Abstract
Enzyme
inhibition
is
a
frequently
employed
technique
for
regulating
enzyme
activity
in
several
biological
systems
that
are
physiologically
significant.
In
this
study,
it
was
evaluated
the
effectiveness
of
six
specific
quinolone
medicines,
namely
lomefloxacin,
nalidixic
acid,
gatifloxacin,
norfloxacin,
sparfloxacin
and
nitrofurantoin,
inhibiting
two
human
isoforms
carbonic
anhydrase
(hCA)
play
role
different
physiological
pathological
circumstances.
order
to
achieve
objective,
both
vitro
silico
investigations
were
conducted
get
deeper
understanding
potential
binding
interactions
affinities
hCA
I
II
isoforms.
The
kinetic
inhibitory
effects
(K
i
s)
ranged
from
1.31
13.07
μM,
comparison
reference
medication
acetazolamide
(AAZ,
K
0.12
μM).
addition,
effectively
suppressed
by
these
drugs,
with
s
ranging
1.42
11.93
compared
AAZ
0.098
Significant
between
medicines
hCAs
indicated
their
support
therapeutic
targets
against
diseases.
Furthermore,
findings
acquired
will
contribute
enhancement
dose
regimens
medications
prevention
unforeseen
drug‐drug
when
administered
concurrently
other
substances.
Scientific Reports,
Год журнала:
2025,
Номер
15(1)
Опубликована: Апрель 14, 2025
Diabetes
mellitus,
as
a
common
chronic
disease,
easily
leads
to
significant
changes
in
the
structure
of
eye,
among
which
diabetic
cataract
is
particularly
common.
Although
surgery
main
treatment
for
this
complication,
it
may
be
accompanied
by
postoperative
complications.
Therefore,
important
develop
specific
drugs
cataract,
aiming
fundamentally
reduce
its
incidence
and
need
surgery.
At
present,
greatest
challenge
therapeutic
agents
with
multiple
synergistic
effects
based
on
complex
pathogenesis
cataract.
1-Acetyl-5-phenyl-1
H-pyrrol-3-ylacetate
(APPA)
designed
pathological
mechanism
potential
drug
alleviate
occurrence
Our
observations
suggest
that
APPA
more
effective
than
bendazaclysine
alleviating
high
galactose-induced
oxidative
stress
(The
malondialdehyde
content
group
was
significantly
reduced
0.45-fold
0.58-fold
compared
group,
respectively.)
apoptosis
rate
0.28-fold
0.35-fold
lens
epithelial
cells
increasing
antioxidant
enzyme
activity,
restoring
mitochondrial
homeostasis.
Mechanistic
studies
have
shown
restoration
homeostasis
mediated
through
SIRT1-PGC-1α
pathway.
In
rat
model,
conclusion,
functions
has
wider
range
indications
benzydalysine.
Abstract
Enzyme
inhibition
is
a
frequently
employed
technique
for
regulating
enzyme
activity
in
several
biological
systems
that
are
physiologically
significant.
In
this
study,
it
was
evaluated
the
effectiveness
of
six
specific
quinolone
medicines,
namely
lomefloxacin,
nalidixic
acid,
gatifloxacin,
norfloxacin,
sparfloxacin
and
nitrofurantoin,
inhibiting
two
human
isoforms
carbonic
anhydrase
(hCA)
play
role
different
physiological
pathological
circumstances.
order
to
achieve
objective,
both
vitro
silico
investigations
were
conducted
get
deeper
understanding
potential
binding
interactions
affinities
hCA
I
II
isoforms.
The
kinetic
inhibitory
effects
(K
i
s)
ranged
from
1.31
13.07
μM,
comparison
reference
medication
acetazolamide
(AAZ,
K
0.12
μM).
addition,
effectively
suppressed
by
these
drugs,
with
s
ranging
1.42
11.93
compared
AAZ
0.098
Significant
between
medicines
hCAs
indicated
their
support
therapeutic
targets
against
diseases.
Furthermore,
findings
acquired
will
contribute
enhancement
dose
regimens
medications
prevention
unforeseen
drug‐drug
when
administered
concurrently
other
substances.
