JP4693964B2 - New antifeedant - Google Patents

Description

[0001]
BACKGROUND OF THE INVENTION
The present invention relates to food intake inhibitor comprising a substance having an anorexigenic action of Abou transient plant as an active ingredient.
[0002]
[Prior art]
Conventionally, various methods have been considered to prevent or eliminate obesity.
As a method for achieving the above object, for example, dietary restriction can be mentioned. Here, in order to easily restrict meals, a drug having an appetite suppressing action may be used. Such drugs include tetrahydropyridine compounds (Japanese Patent Laid-Open No. 57-159714), deoxy-D-glucose derivatives (Japanese Patent Laid-Open No. 60-81127), aminopolysaccharides such as chitin (Japanese Patent Laid-Open No. 62-123122), triglyceride derivatives ( JP-A-3-220123) and the like.
[0003]
Moreover, Abou transient extract lipolysis promoting effect is that has been reported in (JP-A 11-246425), although the effect for obesity prevention or eliminated is expected, facilitates diet in accordance Abou transient plant However, it has not been known that a component having an anti-feeding action is contained.
[0004]
[Problems to be solved by the invention]
An object of the present invention is to provide an antifeedant that is safe and easy to prepare.
[0005]
[Means for Solving the Problems]
The present inventors have were elite searched to solve the above problems, found that an excellent anorexigenic effect in extracts of Abou transient plant, thereby completing the present invention. That is, the present invention is as follows.
[0006]
(1) Abou transient plants and / or food intake inhibitor substance, as an active ingredient with a food intake suppressing effect obtained by extraction with an organic solvent from the treated.
(2) The Abou transient plants and / or extract extracted with an organic solvent from the treated partitioned chromatographic fraction, containing a substance having an anorexic effect obtained by such fractionation as an active ingredient A substance that is an antifeedant and has an antifeedant action is subjected to thin-layer chromatography using silica gel 60 manufactured by Merck as an eluent with an organic solvent having a hexane / ethyl acetate mixing ratio of 4/1. An antifeedant that, when performed, has an Rf value in the range of 0.19 to 0.25.
(3) The eating inhibitor according to (1) or (2), wherein the organic solvent is a nonpolar organic solvent.
(4) The organic solvent according to any one of (1) to (3), wherein the organic solvent is one or more selected from the group consisting of n-hexane, cyclohexane, benzene, and carbon tetrachloride. Antifeedant.
[0007]
(5) The eating inhibitor according to any one of (1) to (3), wherein the organic solvent is n-hexane.
(6) The feeding inhibitor according to any one of (2) to (5), wherein the chromatographic fractionation is performed using a silica gel column.
(7) A pharmaceutical composition for suppressing feeding, comprising the feeding inhibitor according to any one of (1) to (6).
(8) The composition for foodstuffs for feeding suppression containing the feeding inhibitor as described in any one of said (1)-(6).
[0008]
DETAILED DESCRIPTION OF THE INVENTION
Hereinafter, the present invention will be described in detail.
<1> anorexigenic agents eating inhibitors present invention feeding of the present invention contains a substance having anorexigenic action of Abou transient plant as an active ingredient. Abou transient plant used in the present invention is a plant belonging to the Lauraceae Waninashi, Abou mosquito de genus (M. shearei, Persea). Waninashi, as Abou transient species, the United States Na (P. americana), Mexican (Mexican race), Guatemala-based (Guatemalan race), West Indies system (Indian race), and the like, especially the United States Na (P. americana) is preferred.
[0009]
Substances having a phagocytic inhibitory effect feeding of the present invention, pulp Abou transient plant, pericarp, seeds, leaves, stalks, branches and the like, as well as crushing them, drying, have been included in the treated product was concentrated like In particular, since the substance is contained in a large amount in the pulp and pericarp, these tissues and processed products of these tissues are preferable.
[0010]
The above-described processing, the Abou transient plant untreated, but it is also possible as an active ingredient of the anorexigenic agents, further subjected to extraction therefrom, the present invention an extract containing a substance having anorexigenic activity It is preferable to use it as a component of an antifeedant.
