JPH0995452A - Fat-decomposing promoting agent - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a lipid-decomposing promoting agent which contains a specific alkaloid as an active ingredient and is useful for medicines, cosmetics and health food products. SOLUTION: This alkaloid is included, as at least one active ingredient, in the Phellodendri Cortex extract and Coptidis Rhizoma extract, or is a berberine type alkaloid as at least one kind selected from the group consisting of a berberine salt of formula I (R<1> and R<2> are each a 1-5C alkyl; (n) is an integer of 1-5; X is a monovalent anion) or its derivative or a palmatine salt of formula II or its derivative and kopsidine salt of formula III or its derivative.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a lipolysis promoter, and more particularly to a lipolysis promoter containing an extract obtained from a specific plant or a specific alkaloid as an active ingredient. The lipolysis-promoting agent according to the present invention has an excellent lipolysis-promoting action, and can be widely used in various fields such as pharmaceuticals, cosmetics, and health foods.

[0002]

2. Description of the Related Art Excessive accumulation of fat causes various adult diseases and is not preferable in terms of beauty. Conventionally, in order to metabolically decompose excess fat, extracts from various plants and seaweed have been used in the form of cosmetics,
The current situation is that it is not sufficiently effective. Attempts have also been made to extract lipolysis-promoting components from various natural products, but the results have not been satisfactory.

[0003]

In the fields of pharmaceuticals, cosmetics, foods, etc., there is an increasing demand for highly safe naturally-occurring lipolysis promoters. However, the type and amount of the naturally-derived lipolysis promoter currently in practical use are very limited, and it is difficult to formulate various dosage forms and forms even when used. In view of the above problems, the present invention intends to stably supply a large amount of a novel naturally-occurring lipolysis promoter with high safety.

[0004]

According to the present invention, the above-mentioned problems can be solved by at least one component selected from the group consisting of Chinese cabbage extract and Orchid extract, or fat containing berberine-type alkaloid as an active ingredient. It is solved by a decomposition accelerator.

Yellow crow is Phellodendron of Rutaceae.
amurense and its variants, or Phellodendron chin
It is a dried bark excluding the cork layer of ense and its varieties.It contains alkaloids such as berberine, palmatine, and yateolidine, bitterness components such as ovabacnon and obaclactone, and lipids such as linoleic acid and β-sitosterol. It is widely used as a health medicine, an intestinal remedy, and an antiphlogistic astringent for gastroenteritis, abdominal pain, jaundice, diarrhea, etc., and as a herbal medicine and folk medicine for bruising poultice and eye drops. However, the lipolysis promoting action has not been reported at all, and its use as a lipolysis promoting agent has not been known.

Yellow lanterns are Coptis , a family of buttercups.
It is a dried rhizome of japonica or Coptis japonica var.dissecta. It contains alkaloids such as berberine, coptidine, yateolidine, palmatin and magnoflorin, and ferrulic acid, and is used as a bitter stomachic and intestinal medicine. It is also widely used in Chinese medicine as Orengedokuto.

To extract the extract from Huangba or Huanglian,
As the solvent, water, methanol, ethanol, isopropyl alcohol, butanol, ethyl acetate, acetone, ether, chloroform or the like can be used. You may use these solvents in combination of 2 or more types. Of these, particularly preferable solvents are water, methanol and ethanol.

The berberine-type alkaloid has the general formula (I):

[0009]

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(In the formula, R ¹ and R ² are the same or different and each represents an alkyl group having 1 to 5 carbon atoms, n is an integer of 1 to 5, and X represents a monovalent anion. ), A berberine salt or a derivative thereof represented by the general formula (II):

[0011]

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(In the formula, R ¹ , R ² , R ³ and R ⁴ are the same or different and each represents an alkyl group having 1 to 5 carbon atoms;
Represents a monovalent anion. ) The palmat salt or its derivative represented by the general formula (III)

[0013]

[Chemical 6]

(Wherein, n and m are each an integer of 1 to 5 and X represents a monovalent anion), and a coptidine salt or a derivative thereof is preferable.

