Patent Grant
7407674
This application claims priority from Japanese Application JP 2006-072963, filed on Mar. 16, 2006.
The present invention relates to a lipolysis promoter which promotes the degradation of body fat, reduces systemic or local fat, and is effective in preventing and ameliorating obesity, and food-and-drink and feed containing the same.
Obesity results from the accumulation of intake energy in adipocytes as neutral fat in excess of consumption energy, and not only triggers various diseases such as arteriosclerosis, but also is cosmetically undesirable, so that its prevention and amelioration are strongly required. However, recent years have seen an increase in the obesity rate in the industrialized countries including our country year by year. The reason comes from overeating, lack of exercise, stress, and the like, but there are many people who cannot continue dietary restriction and exercise therapy, which require a strong will and long continuance.
This background has given rise to a wide range of development of lipolysis promoters effective in preventing and ameliorating the obesity. For example, there have been known a lipolysis promoter containing a plant or its extract selected from Juniperus communis, Rosa normalis, Rosa canina, Areca catechu, Polygala tenuifolia, Plantago asiatica, Jateorhiza columba, Stellera chamaejasme, Tropaeolum majus, Aristolochia manshuriensis, Myrica rubra Imperata cylindrica, Ligusticum sinense, Hemerocallis plicata, Betula platyphylla var. japonica, Salvia miltiorrhiza, Erodium stephanianum, Brassica hirta, Helianthus annuus, Glechoma hederacea, Lycium chinense, Sophora japonica, Homalomena occulta, Ficus carica, Pueraria thomsonii, Hibiscus rosa-sinensis, chenopodium hybridum, Trigonella foenum-graecum, Juglans regia, Alpinia katsumadai, Prunus humilis Bunge, Gardenia jasminoides, Chrysanthemum indicum, Rubia cordifolia, Hedyotis diffusa, Lysimachia christinae, Schizonepeta tenuifolia, Portulaca oleracea, Angelica dahurica, and Polygonum aviculare as an active ingredient (See Japanese Unexamined Patent Publication No. 2005-60366), a lipolysis promoter comprising an extract of Zygophyllaceae Larrea as an active ingredient (for example, refer to Japanese Unexamined Patent Publication No. 2004-35516), a lipolysis promoter comprising peels or leaves of citrus fruits or extracts therefrom (for example, refer to Japanese Unexamined Patent Publication No. 2002-326947), a lipolysis promoter containing a Cirsium plant as an active ingredient (for example, refer to Japanese Unexamined Patent Publication No. 8(1996)-301780), a lipolysis promoter containing an extract of Geranium nepalense Sweet (for example, refer to Japanese Patent Gazette No. 3537671), a lipolysis promoter containing Tussilago farfara as an active ingredient (for example, refer to Japanese Patent Gazette No. 3306750), and a lipolysis promoter containing an immature green fruit of Piper nigrum-L. or Piper longum-L. as an active ingredient (for example, refer to Japanese Patent Gazette No. 3645608). However, these lipolysis promoters cannot necessarily be said to have a sufficient effect, and some of them are concerned to cause side effects (for example, refer to Experimental Biology and Medicine (2204), Volume 229, pages 698 to 704).
With the foregoing background, there is required further development of a lipolysis promoter having a satisfying effect of preventing and ameliorating obesity, and capable of safe usage.
The present inventor et al. have discovered that plants of the genus Iresine of the family Amaranthaceae, Tipuana tipu, Bocconia pearcei, Argemone mexicana, and Ladenbergia magnifolia have an effect of promoting the degradation of neutral lipid in adipocytes, and brought the present invention to completion as a result of taking note of increased and enlarged adipocytes, which trigger obesity, and making diligent studies of various plants based on an assumption that the obesity can be prevented and ameliorated by promoting the degradation of the neutral fat in the adipocytes.
More specifically, the present invention is a lipolysis promoter containing one or more kinds of plant bodies and/or extracts therefrom selected from the group consisting of the plants of the genus Iresine of the family Amaranthaceae, the Tipuana tipu, the Bocconia pearcei, the Argemone mexicana, and the Ladenbergia magnifolia as the active ingredients. The present invention is also food-and-drink and feed containing the lipolysis promoter described above.
The lipolysis promoter and the food-and-drink and feed containing the same in accordance with the present invention have apparent lipolysis promoting activity in adipose tissue, and have a beneficial effect of preventing or ameliorating obesity, and reforming obese constitution.