[0011]
Extraction of Abou transient plant, continuous, by a method such as batch, carried out at any time by maceration or digestion by a conventional method. For instance, a dry powder of Abou transient plant, finely ground, the extraction solvent is carried out for 1 to 48 hours, soaking and or shaking to room temperature. Thereafter, the extraction residue is removed from the extract, and the extract is concentrated under reduced pressure or ultrafiltration. Further, if necessary, the solvent is distilled off.
[0012]
The solvent used for such extraction is preferably an organic solvent, more preferably a nonpolar organic solvent, and specifically includes n-hexane, cyclohexane, benzene, carbon tetrachloride, etc. Among them, n-hexane Is preferred.
[0013]
Although the extraction example of the substance which has the feeding suppression effect of this invention is illustrated below, this invention is not limited to this extraction example. First, lyophilized Abou transient plant, a water-insoluble non-polar organic solvent is added to the dry powder, extracts a component soluble in the solvent. Preferred examples of the water-insoluble nonpolar organic solvent used in this case include n-hexane and cyclohexane. The amount of solvent added to Abou transient plants per dry powder 1g, is preferably from 1～200Ml, and even more preferably 5～50Ml. Operation After adding the solvent to Abou transient plant, and stirred well with a stirrer or the like, in a non-polar organic solvent to extract the soluble fraction. This operation is usually preferably repeated 2 to 5 times. An oily extract is obtained by removing the solvent of the extract fraction thus obtained. The solvent can be removed by various commonly used removal methods such as evaporation of the solvent under normal pressure or reduced pressure.
[0014]
Furthermore, the extract obtained above is further separated and purified by chromatographic fractionation using various chromatographies such as adsorption chromatography and partition chromatography alone or in combination, and the food intake obtained by such fractionation is obtained. A fraction containing a substance having an inhibitory action is preferably used as a component of the antifeedant of the present invention. Here, the fraction containing the substance having an antifeeding action has an Rf value of 0.19 to 0.00 in thin layer chromatography (silica gel 60 manufactured by Merck, developing solvent: hexane / ethyl acetate = 4/1). Since it has the characteristic that it is a value within the range of 25, the fraction can be selected using this as an index.
[0015]
Although the example of the chromatographic fraction of the substance which has the feeding suppression effect of this invention is illustrated below, it is not limited to these.
The above-mentioned extract is dissolved in an eluate having a low elution power and is applied to a silica gel column as adsorption chromatography. Elution is carried out with an eluate whose elution power is increased stepwise, and the eluate is collected over time to be fractionated and separated and purified. By removing the solvent in the fractionated fraction, a fraction containing a substance having an antifeeding effect can be obtained. The solvent can be removed by various commonly used removal methods such as evaporation of the solvent under normal pressure or reduced pressure. The fraction can be selected by the method described above.
[0016]
In addition, the method for determining whether or not the above-mentioned extract and fraction contain a substance having an antifeeding effect is not particularly limited, but it is applied to a model animal such as a mouse. Create a group that ingests the feed to which the extract or fraction is added and a group that ingests the feed that has not been added, and measure changes in the feed intake and body weight of these groups after a certain period of time Thus, it can be determined whether or not a substance having an antifeeding action is contained.
[0017]
<2> Pharmaceutical composition for feeding suppression containing the feeding inhibitor of the present invention The pharmaceutical composition of the present invention comprises the above feeding inhibitor formulated according to a conventional method. There is no particular limitation as long as a suppressive action can be expected.
The dosage form of the pharmaceutical composition of the present invention is not particularly limited, and is generally mixed with one or more pharmaceutically acceptable carriers, excipients, integrating agents, preservatives, stabilizers, flavoring agents and the like. , Tablets, granules, capsules, liquid medicines, drinks, etc. Such formulation can usually be formulated according to a method used for production of a medicine.
[0018]
The dosage of the pharmaceutical composition, kind of diseases, symptoms, age of the patient, varies in body weight and the like, an adult per day, the 100~5000mg as a non-polar organic solvent extract of Abou transient plant, also the It is preferable that 10 to 500 mg of the extract obtained by performing chromatographic fractionation is orally administered in one or several divided doses.
