EP1888173A2 - Nouvelle utilisation du gallate d'(-)-épigallocatechine - Google Patents

Nouvelle utilisation du gallate d'(-)-épigallocatechine

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Publication number
EP1888173A2
EP1888173A2 EP06743119A EP06743119A EP1888173A2 EP 1888173 A2 EP1888173 A2 EP 1888173A2 EP 06743119 A EP06743119 A EP 06743119A EP 06743119 A EP06743119 A EP 06743119A EP 1888173 A2 EP1888173 A2 EP 1888173A2
Authority
EP
European Patent Office
Prior art keywords
humans
body weight
epigallocatechin gallate
group
mammal
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP06743119A
Other languages
German (de)
English (en)
Inventor
Daniel Raederstorff
Christoph Riegger
Frank Thielecke
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
DSM IP Assets BV
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DSM IP Assets BV
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Filing date
Publication date
Application filed by DSM IP Assets BV filed Critical DSM IP Assets BV
Priority to EP06743119A priority Critical patent/EP1888173A2/fr
Publication of EP1888173A2 publication Critical patent/EP1888173A2/fr
Withdrawn legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Definitions

  • the present invention refers to the use of (-)-epigallocatechin gallate (EGCG), preferably in combination with a sympathomimeticum, - for increasing/stimulating the fat oxidation in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans, especially during post prandial conditions;
  • EGCG epigallocatechin gallate
  • mammals selected from the group consisting of hu- mans, cats, dogs and horses, preferably in humans;
  • the preferred sympathomimeticum is caffeine.
  • the invention further refers to the corre- sponding methods. Uses
  • a first object of the present invention is the use of EGCG for increasing the fat oxidation in mammals selected from the group consisting of humans, cats, dogs and horses, prefera- bly in humans.
  • EGCG has especially an influence on the prandial and post-prandial fat oxidation.
  • the EGCG may be administered in the form of (fortified) food or (fortified) feed, dietary supplements, beverages, tablets, granules, capsules, pastes, food additives, feed additives, or effervescent formulations. If it is administered in the form of a beverage, it shows its positive influence on the fat oxidation faster than if it is administered in the form of a capsule. In a preferred embodiment of the present invention EGCG is therefore administered in such a way that it is present or moreover that its concentration is at a high level during the intake of food/feed/beverages, especially during the fat intake, of the mammal. That means that EGCG is preferably administered before or simultaneously with the food/feed/beverages.
  • the EGCG is part of the food/feed.
  • Examples are cereal bars containing EGCG.
  • EGCG is used in combination with a sympathomimeticum.
  • Espe- cially preferred is also the use of compositions such as dietary supplements consisting essentially of EGCG and caffeine.
  • the energy expenditure is not changed by the increased fat oxidation induced by the use of EGCG.
  • a second object of the present invention is the use of EGCG for supporting the metaboli- zation of fat in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans.
  • EGCG is therefore administered in such a way that it is present or moreover that its concentration is at a high level during the intake of food/feed/beverages, especially during the fat intake, of the mammal selected from the group consisting of humans, cats, dogs and horses, preferably of the humans. That means that EGCG is preferably administered before or simultaneously with the food/feed/beverages.
  • the EGCG is part of the food/feed. Examples are cereal bars containing EGCG.
  • a third object of the present invention is the use of EGCG for reducing the weight of mammals selected from the group consisting of humans, cats, dogs and horses, preferably the weight of humans.
  • EGCG is used in combination with a sympathomimeticum.
  • a forth object of the present invention is the use of EGCG for reducing the fat mass in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans.
  • EGCG is used in combination with a sympathomimeticum.
  • the visceral and/or the subcutaneous fat is reduced by the use of EGCG, preferably in combination with a sympathomimeticum.
  • the visceral fat layer is considered an important element in the development of the metabolic syndrome.
  • a fifth object of the present invention is the use of EGCG, preferably in combination with a sympathomimeticum, for increasing the endurance in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans. Therefore, the present invention is also directed to sport beverages containing EGCG, preferably highly purified EGCG as defined below, more preferably in combination with caffeine.
