Microbial Cell Factories,
Год журнала:
2025,
Номер
24(1)
Опубликована: Янв. 10, 2025
Genome
mining
is
a
promising
avenue
for
expanding
the
repertoire
of
microbial
natural
products,
which
are
important
drug
development.
This
approach
involves
predicting
genetically
encoded
small
molecules
by
examining
bacterial
genomes
via
accumulated
knowledge
biosynthesis.
However,
it
also
that
microbes
produce
predicted
molecule
in
practice.
Here,
we
introduce
an
endophytic
Streptomyces
sp.
N50,
was
isolated
from
medicinal
plant
Selaginella
tamariscina.
Upon
sequencing
its
entire
genome,
33
biosynthetic
gene
clusters
(BGCs)
were
identified
chromosome
and
megaplasmid.
Subsequent
genome
revealed
new
15-deoxynaphthomycin
could
be
produced
due
to
presence
enoyl
reductase
domain,
absent
known
BGC
naphthomycin,
type
ansamycin
antibiotics.
In
addition,
engineered
strain
with
introduction
global
regulatory
afsR2
into
N50
successfully
15-deoxynaphthomycins.
Furthermore,
molecular
network
analysis
MS/MS
selectively
confirmed
additional
sulfur-containing
congeners.
Eventually,
six
15-deoxynaphthomycins
elucidated
N50.
family
compounds
exhibit
various
biological
activities.
Also,
quinone
moieties
these
compounds,
activate
NRF2,
they
tested
their
ability
NRF2.
Among
three
(1,
5,
6)
activated
antioxidant
NRF2-ARE
signaling
pathway.
Treatment
significantly
elevated
NRF2
levels
HepG2
cells
further
induced
expression
target
genes
associated
response.
study
suggests
combination
mining,
engineering
networking
helpful
generating
as
pharmaceutical
candidates
microorganisms.
Journal of the American Chemical Society,
Год журнала:
2024,
Номер
146(4), С. 2583 - 2592
Опубликована: Янв. 17, 2024
Catalytic
electron
donor–acceptor
(EDA)
complexes
have
recently
emerged
as
a
powerful
and
sustainable
alternative
to
iridium-
ruthenium-based
photoredox
synthetic
methods.
Yet,
these
remain
underexplored
reliant
on
the
use
of
meticulously
designed
acceptors
that
require
previous
installation.
Herein,
we
report
novel
EDA
complex
employing
tris(4-methoxyphenyl)
amine
catalytic
donor
for
sulfonylation
alkenes
using
inexpensive
readily
available
sulfonyl
chlorides.
Applying
this
operationally
simple,
visible-light-mediated
general
platform,
both
redox-neutral
net-reductive
functionalization
more
than
60
substrates,
encompassing
vinylic
or
allylic
sulfonylation,
hydrosulfonylation,
sulfamoylation
activated
unactivated
alkynes.
Results in Chemistry,
Год журнала:
2023,
Номер
6, С. 101151 - 101151
Опубликована: Окт. 5, 2023
Infectious
diseases
resulting
from
various
strains
of
pathogenic
bacteria
are
among
the
leading
causes
death
and
morbidity
worldwide.
The
currently-available
antibacterial
medications
developed
natural
or
synthetic
sources
cornerstone
bacterial
infection
intervention,
but
somehow
mounting
spread
expansion
multidrug-resistant
harmful
has
become
a
major
concern
for
medical-providing
communities
pharmaceutical-releasing
companies.
pervasiveness
coumarin-based
products
in
nature
simplicity
their
lab
chemical
synthesis,
addition
to
ability
coumarin
backbone
communicate,
may
interact
with
DNA
gyrase
at
B
subunit
hinder
secondary
structure
by
abolishing
ATPase
activity;
thus,
conjugates
have
potential
act
as
agents.
It
is
conceivable
that
conjugation
nucleus
other
heterocyclic-based
scaffolds
present
opportunities
creation
novel
drugs.
This
presentation
be
based
on
fact
several
coumarin-heterocycle
conjugates,
including
clorobiocin,
coumermycin
A1,
novobiocin,
already
been
used
medical
methods
treatment
infectious
diseases.
study
explores,
during
period
last
5
years,
relationships
between
activity
action.
investigation
also
explored
developing
these
into
medicines.
Marine Life Science & Technology,
Год журнала:
2023,
Номер
5(1), С. 85 - 93
Опубликована: Янв. 20, 2023
Further
insights
on
the
secondary
metabolites
of
a
soft
coral-derived
fungus
Aspergillus
versicolor
under
guidance
MS/MS-based
molecular
networking
led
to
isolation
seven
known
cycloheptapeptides,
namely,
asperversiamides
A-C
(1-3)
and
asperheptatides
A-D
(4-7)
an
unusual
pyrroloindoline-containing
new
cycloheptapeptide,
asperpyrroindotide
A
(8).
The
structure
8
was
elucidated
by
comprehensive
spectroscopic
data
analysis,
its
absolute
configuration
determined
advanced
Marfey's
method.
semisynthetic
transformation
1
into
successfully
achieved
reaction
conditions
were
optimized.
Additionally,
series
derivatives
(10-19)
asperversiamide
(1)
semi-synthesized
their
anti-tubercular
activities
evaluated
against
Mycobacterium
tuberculosis
H37Ra.
preliminary
structure-activity
relationships
revealed
that
serine
hydroxy
groups
tryptophan
residue
are
important
activity.The
online
version
contains
supplementary
material
available
at
10.1007/s42995-022-00157-8.
