Method to increase the bioavailability of cysteine

• US 7,678,833 B2
• Filed: 05/23/2007
• Issued: 03/16/2010
• Est. Priority Date: 05/24/2006
• Status: Active Grant

• Current Assignee: Allium Vitalis Inc.
• Original Assignee: Allium Vitalis Inc.
• Inventors: Ott, David M.
• Primary Examiner(s): Russel; Jeffrey E
• Application Number:
  US11/805,637
• Publication Number:
  US 20070275876A1
• Time in Patent Office: 1,028 Days
• Field of Search: None
• US Class Current: 514/706
• CPC Class Codes: A61K 31/095 Sulfur, selenium, or tellurium compounds, e.g. thiols

Abstract

A method for increasing the bioavailability of cysteine within an animal by reducing extracellular cysteine disulfide molecules to produce extracellular cysteine molecules. A membrane permeable thiol molecule that forms a membrane permeable disulfide molecule after becoming oxidized participates in thiol-disulfide exchange reactions on both sides of the cellular membrane, crossing the membrane randomly via simple diffusion. The membrane permeable disulfide, within or upon entering the highly reductive environment of a cell, becomes reduced to form a membrane permeable thiol molecule. the membrane permeable thiol can then diffuse to the exterior of the cell, where it is available to reduce another cystine molecule. This process can continue cycling, producing net cumulative increase in the concentration of extracellular cysteine. This is beneficial for providing cysteine as a nutrient to cells that require cysteine for nourishment.

Claims

1. A method of treating a cysteine depletion dependent disease or condition selected from the group consisting of

(a) the condition of hyperpigmentation associated with the disease of arsenicosis,

(b) the condition of glycated hemoglobin associated with the disease of diabetes,

(c) the condition of glycated low density lipoprotein associated with cardiovascular disease,

(d) the condition of the loss of skeletal muscle associated with the disease of AIDS,

(e) the condition of the loss of skeletal muscle associated with a disease of cancer,

(f) the condition of super-optimal glycation products due to an insufficient rate of transglycation,

(g) the condition of the loss of skeletal muscle due to physiological aging, or

(h) the condition of muscle fatigue due to a high level of activation of the immune system

said method comprising:

administering to an animal in need thereof an effective amount of a composition comprising a membrane permeable thiol in the form of said membrane permeable thiol itself or in the form of said membrane permeable thiol disulfide bonded to protein that metabolizes in vivo to produce said membrane permeable thiol;

wherein said membrane permeable thiol reduces extracellular cystine or a mixed cysteine disulfide to produce extracellular cysteine and is concurrently oxidized to a disulfide or mixed disulfide;

wherein said disulfide or mixed disulfide is membrane permeable or forms a membrane permeable disulfide or membrane permeable mixed disulfide, which upon cell entry is reduced and re-forms said membrane permeable thiol.

2. The method of claim 1, wherein said administering of said composition produces an increase in the bioavailability of cysteine in said animal.

3. The method of claim 2, wherein said administering of said composition produces an increase in the ratio of plasma cysteine to cystine in said animal.

4. The method of claim 2, wherein said administering of said composition produces an increase in the amount of intracellular glutathione in said animal.

5. The method of claim 1, wherein said administering of said composition produces an increase in the level of plasma albumin in said animal.

6. The method of claim 1, 2, 3, 4, or 5 wherein said membrane permeable thiol is allyl mercaptan or propyl mercaptan in an effective amount up to 5,000 mg per daily dosage.

7. The method of claim 6 wherein said membrane permeable thiol is administered in the form of a mixed disulfide with protein in a dosage sufficient for the composition to metabolize to said membrane permeable thiol in an effective amount up to 250 mg per daily dosage.

8. The method of claim 7 wherein said composition is a nutraceutical.

9. The method of claim 7 wherein said composition is a dietary supplement.

10. The method of claim 6 wherein said composition is a drug.

11. The method of claim 1, 2, 3, 4, or 5 wherein said animal is a human.

12. The method of claim 1, wherein said animal is afflicted by the disease of arsenicosis and said condition is hyperpigmentation.

13. The method of claim 1, wherein said animal is afflicted by the disease of diabetes and said condition is glycated hemoglobin.

14. The method of claim 1, wherein said animal is afflicted by cardiovascular disease and said condition is glycated low density lipoprotein.

15. The method of claim 1, wherein said animal is afflicted by the disease of AIDS and said condition is the loss of skeletal muscle.

16. The method of claim 1, wherein said animal is afflicted by the disease of cancer and said condition is the loss of skeletal muscle.

17. The method of claim 1, wherein said animal is afflicted with the condition of super-optimal glycation products due to an insufficient rate of transglycation.

18. The method of claim 1, wherein said animal is afflicted by physiological aging and said condition is loss of skeletal muscle.

19. The method of claim 1, wherein said animal is afflicted with the condition of muscle fatigue due to a high level of activation of the immune system.