  • a sixth object of the present invention is the use of EGCG for reducing the carbohydrate oxidation in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans.
  • EGCG is used in combination with a sympathomimeticum.
  • a seventh object of the present invention is the use of EGCG for reducing the respiratory quotient in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans.
  • EGCG is used in combination with a sympathomimeticum.
  • Respiratory quotient CRO Animal cells obtain energy in the form of ATP by oxidizing food molecules through the process of respiration. Carbohydrates and fatty acids are the most important fuels for generating ATP in animal cells. - A -
  • the respiratory quotient measures the ratio of the volume of carbon dioxide (V(Co 2 )) produced by an organism to the volume of oxygen consumed (V(O 2 )).
  • the volumes of O 2 and CO 2 are measured by indirect calorimetry
  • An eighth object of the present invention is the use of EGCG for improving the flow mediated dilation, thereby contributing to the beneficial effects on coronary health, in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans.
  • EGCG acutely increases the flow mediated dilation thereby improving the endothelial function.
  • EGCG elicits this effect when present in plasma.
  • Endothelial function is regarded as an important element in the development of the metabolic syndrome. Thus, EGCG prevents the development of the metabolic syndrome.
  • the used EGCG has a purity of at least 80%, preferably of at least 85%, more preferably of at least 90%, even more preferably of at least 92%, most preferably of at least 94%.
  • an aqueous green tea extract containing EGCG in an amount of at least 80% (preferred of at least 85%, more preferred of at least 90%, even more preferred of at least 92%, most preferred of at least 94%), based on the total amount of the extract, as e.g. and preferably obtained by any of the processes described in US 6,383,392, EP 1 103 550, US 10/246 112 and EP 1 077 21 1.
  • the total amount of other polyphenols and catechins such as gallocatechin gallate, catechin gallate, epicatechin gallate, epigallocatechin, gallocatechin and epicate- chin is low, preferably it is ⁇ 5 weight-%, based on the total weight of the green tea extract. More preferably the amount of gallocatechin gallate is ⁇ 2.5 weight-%, and/or the amount of epicatechin gallate is ⁇ 5 weight-% (preferably ⁇ 3 weight-%), and/or the amount of caffeine is ⁇ 2.5 weight-%, preferably ⁇ 0.1 weight-%, and/or the amount of gallic acid is ⁇ 0.1 weight-%, based on the total weight of the green tea extract.
  • a sympathomimeticum is a substance that stimulates the sympathetic nervous system.
  • a preferred example of such a substance is caffeine. Therefore the present invention refers to the use of a combination of EGCG and caffeine for the uses as given above. If caffeine is used in combination with EGCG the daily dosage of caffeine varies preferably from 2.5 mg per kg body weight to 7.5 mg per kg body weight.
  • sympathomimetica that may be used in combination with EGCG are theophylline, theobromine or extracts of xanthine containing plants such as cacao plants, coffee plants, barley and ginger.
  • the sympathetic nervous system is also stimulated by physical activity such as sport, so that sport can also be seen as sympathomimeticum. Therefore, the present invention relates also to the use of EGCG as given above, preferably of highly purified EGCG as defined above, in combination with physical activity.
  • Preferred subjects for the uses/methods of the present invention are humans.
  • the daily dosage of EGCG varies from 0.14 to 25 mg per kg body weight per day, preferably from 2.0 to 9 mg per kg body weight per day, more preferably from 4.0 to 9.0 mg per kg body weight per day, most preferably from 4.0 to 4.5 mg per kg body weight per day.
  • the daily dosage of EGCG varies from 10 to 1500 mg, preferably from 150 to 600 mg, more preferably from 300 to 600 mg, most preferably it is 300 mg.
  • a ninth object of the present invention is a method for increasing the fat oxidation in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans, said method comprising the step of administering an effective dose of EGCG, preferably in combination with an effective dose of a sympathomimeticum, to a mammal selected from the group consisting of humans, cats, dogs and horses, preferably to a human, which is in need thereof, characterized in that the effective dose of (-)- epigallocatechin gallate varies from 0.14 to 25 mg per kg body weight per day, preferably from 2.0 to 9 mg per kg body weight per day, more preferably from 4.0 to 9.0 mg per kg body weight per day, most preferably from 4.0 to 4.5 mg per kg body weight per day.
