Tropical Journal of Natural Product Research,
Год журнала:
2024,
Номер
8(12)
Опубликована: Дек. 29, 2024
The
present
investigation
aims
to
determine
the
effect
of
Umbelliferone
(UMB)
on
pharmacokinetic
(PK)
and
pharmacodynamic
(PD)
parameters
Glibenclamide
(GLB)
in
diabetic
rats.
Simultaneously,
was
studied
normal
Diabetes
rats
induced
by
Streptazocin
(STZ).
PK
are
calculated
PD
studies
were
performed
only
From
results,
about
2.0-fold
improvement
oral
bioavailability
GLB
observed
when
treated
with
A
single-dose
(SD)
multi-dose
(MD)
administration
+
UMB
showed
3.8
4.0-fold
enhancement
GLB,
respectively
group
compared
GLB-treated
group.
Similarly,
SD
MD
2.8-folds
2.7-folds,
Further,
rate
clearance
also
volume
distribution
significantly
changed
No
significant
differences
GLB+
groups
blood
glucose
levels
(p<0.05)
reduced
(12.0
13.5%
after
treatment,
respectively)
alone
during
a
period
24
h
noticed
from
studies.
maximum
reduction
at
2
(44.3
45.6
%
standard
treatment
(32.1%).
Plants,
Год журнала:
2025,
Номер
14(2), С. 239 - 239
Опубликована: Янв. 16, 2025
Plants
have
long
been
used
to
treat
serious
illnesses
in
both
humans
and
animals.
A
significant
underappreciated
medicinal
tree,
Peltophorum
africanum
Sond
is
utilized
by
many
different
ethnic
groups
cure
a
wide
range
of
illnesses.
variety
electronic
databases,
including
ScienceDirect,
Scopus,
Scielo,
Scifinder,
PubMed,
Web
Science,
Medline,
Google
Scholar,
were
search
the
literature
on
P.
africanum,
using
key
words
such
as
uses,
survey,
pharmacology,
antigonococcal,
toxicity,
phytochemistry
others.
Further
data
was
obtained
from
several
scholarly
theses,
dissertations,
books
general
plant
sciences,
ethnomedicine,
other
pertinent
ethnobotanical
topics.
The
species
possess
very
important
pharmacological
activities
vitro,
which
includes
antimicrobial,
anti-HIV,
antioxidant,
anticancer,
antidiabetic,
activities.
Phytochemically,
possesses
various
classes
compounds,
dominated
flavonols,
may
well
explain
its
wider
Although
promising
anti-HIV
activity,
mode
action
safety
profiles
also
need
be
explored
extracts
exerted
some
degree
mutagenicity.
It
further
explore
ethnoveterinary
use
against
plethora
nematodes
that
infects
wild
domestic
Given
potent
vivo
studies
ascertain
comprehensive
toxicology
species,
thereby
developing
possible
medications.
elevated
pharmaceutical
product
infections.
Scientific Reports,
Год журнала:
2025,
Номер
15(1)
Опубликована: Янв. 29, 2025
Abstract
The
VHL-containing
cullin-RING
E3
ubiquitin
ligase
(CRL2
VHL
)
complex
is
an
commonly
used
in
targeted
protein
degradation
(TPD).
Hydroxyproline-based
ligands
that
mimic
substrates
have
been
developed
as
anchor
molecules
for
proteolysis-targeting
chimeras
(PROTACs)
TPD.
To
expand
the
chemical
space
ligands,
we
conducted
fragment
screening
using
VHL–ELOB–ELOC
(VBC)
proteins.
We
found
certain
7-hydroxycoumarin
derivatives
(7HCs),
rather
than
VHL,
would
bind
to
ELOC
component
of
VBC
complex.
7HC
binding
site
overlapped
with
CUL2
interface
on
but
did
not
overlap
CUL5
interface,
suggesting
7HCs
may
influence
formation
CRL2
CRL5.