Berberine chloride represented by the general formula (I) in which R ¹ and R ² are both methyl groups, n is 1 and X is a chlorine ion, or R ^{1 to} R ⁴ are all methyl groups chloride palmatine which X is represented by the general formula (II) is chlorine ion, the Rutaceae Phellodendron Phellodendron amu
rense and its variants, or Phellodendron chinense
And bark of its varieties excluding cork layer, barberry of barberry family
Berberis thunbergii xylem, Columbo of the family Aceraceae
It is contained in the roots of Jateorhiza columba and has a strong antibacterial action against gram-negative bacteria such as Escherichia coli, cholera, typhoid, and as a stomachic agent, intestinal rectifier, as a bactericidal agent, for bacterial diarrhea, abnormal intestinal fermentation, etc. It is also used for poultice and eye drops for bruising.

Coptidine chloride represented by the general formula (III) in which n and m are both 1 and X is a chloride ion,
Coptis japonica or Copti of the buttercup family
It is contained in the rhizome of s japonica var. dissecta and is used for gastroenteritis, abdominal pain, jaundice, diarrhea, etc. as a bitter tasting medicine, antiflatulent, antiphlogistic astringent, and for poultice and eye drops for bruising. However, none of berberine chloride, palmatine chloride, and coptidine chloride has been reported to have a lipolysis-promoting action, and its use as a lipolysis-promoting agent has not been known.

The berberine salt or its derivative, the palmatine salt or its derivative, and the coptidine salt or its derivative may be used alone or in any two of them.
You may use it in combination of 2 or more types.

As these berberine-type alkanoids, those extracted and purified from the above-mentioned plants, synthetic products, and those extracted and purified from callus cultures of Coptis chinensis and the like can be used. Furthermore, it is also possible to use berberine chloride, palmatine chloride, or coptidine chloride-containing extracts such as yellowfin, colombo root, barberry, oren, or fractionated products of these extracts.

Water, methanol, ethanol, isopropyl alcohol, butanol, ethyl acetate, acetone, ether, chloroform and the like can be used as a solvent for the extraction of berberine-type alkanoid. You may use these solvents in combination of 2 or more types. Of these, particularly preferable solvents are water, methanol and ethanol. Further, these berberine-type arkanoids can be added to other preparations such as seaweed extract.

[0020]

[Examples] The following will specifically describe the action of the lipolysis-promoting agent of the present invention by showing Examples.

Example 1 Preparation of yellow oak extract 1000 g of yellow oak was added to 3000 ml of water at 90 to 95 ° C.
After heat extraction for 1 hour, the extract was filtered and then concentrated under reduced pressure to obtain 300 g of the extract.

Measurement of lipolysis promoting effect M. Rodbell et al. (M. Rodbell et. Al., J. B.
iol. Chem. 239 , 375-380 (1964)), the adipocytes prepared from the epididymal adipose tissue of Wistar male rat 5
0 μl was added to a mixed solution of 200 μl of Hank's buffer solution of 2.5% bovine serum albumin and 25 μl of the sample shown in Table 1. Norepinephrine solution (0.5 μg
/ Ml) was added and the mixture was incubated at 37 ° C for 1 hour. Chloroform: heptane: methanol (98: 98: 4) (3 ml) was added to the reaction solution, and the mixture was stirred and shaken for 10 minutes to extract a lipid. Centrifuge at 2500 rpm for 5 minutes, add 1 ml of copper reagent and shake for 10 minutes, then 2500 rp
After centrifuging at m for 10 minutes, 0.5 ml of the supernatant was taken, and a coloring reagent (prepared by dissolving 0.2 g of bathocuproine and 0.1 g of butylhydroxyanisole in 200 ml of chloroform).
5 ml was added and mixed well, and the absorbance at 480 nm was measured to measure the amount of free fatty acid. Table 1 shows the results.