  • a tenth object of the present invention is a method for supporting the metabolization of fat in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans, said method comprising the step of administering an effective dose of EGCG, preferably in combination with an effective dose of a sympathomimeticum, to a mammal selected from the group consisting of humans, cats, dogs and horses, preferably to a human, which is in need thereof, characterized in that the effective dose of (-)- epigallocatechin gallate varies from 0.14 to 25 mg per kg body weight per day, preferably from 2.0 to 9 mg per kg body weight per day, more preferably from 4.0 to 9.0 mg per kg body weight per day, most preferably from 4.0 to 4.5 mg per kg body weight per day.
  • An eleventh object of the present invention is a method for reducing the fat mass in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans, said method comprising the step of administering an effective dose of EGCG, preferably in combination with a sympathomimeticum, to a mammal selected from the group consisting of humans, cats, dogs and horses, preferably to a human, which is in need thereof, characterized in that the effective dose of EGCG varies from 0.14 to 25 mg per kg body weight per day, preferably from 2.0 to 9 mg per kg body weight per day, more preferably from 4.0 to 9.0 mg per kg body weight per day, most preferably from 4.0 to 4.5 mg per kg body weight per day.
  • a twelfth object of the present invention is a method for reducing the weight of mammals selected from the group consisting of humans, cats, dogs and horses, preferably for reducing the weight of humans, said method comprising the step of administering an effective dose of EGCG, preferably in combination with a sympathomimeticum, to a mammal selected from the group consisting of humans, cats, dogs and horses, preferably to a human, which is in need thereof, characterized in that the effective dose of EGCG varies from 0.14 to 25 mg per kg body weight per day, preferably from 2.0 to 9 mg per kg body weight per day, more preferably from 4.0 to 9.0 mg per kg body weight per day, most preferably from 4.0 to 4.5 mg per kg body weight per day.
  • a thirteenth object of the present invention is a method for increasing the endurance in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans, said method comprising the step of administering an effective dose of EGCG, preferably in combination with a sympathomimeticum, to a mammal selected from the group consisting of humans, cats, dogs and horses, preferably to a human, which is in need thereof, characterized in that the effective dose of EGCG varies from 0.14 to 25 mg per kg body weight per day, preferably from 2.0 to 9 mg per kg body weight per day, more preferably from 4.0 to 9.0 mg per kg body weight per day, most preferably from 4.0 to 4.5 mg per kg body weight per day.
  • a forteenth object of the present invention is a method for reducing the carbohydrate oxi- dation in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans, said method comprising the step of administering an effective dose of EGCG, preferably in combination with a sympathomimeticum, to a mammal selected from the group consisting of humans, cats, dogs and horses, preferably to a human, which is in need thereof, characterized in that the effective dose of EGCG varies from 0.14 to 25 mg per kg body weight per day, preferably from 2.0 to 9 mg per kg body weight per day, more preferably from 4.0 to 9.0 mg per kg body weight per day, most preferably from 4.0 to 4.5 mg per kg body weight per day.
  • the methods further comprise the step of the mammals selected from the group consisting of humans, cats, dogs and horses performing physical activity, preferably the methods further comprise the step of the humans performing physical activity.
  • a fifteenth object of the present invention is a method for reducing the respiratory quotient in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans, said method comprising the step of administering an effective dose of (-)- epigallocatechin gallate, preferably in combination with a sympathomimeticum, to a mammal selected from the group consisting of humans, cats, dogs and horses, preferably to a human, which is in need thereof, characterized in that the effective dose of (-)-epigallo- catechin gallate varies from 0.14 to 25 mg per kg body weight per day, preferably from 2.0 to 9 mg per kg body weight per day, more preferably from 4.0 to 9.0 mg per kg body weight per day, most preferably from 4.0 to 4.5 mg per kg body weight per day.
