Re-discovery of MS-347a as a fungicide candidate through a new drug discovery platform with a multidrug-sensitive Saccharomyces cerevisiae screening system and the introduction of a global secondary metabolism regulator, laeA gene
Bioscience Biotechnology and Biochemistry,
Год журнала:
2024,
Номер
88(7), С. 824 - 829
Опубликована: Апрель 25, 2024
ABSTRACT
We
found
that
the
culture
broth
of
fungi
showed
anti-fungal
activity
against
multidrug-sensitive
budding
yeast.
However,
we
could
not
identify
compound
due
to
small
quantity.
Therefore,
attempted
increase
productivity
target
by
introduction
a
global
secondary
metabolism
regulator,
laeA
strain,
which
led
successful
isolation
10-folds
greater
amount
MS-347a
(1)
than
Aspergillus
sp.
FKI-5362.
Compound
1
was
effective
Candida
albicans
and
detailed
remains
unverified.
After
our
screening,
inhibit
growth
broad
plant
pathogenic
fungal
species
belonging
Ascomycota.
It
is
noteworthy
little
insecticidal
silkworms,
suggesting
its
selective
biological
fungi.
Our
study
implies
combination
strategy
yeast
useful
for
new
drug
discovery.
Язык: Английский
Corey–Fuchs reaction enabled synthesis of natural products: a review
RSC Advances,
Год журнала:
2025,
Номер
15(11), С. 8121 - 8155
Опубликована: Янв. 1, 2025
Corey–Fuchs
reaction
is
a
two-step
involving
the
synthesis
of
terminal
alkyne
from
aldehyde.
It
pivotal
organic
reaction,
plays
significant
role
in
various
natural
products
and
their
derivatives.
Язык: Английский
Synthesis and biological evaluation of MS-347a derivatives against plant pathogenic fungi based on a strategy of <i>laeA</i> gene introduction
Nippon Nōyaku Gakkaishi,
Год журнала:
2024,
Номер
49(4), С. 224 - 231
Опубликована: Ноя. 20, 2024
Our
group
previously
identified
MS-347a
(1)
as
a
new
fungicide
candidate
from
the
culture
broth
of
mutant
strain,
Aspergillus
sp.
KTF-0058,
which
had
laeA
gene
inserted.
This
strain
was
able
to
produce
sufficient
supply
1,
allowing
for
its
use
investigate
structure-activity
relationship.
To
this
end,
we
synthesized
11
derivatives
and
evaluated
their
antifungal
activity.
Among
these
derivatives,
aldehyde
derivative
exhibited
superior
potency
compared
some
acyl
were
maintain
activity
1
despite
significant
structural
changes.
From
results,
it
is
found
that
one
most
promising
fungicidal
candidates,
introduction
groups
could
be
utilized
create
chemical
probes
target-identification
experiments.
Язык: Английский
Synthesis, Structural Validation, and SAR of Antifungal Fusaramin
Synfacts,
Год журнала:
2024,
Номер
20(03), С. 0311 - 0311
Опубликована: Фев. 14, 2024
Key
words
structure–activity
relationship
(SAR)
-
antimicrobial
antifungal
Язык: Английский
Discovery of an anti-malarial compound, burnettiene A, with a multidrug-sensitive Saccharomyces cerevisiae screening system based on mitochondrial function inhibitory activity
Bioscience Biotechnology and Biochemistry,
Год журнала:
2024,
Номер
88(10), С. 1212 - 1216
Опубликована: Июль 9, 2024
In
this
paper,
we
describe
our
discovery
of
burnettiene
A
(1)
as
an
antimalarial
compound
from
the
culture
broth
Lecanicillium
primulinum
(current
name:
Flavocillium
primulinum)
FKI-6715
strain
utilizing
original
multidrug-sensitive
yeast
system.
This
polyene-decalin
polyketide
natural
product
was
originally
isolated
antifungal
active
Aspergillus
burnettii.
However,
activity
1
has
been
revealed
in
only
one
fungal
species,
and
mechanism
action
remains
unknown.
After
validation
mitochondrial
function
inhibitory
1,
envisioned
a
new
drug
platform
based
on
activity.
We
evaluated
showed
against
Plasmodium
falciparum
FCR3
(chloroquine
sensitive)
K1
resistant).
Our
study
utility
screening
system
for
candidates.
Язык: Английский
Synthesis and biological evaluation of burnettiene A derivatives enabling discovery of novel fungicide candidates
Nippon Nōyaku Gakkaishi,
Год журнала:
2024,
Номер
unknown
Опубликована: Янв. 1, 2024
An
antifungal
polyene-decalin
polyketide
natural
product,
burnettiene
A
(
Язык: Английский