U.S. patent application number 10/569970 was filed with the patent office on 2009-11-05 for dietetic composition.
Invention is credited to Michio Aitani, Hiromichi Murai, Tadashi Okada, Hiroshi Shimoda, Tomoko Sugishita, Emi Yamada.
Application Number | 20090274777 10/569970 |
Document ID | / |
Family ID | 34419547 |
Filed Date | 2009-11-05 |
United States Patent
Application |
20090274777 |
Kind Code |
A1 |
Shimoda; Hiroshi ; et
al. |
November 5, 2009 |
Dietetic composition
Abstract
(Problems) To provide a highly safe dietetic composition
originating in green coffee beans by which excellent dietetic
effects can be obtained and which contributes to the prevention and
treatment of life style-related diseases such as diabetes. (Means
for Solving Problems) A dietetic composition characterized by
comprising, as the active ingredient, a polar solvent extract of
defatted green coffee beans. It is preferable that the
above-described polar solvent extract is an extract obtained by
using water-containing ethanol, still preferably water-containing
ethanol having an ethanol concentration of from 40 to 90% (wt/wt).
It is preferable that the above-described defatted green coffee
beans are those obtained by extracting green coffee beans with
N-hexane to thereby separate oily components therefrom. It is
recommended to combine the above-described dietetic composition
with one or more members selected from among salacia extract,
evening primrose extract, sesamine and garcinia. This dietetic
composition is usable as a material for foods, drinks, drugs, or
skin preparations for external use.
Inventors: |
Shimoda; Hiroshi; (Aichi,
JP) ; Aitani; Michio; (Aichi, JP) ; Sugishita;
Tomoko; (Aichi, JP) ; Okada; Tadashi; (Aichi,
JP) ; Murai; Hiromichi; (Aichi, JP) ; Yamada;
Emi; (Aichi, JP) |
Correspondence
Address: |
CLARK & BRODY
1090 VERMONT AVENUE, NW, SUITE 250
WASHINGTON
DC
20005
US
|
Family ID: |
34419547 |
Appl. No.: |
10/569970 |
Filed: |
October 5, 2004 |
PCT Filed: |
October 5, 2004 |
PCT NO: |
PCT/JP2004/014622 |
371 Date: |
December 23, 2008 |
Current U.S.
Class: |
424/725 |
Current CPC
Class: |
A61P 43/00 20180101;
A61Q 19/06 20130101; A61K 36/74 20130101; A61K 8/9789 20170801;
A23F 5/02 20130101; A61Q 19/00 20130101; A61P 3/04 20180101 |
Class at
Publication: |
424/725 |
International
Class: |
A61K 36/74 20060101
A61K036/74; A61P 3/04 20060101 A61P003/04 |
Foreign Application Data
Date |
Code |
Application Number |
Oct 6, 2003 |
JP |
2003-346446 |
Claims
1. A dietetic composition characterized by comprising a polar
solvent extract as an active substance derived from the defatted
green coffee beans.
2. A dietetic composition of claim 1, therein the aforementioned
polar solvent extract is a hydroethanol extract.
3. A dietetic composition of claim 1, therein the aforementioned
polar solvent extract is a hydroethanol extract having an ethanol
concentration of 40 to 90% (wt/wt).
4. A dietetic composition of claim 1, therein the aforementioned
defatted green coffee bean is prepared by extracting and separating
the oil from the green coffee beans with N-hexane.
5. A dietetic composition described in claim 1, which is formed by
adding one or more substances from among salacia extract, evening
primrose extract, sesamin, and garcinia.
6. A food and drink comprising a dietetic composition as an active
substance described in claim 1.
7. A medicine comprising a dietetic composition as an active
substance described in claim 1.
8. A medicine for external use comprising a dietetic composition as
an active substance described in claim 1.
9. A composition for suppressing the fat absorption characterized
by comprising the green coffee bean extract as an active
substance.
10. A composition for suppressing the fat absorption described in
claim 9, therein the aforementioned green coffee bean extract is a
polar solvent extract derived from the defatted green coffee
beans,
11. A composition for suppressing the fat absorption described in
claim 10, therein the polar solvent extract is a hydroethanol
extract.
12. A composition for suppressing the fat absorption described in
claim 10, therein the polar solvent extract is a hydroethanol
extract having an ethanol concentration of 40 to 90% (wt/wt).
13. A composition for suppressing the fat absorption described in
claim 10, therein the defatted green coffee bean is prepared by
extracting and separating the oil from the green coffee bean with
N-hexane.
14. A food and drink comprising a composition as an active
substance for suppressing the fat absorption described in claim
9.
15. A medicine comprising a composition as an active substance for
suppressing the fat absorption described in claim 9.
16. A composition for inhibiting the pancreatic lipase activity
comprising the green coffee bean extract as an active
substance.
17. A composition for inhibiting the pancreatic lipase activity of
claim 9, therein the green coffee bean extract is a polar solvent
extract derived from the defatted green coffee bean.
18. A composition for inhibiting the pancreatic lipase activity of
claim 17, therein the polar solvent extract is a hydroethanol
extract.
19. A composition for inhibiting the pancreatic lipase activity of
claim 17, therein the polar solvent extract is a hydroethanol
extract having an ethanol concentration of 40 to 90% (wt/wt).
20. A composition for inhibiting the pancreatic lipase activity of
claim 17, therein the defatted green coffee bean is prepared by
extracting and separating the oil from the green coffee bean with
N-hexane.
21. A food and drink comprising a composition as an active
substance for inhibiting the pancreatic lipase activity described
in claim 16.
22. A medicine comprising a composition as an active substance for
inhibiting the pancreatic lipase activity described in claim
16.
23. A composition for promoting the carnitine palmitoyltransferase
activity characterized by comprising the green coffee bean extract
as an active substance.
24. A composition for promoting the carnitine palmitoyltransferase
activity of claim 23, therein the green coffee bean extract is a
polar solvent extract derived from the defatted green coffee
beans.
25. A composition for promoting the carnitine palmitoyltransferase
activity of claim 24, therein the polar solvent extract is a
hydroethanol extract.
26. A composition for promoting the carnitine palmitoyltransferase
activity of claim 24, therein the polar solvent extract is a
hydroethanol extract having an ethanol concentration of 40 to 90%
(wt/wt).
27. A composition for promoting the carnitine palmitoyltransferase
activity of claim 24, therein the defatted green coffee bean is
prepared by extracting and separating the oil from the green coffee
beans with N-hexane
28. A food and drink comprising a composition as an active
substance for promoting the carnitine palmitoyltransferase activity
described in claim 23.
29. A medicine comprising a composition as an active substance for
promoting the carnitine palmitoyltransferase activity described in
claim 23.
30. A composition for inhibiting the .alpha.-glucosidase activity
comprising the green coffee bean extract as an active
substance.
31. A composition for inhibiting the .alpha.-glucosidase activity
of claim 30, therein the green coffee bean extract is a polar
solvent extract derived from the defatted green coffee beans.
32. A composition for inhibiting the .alpha.-glucosidase activity
of claim 31, therein the polar solvent extract is a hydroethanol
extract.
33. A composition for inhibiting the .alpha.-glucosidase activity
of claim 31, therein the polar solvent extract is a hydroethanol
extract having an ethanol concentration of 40 to 90% (wt/wt).
34. A composition for inhibiting the .alpha.-glucosidase activity
of claim 31, therein the defatted green coffee bean is prepared by
extracting and separating the oil from the green coffee beans with
N-hexane.
35. A food and drink comprising a composition as an active
substance for inhibiting the .alpha.-glucosidase activity described
in claim 30.
36. A medicine comprising a composition as an active substance for
inhibiting the .alpha.-glucosidase activity described in claim 30.
Description
FIELD OF THE INVENTION
[0001] This invention relates to a dietetic composition derived
from green coffee beans and is applicable for ingredients of food
and drink, medicines, cosmetics, or the like.
[0002] Obesity is caused by excessive eating, insufficient exercise
or the like, and is considered as a risk factor for
lifestyle-related diseases typically seen in diabetic persons. The
total number of diabetic patients and people standing a good chance
of developing diabetes is increasing yearly.
[0003] As dietetic substances, capsaicin to enhance fat metabolism,
chitosan to reduce fat absorption, citrus aurantium to enhance
lipolysis and others are already known. The above dietetic
substances are now used for food or the like to support slimming
for the purpose of beautification such as cellulite reduction,
excess body water extraction, body fat reduction or the like.
However, some of the above dietetic substances are not sufficient
to achieve a dietary effect. Therefore, high-value added dietetic
substances for treatment or prevention of the lifestyle-related
diseases are now highly demanded in the market.
[0004] Prior arts concerning dietetic substances are disclosed in
the following publications:
Publication of application 1: JP2003-34636 Publication of
application 2: JP2002-308766 Nonpatent literature 1: Tholon L, et
al., An in vitro, ex vivo, and vivo demonstration of the lipolytic
effect slimming liposomes: An unexpected alpha(2)-adrenergic
antagonism. J. Cosmet. Sci. 53, 209-18 (2002)
DISCLOSURE OF THE INVENTION
Problems to be Resolved by the Invention
[0005] In such circumstance as described above, the inventors
researched contained components, contained amount, SOD mimicking
activity, and others regarding extracts derived from various
plants. It was found that green coffee beans contain plenty of
chlorogenic acids and caffeine. After conducting various
experiments, it was found that an extract derived from green coffee
beans, especially a polar solvent extract derived from defatted
green coffee beans contain dietetically effective components.
Furthermore, as a novel bioactivity of extract derived from green
coffee beans, fat absorption suppressing activity, carnitine
palmitoyltransferase activity promoting action in connection with
fat burning metabolism, and .alpha.-glucosidase activity inhibiting
activity in connection with control of blood sugar level were all
found and resulted in this invention.
[0006] This invention provides a highly safe dietetic composition,
fat absorption suppressive composition, pancreatic lipase activity
inhibiting composition, carnitine palmitoyltransferase activity
promoting composition and cl-glucosidase activity inhibiting
composition derived from green coffee beans.
[0007] Also, this invention provides a dietetic food and drink,
medicine, and dermatological preparation derived from green coffee
beans.
[0008] Furthermore, this invention provides
green-coffee-beans-derived food and drink and medicines comprising
a fat absorption inhibitory action, pancreatic lipase activity
inhibitory action, carnitine palmitoyltransferase promoting
activity or .alpha.-glucosidase activity inhibitory action.
