Biomolecules,
Год журнала:
2024,
Номер
14(12), С. 1535 - 1535
Опубликована: Ноя. 30, 2024
Despite
significant
advances
in
drug
discovery
and
the
promising
antitumor
potential
of
combretastatin
A4
(CA-4),
which
selectively
targets
rapidly
dividing
cancer
cells,
CA-4’s
effects
on
non-dividing
human
such
as
peripheral
blood
mononuclear
cells
(PBMCs),
remain
unclear.
The
aim
this
study
is
to
evaluate
vitro
bioactivity
CA-4
PBMCs,
focusing
its
antigenotoxic
antioxidant
properties,
while
comparing
cytotoxic
potency
against
cell
lines
(JAR
HeLa),
normal
trophoblast
line
HTR-8/SVneo.
Cell
viability
metabolic
activity
were
evaluated
using
MTT
assay.
ROS
production
PBMCs
was
measured
H2DCFDA
assay,
DNA
damage
assessed
Comet
showed
cytotoxicity
HTR-8/SVneo
at
concentrations
above
200
µM,
JAR
HeLa,
100
µM
1
respectively.
also
reduced
levels
under
oxidative
stress
from
µM.
In
addition,
H2O2-induced
up
exhibited
lower
compared
inhibited
production,
providing
insight
into
therapeutic
efficacy
safety.
Results in Chemistry,
Год журнала:
2024,
Номер
7, С. 101511 - 101511
Опубликована: Янв. 1, 2024
Cancer
and
bacterial
infections
are
among
the
most
high-interest
health
threats
facing
humanity.
The
growing
resistance
to
current-found
anticancer
antibacterial
drugs
necessitates
exploration
of
new,
effective
agents.
To
synthesize
some
them,
4-chloroskimmetine
(4-CSM),
with
undefined
biological
effects,
was
used
as
a
building
block
create
thirteen
its
derived
coumarins.
This
precursor
Bargellini
reaction
were
produce
first
coumarin,
designated
Y0.
From
which,
twelve
coumarins
coded
Y1-Y12
created
by
esterifying
Y0
various
halophenols
using
SOCl2-promoted
reaction.
FTIR,
1HNMR,
13CNMR
spectra
analyzed
ascertain
chemical
framework
Their
potential
function
prospects
evaluated
against
six
cancer-derived
populations
employing
preliminary
MTT-facilitated
methodology.
These
MCF-7,
HeLa,
SKG,
AMN3,
SK-OV-3,
KYSE-30.
On
other
hand,
broth
microdilution
protocol
followed
specify
activity
high-infective
aerobes.
include
Pseudomonas
aeruginosa,
Shigella
dysenteriae,
Haemophilus
influenza,
Klebsiella
pneumonia,
Escherichia
coli,
Salmonella
typhi.
results
evaluation
indicated
that
presence
fluoride
on
off-side
aromatic
ring
afforded
potent
activity,
Y5
best.
For
second
same
findings
true,
but
when
halogen
is
chloride
Y2
superior
one.
authors
concluded
4-CSM,
can
be
exploited
bioactive
activities.
Also,
considered
promising
structural
templates
for
producing
medications,
respectively.
Results in Chemistry,
Год журнала:
2024,
Номер
7, С. 101494 - 101494
Опубликована: Янв. 1, 2024
Various
pharmacological
properties
of
coumarins
brought
them
under
light
among
the
heterocyclics.
Also,
coumarin
derivatives
still
approve
their
importance
in
medical
field
as
a
valuable
building
block
to
elicit
further
with
diverse,
potent,
and
interesting
biological
activities.
Moreover,
numerous
actions
thiadiazole-based
compounds
contribute
notion
this
unique
synthesis
linearly
fused
thiadiazolocoumarins
using
molecular
hybridization
method.
This
work
reported
novel
seven
thiadiazolocoumarins,
including
Precursor
N-III
TDA1-TDA6.
These
were
characterized
by
physicochemical
through
spectrophotometric
tools,
FTIR,
1H
NMR,
13C
NMR.
pharmacokinetics
predicted
computer-based
studies
SwissADME
PreADMET
programs.
Furthermore,
checked
for
several
activities,
anticancer,
biosafety,
anti-oxidative
stress,
anti-inflammatory,
antimicrobial,
normal
flora
safety,
antidiabetic
According
results,
TDA3
showed
greatest
anticancer
activity
against
examined
cancer
cell
lines,
highest
cellular
biosafety.
TDA4
higher
stress
than
other
derivatives.
All
prepared
significant
inflammation-inhibitory
toward
LOX-5
enzyme
while
showing
poor
towards
COX
enzymes.
antimicrobial
activity,
exhibited
anti-gram-negative
also
best
safety
flora.
TDA1
promising
anaerobic
bacteria,
N-III,
TDA3,
antifungal
activity.
Finally,
demonstrated
moderate
which
was
The
authors
concluded
from
gathered
results
that
represent
key
structures
developing
versatile
bioactivities.
Chemistry & Biodiversity,
Год журнала:
2024,
Номер
21(6)
Опубликована: Апрель 15, 2024
For
the
first
time,
kinetic
thermomagnetic
extraction
is
a
novel
approach
presented
in
this
work.
It
required
application
of
four
distinct
variables:
rotation
speed
(50,
75,
and
100
rpm),
magnetic
field
(0.8,
1.2,
1.6
T),
time
interval
(30,
60,
90
min),
temperature
(45,
55,
65
°C).
Numerous
phytochemical
categories
were
detected
81
crude
chloroform
extracts
green
sweet
bell
pepper
seeds
that
collected,
according
to
analysis.
Nine
discovered
be
linked
coumarin
chemical
class
have
same
two
parameters:
90-minute
duration
55
°C
temperature.
To
enable
their
contents
chemically
separated
chromatographically
purified,
these
containing
chosen.
Four
new
phytocoumarins
been
identified
molecular
structures
distinguished
using
FTIR
spectra,
