International Journal of Molecular Sciences,
Год журнала:
2023,
Номер
24(17), С. 13301 - 13301
Опубликована: Авг. 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.
Angewandte Chemie International Edition,
Год журнала:
2024,
Номер
63(27)
Опубликована: Апрель 24, 2024
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.
Frontiers in Chemistry,
Год журнала:
2025,
Номер
13
Опубликована: Фев. 27, 2025
Advanced
silicate
nano-sheets
as
exfoliated
and
separated
layers
were
developed
from
natural
glauconite
hybridized
with
methanol,
producing
a
methoxy
structure
(Mth/EXGL).
The
was
assessed
an
enhanced
carrier
of
the
cisplatin
drug
(CSPN)
significant
loading,
release,
cytotoxicity
properties.
form
showed
better
loading
properties
(327.7
mg/g)
than
sample
(202.4
well
raw
(119.3
mg/g).
This
enhancement
assigned
to
incorporated
active
centers
after
methanol
hybridization
step,
which
is
in
agreement
steric
studies
determined
site
density
(Nm
=
45.5
mg/g
(Mth/EXGL),
38.4
(EXGL),
26.3
(glauconite).
Moreover,
each
across
interface
Mth/EXGL
has
capacity
be
loaded
8
CSPN
molecules,
donating
multi-molecular
mechanisms
their
vertical
orientation.
energy
value
(<8
kJ/mol)
into
reflected
dominant
impact
physical
mechanisms,
including
electrostatic
attractions
hydrogen
bonding.
recognized
release
profile
demonstrates
continuous
controlled
behavior
that
can
extend
up
110
h
at
pH
7.4
170
5.5.
releasing
regulated
by
two
main
processes
(diffusion
erosion)
based
on
kinetic
findings.
Also,
induces
its
cytotoxic
effect
human
cervical
epithelial
tumors
(HeLa)
(0.65%
cell
viability)
compared
free
(6.6%
viability).
recommended
delivery
system
for
considering
Materials Today Bio,
Год журнала:
2025,
Номер
32, С. 101709 - 101709
Опубликована: Март 27, 2025
Cancer
poses
a
significant
threat
to
human
life
and
health.
Cancers
treated
with
cisplatin
invariably
develop
drug
resistance.
This
challenge
can
be
overcome
by
identifying
exploiting
the
vulnerabilities
acquired
drug-resistant
cancer
cells,
paving
way
for
finding
effective
novel
treatment
options
cisplatin-resistant
cancers.
Our
previous
study
revealed
that
resistance
in
cells
comes
at
cost
of
increased
intracellular
hypoxia.
In
this
study,
we
used
2-nitroimidazole
modified
hyaluronic
acid
(HA-NI)
as
carrier.
The
tumor
cell
specific
hypoxia
programmed
activation
nanomedicine
(T/C@HN
NPs)
was
constructed
hypoxic
toxic
tirapazamine
(TPZ)
encapsulating
chlorin
e6
(Ce6)
into
HA-NI
using
polymer
assembly
technology.
amphiphilic
carrier
could
release
free
Ce6
molecules
under
stimulation
environment,
exhibit
"activated
state"
photodynamic
properties
cells.
Upon
irradiation,
Ce6-mediated
therapy
further
intensifies
hypoxia,
amplifying
its
cytotoxicity.
project
systematically
evaluated
effects
T/C@HN
NPs
on
identification
recognition
tumors
patient-derived
xenograft
(PDX)
models.
provides
promising
avenue
development
tumors.
Pharmaceutics,
Год журнала:
2024,
Номер
16(9), С. 1237 - 1237
Опубликована: Сен. 23, 2024
Cancer
remains
a
leading
cause
of
death
globally.
patients
often
seek
alternative
therapies
in
addition
to,
or
instead
of,
conventional
treatments
like
chemotherapy,
radiation,
and
surgery.
The
progress
medical
advancements
early
detection
provides
more
treatment
options;
however,
the
development
cancer
drugs
requires
significant
amount
time,
demands
substantial
investments,
results
an
overall
low
percent
regulatory
approval.
complex
relationship
between
patent
protection
pharmaceutical
innovation
complicates
drug
contributes
to
high
mortality
rates.
Adjusting
criteria
for
therapeutics
could
stimulate
innovation,
enhance
options,
ultimately
improve
outcomes
patients.
This
article
explores
potential
therapeutics,
chemopreventive
agents,
natural
products,
off-patent
drugs,
generic
unpatentable
chemicals,
repurposed
treatment,
emphasizing
mechanisms
therapeutic
these
unconventional
compounds
as
combinatorial
therapies.
biological
pathways,
effects,
existing
are
reviewed,
demonstrating
their
cost-effective
accessible
options
adjuvant
New Journal of Chemistry,
Год журнала:
2024,
Номер
48(25), С. 11243 - 11258
Опубликована: Янв. 1, 2024
A
zinc
phosphate/hydroxyapatite
composite
(ZP/HAP)
with
a
core–shell
nano-rod
morphology
and
its
functionalized
derivative
β-cyclodextrin
(β-CD)
were
evaluated
as
potential
carriers
of
the
cisplatin
drug
(CPN).
Advanced Healthcare Materials,
Год журнала:
2024,
Номер
unknown
Опубликована: Ноя. 21, 2024
Abstract
A
transdermal
drug
delivery
cream,
which
is
non‐invasive
and
painless,
containing
a
liposome‐encapsulated
Ru(II)
complex
(
LipoRu
)
created
for
the
treatment
of
skin
cancer.
This
formulation
capitalizes
on
synergistic
antitumor
effects
two‐photon
excited
photodynamic
therapy
(PDT),
photothermal
(PTT),
chemotherapy.
exhibits
effective
tumor
accumulation,
efficient
cellular
uptake,
pH‐sensitive
infrared‐accelerated
release,
dual
localization
to
nucleus
mitochondria.
The
released
complexes
within
cells
exert
multiple
mechanisms,
such
as
DNA
topoisomerase
RNA
polymerase
inhibition,
Type
I
II
PDT,
PTT,
photodamage,
apoptosis
ferroptosis
induction.
biodistribution
therapeutic
efficacy
in
vivo
are
systematically
compared
via
three
distinct
administration
routes:
intratumoral
injection,
intravenous
through
topical
cream
application.
positive
fabricated
here
subcutaneous
tumor‐bearing
mice
offer
optimistic
potential
painless
both
early‐stage
advanced
cancers,
well
superficially
located
solid
tumors.
The
search
for
better
chemotherapeutic
drugs
to
alleviate
the
deficiencies
of
existing
platinum
(Pt)
has
picked
up
pace
in
millennium.
There
been
a
disparate
effort
design
and
safer
Pt
deal
with
problems
deactivation,
resistance
toxic
side
effects
clinical
drugs.
In
this
review,
we
have
discussed
potential
kinetically
inert
complexes
as
an
emerging
class
next-generation
introduction
gives
overview
about
development,
use,
mechanism
action
well
various
approaches
improve
some
their
pharmacological
properties.
We
then
describe
impact
kinetic
lability
on
pharmacology
functional
including
antitumor
efficacy,
toxicity
resistance.
Following
brief
numerous
advantages
that
non-functional
complex
can
offer;
structurally
different
classes
(II)
highlighting
unique
features.
