WO2000072854A1 - Complement alimentaire contenant un sulfate vanadyl, un acide alpha-lipoique et une taurine - Google Patents
Complement alimentaire contenant un sulfate vanadyl, un acide alpha-lipoique et une taurine Download PDFInfo
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- WO2000072854A1 WO2000072854A1 PCT/US2000/015196 US0015196W WO0072854A1 WO 2000072854 A1 WO2000072854 A1 WO 2000072854A1 US 0015196 W US0015196 W US 0015196W WO 0072854 A1 WO0072854 A1 WO 0072854A1
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- composition
- alpha
- lipoic acid
- sulfate
- taurine
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- AGBQKNBQESQNJD-UHFFFAOYSA-N lipoic acid Chemical compound OC(=O)CCCCC1CCSS1 AGBQKNBQESQNJD-UHFFFAOYSA-N 0.000 title claims abstract description 44
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 title claims abstract description 34
- 235000019136 lipoic acid Nutrition 0.000 title claims abstract description 22
- 229960002663 thioctic acid Drugs 0.000 title claims abstract description 22
- 235000015872 dietary supplement Nutrition 0.000 title claims abstract description 19
- 229960003080 taurine Drugs 0.000 title claims abstract description 17
- UUUGYDOQQLOJQA-UHFFFAOYSA-L vanadyl sulfate Chemical compound [V+2]=O.[O-]S([O-])(=O)=O UUUGYDOQQLOJQA-UHFFFAOYSA-L 0.000 title claims abstract description 15
- 229940041260 vanadyl sulfate Drugs 0.000 title claims abstract description 15
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Classifications
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/17—Amino acids, peptides or proteins
- A23L33/175—Amino acids
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
Definitions
- the present ⁇ n ⁇ ention relates generally to dietary supplements and more particularly, to a formulation of ⁇ anadyl sulfate. alpha-hpoic acid, and tau ⁇ ne to augment or normalize cellular t rosine phosphorvlation responses to insulin thereby decreasing catabolic activity in the diabetic state and decreasing serum hpoproteins and maintaining normal bodv weight in diabetic. HIV-infected and healthy humans and animals
- Insulin binding causes conformational changes in insulin receptor that lead to autophosphorvlation of the receptor and activation of the receptor ' s intrinsic tvrosine kinase activity
- the function of the tvrosine kinase of insulin receptor is essential for the biological effects of insulin After autophosphorylation, insulin receptor can phosphorvlate the tyrosine residues of several substrates, including insulin
- receptor substrate (IRS) proteins which in turn can activate downstream signaling molecules in the liver and muscle cells
- PTP-1 B protein tvrosine phosphatase termed PTP-1 B can terminate the signalling cascade initiated bv insulin b ⁇ removing the phosphate from insulin receptor Studies indicate that
- NIDDM non-insulin dependent diabetes melhtus
- Vanadate is known to be an inhibitor of many phosphatases Some researchers have proposed that vanadate administration may mimic the activity of insulin
- U S patent 5 550 1 13 and U S patent 5 888 993 disclose vanadium salts for blood sugar regulation
- U S Patent 5 885 980 and U S Patent 5,614,224 disclose vanadium salts for the treatment of diabetes
- Vanadyl sulfate is not widely used to mimic the activity of insulin because chronic administration of vanadate can be toxic Vanadyl sulfate has been shown to induce chromosomal damage and mitotic recombination in the fruit fly Vanadyl sulfate can induce pulmonary inflammation in rats when inhaled In vitro studies of bovine papilloma virus
- vanadvl sulfate Given the potential usefulness of vanadvl sulfate in the treatment ot diabetes it would be desirable to administer compositions containing vanadvl sulfate to diabetic patients, HIV- mfected and normal individuals wishing to minimize their risk of developing NEDDM, if the undesirable side effects of vanadate could be avoided
- a dietary supplement that comprises vanadvl sulfate alpha-hpoic acid, and tau ⁇ ne
- the present supplement (1) increases cell sensitivity to insulin, (n) maintains normal serum glucose, (in) decreases hypert ⁇ glyce ⁇ demia and/or hpoproteins, and (iv) maintains normal body weight even with consumption of a high fat diet
- the supplement can be used by normal, healthy individuals as well as diabetics or persons infected with the HIV virus
- the present invention also provides a method of dietary supplementation in animals which includes administering to an animal suffering symptoms of diabetes a composition including synergisticaliy effective amounts of vanadyl sulfate alpha-hpoic acid and tau ⁇ ne and continuing administration of the composition until the svmptoms are reduced
- the present inv ention further provides a method of dietary supplementation in animals which includes administering to an animal a composition which includes svnergistically effective amounts of v anadvl sulfate. alpha-hpoic acid and tau ⁇ ne and continuing administration of the composition until normalization of serum glucose is achieved
- the present invention still further provides a method of dietary supplementation in animals which includes administering to an animal a composition w hich includes synergisticaliy effective amounts of vanadvl sulfate, alpha-hpoic acid and tau ⁇ ne and continuing administration of the composition until normalization of serum t ⁇ glye ⁇ ceds is achieved
- the present invention additionally provides a method of treating obesity in an animal which includes administering to an animal a composition including synergisticaliy effective amounts of vanadvl sulfate, alpha-hpoic acid and tau ⁇ ne
- the animal is a mammal selected from the group consisting of humans nonhuman primates, dogs, cats, horses or cattle Administration can be bv anv method available to the skilled artisan, for example, bv oral and by injection routes
- Figure 1 provides a schematic diagram illustrating, according to the present invention, how the components of the present formulation vanadvl sulfate.
