Molecules,
Год журнала:
2023,
Номер
28(4), С. 1739 - 1739
Опубликована: Фев. 11, 2023
Propolis
is
a
complex
natural
compound
that
honeybees
obtain
from
plants
and
contributes
to
hive
safety.
It
rich
in
phenolic
flavonoid
compounds,
which
contain
antioxidant,
antimicrobial,
anticancer
properties.
In
this
study,
the
chemical
composition
antioxidant
activities
of
propolis
were
investigated;
ABTS
Pharmaceuticals,
Год журнала:
2023,
Номер
16(5), С. 659 - 659
Опубликована: Апрель 28, 2023
Astragalus
species
are
traditionally
used
for
diabetes,
ulcers,
leukemia,
wounds,
stomachaches,
sore
throats,
abdominal
pain,
and
toothaches.
Although
the
preventive
effects
of
against
diseases
known,
there
is
no
record
therapeutic
alopecurus.
In
this
study,
we
aimed
to
evaluate
in
vitro
antiglaucoma,
antidiabetic,
anti-Alzheimer's
disease,
antioxidant
activities
methanolic
(MEAA)
water
(WEAA)
extracts
aerial
part
A.
Additionally,
its
phenolic
compound
profiles
were
analyzed
by
liquid
chromatography-tandem
mass
spectrometry
(LC-MS/MS).
MEAA
WEAA
evaluated
their
inhibition
ability
on
α-glycosidase,
α-amylase,
acetylcholinesterase
(AChE),
human
carbonic
anhydrase
II
(hCA
II)
enzymes.
The
compounds
LC-MS/MS.
Furthermore,
total
flavonoid
contents
determined.
context,
activity
was
1,1-diphenyl-2-picrylhydrazyl
(DPPH),
2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic
acid)
(ABTS),
N,N-dimethyl-p-phenylene
diamine
(DMPD),
ferric
reducing
power
(FRAP),
cupric
ions
(Cu2+)
capacity
(CUPRAC),
(Fe3+)
reducing,
ferrous
(Fe2+)
chelating
methods.
had
IC50
values
9.07
2.24
μg/mL
693.15
346.58
1.99
2.45
AChE,
147.7
171.7
hCA
II.
While
amounts
16.00
18.50
μg
gallic
acid
equivalent
(GAE)/mg
extract,
both
calculated
as
66.23
33.115
quercetin
(QE)/mg,
respectively.
showed,
respectively,
variable
DPPH
radical
scavenging
(IC50:
99.02
115.53
μg/mL),
ABTS
32.21
30.22
µg/mL),
DMPD
231.05
65.22
Fe2+
46.21
33.01
μg/mL).
abilities
were,
Fe3+
(λ700:
0.308
0.284),
FRAP
(λ593:
0.284
CUPRAC
(λ450:
0.163
0.137).
A
35
phenolics
scanned,
10
determined
LC-MS/MS
analysis.
revealed
that
mainly
contained
isorhamnetin,
fumaric
acid,
rosmarinic
derivatives.
This
first
report
indicating
have
abilities,
activities.
These
results
demonstrate
potential
through
properties
enzyme
inhibitor
medicine.
work
provides
foundation
further
research
into
establishment
novel
therapeutics
glaucoma,
Alzheimer's
disease.
Abstract
The
development
of
innovative
pharmacological
formulations
for
the
treatment
and
prevention
various
major
diseases,
including
cancer,
diabetes,
glaucoma,
has
been
facilitated
by
some
natural
compounds.
This
study
tested
inhibitory
effects
isofraxidin
on
acetylcholinesterase,
α‐glycosidase,
butyrylcholinesterase
enzymes,
as
well
human
carbonic
anhydrase
I
II
(hCA
II)
isoenzymes.
Esterase
activity
was
used
to
gauge
Isofraxidin's
ability
inhibit
CA
(in
vitro).
For
isoenzymes
hCA
II,
half
maximal
concentration
(IC
50
)
values
were
determined
be
67.61
52.42
nM,
respectively.
At
same
manner,
inhibition
constant
(K
i
12.58±0.50
4.41±0.35
Then,
IC
value
compound
acetylcholinesterase
(AChE)
(BChE)
calculated
18.50
10.75
On
other
hand,
K
α‐glycosidase
55.16
56.81±2.30
Additionally,
antioxidant
properties
investigated
using
techniques
like
2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulfonic
acid)
(ABTS),
1,1‐Diphenyl‐2‐picrylhydrazyl
(DPPH),
N,N‐dimethyl‐ρ‐phenylenediamine
(DMPD),
cupric
ions
(Cu
2+
reducing
capacity
(CUPRAC),
iron
reduction
procedures.
Following
graphing
results,
determined.
As
a
result,
phenolic
molecule
showed
strong
profiles
profile.
We
therefore
think
that
these
findings
may
pave
way
novel
therapeutic
management
illnesses.
Several
plant‐based
substances
extracts
have
gained
attention
in
recent
years
potential
inhibitors
enzyme.
activities
Isofraxidin
with
enzyme
proteins
compared.
Finally,
ADME/T
analysis
performed
predict
movements
molecules
metabolism.
Chemical Biology & Drug Design,
Год журнала:
2024,
Номер
103(2)
Опубликована: Фев. 1, 2024
Abstract
In
this
project,
non‐sulfonamide
bistrifluoromethyl‐derived
hydrazide‐hydrazones
were
synthesized
as
multi‐target‐directed
ligands
to
treat
Alzheimer's
disease
and
then,
the
novel
derivatives
characterized
by
diverse
spectral
methods.
Acetylcholinesterase
(AChE),
human
carbonic
anhydrase
(hCA)
inhibitory
qualifications
of
these
compounds
determined.
The
reported
(
2a
‐
y
)
determined
be
effective
inhibitors
hCA
I,
II
AChE
enzymes
with
K
i
values
in
range
1.130
±
0.15–5.440
0.93
μM
for
0.894
0.05–6.647
1.35
II,
0.196
0.03–4.222
1.04
AChE.
silico
studies
also
performed
illuminate
binding
interactions.
Abstract
A
series
of
coumarin‐1,3,5‐triazine
derivatives
were
designed,
synthesized
and
evaluated
as
acetylcholinesterase
inhibitors.
The
structures
those
compounds
characterized
by
IR,
NMR,
HRMS,
HPLC,
X‐ray.
are
the
mixtures
two
geometric
isomers.
1
H‐NMR
compound
3
g
without
coumarin
structure
its
hydrochloride
single
crystal
studied
to
prove
butyrylcholinesterase
inhibitory
activities
determinated
Ellman's
method.
results
showed
that
all
could
inhibit
selectively.
Among
them,
b
was
found
have
strongest
effect
on
with
an
IC
50
value
0.018
μM,
which
closest
positive
control
donepezil
(IC
=0.016
μM).
Enzyme
kinetic
studies
indicate
this
inhibited
a
mixed
mode.
Molecular
docking,
molecular
dynamics
simulation
study
binding
free
energy
calculation
experiments
demonstrated
stably
interact
key
amino
acids
in
catalytically
active
site
peripheral
anion
acetylcholinesterase.
According
results,
demonstrates
promising
potential
inhibitors
for
treatment
Alzheimer's
disease.
