

Cells (1 x 10 ⁵ cell/ml) Cells were dispensed into a 96-well plate at 180 μL and cultured in a CO ₂ incubator for 12 hours or more, and then treated according to each condition to incubate for 24 hours. After culturing, the culture solution was removed, and 200 μL of a medium containing 0.5 mg/ml MTT was added, followed by incubation for 4 hours to reduce MTT. Thereafter, the culture medium was removed and 100 μL of dimethylsulfoxide (DMSO) was added to dissolve the produced formazone crystals, and absorbance was measured at 540 nm using an ELISA reader. Cell viability was expressed as a percentage (%) compared to the control.

The results are shown in FIG. 2. Figure 2 is a graph showing the cell viability (BV-2 cells) of the persimmon and volcanic cluster extract. As a result of measuring the cell viability, LPS and extracts according to the ratios of ecological and volcanic clusters alone or together showed a survival rate of 90% or more in the 1,2,3,4,5 treatment group, but 6,7,8,9, The 10,11 treatment group had a survival rate of 90% or less (see FIG. 2 ). This is thought to show toxicity as the volcanic cluster content increases.

Example 4: Inhibition of NO production and inhibition of oxidative and volcanic cluster complex extracts in glial cells activated with LPS

In order to analyze the anti-inflammatory efficacy of the Ecklonia cava and volcanic pine mushroom extract, this study confirmed that the concentration of NO produced by glial cells stimulated by each concentration of LPS, an inflammation-inducing factor, was dependent on efficacy.

For NO measurement, after seeding 5 x 10 ⁵ cells/ in a 24 well plate, add LPS and extract at different concentrations, react in a 24 h incubator, and each 50 μL Griess reagent (1% sulfanilamide) After reacting with /0.1% N-(1-naphthyl)-ethylenediamine dihydrochloride/2.5% H3PO4), the value is measured using a Sunrise basic 96-well microplate spectrophotometer (TECAN AUSTRIA) with a wavelength of 540 nm.

The results are shown in FIG. 3. Figure 3 is a graph showing the inhibition of NO production of persimmon and volcanic cluster extract.

The NO induced by LPS (1 μg/mL) in glial cells was about 33.1 μM, which was increased by about 10 times or more compared to 2.3 μM used as a control group. One result showed the best effect in group 2 except for groups 6 to 11, which showed cytotoxicity (FIG. 3). Therefore, it was confirmed that the composite ratio of persimmon and volcanic cluster 9:1 showed the best antioxidant and anti-inflammatory effects.

Example 5: Preparation of pharmaceutical preparations (tablets)

Combined extract of persimmon and volcanic pine (9:1 weight ratio) 10mg

Lactose 60mg

Starch 17mg

Magnesium stearate 3mg

Crystalline cellulose 10mg

Tablets may be prepared by conventional methods, and one preferred embodiment is in the form of tablets or soft capsules with a conventional enteric coating (eg, hydroxypropylmethyl cellulose phthalate), sugar coating or film coating.

The present invention described above is not limited by the above-described embodiments and the accompanying drawings, and in the technical field to which the present invention pertains, that substitution, modification, and conversion are possible within the scope of the technical spirit of the present invention. It will be clear to those who have knowledge.

Claims (5)

Contains the composite extract of persimmon and volcanic pine as an active ingredient,
Antioxidant and anti-inflammatory composition, characterized in that it is an alcohol extract of persimmon and volcanic pine, extracted for 72 hours at room temperature using 5 to 20 times the alcohol extraction solvent after mixing the persimmon and volcanic pine in a weight ratio of 9:1. delete The antioxidant and anti-inflammatory composition according to claim 1, wherein the composition attenuates inducible nitrogen oxide synthase (iNOS) and NO production. delete delete

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