Chemistry & Biodiversity,
Год журнала:
2024,
Номер
unknown
Опубликована: Ноя. 11, 2024
Macroporous
resin
was
used
to
enrich
flavonoids
in
the
ethyl
acetate
extract
of
Artemisia
Selengensis
Turcz.
Based
on
a
single
factor
experiment,
enrichment
process
optimized
using
response
surface
method.
The
optimal
parameters
were
sample
concentration
0.3
mg/mL,
loading
rate
1
mL/min,
an
elution
flow
2
and
total
flavonoid
content
155.38±0.97
mg/g.
enriched
by
AB-8
macroporous
demonstrated
significant
scavenging
activities
against
DPPH,
ABTS
Drug Development Research,
Год журнала:
2025,
Номер
86(1)
Опубликована: Фев. 1, 2025
ABSTRACT
In
this
study,
hydrazine
clubbed
thiazole
derivatives
(
3a
–
3j
)
were
obtained
by
Hantzsch
synthesis
and
characterized
MS,
1
H
NMR,
13
C
NMR.
The
inhibitory
potentials
of
the
against
diabetes‐related
enzymes
such
as
aldose
reductase
(AR),
α‐glycosidase
(α‐GLY),
α‐amylase
(α‐AMY)
experimentally
determined,
results
supported
molecular
docking.
showed
that
displayed
varied
degree
potential
activity,
with
K
I
values
covering
following
ranges:
5.47
±
0.53
to
23.89
1.46
nM
for
AR
1.76
0.01
24.81
0.15
μM
α‐GLY,
IC
50
4.94–28.17
α‐AMY,
compared
standard
epalrestat
acarbose
:
34.53
2.52
23.53
2.72
respectively).
selective
activity
these
on
antidiabetic
may
be
important
treatment
diabetes
lead
development
alternative
new
compounds
purpose.
ACS Omega,
Год журнала:
2025,
Номер
10(9), С. 9368 - 9380
Опубликована: Фев. 26, 2025
A
series
of
chalcones
containing
a
pyrrolidine
moiety
were
synthesized
to
examine
their
in
vitro
α-amylase
and
α-glucosidase
inhibitory
activities,
for
the
treatment
Diabetes
mellitus,
which
is
one
most
dangerous
rapidly
increasing
disorders
today.
Compound
3
exhibited
an
excellent
dual
effect
with
IC50
value
14.61
±
0.12
μM
against
α-amylase,
IC50:
25.38
2.09
α-glucosidase.
The
cytotoxic
effects
all
compounds
nonsmall
lung
cancer
(A549)
bronchial
epithelial
normal
(BEAS-2B)
cell
lines
also
evaluated.
5
(IC50:
82.20
μM)
compound
8
59.96
showed
better
activity
than
cisplatin
A549
84.39
cells.
Furthermore,
these
had
no
harmful
on
healthy
BEAS-2B
cells
at
determined
values.
Moreover,
molecular
docking
dynamics
simulation
analysis
revealed
that
stronger
binding
affinities
toward
compared
positive
control
acarbose.
Drug Development Research,
Год журнала:
2025,
Номер
86(2)
Опубликована: Март 28, 2025
ABSTRACT
Recently,
there
has
been
an
increasing
interest
in
the
use
of
protein
kinase
inhibitors
as
a
therapeutic
strategy
for
treatment
cancer.
In
this
study,
new
series
2
H
‐chromene
derivatives
(
‐
5
and
6
8
)
3
‐benzo[
f
]chromene
carbohydrazide
derivative
9
were
synthesized.
The
structure
designed
was
characterized
by
IR,
1
H/
13
C
NMR,
elemental
analysis.
Moreover,
cytotoxic
activity
newly
synthesized
chromenes
evaluated
against
breast
cancer
cell
lines
(MDA‐MB‐231
MCF‐7)
cervical
line
(HeLa).
results
these
evaluations
demonstrated
promising
activity,
ranging
from
good
to
moderate.
Additionally,
lung
fibroblast
(WI‐38),
normal
line,
also
utilized
assess
active
derivatives'
selectivity.
Among
compounds
tested,
chromene
highest
potency,
exhibiting
IC
50
values
5.36
±
0.50,
7.82
0.60,
9.28
0.70
µM
MDA‐MB
231,
MCF‐7,
HeLa
lines,
respectively.
potential
chromone
multi‐targeted
anticancer
agent
assessed
evaluating
its
BRAF
VEGFR‐2.
Notably,
most
significant
VEGFR2
with
value
0.224
compared
sorafenib's
0.045
µM,
while
inhibitory
1.695
relative
Vemurafenib's
0.468
µM.
addition,
compound
inhibits
DHFR
enzyme
2.217
0.014
methotrexate
(IC
=
0.4315
0.019
µM).
These
revealed
that
multifaceted
mechanisms
action
may
augment
effectiveness.
causes
overexpression
caspase‐3
Bax
6.13
8.85‐fold,
It
downregulates
antiapoptotic
Bcl‐2
level
0.4775‐fold
untreated
231
cells.
Flow
cytometry
analysis
MDA‐MB‐231
cells
indicates
induces
cycle
arrest
G0‐G1
phase,
observed
percentage
73.15%.
in‐silico
toxicity
prediction
profile.
Finally,
molecular
docking
studies
supported
findings
confirming
strong
binding
affinities
VEGFR‐2,
BRAF,
DHFR.
