Journal of Medicinal Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Jan. 23, 2025
Pulmonary
inflammation
is
the
main
cause
of
lung
injury.
Phosphodiesterase
4
(PDE4)
a
promising
anti-inflammatory
target
for
treatment
respiratory
diseases.
Herein,
we
designed
and
synthesized
43
compounds
in
two
novel
series
benzimidazole
derivatives
as
PDE4
inhibitors.
Among
them,
compound
A5
showed
highly
selective
inhibition
PDE4,
good
safety,
liver
microsomal
stability
vitro.
administration
remarkably
attenuated
inflammatory
infiltration
pathologic
injury
models
acute
mice
chronic
obstructive
pulmonary
disease
(COPD)
mice.
In
addition,
enhanced
sputum
secretion,
relieved
cough
mice,
inhibited
phosphorylation
p38
MAP
kinase,
an
important
protein
regulation
Overall,
A5,
effective
inhibitor
without
toxicity
gastrointestinal
reaction,
may
be
potent
candidate
Aging Cell,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Feb. 13, 2025
ABSTRACT
As
global
life
expectancy
increases,
the
focus
has
shifted
from
merely
extending
lifespan
to
promoting
healthy
aging.
GSTA1,
GSTA2,
and
GSTA3
(GSTA1‐3),
members
of
alpha
class
glutathione
S‐transferases,
are
involved
in
diverse
biological
processes,
including
metabolism
immune
regulation,
highlighting
their
potential
influence
on
human
health
span
lifespan.
In
this
study,
we
employed
Caenorhabditis
elegans
as
a
model
organism
investigate
role
gst‐35
,
an
ortholog
mammalian
GSTA1‐3,
Our
results
demonstrated
that
overexpression
detrimental
effects
multiple
physiological
functions
nematodes.
Specifically,
significantly
reduced
lifespan,
impaired
development
growth,
substantially
diminished
reproductive
capacity,
physical
fitness,
stress
resistance.
contrast,
knockout
partially
enhanced
fitness
Comprehensive
RNA‐sequencing
transcriptome
analysis
revealed
disrupted
metabolic
homeostasis
induced
lysosomal
dysfunction.
These
were
mediated
through
activation
pmk‐1
signaling
pathway
suppression
skr
genes,
which
collectively
aging
processes.
findings
illuminate
complex
provide
valuable
insights
into
molecular
mechanisms
underlying
aging,
offering
targets
for
interventions
aimed
at
span.
Scientific Reports,
Journal Year:
2025,
Volume and Issue:
15(1)
Published: Feb. 14, 2025
Lymphedema
is
a
chronic
condition
that
can
follow
cancer
treatment,
and
liposuction
has
been
shown
to
be
an
effective
approach
for
reducing
limb
volume
in
advanced
cases.
However,
recurrence
rates
vary
widely,
with
prior
erysipelas
identified
as
potentially
significant
factor
influencing
prognosis.
This
study
aimed
identify
key
risk
factors
following
patients
cancer-associated
secondary
lymphedema,
develop
predictive
nomogram
model,
investigate
the
molecular
mechanisms
by
which
previous
may
affect
recurrence.
In
retrospective
analysis
of
1,016
patients,
multivariate
logistic
regression
propensity
score
matching
four
independent
factors,
namely,
erysipelas,
hyperlipidemia,
severe
distal
edema,
older
age,
showing
strongest
association
poor
outcomes
(OR
3.98;
95%
CI:
2.81–5.69).
A
validated
demonstrated
high
accuracy
(C-index
0.757,
Brier
0.176)
net
clinical
benefit
estimating
risk.
The
supports
personalized
treatment
strategies,
improving
patient
outcomes.
Transcriptome
sequencing
further
revealed
exacerbates
lymphedema
through
inflammation,
tissue
remodeling,
metabolic
dysregulation,
suggesting
potential
therapeutic
targets.
Natural Product Reports,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Jan. 1, 2025
This
review
highlights
six
privileged
classes
of
natural
products
–
coumarins,
polyphenols,
labdane
diterpenoids,
sesquiterpene
lactones,
isoquinoline
and
indole
alkaloids—for
potential
anti-inflammatory
drug
development.
Pharmaceuticals,
Journal Year:
2025,
Volume and Issue:
18(4), P. 600 - 600
Published: April 20, 2025
Background/Objectives:
The
kinase
p38α,
a
member
of
the
mitogen-activated
protein
(MAPK)
family,
is
activated
by
external
stimuli
and
plays
crucial
role
in
inflammation,
tumor
growth,
metabolic
disorders.