- alpha-hpoic acid and tau ⁇ ne can act together to enhance augment or 3 pare [modulate 9 ] the effect of insulin on liver, muscle or fat cells
- the tyrosine kinase signaling pathway is initiated through the interaction of insulin and the insulin receptor (IR), leading to the phosphorylation of insulin receptor PTP-1B can remove the phosphate from insulin receptor, thereby inactivating its kinase activity
- Vanadvl sulfate can block the activity of phosphatases like
- the present invention provides a composition that can be taken as a dietary supplement which includes v anadvl sulfate alpha-hpoic acid, and tau ⁇ ne
- v anadvl sulfate alpha-hpoic acid and tau ⁇ ne
- Each of these individual components affect the insulin-induced chain of activities to some degree
- the resulting dietary supplement addresses the decreased insulin sensitivity and secondary pathologies associated with diabetes, HIV infection normal aging and with NIDDM
- compounds which inhibit PTP- 1 B can be used to prevent and treat obesitv diabetes and the side effects of HIV infection
- Vanadyl sulfate can inhibit PTP- IB but its toxicitv prevents chronic administration and widespread acceptance
- vanadvl sulfate can be used in such small dosages that it will not be toxic
- the present composition works synergisticaliy to enhance signaling by stimulating PI-3k with alpha-hpoic acid and by increasing the amount of phosphorvlated IRS- 1 with vanadvl sulfate which maintains high levels of insulin receptor kinase activity (see Figure 1 ) Attacking the insulin activated cascade of events in at two different places by administering by vanadyl sulfate and alpha-hpoic acid, permits administration of lower dosages of vanadyl sulfate, thereby reducing the potential for adverse side effects
- the combination of vanadyl sulfate, alpha-hpoic acid and tau ⁇ ne works synergisticaliy to mimic not only insulin's glucose- normalizing properties but also insulin's lipid-lowe ⁇ ng properties
- the activation of the phosphodiesterase and production of c-AMP is independent of the tyrosine phosphorvlation of IRS- 1 and subsequent PI-3k activation
- tau ⁇ ne and its effect on c- AMP provides s ⁇ nergistic lowering of hpids when combined with ⁇ anadyl sulfate and alpha- lipoic acid
- the current inv ention is designed to normalize insulin action in both glucose tolerance and weight management
- the current invention may be consumed by healthy persons wishing to decrease their odds of (l) developing NIDDM (n) exhibiting high serum hpoprotein levels and (in) gaining weight on high fat diets
- v anadvl sulfate lipoic acid and tau ⁇ ne suggested bv the present invention is unique (1) it prov ides a dietan, formulation for the maintenence of normal insulin action at the insulin receptor that can be consumed by healthy persons as well as diabetics; (ii) it can be taken orally; (ii) it maintains its insulin-sparing activity over many months; (iv) it normalizes serum glucose levels; (v) it normalizes serum lipoprotein levels; (vi) it is safe over long periods of time; (vii) it can be used to maintain normal body weight on high-fat diets; and (viii) it can be cost-effective.
- HTV-infected persons can be treated with the present formulations to normalize insulin sensitivity and prevent the abnormal redistribution of fat.
- protease therapy for the treatment of HIV infection, persons may now live with the infection for a substantially longer period of time.
- a syndrome similar to type II diabetes has been observed among these long-term survivors where fat is abnormal distributed and insulin sensitivity is decreased.
