# US 7,407,778 B2 · Compounds, compositions and methods for treating neuropsychiatric disorders

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- Number: US 7,407,778 B2
- Document ID: US7407778B2
- Status: Granted
- Kind: B2
- Application number: 11/198,761
- Filed: 2005-08-05
- Published: 2006-04-27
- Granted: 2008-08-05
- Earliest claimed: 2002-02-07
- Inventors: Jay W. Pettegrew; Samuel Gershon; Kanagasabai Panchalingam
- Web page: https://patentgrep.com/patent/US7407778B2

## CPC

- A61K 36/28: Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
- A23L 33/175: Amino acids
- A61K 31/205: Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
- A61K 31/22: of acyclic acids, e.g. pravastatin
- A61K 31/221: with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
- A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)
- A23V: INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION

## Abstract

Acetyl-L-carnitine (ALCAR) and L-carntine (LCAR) are nutraceuticals with indications in treating a variety of mental health disorders. A metabolomics-guided bioprocess method is presented to enhance ALCAR and LCAR formation in germinating plant seeds. Metabolic fluxes are manipulated by germination in bioreactors to increase oxygen availability as well as provide an aseptic environment to alter carbohydrate consumption and feedback repress gluconeogenesis. Large shifts in sunflower seed fatty acid, phospholipid and high-energy metabolism change the germination environment and these metabolic changes lead to an approximate 1000-fold increase in natural LCAR and ALCAR production by the seeds. The resulting LCAR and ALCAR products from the seeds are used for treating mental health disorders including Alzheimer's disease, geriatric depression, non-geriatric depression and schizophrenia.

## Claims

### Claim 1

A method for producing a pharmaceutical composition comprising:
i) a manipulated germination process wherein a sucrose controlled and oxygen controlled environment are applied to a plurality of germinating sunflower seeds to enhance the generation of a metabolite selected from L-camitine (LCAR), acetyl-L-camitine (ALCAR) and combinations thereof wherein the oxygen controlled environment includes at least 40% O2;
ii) isolating said metabolite therefrom by solvent extraction; and
iii) mixing said metabolite with one or more pharmaceutically acceptable carriers or excipients.

### Claim 2

A method for producing L-camitine (LCAR) and acetyl-L-camitine (ALCAR), comprising:
i) enhancing fatty acid β-oxidation with sucrose suppression of a plurality of germinating sunflower seeds; and
ii) stimulating β-oxidation of the fatty acids in the plurality of sunflower seeds with an oxygen enhanced environment for a pre-determined time period, wherein the oxygen enhanced environment comprises at least 40% O2,
thereby enhancing LCAR and/or ALCAR synthesis in the plurality of germinating sunflower seeds.

### Claim 3 (depends on 2)

The method of claim 2 further comprising: extracting LCAR and ALCAR from the plurality of germinating sunflower seeds by contacting said seeds with an organic solvent.

### Claim 4 (depends on 3)

The method of claim 3 wherein the step of extracting LCAR and ALCAR from the plurality of germinating sunflower seeds comprises contacting said seeds with an organic solvent or solvents selected from the group consisting of hexane, methylene chloride and methyl alcohol.

### Claim 5 (depends on 4)

The method of claim 4 further comprising contacting said extracted LCAR and ALCAR with a pharmaceutically acceptable carrier(s) or excipient(s) to generate a pharmaceutically acceptable composition suitable for human consumption.

### Claim 6

A method for producing L-camitine (LCAR) and/or acetyl-L-camitine (ALCAR), comprising:
i) enhancing fatty acid β-oxidation with sucrose suppression of a plurality of glycoxylate cycles in a plurality of germinating sunflower seeds over a pre-determined time period; and
ii) stimulating β-oxidation of the fatty acids in the plurality of sunflower seeds with O2 for a pre-determined time period, wherein the O2 enhanced environment comprises at least 40% O2,
thereby enhancing LCAR and/or ALCAR synthesis in the plurality of germinating sunflower seeds.