JPH02243632A - Peroxide lipid formation inhibitor comprising vegetable oil extract - Google Patents

Abstract

PURPOSE:To obtain the title inhibitor having excellent stability and maintaining effects in a solution for a long period of time, containing an extract prepared by extracting specified plants with a specific mixed solvent. CONSTITUTION:(A) Green tea or tea, (B) herbaceous peony, (C) mugwort, (D) clove, (E) Geranium thunbergii Sieb., (F) Vncania gambir Roxburgh, (G) Cork tree bark and (H) leaves of peach tree as starting raw materials are extracted in such a way that the components A and B are extracted with a mixed solvent of water, ethanol and 1,3-butylene glycol in the ratio of 5:3:2, the component C to the component G are extracted with a mixed solvent of water and ethanol in the ratio of (7:3)-(4:6) and the component H is extracted with a mixed solvent of water and 1,3-butylene glycol in the ratio of (6:4)-(3:7) and the prepared plant extract is contained as an active ingredient of peroxide lipid formation inhibitor comprising the plant extract.

Description

[Detailed Description of the Invention] (a) Purpose of the Invention The present invention aims to find ingredients based on plants (Japanese and Chinese plants) that have the effect of suppressing the production of lipid peroxides.
The purpose of this study is to apply components with particularly excellent inhibitory effects as lipid peroxide inhibitors.

As a result, in the present invention, A: tea leaves (green tea, black tea), B: peony, C: mugwort, D: clove, E:
Gennoshoko, F: 7 Senyaku, G: Oubaku, H:
The raw material is peach leaves.

The extraction solution was identified and obtained. The extracts of each of A to G are used as a novel lipid peroxide inhibitor.

In addition, the ultra-thickness of each of the above-mentioned plants is B: Peony;
D: cloves, F: aspen yakuza, G: the parts used are those that are extremely thick as stipulated by the Japanese Pharmacopoeia, A: tea leaves processed for daily drinking, C: mugwort and E: Gennoshoko has two leaves and stem, H
: Peach leaves may contain twigs.

"Industrial Application Field" The extracts obtained by elution (extraction) in the specified mixed solvents based on the specified plants A to H shown above are capable of producing lipid peroxides. Because it significantly suppresses
For example, it is used for skin and hair in the form of lotions, creams, emulsions, and other formulations. It can be used by blending it into cosmetics.

Furthermore, it can be added to beverages or processed foods.

Furthermore, when the extract according to the present invention is added to a formulation, it prevents the oxidation of the lipid components contained in the formulation and contributes to stabilization. If taken (drinked), it can be expected to improve various symptoms caused by an abnormal increase in lipid peroxide in the body.

"Conventional technology" It has been known for a long time that extracts obtained from plants can be applied to fields such as cosmetics, processed foods, and pharmaceuticals. The search for ingredients that can suppress the production of lipid peroxides and their uses have only recently been attracting attention. One of the reasons for this is that since the discovery of superoxide dismutase (50D) in living organisms, the metabolic mechanism of living organisms through oxidation and reduction has become clearer.

For example, when lipids in the living body are in an abnormally advanced state with excessive oxidized lipids, it is thought to be one of the triggers of liver dysfunction, dementia, arteriosclerosis, etc.

In addition, when it comes to skin and hair, if the lipid peroxide in the skin tissue and the increase in sebum secretion continue for a long period of time, it will interfere with normal skin and hair growth, causing dandruff, itching, rough skin, hair loss, and hair loss. It promotes the so-called aging phenomenon, and is also caused by the deposition of one pigment, melanin, in the skin. The factors that promote the development of age spots are being estimated from a cytological and clinical perspective.

Furthermore, active efforts are already being made to apply plant-derived ingredients (extracts) and SOD that have the effect of inhibiting lipid peroxide production to cosmetics and other fields. If you investigate, you will find the following table "Table 1"
There is a published patent publication as shown in ().