In
particular,
p38α
involved
thermogenesis
metabolism
glucose
brown
adipose
tissue
(BAT),
it
contributes
to
suppression
obesity
diabetes.
noninvasive
imaging
could
help
elucidate
diverse
pathological
processes,
including
inflammatory
conditions.
This
study
aimed
develop
evaluate
novel
fluorine-18-labeled
positron
emission
tomography
(PET)
probe
for
vivo.
Methods:
We
designed
6-(4-[18F]fluoro-2-fluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)-pyrido[2,3-d]pyrimidin-7(8H)-one
([18F]R1487)
replacing
fluorine
atom
R1487,
which
highly
selective
inhibitor,
with
18F.
A
tributylstannyl
precursor
was
reacted
[18F]KF
presence
copper
catalyst
synthesize
[18F]R1487.
Biodistribution
studies
PET/computed
(CT)
were
performed
on
normal
mice
vivo
potential
Results:
[18F]R1487
obtained
decay-corrected
radiochemical
conversion
30.6
±
5.6%
yield
6.9
3.6%
purity
>99%
after
reversed-phase
high-performance
liquid
chromatography
purification.
biodistribution
demonstrated
high
rapid
radioactivity
accumulation
BAT
(16.3
2.7
%ID/g
at
5
min
post-injection),
consistently
BAT-to-blood
ratio
(>5
over
2
h
post-injection).
PET/CT
successfully
visualized
contrast.
Conclusions:
These
results
suggest
that
promising
PET
vivo,
has
applications
pathophysiological
conditions
such
as
cancer,
Journal of Agricultural and Food Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown
Published: April 25, 2025
Nutmeg
(Myristica
fragrans)
has
been
traditionally
valued
for
its
culinary
and
medicinal
properties.
In
our
ongoing
efforts
to
discover
pharmacologically
active
compounds
from
this
spice,
five
new
furan
acids
(2-6,
jusahos
B-F),
one
neolignan
(7,
jusaho
G),
six
known
(1
8-12)
were
isolated
nutmegs.
The
chemical
structures
of
the
elucidated
using
NMR
spectroscopy
HRESIMS.
Among
them,
compound
3
(jusaho
C)
demonstrated
promising
antineuroinflammatory
neuroprotective
effects
in
BV2
HT22
cells
by
modulating
MAPK/NF-κB
signaling
pathway,
which
was
explored
through
network
pharmacology,
molecular
docking,
experimental
verification.
Compound
also
showed
improvement
locomotor
activity
Caenorhabditis
elegans
model
infected
with
Pseudomonas
aeruginosa.
These
findings
expand
phytochemical
profile
M.
fragrans,
where
only
acid
previously
reported,
highlight
nutmeg-derived
compounds,
particularly
C,
as
potential
functional
food
ingredients
or
nutraceuticals
managing
neuroinflammatory
conditions.
Current Issues in Molecular Biology,
Journal Year:
2025,
Volume and Issue:
47(5), P. 316 - 316
Published: April 28, 2025
Background:
Sapindus
mukorossi
Gaertn
is
a
deciduous
tree
with
saponins
as
the
main
active
ingredients
and
has
been
utilized
in
medicine
cosmetic
industries.
Currently,
investigations
of
S.
mainly
focus
on
pericarp
seed
kernel
parts,
while
other
parts
are
yet
to
be
studied
developed.
This
study
aimed
investigate
anti-acne
potential
flower
water
extract
(SMFW)
by
vitro
experiments.
Methods
Results:
The
DPPH,
ABTS,
superoxide
anion
radical
scavenging
assay,
FRAP
assay
revealed
strong
antioxidant
activities
SMFW.
antibacterial
activity
SMFW
against
Cutibacterium
acnes
evaluated
an
inhibition
diameter
14.08
±
0.63
mm.
Furthermore,
significantly
inhibited
secretion
pro-inflammatory
cytokines
(TNF-α,
IL-6,
IL-β)
lipopolysaccharide
(LPS)-stimulated
THP-1
macrophages.
Transcriptome
analysis
showed
that
treatment
reversed
448
LPS-upregulated
DEGs
349
LPS-downregulated
DEGs,
KEGG
enrichment
indicated
might
exert
its
anti-inflammatory
effect
via
NOD-like
receptor
JAK-STAT
signaling
pathways.
Conclusions:
exhibited
antioxidant,
antibacterial,
properties
RNA-seq
may
alleviate
inflammation
regulating
In
summary,
shown
for
efficacy
can
used
natural
raw
material
cosmetics.
