Molecules,
Journal Year:
2024,
Volume and Issue:
29(22), P. 5481 - 5481
Published: Nov. 20, 2024
Acetylcholinesterase
and
butyrylcholinesterase
are
two
related
enzymes
that
represent
pharmacologically
suitable
targets
in
neurodegenerative
disorders,
given
their
physiological
roles
the
body.
The
treatment
of
disorders
currently
includes
common
reversible
cholinesterase
inhibitors.
Resveratrol
analogues,
as
molecules
focus,
have
shown
very
strong
inhibition
potential
cholinesterases.
In
this
research,
experimental
DFT
approaches
for
p
Antioxidants,
Journal Year:
2024,
Volume and Issue:
13(2), P. 177 - 177
Published: Jan. 31, 2024
Resveratrol
is
a
natural
phenolic
compound
with
known
benefits
against
neurodegeneration.
We
analyzed
in
vitro
the
protective
mechanisms
of
resveratrol
proinflammatory
monomeric
C-reactive
protein
(mCRP).
mCRP
increases
risk
AD
after
stroke
and
we
previously
demonstrated
that
intracerebral
induces
AD-like
dementia
mice.
Here,
used
BV2
microglia
treated
for
24
h
presence
or
absence
resveratrol.
Cells
conditioned
media
were
collected
analysis.
Lipopolysaccharide
(LPS)
has
also
been
implicated
progression
so
LPS
was
as
resveratrol-sensitive
reference
agent.
at
concentration
50
µg/mL
activated
nitric
oxide
pathway
NLRP3
inflammasome
pathway.
Furthermore,
induced
cyclooxygenase-2
release
cytokines.
effectively
inhibited
these
changes
increased
expression
antioxidant
enzyme
genes
Cat
Sod2.
As
central
defense,
hub
Sirt1
Nfe2l2
nuclear
translocation
signal
transducer
NF-ĸB.
Proinflammatory
by
primary
mixed
glial
cultures
protected
This
work
provides
mechanistic
insight
into
preventing
agents.
The
targeted
compounds
in
this
research,
resveratrol
analogs
1–14
were
synthesized
as
mixtures
of
isomers
by
the
Wittig
reaction
using
heterocyclic
triphenylphosphonium
salts
and
various
benzaldehydes.
planned
those
possessing
trans-configuration
biologically
active
trans-resveratrol.
pure
obtained
repeated
column
chromatography
isolated
yields
depending
on
heteroaromatic
ring.
It
was
found
that
butyrylcholinesterase
(BChE)
more
sensitive
to
than
acetylcholinesterase
(AChE),
except
for
6,
methylated
thiophene
derivative
with
chlorine,
which
showed
equal
inhibition
toward
both
enzymes.
Compounds
5
8
achieved
highest
BChE
IC50
values
22.9
24.8
μM,
respectively.
same
AChE
BChE,
subunits
better
enzyme
unmethylated
ones.
Two
antioxidant
spectrophotometric
methods,
DPPH
CUPRAC,
applied
determine
potential
new
analogs.
Molecular
docking
these
conducted
visualize
ligand-active
site
complexes'
structure
identify
non-covalent
interactions
responsible
complex's
stability,
influence
inhibitory
potential.
As
ADME
properties
are
crucial
developing
drug
product
formulations,
they
have
also
been
addressed
work.
genotoxicity
is
evaluated
silico
studies
all
synthesized.
Osmaniye Korkut Ata Üniversitesi Fen Bilimleri Enstitüsü Dergisi,
Journal Year:
2025,
Volume and Issue:
8(1), P. 145 - 166
Published: Jan. 15, 2025
Purpose:
The
aim
of
this
study
is
to
compare
13
stilbenes
and
5
FDA-approved
drugs
used
in
the
treatment
Alzheimer’s
disease
(AD)
by
ADME
prediction
molecular
docking
method.
Cholinergic,
amyloid,
tau,
oxidative
stress
inflammation
hypotheses
involved
AD
pathology
were
targeted
docking.
Materials
Methods:
SwissADME
has
been
determine
physicochemical,
lipophilicity,
water
solubility,
pharmacokinetics,
drug-likeness
medicinal
chemistry
properties
(resveratrol,
pterostilbene,
oxyresveratrol,
piceatannol,
pinosylvin,
isorhapontigenin,
isorhapontin,
astringin,
piceid
(polydatin),
mulberroside
A)
(tacrine,
donepezil,
rivastigmine,
galantamine,
memantine).
CBDOCK2
binding
affinity
target
proteins
(AChE,
BuChE,
APP,
BACE,
GSK-3β,
CDK5,
SOD,
CAT,
GPx,
Cox-2,
iNOS,
IL-1β,
TNF-α).