  • a sixteenth object of the present invention is a method for improving the flow mediated dilation in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans, thereby contributing to a beneficial effect on the coronary health, said method comprising the step of administering an effective dose of (-)-epigallocatechin gallate to a mammal selected from the group consisting of humans, cats, dogs and horses, preferably to a human, which is in need thereof, characterized in that the effective dose of (-)-epigallocatechin gallate varies from 0.14 to 25 mg per kg body weight per day, preferably from 2.0 to 9 mg per kg body weight per day, more preferably from 4.0 to 9.0 mg per kg body weight per day, most preferably from 4.0 to 4.5 mg per kg body weight per day.
  • the mammals are humans with a body mass index above 25.
  • the body mass index is the number obtained by dividing the body weight in kilogramm of a human by the square of its height in meters.
  • the EGCG has a purity of at least 80%, preferably of at least 85%, more preferably of at least 90%, even more preferably of at least 92%, most preferably of at least 94%.
  • an EGCG obtained by any of the processes described in US 6,383,392, EP 1 103 550, US 10/246 112 and EP 1 077 211.
  • the EGCG may be administered in the form of (fortified) food or (fortified) feed, dietary supplements, beverages, food additives, or feed additives.
  • Non-limiting examples of food are dairy products such as yoghurts, cereal bars and bakery items such as cakes and cookies; but EGCG may also be added to any other food/feed a mammal selected from the group consisting of humans, cats, dogs and horses regularly eats. Food may also be in liquid form such as soups and dairy products (muesli drinks).
  • Non-limiting examples of beverages for humans are non-alcoholic drinks such as soft drinks, sport drinks, fruit juices, lemonades, near-water drinks (i.e. low calorie drinks based on water), teas and milk based drinks.
  • Preferred forms of dietary supplements are tablets, pills, granules, dragees, capsules, and effervescent formulations.
  • EGCG is administered in the form of a beverage, it shows its positive influence on the fat oxidation and the endurance faster than if it is administered in the form of a capsule.
  • EGCG is therefore administered in such a way that it is present or moreover that its concentration is at a high level during the intake of food/feed/beverages, especially during the fat intake, of the mammal selected from the group consisting of humans, cats, dogs and horses, preferably of the human, and during the activity for which endurance is needed, respectively. That means that EGCG is preferably administered before or simultaneously with the food/feed/beverages.
  • the (composition/dietary supplement containing) EGCG is incorporated by the mammal selected from the group consisting of humans, cats, dogs and horses, preferably of the human, at least half an hour before the intake of food, feed or beverages, preferably at a point in time between 0.5 and 1.5 hours before the intake of food, feed or beverages. If EGCG is administered in form of fortified food, feed or beverages it is simultaneously incorporated by the mammal selected from the group consisting of humans, cats, dogs and horses, preferably of the human, with such fortified food, feed or beverage.
  • EGCG is used in combination with a sympathomimeticum.
  • the present invention is also directed to the use of (-)-epigallocatechin gallate, preferably in combination with a sympathomimeticum, for the manufacture of a composition - for increasing the fat oxidation in mammals selected from the group consisting of humans, cats, dogs and horses, preferably in humans;*
  • composition is administered in such a way that (-)-epigallocatechin gallate is present in the body during the intake of food/feed/beverages of the mammal, preferably that it is present in a high concentration in the body during the intake of food/feed/beverages of the mammal selected from the group consisting of humans, cats, dogs and horses, preferably of the human.
  • composition is administered in such a way that (-)-epigallocatechin gallate is present, preferably in high concentration, in the body when the mammal selected from the group consisting of humans, cats, dogs and horses, preferably when the human, is performing the activity for which endurance is needed.
  • the dietary supplement is incorporated by said mammal at least half an hour before the intake of food, feed or beverages, even more pre- ferred at a point in time between half an hour and one and a half hour before the intake of food, feed or beverages.
  • the EGCG has a purity of at least 80%, preferably of at least 85%, more preferably of at least 90%, even more preferably of at least 92%, most preferably of at least 94%.
  • an aqueous green tea extract containing EGCG in an amount of at least 80% (preferred of at least 85%, more preferred of at least 90%, even more preferred of at least 92%, most preferred of at least 94%), based on the total amount of the extract, as e.g. and preferably obtained by any of the processes described in US 6,383,392, EP 1 103 550, US 10/246 112 and EP 1 077 211.
