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Bryostatin
1 for Alzheimer’s Disease and Cognitive Disorders
The symptoms of Alzheimer’s Disease are associated
with gradual brain tissue shrinkage and death. In the early
stage of the disease, short-term memory and the ability to
perform routine tasks begin to decline with degeneration of
cells in the hippocampus. As Alzheimer’s Disease spread
through the cerebral cortex, judgment declines, emotional
outbursts may occur and language is impaired. Progression
of the disease leads to the death of more nerve cells and
progressively worsening behavior changes such as wandering
and agitation. In the final stages, patients lose the ability
to recognize faces, communicate, and control bladder and bowel
movements. The average time from diagnosis to death is 4 to
8 years, although it may take 20 years or more for the disease
to run its course. While there is some understanding of the
disorder, there is still a lack of preventative and therapeutic
remedies.
Recently,
researchers at The Blanchette Rockefeller Neurosciences Institute,
Rockville, MD have hypothesized and shown that protein kinase
C (PKC) and its activation are important means of ameliorating
AD pathophysiology and cognitive impairment. They have shown
that sub-nanomolar concentrations of bryostatin 1, a potent
PKC activator, dramatically enhance the generation of non-amyloidogenic
soluble amyloid precursor protein (sAPP) in fibroblasts from
AD patients. Bryostatin 1 was effective in reducing brain
amyloid plaques (Aß40 and Aß42 in AD) in double-transgenic
mice while improving behavioral outcomes and the rate of premature
death (U.S. Patent). These researchers have also shown that
bryostatin 1 not only produces a neuroprotective effect but
also enhances cognitive memory in AD animal models.
Aphios has developed and patented improved methodologies
and manufacturing processes for the isolation of bryostatin
1 from Bugula neritina (U.S. Patent). Aphios currently
sells pharmaceutical-grade bryostatin 1 and other bryostatins
to reagent-distribution companies such as Sigma-Aldrich, PKC
Pharmaceuticals, Axxora and Biomol. Aphios has also developed
and patented improved methods for formulating bryostatin 1
into phosopholipid nanosomes, Bryosomes™ (U.S., Patent)
that can be utilized to enhance efficacy, reduce toxicity
and improve quality-of-life.
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