International Journal of Molecular Sciences,
Journal Year:
2023,
Volume and Issue:
24(17), P. 13301 - 13301
Published: Aug. 27, 2023
We
conducted
the
first
comprehensive
investigation
on
impact
of
head
group
modifications
anticancer
activities
fatty-acid-like
Pt(IV)
prodrugs
(FALPs),
which
are
a
class
platinum-based
metallodrugs
that
target
mitochondria.
created
small
library
FALPs
(1–9)
with
diverse
modifications.
The
outcomes
our
study
demonstrate
hydrophilic
exclusively
enhance
potency
these
metallodrugs,
whereas
hydrophobic
significantly
decrease
their
cytotoxicity.
To
further
understand
this
interesting
structure–activity
relationship,
we
chose
two
representative
(compounds
2
and
7)
as
model
compounds:
one
(2)
polyethylene
glycol
(PEG)
group,
other
(7)
hydrocarbon
modification
same
molecular
weight.
Using
FALPs,
targeted
mechanism
action.
Our
revealed
compound
2,
modifications,
exhibited
remarkable
penetration
into
cancer
cells
mitochondria,
leading
to
subsequent
mitochondrial
DNA
damage,
effectively
eradicating
cells.
In
contrast,
7,
displayed
lower
uptake
weaker
cellular
responses.
collective
results
present
different
perspective,
indicating
increased
hydrophobicity
may
not
necessarily
is
conventionally
believed.
These
findings
provide
valuable
new
insights
fundamental
principles
developing
metallodrugs.
International Journal of Pharmaceutics X,
Journal Year:
2023,
Volume and Issue:
6, P. 100218 - 100218
Published: Nov. 8, 2023
Synergistic
chemotherapy
and
photothermal
therapy
(PTT)
holds
the
promise
of
addressing
weakness
individualized
PTT.
In
this
study,
we
synthesized
a
chemotherapeutic
agent,
PDA-Ce-CDs,
which
combines
conversion
ability
generation
hydroxyl
radicals
(•OH),
enabling
synergistic
enhancement
antitumor
effects.
Furthermore,
localized
heating
effect
NIR
radiation
promoted
uptake
PDA-Ce-CDs
enhances
sensitivity
intracellular
reactive
oxygen
species
(ROS).
Finally,
activity
was
evaluated
through
cell
experiments
tumor-bearing
mice
experiments,
confirming
its
excellent
efficacy
in
vivo
vitro.
Our
work
presents
new
strategy
cancer
treatment
by
utilizing
carbon
dots
combination
with
agents
for
chemotherapy-photothermal
therapy.
This
innovative
approach
offers
therapeutic
avenue
tumor
harnessing
combined
effects
chemotherapy.
Angewandte Chemie,
Journal Year:
2024,
Volume and Issue:
136(27)
Published: April 24, 2024
Abstract
A
planar
conjugated
ligand
functionalized
with
bithiophene
and
its
Ru(II),
Os(II),
Ir(III)
complexes
have
been
constructed
as
single‐molecule
platform
for
synergistic
photodynamic,
photothermal,
chemotherapy.
The
significant
two‐photon
absorption
at
808
nm
remarkable
singlet
oxygen
superoxide
anion
production
in
aqueous
solution
cells
when
exposed
to
infrared
irradiation.
most
potent
Ru(II)
complex
Ru7
enters
tumor
via
the
rare
macropinocytosis,
locates
both
nuclei
mitochondria,
regulates
DNA‐related
chemotherapeutic
mechanisms
intranuclearly
including
DNA
topoisomerase
RNA
polymerase
inhibition
their
effects
photoactivated
apoptosis,
ferroptosis
cleavage.
exhibits
high
efficacy
vivo
malignant
melanoma
cisplatin‐resistant
non‐small
cell
lung
cancer
tumors,
a
100
%
survival
rate
of
mice,
low
toxicity
normal
residual
rate.
Such
an
activatable
metal
may
contribute
new
generation
single‐molecule‐based
integrated
diagnosis
treatment
address
drug
resistance
clinical
practice
phototherapy
large,
deeply
located
solid
tumors.
Molecules,
Journal Year:
2024,
Volume and Issue:
29(17), P. 4095 - 4095
Published: Aug. 29, 2024
In
this
study,
we
report
a
novel
platinum-doxorubicin
conjugate
that
demonstrates
superior
therapeutic
indices
to
cisplatin,
doxorubicin,
or
their
combination,
which
are
commonly
used
in
cancer
treatment.
This
new
molecular
structure
(
International Journal of Molecular Sciences,
Journal Year:
2023,
Volume and Issue:
24(17), P. 13301 - 13301
Published: Aug. 27, 2023
We
conducted
the
first
comprehensive
investigation
on
impact
of
head
group
modifications
anticancer
activities
fatty-acid-like
Pt(IV)
prodrugs
(FALPs),
which
are
a
class
platinum-based
metallodrugs
that
target
mitochondria.
created
small
library
FALPs
(1–9)
with
diverse
modifications.
The
outcomes
our
study
demonstrate
hydrophilic
exclusively
enhance
potency
these
metallodrugs,
whereas
hydrophobic
significantly
decrease
their
cytotoxicity.
To
further
understand
this
interesting
structure–activity
relationship,
we
chose
two
representative
(compounds
2
and
7)
as
model
compounds:
one
(2)
polyethylene
glycol
(PEG)
group,
other
(7)
hydrocarbon
modification
same
molecular
weight.
Using
FALPs,
targeted
mechanism
action.
Our
revealed
compound
2,
modifications,
exhibited
remarkable
penetration
into
cancer
cells
mitochondria,
leading
to
subsequent
mitochondrial
DNA
damage,
effectively
eradicating
cells.
In
contrast,
7,
displayed
lower
uptake
weaker
cellular
responses.
collective
results
present
different
perspective,
indicating
increased
hydrophobicity
may
not
necessarily
is
conventionally
believed.
These
findings
provide
valuable
new
insights
fundamental
principles
developing
metallodrugs.