- estimates of the prevalence of this svndrome range from 20 to 70 percent in the HIV-infected population. While it is not known whether this syndrome is due to the combinations of anti-HIV drugs used or to changes in metabolism induced by the virus, the present methods and formulations can be used to treat it, by normalizing insulin sensitivity and fat distribution.
- Vanadyl sulfate, alpha-lipoic acid and taurine can be obtained commercially, for example, as pharmaceutical grade preparations with a purity of greater than
- Vanadyl sulfate can be purchased from Spectrum Chemicals MFG, Corp (Gardena, CA).
- Alpha-lipoic acid can be obtained from Technical Sourcing International, (Missoula, MT) and taurine can be obtained from Premium Ingredients, Ltd. The currently proposed formulation of these three agents does not exist commercially.
- a daily dose (mg/kg-day) of the present dietary supplement would be formulated to deliver per kg body weight of the mammal the following active ingredients within the suggested ranges: (a) about 0.7 ⁇ g/kg to 1.4 mg/kg vanadyl sulfate; (b) about 1.4 to 71 mg kg alpha-lipoic acid; and (c) about 7 to 43 mg/kg taurine.
- the relative amount of the individual components would vary to optimize cost-effectiveness and biochemical svnergy.
- the present dietary supplement mav include complementary herbs v arious additives such as other vitamins and minerals as well as inert ingredients such as talc and magnesium stearate that are standard excipients in the manulacture ol tablets and capsules
- complementary herbs v arious additives such as other vitamins and minerals as well as inert ingredients such as talc and magnesium stearate that are standard excipients in the manulacture ol tablets and capsules
- Other ingredients to affect the manufacture of this formulation as a dietary bar or functional food would obviously include flavorings sugars modified starches, grain products as well as fats and oils
- composition of the dietary supplement in capsule form would supply the follow ing amounts of active ingredients per kg body weight per day (a) 0 4 mg/kg v anadvl sulfate (b) 3 mg/kg alpha-lipoic acid (c) 14 mg/kg taurine Improvement in glucose utilization in the diabetic state would be expected to occur following one to two doses Additionally the formulation mav be used to support or normalize serum hpoprotein levels in nondiabetic subjects This result would be expected in all mammals within one to two weeks
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- Life Sciences & Earth Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Mycology (AREA)
- Health & Medical Sciences (AREA)
- Nutrition Science (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
L'invention concerne un complément alimentaire ou une composition thérapeutique servant à (i) augmenter la sensibilité du muscle, du foie ou des cellules grasses à l'insuline, (ii) à maintenir un glucose de sérum normal, (iii) à diminuer les lipoprotéines de sérum et (iv) à maintenir un poids du corps normal avec la consommation d'un régime très gras. Le complément peut être utilisé par des personnes normales, des individus en bonne santé, des personnes infectées par le VIH et souffrant de diabète. La composition préférée du complément alimentaire sous forme de capsule est à même de fournir la quantité suivante de principes actifs par poids corporel en kilo par jour : (a) environ 0,4 mg/kg de sulfate vanadyl; (b) environ 3,0 mg/kg d'acide alpha-lipoïque et (c) environ 14 mg/kg de taurine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU57255/00A AU5725500A (en) | 1999-06-02 | 2000-06-02 | A dietary supplement containing vanadyl sulfate, alpha-lipoic acid, and taurine |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13708099P | 1999-06-02 | 1999-06-02 | |
| US60/137,080 | 1999-06-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2000072854A1 true WO2000072854A1 (fr) | 2000-12-07 |
Family
ID=22475744
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US2000/015196 WO2000072854A1 (fr) | 1999-06-02 | 2000-06-02 | Complement alimentaire contenant un sulfate vanadyl, un acide alpha-lipoique et une taurine |
Country Status (2)
| Country | Link |
|---|---|
| AU (1) | AU5725500A (fr) |
