Molecules,
Год журнала:
2022,
Номер
27(3), С. 901 - 901
Опубликована: Янв. 28, 2022
Alzheimer’s
disease
(AD)
is
a
progressive,
neurodegenerative
disorder
that
currently
has
reached
epidemic
proportions
among
elderly
populations
around
the
world.
In
China,
available
traditional
Chinese
medicines
(TCMs)
organically
combine
functional
foods
with
medicinal
values
are
named
“Medicine
Food
Homology
(MFH)”.
this
review,
we
focused
on
MFH
varieties
for
their
features,
substance
bases,
clinical
uses,
and
mechanisms
of
action
(MOAs)
AD
prevention
treatment.
We
consider
antiAD
active
constituents
from
species,
effects
in
vitro/in
vivo
models,
drug
targets
signal
pathways
by
summing
up
literature
via
systematic
electronic
search
(SciFinder,
PubMed,
Web
Science).
paper,
several
plant
sources
discussed
detail
models
methods,
to
MOAs.
found
most
exert
neuroprotective
ameliorate
cognitive
impairments
inhibiting
neuropathological
signs
(Aβ-induced
toxicity,
amyloid
precursor
protein,
phosphorylated
Tau
immunoreactivity),
including
anti-inflammation,
antioxidative
stress,
antiautophagy,
antiapoptosis,
etc.
Indeed,
some
substances
related
phytochemicals
have
broad
spectrum
activities,
so
they
superior
simple
single-target
drugs
treating
chronic
diseases.
This
review
can
provide
significant
guidance
people’s
healthy
lifestyles
development
Chemical Biology & Drug Design,
Год журнала:
2024,
Номер
104(4)
Опубликована: Окт. 1, 2024
ABSTRACT
Alzheimer's
disease
(AD)
is
a
chronic
progressive,
age‐related
neurodegenerative
brain
disorder
characterized
by
the
irreversible
decline
of
memory
and
other
cognitive
functions.
It
one
major
health
threat
21st
century,
which
affects
around
60%
population
over
age
60
years.
The
problem
this
even
more
because
existing
pharmacotherapies
only
provide
symptomatic
relief
without
addressing
basic
factors
disease.
extracellular
deposition
amyloid
β
(Aβ)
to
form
senile
plaques,
intracellular
hyperphosphorylation
tau
neurofibrillary
tangles
(NFTs).
Due
complex
pathophysiology
disease,
various
hypotheses
have
been
proposed,
including
cholinergic,
Aβ,
tau,
oxidative
stress,
metal–ion
hypothesis.
Among
these,
cholinergic
Aβ
are
primary
targets
for
AD.
Therefore,
continuous
advances
made
in
developing
potential
cholinesterase
inhibitors
N
‐methyl‐D‐aspartate
(NMDA)
receptor
antagonists
delay
progression
restore
neurotransmission.
In
review
article,
we
tried
comprehensively
summarize
recent
advancement
NMDA
antagonist
(memantine)
their
hybrid
analogs
as
disease‐modifying
agents
treatment
Furthermore,
also
depicted
design,
rationale,
SAR
analysis
memantine‐based
hybrids
used
last
decade
Arabian Journal of Chemistry,
Год журнала:
2021,
Номер
14(12), С. 103449 - 103449
Опубликована: Сен. 22, 2021
•
2-methylindole
analogs
were
designed,
synthesized
and
characterized.
The
target
(
4a–4j
)
evaluated
for
their
inhibitory
potential
against
glutathione
S-transferase
(GST),
acetylcholinesterase
(AChE),
butyrylcholinesterase
(BChE)
activities.
Molecular
docking
studies
conducted
to
correlate
the
in
vitro
results
identify
possible
mode
of
interactions
at
active
pocket
site
receptors.
pharmacokinetic
carried
out
using
SwissADMET
analyses.
In
this
study,
we
aimed
(i)
synthesize
new
containing
various
amino
structures,
pyrrolidine,
piperidine,
morpholine,
substituted
phenyl
groups
through
structural
molecular
modifications,
(ii)
evaluate
pharmaceutical
via
assessing
enzyme
activity
(BChE),
(iii)
predict
ADMET
properties
analogs,
(iv)
reveal
between
with
GST,
AChE,
BChE
enzymes
several
software.
inhibition
assays
showed
that
indole
exhibited
moderate
good
activities
enzymes.
Briefly,
4b
4i
4a
BChE,
1
GST
detected
be
higher
or
close
standard
inhibitor
compounds.
analog
was
have
best
both
AChE
lowest
IC
50
values
as
0.648
µM
0.745
BChE.
analyses
relationship
could
help
design
inhibitors
cholinergic
pathways
based
on
derivatives.