[0019]
<3> The composition for foodstuffs for feeding suppression containing the feeding inhibitor of this invention The foodstuff composition of this invention mix | blends said feeding inhibitor according to a conventional method. The food composition of the present invention is not particularly limited as long as it contains the above-mentioned antifeedant, but various foods, together with optional ingredients that are usually used as food, are food ingredients. The required amount of extract can be added to This extract is not specifically noted to Rukoto in formulating, by processing prepared by conventional manufacturing methods, it is possible to manufacture a health food, functional food. The blending amount differs depending on the type of food, but in order to obtain a sufficient food intake suppression effect without impairing the taste of the food, it is blended at a ratio of 0.01 to 10% by weight with respect to the total amount of the food. Is preferred.
[0020]
【Example】
Hereinafter, the present invention will be described more specifically with reference to examples.
[Example 1]
<Extraction of active ingredient of the present invention>
The pulp portion of Abou transient and lyophilized to give a dry powder. This dry powder was fractionated according to the flow shown in FIG. 1 below and used for later evaluation.
[0021]
(A) Fractionation Abou transient of a dry powder 100g of a pulp portion obtained by freeze-drying 1L After stirring n- hexane was added enough with hexane to give the removal of the residue supernatant as hexane extract. This operation was further repeated twice, and 3000 ml of hexane extract was obtained by a total of three operations. By concentrating this extract using an evaporator, 58.6 g of an oily concentrate was obtained from the hexane fraction.
[0022]
(B) Fractionation with ethyl acetate Next, 1 L of ethyl acetate was added to 41.4 g of the residue obtained in the above operation (a), and after sufficient stirring, a supernatant from which the residue was removed was obtained as an ethyl acetate extract. This operation was further repeated twice to obtain 3000 ml of ethyl acetate extract by a total of three operations. The extract was concentrated to dryness using an evaporator to obtain 0.8 g of a solid from the ethyl acetate fraction.
[0023]
(C) Fractionation with 70% ethanol Next, 1 L of 70% ethanol was added to 40.6 g of the residue obtained in the above-mentioned operation (b), and after sufficient stirring, a supernatant from which the residue was removed was obtained as a 70% ethanol extract. This operation was further repeated 4 times, and 5000 ml of 70% ethanol extract was obtained by a total of 5 operations. The extract was concentrated to dryness using an evaporator to obtain 16.0 g of a solid from the 70% ethanol fraction. In addition, 24.6 g of ethanol residue was obtained by the operation (c).
[0024]
(D) Fractionation with butyl alcohol (butanol) Next, 16.0 g of the concentrated dried product obtained by the above operation (c) was dissolved in 500 ml of distilled water. Then, 500 ml of n-butanol was added to this solution and sufficiently stirred, and then the butanol layer was extracted by countercurrent distribution using a separatory funnel. To the remaining aqueous layer, 500 ml of n-butyl alcohol was further added and sufficiently stirred, followed by extraction with n-butyl alcohol. This extraction was further repeated 3 times, and a total of 5 extraction operations yielded 2500 ml of butyl alcohol extract. The butyl alcohol extract was concentrated to dryness using an evaporator to obtain 2.8 g of a solid from the butyl alcohol fraction.
[0025]
In addition, 13.2 g of a solid was obtained from the water-soluble fraction by concentrating and drying the solution in the aqueous layer portion using a freeze-drying apparatus in operation (d).
Table 1 shows the distribution ratio (% by weight) to each fraction obtained by fractionation by the above operation. Here, the distribution ratio is a value obtained by dividing the weight of the solid matter obtained from each fraction by the weight (100 g) before the start of fractionation and multiplying by 100 to display the percentage.
[0026]
[Table 1]
[0027]
(E) Fractionation of hexane fraction by silica gel column The same operation as that of the operation (a) was performed again on a scale to obtain an oily concentrate of the hexane fraction. 100 g of the obtained dry solid was redissolved in 500 ml of a mixed solvent of hexane / ethyl acetate (5/1) and applied to a silica gel column (silica gel 60, 8 × 73 cm manufactured by Merck). Elute. The elution solvent used here was hexane / ethyl acetate (5/1) , hexane / ethyl acetate (4/1) , hexane / ethyl acetate (3/2) , hexane / ethyl acetate (2/3) , ethyl acetate. Methanol was applied to the column in this order and fractionated by collecting the eluate over time. These eluates were subjected to thin layer chromatography (silica gel 60 manufactured by Merck, eluent: hexane / ethyl acetate = 4/1), and when no band having ultraviolet absorption could be confirmed, the elution was changed to the next elution solvent. did. The fractions of these fractionated eluates were subjected to thin layer chromatography (silica gel 60, Merck & Co., developing solvent; hexane / ethyl acetate = 4/1), and finally the results of the Rf values were used as indices. Divided into 7 fractions. The yield of each fraction was as follows: fraction [1] 84.1 g, fraction [2] 1.2 g, fraction [3] 1.8 g, fraction [4] 7.1 g [5] was 1.9 g, fraction [6] was 1.5 g, and fraction [7] was 2.4 g. Table 2 shows the Rf value, the distribution rate, and the composition of the elution solvent in the thin layer chromatography of each fraction.