Results:
SWISS
results
showed
that
could
be
as
natural
products
AD.
indicated
A
best
vina
score
(kcal/mol)
followed
galanthamine,
resveratrol,
tacrine,
memantine.
Conclusion:
Our
evaluated
for
using
computational
approaches.
highlight
its
potential
therapeutic
effects
on
various
pathology.
More
research
needed
validate
these
findings
clinical
practice.
Journal of Natural Products,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Jan. 24, 2025
An
activity-guided
isolation
study
on
the
EtOH
extract
prepared
from
bulbs
of
Prospero
autumnale
yielded
four
new
phenolic
compounds,
including
a
stilbenoid
(1),
homoisoflavonoid
derivative
(8),
dimer
(9),
and
an
unprecedented
homoisoflavone–stilbene
heterodimer
(10),
together
with
six
known
(2–7)
analogs.
Their
chemical
structures
were
elucidated
by
spectroscopic
analysis
theoretical
NMR
ECD
calculations.
Compounds
9
10
are
unique
in
their
scaffolds.
The
vitro
cytotoxic
activity
purified
compounds
was
evaluated
against
eight
tumor
cell
lines
(HCT116,
LoVo,
DU145,
PC3,
HEP3B,
HEPG2,
MCF7,
MDA-MB-231)
one
nontumor
line
(L929)
MTS
assay.
1,
2,
4,
exhibited
inhibition
IC50
values
ranging
8.2
to
37.6
μM.
Cytotoxic
death
mechanisms
further
investigated,
indicating
variability
apoptosis,
necrosis,
or
cycle
arrest.
International Journal of Molecular Sciences,
Journal Year:
2024,
Volume and Issue:
25(13), P. 7401 - 7401
Published: July 5, 2024
The
targeted
compounds
in
this
research,
resveratrol
analogs
1–14,
were
synthesized
as
mixtures
of
isomers
by
the
Wittig
reaction
using
heterocyclic
triphenylphosphonium
salts
and
various
benzaldehydes.
planned
those
possessing
trans-configuration
biologically
active
trans-resveratrol.
pure
obtained
repeated
column
chromatography
isolated
yields
depending
on
heteroaromatic
ring.
It
was
found
that
butyrylcholinesterase
(BChE)
more
sensitive
to
than
acetylcholinesterase
(AChE),
except
for
6,
methylated
thiophene
derivative
with
chlorine,
which
showed
equal
inhibition
toward
both
enzymes.
Compounds
5
8
achieved
highest
BChE
IC50
values
22.9
24.8
μM,
respectively.
same
AChE
BChE,
subunits
better
enzyme
unmethylated
ones.
Two
antioxidant
spectrophotometric
methods,
DPPH
CUPRAC,
applied
determine
potential
new
analogs.
molecular
docking
these
conducted
visualize
ligand-active
site
complexes’
structure
identify
non-covalent
interactions
responsible
complex’s
stability,
influence
inhibitory
potential.
As
ADME
properties
are
crucial
developing
drug
product
formulations,
they
have
also
been
addressed
work.
genotoxicity
is
evaluated
silico
studies
all
synthesized.
International Journal of Biological Sciences,
Journal Year:
2024,
Volume and Issue:
20(14), P. 5474 - 5494
Published: Jan. 1, 2024
Neurological
disorders
(NDs)
encompass
a
range
of
debilitating
conditions
that
affect
the
nervous
system,
including
prevalent
illnesses
such
as
Alzheimer's
disease,
Parkinson's
and
ischemic
stroke.
Despite
significant
ongoing
studies,
effective
therapeutic
strategies
to
halt
or
slow
down
progression
these
are
still
lacking.
Stilbenes,
class
natural
polyphenols,
have
shown
potential
candidates
for
due
their
capacity
protect
system.
Preclinical
studies
provided
strong
evidence
stilbenes
can
regulate
many
cellular
pathways
implicated
in
neurodegeneration,
with
resveratrol
being
well-studied
compound
has
ability
reduce
oxidative
damage,
promote
neurogenesis,
enhance
mitochondrial
function
-
crucial
maintaining
brain
health.
In
preclinical
animal
models,
initial
research
also
promise
additional
substances
piceatannol
pterostilbene.
Furthermore,
clinical
explored
benefits
NDs.
promising
results
research,
use
trials
is
currently
limited,
most
focusing
on
resveratrol.
Although
several
demonstrated
beneficial
impact
supplementation
health
degenerative
consequences,
other
investigations
yielded
ambiguous
findings,
underscoring
urgent
need
more
comprehensive
precisely
planned
research.
This
study
delves
into
neuroprotective
agents
It
emphasizes
our
understanding
effectiveness
specific
patient
groups.