Bryoid compositions, methods of making and use thereof
Inventors
Assignees
Publication Number
US-11639359-B2
Publication Date
2023-05-02
Expiration Date
2038-12-04
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Abstract
Embodiments of the present invention feature novel Bryoid compositions, methods of making and methods of treating disease.
Core Innovation
The invention features novel Bryoid compositions, specifically four Bryoid compounds named B10, B12, B14B, and B14C, with distinct molecular weights not previously identified among known bryostatins (1-20). These compositions are characterized by specific molecular weight ranges, crystal forming purity reaching above 90%, and unique structural features as confirmed by analytical techniques such as HPLC and NMR.
The problem addressed by the invention is the need for new, potent Bryoid compounds with high activity for the treatment of various diseases, including neurodegenerative diseases (such as Alzheimer's, Hutchinson's, and Parkinson's), cancers (including prostate cancer), and virus latency diseases (such as HIV and Herpes). Current treatment options for these conditions are very limited, particularly for neurodegenerative diseases, which are associated with beta amyloid plaque formation.
The Bryoid compositions of the invention have utility as therapeutics due to their ability to modulate protein kinase C (PKC) isoforms and amyloid precursor protein, stimulating the production of alpha-secretase, which transforms amyloid precursor protein into soluble forms and inhibits the formation of beta amyloid plaques. These Bryoids demonstrate in vitro activity equal to or exceeding that of Bryostatin-1, as shown in neuroblastoma cell assays measuring alpha-secretase and PKC activity.
The invention also provides methods for purifying these Bryoid compositions from Bugula neritina to high levels of purity suitable for therapeutic use, as well as pharmaceutical dosage forms and methods of treating diseases that respond to Bryoid administration.
Claims Coverage
There is one independent claim in the patent, which covers the main inventive features related to making the second Bryoid composition with specified purification levels and molecular weights.
Method of making a second Bryoid composition with defined molecular weight and purity
A method comprising the steps of isolating a second Bryoid composition from a source of Bryoids and purifying the second Bryoid composition in a range from 50% to a crystal forming purity, where the second Bryoid composition has: - A molecular weight of approximately 910-912 Amu (Mass + Sodium) - A monoisotopic mass of approximately 888-890 Amu The process involves obtaining the Bryoid from a suitable source and achieving high purity within the stated measured mass constraints.
The claim coverage is focused on a method for isolating and purifying a novel second Bryoid composition with specific molecular characteristics and high purity.
Stated Advantages
The Bryoid compositions possess high potency and activity.
The Bryoid compositions exhibit high levels of activity similar to or greater than bryostatin 1.
The Bryoid compositions are highly active modulators of certain isoforms of protein kinase C (PKC) and amyloid precursor protein.
Certain Bryoid compositions improve the production of alpha-secretase and PKC isoforms over Bryostatin-1 in neuroblastoma cells.
Documented Applications
Therapeutic use in neurodegenerative diseases such as Hutchinson Disease, Parkinson's disease, Down's syndrome, and Alzheimer's disease.
Treatment of virus latency diseases such as HIV and Herpes.
Treatment of cancers including prostate cancer.
Treatment of other amyloid mediated diseases such as glaucoma.
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