In Table 1, numbers 1 and 2 indicate the location of publications regarding the application of SOD.

SOD exists in the living bodies of various animals, plants, and microorganisms, including humans, and in living bodies, it acts as a scavenger to capture and remove excessively produced active oxygen, Q, and l-1. It has attracted attention as a special enzyme,
SOD has been applied to cosmetics, etc., to suppress lipids in prescriptions and lipid peroxides in sebum secreted on the skin epidermis, to prevent degeneration and deterioration of the keratin protein structure of skin and hair, to prevent spots, wrinkles, and hair loss. It is expected to be effective in preventing aging phenomena such as 1), and in particular to suppress inflammation (red BI) caused by sunburn on the skin and hair caused by ultraviolet 1] (sunlight) when going out.1) It is expected to be effective in preventing pigmentation. .

On the other hand, No. 003 in Table 1 was described in that publication.

Among plant-derived extracts, we selected those that suppress the production of lipid peroxides, and among the relevant plant names, we particularly selected the underlined ones: rosemary, salvia, allspice, and paprika. , sesame, and thyme are preferred.

Furthermore, it has been disclosed that various organic solvents are used as extraction solvents, but specifically, acetone is used as an extraction solvent when rosemary, salvia, and allspice are used as starting materials. Furthermore, the extract obtained using acetone is disclosed in a mixture of a specific surfactant and ethanol, or by adding a carboxymethyl polymer to the surfactant. Examples of formulations such as gels and ointments are shown.

"Table 1" Location of Publications "Problems to be Solved by the Invention" The present inventors have focused on the effective use of natural products, and have discovered that they have the ability to inhibit the production of lipid peroxides from various plant tissues. I've been searching for ingredients.

In other words, it is no exaggeration to say that in the activities of all living things, including not only plants but also animals and microorganisms, there are always substances that suppress the production of lipid peroxide, although there may be differences in their strength.

Therefore, the problems to be solved by the present invention can be summarized as follows.

1: First, based on a test to measure the action of lipid peroxide, a wide variety of plant tissues (starting materials) are searched (screened) for the strength or weakness of the action.

2: Next is its yield (yield).

3: At the same time, if the stability is poor, it is not preferable in terms of formulation.

4: Furthermore, for example, among the raw materials commonly used in systems such as lotions and drinking water, at least (a)
It is desired that it be soluble in either water, (b) ethanol, or (c) polyol solvents (glycerin, propylene glycol, 1,3-butylene glycol, etc.).

If an extract that can satisfy the above four conditions is discovered, it means that the object of the present invention has been achieved.

However, it is no exaggeration to say that when dealing with a large number of plants, it is extremely rare to be satisfied with all of the above four conditions.

For example, at the basic testing stage of screening, differences in the selection of solvents used for extraction with respect to the starting materials are important in determining the effectiveness of the resulting extract, i.e., the desired There is a big difference in the strength of the inhibitory effect of oxidized lipids.

Therefore, in developing the present invention, the present inventors first narrowed down their focus to the three solvents (a) to (b) mentioned above, and based on various plants, the leaves and stems of plants were used. , and began searching mainly for parts such as roots.

As a result, as mentioned at the beginning of 9, the herbal medicines shown by A to H,
Alternatively, the present invention was successfully accomplished using extracts obtained from folk medicines.

(mouth) Structure of the invention The present invention consists of A: li tea or black tea, B: peony, C
: Mugwort, D = Clove, E: Gennoshoko, F: Asperianium, G: Peach leaf, H: Peach leaves are used as the starting material, and the extraction solvent for each of A to H is extracted using the mixed solvent shown below. Among the (eluted) extracts,
It is characterized by containing one or more of them.

Specified as a lipid peroxide production inhibitor.

The extraction solvent varies depending on the starting material plant, and the extraction solvent for A-B is a mixed solution of water, ethanol, and 1,3-butylene glycol in a ratio of 5:3:2 to 3:3:4. .

