Bryoid compositions, methods of making and use thereof
Inventors
Assignees
Publication Number
US-10954248-B2
Publication Date
2021-03-23
Expiration Date
2033-11-26
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Abstract
Embodiments of the present invention feature novel Bryoid compositions, methods of making and methods of treating disease.
Core Innovation
Embodiments of the present invention feature several novel Bryoid compositions, specifically four characterized Bryoid compounds (B10, B12, B14B, and B14C) with unique molecular weights distinct from bryostatins 1-20. These compositions are provided at a range of purities including high, crystal forming purity, and are described by precise mass measurements for both monoisotopic and sodium-adduct forms. The invention also includes methods for isolating and purifying these Bryoid compositions from sources such as Bugula neritina.
The background identifies neurodegenerative diseases, such as Alzheimer's, Parkinson's, and Hutchinson's diseases, as major health problems with limited treatment options. These diseases are associated with beta amyloid plaque formation. The invention addresses the need for new, potent Bryoid compounds by providing specific Bryoid analogues that act as potent modulators of protein kinase C (PKC) and amyloid precursor protein, with activities at least as high as or greater than bryostatin 1. Additionally, the invention has relevance for amyloid-mediated diseases, virus latency diseases such as HIV and Herpes, and cancers including prostate cancer.
The invention describes detailed processes for obtaining, purifying, and characterizing these novel Bryoid compounds. This includes extraction with organic or supercritical fluids, sequential chromatographic purification steps, and crystallization to achieve high purity. The methods presented aim to generate Bryoid compositions suitable for therapeutic use in various Bryoid-responsive conditions.
Claims Coverage
There is one independent claim described, containing a main inventive feature regarding a method of making a specific Bryoid composition.
Method of making a first Bryoid composition with defined molecular weight and purity
The inventive feature covers: - Isolating a first Bryoid composition from a source of Bryoids. - Purifying the first Bryoid composition to a range from 50% to a crystal forming purity. - Defining the first Bryoid composition as having a molecular weight of approximately 896-898 Amu (Mass+Sodium) and 873-875 Amu (monoisotopic mass).
The independent claim establishes the method for obtaining a Bryoid composition that meets strict molecular weight and purity criteria, specifically distinguishing it from other known bryostatins.
Stated Advantages
The Bryoid compositions of the present invention possess high potency and activity.
These compositions are highly active modulators of certain isoforms of protein kinase C (PKC) and amyloid precursor protein.
The compositions stimulate the production of alpha-secretase, leading to the transformation of amyloid precursor protein into soluble forms and potentially inhibiting the formation of beta amyloid plaques.
The Bryoid compositions exhibit levels of biological activity similar to or greater than bryostatin 1.
Documented Applications
Treatment of neurodegenerative diseases such as Hutchinson Disease, Parkinson's disease, Down's syndrome, Alzheimer's disease, and amyloid mediated diseases such as glaucoma.
Treatment of virus latency diseases such as HIV and Herpes.
Treatment of cancers including prostate cancer.
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