  • the total amount of other polyphenols and catechins such as gallocatechin gallate, catechin gallate, epicatechin gallate, epigallocatechin, gallocatechin and epicatechin is low, preferably it is ⁇ 5 weight-%, based on the total weight of the green tea extract. More preferably the amount of gallocatechin gallate is ⁇ 2.5 weight-%, and/or the amount of epicatechin gallate is ⁇ 5 weight-% (preferably ⁇ 3 weight-%), and/or the amount of caffeine is ⁇ 2.5 weight-%, preferably ⁇ 0.1 weight-%, and/or the amount of gallic acid is ⁇ 0.1 weight-%, based on the total weight of the green tea extract.
  • the dietary supplement preferably additionally contains a sympathomimeticum such as caffeine. Therefore the present invention refers to the use of a combination of EGCG and caffeine for the uses as given above. If caffeine is used in combination with EGCG the daily dosage of caffeine varies preferably from 2.5 mg per kg body weight to 7.5 mg per kg body weight.
  • the sympathetic nervous system is also stimulated by physical activity such as sport, so that sport can also be seen as sympathomimeticum. Therefore, the present invention relates also to the use of EGCG as given above, preferably of highly purified EGCG as defined above, in combination with physical activity.
  • Preferred subjects for the uses/methods of the present invention are humans.
  • the daily dosage of EGCG varies from 0.14 to 25 mg per kg body weight per day, preferably from 2.0 to 9 mg per kg body weight per day, more preferably from 4.0 to 9.0 mg per kg body weight per day, most pref- erably from 4.0 to 4.5 mg per kg body weight per day.
  • the daily dosage of EGCG varies from 10 to 1500 mg, preferably from 150 to 600 mg, more preferably from 300 to 600 mg, most preferably it is 300 mg.
  • the dietary supplement containing (-)-epigallocatechin gallate may be incorporated by the mammal simultaneously with the food, feed or beverage, respectively.
  • further objects of the present invention are: 0 Use of a dietary supplement containing (-)-epigallocatechin gallate for increasing the fat oxidation in mammals selected from the group consisting of humans, cats, dogs and horses, whereby the dietary supplement is incorporated by said mammal simultaneously with the regular intake of food, feed or beverages containing said fat whose oxidation is increased.
  • a dietary supplement containing (— )-epigallocatechin gallate for reducing the weight of a mammal selected from the group consisting of humans, cats, dogs and horses, whereby the dietary supplement is incorporated by said mammal simultaneously with the intake of food, feed or beverages.
  • a dietary supplement containing (-)-epigallocatechin gallate for reducing the fat mass in mammals selected from the group consisting of humans, cats, dogs and horses, whereby the dietary supplement is incorporated by said mammal simultaneously with the intake of food, feed or beverages.
  • a dietary supplement containing (-)-epigallocatechin gallate for reducing the carbohydrate oxidation in mammals selected from the group consisting of humans, cats, dogs and horses, whereby the dietary supplement is incorporated by said mammal simultane- ously with the regular intake of food, feed or beverages containing said carbohydrate whose oxidation is reduced.
  • the food, feed or beverage itself may be fortified with (-)-epigallocatechin gallate.
  • (-)-epigallocatechin gallate is incorporated by said mammal simultaneously with the intake of food, feed and beverages, respectively.
  • the food, feed or beverage is fortified with EGCG in such an amount so that the daily dosage of EGCG varies from 0.14 to 25 mg per kg body weight per day, preferably from 2.0 to 9 mg per kg body weight per day, more preferably from 4.0 to 9.0 mg per kg body weight per day, most preferably from 4.0 to 4.5 mg per kg body weight per day.
  • the food, feed or beverage is fortified with EGCG in such an amount so that the daily dosage of EGCG varies from 10 to 1500 mg, preferably from 150 to 600 mg, more preferably from 300 to 600 mg, most preferably it is 300 mg.
  • Experiment D 150 mg EGCG + 100 mg caffeine, one capsule, twice per day per os for two days;
  • Experiment E placebo, one capsule, twice per day per os for two days; two capsules, prior basal and one capsule prior to post-prandial measurement.
  • the study supplements were taken orally twice daily, 1.0 hours before breakfast and dinner, respectively for which specific nutritional guidelines had to be followed.
  • variable was treatment (EGCG, caffeine, placebo). Pairwise comparison across treatments was per- formed by using t-test with bonferroni's correction. A p- value smaller than 0.05 was considered significant. Values are given as mean ⁇ SD. Graphical displays were generated. If a numeric and/or statistical analysis was not possible a descriptive analysis was done.