Chemistry & Biodiversity,
Год журнала:
2024,
Номер
21(7)
Опубликована: Май 9, 2024
Sulfur-containing
heterocyclic
derivatives
have
been
disclosed
for
binding
with
a
wide
range
of
cancer-specific
protein
targets.
Various
interesting
sulfur-containing
heterocyclics
such
as
benzothiazole,
thiazole,
thiophene,
thiazolidinedione,
benzothiophene,
and
phenothiazine,
etc
shown
to
inhibit
diverse
signaling
pathways
implicated
in
cancer.
Significant
progress
has
also
made
molecular
targeted
therapy
against
specific
enzymes
kinase
receptors
due
potential
interactions
inside
the
ATP
pocket.
ring
metal
complexes
i.
e.,
benzothiophene
phenothiazines
are
among
most
promising
active
anticancer
compounds.
However,
sulfur
heteroaromatic
rings,
particularly
high
structural
alert
their
metabolism
reactive
metabolites.
The
mere
presence
itself
does
not
determine
compound
toxicity
therefore,
this
review
focuses
on
some
findings
that
shed
light
factors
influencing
toxicity.
In
current
review,
synthetic
strategies
introducing
core
synthesized
discussed
structure-activity
relationships
enhance
our
understanding
mechanisms
develop
safer
therapeutic
options.
marketed
drugs
included
direct
synthesis
novel
compounds
will
help
development
potent,
sulfur-based
near
future.
Plants,
Год журнала:
2022,
Номер
11(4), С. 539 - 539
Опубликована: Фев. 17, 2022
Naturally,
thiophenes
represent
a
small
family
of
natural
metabolites
featured
by
one
to
five
thiophene
rings.
Numerous
plant
species
belonging
the
Asteraceae
commonly
produce
thiophenes.
These
possessed
remarkable
bioactivities,
including
antimicrobial,
antiviral,
anti-inflammatory,
larvicidal,
antioxidant,
insecticidal,
cytotoxic,
and
nematicidal
properties.
The
current
review
provides
an
update
over
past
seven
years
for
reported
derivatives,
their
sources,
biosynthesis,
spectral
data,
bioactivities
since
last
published
in
2015.
Additionally,
with
help
SuperPred
webserver,
AI
(artificial
intelligence)
tool,
potential
drug
target
compounds
was
predicted.
In
silico
studies
were
conducted
Cathepsin
D
ADMET
(drug
absorption/distribution/metabolism/excretion/and
toxicity)
properties
prediction,
molecular
docking
binding
interaction,
dynamics
evaluate
ligand-target
interaction
stability
under
simulated
physiological
conditions.
Marine Life Science & Technology,
Год журнала:
2023,
Номер
5(1), С. 94 - 101
Опубликована: Фев. 6, 2023
The
Janus
kinase
(JAK)/signal
transducer
and
activator
of
transcription
3
(STAT3)
regulates
the
expression
various
critical
mediators
cancer
is
considered
as
one
central
communication
nodes
in
cell
growth
survival.
Marine
natural
products
(MNP)
represent
great
resources
for
discovery
bioactive
lead
compounds,
especially
anti-cancer
agents.
Through
medium-throughput
screening
our
in-house
MNP
library,
Pretrichodermamide
B,
an
epidithiodiketopiperazine,
was
identified
a
JAK/STAT3
signaling
inhibitor.
Further
studies
that
B
directly
binds
to
STAT3,
preventing
phosphorylation
thus
inhibiting
signaling.
Moreover,
it
suppressed
growth,
vitro,
at
low
micromolar
concentrations
demonstrated
efficacy
vivo
by
decreasing
tumor
xenograft
mouse
model.
In
addition,
shown
able
induce
cycle
arrest
promote
apoptosis.
This
study
novel
STAT3
inhibitor,
which
should
be
further
exploration
promising
therapy.
Dalton Transactions,
Год журнала:
2024,
Номер
53(33), С. 14077 - 14088
Опубликована: Янв. 1, 2024
Complexes
of
Co(
iii
)
(1),
Ni(
ii
(2),
Cu(
(3),
and
Zn(
(4)
derived
from
an
N
-(4-fluorobenzyl)
-(pyridin-2-ylmethyl)
dithiocarbamate
ligand.
Complex
3
showed
maximum
reduction
in
clonidine-induced
catalepsy
after
180
minutes
treatment.
Marine Drugs,
Год журнала:
2024,
Номер
22(10), С. 433 - 433
Опубликована: Сен. 25, 2024
Inflammation
is
considered
as
one
of
the
most
primary
protective
innate
immunity
responses,
closely
related
to
body’s
defense
mechanism
for
responding
chemical,
biological
infections,
or
physical
injuries.
Furthermore,
prolonged
inflammation
undesirable,
playing
an
important
role
in
development
various
diseases,
such
heart
disease,
diabetes,
Alzheimer’s
atherosclerosis,
rheumatoid
arthritis,
and
even
certain
cancers.
Marine-derived
fungi
represent
promising
sources
structurally
novel
bioactive
natural
products,
have
been
a
focus
research
anti-inflammatory
drugs.
This
review
covers
secondary
metabolites
with
activities
from
marine-derived
fungi,
over
period
spanning
August
2018
July
2024.
A
total
285
metabolites,
including
156
compounds
11
skeleton
structures,
are
described.
Their
structures
categorized
into
five
categories:
terpenoids,
polyketides,
nitrogen-containing
compounds,
steroids,
other
classes.
The
targets,
well
vitro
vivo
screening
models,
were
surveyed
statistically
summarized.
paper
aims
offer
valuable
insights
researchers
exploration
products
discovery