Assessment of Antidiarrheal Effect of Oleuropein Through µ‐Oopioid Receptor Interaction Pathway: In Vivo and in Silico Studies
Drug Development Research,
Год журнала:
2025,
Номер
86(1)
Опубликована: Фев. 1, 2025
Oleuropein
(OLP),
a
compound
predominantly
found
in
olive
leaves,
has
been
known
for
its
numerous
biological
activities,
including
antioxidant,
anti-inflammatory,
and
antimicrobial
properties.
Despite
established
therapeutic
potential,
role
treating
diarrhea
not
extensively
explored.
This
study
aimed
to
evaluate
the
antidiarrheal
effects
of
OLP
an
vivo
model
investigate
molecular
interactions
using
silico
docking
studies,
pharmacokinetic
predictions,
toxicity
analysis.
In
study,
castor
oil
was
used
induce
3-day-old
chicks,
effect
tested
at
doses
10
20
mg/kg.
The
standard
drug,
loperamide
(LOP)
3
mg/kg,
comparison.
results
showed
that
both
significantly
(p
<
0.05)
reduced
diarrheal
secretions
increased
latency,
with
mg/kg
dose
demonstrating
most
effective
results.
combination
(20
mg/kg)
LOP
(3
further
enhanced
effect.
revealed
exhibited
strong
binding
affinities
(BAs)
key
receptor,
μ-opioid
receptor
associated
diarrhea,
while
higher
BA
(‒8.9
kcal/mol)
compared
(‒8.7
kcal/mol).
Pharmacokinetic
analysis
favorable
properties
studies
no
acute
toxicity,
LD50
2000
conclusion,
findings
suggest
possesses
significant
potential
through
interaction,
positioning
it
as
promising
natural
agent
managing
diarrhea.
Further
are
warranted
fully
elucidate
mechanisms
action
clinical
applicability.
Язык: Английский
Tangeretin enhances sedative activity of diazepam in Swiss mice through GABAA receptor interaction: In vivo and in silico approaches
Neuroscience,
Год журнала:
2025,
Номер
572, С. 1 - 10
Опубликована: Март 5, 2025
Язык: Английский
Anti-arthritic potential of linalool: in vitro, in vivo, and in silico mechanistic insights for safer therapeutic applications
Naunyn-Schmiedeberg s Archives of Pharmacology,
Год журнала:
2025,
Номер
unknown
Опубликована: Март 7, 2025
Язык: Английский
Protective Effects of Multiple-Chemical Engineered Biochar On Hormonal Signalling, Antioxidant Pathways and Secondary Metabolites in Lavender Exposed to Chromium and Fluoride Toxicity
Deleted Journal,
Год журнала:
2025,
Номер
77(2)
Опубликована: Март 11, 2025
Язык: Английский
Citronellal Exerts Sedative‐Like Effects and Augments Diazepam's Action in Swiss Mice, Possibly Through the GABAergic Pathway
Brain and Behavior,
Год журнала:
2025,
Номер
15(3)
Опубликована: Март 1, 2025
ABSTRACT
Introduction
Citronellal
(CTL),
a
monoterpenoid,
exhibits
notable
neurological
activity,
including
anxiolytic,
and
anticonvulsant
effects,
primarily
through
GABAergic
pathways.
Our
current
study
aimed
to
explore
CTL's
sedative
potential
using
in
vitro,
vivo,
silico
approaches
the
pathway.
Methods
The
vitro
activity
of
CTL
was
assessed
via
colorimetric
assay,
while
acute
toxicity
evaluated
Swiss
mice
per
OECD
guidelines
with
doses
up
2000
mg/kg
establish
safety
margins.
Sedative
effects
were
thiopental
sodium
(TS,
40
mg/kg)‐induced
sleep
protocols.
administered
at
62.5,
125,
250
doses,
alone
or
combined
diazepam
(DZP,
2
mg/kg)
flumazenil
(FLU,
0.1
mg/kg).
studies
also
performed
GABA
A
receptors
(α1
β2
subunits)
investigate
possible
molecular
mechanism.
Results
results
demonstrated
that
exhibited
significantly
concentration‐dependent
activity.
Acute
tests
indicated
high
margin
(no
behavioral
physiological
abnormalities
dose).
Additionally,
(
p
<
0.05)
dose‐dependently
reduced
latency
augmented
duration
animals,
compared
control
group.
It
decreased
increased
DZP‐2
reducing
this
parameter
FLU‐0.1.
In
studies,
binding
affinities
(BAs)
receptor
–5.6
kcal/mol.
Conclusion
potent
strong
profile
interaction
subunits).
Язык: Английский
Assessment of Antihyperglycemic and Modulatory Effects of trans‐Ferulic Acid on Glibenclamide and Metformin: In Vivo and Molecular Docking Studies
ChemistrySelect,
Год журнала:
2025,
Номер
10(14)
Опубликована: Апрель 1, 2025
Abstract
Diabetes
mellitus
(DM)
is
a
chronic
metabolic
disorder
characterized
by
persistent
hyperglycemia
due
to
impaired
insulin
secretion,
resistance,
or
both.
trans
‐Ferulic
acid
(TFA)
has
several
biological
activities,
including
sedative,
anxiolytic,
anti‐inflammatory,
and
so
on.
However,
there
no
in
vivo
silico
study
on
the
antihyperglycemic
activity
of
TFA.
This
assessed
antidiabetic
potential
TFA
its
modulatory
effect
glibenclamide
(GLI)
metformin
(MET)
through
hypoglycemic
tests
mice
molecular
docking
targeting
glucose
metabolism
proteins.
(25,
50,
75
mg/kg,
p.o.)
was
tested
glucose‐induced
hyperglycemic
alongside
GLI
(10
MET
(100
p.o.),
with
blood
levels
(BGLs)
monitored.
significantly
(
p
<
0.05)
reduced
BGLs
dose‐dependent
manner,
mg/kg
dose
achieving
30.99%
reduction
at
180
min,
compared
52.04%
55.27%
(MET).
Combination
therapy
(TFA‐50+GLI‐10
TFA‐50+MET‐100)
further
enhanced
glucose‐lowering
effects,
TFA‐50+GLI‐10
showing
highest
(58.90%).
In
analysis
revealed
that
exhibited
elevated
binding
affinities
complex
I
(−6.4
kcal/mol)
mitochondrial
glycerol‐3‐phosphate
dehydrogenase
(−6.8
kcal/mol).
These
findings
suggest
significant
potential,
supporting
role
regulation.
Язык: Английский