(Invention 1)
[0009] A dietetic composition in this invention to resolve the
above problems is characterized by comprising a polar solvent
extract derived from defatted green coffee beans.
[0010] And, a dietetic composition in this invention is
characterized in that the aforementioned polar solvent extract is a
hydroethanol extract.
[0011] Also, a dietetic composition in this invention is
characterized in that the aforementioned solar solvent extract has
an ethanol concentration of 40 to 90% (wt/wt).
[0012] Moreover, a dietetic composition in this invention is
characterized in that the oil of the aforementioned green coffee
beans is extracted and separated with N-hexane.
[0013] Furthermore, a dietetic composition in this invention is
characterized in that one or more substances selected from among
salacia extract, evening primrose extract, sesamine, and garcia is
added to any of the aforementioned compositions.
[0014] Obesity is likely caused by excessive amounts of fat that
stay in the fat metabolic pathway in the body. (See FIG. 11)
Therefore, to prevent or treat the obesity caused by fat, the
following diet programs should be effectively done.
Suppression of fat absorption, Inhibition of fat accumulation
Enhancement of lipolysis, and Enhancement of fat burning
[0015] In this invention (Invention 1), an excellent and
highly-safe diet-promoting composition can be derived from green
coffee beans, and the effect on the above programs (1) to (4) can
be entirely obtained in a balanced manner. Thus, the weight gain by
taking fat into the body can be prevented, and the effective diet
can be done.
[0016] Referring now to the aforementioned Publications 1 and 2, a
medicine for improving lipid metabolism focused on a function of
chlorogenic acid contained in the coffee beans is disclosed in
Publication 1 and another different medicine for preventing and
improving lifestyle-related diseases is disclosed in Publication 2.
And it is disclosed in common that an extract derived from green
coffee beans contains an anti-obesity effect.
[0017] However, a dietetic composition in the present invention is
a highly-concentrated bioactive composition containing chlorogenic
acid derived from green coffee beans after extracting "defatted
green coffee beans" with the solar solvent, and is different from
the composition obtained simply by extracting the green coffee
beans. And, the polar solvent extract derived from the defatted
green coffee beans contains plenty of excellent diet-promoting
composition as well as chrologenic acid. Therefore, compared to the
extract derived from non-defatted green coffee beans, a good effect
of diet (weight-reducing effect) can be expected in the present
invention. (See Groups 3 and 4 in Chart 9, Example 5 of the
Publication 1). In the polar solvent extract derived from the green
coffee beans in the present invention, such an excellent
weigh-reducing effect can be more expected than in other cases
which are done by simply taking the chlorogenic acid into the body.
Such an excellent effect is a unique effect which can not be
predicted in the Publications 1, 2 and others.
(Inventions 2 and 3)
[0018] A composition for inhibiting fat absorption in this
invention (Invention 2) is characterized by comprising an extract
as an active substance derived from the green coffee beans.
[0019] Also, a composition for inhibiting fat absorption in this
invention (Invention 2) is characterized in that the aforementioned
extract derived from the green coffee beans is a solar solvent
extract derived from the defatted green coffee beans.
[0020] In addition, a composition for inhibiting fat absorption in
this invention (Invention 2) is characterized in that the
aforementioned solar solvent extract contains a hydroethanol
extract.
[0021] Moreover, a composition for inhibiting fat absorption in
this invention (Invention 2) is characterized in that the
aforementioned polar solvent extract is a hydroethanol having an
ethanol concentration of 40 to 90% (wt/wt).
[0022] Furthermore, a composition for inhibiting fat absorption in
this invention (Invention 2) is characterized in that the oil of
the aforementioned green coffee beans is extracted and separated
with N-hexane.
[0023] A composition for inhibiting a pancreatic lipase activity in
this invention (Invention 3) is characterized by comprising an
extract as an active substance derived from green coffee beans.
[0024] Also, a composition for inhibiting a pancreatic lipase
activity in this invention (Invention 3) is characterized in that
the aforementioned extract derived from the green coffee beans is a
solar solvent extract derived from the defatted green coffee
beans.
[0025] In addition, a composition for inhibiting a pancreatic
lipase activity in this invention (Invention 3) is characterized in
that the aforementioned solar solvent extract contains a
hydroethanol extract.
[0026] Moreover, a composition for inhibiting a pancreatic lipase
activity in this invention (Invention 2) is characterized in that
the aforementioned polar solvent extract is a hydroethanol having
an ethanol concentration of 40 to 90% (wt/wt).
[0027] Furthermore, a composition for inhibiting a pancreatic
lipase activity in this invention (Invention 3) is characterized in
that the oil content of the aforementioned green coffee beans is
extracted and separated with N-hexane.
[0028] As described above, when determining the diet effect
focusing on fat, normally one of the following effects on the fat
metabolism pathway is reviewed; (1) suppression of fat absorption,
(2) inhibition of fat accumulation (3) enhancement of lipolysis,
and (4) enhancement of fat burning. The aforementioned Publications
1 and 2 teach the lipolysis promoting effect indicated by measuring
the amount of triglycerol, and also suggests an anti-obesity effect
contained in the green coffee beans. However, it is little known
that the extract derived from the green coffee beans has a fat
absorption suppressive effect when the fat is taken into the
body.
[0029] In the experiments conducted by the inventors, bioactivity
of the extract derived from the green coffee beans was tested in
the fat absorption system of the lipolysis, and then the pancreatic
lipase inhibitory action relating to the fat absorption suppressive
action and fat absorption metabolism was found. Thus, in this
invention, the diet effect can be improved in terms of the fat
absorption suppressive effect by the extract derived from the green
coffee beans (Invention 2) and the pancreatic lipase inhibitory
effect (Invention 3). In other words, a dietetic composition
including the extract, such as active substances for suppressing
fat absorption or inhibiting pancreatic lipase action, derived from
the green coffee beans can be provided in this invention. And the
polar solvent extract (including ethanol extract and N-hexane
defatted substance) derived from the defatted green coffee beans
described in the above Inventions 2 and 3 can be used for the
active substances for effect.
(Invention 4)
[0030] A composition for promoting a carnitine palmitoyltransferase
activity in this invention (Invention 4) is characterized by
comprising an extract as an active substance derived from green
coffee beans.
[0031] Also, a composition for promoting a carnitine
palmitoyltransferase activity in this invention (Invention 4) is
characterized in that the aforementioned extract derived from the
green coffee beans is a solar solvent extract derived from the
defatted green coffee beans.
[0032] In addition, a composition for promoting a carnitine
palmitoyltransferase activity in this invention (Invention 4) is
characterized in that the aforementioned solar solvent extract
contains a hydroethanol extract.
[0033] Moreover, a composition for promoting a carnitine
palmitoyltransferase activity in this invention (Invention 4) is
characterized in that the aforementioned polar solvent extract is a
hydroethanol having an ethanol concentration of 40 to 90%
(wt/wt).
[0034] Furthermore, a composition for promoting a carnitine
palmitoyltransferase activity in this invention (Invention 4) is
characterized in that the oil of the aforementioned green coffee
beans is extracted and separated with N-hexane.
[0035] A brown adipose tissue related to the fat metabolism is one
of fat-burning tissues which can convert energy to heat and burn it
off. It is known that heat production is done on a membrane of the
brown adipose tissue mitochondria and a special uncoupling protein
(UCP-1) functions the heat conversion.
[0036] It is reported that the caffeine contained in the green
coffee beans has a promoting effect of the UCP-1 expression of the
brown adipose tissue of diabetic mice. As a result, it is
contemplated that the green coffee beans containing caffeine
function to burn and consume the fat producing heat.
[0037] On the other hand, the fatty acid degraded and separated
from the adipose tissue is partially delivered into the liver and
metabolized by .beta.-oxidation in the mitochondria of the hepatic
cell. When the fatty acid is delivered into the mitochondria, the
carnitine and a transfer enzyme like carnitine palmitoyltransferase
(CPT) function and both are on the rate-limiting step of the
.beta.-oxidation.
[0038] The Publication 1 teaches that chrologenic acids contained
in the green coffee beans activate a gene transcription of the
enzyme which is important to the fatty acid metabolism of the
.beta.-oxidation. However, it does not teach any effects on the
activity of the enzyme itself by the chlorogenic acids.
[0039] In the experiments conducted by the inventors, the
bioactivity of the extract derived from the green coffee beans was
tested in the fat burning system of the fat metabolism, and a
stimulatory effect of carnitine palmitoyltransferase (CPT) relating
to the .beta.-oxidation has been finally found. Thus, in this
invention (Invention 4), the diet effect can be improved in terms
of the fat burning promoting effect by activating the carnitine
palmitoyltransferase (CPT). In other words, the dietetic
composition including extracts such as active substances for
promoting the carnitine palmitoyltransferase that are derived from
the green coffee beans can be provided in this invention. And as an
active substance for promoting the carnitine palmitoyltransferase
(CPT), the polar solvent extract (including the ethanol extract and
the N-hexane defatted substance) derived from the defatted green
coffee beans described in the above Invention 4 can be used for the
active substances for effect.
(Invention 5)
[0040] A composition for inhibiting an .alpha.-glucosidase activity
in this invention (Invention 5) is characterized by comprising the
extract as the active substance derived from the aforementioned
green coffee beans.
[0041] Also, a composition for inhibiting the .alpha.-glucosidase
activity in this invention (Invention 5) is characterized in that
the aforementioned extract derived from the green coffee beans is a
solar solvent extract derived from the defatted green coffee
beans.
[0042] In addition, a composition for inhibiting the
.alpha.-glucosidase activity in this invention (Invention 5) is
characterized in that the aforementioned solar solvent extract
contains a hydroethanol extract.
[0043] Moreover, a composition for promoting the
.alpha.-glucosidase activity in this invention (Invention 5) is
characterized in that the aforementioned polar solvent extract is a
hydroethanol having an ethanol concentration of 40 to 90%
(wt/wt).
[0044] Furthermore, a composition for inhibiting the
.alpha.-glucosidase activity in this invention (Invention 5) is
characterized in that the oil of the aforementioned green coffee
beans is extracted and separated with N-hexane.
[0045] In the test of the bioactivity of glycolytic enzyme, such as
.alpha.-amylase, .alpha.-glucosidase or the like, derived from the
green coffee beans, it was found that the extract derived from the
green coffee beans has an excellent inhibitory effect especially in
regard to the .alpha.-glucosidase. Thus, in this invention
(Invention 5), .alpha.-glucosidase enzyme activity is inhibited so
that postprandial elevation of blood glucose levels can be
suppressed and the diabetes and obesity can be finally prevented.