The extraction solvent for C^G is such that the ratio of water and ethanol is
Use a mixture of 7:3 to 4:6.

As the extraction solvent for H, a mixed solution of water and 1,3-butylene glycol in a ratio of 6:4 to 3:7 is used.

"Means for Solving the Problems" In order to more specifically illustrate the present invention specified above, the following is an example of extraction and an experimental method (screening).
The results (data) will be disclosed and described in more detail as follows.

"Extraction method 1" (Production examples of plant super thick: A to H) When the starting materials are A: green tea or black tea, B: peonies, water and ethanol are used as extraction solvents for 1 part by weight of each. and l,3-butylene glycol in a ratio of 5:3:2 to 3:3:4.
The extracted solution obtained by immersion and squeezing with ~15 parts (preferably 10 parts for extraction operation) is used as a crude liquid, and the solution after filtration is used as it is or as appropriate. Alternatively, it can be made into a dry powder to act as an inhibitor against lipid peroxide formation.

"Extraction method 2" (Manufacturing example of Ueso super thick: C-G) When the starting materials are C: mugwort, D: clove, E: gennoshoko, F: asenyaku, G: sycamore,
For each part by weight, 5 to 15 parts (extraction soil, preferably 10 parts) of a mixed solvent of water and ethanol in a ratio of 7:3 to 4:6 are used as the extraction solvent. After soaking, the extracted solution obtained by squeezing is used as a crude liquid,
The solution after filtration is used as an inhibitor against lipid peroxide production, either as it is, in the form of an appropriately concentrated solution, or in the form of a dry powder.

At this time, an appropriate amount of a polyol solvent such as 1,3-butylene glycol, propylene glycol, or glycerin may be added to the filtered solution or the appropriately concentrated solution depending on the field of use. It may also be used as a product.

Also, during the steps in the above (extraction methods 1 to 2),
When converting the A-G-derived extract solutions obtained in each case into dry powder, use methods such as reduced pressure concentration (vacuum concentration), freeze drying, and spray drying. It is desirable to avoid drying.

In addition, when dry powdering, 5 other excipients, binders 1, etc., such as dextrin, various vegetable starches, or water-soluble polysaccharides thereof, are added as appropriate to powder (product ) may also be used.

In this case, in the case of a powdered product, the water content in the powder is preferably 12% or less, preferably 7 to 8%.
Stability is maintained over long periods of time by finishing the product as follows and storing it in a container that does not absorb moisture.

"Extraction method 3" (Example of production of plant-based R:H) When extracting from H: peach leaves, the ratio of water and 1,3-butylene glycol is from 6 to 4 as the extraction solvent. By using a 3:7 mixed solvent, the following:
The other steps are the same as those described above (extraction methods 1 and 2), and the extracted solution is filtered, and if necessary, a further concentrated solution is prepared, and this is used as a lipid peroxide production inhibitor.

The solution extracted by the above step (extraction method 3) is
Although it can be used in the form of powder as shown in Extraction Methods 1 and 2), when used in cosmetics, it is usually in the form of a solution because it can be easily blended into various cosmetics in any desired amount. It can be used in a wide range of applications, from skin cosmetics to hair cosmetics, and can be particularly easily added to hair shampoos and conditioners.

Regarding the combination of extraction solvents when used in foods, beverages, and cosmetics, a mixed solvent of water and 1,3-butylene glycol was used in the process of the above (extraction method 3).
It is also possible to use a solution obtained by replacing 1.3-butylene glycol with propylene glycol and using a mixed solvent of water and propylene glycol in a ratio of 6:4 to 3:7.

[Results of examination of combinations (ratios) of extraction solvents] According to the above-mentioned extraction methods 1 to 3, all of them can serve as the desired excellent lipid peroxide production inhibitor. But further.

Here, corresponding to each plant superthickness = A to H.