[0028]
[Table 2]
[0029]
[Example 2]
<Evaluation of feeding suppression effect>
For evaluation, 5-week-old male Wistar rats were used. After 4-5 days of pre-feeding, each group was divided into 7 groups so that the average body weights were approximately equal, and each test feed was ingested for 2 weeks. Feed intake and body weight were measured daily throughout the test feed intake period.
[0030]
Table 3 shows the feed composition used in the test. Moreover, each fraction in Example 1 is used as a test additive, and the addition amount of the test additive is shown in Tables 4 and 5. Here, the amount of each composition in Table 3 is shown in g per kg of feed. Moreover, the test additive and corn starch in Table 3 are prepared such that corn starch is added to the test additives having the addition amounts shown in Table 4 and Table 5, respectively, so that the total is 401 g / kg. In addition, the feed ingested by the control group is prepared so that it may become 401 g / kg only by a corn starch without a test additive. The addition amount of each test additive in Table 4, both have a Abou transient pulp partially dried amount corresponding to 5% by weight addition of the powder, the amount of each test additive in Table 5, both The amount added corresponds to the addition of 3.8% by weight of the hexane fraction.
[0031]
[Table 3]
[0032]
[Table 4]
[0033]
[Table 5]
[0034]
Table 6 and Table 7 show the weight gain and feed intake of each group for 3 days after switching to the test feed. In the hexane fraction, feed intake and body weight gain were significantly lower than those in the other groups, and it was observed that they decreased with intake for 3 days. It was clear that the hexane extract fraction had an antifeeding effect. It became. Furthermore, in the fraction [4] obtained by chromatographic fractionation of the hexane fraction, the amount of feed intake and body weight gain was significantly less than those of the other groups, and decreased with intake for 3 days. Observed, it was revealed that fraction [4] has an antifeedant action.
[0035]
[Table 6]
[0036]
[Table 7]
[0037]
【The invention's effect】
Antifeedant agent containing Abou transient of the extract of the present invention as an active ingredient has an excellent anorexigenic effect. In addition, since the antifeedant of the present invention is derived from a plant and is safe and easy to extract, it provides a pharmaceutical or food composition containing the antifeedant that is easy to formulate. be able to.
[Brief description of the drawings]
1 is a diagram showing an example of extracting an active ingredient of a food intake inhibitor from Abo transient.

Claims (7)

Anorexigenic agent a substance having anorexic activity, to human comprising as an active ingredient for human obtained by extraction with an organic solvent from the pulp and / or a processed material thereof in Abou transient plant. Containing Abou transient the extracted extract partitioned chromatographic fraction using organic solvents from the pulp and / or treatment of plants, a substance having an anorexic effect on human obtained by such fractionation as an active ingredient The anti-feeding substance, which is an anti-feeding substance, is a thin-layer chromatography using silica gel 60 manufactured by Merck as an eluent with an organic solvent having a hexane / ethyl acetate mixing ratio of 4/1. An antifeedant to humans having an Rf value in the range of 0.19 to 0.25.   The eating inhibitor according to claim 1 or 2, wherein the organic solvent is a nonpolar organic solvent.   The eating inhibitor according to any one of claims 1 to 3, wherein the organic solvent is one or more selected from the group consisting of n-hexane, cyclohexane, benzene, and carbon tetrachloride. .   The eating inhibitor according to any one of claims 1 to 3, wherein the organic solvent is n-hexane.   The feeding inhibitor according to any one of claims 2 to 5, wherein the chromatographic fractionation is performed using a silica gel column. The pharmaceutical composition for feeding suppression with respect to the human containing the feeding inhibitor as described in any one of the said Claims 1-6.