In other words, this invention provides an anti-diabetic
composition or dietetic composition containing an extract derived
from the green coffee beans, as an active substance for inhibiting
.alpha.-glucosidase activity. And as an active substance for
inhibiting .alpha.-glucosidase activity, the polar solvent extract
(including ethanol extract and N-hexane defatted substance) which
is derived from the defatted green coffee beans described in the
above Invention 5 can be used for the active substances for
effects.
BRIEF DESCRIPTION OF THE DRAWINGS
[0046] FIG. 1 is a graph showing an effect on the weight gain of
mice which continuously take an extract derived from the green
coffee beans and substances derived from coffee beans (caffeine and
chlorogenic acid).
[0047] FIG. 2 is a graph showing an effect on the visceral fat of
mice which continuously take an extract derived from the green
coffee beans and substances derived from coffee beans (caffeine and
chrologenic acid).
[0048] FIG. 3 is a graph showing an effect on the weight gain of
mice which continuously take an extract derived from the green
coffee beans and roasted coffee beans.
[0049] FIG. 4 is a graph showing an effect of the extract derived
from the green coffee beans on the triglyceride in the blood when
olive oil is taken into the body.
[0050] FIG. 5 is a graph showing the pancreatic lipase inhibitory
activity of the extract derived from the green coffee beans and
substances derived from coffee beans (caffeine and chlorogenic
acid).
[0051] FIG. 6 is a graph showing the effect on a 3T3-L1 adipocyte
differentiation of the extract derived from the green coffee beans
and substances derived from coffee beans (caffeine and chlorogenic
acid).
[0052] FIG. 7 is a graph showing the effect on the hepatic fatty of
the mice which continuously takes the extract derived from the
green coffee beans and substances derived from coffee beans
(caffeine and chlorogenic acid).
[0053] FIG. 8 is a graph showing the effect of the extract derived
from the green coffee beans, substances derived from coffee beans
(caffeine and chlorogenic acid) and lipolytic substances on the
glycerol release of the epididymal fat.
[0054] FIG. 9 is a graph showing the effect of the extract derived
from the green coffee beans, substances derived from coffee beans
(caffeine and chlorogenic acid) and the existing dietetic materials
on the triglyceride in the blood of the mice.
[0055] FIG. 10 is a graph showing the effect of the extract derived
from the green coffee beans on promoting activity of the hepatic
mitochondrial fraction CPT.
[0056] FIG. 11 is an illustration indicating the diet effect in the
fat metabolic pathway.
[0057] FIG. 12 is a graph showing the suppressive effect of the
extract derived from the green coffee beans on the elevation of
blood glucose levels when glucose or sucrose is taken into the
body.
DETAILED DESCRIPTION OF THE PREFERRED EXAMPLES
[0058] An example of the dietetic composition in this invention
(Invention 1) is here described. Invention 1 is applicable
similarly with Invention 2 (a composition for suppressing fat
absorption), Invention 3 (a composition for inhibiting pancreatic
lipase activity), Invention 4 (a composition for promoting
carnitine palmitoyltransferase activity) and Invention 5 (a
composition for inhibiting .alpha.-glucosidase activity).
[0059] In this invention, the green coffee beans, which are used as
a basic ingredient to produce a dietetic composition, are the same
used to brew coffee. The coffee beans used brewing coffee are
normally roasted for approx. 15 minutes at the maximum temperature
of 200 to 215.degree. C. However, green coffee beans not roasted
coffee beans are used in this invention.
[0060] The coffee tree, a rubiaceous evergreen shrub of Ethiopian
origin produces the ingredient used in this invention. Normally,
each coffee berry has two beans (seeds) inside. Each bean (seed) is
of a hemispheric shape and has a deep vallecula on its flat
surface. The Arabian coffee tree (Coffea Arabica L.), the Congolese
coffee tree (C. robusta Linden), Land the Liberian coffee tree (C.
liberica Bull), or others are widely cultivated. In this invention,
the type of coffee bean or where it is grown (rabica, robusta, or
the like) is not specified.
[0061] To prepare the coffee beans for beverage use, there are two
methods used: the dry process and the wet process. In the dry
process, the coffee berries are first dried, then the dried flesh
and outer covering of the coffee beans are removed. In the wet
process, the coffee berries are first soaked in water, then the
flesh and outer covering of the coffee beans are fermented and
dried, they are simply removed. In this invention, either on of the
above methods can be used.
[0062] Defatted green coffee beans are preferably used for
extracting the ingredients needed for the inventive dietetic
composition used in this invention. After removing the oil from the
green coffee beans, the dietetically functioning substances can
easily be extracted with solvent. To defat the green coffee beans,
it is preferable to first compress the green coffee beans to remove
the oil. Then, to extract and separate the remaining oil from the
compressed cake to use the defatting solvent, lipophilic organic
solvent. Also, when the aforementioned Inventions 2 to 5 are put
into practice, non-defatted green coffee beans can be used. For
example, it is also possible to crush the green coffee beans and to
extract the active substances from the crushed beans with
solvent.
[0063] An N-hexane, acetone or the like can preferably be used for
the defatting solvent. If the N-hexane is especially used as a
defatting solvent, the extracted oil can be used for an edible oil,
and the extract derived from the defatted green coffee beans can
easily be used for food materials.
[0064] To extract the dietetically functioning ingredients from the
defatted green coffee beans, solar solvents such as water,
methanol, ethanol, isopropyl alcohol, 1,3-butylene glycol, ethylene
glycol, propylene glycol, glycerin, ethyl acetate, or the like can
be used. Two or more solvents described above can be mixed.
[0065] If the water and ethanol are preferably mixed and used as an
extracting solvent, the active substances are efficiently
extracted. Particularly, the action of the active substance is not
easily lowered by the hydroethanol when being extracted. Thus,
hydroethanol is a preferable extracting solvent since the extract
can safely be used for food. The type of water used for extracting
process is not specified. Tap water, distilled water, mineral
water, ionized alkaline water, deep water or the like can be used.
Also, the active substances can be extracted by using a non-polar
solvent (acetone or the like when practicing the above Inventions 2
to 5.
[0066] If the hydroethanol is used for extracting the dietetically
functioning ingredients from the defatted coffee beans, the
extraction temperature should be from 20 to 80.degree. C.,
preferably from 40 to 50.degree. C. If the extraction temperature
is too low, the active substances will not easily be extracted, and
if the temperature is too high, the activity of the active
substances will easily be reduced.
[0067] The extracting solvent is a hydroethanol which has an
ethanol concentration of 40 to 90% (wt/wt), preferably the
concentration of 60 to 80% (wt/wt). The reason why the ethanol
concentration should be 40% (wt/wt) or more is that if the ethanol
content is too low, the active substance will not sufficiently be
extracted. Also the reason why the ethanol concentration should be
90% (wt/wt) or less is that if the ethanol content is too high, the
remaining oil of the defatted green coffee beans will easily be
leached into the hydroethanol. It is preferable to repeat the
hydroethanol extractions, with changes in the ethanol concentration
as needed, so that the content rate of the active substance will
increase.
[0068] To extract the dietetically functioning ingredients,
continuous extraction, soaking extraction, countercurrent
extraction, supercritical extraction, or the like can also be used,
and any equipment can be sued at room temperature or under reflux
heating.
[0069] A more specific way of extraction is herein described.
Firstly, put an ingredient (green coffee beans) into the processing
tank which is filled with extracting solvent, and stir the
ingredient. For instance, in the case that the hydroethanol is used
as an extracting solvent, the extracting solvent should be used in
approx. 5 to 100 times its volume of the ingredient (weight ratio),
and the extraction should be done for approx. 30 minutes to 2
hours. After the active substance is eluted into the extracting
solvent, the liquid extract is obtained by filtering and reducing
the residue. After that, the liquid extract is diluted,
concentrated, dried, purified, or processed in the other usual
ways, and the inventive dietetic composition can finally be
obtained.
[0070] Also, the active carbon treatment, the resin absorption
treatment, the ion-exchange resin method, the liquid-liquid
countercurrent distribution method, or the like can be used as a
purification method. However, a large quantity of the dietetic
composition is not added to the food or the like. Therefore,
unpurified composition can also be used.
[0071] According to the research conducted by the inventors, the
polar solvent extract of the defatted green coffee beans contains a
comparatively large amount of chlorogenic acids and caffeine.
Especially the dietetically-functioning chlorogenic acids are
concentrated therein. More specifically, the extracts containing
chlorogenic acid in concentration of 20 wt % or more, and the
extract containing chlorogenic acids (chlorogenic acid, ferulic
acid, p-coumaric acid, coffeic acid or the like) in concentration
of 45 wt % or more can greatly improve the effect of the dieting
method.
[0072] The inventive dietetic composition can be used as an
ingredient for any food and drink such as, confectionary (chewing
gums, candies, caramels, chocolates, cookies, jellies, gummies,
tablet shaped sweets or the like), noodles (Japanese buckwheat
noodle called Soba, Japanese wheat noodle called Udon, Chinese
noodle called Ramen or the like), dairy food (milk, ice cream,
yoghurt, or the like), seasoning (fermented bean paste called Miso,
Soy sauce called Shoyu, or the like), soups, drinks (uice, coffee,
black tea, green tea, carbonated drink, or the like).
[0073] According to the types of the above foods and drinks, the
following ingredients can be added:
[0074] Glucose, fructose, sucrose, maltose, sorbitol, stevioside,
corn syrup, lactose, citric acid, tartaric acid, malic acid,
saccinic acid, lactic acid, L-ascorbic acid, dl-.alpha.-tocopherol,
sodium erythorbate, glycerin, propylene glycol, glycerin fatty acid
ester, polyglycerol fatty acid ester, sucrose fatty acid ester,
sorbitan fatty acid ester, propylene glycol fatty acid ester,
Arabian gum, carrageenan, casein, gelatin, pectine, agar-agar
(gelatin made from seaweed), vitamin B family, nicotinic-acid
amide, pantothenate acid calcium, amino acids, calcium salts,
pigment, aroma chemicals, preservatives, or the like.
[0075] A more specific use of the extracting method is herein
described. Firstly, spray-dry or freeze-dry the polar solvent
extract derived from the defatted green coffee beans with powdered
cellulose, then make it powder, granule, tablet, or liquid to
easily use with food and drink (ready-to eat meals or the like).
