Appeal of Urolithins from Synthesis to Biological Activities
Journal of Agricultural and Food Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Апрель 29, 2025
Urolithins
(Uros),
a
series
of
natural
polyphenols
derived
from
ellagic
acid
through
gut
bacteria
metabolism,
have
gathered
significant
attention
due
to
their
diverse
bioactivities
such
as
maintaining
mitochondrial
health
and
anti-inflammatory
antioxidative
effects.
However,
the
ability
metabolize
Uros
varies
among
individuals.
This
Review
provides
comprehensive
insight
into
synthesis,
encapsulation
Uros,
focusing
on
biotransformation
in
vivo.
We
highlight
critical
role
microbiota
urolithins,
including
primary
bacterial
species
Gordonibacter
urolithinfaciens,
Enterocloster
bolteae
Enterococcus
faecium.
Furthermore,
therapeutic
potential
alleviating
neurodegenerative
diseases,
cancer,
Duchenne
muscular
dystrophy
is
discussed.
Finally,
several
strategies
for
enhancing
solubility
bioavailability
are
summarized.
Future
research
direction
includes
identifying
key
genes
involved
biotransformation,
elucidating
bioactive
mechanisms
improving
bioavailability.
In
conclusion,
we
synthesized
biosynthetic
pathways
properties
better
utilization
management.
Язык: Английский
Design and Synthesis of O‐Dialkylaminoalkyl Substituted Urolithin Derivatives: DNA Topoisomerase IIα Inhibition With Promising Antiproliferative Activity
Xintong Li,
Xiaochun Zhang,
Chan Yin
и другие.
Archiv der Pharmazie,
Год журнала:
2025,
Номер
358(5)
Опубликована: Май 1, 2025
ABSTRACT
Based
on
the
pharmacophore
structural
characteristics
of
topoisomerase
II
(TopoII)
inhibitors:
(i)
planar
polyaromatic
skeleton;
(ii)
cation
core;
(iii)
a
groove‐binding
side
chain
moiety,
16
urolithin
derivatives
with
O
‐dialkylaminoalkyl
substitutions
were
designed
and
synthesized.
Most
synthesized
compounds
showed
improved
TopoIIα
inhibitory
antiproliferative
activities.
20
best
activity
also
exhibited
excellent
IC
50
values
0.91
±
0.01,
1.93
0.04,
2.84
0.34
μM
against
MDA‐MB‐231,
HeLa,
A549
cell
lines,
being
about
12.55,
3.95,
2.17
times
more
active
than
VP‐16
(IC
11.42
0.82,
7.63
0.46,
6.15
0.43
μM,
respectively).
Meanwhile,
weak
toxicity
to
normal
cells.
In
addition,
exerted
anti‐migration
anti‐invasion
MDA‐MB‐231
Our
results
supported
that
might
act
as
inhibitor
potential
become
new
type
antitumor
drug
lead.
Язык: Английский
Advanced Spray-Dried Inhalable Microparticles/Nanoparticles of an Innovative Mitophagy Activator for Targeted Lung Delivery: Design, Comprehensive Characterization, Human Lung Cell Culture, and In Vitro Aerosol Dispersion Performance
ACS Pharmacology & Translational Science,
Год журнала:
2024,
Номер
7(11), С. 3540 - 3558
Опубликована: Окт. 15, 2024
Urolithin
A
(UA)
has
demonstrated
the
ability
to
stimulate
mitophagy
and
enhance
mitochondrial
cellular
health
in
skeletal
muscles
humans
after
oral
administration.
It
is
hypothesized
that
targeted
delivery
of
UA
as
inhaled
dry
powders
lungs
will
through
biogenesis.
This
study
aimed
engineer
inhalable
excipient-free
powder
inhalers
(DPIs)
for
pulmonary
delivery.
The
particles
were
designed
by
particle
engineering
from
dilute
organic
solutions
using
state-of-the-art
spray
drying
technology
a
closed
mode.
Comprehensive
physicochemical
characterization
advanced
microscopy
techniques
conducted
examine
phase
behavior,
molecular
properties,
which
are
necessary
rational
design
inhalation
aerosols.
Molecular
fingerprinting
was
attenuated
total
reflectance-Fourier
transform
infrared
(ATR-FTIR)
spectroscopy
Raman
spectroscopy.
Chemical
imaging
mapping
confocal
(CRM)
IR
microscopy.
spray-dried
(SD)
successfully
produced
at
different
spraying
pump
feed
rates
exhibited
favorable
properties.
SD
outstanding
vitro
aerosol
dispersion
performance
with
an
FDI-approved
human
DPI
device
(Neohaler)
correlated
rate.
In
Язык: Английский