Pharmaceutics,
Год журнала:
2022,
Номер
14(2), С. 235 - 235
Опубликована: Янв. 20, 2022
It
has
become
increasingly
apparent
that
defective
insulin
signaling
may
increase
the
risk
for
developing
Alzheimer’s
disease
(AD),
influence
neurodegeneration
through
promotion
of
amyloid
formation
or
by
increasing
inflammatory
responses
to
intraneuronal
β-amyloid.
Recent
work
demonstrated
hyperglycemia
is
linked
cognitive
decline,
with
elevated
levels
glucose
causing
oxidative
stress
in
vulnerable
tissues
such
as
brain.
The
ability
β-amyloid
peptide
form
β-sheet-rich
aggregates
and
induce
apoptosis
made
fibrils
a
leading
target
development
novel
pharmacotherapies
used
managing
treatment
neuropathological
conditions
AD-related
decline.
Additionally,
deposits
β-sheets
folded
amylin,
homeostasis
regulator,
are
also
present
diabetic
patients.
Thus,
therapeutic
compounds
capable
reducing
intracellular
protein
aggregation
models
neurodegenerative
disorders
prove
useful
ameliorating
type
2
diabetes
mellitus
symptoms.
Furthermore,
both
conditions,
AD,
characterized
chronic
accompanied
presence
dysregulated
biomarkers.
This
review
presents
current
evidence
describing
role
various
small
bioactive
molecules
known
ameliorate
amyloidosis
subsequent
effects
prevention
AD.
highlights
potential
efficacy
peptide–drug
conjugates
targeting
targets.
Journal of Functional Foods,
Год журнала:
2022,
Номер
95, С. 105180 - 105180
Опубликована: Июль 18, 2022
We
aimed
to
examine
the
hypothesis
that
dietary
ferulic
acid
and
vinpocetine
intake
improve
memory
deficits
caused
by
hippocampal
amyloid-β
accumulation
in
type
2
diabetic(T2DM)
rats
with
induced
Alzheimer's
disease(AD).
Their
mechanisms
were
also
tested.
Partial
pancreatectomized
animals
amyloid-β(25–35)
infusion
representing
Asian
T2DM
developed
AD
(AD
rats;
deficit).
After
eight-week
intervention,
impairment
was
impeded
AD-FRA
fed
acid(50
mg/kg
BW)
AD-VPC
vinpocetine(50
BW;
AD-VPC)
through
inhibition
of
deposition
neuroinflammation
compared
AD-CON.
The
showed
less
than
group.
groups
an
inhibited
attenuation
phosphorylated
Akt
→
glycogen-synthase
kinase(GSK)-3β
forkhead
box
protein
O1(FOXO1)
pathway,
similar
protection
as
CON.
No
adverse
effects
detected.
In
conclusion,
supplementation
suppressed
AD,
better
improvement
vinpocetine,
no
AD-induced
rats.
Molecules,
Год журнала:
2022,
Номер
27(3), С. 901 - 901
Опубликована: Янв. 28, 2022
Alzheimer’s
disease
(AD)
is
a
progressive,
neurodegenerative
disorder
that
currently
has
reached
epidemic
proportions
among
elderly
populations
around
the
world.
In
China,
available
traditional
Chinese
medicines
(TCMs)
organically
combine
functional
foods
with
medicinal
values
are
named
“Medicine
Food
Homology
(MFH)”.
this
review,
we
focused
on
MFH
varieties
for
their
features,
substance
bases,
clinical
uses,
and
mechanisms
of
action
(MOAs)
AD
prevention
treatment.
We
consider
antiAD
active
constituents
from
species,
effects
in
vitro/in
vivo
models,
drug
targets
signal
pathways
by
summing
up
literature
via
systematic
electronic
search
(SciFinder,
PubMed,
Web
Science).
paper,
several
plant
sources
discussed
detail
models
methods,
to
MOAs.
found
most
exert
neuroprotective
ameliorate
cognitive
impairments
inhibiting
neuropathological
signs
(Aβ-induced
toxicity,
amyloid
precursor
protein,
phosphorylated
Tau
immunoreactivity),
including
anti-inflammation,
antioxidative
stress,
antiautophagy,
antiapoptosis,
etc.
Indeed,
some
substances
related
phytochemicals
have
broad
spectrum
activities,
so
they
superior
simple
single-target
drugs
treating
chronic
diseases.
This
review
can
provide
significant
guidance
people’s
healthy
lifestyles
development
