International Journal of Molecular Sciences,
Год журнала:
2024,
Номер
25(15), С. 8252 - 8252
Опубликована: Июль 28, 2024
Chlorambucil-platinum(IV)
prodrugs
exhibit
multi-mechanistic
chemotherapeutic
activity
with
promising
anticancer
potential.
The
platinum(II)
precursors
of
the
have
been
previously
found
to
induce
changes
in
microtubule
cytoskeleton,
specifically
actin
and
tubulin
HT29
colon
cells,
while
chlorambucil
alkylates
DNA.
These
demonstrate
significant
2D
cell
3D
spheroid
viability
assays.
A
notable
production
reactive
oxygen
species
has
observed
cells
72
h
post
treatment
this
type,
mitochondrial
membrane
potential
was
substantially
reduced.
cellular
uptake
chlorambucil-platinum(IV)
prodrugs,
assessed
by
ICP-MS,
confirmed
that
active
transport
primary
mechanism,
platinum
localisation
identified
primarily
cytoskeletal
fraction.
Apoptosis
necrosis
were
at
as
demonstrated
Annexin
V-FITC/PI
assay
using
flow
cytometry.
Immunofluorescence
measured
via
confocal
microscopy
showed
intensity
architecture.
Western
blot
analysis
intrinsic
extrinsic
pathway
apoptotic
markers,
cytoskeleton
proliferation
well
autophagy
markers
studied
treatment.
proteomic
profile
also
a
total
1859
proteins
quantified
mass
spectroscopy,
several
dysregulated
proteins.
Network
revealed
dysregulation
transcription,
MAPK
microtubule-associated
dysfunction.
This
study
confirms
are
candidates
act
chemotherapeutics.
Inorganics,
Год журнала:
2025,
Номер
13(6), С. 177 - 177
Опубликована: Май 23, 2025
In
this
study,
a
novel
4-methylbenzoylhydrazide·dimethyl
sulfoxide·dichloro
platinum(II)
complex
(Pt2)
was
synthesized
and
characterized,
its
anti-tumor
activity
action
mechanism
were
explored.
The
molecular
structure
spatial
configuration
of
the
determined
using
X-ray
diffraction.
results
obtained
fluorescence
spectroscopy
demonstrate
that
can
effectively
bind
to
DNA
affect
properties.
experimental
show
Pt2
exhibited
significant
inhibitory
effects
on
variety
tumor
cell
lines
(MCF-7,
HepG-2,
NCI-H460,
T24,
A549),
IC50
values
lower
than
those
cisplatin
(DDP),
indicating
stronger
activity.
addition,
not
only
significantly
induced
apoptosis
MCF-7
cells
but
also
inhibited
cycle
arrest
at
G2
phase,
with
proportion
G2-phase
as
high
49.47%.
conclusion,
4-methylbenzoylhydrazide
exhibits
good
by
inducing
inhibiting
cycle,
providing
an
important
basis
for
development
platinum-based
drugs.
Hypoxia
is
a
state
characterized
by
low
concentration
of
Oxygen.
Hypoxic
often
found
in
the
central
region
solid
tumors.
associated
with
abnormal
neovascularization
resulted
poor
blood
flow
tissues
and
increased
proliferation
tumor
cells,
imbalance
between
O
ACS Applied Bio Materials,
Год журнала:
2024,
Номер
7(7), С. 4795 - 4803
Опубликована: Июль 3, 2024
Metallic
nanoparticles
are
promising
candidates
for
anticancer
therapies.
Among
the
different
metallic
systems
studied,
copper
is
an
affordable
and
biologically
available
metal
with
a
high
redox
potential.
Copper-based
widely
used
in
studies
owing
to
their
ability
react
intracellular
glutathione
(GSH)
induce
Fenton-like
reaction.
However,
considering
metastatic
potential
versatility
of
tumor
microenvironment,
modalities
single
therapeutic
agent
may
not
be
effective.
Hence,
enhance
efficiency
chemotherapeutic
drugs,
repurposing
them
or
conjugating
other
essential.
Omeprazole
FDA-approved
proton
pump
inhibitor
clinics
treatment
ulcers.
has
also
been
studied
its
sensitize
cancer
cells
chemotherapy
apoptosis.
Herein,
we
report
nanosystem
comprising
encapsulating
omeprazole
(CuOzL)
against
B16
melanoma
cells.
The
developed
nanoformulation
exerted
significant
synergistic
activity
when
compared
either
alone
by
inducing
cell
death
through
excessive
ROS
generation
subsequent
mitochondrial
damage.
International Journal of Molecular Sciences,
Год журнала:
2024,
Номер
25(15), С. 8252 - 8252
Опубликована: Июль 28, 2024
Chlorambucil-platinum(IV)
prodrugs
exhibit
multi-mechanistic
chemotherapeutic
activity
with
promising
anticancer
potential.
The
platinum(II)
precursors
of
the
have
been
previously
found
to
induce
changes
in
microtubule
cytoskeleton,
specifically
actin
and
tubulin
HT29
colon
cells,
while
chlorambucil
alkylates
DNA.
These
demonstrate
significant
2D
cell
3D
spheroid
viability
assays.
A
notable
production
reactive
oxygen
species
has
observed
cells
72
h
post
treatment
this
type,
mitochondrial
membrane
potential
was
substantially
reduced.
cellular
uptake
chlorambucil-platinum(IV)
prodrugs,
assessed
by
ICP-MS,
confirmed
that
active
transport
primary
mechanism,
platinum
localisation
identified
primarily
cytoskeletal
fraction.
Apoptosis
necrosis
were
at
as
demonstrated
Annexin
V-FITC/PI
assay
using
flow
cytometry.
Immunofluorescence
measured
via
confocal
microscopy
showed
intensity
architecture.
Western
blot
analysis
intrinsic
extrinsic
pathway
apoptotic
markers,
cytoskeleton
proliferation
well
autophagy
markers
studied
treatment.
proteomic
profile
also
a
total
1859
proteins
quantified
mass
spectroscopy,
several
dysregulated
proteins.
Network
revealed
dysregulation
transcription,
MAPK
microtubule-associated
dysfunction.
This
study
confirms
are
candidates
act
chemotherapeutics.