Also, it is possible to solve the polar solvent extract derived
from the defatted coffee beans into, for instance, oil and fat,
ethanol, glycerin, or a mixture of these substances, and to use
such a liquid for dry food or drink. Also it is possible to make it
into powder or granule by mixing it with a binder such as Arabian
gum, dextrin, or the like to add to dry food or drink.
[0076] The total amount of the active substance in the inventive
dietetic composition which is added to the food and drink is
preferably 1 to 20 wt % or less, since the major objective of this
invention is disease prevention or health maintenance.
[0077] The inventive dietetic composition can be used as the raw
material of medicines (including drugs and quasi-drugs). The
inventive dietetic composition can be appropriately mixed with raw
materials for drug formulations, for instance, vehicles (glucose,
sucrose, white soft sugar, sodium chloride, starch, calcium
carbonate, kaolin, crystalline cellulose, cacao oil, hydrogenated
vegetable oil, talc, or the like), binders (distilled water, normal
saline solution, ethanol in water, ethanolic solution, simple
syrup, dextrose in water, starch solution, gelatin solution,
carboxymethyl cellulose, potassium phosphate, polyvinyl
pyrrolidone, or the like), disintegrating agents (alginate sodium,
agar-agar, sodium hydrogen carbonate, sodium lauryl sulphate,
stearic acid monoglyceride, starch, lactose, powdered aracia,
gelatin, ethanol, or the like), suppressive agents for
disintegration (white soft sugar, stearin, cacao oil, hydrogenated
oil, or the like), absorption promoters (quaternary ammonium base,
sodium lauryl sulphate, or the like), adsorbents (glycerin, starch,
lactose, kaolin, bentonite, silic acid, or the like), lubricant
agents (purified talc, stearate, polyethyleneglycol, or the
like)
[0078] The inventive dietetic composition can be orally
administered in the form of tablets, pills, soft or hard capsules,
subtle granules, powders, granules, liquids, or the like. However,
it can also be parenterally administered in the form of solution or
together with a dispersant, a suspending agent, a stabilizer, or
the like by local tissue administration, intradermal injection,
subcutaneous injection, intramuscular injection, intravenous
injection, or the like. Also, it can be administered in suppository
form.
[0079] The applied dose can be adjusted according to the method of
administration, the condition of the disease, the age of the
patient, or the like. However, adults can normally take approx. 0.5
to 5,000 mg of an active substance per day, while children can take
0.5 to 3,000 mg per day.
[0080] The compounding ratio of the dietetic composition can be
adjusted according to the mode of administration. When the dietetic
composition is orally administered or mucosally administered, the
applied dose is preferably 0.3 to 15.0 wt %, and when the dietetic
composition is parenterally administered, the dose is preferably
0.01 to 10 wt %. The dose varies depending on the conditions.
Therefore, the dose which is less than the above-stated amount may
be sufficient, or a greater amount may sometimes be needed.
[0081] A dietetic composition in this invention contains
chlorogenic acid and caffeine. There is a report that a combined
formulation of caffeine and some other ingredients gives good
results for the slimming therapy (non-patent literature 1). From
this result, it can be reasonably expected that the inventive
dietetic composition can be used as a drug for external skin use
(including cosmetics, drugs, and quasi-drugs) and effectively works
in a partial-targeted body slimming program, or to remove cellulite
from the body.
[0082] The inventive dietetic composition can be mixed with
cosmetics such as emulsions, soaps, facial cleansers, bath agents,
creams, skin lotions, colognes, shaving creams, shaving lotion,
beauty oils, tanning lotions, sunscreen lotions, face powders,
foundations, perfumes, facial masks, nail creams, nail enamels,
nail-polish removers, eyebrow pencils, blushers, eye creams, eye
shadows, mascaras, eye liners, Lip sticks, lip creams, shampoos,
hair conditioners, hairdyes, dispersion liquids, cleansing
preparations, or the like.
[0083] Also, the inventive dietetic composition can be mixed with
the drugs and quasi-drugs such as ointments, cream pharmaceuticals,
liquids for external use or the like.
[0084] Within the functional range of the inventive dietetic
composition, the above items for external use can also be mixed
with the ingredients of cosmetics, quasi-drugs, or the like. Those
ingredients include, for example, oil, higher alcohol, fatty acid,
ultraviolet absorber, powder, pigment, surface active agent,
polyhydric alcohol and sugar, polymer, biologically active
ingredient, solvents, antioxidant, aroma chemical (perfume
material), antiseptic. However, those ingredients usable in the
present invention are not limited to these examples.
Specific Examples of Oil
[0085] (Ester-type oil phase ingredient) Triglyceryl
2-ethylhexanoate, cetyl 2-ethylhexanoate, isopropyl myristate,
butyl myristate, isopropyl palmitate, ethyl stearate, octyl
palmitate, isocetyl isostearate, butyl stearate, butyl myristate,
ethyl linoleate, isopropyl linoleate, ethyl oleate, isocetyl
myristate, isostearyl myristate, isostearyl palmitate, octyldodecyl
myristate, isocetyl isostearate, diethyl sebacate, diisopropyl
adipate, isoarachyl neopentanoate, caprylic-capric acid
triglyceride, trimethylolpropane tri-2-ethylhexanoate,
trimethylolpropane triisostearate, pentaerythritol
tetra-2-ethylhexanoate, cetyl caprylate, decyl laurate, hexyl
laurate, decyl myristate, myristyl myristate, cetyl myristate,
stearyl stearate, decyl oleate, cetyl ricinoleate, isostearyl
laurate, isotridecyl myristate, isocetyl myristate, isostearyl
myristate, isocetyl palmitate, isostearyl palmitate, octyl
stearate, isocetyl stearate, isodecyl oleate, octyldodecyl oleate,
octyldodecyl linoleate, isopropyl isostearate, cetostearyl
2-ethylhexanoate, stearyl 2-ethylhexanoate, hexyl isostearate,
ethylene glycol dioctanoate, ethylene glycol dioleate, propylene
glycol dicaprate, propylene glycol di(caprylate/caprate), propylene
glycol dicaprylate, neopentyl glycol dicaprate, neopentyl glycol
dioctanoate, glyceryl tricaprylate, glyceryl triundecylate,
glyceryl triisopalmitate, glyceryl triisostearate, octyldodecyl
neopentanoate, isostearyl octanoate, octyl isononanoate, hexyldecyl
neodecanoate, octyldodecyl neodecanoate, isocetyl isostearate,
isostearyl isostearate, octyldecyl isostearate, polyglycerin
oleate, polyglycerin isostearate, dipropyl carbonate, dialkyl
carbonate (C12-18), triisocetyl citrate, triisoarachyl citrate,
triisooctyl citrate, lauryl lactate, myristyl lactate, cetyl
lactate, octyldecyl lactate, triethyl citrate, acetyltriethyl
citrate, acet-yltributyl citrate-trioctyl citrate, diisostearyl
malate, 2-ethylhexyl hydroxystearate, 2-ethylhexyl succinate,
diisobutyl adipate, diisopropyl sebacate, dioctyl sebacate,
cholesteryl stearate, cholesteryl isostearate, cholesteryl
hydroxystearate, cholesteryl oleate, dihydrocholesteryl oleate,
phytosteryl isostearate, phytosteryl oleate, isocetyl
12-stearoylhydroxystearate, stearyl 12-stearoylhydroxystearate and
isostearyl 12-stearoylhydroxystearate.
[0086] (Hydrocarbon-type oil phase ingredient) Squalane, liquid
paraffin, .alpha.-olefin oligomer, isoparaffin, ceresin, paraffin,
liquid isoparaffin, polybutene, microcrystalline wax and
vaseline.
[0087] (Animal and plant oil, hardened oil thereof, and wax of
natural origin) Animal oils and hardened oils thereof, such as beef
tallow, hardened beef tallow, lard, hardened lard, horse oil,
hardened horse oil, mink oil, orange roughy oil, fish oil, hardened
fish oil and egg yolk oil; plant oils and hardened oils thereof
such as avocado oil, almond oil, olive oil, cacao oil, apricot
kernel oil, kukui nut oil, sesame oil, wheat germ oil, rice germ
oil, rice bran oil, safflower oil, shea butter, soybean oil,
evening primrose oil, perilla oil, tea seed oil, tsubaki oil
(camellia japonica oil), corn oil, rapeseed oil, hardened rapeseed
oil, palm kernel oil, hardened palm kernel oil, palm oil, hardened
palm oil, peanut oil, hardened peanut oil, castor oil, hydrogenated
castor oil, sunflower oil, grape seed oil, jojoba oil, hardened
jojoba oil, macadamia nut oil, meadowfoam seed oil, cottonseed oil,
hardened cottonseed oil, coconut oil, hardened coconut oil; and
waxes such as beeswax, high acid number beeswax, lanolin, reduced
lanolin, hardened lanolin, liquid lanolin, carnauba wax and montan
wax.
[0088] (Silicone-type oil phase ingredient) Dimethylpolysiloxane,
methylphenylpolysiloxane, methylcyclopolysiloxane,
octamethylpolysiloxane, decamethylpolysiloxane,
dodecamethylcyclosiloxane, methylhydrogenpolysiloxane,
polyether-modified organopolysiloxane,
dimethylsiloxanemethylcetyloxysiloxane copolymer,
dimethylsiloxane-methylstearoxysiloxane copolymer, alkyl-modified
organopolysiloxane, terminal-modified organopolysiloxane,
amino-modified silicone oil, amino-modified organopolysiloxane,
dimethiconol, silicone gel, acryl silicone, trimethylsiloxysilicic
acid and silicone RTV rubber.
[0089] (Fluorine-type oil phase ingredient) Perfluoropolyether,
fluorine-modified organopolysiloxane, fluorinated pitch,
fluorocarbon, fluoroalcohol and
fluoroalkyl-polyoxyalkylene-comodified organopolysiloxane.
(2) Specific Examples of Higher Alcohol
[0090] Lauryl alcohol, myristyl alcohol, cetyl alcohol, stearyl
alcohol, isostearyl alcohol, oleyl alcohol, behenyl alcohol,
2-ethylhexanol, hexadecyl alcohol and octyl dodecanol.
(3) Specific Examples of Fatty Acid
[0091] Caprylic acid, capric acid, undecylenic acid, lauric acid,
myristic acid, palmitic acid, palmitoleic acid, stearic acid,
isostearic acid, oleic acid, linoleic acid, linolenic acid, arachic
acid, arachidonic acid, behenic acid, erucic acid and
2-ethylhexanoic acid.
