Micro,
Год журнала:
2024,
Номер
4(4), С. 734 - 750
Опубликована: Ноя. 27, 2024
Mycoplasma
infections
pose
significant
challenges
in
the
poultry
industry,
necessitating
effective
therapeutic
interventions.
Tiamulin,
a
veterinary
antibiotic,
has
demonstrated
efficacy
against
species.
However,
emergence
of
resistant
species
could
dramatically
reduce
potential,
contributing
to
economic
losses.
Optimizing
tiamulin’s
pharmacokinetic
profile
via
nanocarrier
incorporation
enhance
its
potential
and
administration
frequency,
ultimately
reducing
strain
emergence.
Niosomes,
type
self-assembled
non-ionic
surfactant-based
nanocarrier,
have
emerged
as
promising
drug
delivery
system,
offering
improved
stability,
sustained
release,
enhanced
bioavailability.
In
this
study,
niosomal
nanocarriers
encapsulating
tiamulin
were
prepared,
characterized
assessed
Mycoplasma-inoculated
broilers
following
oral
administration.
Differential
scanning
colorimetry
(DSC)
confirmed
alterations
crystalline
state
components
integration
into
structures
formed
during
formulation
procedure.
Transmission
electron
microscopy
(TEM)
showed
spherical
nanostructure
niosomes.
The
formulated
exhibited
zeta
average
hydrodynamic
diameter
−10.65
±
1.37
mV
339.67
30.88
nm,
respectively.
Assessment
parameters
gallisepticum-infected
revealed
ability
increase
bioavailability
systemic
exposure,
marked
by
significantly
higher
area
under
curve
(AUC)
(p
<
0.01)
prolonged
elimination
half-life
(T1/2)
0.05).
Enhanced
residence
time
are
crucial
factors
maintaining
concentrations
at
reduced
doses
frequencies.
This
approach
provides
viable
strategy
decrease
risk
subtherapeutic
levels,
thereby
mitigating
development
antibiotic
resistance.
findings
presented
herein
offer
sustainable
for
efficient
use
antibiotics
medicine.
The Journal of Steroid Biochemistry and Molecular Biology,
Год журнала:
2024,
Номер
243, С. 106581 - 106581
Опубликована: Июль 10, 2024
Despite
being
the
focal
point
of
decades
research,
female
breast
cancer
(BC)
continues
to
be
one
most
lethal
cancers
in
world.
Given
that
80
%
all
diagnosed
BC
cases
are
estrogen
receptor-positive
(ER+)
with
carcinogenesis
driven
by
estrogen-ERα
signalling,
current
standard
care
(SOC)
hormone
therapies
geared
towards
modulating
function
and
expression
levels
its
receptors,
ERα
ERβ.
Currently,
aromatase
inhibitors
(AIs),
selective
ER
modulators
(SERMs)
degraders
(SERDs)
clinically
prescribed
for
management
treatment
ER+
BC,
anti-aromatase
activity
AIs
abrogating
biosynthesis,
while
anti-estrogenic
SERMs
SERDs
antagonise
degrade
ER,
respectively.
The
use
SOC
is,
however,
significantly
hampered
onset
severe
side-effects
development
resistance.
numerous
studies
have
reported
on
beneficial
effects
plant
compounds
and/or
extracts
multiple
pathways
through
which
they
target
carcinogenesis,
recent
research
has
focused
dietary
chemopreventive
agents
management.
When
combined
treatments,
several
these
components
demonstrated
improved
efficacy
synergistic
impact.
Moreover,
despite
a
lack
vivo
investigations,
products
generally
lower
side-effect
profile
than
therefore
thought
safer
therapeutic
choice.
Thus,
review
summarizes
findings
from
last
five
years
regarding
products,
as
well
their
anti-ER+
combination
therapies.
Scientific Reports,
Год журнала:
2024,
Номер
14(1)
Опубликована: Окт. 28, 2024
Pistacia
lentiscus
L.
is
an
aromatic
plant
containing
a
significant
percentage
of
essential
oil
(EO)
used
in
fragrance,
pharmaceuticals,
cosmetics,
and
the
food
industry.
The
purpose
this
work
focused
on
optimization
oleo
gum
resin
EO
yield
extracted
by
superheated
steam
extraction
(SHSE)
response
surface
methodology,
including
parameters
particle
size
(0.
5
−
1
mm),
temperature
(140–180
°C)
time
(90–150
min).
optimum
conditions
for
SHSE
were
found
to
be
(particle
size:
0.75
mm,
time:
120
min
temperature:
160
℃)
which
produced
highest
5.7%.
A
regression
model
was
developed,
demonstrating
robust
quadratic
correlation
with
R2
value
0.9991,
making
it
suitable
predictions.
Furthermore,
compared
conventional
hydro
distillation
techniques.
study
revealed
that
yielded
higher
quantities
than
other
methods.
