Innovative Biosystems and Bioengineering,
Год журнала:
2023,
Номер
7(3), С. 55 - 64
Опубликована: Окт. 29, 2023
Background.
Excessive
melanin
accumulation
in
the
skin
can
lead
to
various
diseases
and
cosmetic
issues.
While
tyrosinase
inhibitors
are
commonly
used
reduce
pigment
biosynthesis,
many
of
them
associated
with
significant
side
effects.
When
multiple
drugs
combination,
it
result
synergism,
additive
effects,
or
antagonism.
Combining
is
considered
a
promising
approach
minimize
effects
enhance
therapeutic
efficacy.
Objective.
This
study
aims
investigate
combined
use
determine
nature
their
interaction,
whether
it's
synergistic
additive.
Methods.
We
utilized
isolated
from
Agaricus
bisporus
mushrooms.
Enzyme
inhibition
by
test
compounds
was
assessed
measuring
activity
using
tyrosine
(30
min
0.05
M
Na-phosphate
buffer
solution,
pH
6.5,
25
°C).
To
explore
joint
inhibition,
compound
solutions
were
mixed
pairs
at
concentrations.
The
interaction
quantified
combination
index
isobolograms.
Results.
effect
action
agents
on
activity,
we
examined
standard
enzyme
(kojic
acid,
arbutin,
phenylthiourea)
our
discovered
compound,
3-(2-hydroxyphenylamino)-1,3-dihydro-indol-2-one.
Calculations
isobolograms
for
all
studied
combinations
revealed
cases.
Simultaneous
kojic
acid
arbutin
3-(2-hydroxyphenylamino)-1,3-dihydro-indol-2-one
demonstrated
effect.
However,
mixture
phenylthiourea
indole
derivative
an
Conclusions.
usage
displayed
both
two
simultaneously
presents
opportunities
development
more
effective
cost-efficient
treatments
hyperpigmentation
reducing
concentration
each
inhibitor.
Journal of Dairy Science,
Год журнала:
2024,
Номер
107(7), С. 4174 - 4188
Опубликована: Фев. 2, 2024
Complete
self-assembly
and
reassembly
behavior
of
bitter
peptide-protein
necessitates
multilevel
theories
that
encompass
phenomena
ranging
from
the
recombinant
complex
to
atomic
trajectories.
An
extension
level
mechanism
method
was
put
forth,
involves
limited
enzymatic
digestion
bottom-up
proteomics
dissect
inherent
heterogeneity
within
β-lactoglobulin
β-lactoglobulin-PPGLPDKY
uncover
conformational
dynamic
alterations
occurring
in
specific
local
regions
model
protein.
Bitter
peptide
PPGLPDKY
spontaneously
bound
IIAEKTK,
IDALNENK,
YLLFCMENSAEPEQSLACQCLVR
1:1
stoichiometric
ratio
mask
bitterness
perception.
Molecular
simulation
free
energy
calculation
provided
time-varying
trajectories
complex,
found
stabilized
upper
region
hydrophobic
cavity
with
binding
−30.56
kJ
mol−1
through
4
hydrogen
bonds
(Glu74,
Glu55,
Lys69,
Ser116)
interactions
(Asn88,
Asn90
Glu112).
Current
research
endeavors
provide
valuable
physical
insights
into
macroscopic
between
protein
peptide,
meticulous
design
highly
acceptable
taste
characteristics
goat
milk
products.
Ageing Research Reviews,
Год журнала:
2024,
Номер
100, С. 102406 - 102406
Опубликована: Июль 11, 2024
Urolithin
A
(UA)
is
a
gut
metabolite
derived
from
ellagic
acid.
This
systematic
review
assesses
the
potential
geroprotective
effect
of
UA
in
humans.
In
five
studies
including
250
healthy
individuals,
(10-1000
mg/day)
for
duration
ranging
28
days
to
4
months,
showed
dose-dependent
anti-inflammatory
and
upregulated
some
mitochondrial
genes,
markers
autophagy,
fatty
acid
oxidation.
It
did
not
affect
maximal
adenosine
triphosphate
production,
biogenesis,
dynamics,
or
microbiota
composition.
increased
muscle
strength
endurance,
however,
had
no
on
anthropometrics,
cardiovascular
outcomes,
physical
function.
Unrelated
adverse
events
were
mild
moderate.
Further
research
across
more
physiological
systems
longer
intervention
periods
required.
Food & Function,
Год журнала:
2024,
Номер
15(14), С. 7452 - 7467
Опубликована: Янв. 1, 2024
Dental
caries
is
a
chronic
and
destructive
disease
matrix
metalloproteinase-2
(MMP-2)
plays
major
role
in
caries.
The
inhibitory
mechanisms
of
theaflavins
[theaflavin
(TF1),
theaflavin-3-gallate
(TF2A),
theaflavin-3'-gallate
(TF2B),
theaflavin-3,3'-digallate
(TF3)]
on
MMP-2
were
investigated
using
techniques
such
as
enzyme
inhibition
kinetics,
multi-spectral
methods,
molecular
docking,
dynamics
simulations.
results
showed
that
TF1,
TF2A,
TF2B,
TF3
all
competitively
reversibly
inhibited
activity.
Fluorescence
spectra
docking
indicated
four
spontaneously
bind
to
through
noncovalent
interactions,
driven
by
hydrogen
bonds
hydrophobic
constituting
static
quenching
mechanism
resulting
an
altered
tryptophan
residue
environment
around
MMP-2.
Molecular
dynamic
simulations
demonstrated
can
form
stable,
compact
complexes
with
In
addition,
the
order
theaflavins'
ability
inhibit
was
found
be
TF1
>
TF2B
TF2A
TF3.
Interestingly,
binding
capacity
between
consistent
capacity,
opposite
steric
hindrance
theaflavins.
This
may
due
narrow
space
active
pocket
MMP-2,
smaller
theaflavins,
easier
it
enter
study
provided
novel
insights
into
functional
components
exploration
natural
inhibitors.
Scientific Reports,
Год журнала:
2025,
Номер
15(1)
Опубликована: Март 22, 2025
Considering
the
global
incidence
of
diabetes,
developing
new
compounds
to
lower
blood
sugar
levels
has
become
increasingly
crucial.
As
a
result,
there
been
growing
focus
on
synthesis
α-glucosidase
inhibitors
in
recent
years.
This
study
investigated
design,
synthesis,
and
effects
novel
5-aryl
pyrazole-glucose
hybrids
as
inhibitors.
Thirteen
derivatives
from
this
class
were
synthesized,
demonstrating
superior
vitro
inhibitory
(IC50
values
ranging
0.5
438.6
µM,
compared
acarbose
at
750.0
µM).
Among
them,
compound
8g
=
µM)
was
selected
for
further
investigations
kinetic
studies
revealed
that
it
is
competitive
inhibitor
(Ki
0.46
Fluorescence
assays
indicated
changes
fluorescence
intensity,
while
thermodynamic
analyses
suggested
promoted
transition
enzyme
into
an
unfolded
state.
Furthermore,
vivo
demonstrated
effectively
reduced
rats
doses
comparable
acarbose.
Molecular
docking
interacted
with
enzyme's
active
site,
molecular
dynamics
simulations
showed
pharmacophores
engaged
various
interactions
enzyme.