Hereinafter, the present invention will be described in detail. While a description will be given of the lipolysis promoter, the food-and-drink and feed containing the same, and the process for producing the same, as well as its efficacy in accordance with the present invention, it is to be understood that the present invention is not intended to be limited to these examples.
The lipolysis promoter of the present invention may directly contain each plant as an active ingredient, but may contain a dried product, and further a powder-processed dry product as active ingredients. In addition, it may contain extracts from each plant as active ingredients. The plant extracts may be in water, various kinds of organic solvents or liquid extracts extracted with various kinds of organic solvents containing water, or may be substances in which the liquid extracts are evaporated to dryness by a normal drying process (for example, drying under reduced pressure, freeze-drying, and the like) or concentrated by a concentrating process. The kinds of organic solvents include ethanol, methanol, acetone, ethyl acetate, and hexane, but are not particularly limited. Furthermore, the plant extracts may be subjected to purification treatment such as deodorization and decolorization within the bounds of not affecting the effectiveness thereof, as necessary.
The lipolysis promoter of the present invention can be used in any form of an oral preparation, an external preparation, and the like. Accordingly, the lipolysis promoter of the present invention may be made into an pharmaceutical preparation adapted for ease of use as an internal medicine, for example, putting the plant extracts into granules with the use of an excipient, and the like, as appropriate. Moreover, the lipolysis promoter may locally reduce fat in the face or the abdomen by direct application to the above site, and thus may be used as lotion, gel, skin lotion, an ointment, a paste, a cataplasm, a plaster, a stick agent, a sheet agent, a bath agent, a tablet for body cleaning, and the like.
The compounding amount of the lipolysis promoter of the present invention may be selected from a wide range of options though being dependent on an adding form and a dosage form. For example, in the case of the external preparation, it is preferable that the compounding amount thereof be not less than 0.005% by weight (hereinafter, expressed simply by %), particularly 0.01 to 30% by weight in a composition on a solvent extraction dried product basis. In the case of the oral preparation, it is also preferable that the compounding amount thereof be 0.01 to 10 g, particularly 0.05 to 3 g per day for adults on the solvent extraction dried product basis.
Said lipolysis promoter is compounded in the food-and-drink of the present invention, in which compoundable food and drink is not particularly limited, and may be compounded in various forms of confectionery such as chewing gum, candies, and chocolate, health food, drinks, health drinks, flavoring, bread, and noodles. The food-and-drink in accordance with the present invention may take the form of health food, functional food, or food for specified health use which is given an obesity protective effect and an obesity ameliorating effect. The food-and-drink in accordance with the present invention can also be used in general diet. And, intake of such compounded food-and-drink as described above allows amelioration of obesity and improvement in lifestyle-related disease derived from the obesity. In this case, it is preferable that the compounding amount of the lipolysis promoter be not less than 0.0001% by weight, particularly 0.01 to 99% by weight in the food-and-drink on the solvent extraction dried product basis.
Said lipolysis promoter is compounded in the feed of the present invention, in which compoundable feed is not particularly limited, and may be compounded in pet food, dairy feed, feed for hog raising, poultry feed, and the like. In this case, it is preferable that the compounding amount of the lipolysis promoter be not less than 0.0001% by weight, particularly 0.01 to 99% by weight in the feed on the solvent extraction dried product basis. And, amelioration of obesity can be achieved when pets such as dogs or cats whose obesity is becoming a problem take such compounded feed as described above in particular, and the fat content of meat can be reduced when such compounded feed as described above is further compounded in the dairy feed, the feed for hog raising, the poultry feed, and the like.
The plants used in the present invention are all commercially available as herbs.
Plants of the genus Iresine of the family Amaranthaceae include Iresine angustifolia, Iresine argentata, Iresine calea, Iresine celosia, Iresine cassiniiformis, Iresine diffusa, Iresine herbstii, Iresine interrupta, Iresine lindenii, Iresine nigra, Iresine tricolor, Iresine viroid, and Iresine weberbaueri. While any of these plants can be used in the present invention, the Iresine weberbaueri is particularly preferable. Dried flowers, flower buds, or inflorescence of the Iresine weberbaueri are called Flor blanca, and are being used as herbs effective for diarrhea, vomiting, inflammation of the uterus, inflammation of the stomach, renautubular infection, and ulcers.
The Tipuana tipu is a tree of the family Lequminosae, called Tipa, and widely used as building materials or trees lining a street, whereas the bark and leaves thereof are used as herbs effective for rheumatism and hemorrhoids.