(4) Specific Examples of Ultraviolet Absorber
[0092] Para-aminobenzoic acid, amyl para-aminobenzoate,
ethyldihydroxypropyl para-aminobenzoate, glyceryl
para-aminobenzoate, ethyl para-aminobenzoate, octyl
para-aminobenzoate, octyldimethyl para-aminobenzoate, ethylene
glycol salicylate, octyl salicylate, triethanolamine salicylate,
phenyl salicylate, butylphenyl salicylate, benzyl salicylate,
homomethyl salicylate, benzyl cinnamate, octyl
para-methoxycinnamate, 2-ethylhexyl para-methoxycinnamate, glyceryl
mono-2-ethyl hexanoate di-para-methoxycinnamate, isopropyl
para-methoxycinnamate, diethanolamine para-methoxyhydrocinnamate,
diisopropyl diisopropylcinnamic acid ester mixture, urocanic acid,
ethyl urocanate, hydroxymethoxybenzophenone,
hydroxymethoxybenzophenone sulfonic acid and a salt thereof,
dihydroxymethoxybenzophenone, sodium
dihydroxymethoxybenzophenonedisulfonate, dihydroxybenzophenone,
dihydroxydimethoxybenzophenone, hydroxyoctoxybenzophenone,
tetrahydroxybenzophenone, butylmethoxydibenzoylmethane,
2,4,6-trianilino-p-(carbo-2-ethylhexyl-1-oxy)-1,3,5-triazine,
2-(2-hydroxy-5-methylphenyl)benzotriazole, methyl-0-aminobenzoate,
2-ethylhexyl-2-cyano-3,3-diphenylacrylate, phenylbenzimidazole
sulfuric acid, 3-(4-methylbenzylidene) camphor,
isopropyldibenzoylmethane,
4-(3,4-dimethoxyphenylmethylene)-2,5-doxy-1-imidazolidinepropionate,
and polymer derivatives and silane derivatives thereof.
(5) Specific Examples of Powder and Pigment
[0093] Pigments such as Food Red 104, Food Red 201, Food Yellow 4,
Food Blue 1 and Food Black 401; lake pigments such as Food Yellow 4
AL lake and Food Yellow 203 BA lake; polymers such as nylon powder,
silk powder, urethane powder, Teflon.RTM. powder, silicone powder,
polymethyl methacrylate powder, cellulose powder, starch, silicone
elastomer spherical powder and polyethylene powder; color pigments
such as yellow iron oxide, red iron oxide, black iron oxide,
chromium oxide, carbon black, ultramarine and iron blue; white
pigments such as zinc oxide, titanium oxide and cerium oxide;
extender pigments such as talc, mica, sericite, kaolin and plate
barium sulfate; pearl pigments such as mica titanium; metal salts
such as barium sulfate, calcium carbonate, magnesium carbonate,
aluminum silicate and magnesium silicate; inorganic powders such as
silica and alumina; metal soaps such as aluminum stearate,
magnesium stearate, zinc palmitate, zinc myristate, magnesium
myristate, zinc laurate and zinc undecylenate; bentonite; smectite;
and boron nitride.
[0094] The shape (e.g., sphere, bar, needle, plate, amorphous,
scale, spindle) and the particle size of these powders are not
particularly limited.
[0095] These powders may or may not be previously surface-treated
by a conventionally known surface treatment such as fluorine
compound treatment, silicone treatment, silicone resin treatment,
pendant treatment, saline coupling agent treatment, titanium
coupling agent treatment, lubricant treatment, N-acylated lysine
treatment, polyacrylic acid treatment, metal soap treatment, amino
acid treatment, lecithin treatment, inorganic compound treatment,
plasma treatment and mechanochemical treatment.
(6) Specific Examples of Surfactant
[0096] Anionic surfactant: Fatty acid soap, a-acyl sulfonate, alkyl
sulfonate, alkylallyl sulfonate, alkylnaphthalene sulfonate, alkyl
sulfate, POE alkyl ether sulfate, alkylamide sulfate, alkyl
phosphate, POE alkyl phosphate, alkylamide phosphate, alkyloylalkyl
taurine salt, N-acylamino acid salt, POE alkyl ether carbonate,
alkyl sulfosuccinate, sodium alkylsulfoacetate, acylated hydrolyzed
collagen peptide salt and perfluoroalkylphosphoric acid ester.
[0097] Cationic surfactant: Alkyltrimethylammonium chloride,
stearyltrimethylammonium chloride, stearyltrimethylammonium
bromide, cetostearyltrimethylammonium chloride,
distearyldimethylammonium chloride, stearyldimethylbenzylammonium
chloride, behenyltrimethylammonium bromide, benzalkonium chloride,
behenic acid amidopropyldimethyl hydroxypropylammonium chloride,
diethylaminoethylamide stearate, dimethylaminoethylamide stearate,
dimethylaminopropylamide stearate and lanolin derivative quaternary
ammonium salt.
[0098] (Amphoteric surfactant) Carboxybetaine type, amidobetaine
type, sulfobetaine type, hydroxysulfobetaine type,
amidosulfobetaine type, phosphobetaine type, aminocarboxylate type,
imidazoline derivative type and amidoamine type.
[0099] (Nonionic surfactant) Propylene glycol fatty acid ester,
glycerin fatty acid ester, polyglycerin fatty acid ester, sorbitan
fatty acid ester, POE sorbitan fatty acid ester, POE sorbitol fatty
acid ester, POE glycerin fatty acid ester, POE alkyl ether, POE
fatty acid ester, POE hydrogenated castor oil, POE castor oil,
POE-POP copolymer, POE-POP alkyl ether, polyether-modified silicone
lauric acid alkanolamide, alkylamine oxide and hydrogenated soybean
phospholipid.
[0100] (Natural-type surfactant) Lecithin, saponin and sugar-type
surfactant.
(7) Specific Examples of Polyhydric Alcohol and Sugar
[0101] Ethylene glycol, diethylene glycol, polyethylene glycol,
propylene glycol, dipropylene glycol, polypropylene glycol,
glycerin, diglycerin, polyglycerin, 3-methyl-1,3-butanediol,
1,3-butylene glycol, sorbitol, mannitol, raffinose, erythritol,
glucose, sucrose, fruit sugar, xylitol, lactose, maltose, maltitol,
trehalose, alkylated trehalose, mixed isomerized sugar, sulfated
trehalose and pullulan. Chemically modified products thereof can
also be used.
(8) Specific Examples of Polymer Compound
[0102] Anionic polymer compounds such as acrylic acid
ester/methacrylic acid ester copolymer (PLUS-SIZE, produced by
Sogokagaku K. K.), vinyl acetate/crotonic acid copolymer (Resin
28-1310, produced by NSC), vinyl acetate/crotonic acid/vinyl
neodecanate copolymer (28-2930, produced by NSC), methyl vinyl
ether maleic acid half ester (GANTREZ ES, produced by ISP), T-butyl
acrylate/ethyl acrylate/methacrylic acid copolymer (RUBIMER,
produced by BASF), vinylpyrrolidone/vinyl acetate/vinyl propionate
copolymer (RUBISCOL VAP, produced by BASF), vinyl acetate/crotonic
acid copolymer (RUBISET CA, produced by BASF), vinyl
acetate/crotonic acid/vinylpyrrolidone copolymer (RUBISET CAP,
produced by BASF), vinylpyrrolidone/acrylate copolymer (RUBIFLEX,
produced by BASF), acrylate/acrylamide copolymer (ULTRAHOLD,
produced by BASF), vinyl acetate/butyl maleate-isobornyl acrylate
copolymer (ADVANTAGE, produced by ISP), carboxy vinyl polymer
(CARBOPOL, produced by BF Goodrich) and acrylic acid-alkyl
methacrylate copolymer (PAMUREN, produced by BF Goodrich);
amphoteric polymer compounds such as acetic acid amphoteric
compound of dialkylaminoethyl methacrylate polymer (YUKAFORMER,
produced by Mitsubishi Chemical) and octylacrylamide
acrylate/hydroxypropyl acrylate/butylaminoethyl methacrylate
copolymer (AMPHOMER, produced by NSC); cationic polymer compounds
such as quaternized compound of vinylpyrrolidone/dimethylaminoethyl
methacrylate (GAFQUAT, produced by ISP) and methyl vinyl
imidazolium chloride/vinylpyrrolidone copolymer (RUBICOTE, produced
by BASF); and nonionic polymer compounds such as
polyvinylpyrrolidone/vinyl acetate copolymer (RUBISCOL VA, produced
by BASF) and vinylpyrrolidone/dimethylaminoethyl methacrylate
copolymer (COPOLYMER VC713, produced by ISP).
[0103] In addition, polymer compounds of natural origin, such as
cellulose and derivatives thereof, calcium alginate, pullulan,
agar, gelatin, tamarind seed polysaccharides, xanthane gum,
carrageenan, high-methoxyl pectin, low-methoxyl pectin, guar gum,
gum arabi, crystal cellulose, arabino galactan, karaya gum,
tragacanth gum, alginic acid, albumin, casein, cardrun, gellan gum
and dextran, can also be suitably used.
(9) Specific Examples of Biologically Active Ingredient
[0104] The biologically active ingredient may include substances
which are capable of imparting some biological activity to skin,
when such a substance is applied to the skin. Specific examples
thereof may include: whitening ingredient, anti-inflammatory, age
resistor, ultraviolet protection, slimming agent, skin tightening
agent, antioxidant, hair restorer, hair growing agent, moisturizer,
blood circulation accelerator, antibacterial agent, bactericide,
desiccant, cooling agent, warming agent, vitamin compound, amino
acid, wound healing accelerator, torpent, analgetic, cell activator
and enzyme ingredient.