The question of which solution has the strongest ability to inhibit lipid peroxide production and has the best stability is determined from the relationship with the extraction solvent employed in the present invention, as shown below.

In the case of A: green tea & black tea and B: peonies.

Both water and ethanol! , the ratio with 3-butylene glycol is around 5:3:2.

C: Mugwort, D = Clove, E: Gennoshoko, F:
Asenyaku, G: In the case of Oubaku.

The ratio of water to ethanol is around 7:3.

H: In the case of peach leaves, the mixing ratio of water and polyol solvent can be determined from the ability to suppress the production of lipid peroxide! 3 parts water to 6 parts polyol solvent (1 part)
, 3-butylene glycol, propylene glycol) is around 4, the solution can be in its strongest state.

In addition, the lipid peroxide production inhibitor obtained by extraction method 3 (
In order to use the solution as food (drinkable), it is preferable to use water and propylene glycol as the polyol solvent.

"Confirmation of lipid peroxide production inhibiting action (effect) j (a) Test method In order to confirm the action/effect of the present invention, testing was carried out under the following test conditions.

A 0.1% lyric acid solution was added to a 0.8% sodium lauryl sulfate aqueous solution to dissolve it.

Take 3.9mβ of this solution and adjust it to an appropriate concentration.
After adding 0.1rnρ of various extract solutions “specimen”,
Apply ultraviolet light (Toshiba lamp: FL-20) to the solution.
After irradiating 3 SE lamps and FL-20SBLB lamps (3 lights in parallel, irradiation distance: 15 cm) for 1 hour, take this liquid at 1+r+12, and then apply 0.
8% thiobarbylic acid (Ding B^) aqueous solution 1.5rnI
After adding 1.5 mj2 of 20% acetic acid (pH 3,5), the mixture was heated at 95°C for 1 hour. Cool, add 1 ml of purified water and 5 ml of n-butanol:pyridine (15: 1), shake, centrifuge, and measure the absorbance of the n-butanol layer at 532 nm to determine the amount of lipid peroxide produced. measure the amount of

In addition, the amount of lipid peroxide when adding a sample and irradiating ultraviolet rays is a, the amount of lipid peroxide when adding a sample and not irradiating ultraviolet rays, and the amount of lipid peroxide when irradiating ultraviolet rays without adding a sample. a ° Lipid peroxide when no sample is added and no ultraviolet rays are irradiated is bo, a-b and a'-b'
The suppression rate is determined from the 9th order equation, where is the amount of lipid peroxide produced.

The method adopted in the present invention is a quantitative method numerically called the TBA method, and its details are described in 1.
It is shown in the following literature (magazine).

(References related to TBA method) Analytical, Biochemistry v02゜95, p3
51-358. (1979) (b) Effect/Inhibition of lipid peroxide production As a result of continued searching based on the above test method, 1. In the present invention,
As mentioned above, we were able to specify the ultra-thickness of plants A to H and select the most suitable extraction solvent for each.

The following table "Table 2" shows the solutions obtained by filtering the crude extract solution in the process of producing the extract (manufacturing method: extraction methods 1 to 3) according to the present invention (a). Using the test method of 25.12, 5.2, the concentration added to the system was
．． The results are shown when measurements were performed using 5 μl in three stages. In addition, in "Table 2", in order to understand the amount of components contained in each solution used in the nine tests: the concentration of the extract component, the column "Evaporation residue" is included as one indicator. I set it up and showed the measured values.

identified here. It can be confirmed that all of the extracts derived from plants A to H have a strong inhibitory effect on the production of lipid peroxide even at extremely small concentrations.

"Table 2" Ability to inhibit the production of lipid peroxide (c) Storage stability In Table 2 above, the extract solutions obtained from each of A to H, which showed the evaporation residue, remained for a long period of time. ,
There is very little generation of sludge or precipitates, and the stability is good.

However, along with these apparent stability, solutions stored for a long period of time still have the ability to suppress the formation of lipid peroxides.

