Pharmaceuticals,
Год журнала:
2024,
Номер
17(12), С. 1658 - 1658
Опубликована: Дек. 9, 2024
Food
supplements
are
used
for
a
variety
of
purposes,
one
which
is
weight
reduction.
As
excess
long-term
condition,
some
expected
to
be
long
periods
time.
The
use
these
dietary
makes
it
highly
likely
that
they
will
combined
with
medications,
increasing
the
risk
food
supplement–drug
interactions,
not
always
known
or
disclosed,
and
can
lead
serious
health
problems,
as
has
been
observed.
This
article
discusses
compounds
reduction
(green
tea
extract,
Garcinia
cambogia,
chitosan,
quercetin
resveratrol)
interactions
may
cause
drugs
such
as:
dextromethorphan,
buspirone,
diclofenac,
irinotecan,
5-fluorouracil,
cytochrome
P450
inducers
inhibitors,
statins,
orlistat,
warfarina,
acenocoumarol,
fluoxetine,
valproate,
quetiapine,
carbamazepine.
information
useful
healthcare
professionals
detect
intervene
on
ensure
optimization
therapy
patient
safety.
Frontiers in Chemistry,
Год журнала:
2025,
Номер
13
Опубликована: Май 8, 2025
Peroxisome
proliferator-activated
receptor
gamma
(PPARγ)
is
a
key
target
for
metabolic
disorders
that
contribute
to
obesity
and
type
2
diabetes
mellitus
(T2DM).
However,
full
agonists
such
as
thiazolidinediones
(TZDs)
have
limitations
in
terms
of
side
effects.
Selective
PPARγ
modulators
(SPPARγMs)
alternative
binding
pockets
offer
the
potential
safer
partial
agonists.
Here,
we
employed
six
computational
algorithms
(Fpocket,
DeepSite,
CavityPlus,
DoGSiteScorer,
CASTpFold,
POCASA)
identify
novel
allosteric
pocket
(pocket
6-5)
ligand-binding
domain
(LBD),
localized
at
helix
3
(H3),
(H2),
2'(H2'),
β-sheet
interface.
A
virtual
screening
4,097
natural
compounds
from
traditional
Chinese
medicine
(TCM)
libraries
was
conducted,
which
led
identification
ginsenoside
Rg5
(TWSZ-5)
top
hit.
Molecular
docking
molecular
dynamics
(MD)
revealed
TWSZ-5
stabilizes
6-5
through
hydrogen
bonds
with
Ser342,
Gln345,
Lys261,
Lys263.
promoted
beige
adipocyte
differentiation
adipose-derived
stem
cells
(ADSCs)
vitro,
upregulating
Ucp1,
Prdm16,
Cpt1α,
Pgc1α.
The
present
study
identifies
SPPARγM
utilizes
an
enhance
thermogenesis
while
mitigating
adverse
These
findings
emphasize
TCM
derivatives
structure-based
strategies
develop
antidiabetic
therapies
precision
pharmacology.
Phytotherapy Research,
Год журнала:
2025,
Номер
unknown
Опубликована: Май 9, 2025
ABSTRACT
Obesity
has
become
a
major
global
health
problem,
and
strategies
to
improve
metabolic
disorders
are
urgently
needed.
This
review
focused
on
the
roles
of
natural
active
ingredients
in
regulating
communication
between
liver
brown
adipose
tissue
(BAT),
especially
highlighting
associated
signaling
pathways
structure–activity
relationship
(SAR).
Natural
polyphenols,
flavonoids,
terpenoids,
their
potential
modulating
metabolism
were
elaborated.
Particularly,
some
factor
including
insulin,
adiponectin,
leptin,
NRG4,
FGF21,
inflammatory
factor,
BMP
summarized,
detailing
how
modulated
liver–BAT
crosstalk,
such
as
celastrol,
genistein,
sesamin,
etc.
FGF21
NRG4
acted
key
factors,
playing
important
transduction
crosstalk
BAT.
More
importantly,
SAR
phenolic
acids,
polysaccharides,
terpenoid
compounds
was
discussed.
The
presence
functional
groups,
hydroxyl
or
methoxyl
substituents,
molecular
size
analyzed
relation
interaction
biological
targets.
Furthermore,
structural
modifications
enhanced
bioactivity
bioavailability
while
reducing
side
effects
elucidated.