[0105] Suitable examples of the ingredient to be blended therefor
may include: angelica extract, avocado extract, hydrangea extract,
althea extract, arnica extract, aloe extract, apricot extract,
apricot core extract, ginkgo extract, fennel extract, turmeric
extract, oolong tea extract, rose fruit extract, echinacea leaf
extract, scutellaria root extract, phellodendron bark extract,
goldthread extract, barley extract, hypericum extract, white nettle
extract, watercress extract, orange extract, sea salt, seaweed
extract, hydrolyzed elastin, hydrolyzed wheat powder, hydrolyzed
silk, chamomile extract, carrot extract, artemisia capillaris
extract, glycyrrhiza extract, sabdariffa extract, pyracantha
fortuneana fruit extract, kiwi extract, cinchona extract, cucumber
extract, guanosine, gardenia extract, sasa albo-marginata extract,
sophora root extract, walnut extract, grapefruit extract, clematis
extract, chlorella extract, mulberry bark extract, gentian extract,
black tea extract, yeast extract, burdock extract, fermented rice
bran extract, rice germ oil, comfrey extract, collagen, cowberry
extract, asiasarum root extract, bupleurum falcatum root extract,
umbilical cord extract, salvia extract, saponaria extract, bamboo
grass extract, crataegus extract, zanthoxylum fruit extract,
shiitake mushroom extract, rehmannia root extract, lithospermum
root extract, perilla extract, linden extract, filpendula extract,
peony root extract, calamus rhizome extract, birch extract,
horsetail extract, ivy extract, hawthorn extract, sambucus nigra
extract, yarrow extract, peppermint extract, sage extract, mallow
extract, cnidium rhizome extract, swertia herb extract, soy
extract, jujube extract, wild thyme extract, green tea extract,
clove extract, cogon extract, citrus unshiu peel extract, angelica
root extract, calendula extract, peach seed extract, bitter orange
extract, houttuynia extract, tomato extract, natto extract, ginseng
extract, garlic extract, wild rose extract, hibiscus sabdariffa
flower extract, ophiopogon tuber extract, parsley extract, honey,
witch hazel extract, pellitory extract, isodonis extract,
matricaria extract, loquat extract, coltsfoot extract, butterbur
scape extract, Poria cocos extract, butcher bloom extract, grape
extract, propolis, luffa extract, safflower extract, peppermint
extract, linden extract, peony extract, hop extract, pine extract,
horse chestnut extract, skunk cabbage extract, sapindaceae extract,
balm mint extract, peach extract, cornflower extract, eucalyptus
extract, saxifrage extract, citrus extract, coix seed extract,
mugwort extract, lavender extract, apple extract, lettuce extract,
lemon extract, Chinese milk vetch extract, rose extract, rosemary
extract, Roman chamomile extract and royal jelly extract.
[0106] Other examples may include biopolymers such as
deoxyribonucleic acid, mucopolysaccharide, sodium hyaluronate,
sodium chondroitin sulfate, collagen, elastin, chitin, chitosan and
hydrolyzed eggshell membrane; moisture retentive ingredients such
as amino acid, hydrolyzed peptide, sodium lactate, urea, sodium
pyrrolidonecarboxylate, betaine, whey and trimethylglycine; oily
ingredients such as sphingolipid, ceramide, phytosphingosine,
cholesterol, cholesterol derivatives and phospholipid;
anti-inflammatory such as E-aminocaproic acid, glycyrrhizic acid,
glycyrrhetic acid, lysozyme chloride, guaiazlene and
hydrocortisone; vitamins such as vitamin A, vitamin B2, vitamin B6,
vitamin D, vitamin E, calcium pantothenate, biotin and nicotinic
acid amide; active ingredients such as allantoin, diisopropylamine
dichloroacetate and 4-aminomethylcyclohexanecarboxylic acid;
antioxidants such as tocopherol, carotenoid, flavonoid, tannin,
lignin and saponin; cell activators such as a-hydroxy acid and
hydroxy acid; blood circulation accelerators such as y-orizanol and
vitamin E derivatives; wound healing agents such as retinol and
retinol derivatives; whitening agents such as albumin, kojic acid,
placenta extract, sulfur, ellagic acid, linoleic acid, tranexamic
acid and glutathione; and hair growing agents such as
cepharanthine, glycyrrhiza extract, capsicum tincture, hinokitiol,
iodized garlic extract, pyridoxine hydrochloride, DL-a-tocopherol,
DL-a-tocopheryl acetate, nicotinic acid, nicotinic acid
derivatives, calcium pantothenate, D-pantothenyl alcohol, acetyl
pantothenylethyl ether, biotin, allantoin, isopropylmethylphenol,
estradiol, ethynyl estradiol, capronium chloride, benzalkonium
chloride, diphenhydramine hydrochloride, Takanal, camphor,
salicylic acid, vanillylamide nonylate, vanillylamide nonanoate,
pyroctone olamine, glyceryl pentadecanoate, L-menthol,
mononitroguaiacol, resorcinol, .gamma.-aminobutyric acid,
benzethonium chloride, mexiletine hydrochloride, auxin, female
hormone, cantharis tincture, cyclosporine, zinc pyrithione,
hydrocortisone, minoxidil, polyoxyethylene sorbitan monostearate,
peppermint oil and SADANISHIKI extract.
[0107] (10) Specific examples of antioxidant Sodium
hydrogensulfite, sodium sulfite, erythorbic acid, sodium
erythorbate, dilauryl thiodipropionate, tocopherol, tolylbiguanide,
nordihydroguaiaretic acid, parahydroxy anisole, butylhydroxy
anisole, dibutylhydroxy toluene, ascorbyl stearate, ascorbyl
palmitate, octyl gallate, propyl gallate, carotenoid, flavonoid,
tannin, lignin, saponin and plant extracts having antioxidant
effect, such as apple extract and clove extract.
[0108] (11) Specific examples of solvent Purified water, ethanol,
lower alcohol, ethers, LPG, fluorocarbon, N-methylpyrrolidone,
fluoroalcohol, volatile linear silicone and next generation fleon
(such as fluorocarbon, chlorofluorocarbon, CFC).
EXAMPLES
[0109] The examples in this invention are herein described. The
descriptions indicated below are only the explanations to determine
the diet effect or the like on the inventive dietetic composition.
They are not limited to the products and method for manufacturing
the products.
(Method for Manufacturing the Dietetic Composition)
[0110] Indonesia's robusta green coffee beans are used as an
ingredient. Firstly, compress the green coffee beans to reduce the
oil, then obtain one kilogram of the compressed coffee beans.
Secondly, crush all the compressed coffee beans, reflux them with
hexane, and remove the remaining oil from them. Thirdly, extract
the defatted coffee beans with the hydroethanol having the ethanol
concentration of 60 wt % and dry the ethanol extract so that 60
grams of the green coffee bean extract (example: dietetic
composition) can be obtained. Also, HPLC (high-performance liquid
chromatography) of the ingredient of the green coffee bean extract
detected approx. 45 wt % of chlorogenic acids (including approx. 20
wt % of chlorogenic acid) and approx. 10 wt % of caffeine.
(Verification Test (In Vivo) for Diet Effect on Weight Gain and
Body Fat Accumulation)
[0111] Also let the mice eat freely three types of foods mixed with
the green coffee bean extract, caffeine, or chlorogenic acid
respectively (each ingredient should be put until the prescribed
content ratio is obtained) so as to verify each diet effect on the
weight gain and body fat accumulation.
[0112] Let the mice (ddY, male, 6-week-old) eat freely the three
types of foods (CE-2, CLEA Japan, Inc.) mixed with the green coffee
bean extract (0.5 wt % and 1.0 wt %), caffeine (0.05 wt % and 0.1
wt %), or chlorogenic acid (0.15 wt % and 0.3 wt %) respectively
for 13 days. The weight of each mouse was measured every other day
during the feeding period, and the weight of the epididymal fat of
each mouse on the last day of the feeding period. There was little
difference in intake of the food among the control group (for only
normal food given) and individual sample administration groups. The
results are shown in FIGS. 1 and 2.
[0113] As shown in FIG. 1, it is obvious that the green coffee bean
extract (Example) has a suppressive effect on the weight gain.
However the chlorogenic acid and caffeine contained in the green
coffee bean extract do not have a sufficient suppressive effect on
the weight gain. From this result, it is considered that specific
substances other than the chlorogenic acid and caffeine contained
in the green coffee bean extract (Example) are complexly associated
with the suppressive factors of the weight gain.
[0114] Also, as shown in FIG. 2, the green coffee bean extract
(Example) indicates a suppressive effect on the accumulation of the
weight of the epididymal fat and the weight of perinephric fat.
Chlorogenic acid and caffeine slightly indicates a suppressive
effect on the accumulation of the fat.
[0115] FIG. 3 shows a comparison of the anti-obesity effect on the
weight gain of the mice which ate different foods with the green
coffee bean extract (Example) or with the roasted coffee bean
extract (Comparative example). In the test, the non-defatted green
coffee beans are roasted and extracted under the same condition to
obtain the green coffee bean extract (Example). Also, the weight
change of the mice when using the roasted coffee bean extract
should be measured for 5 days under the same condition as the mice
using the aforementioned green coffee bean extract (Example).
[0116] As shown in FIG. 3, the green coffee bean extract (Example)
has a greater suppressive effect on the weight gain of the mice
compared to that of the roasted coffee bean extract (Comparative
example). Therefore, the green coffee bean extract (Example) has
obviously a greater diet effect compared to that of the roasted
coffee bean extract.
[0117] Next, the diet effect of the dietetic composition on the
weight gain, which is made by the green coffee bean extract
(Example) and the existing dietetic materials (salacia extract,
evening primrose extract, sesamine, garcinia), can be verified in
the following Chart 1. Salacia extract can be obtained by
extracting the salacia root with solvent. Evening primrose extract
can also be obtained by extracting the evening primrose with
solvent.
[0118] As a test method, as shown in Chart 1, a four-day experiment
was conducted with the mice (ddY, male, 5-week-old) to freely eat
the food (CE-2, CLEA Japan, Inc.) mixed with the sample as
indicated in Chart 1. The weight of each mouse was measured on the
first day and on the final day of the experimental period.
[0119] In the test, green coffee bean extract (0.5 wt %), salacia
extract (0.5 wt %), evening primrose extract (3.0 wy %), sesamine
(0.5 wy %) and garcinia (1.0 wy %) should be respectively mixed
with the food.
TABLE-US-00001 CHART 1 Difference in the weight Weight (g) compared
to Prior to the Weight the control Class test 4.sup.th day increase
(g) (g) Control 26.85 .+-. 1.02 31.23 .+-. 1.18 4.38 -- Green
coffee bean extract 26.71 .+-. 0.74 30.47 .+-. 0.94 3.76 -0.62
Green coffee bean extract & 27.20 .+-. 1.13 31.42 .+-. 0.54
3.06 -1.32 salacia extract Salacia extract 27.29 .+-. 1.29 30.64
.+-. 1.85 3.35 -1.03 Green coffee bean extract & 28.26 .+-.