  • the "*" indicates a statistical significance between treatment and placebo, whereas "p” represents the probability that an observed difference between the intervention and control groups is due to chance alone if the null hypothesis is true.
  • a p- value of 0.05 or less rejects the null hypothesis "at the 5% level", i.e. the statistical assumptions used imply that only 5% of the time the supposed statistical process would pro- prise a finding this extreme that the null hypothesis is true.
  • 5% and 10% are common significance levels to which p-values are compared.
  • Fig. 1 shows the difference in the respiratory quotient of the groups A to D in comparison to group E.
  • the respiratory quotient was assessed by indirect calorimetry using a Deltatrac.
  • group A, C and D the respiratory quotient was reduced in comparison to group E during basal conditions.
  • these differences were still existing or even increased.
  • the respiratory quotient was also different between group B and group E.
  • Fig. 2 shows the difference in the lipid oxidation rate of the groups A to D in comparison to group E.
  • the lipid oxidation rate was assessed by indirect calorimetry using a Deltatrac.
  • group A, B, C and D the lipid oxidation rate was increased in comparison to group E during basal conditions. During post prandial conditions these differences were more pronounced.
  • Statistical significance was observed for group C and D during basal conditions and for group D at post prandial conditions.
  • Fig. 3 shows the difference in the carbohydrate oxidation rate of the groups A to D in comparison to group E.
  • the carbohydrate oxidation rate was assessed by indirect calorimetry using a Deltatrac.
  • group A, B, C and D the carbohydrate oxidation rate was reduced in comparison to group E during basal conditions. During post prandial conditions these differences were more pronounced. Statistical significance was observed for group D during prandial conditions.
  • Fig. 4 shows the increase in the lipid oxidation rate of the groups A to D relative to group E between basal and post prandial conditions.
  • the lipid oxidation rate was assessed by indirect calorimetry using a Deltatrac. There was an increase in lipid oxidation rate from basal to post prandial conditions in group A, B, and C, whereas it was highest in group A. No change was observed for group D.
  • Fig. 5 shows the lipid oxidation rate of the groups A, C, D and E during maximum post prandial stimulation due to the test meal.
  • the lipid oxidation rate was assessed by indirect calorimetry using a Deltatrac. Lipid oxidation rate increased in group A, C, D, and E, whereas the lipid oxidation rate of group A, C and D were higher compared to group E,
  • Fig. 6 shows the synergism between groups A and C on fat oxidation during maximum post prandial stimulation.
  • the lipid oxidation rate was assessed by indirect calorimetry using a Deltatrac.
  • Group D has higher lipid oxidation than the sum of group A and group C, suggesting a synergism.
  • FIG. 8 TEAVIGOTM improves flow mediated dilation
  • Fig. 8 shows the difference in flow mediated dilation (FMD) of the groups A and E in comparison to baseline for acute (2 hours), and chronic (2 weeks) treatment.
  • FMD flow mediated dilation
  • Fig. 9 shows the difference in EGCG plasma levels the groups A and E in comparison to baseline for acute (2 hours), and chronic (2 weeks) treatment.
  • EGCG in plasma was determined by High Performance Liquid Chromatography-Mass Spectrometry.
  • group A EGCG levels were increased after acute administration.
  • group E after acute administration.
  • group E after chronic treatment.
  • the plasma EGCG level returned to baseline after chronic treatment. This is due to assessing the EGCG level 14 hours after the last administration. Therefore, EGCG does not accumulate in plasma.
  • Fig. 10 shows the lipid oxidation rate of the groups A to E.
  • the lipid oxidation rate was assessed by indirect calorimetry using a Deltatrac. In all groups the lipid oxidation rate is higher during basal conditions compared to post prandial conditions. Between groups, lipid oxidation rate in group E is lowest under the respective condition. Statistical significance was observed for group C and D during basal conditions and for group D at post prandial conditions.
  • Fig. 11 shows the carbohydrate oxidation rate of the groups A to E.
  • the carbohydrate oxidation rate was assessed by indirect calorimetry using a Deltatrac. In all groups the carbo- hydrate oxidation rate is higher during post prandial conditions compared to basal conditions. Between groups, carbohydrate oxidation rate in group E is highest under the respective condition. Statistical significance was observed for group D during post prandial.

