Assessment of Antidiarrheal Effect of Oleuropein Through µ‐Oopioid Receptor Interaction Pathway: In Vivo and in Silico Studies
Nishat Jahan,
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Manoj Mandal,
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Imam Hossen Rakib
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et al.
Drug Development Research,
Journal Year:
2025,
Volume and Issue:
86(1)
Published: Feb. 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.
Language: Английский
Tangeretin enhances sedative activity of diazepam in Swiss mice through GABAA receptor interaction: In vivo and in silico approaches
Neuroscience,
Journal Year:
2025,
Volume and Issue:
572, P. 1 - 10
Published: March 5, 2025
Language: Английский
Assessment of antiemetic and modulatory activity of dihydrocoumarin on copper sulfate induced emetic chicks: An in vivo investigation
Food Chemistry Advances,
Journal Year:
2025,
Volume and Issue:
6, P. 100930 - 100930
Published: Feb. 23, 2025
Language: 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,
Journal Year:
2025,
Volume and Issue:
unknown
Published: March 7, 2025
Language: Английский
Caffeine and sclareol take the edge off the sedative effects of linalool, possibly through the GABAA interaction pathway: molecular insights through in vivo and in silico studies
Naunyn-Schmiedeberg s Archives of Pharmacology,
Journal Year:
2025,
Volume and Issue:
unknown
Published: March 11, 2025
Language: Английский
Citronellal Exerts Sedative‐Like Effects and Augments Diazepam's Action in Swiss Mice, Possibly Through the GABAergic Pathway
Brain and Behavior,
Journal Year:
2025,
Volume and Issue:
15(3)
Published: March 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).
Language: Английский
Assessment of Antihyperglycemic and Modulatory Effects of trans‐Ferulic Acid on Glibenclamide and Metformin: In Vivo and Molecular Docking Studies
ChemistrySelect,
Journal Year:
2025,
Volume and Issue:
10(14)
Published: April 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.
Language: Английский
Anticancer activity of Jasminum sambac and its bioactive phytochemicals against the PI3K-AKT-mTOR pathway: A literature-based in silico study
South African Journal of Botany,
Journal Year:
2025,
Volume and Issue:
180, P. 431 - 443
Published: March 23, 2025
Language: Английский
Tangeretin Improves the Memory of Swiss Mice, Suggesting Potential Molecular Interventions Through Animal Behavior Assessments and In Silico Studies
Brain and Behavior,
Journal Year:
2025,
Volume and Issue:
15(5)
Published: May 1, 2025
ABSTRACT
Introduction
Tangeretin
(TAN),
a
polymethoxylated
flavone
from
citrus
peels,
exhibits
neuroprotective,
anti‐inflammatory,
and
antioxidant
properties.
This
study
aims
to
evaluate
the
memory‐enhancing
effects
of
TAN
in
Swiss
mice
explore
its
potential
molecular
interactions
with
D
2
dopamine
(DOP)
receptor
through
vivo
behavioral
assessments
silico
approaches.
Methods
were
administered
(10
20
mg/kg),
DOP
(22
olanzapine
(OLN)
(2
alone
combinations
per
orally
(p.o.),
followed
by
cognitive
using
marble
burying,
dust
removal,
trained
swimming
tests.
In
studies
included
docking
against
(PDB:
6CM4),
pharmacokinetics
(SwissADME,
pkCSM),
toxicity
predictions
(ProTox‐3).
Results
significantly
(
p
<
0.05)
improved
functions,
including
memory,
anxiety,
motor
coordination,
dose‐dependent
manner,
mg/kg
showing
most
notable
effect.
The
combination
TAN‐10
DOP‐22
enhanced
these
benefits,
whereas
OLN‐2
reduced
improvements.
TAN‐treated
showed
better
performance
tests,
indicating
problem‐solving,
coordination.
These
results
suggest
TAN's
enhancement,
particularly
DOP‐22.
No
deaths
observed
any
treatment
group,
all
treated
animals
exhibited
normal
physiological
activity
no
signs
acute
toxicity.
revealed
that
strongest
binding
affinity
(BA)
(−6.6
kcal/mol)
receptor,
forming
multiple
hydrogen
bonds
(HBs),
which
indicates
mechanism
for
memory
enhancement
via
dopaminergic
modulation.
Pharmacokinetic
analyses
also
has
favorable
ADMET
properties,
high
gastrointestinal
absorption,
blood–brain
barrier
penetration,
low
Conclusion
findings
highlight
as
promising
therapeutic
candidate
memory‐related
disorders,
warranting
further
clinical
exploration.
Language: Английский