[0023]

[Table 1]

The Huangqiao water extract extracted the fatty acids of triglyceride contained in adipocytes in a concentration-dependent manner.
Furthermore, a remarkable effect of enhancing the lipolysis of norepinephrine, which is involved in lipolysis in vivo, was observed. From these results, it was revealed that yellow oak has a strong lipolysis promoting action.

Example 2 250 μl of a sample solution of berberine chloride, palmatine chloride or coptidine chloride (2.5% bovine serum albumin Hanks buffer solution) was mixed with 50 μl of adipocytes prepared from epididymal adipose tissue of wistar male rat. Plus 3
Incubated at 7 ° C for 1 hour. 3 ml of chloroform: pentane: methanol (98: 98: 4) was added to the reaction solution.
Was added and the mixture was stirred and shaken for 10 minutes to extract lipid. 2500
Centrifuge at rpm for 10 minutes, remove the upper layer (aqueous layer) by suction, add 1 ml of copper reagent, shake for 10 minutes, centrifuge at 2500 rpm for 10 minutes, then add 0.5 ml of the upper layer to another test tube to develop color. 0.5 ml of the reagent was added and mixed well, and the absorbance at 480 nm was measured to measure the amount of free fatty acid. The respective results are shown in FIGS. All of them released the fatty acid of triglyceride contained in adipocytes in a concentration-dependent manner.
That is, berberine chloride, it showed high fat resolution 10 ^-3 mole, palmatine chloride, cause lipolysis in 10 ^-5 mole, caused lipolysis apparent at 10 ^-3 mole. It was confirmed that coptidine chloride causes a lipolysis at 10 ^-5 mole and that the lipolytic ability is increased depending on the concentration, which is a remarkable effect. From these results, it was clarified that berberine chloride, palmatine chloride and coptidine chloride have strong lipolysis promoting action.

As mentioned above, the yellow oak extract, berberine chloride, palmatine chloride and coptidine chloride all have a lipolysis promoting action, and are used in the fields of medicines and health foods for the prevention of obesity, and for slimming effects in cosmetics. Can be widely used in. These compounds have been used for various internal and external medicines since ancient times, and their safety has already been confirmed.

[0027]

EFFECTS OF THE INVENTION According to the present invention, it is possible to provide a highly safe and novel naturally-occurring lipolysis promoter. The lipolysis promoter can be used in a wide variety of fields depending on fields such as pharmaceuticals, cosmetics, and health foods.

[Brief description of drawings]

FIG. 1 is a graph showing the result of fatty acid decomposition by palmatine chloride in Example 2.

FIG. 2 is a graph showing the result of fatty acid decomposition by berberine chloride in Example 2.

FIG. 3 is a graph showing the result of fatty acid decomposition by copsicitin chloride in Example 2.

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁶ Identification number Internal reference number FI Technical display location A61K 7/00 A61K 7/00 KD (72) Inventor Koichiro Hino 888 Yabuhara Kisomura, Kiso-gun, Nagano Prefecture

Claims (3)

[Claims] 1. A lipolysis promoter comprising, as an active ingredient, at least one component selected from the group consisting of Chinese cabbage extract and Orchid extract. 2. A lipolysis promoter comprising a berberine-type alkaloid as an active ingredient. 3. A berberine-type alkaloid has the general formula (I): (In the formula, R ¹ and R ² are the same or different and represent an alkyl group having 1 to 5 carbon atoms, n is an integer of 1 to 5,
X represents a monovalent anion. ), A berberine salt or a derivative thereof, represented by the general formula (II): (In the formula, R ¹ , R ² , R ³ and R ⁴ are the same or different and each represents an alkyl group having 1 to 5 carbon atoms, and X represents a monovalent anion). Derivatives thereof, and general formula (III) (In the formula, n and m are each an integer of 1 to 5, and X
Represents a monovalent anion. ) At least one selected from the group consisting of coptidin salts represented by
The lipolysis-promoting agent according to claim 2, which is a kind of compound.