Do you have the power to do so?

For example, as introduced in the introduction, some lipid peroxides are known to have a suppressive effect, and the solution after extraction not only generates scum and precipitates within a short period of time, but also
When stored for a long period of time, its ability to generate lipid peroxide is significantly reduced, and many of them are completely useless and unstable.

In other words, if the product is stored in a state such as lyophilized, hermetically sealed, or at a low temperature, there is little decrease in the 5 effects, but if it is in a solution or dissolution solution containing those active ingredients, this When we investigated its effects over time under room temperature storage, we found that the extracts often had the property of deteriorating. For example, in the case of SOD, Because of its specificity, it shows a decrease in its activity, and therefore, if it is to be used specifically in the formulation of cosmetics, there are still many problems that remain to be solved in formulation. However,
In this regard, the present invention has the advantage that, as shown in the following table "Table 3", even when the extract solution is stored for a long period of time, its action hardly decreases and excellent long-term stability is maintained. That's true.

This sustained stability lies in the balance between the selection of organic solvents and their combination during extraction.

For example, the active substance can be extracted using hydrophilic organic solvents similar to ethanol such as methanol and impropatul, but the solubility stability is significantly reduced and lipid peroxide is generated. Regarding the inhibitory effect on
Its sustainability will be poor.

In order to specifically illustrate this point, Table 3 lists five samples based on the same raw materials as specified in the present invention.

Extracts from some plants using a single organic solvent were first freeze-dried and then dissolved in a mixture of water and ethanol at a ratio of 5:5 (in the sample column of Table 3). The solvents used are also shown in the lower part of ti).

That is, as can be understood from Table 3, the combination of extraction solvents has a large effect on the suppressing effect, sedimentation, precipitation, etc.

In other words, even though it is possible to incorporate a simple extract into emulsified products such as creams or powdered preparations, transparent liquid products such as lotions, shampoos, conditioners, etc. In such cases, sludge and precipitates are generated, and at this point, the inhibitory effect on the production of lipid peroxide rapidly decreases.

Also, in Table 3, in the columns of sludge and sediment.

The O mark indicates that no such formation was observed, and the mark indicates that sludge or precipitate was formed.

(Search for dl main components contained in each of the extracts specified in A to H above. Regarding this point, what component in the extract achieves the effect of suppressing the production of lipid peroxides? It has not yet been confirmed.

However, when we analyze the main components based on each extract, we find that the components shown in Table 4 below have been confirmed so far. , is estimated to be one of the potentially involved substances.

"Table 4" Contains the main confirmed components contained in the extract. Therefore, for example, it can be incorporated into a wide range of formulations, and even in formulations containing water, it can be used without using a dispersant (surfactant).

In particular, conventional inhibitors of lipid peroxide production have not been fully applied to cosmetics because many of them are unstable or insoluble in systems containing water. , if it is an inhibitor according to the present invention, the second to third
As can be seen from the stability and sustained inhibitory effect shown in the table, it can be easily incorporated into everything from lotions to creams, which can be said to be a great advantage.

(c) Effects of the invention

Claims (1)

[Claims] [1] A: green tea or black tea, B: peony, C: mugwort, D
:Choji,E:Gennoshouko,F:Asenyaku,G
: Peach leaf, H: Using peach leaves as starting material, its A~
A lipid peroxide production inhibitor characterized in that the extraction solvent for each of H contains one or more of the plant extracts eluted using the following mixed solvents. [Extraction Solvent for A to B] A mixed solvent of water, ethanol, and 1,3-butylene glycol in a ratio of 5:3:2 to 3:3:4 is used. [Extraction solvent for C to G] A mixed solvent of water and ethanol in a ratio of 7:3 to 4:6 is used. [Extraction Solvent for H] A mixed solvent containing water and 1,3-butylene glycol in a ratio of 6:4 to 3:7 is used.