Journal of Enzyme Inhibition and Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
39(1)
Published: May 30, 2024
Tyrosinase,
a
pivotal
enzyme
in
melanin
synthesis,
is
primary
target
for
the
development
of
depigmenting
agents.
In
this
work,
vitro
and
silico
techniques
were
employed
to
identify
novel
tyrosinase
inhibitors
from
set
12
anilino-1,4-naphthoquinone
derivatives.
Results
mushroom
activity
assay
indicated
that,
among
derivatives,
three
compounds
(1,
5,
10)
demonstrated
most
significant
inhibitory
against
tyrosinase,
surpassing
effectiveness
kojic
acid.
Molecular
docking
revealed
that
all
studied
derivatives
interacted
with
copper
ions
amino
acid
residues
at
active
site.
dynamics
simulations
provided
insights
into
stability
enzyme–inhibitor
complexes,
which
1,
particularly
10
displayed
greater
stability,
atomic
contacts,
structural
compactness
than
Drug
likeness
prediction
further
strengthens
potential
anilino-1,4-naphthoquinones
as
promising
candidates
treatment
hyperpigmentation
disorders.
Biochemistry,
Journal Year:
2024,
Volume and Issue:
63(16), P. 2063 - 2074
Published: Aug. 7, 2024
Melanin
biosynthesis
in
different
organisms
is
performed
by
a
tyrosinase
action.
Excessive
enzyme
activity
and
pigment
accumulation
result
diseases
disorders
including
skin
cancers,
blemishes,
darkening.
In
fruits
vegetables,
it
causes
unwanted
browning
of
these
products
reduces
their
appearance
quality
economic
value.
Inhibiting
finding
novel
powerful
safe
inhibitors
are
highly
important
agriculture,
food,
medical,
pharmaceutical
industries.
this
regard,
the
present
study,
some
synthetic
pyridine-based
compounds
2,6-bis
(tosyloxymethyl)
pyridine
(compound
3),
(butylthiomethyl)
4),
(phenylthiomethyl)
5)
were
synthesized
for
first
time,
inhibitory
potencies
assessed
on
mushroom
diphenolase
activity.
The
results
showed
that
while
all
tested
significantly
decreased
activity,
4
5
had
highest
effects
(respectively,
80
89%
inhibition
with
IC50
values
17.0
9.0
μmol
L–1),
mechanism
was
mixed-type
both
compounds.
Ligand-binding
studies
carried
out
fluorescence
quenching
molecular
docking
methods
to
investigate
enzyme–compound
interactions.
Fluorescence
revealed
can
form
nonfluorescent
complexes
its
intrinsic
emission
static
process.
Molecular
analyses
predicted
binding
positions
amino
acid
residues
involved
These
appear
be
suitable
candidates
more
inhibition.
Plants,
Journal Year:
2023,
Volume and Issue:
12(21), P. 3741 - 3741
Published: Oct. 31, 2023
With
the
increase
in
global
life
expectancy,
maintaining
health
into
old
age
becomes
a
challenge,
and
research
has
thus
concentrated
on
various
strategies
which
aimed
to
mitigate
effects
of
skin
aging.
Aromatic
plants
stand
out
as
promising
sources
anti-aging
compounds
due
their
secondary
metabolites,
particularly
essential
oils
(EOs).
The
aim
this
study
was
ascribe
Ferulago
lutea
EO
several
biological
activities
that
could
be
useful
context
obtained
using
hydrodistillation
characterized
by
gas
chromatography–mass
spectrometry
(GC/MS).
anti-inflammatory
potential
assessed
lipopolysaccharide
(LPS)-stimulated
macrophages.
effect
cell
migration
disclosed
scratch
wound
assay.
Lipogenesis
induced
T0901317,
hyperpigmentation
with
3-isobutyl-1-methylxantine
(IBMX)
senescence
etoposide.
Our
results
show
mainly
α-pinene
limonene.
able
decrease
nitric
oxide
(NO)
release
well
iNOS
pro-IL-1β
protein
levels.
promoted
healing
while
decreasing
lipogenesis
having
depigmenting
effects.
also
reduced
senescence-associated
β-galactosidase,
p21/p53
levels
nuclear
accumulation
γH2AX.
Overall,
our
highlights
properties
F.
make
it
compelling
candidate
for
dermocosmetics
applications.
Journal of Research in Pharmacy,
Journal Year:
2024,
Volume and Issue:
28(2)(28(2)), P. 470 - 481
Published: Jan. 1, 2024
This
study
investigates
the
encapsulation
of
bakuchiol,
a
renowned
compound
for
hyperpigmentation
treatment,
utilizing
transfersomes
as
delivery
system.The
were
fabricated
using
thin-film
hydration
technique
and
subjected
to
thorough
characterization
across
various
parameters.The
resulting
transfersome
formulation,
after
optimization,
demonstrated
notably
high
efficiencies,
with
bakuchiol
registering
at
86.7±3.6%,accompanied
by
narrow
particle
size
distribution
(179.9
±
5.4
nm).In
vitro
release
studies
unveiled
cumulative
percentages
71.98±6.52%for
over
24-hour
period.Ex
vivo
permeation
further
affirmed
heightened
retention
within
skin
layers
compared
control
group.Stability
assessments
indicated
that
optimized
remained
stable
5°C
least
90
days.These
findings
underscore
remarkable
potential
in
facilitating
offering
compelling
viable
alternative
formulations.
Journal of Enzyme Inhibition and Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
39(1)
Published: May 30, 2024
Tyrosinase,
a
pivotal
enzyme
in
melanin
synthesis,
is
primary
target
for
the
development
of
depigmenting
agents.
In
this
work,
vitro
and
silico
techniques
were
employed
to
identify
novel
tyrosinase
inhibitors
from
set
12
anilino-1,4-naphthoquinone
derivatives.
Results
mushroom
activity
assay
indicated
that,
among
derivatives,
three
compounds
(1,
5,
10)
demonstrated
most
significant
inhibitory
against
tyrosinase,
surpassing
effectiveness
kojic
acid.
Molecular
docking
revealed
that
all
studied
derivatives
interacted
with
copper
ions
amino
acid
residues
at
active
site.
dynamics
simulations
provided
insights
into
stability
enzyme–inhibitor
complexes,
which
1,
particularly
10
displayed
greater
stability,
atomic
contacts,
structural
compactness
than
Drug
likeness
prediction
further
strengthens
potential
anilino-1,4-naphthoquinones
as
promising
candidates
treatment
hyperpigmentation
disorders.