0.86 31.45 .+-. 1.443 3.20 -1.18 evening primrose extract Evening
primrose extract 28.18 .+-. 1.24 1.58 .+-. 1.10 3.39 -0.99 Green
coffee bean extract & 27.30 .+-. 0.89 30.76 .+-. 1.64 3.45
-0.93 sesamine Sesamine 27.36 .+-. 0.86 30.91 .+-. 1.79 3.55 -0.83
Green coffee bean extract & 27.47 .+-. 0.88 30.55 .+-. 1.41
3.08 -1.3 garcinia Garcinia 26.93 .+-. 1.24 30.51 .+-. 1.96 3.58
-0.8 Average .+-. standard error (n = 5)
[0120] As shown in Chart 1, when using the green coffee bean
extract (Example) together with the salacia extract, evening
primrose extract, sesamine, or garcinia, the suppressive effect of
those complex ingredients on the weight gain greatly increases,
compared with the administration of the green coffee bean extract
alone.
[0121] Thus, in the diet prescription of the green coffee bean
extract (Example), the combination of the green coffee bean extract
(Example) with the salacia extract, evening primrose extract,
sesamine, or garcinia can increase the diet effect. In other words,
the diet of the green coffee bean extract (Example) combined with
one or more substances from among the salacia extract, evening
primrose extract, sesamine, or garcinia can produce a greater
effect.
[0122] In other examples, the green coffee bean extract combined
with one or more substances from among gymnema sylvestre, mulberry
leaf, guava leaf, white kidney bean, glucomannan, yacon, chia seed,
fenugreek, wheat amylase inhibitor, balsam pear, conjugated
linoleic acid, L-carnitine, coleus forskohlli, yerba mate, astibe
thunbergii, citrus aurantium, paprika, capsiate, cassia polyphenol,
malus extract, green tea extract, green tea polyphenol, soybean
isoflavone, purple rice extract, chitosan, raspberry ketone, or the
like also show an excellent effect on the diet.
(Verification Test of The Diet Effect on the Fat Metabolic
Pathway)
(1) Verification Test of the Suppressive Effect on the Absorption
of Fat
[0123] a. Retarding Effect on Fat Absorption (In Vivo):
[0124] Administer a single dose of olive oil to the mice. Then
verify the effect of the green coffee bean extract (Example) on the
absorption of fat in the body of each mouse.
[0125] In the test, blood samples were taken from 20-hour fasting
mice (ddY, male, 6-week-old). Half an hour after the blood
sampling, the gum aracia suspension (10 mL/kg) with the green
coffee bean extract (Example) in concentration of 5 w/v % was
orally administered to the mice. One hour later, the olive oil was
orally administered to the mice. Two, four, and six hours later,
the blood samples were respectively taken. Then, the blood serum
was separated from the blood sample and the concentration of
triglyceride was measured by using the enzyme method (triglyceride
E-Test Wako, Wako Pure Chemical Industries Ltd. of Japan).
[0126] As shown in FIG. 4, compared to the control group, the green
coffee bean extract (Example) shows a significant suppressive
effect on the blood triglyceride level. Therefore, it is considered
that the green coffee bean extract has a strong suppressive effect
on the absorption of fat.
b. Pancreatic Lipase Inhibitory Activity (In Vitro):
[0127] In regard to the green coffee bean extract (Example) and its
contained substances (caffeine and chlorogenic acid), the
pancreatic lipase inhibitory activity related to the lipolysis was
evaluated by in vitro experiment.
[0128] The lipase inhibitory activity was analyzed by using a
pancreatic lipase (product of SIGMA ADLRICH JAPAN K.K., final
concentration 105.8 units/mL) derived from the swine and a lipase
kit-s (Dainippon Pharmaceutical Co., Ltd.). FIG. 5 shows the
result.
[0129] As shown in FIG. 5, the green coffee bean extract (Example),
the chlorogenic acid and the caffeine indicate a pancreatic lipase
inhibitory activity and all three substances suppress the fat
absorption level. Yet, the green coffee bean extract shows a
greater effect on the pancreatic lipase inhibitory activity than
that of chlorogenic acid and caffeine. Considering the content of
the chlorogenic acid (approx. 20 wt %) and caffeine (approx. 10 wt
%) in the green coffee bean extract, it is thought that substances
other than the chlorogenic acid and caffeine affect the pancreatic
lipase inhibitory activity.
(2) Verification Test of Inhibitory Effect on Fat Accumulation
[0130] a. Suppressive Effect on 3T30L1 Adipocyte Degradation (In
Vitro):
[0131] Apply the green coffee bean extract (Example) and its
contained substance (caffeine and chlorogenic acid) to the mouse
adipose cell line (3T30L1) in culture and verify the effect on the
fat accumulation after the differentiation induction.
[0132] The test method is herein described. Cultivate the 3T30L1
adipose cell (5.times.10.sup.4 cells/mL) in DMEM medium (high
glucose) including fetal calf serum (10 wt %) for two days. Then,
replace the medium with a different type of medium containing
insulin (1 .mu.g/mL), dexamethasone (0.25 .mu.M) and isobutyl
methyl xanthin (0.5 mM) for the differentiation induction. Two days
later, replace the medium again with the different medium
containing the samples and insulin (1 .mu.g/mL), and cultivate them
for six days replacing the medium every other day. After completing
the cultivation, analyze the glycerol 3-phosphate dehydrogenase
(GPDH) activity which is to be an indicator of the concentration of
triglyceride in the cell and adipocyte differentiation.
[0133] As shown in FIG. 6, the green coffee bean extract (Example),
the caffeine, and the chlorogenic acid indicate a mild inhibitory
effect on the fat accumulation (decrease in triglyceride
accumulation).
[0134] Also, it is obvious that the green coffee bean extract
(Example), the caffeine, and the chlorogenic acid have a mild
inhibitory effect on the GPDH activity which is to be an indicator
of the concentration of triglyceride in the cell and adipocyte
differentiation. Furthermore, the concentration indicates no
toxicity.
b. Suppressive Effect on Fatty Liver (In Vivo):
[0135] The effect on the hepatic lipid (triglyceride and total
cholesterol) is evaluated after the green coffee bean extract and
its contained substances (caffeine, and chlorogenic acid) are
continuously administered to the mice for two weeks.
[0136] The test method is herein described. Keep the mice (ddY,
male, 5-week-old) in the laboratory for one week. Then, divide them
into four groups and orally administer the samples suspended in the
gum aracia (5 w/v %) once a day for two weeks. On the final day of
the test, remove the livers from the non-food-derived mice, and
measure the amount of liver triglyceride and total cholesterol
contained therein by using the test kit of Wako Pure Chemical
Industries Ltd. of Japan. (The result shown in FIG. 7)
[0137] As shown in FIG. 7, the green coffee bean extract (Example),
the caffeine and the chlorogenic acid reduce the liver
triglyceride. The caffeine and the chlorogenic acid especially
indicate a strong effect. On the other hand, the total cholesterol
value is almost the same as the value of the control group. As the
results of this test show, it is thought that the green coffee bean
extract has a suppressive effect on the accumulation of neutral fat
in the liver and that the caffeine and chlorogenic acid are related
with the suppressive effect.
(3) Verification Test of Promotive Effect on Lipolysis
[0138] a. Lipolysis Effect (In Vitro):
[0139] It is known that caffeine enhances the activity of lipase in
the adipose cell and promotes the degradation of neutral fat. In
this test, the lipolysis effect of the green coffee bean extract
and its contained substances (caffeine and chlorogenic acid) are
respectively reviewed, compared to the existing dietetic
composition.
[0140] The test method is herein described. Remove the epididymal
fat from male Wister rats, and incubate the fat in each sample
solved in Medium 199 (medium culture) at a temperature of
37.degree. C. for three hours. After completing the incubation,
remove the fat and measure the amount of glycerol in the medium by
using F-kit glycerol (product of Nippon Roche). The result is shown
in FIG. 8.
[0141] As shown in FIG. 8, when using 1000 .mu.g/mL of the green
coffee bean extract (Example), the lipolysis effect is the same as
that of the single compound--caffeine, capsaicin, and synephrine,
and is greater than that of the citrus extract containing approx.
30 wt % of synephrine. Also, the chlorogenic acid indicates a mild
lipolysis effect.
b. Hypotriglyceridemic Action in Blood (In Vivo)
[0142] The green coffee bean extract or its contained substances
(caffeine and chlorogenic acid) are respectively administered to
the food-deprived mice. Then the effects on the blood triglyceride
level are observed.
[0143] The test method is herein described. First of all, take a
blood sample from the veins of the 24-hour food-deprived mice (ddy.
Male, 6-week-old). Half an hour later, orally apply each sample (10
mL/kg) suspended with the gum aracia of 5 w/v % to the mice. Then,
take a blood sample from the mice every one hour, and measure the
blood triglyceride levels. Under the same condition, measure the
blood triglyceride levels of the mice as a control, in which only
gum aracia is orally administered.
[0144] As shown in FIG. 9, the green coffee bean extract (Example)
indicates a strong lowering effect on the blood-triglyceride, which
is similar to the effect of capsaicin. Also, the caffeine indicates
a strong lowering effect on the blood-triglyceride. On the other
hand, the chlorogenic acid indicates a lowering effect on the
blood-triglyceride identical to the effect of synephrine.
[0145] Considering the above test result, it is thought that the
green coffee bean extract (Example) has a promotive effect on the
lipolysis of the adipose cell, and that the caffeine and
chlorogenic acid are related to this effect.
(4) Verification Test of the Promotive Effect on Fat-Burning
Activity
[0146] (Verification Test of the Promotive Effect on Carnitine
Palmitoyltransferase (CPT) Activity: in vivo).
[0147] The food mixed with the green coffee bean extract (Example)
was given to the mice, and the carnitine palmitoyltransferase (CPT)
activity which contributes the .beta.-oxidation of the fat-burning
metabolism is measured.
[0148] The test method is herein described. Firstly, let the mice
(ddY, male, 7-week-old) eat freely for six days the food (CE-2,
product of CLEA Japan, Inc) which is mixed with the green coffee
bean extract (0.5 and 1 wt %). Secondly, after dislocating the
cervical spines, remove the livers from the mice, and add the
buffer solution (pH7.4) containing 0.25M of sucrose and 1.0 mM of
EDTA which are in six times its volume of the liver for homogenate
and centrifugal separation (3,000 r.p. 10 min.). Thirdly,
centrifugalize the supernatant (11,000 r.p. 10 min.) to obtain
precipitate (mitochondrial fraction), and suspend it with the
buffer solution (2.5 mL). After protein determination, measure the
CPT activity by the DTNB method. The result is indicated in FIG.