| WO (1) | WO2000072854A1 (fr) |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001056402A2 (fr) * | 2000-02-01 | 2001-08-09 | Muscletech Research And Development Inc. | Complement alimentaire a base d"acide $g(a)-lipoique destine a la masse maigre et a la resistance musculaire |
| WO2002013814A1 (fr) * | 2000-08-11 | 2002-02-21 | The Lawson Health Research Institute | Compositions enrayant un dysfonctionnement des ilots de langerhans ainsi que des maladies auto-immune et methodes afferentes |
| EP1330957A2 (fr) * | 2002-01-15 | 2003-07-30 | Karl-Heinz Bauer | Supplement nutritive |
| WO2003101469A1 (fr) * | 2002-06-04 | 2003-12-11 | Metaproteomics, Llc | Composition orale insulinoide et procedes d'utilisation correspondants |
| KR100427637B1 (ko) * | 2001-06-05 | 2004-04-27 | 이인규 | 세포내 에너지 소비 증가제 |
| US8715717B2 (en) * | 2003-09-05 | 2014-05-06 | Hill's Pet Nutrition, Inc. | Composition for animal consumption |
| US20180092878A1 (en) * | 2015-05-21 | 2018-04-05 | Ophtalmis Monaco | Combination of lipoic acid and taurine as osmoprotective agent |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4751085A (en) * | 1984-08-29 | 1988-06-14 | Gaull Gerald E | Human nutritional compositions containing taurine and vitamins and/or minerals |
| US5693664A (en) * | 1993-12-21 | 1997-12-02 | Asta Medica Aktiengesellschaft | Use of R-(+)-α-lipoic acid, R-(-)dihydrolipoic acid and metabolites in the form of the free acid or salts or esters or amides for the preparation of drugs for the treatment of diabetes mellitus as well as of its sequelae |
| US5730988A (en) * | 1995-04-20 | 1998-03-24 | Lynntech, Inc. | Nutritional supplements for improving glucose metabolism |
-
2000
- 2000-06-02 AU AU57255/00A patent/AU5725500A/en not_active Abandoned
- 2000-06-02 WO PCT/US2000/015196 patent/WO2000072854A1/fr active Application Filing
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4751085A (en) * | 1984-08-29 | 1988-06-14 | Gaull Gerald E | Human nutritional compositions containing taurine and vitamins and/or minerals |
| US5693664A (en) * | 1993-12-21 | 1997-12-02 | Asta Medica Aktiengesellschaft | Use of R-(+)-α-lipoic acid, R-(-)dihydrolipoic acid and metabolites in the form of the free acid or salts or esters or amides for the preparation of drugs for the treatment of diabetes mellitus as well as of its sequelae |
| US5730988A (en) * | 1995-04-20 | 1998-03-24 | Lynntech, Inc. | Nutritional supplements for improving glucose metabolism |
Cited By (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001056402A2 (fr) * | 2000-02-01 | 2001-08-09 | Muscletech Research And Development Inc. | Complement alimentaire a base d"acide $g(a)-lipoique destine a la masse maigre et a la resistance musculaire |
| WO2001056402A3 (fr) * | 2000-02-01 | 2002-08-22 | Muscletech Res And Dev Inc | Complement alimentaire a base d"acide $g(a)-lipoique destine a la masse maigre et a la resistance musculaire |
| WO2002013814A1 (fr) * | 2000-08-11 | 2002-02-21 | The Lawson Health Research Institute | Compositions enrayant un dysfonctionnement des ilots de langerhans ainsi que des maladies auto-immune et methodes afferentes |
| WO2002013813A1 (fr) * | 2000-08-11 | 2002-02-21 | The Lawson Health Research Institute | Inhibition du dysfonctionnement des îlots de langerhans et de troubles autoimmunes, et compositions à cet effet |
| KR100427637B1 (ko) * | 2001-06-05 | 2004-04-27 | 이인규 | 세포내 에너지 소비 증가제 |
| EP1330957A2 (fr) * | 2002-01-15 | 2003-07-30 | Karl-Heinz Bauer | Supplement nutritive |
| EP1330957A3 (fr) * | 2002-01-15 | 2003-10-22 | Karl-Heinz Bauer | Supplement nutritive |
| WO2003101469A1 (fr) * | 2002-06-04 | 2003-12-11 | Metaproteomics, Llc | Composition orale insulinoide et procedes d'utilisation correspondants |
| US6733793B2 (en) | 2002-06-04 | 2004-05-11 | Metaproteomics, Llc | Oral composition with insulin-like activities and methods of use |
| US8715717B2 (en) * | 2003-09-05 | 2014-05-06 | Hill's Pet Nutrition, Inc. | Composition for animal consumption |
| US20180092878A1 (en) * | 2015-05-21 | 2018-04-05 | Ophtalmis Monaco | Combination of lipoic acid and taurine as osmoprotective agent |
| US11224588B2 (en) * | 2015-05-21 | 2022-01-18 | Ophtalmis Monaco | Combination of lipoic acid and taurine as osmoprotective agent |
Also Published As
| Publication number | Publication date |
|---|---|
| AU5725500A (en) | 2000-12-18 |
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