Although
affinities
these
were
relatively
low,
they
represent
novel
and
promising
foundational
agents
development
probes
or
inhibitors
target
ELOC-containing
CRLs.
Molecules,
Год журнала:
2025,
Номер
30(3), С. 651 - 651
Опубликована: Фев. 1, 2025
The
current
study
is
a
continuation
of
our
previous
investigations
into
the
radical
homodimeric
reaction
mechanism
3-acetylcoumarin.
In
study,
effects
different
substituents
on
coumarin
ring
3-acetylcoumarin
are
investigated
both
experimentally
and
theoretically.
Several
derivatives
(substituted
at
C-6,
C-7,
C-8)
were
tested
in
optimized
conditions
under
ultrasound
irradiation,
biscoumarin
species
isolated
characterized.
elucidation
substituent’s
effect
was
further
by
means
DFT
calculations
(free-energy
calculations,
NBO
analysis),
initial
substituted
coumarins
formed
radicals.
It
observed
that
presence
C-6
C-8
positions
moiety
would
not
affect
significantly
formation
radical,
while
group
position
C-7
could
either
stabilize
or
destabilize
depending
electronic
properties
substituent.
By
combining
protein
engineering
and
synthetic
biology
strategies,
the
novel
de
novo
biosynthesis
of
4,6-dihydroxycoumarin
from
glycerol
was
realized
in
Escherichia
coli
for
first
time.
Abstract
Khellin
(1)
is
a
natural
furanocoumarin
found
in
Ammi
visnaga
majus,
renowned
for
its
abundance
of
biological
activities
various
physiological
conditions,
including
tumors,
bacterial
infections,
inflammation,
viral
fibrosis,
obesity,
respiratory
disease,
and
diabetes.
Based
on
extensive
site‐selective
chemical
modifications
1
,
new
entities
(NCEs)
with
enhanced
bioavailability,
potency,
pharmacokinetics,
druggability
have
been
developed
over
the
years.
Furthermore,
mechanisms
action
at
molecular
cellular
level
thoroughly
investigated
conjunction
preclinical
studies.
In
this
article,
we
present
medicinal
chemistry
derivatives
diverse
drug
discovery
efforts
covering
period
from
2015
to
present.
We
also
elucidated
future
perspectives,
challenges,
limitations.
posit
that
review
will
elucidate
areas
where
can
be
more
beneficial
identifying
hits
leads
enhance
knowledge
regarding
therapeutic
applications.
Frontiers in Microbiology,
Год журнала:
2024,
Номер
15
Опубликована: Авг. 16, 2024
Walnut
green
husk
(WGH)
is
a
waste
byproduct
from
walnut
industry.
However,
it
not
well-known
about
its
bioactive
effect
on
human
gut
health.
This
study
conducted
in
vitro
digestion
and
fermentation
experiments
to
the
of
WGH.
Microbial
was
primary
mechanism
efficiently
release
phenolics
flavonoids,
resulting
more
excellent
antioxidant
capacities
(DPPH,
ABTS,
FRAP
assays),
which
reached
highest
value
with
14.82
±
0.01
mg
VcE/g
DW,
3.47
mmol
TE/g
0.96
0.07
FeSO4·7H2O/g
respectively.
The
surface
microstructure
WGH
became
loose
fragmented
after
microbial
fermentation.
analytical
results
microbiota
demonstrated
that
could
significantly
increase
relative
abundance
Proteobacteria
phylum
level
Phascolarctobacterium
genus
while
certain
pro-inflammatory
bacteria
(such
as
Clostridium_sensu_stricto_1,
Dorea,
Alistipes,
Bilophila)
inhibited.
Additionally,
1,373
differential
metabolites
were
identified
enriched
283
KEGG
pathways.
Of
some
upregulated
including
ferulic
acid,
chlorogenic
umbelliferone,
scopolin,
muricholic
so
forth.
These
indicated
have
anti-inflammatory
activities
gut,
improve
economical
food