10.
[0149] As shown in FIG. 10, the green coffee bean extract (Example)
indicates a dose-dependent promotive effect on the CPT activity.
Thus, it is thought that the green coffee bean extract (Example)
promotes the CPT activity and supports the fat-burning
activity.
(Verification Test of the Effect on Diabetes Prevention)
[0150] a. Retarding Effect on Carbohydrate Absorption (In
Vivo):
[0151] Carbohydrate is administered to the mice. Then the
suppressive effect of the green coffee bean extract on the
elevation of the blood glucose levels is verified by using the
mouse carbohydrate load model.
[0152] The test method is herein described. First of all, take the
blood sample from the 18-hour food-deprived mice (ddy, male,
6-week-old). Immediately after the blood sampling, orally
administer the green coffee bean extract (Example) aqueous solution
(10 mL/kg) to the mice. One hour later, orally administer a dose (5
mL/kg) of the glucose (0.5 g/kg) or sucrose (2 g/kg) to the mice.
Then, take the blood samples a half an hour, one hour, and two
hours later. Furthermore, separate the serum from the blood and
determine the glucose concentration by the enzyme method
(determiner GL-E: product of Kyowa Medex Co., Ltd).
[0153] As shown in FIG. 12, administrating 400 mg/kg of the green
coffee bean extract (Example) with a glucose load and 200 mg/kg of
the green coffee bean extract (EXAMPLE) with sucrose load to the
mice, respectively, suppresses the elevation of the blood glucose
levels.
b. .alpha.-Glucosidase Inhibitory Activity (In Vivo):
[0154] In regard to the green coffee bean extract (Example) and its
contained substances (chlorogenic acid, caffeine, and quinic acid),
the .alpha.-glucosidase inhibitory activity which is a
carbohydrate-degrading enzyme was evaluated by the in vivo
experiment.
[0155] The test method is herein described. First of all, mix the
acetone powder of the rat small intestine with the pH7.0. 0.1M
phosphate buffer solution (product of SIGMA ADLRICH JAPAN K.K.),
which is approx. 10 times as much as the volume of the acetone
powder, and obtain the enzyme liquid from the centrifuged
supernatant. Use the 0.2 mM 4-methyl umbel
phelyl-.alpha.-D-gluco-pyranoside (SIGMA ADLRICH JAPAN K.K.) as a
substrate. After dissolving each sample in the DMSO, prepare the
two-fold dilution series with the 4% DMSO containing phosphate
buffer solution. The diluted solution (50 .mu.L/well) and buffered
substrate (25 .mu.L/well) are mixed in a microplate, and after
preheating it at 37.degree. C. for 10 minutes, add the enzyme
liquid (25 .mu.L/well) to induce the reaction at 37.degree. C. for
30 minutes (final concentration of enzyme: 1 mg proteinmL, final
concentration of substrate: 0.05 mM). Then, add the 0.2M
Na.sub.2CO.sub.3 (100 .mu.L/well) to stop the reaction. Measure the
fluorescence intensity (excitation wavelength: 366 nm, determined
wavelength: 45 nm) using a microplate reader.
[0156] As shown in Chart 2, the green coffee bean extract
(Example), chlorogenic acid and coffeic acid respectively indicate
a strong inhibitory activity of .alpha.-glucosidase. However,
caffeine and quinic acid does not indicate the inhibitory activity.
The inhibitory activity of the green coffee bean extract (Example)
is greater than that of the chlorogenic acid and coffeic acid.
TABLE-US-00002 CHART 2 Class IC.sub.50 (.mu.g/mL) Green coffee bean
70 extract: Caffeine: >1000 Chlorogenic acid: 100 Coffeic acid:
100 Quinic acid: >1000
(Blending Sample)
[0157] The blending samples of the dietetic composition in this
invention are herein described. In the following samples, an
hydroethanol extract derived from the defatted green coffee bean
can also be used for the green coffee bean extract. Each blending
example is also applicable for Invention 2 (a composition for
suppressing the fat absorption), Invention 3 (a composition for
inhibiting the pancreatic lipase activity), Invention 4 (a
composition for promoting the carnitine palmitoyltransferase
activity), and Invention 5 (a composition for inhibiting the
.alpha.-glucosidase activity), respectively.
TABLE-US-00003 CHART 3 Blending sample 1: Chewing gums Sugar: 53.0
wt % Gum base: 20.0 Glucose: 10.0 Starch syrup: 16.0 Aroma
chemical: 0.5 Green coffee bean syrup (Dietetic composition): 0.5
100.0 wt %
TABLE-US-00004 CHART 4 Blending sample 2: Gummies Reduced starch
syrup: 40.0 wt % Granulated sugar: 20.0 Glucose sugar: 20.0
Gelatin: 4.7 Water: 9.68 Japanese plum juice: 4.0 Japanese plum
flavor: 0.6 Pigment: 0.02 Green coffee bean syrup (Dietetic
composition): 1.05 100.0 wt %
TABLE-US-00005 CHART 5 Blending example 3: Candies Sugar: 50.0 wt %
Starch syrup: 33.0 Water: 14.4 Organic acid: 2.0 Aroma chemical:
0.2 Green coffee bean extract (Dietetic composition): 0.4 100.0 wt
%
TABLE-US-00006 CHART 6 Blending example 4: Yogurts (Natural/Firm)
Milk: 41.5 wt % Skimmed milk: 5.8 Sugar: 8.0 Agar-agar: 0.15
Gelatin: 0.1 Lactobacillus: 0.005 Green coffee bean extract
(Dietetic composition): 0.4 Aroma chemical: Trace amount Water:
Rest 100.0 wt %
TABLE-US-00007 CHART 7 Blending sample 5: Soft capsules Sprouted
brown rice oil: 87.0 wt % Emulsifying agent: 12.0 Green coffee bean
extract (Dietetic composition): 1.0 100.0 wt %
TABLE-US-00008 CHART 8 Blending sample 6: Coffee drinks (Liquid
type) Roasted coffee bean: 6.0 wt % Sugar: 6.0 Baking soda: 0.2
Emulsifying agent: 0.15 Green coffee bean extract (Dietetic
composition): 1.0 Water: Rest 100.0 wt %
TABLE-US-00009 CHART 9 Blending sample 7: Coffee drinks (Powder
type) Instant coffee granule: 90.0 wt % Skimmed milk: 7.0 Green
coffee bean extract (Dietetic composition): 3.0 100.0 wt %
TABLE-US-00010 CHART 10 Blending sample 8: Soft drinks High
fructose corn syrup: 30.0 wt % Emulsifying agent: 0.5 Green coffee
bean extract (Dietetic composition): 0.05 Aroma chemical:
Appropriate amount Distilled water: Rest 100.0 wt %
TABLE-US-00011 CHART 11 Blending sample 11: Tablets Lactose: 54.0
wt % Crystalline cellulose: 30.0 Starch splitting product: 10.0
Glycerin fatty acid ester: 5.0 Green coffee bean extract (Dietetic
composition): 1.0 100.0 wt %
TABLE-US-00012 CHART 12 Blending sample 10: Tablet-shaped sweets
Sugar: 76.4 wt % Glucose: 19.0 Glycerin fatty acid ester: 0.2 Green
coffee bean extract (Dietetic composition): 0.5 Distilled water:
3.9 100.0 wt %
TABLE-US-00013 CHART 13 Blending sample: Cosmetic creams Squalene:
20.0 wt % Bees wax: 5.0 Distilled jojoba oil: 5.0 Glycerin: 5.0
Glycerin monostearate: 2.0 Polyoxyethylene (20)
sorbitan-monostearate: 2.0 Green coffee bean extract (Dietetic
composition): 2.0 Food preservative: Appropriate amount Aroma
chemical: Appropriate amount Distilled water: Rest 100.0 wt %
TABLE-US-00014 CHART 14 Blending example 12: Skin lotions Ethanol:
5.0 wt % Glycerin: 2.0 1,3-butylene glycol: 2.0 Polyethylene oleyl
ether: 0.5 Sodium citrate: 0.1 Citric acid: 0.1 Green coffee bean
extract (Dietetic composition): 0.1 Distilled water: Rest 100.0 wt
%
TABLE-US-00015 CHART 15 Blending example 13: Body gel Macadamia nut
oil: 2.0 wt % Octyl decyl myristate: 10.0 Methylphenyl
polysiloxane: 5.0 Behenyl alcohol: 3.0 Stearic acid: 3.0 Batyl
alcohol: 1.0 Glycel monostearate: 1.0 Tetra oleic acid
polyoxyethylene sorbit: 2.0 Hydrogenated soybean phosphatide: 1.0
Ceramide: 0.1 Retinol palmitate: 0.1 Preservative: Appropriate
amount Centella asiatica extract: 1.0 Green coffee bean extract
(Dietetic composition): 1.0 1,3-butylene glycol: 5.0 Distilled
water: Rest 100.0 wt %
TABLE-US-00016 CHART 16 Blending example 14: Cosmetic emulsion
Squalene: 4.0 wt % Vaseline: 2.5 Cetanol: 2.0 Glycerin: 2.0
Oleophilic glycerin monostearate: 1.0 Stearic acid: 1.0 L-arginine:
1.0 Green coffee bean extract (Dietetic composition): 0.5 Potassium
hydroxide: 0.1 Aroma chemical: Trace amount Distilled water: Rest
100.0 wt %
TABLE-US-00017 CHART 17 Blending example 15: Bath agent (liquid
type) Propylene glycol: 50.0 wt % Ethanol: 20.0 Sodium sulphate:
5.0 Green coffee bean extract (Dietetic composition): 0.5 Lanoline:
0.5 Avocado oil agent: 0.5 Pigment: 1.5 Aroma chemical: 22.0 100.0
wt %
INDUSTRIAL APPLICABILITY
[0158] As described above, this invention provides the following
excellent effects. [0159] (a) Excellent dietetic effect can be
obtained by taking a highly safe extract derived from the green
coffee beans, and which contributes the prevention and treatment of
life-style diseases such as diabetes or the like. [0160] (b) The
safe extract derived from the green coffee beans is usable as a
material for foods, drinks, drugs or the like.
* * * * *