The Bocconia pearcei is a plant of the family Papaveraceae, and its seeds are called Yanala and used for eye irrigation, and the like.
The Argemone mexicana is also a plant of the family Papaveraceae, and its flowers are called Flor cardo santo.
The Ladenbergia magnifolia is a plant of the family Rubiaceae, and used for a tonic, a digestive agent, a hair-growth formula, prevention or treatment of malaria, treatment of a febrile disease, and the like. Its flowers are called Flor azahar.
It should be noted that in the lipolysis promoter of the present invention, the desired sites of the plants of the genus Iresine of the family Amaranthaceae to be used are flowers, flower buds, inflorescence, and the like, the desired sites of the Tipuana Tipu to be used are bark, branches, leaves and the like, the desired sites of the Bocconia pearcei to be used are seeds and the like, the desired sites of the Argemone mexicana to be used are flowers and the like, and the desired sites of the Ladenbergia magnifolia to be used are also flowers and the like.
Hereinafter, while the present invention will be described in more detail with Test examples, it is to be understood that the scope of the present invention is not intended to be limited by these examples.
The present test was carried out to obtain plant extracts from plant bodies.
1) Sample Under Test
Nine kinds of plants shown in Table 1 were used.
2) Test Method
To 10 g of a dried plant body, 100% ethanol, 50% ethanol or 100 ml of water was added, and extraction treatment was carried out under agitation at 70 C for 2 hours. The resultant extracts were filtered, and then subjected to vacuum concentration, followed by being freeze dried.
3) Test Result
Each extract yield is shown in Table 1.
Iresine
weberbaueri
Iresine diffusa
Iresine herbstill
Iresine lindenii
Iresine tricolor
Tipuana tipu
Bocconia pearcei
Argemone
mexicana
Ladenbergia
Magnifolia
The present test was carried out to examine the lipolysis promoting activity of plant extracts
1) Sample Under Test
The dried products of the 100% ethanol extracts, the 50% ethanol extracts and the water extracts, which were prepared in Test Example 1 were used.
2) Test Method
(1) Adipocyte Culture
MC3T3-G2/PA6 cells, mouse-derived preadipocytes, were seeded in a 24-well plate so as to achieve 5×104 cells/well, and incubated in a 10% fetal bovine serum (FBS) adding α-MEM culture medium in the presence of 5% CO2 at 37° C. Immediately before the plate becomes confluent, the culture medium was replaced by a 10% FBS α-MEM culture medium to which dexamethasone, 3-isobutyl-1-methylxanthine, and glucose were added to induce differentiation to adipocytes. The incubation was performed for 8 to 9 days after the induction, and the test was carried out after adipocyte maturation.
(2) Lipolysis Activity Measurement Method
After culture supernatant was discarded, and the well was cleaned with PBS (−), the sample and Dulbecco's Phoshate Buffered Saline containing 2% BSA and 4.5 g/L glucose were added, and incubated for 1 hour. It should be noted that the amount of the sample was adjusted so that the final concentration in this reaction system was 100 μg/ml.
After the incubation, the supernatant was sampled, and the release amount of glycerol, a lipolytic product, was measured using triglyceride E-Test Wako. The results are shown in Tables 2 to 4, provided that the release amount of the glycerol is a relative value with a control value as 100%.
Lipolysis promoting rate (%)=[A/B]×100
A: amount of released glycerol when adding the extracts
B: amount of released glycerol when adding no extracts
3) Test Results
The lipolysis promoting activity was determined on the basis of the lipolysis promoting rate shown in Tables 2 to 4, which was found from the measurements of the amount of the glycerol produced by lipolysis.
When the plant extracts under test were added, the lipolysis was apparently promoted compared with the control value.
Iresine weberbaueri
Iresine diffusa
Iresine herbstill
Iresine lindenii
Iresine tricolor
Tipuana tipu
Bocconia pearcei
Argemone mexicana
Ladenbergia magnifolia
Iresine weberbaueri
Iresine diffusa
Iresine herbstill
Iresine lindenii
Iresine tricolor
Tipuana tipu
Bocconia pearcei
Argemone mexicana
Ladenbergia magnifolia
Iresine weberbaueri
Iresine diffusa
Iresine herbstill
Iresine lindenii
Iresine tricolor
Tipuana tipu
Bocconia pearcei
Argemone mexicana
Ladenbergia magnifolia
The present test was carried out to examine the lipolysis promoting activity of plant extracts in adding the plant extracts at the same time.
