Aphios Granted European Patent for Novel Bryostatin to Treat Alzheimer’s Disease, HIV-1, and Cancers
March 26, 2019WOBURN, Mass.–(BUSINESS WIRE)–lt;a href="https://twitter.com/hashtag/Alzheimer?src=hash" target="_blank"gt;#Alzheimerlt;/agt;–Aphios Corporation today announced that it has been granted European
Patent No. 2 925 315 B1 entitled “Bryoid Compositions, Methods of Making
and Use Thereof,” for the composition of matter of a novel Bryostatin,
method of manufacturing and for use in the treatment of
neurodegenerative diseases such as Alzheimer’s, Parkinson’s, Down’s
syndrome, Hutchinson’s and Multiple Sclerosis; virus latency diseases
such as HIV and Herpes; cancers such as prostate and leukemia; and
amyloid mediated diseases such as glaucoma.
Bryoids consist of a family of Bryostatins, such as Bryostatin-1, that
are complex cyclic macrolide molecules. Bryoids were originally isolated
from the marine bryozoan, Bulgula neritina, in small quantities.
Methods of synthesis are awkward and costly. Twenty-one Bryoid
compositions, known as Bryostatins and numbered 1-21, have been
identified. Many of the Bryoids are known to possess anticancer
properties.
Neurodegenerative diseases, such as Alzheimer’s, Parkinson’s, Down’s
syndrome, Hutchinson’s and Multiple Sclerosis, Kuru, Creutzfeldt-Jakob
and other spongiform encephalopathies remain major health problems.
Currently there are very limited means to treat these diseases. With
respect to Alzheimer’s, Hutchinson’s and Parkinson’s diseases, these
disorders tend to manifest themselves in older individuals and as the
diseases progress, the afflicted individuals are less able to care for
themselves. The neurogenerative diseases are associated with the
formation of beta amyloid plaques. Bryoids stimulate the production of
certain isoforms of protein kinase C (PKC) that increase the production
of alpha-secretase which makes soluble amyloid precursor protein, thus
inhibiting the formation of beta amyloid plaques. With respect to
cancers such as prostate cancer, Bryoids inhibit phorbol ester-induced
apoptosis in prostate cancer cells by differentially modulating protein
kinase C (PKC) delta translocation and preventing PKC-delta-mediated
release of tumor necrosis factor-alpha. With respect to latent virus
diseases such as HIV-1 latency, Bryoids, as well as many PKC agonists,
activate cellular transcription factors such as NF-kB that binds the
HIV-1 promoter and regulates its transcriptional activity. In HIV-1
latency the viral promoter is less accessible to cellular transcription
factors because nuclear histones surrounding the viral promoter are
deacetylated (compacted chromatin). Thus, HDAC inhibitors may increase
the acetylation of histones (relaxed chromatin) allowing transcription
factors easier access to the HIV promoter.
According to Dr. Trevor P. Castor, President and CEO, Aphios
Corporation, and inventor of this patent: “This novel Bryoid,
Bryostatin-22, is a highly potent nanomolar activator of α-secretase
activity in neuroblastoma cell models, being more effective than
Bryostatin-1 as well as more effective at increasing activity of all PKC
isoforms, particularly the novel PKC isoforms, delta and epsilon. Aphios
plans to develop this compound for Alzheimer’s and other diseases and is
seeking collaborative research and licensing partners.”
About Aphios Corporation
Aphios Corporation (www.aphios.com)
is a clinical stage, green biotechnology company developing enabling
technology platforms for improving drug discovery, manufacturing,
delivery and safety, and enhanced natural therapeutics for health
maintenance and disease prevention, and the treatment of cancers and
supportive care, infectious diseases such as HIV, and CNS disorders such
as Alzheimer’s disease and opioid addiction.
Contacts
Trevor P. Castor, Ph.D., CEO
(001) 781-932-6933
[email protected]