In
conclusion,
played
an
role
BAT,
underscoring
these
components
treating
disorders.
Further
research
different
long‐term
impacts
still
needed
provide
more
effective
safer
solutions
for
diseases
prevention
treatment.
Current Medicinal Chemistry,
Год журнала:
2023,
Номер
31(1), С. 25 - 61
Опубликована: Май 18, 2023
Obesity
is
a
complex,
chronic
and
inflammatory
disease
that
affects
more
than
one-third
of
the
world's
population,
leading
to
higher
incidence
diabetes,
dyslipidemia,
metabolic
syndrome,
cardiovascular
diseases,
some
types
cancer.
Several
phytochemicals
are
used
as
flavoring
aromatic
compounds,
also
exerting
many
benefits
for
public
health.
This
study
aims
summarize
scrutinize
beneficial
effects
most
important
against
obesity.
Systematic
research
current
international
literature
was
carried
out
in
accurate
scientific
databases,
e.g.,
Pubmed,
Scopus,
Web
Science
Google
Scholar,
using
set
critical
representative
keywords,
such
phytochemicals,
obesity,
metabolism,
etc.
studies
unraveled
potential
positive
berberine,
carvacrol,
curcumin,
quercetin,
resveratrol,
thymol,
etc.,
obesity
disorders.
Mechanisms
action
include
inhibition
adipocyte
differentiation,
browning
white
adipose
tissue,
enzymes
lipase
amylase,
suppression
inflammation,
improvement
gut
microbiota,
downregulation
obesity-inducing
genes.
In
conclusion,
multiple
bioactive
compounds-phytochemicals
exert
Future
molecular
clinical
must
be
performed
unravel
mechanisms
anti-obesity
activities
these
naturally
occurring
compounds.
Cell Biochemistry and Function,
Год журнала:
2024,
Номер
42(1)
Опубликована: Янв. 1, 2024
Abstract
Obesity
is
a
complex
disorder,
and
the
incidence
of
obesity
continues
to
rise
at
an
alarming
rate
worldwide.
In
particular,
growing
overweight
in
children
major
health
concern.
However,
underlying
mechanisms
remain
unclear
efficacy
several
approaches
for
weight
loss
limited.
As
important
calcium‐permeable
temperature‐sensitive
cation
channel,
transient
receptor
potential
vanilloid
(TRPV)
ion
channels
directly
participate
thermo‐,
mechano‐,
chemosensory
responses.
Modulation
TRPV
channel
activity
can
alter
physiological
function
leading
neurodegenerative
diseases,
chronic
pain,
cancer,
skin
disorders.
recent
years,
increasing
studies
have
demonstrated
that
are
abundantly
expressed
metabolic
organs,
including
liver,
adipose
tissue,
skeletal
muscle,
pancreas,
central
nervous
system,
which
has
been
implicated
various
diabetes
mellitus.
addition,
as
process
pathophysiology
adipocyte
metabolism,
differentiation
plays
critical
role
obesity.
this
review,
we
focus
on
broaden
ideas
prevention
control
strategies
ABSTRACT
The
pharmacological
activation
of
peroxisome
proliferator‐activated
receptor
gamma
(PPARγ)
is
a
convenient
and
promising
strategy
for
promoting
beige
adipocyte
biogenesis
to
combat
obesity‐related
metabolic
disorders.
However,
thiazolidinediones
(TZDs),
the
full
agonists
PPARγ
exhibit
severe
side
effects
in
animal
models
clinical
settings.
Therefore,
development
efficient
safe
modulators
treatment
diseases
emerging.
In
this
study,
using
comprehensive
methods,
we
report
previously
unidentified
ligand‐binding
pocket
(LBP)
link
it
differentiation.
Further
virtual
screening
4097
natural
compounds
based
on
novel
LBP
revealed
that
saikosaponin
A
(NJT‐2),
terpenoid
compound,
can
bind
induce
coactivator
recruitment
effectively
activate
PPARγ‐mediated
transcription
program.
mouse
model,
NJT‐2
administration
efficiently
promoted
improved
obesity‐associated
dysfunction,
with
significantly
fewer
adverse
than
those
observed
TZD.
Our
results
not
only
provide
an
advanced
molecular
insight
into
structural
details
PPARγ,
but
also
develop
linked
selective
agonist
obesity
treatment.