GC-MS
analyzed
chemical
composition
EO.
predominant
compound
determined
α-pinene,
while
identified
compounds
include
trans-verbenol,
verbenol,
cis-verbenone,
camphene,
β-myrcene,
d-limonene,
cymene,
α-myrtenol,
α-campholenal,
α-copaene,
α-thujene,
whose
content
differed
according
different
Overall,
efficient
technique
extracting
enhances
yield,
requiring
less
extraction.
Journal of Drug Delivery Science and Technology,
Год журнала:
2023,
Номер
89, С. 105047 - 105047
Опубликована: Окт. 5, 2023
As
the
globe's
population
increases,
incidences
of
Alzheimer's
disease
(AD)
are
steadily
increasing.
AD
represents
most
common
neurological
disorder
and
constitutes
60–70%
all
dementia
cases.
The
accumulation
amyloid
plaques,
intraneuronal
fibrillary
tangles,
decrease
in
choline
acetyltransferase,
loss
cholinergic
neurons
considered
hallmarks
AD.
current
FDA-approved
anti-AD
drugs
can
only
inhibit
symptoms
for
a
limited
time
without
stopping
or
reversing
progression
disease.
In
addition,
their
clinical
applications
hindered
by
partial
ability
to
cross
blood-brain
barrier
(BBB),
poor
bioavailability,
systemic
adverse
effects.
Nevertheless,
nanoformulation
synthetic
natural
into
advanced
nanodelivery
systems
has
been
utilized
efficient
brain
delivery.
addition
brief
introduction
AD,
its
pathology,
treatment
options,
this
review
sheds
light
on
novel
used
recently
delivery
various
therapeutic
agents.
ACS Omega,
Год журнала:
2023,
Номер
8(41), С. 37864 - 37881
Опубликована: Окт. 6, 2023
Translation
of
mRNA
is
one
the
processes
adopted
by
cancer
cells
to
maintain
survival
via
phosphorylated
(p)-eIF4E
overexpression.
Once
p-eIF4E
binds
cap
structure
mRNA,
it
advocates
a
nonstop
translation
process.
In
this
regard,
15
new-based
GMP
analogs
were
synthesized
target
eIF4E
and
restrain
its
binding
mRNA.
The
compounds
tested
against
three
types
cell
lines:
Caco-2,
HepG-2,
MCF-7,
normal
kidney
(Vero
cells).
Most
showed
high
potency
breast
(MCF-7),
characterized
highest
type
for
overexpression
p-eIF4E.
Compound
4b
was
found
be
most
active
lines,
colon
(Caco-2),
hepatic
(HepG-2),
with
positive
IC50
values
31.40,
27.15,
21.71
μM,
respectively.
Then,
chitosan-coated
niosomes
loaded
compound
(Cs/4b-NSs)
developed
(as
kinetically
enhanced
molecules)
improve
anticancer
effects
further.
prepared
Cs/4b-NSs
pronounced
cytotoxicity
compared
free
Caco2,
Hepg2,
MCF-7
16.15,
26.66,
6.90
expression
both
nonphosphorylated
western
blot
techniques
conducted
on
treated
(based
obtained
values)
determine
total
protein
p-eIF4e.
Interestingly,
selected
displayed
35.8–40.7%
inhibition
when
evaluated
Ribavirin
(positive
control).
CS/4b-NSs
best
(40.7%).
findings
present
joint
in
silico
molecular
docking,
simulation
dynamic
studies,
experimental
investigation
suggest
potential
use
niosomal
nanovesicles
as
promising
nanocarrier
targeted
delivery
newly
eukaryotic
initiation
factor
4E.
These
outcomes
support
possible
therapy.
Cancers,
Год журнала:
2024,
Номер
16(11), С. 2033 - 2033
Опубликована: Май 27, 2024
Numerous
studies
have
reported
that
Dyrk1A,
Dyrk1B,
and
Clk1
are
overexpressed
in
multiple
cancers,
suggesting
a
role
malignant
disease.
Here,
we
introduce
novel
class
of
group-selective
kinase
inhibitors
targeting
Clk1.
This
was
achieved
by
modifying
our
earlier
selective
inhibitors,
which
were
based
on
the
5-methoxybenzothiophene-2-carboxamide
scaffold.
By
incorporating
5-hydroxy
group,
increased
potential
for
additional
hydrogen
bond
interactions
broadened
inhibitory
effect
to
include
Dyrk1A
Dyrk1B
kinases.
Within
this
series,
compounds
12
17
emerged
as
most
potent
multi-kinase
against
Furthermore,
when
assessed
closely
related
kinases
also
implicated
cancer,
frontrunner
revealed
activity
Haspin
Clk2.
Compounds
displayed
high
potency
across
various
cancer
cell
lines
with
minimal
non-tumor
cells.
examining
these
cycle
distribution,
compound
retained
cells
G2/M
phase
induced
apoptosis.
could
increase
levels
cleaved
caspase-3
Bax,
while
decreasing
expression
antiapoptotic
Bcl-2
protein.
These
findings
support
further
study
development
anticancer
therapeutics.