1) Sample Under Test
The plant extracts prepared in Test example 1 were combined as shown in Table 5, and a mixture of each plant extract in equal proportions was used.
2) Test Method
(1) Adipocyte Culture
MC3T3-G2/PA6 cells, mouse-derived preadipocytes, were seeded in a 24-well plate so as to achieve 5×104 cells/well, and incubated in a 10% fetal bovine serum (FBS) adding α-MEM culture medium in the presence of 5% CO2 at 37° C. Immediately before the plate becomes confluent, the culture medium was replaced by a 10% FBS α-MEM culture medium to which dexamethasone, 3-isobutyl-1-methylxanthine, and glucose were added to induce differentiation to adipocytes. The incubation was performed for 8 to 9 days after the induction, and the test was carried out after adipocyte maturation.
(2) Lipolysis Activity Measurement Method
After culture supernatant was discarded, and the well was cleaned with PBS (−), the sample and Dulbecco's Phoshate Buffered Saline containing 2% BSA and 4.5 g/L glucose were added, and incubated for 1 hour. It should be noted that the amount of the sample was adjusted so that the final concentration in this reaction system was 100 μg/ml.
After the incubation, the supernatant was sampled, and the release amount of glycerol, a lipolytic product, was measured using triglyceride E-Test Wako. The result is shown in Table 5, provided that the release amount of the glycerol is a relative value with a control value as 100%.
Lipolysis promoting rate (%)=[A/B]×100
A: amount of released glycerol when adding the extracts
B: amount of released glycerol when adding no extracts
3) Test Result
As shown in Table 5, it was confirmed that even a mixture of two or more kinds of plant extracts had high lipolysis activity compared with the control value.
Iresine weberbaueri + Tipuana tipu
Iresine lindenii + Bocconia pearcei
Iresine herbstill + Argemone mexicana
Tipuana tipu + Ladenbergia magnifolia
Bocconia pearcei + Ladenbergia magnifolia
Iresine lindenii + Tipuana tipu + Bocconia pearcei
Iresine herbstill + Tipuana tipu + Argemone mexicana
Iresine weberbaueri + Bocconia pearcei + Ladenbergia +
magnifolia
Hereinafter, while the present invention will be described in more detail with Examples, it is to be understood that the scope of the present invention is not intended to be limited by these Examples.
Iresine weberbaueri 50% ethanol extract
Tipuana tipu water extract
Iresine weberbaueri 50% ethanol extract
Bocconia pearcei 50% ethanol extract
Tipuana tipu 50% ethanol extract
Bocconia pearcei powder
Iresine herbstii powder
Argemone mexicana powder
Iresine weberbaueri water extract
Argemone mexicana 50% ethanol extract
Iresine lindenii water extract
Ladenbergia magnifolia water extract
Bocconia pearcei water extract
Iresine weberbaueri powder
Argemone mexicana water extract
Argemone mexicana 50% ethanol extract
Ladenbergia magnifolia powder
Tipuana tipu 100% ethanol extract
Tipuana tipu 100% ethanol extract
Bocconia pearcei 50% ethanol extract
Ladenbergia magnifolia water extract
Iresine lindenii 50% ethanol extract
Iresine weberbaueri water extract
Tipuana tipu powder
Iresine herbstill 50% ethanol extract
Iresine weberbaueri water extract
Iresine herbstill 50% ethanol extract
Iresine weberbaueri water extract
Iresine herbstill water extract
| Number | Date | Country | Kind |
|---|---|---|---|
| 2006-072963 | Mar 2006 | JP | national |
| Number | Name | Date | Kind |
|---|---|---|---|
| 5698199 | Mori | Dec 1997 | A |
| 20030017997 | Yokota et al. | Jan 2003 | A1 |
| 20030036565 | Parkin et al. | Feb 2003 | A1 |
| 20050064049 | Mori | Mar 2005 | A1 |
| 20060134294 | McKee et al. | Jun 2006 | A1 |
| Number | Date | Country |
|---|---|---|
| 08-301780 | Nov 1996 | JP |
| 3306750 | Jul 2002 | JP |
| 2002-326947 | Nov 2002 | JP |
| 2004-035516 | Feb 2004 | JP |
| 3537671 | Jun 2004 | JP |
| Number | Date | Country | |
|---|---|---|---|
| 20070218108 A1 | Sep 2007 | US |