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  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Fodder In General (AREA)
  • Feed For Specific Animals (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Medicinal Preparation (AREA)

Abstract

Utilisation de gallate de (-)-épigallocatéchine, de préférence en combinaison avec un sympathomimétique, pour augmenter/stimuler l'oxydation des graisses chez un mammifère pouvant être : homme, chat, chien et cheval, de préférence l'homme, en particulier durant les phases postprandiales; soutenir la métabolisation des graisses chez un mammifère pouvant être : homme, chat, chien et cheval, de préférence l'homme; pour réduire le poids d'un mammifère pouvant être : homme, chat, chien et cheval, de préférence l'homme; pour réduire la masse graisseuse chez un mammifère pouvant être : homme, chat, chien et cheval, de préférence l'homme; pour augmenter l'endurance pouvant être : homme, chat, chien et cheval, de préférence l'homme; pour réduire l'oxydation des hydrates de carbone chez un mammifère pouvant être : homme, chat, chien et cheval, de préférence l'homme; pour réduire le quotient respiratoire chez un mammifère pouvant être : homme, chat, chien et cheval, de préférence l'homme; et pour améliorer la dilatation à médiation par flux, contribuant ainsi aux effets bénéfiques pour la santé coronarienne, chez un mammifère pouvant être :homme, chat, chien et cheval, de préférence l'homme. Le sympathomimétique préféré est la caféine. On décrit aussi les procédés correspondants. De préférence, le gallate de (-)-épigallocatéchine a une pureté d'au moins 80 % ou plus et de préférence encore on l'élabore selon les procédés décrits dans US 6,383,392, EP 1 103 550, US 10/246 112 et EP 1 077 211.
EP06743119A 2005-06-07 2006-06-07 Nouvelle utilisation du gallate d'(-)-épigallocatechine Withdrawn EP1888173A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP06743119A EP1888173A2 (fr) 2005-06-07 2006-06-07 Nouvelle utilisation du gallate d'(-)-épigallocatechine

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP05012235 2005-06-07
EP05025412 2005-11-22
EP06743119A EP1888173A2 (fr) 2005-06-07 2006-06-07 Nouvelle utilisation du gallate d'(-)-épigallocatechine
PCT/EP2006/005410 WO2006131326A2 (fr) 2005-06-07 2006-06-07 Utilisation de gallate de (-)-epigallocatechine

Publications (1)

Publication Number Publication Date
EP1888173A2 true EP1888173A2 (fr) 2008-02-20

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EP06743119A Withdrawn EP1888173A2 (fr) 2005-06-07 2006-06-07 Nouvelle utilisation du gallate d'(-)-épigallocatechine

Country Status (4)

Country Link
EP (1) EP1888173A2 (fr)
JP (1) JP2008545766A (fr)
KR (1) KR20080020617A (fr)
WO (1) WO2006131326A2 (fr)

Families Citing this family (4)

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Publication number Priority date Publication date Assignee Title
EP1961310A1 (fr) * 2007-02-01 2008-08-27 DSMIP Assets B.V. Nouvelle utilisation du gallate d'(-)épigallocatechine
EP1969954A1 (fr) * 2007-02-01 2008-09-17 DSMIP Assets B.V. Sauce comprenant du gallate d'epigallocatechine(-)
EP2022344A1 (fr) * 2007-08-02 2009-02-11 Nestec S.A. Réduction de la fatigue grâce à l'exercice
US20110052751A1 (en) * 2007-10-10 2011-03-03 Martin Karutz Feed composition for companion animals

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Publication number Priority date Publication date Assignee Title
ATE346059T1 (de) * 1999-08-16 2006-12-15 Dsm Ip Assets Bv Verfahren zu herstellung von epigallocatechin gallate
JP3756438B2 (ja) * 2001-03-02 2006-03-15 花王株式会社 容器詰飲料
JP3756510B2 (ja) * 2001-03-02 2006-03-15 花王株式会社 体脂肪燃焼のための容器詰飲料。
JP4324335B2 (ja) * 2001-09-07 2009-09-02 花王株式会社 カテキン含有飲料
US20050256178A1 (en) * 2002-08-23 2005-11-17 Eggersdorfer Manfred L Novel nutraceutical compositions comprising boitin
CN100361599C (zh) * 2002-10-23 2008-01-16 克尔塞根控股有限公司 抗氧化组合物
JP4494033B2 (ja) * 2003-02-10 2010-06-30 株式会社 伊藤園 血清コレステロール低下剤、飲食物およびその製造方法
DE602004022806D1 (de) * 2003-06-04 2009-10-08 Nestec Sa Getränk zur gewichtskontrolle
US20050008712A1 (en) * 2003-07-08 2005-01-13 Debasis Bagchi Compositions incorporating high-caffeine green tea extract and related methods for promoting healthy body weight
AU2004257756A1 (en) * 2003-07-10 2005-01-27 Carl A. Forest Foods, beverages, condiments, spices and salad dressings with specialized supplements
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See references of WO2006131326A2 *

Also Published As

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WO2006131326A2 (fr) 2006-12-14
WO2006131326A3 (fr) 2007-07-19
JP2008545766A (ja) 2008-12-18
WO2006131326B1 (fr) 2007-11-01
KR20080020617A (ko) 2008-03-05

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