Tomatidine, analogs thereof, compositions comprising same, and uses for same
Inventors
Adams, Christopher M. • DYLE, Michael C. • Welsh, Michael
Assignees
University of Iowa Research Foundation UIRF • US Department of Veterans Affairs
Publication Number
US-9254295-B2
Publication Date
2016-02-09
Expiration Date
2033-08-02
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Abstract
In one aspect, the invention relates to methods for promoting muscle hypertrophy or decreasing adiposity by providing to an animal in need thereof an effective amount of a compound. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Core Innovation
The invention relates to methods for promoting muscle hypertrophy or decreasing adiposity by providing an effective amount of compounds to animals in need thereof. The compounds disclosed include tomatidine and analogs thereof, which can promote muscle hypertrophy, decrease adiposity, treat muscle atrophy, promote muscle health, promote normal muscle function, and/or promote healthy aging muscles in animals such as mammals, birds, or fish, including humans. The invention also discloses pharmaceutical compositions comprising these compounds and related kits and methods for manufacture of medicaments associated with muscle atrophy and muscle health.
The background describes a significant medical need due to the widespread occurrence of skeletal muscle atrophy, which is common in aging, starvation, and severe diseases such as cancer and chronic illnesses, leading to serious health complications without existent effective medical therapies. Atrophy is linked to impaired signaling pathways, particularly insulin/IGF1 signaling, which promotes muscle hypertrophy and inhibits muscle atrophy but is reduced under atrophy-inducing stresses. Additionally, obesity caused by high adiposity presents major health problems, with current treatments insufficient to address these issues effectively.
The invention addresses these needs by providing compounds that are potent, efficacious, and selective modulators of muscle growth that can also effectively treat muscle atrophy conditions and decrease adiposity. Tomatidine, a natural steroidal alkaloid derived from tomato plants, is demonstrated to have such beneficial effects, including promotion of muscle hypertrophy, increase of muscle strength, increase of exercise capacity, and reduction of adiposity, all without evidence of toxicity. These compounds fulfill the need for therapies that can modulate muscle mass and adiposity beneficially.
Claims Coverage
The claims include one independent claim focused on a method for promoting muscle health, normal muscle function, and/or healthy aging of skeletal muscle by administering a compound of defined structure at specified concentrations. The main inventive features focus on the compound's structure and dosage in the administered solution or preparation.
Use of a specific compound to promote muscle health and function
Administering to an animal a solution, dispersion, suspension or emulsion containing not less than 0.14% by weight of a compound having a defined steroidal alkaloid structure for promoting muscle health, normal muscle function, and/or healthy aging of skeletal muscle.
Specific structural definition of the compound
The compound has a specific structure represented by formula E1 with variants where R51 is selected from H and C1-C6 alkyl, and R54 is H or other defined substituents, including a defined steroidal framework.
Concentration of the compound in the composition
The composition can comprise the compound at not less than 0.28% by weight, indicating dosing ranges relevant to effective administration.
Amount of the compound administered
The compound is present in an administered amount greater than 5 mg, detailing the effective dosage range for therapeutic benefit.
The claims cover methods of treatment involving administration of defined steroidal alkaloid compounds, including tomatidine or analogs, at effective concentrations and doses to promote muscle health, function, and aging in skeletal muscle of animals, emphasizing specific chemical structure and dosage ranges.
Stated Advantages
The compounds have the ability to promote muscle hypertrophy, increase muscle strength, and increase exercise capacity.
The compounds decrease adiposity and fat mass in animals.
The compounds can treat or prevent muscle atrophy, including that associated with various diseases and aging.
Tomatidine and analogs have a favorable safety profile without evidence of toxicity.
Documented Applications
Promoting muscle hypertrophy in animals including humans and other mammals, fish, or birds.
Decreasing adiposity or fat mass in animals including those with obesity or high body fat.
Treating muscle atrophy caused by malnutrition, diseases (e.g., cancer, chronic diseases), immobilization, aging, and other conditions.
Promoting muscle health, normal muscle function, and healthy aging muscles.
Increasing anabolic signaling, protein synthesis, mitochondria in muscle cells, muscle strength, and exercise capacity.
Pharmaceutical and nutraceutical compositions comprising tomatidine or analogs for the above treatments.
Use in livestock and domesticated animals to increase muscle mass and potentially improve meat production.
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