Journal of Antimicrobial Chemotherapy,
Journal Year:
2014,
Volume and Issue:
69(7), P. 1888 - 1891
Published: March 25, 2014
There
is
an
urgent
need
to
develop
new
and
effective
treatments
for
poverty-related
neglected
diseases.
In
light
of
the
time
required
bring
a
drug
market
cost
involved
(10–15
years,
>1
billion
US$),
one
approach
identifying
diseases
like
leishmaniasis
evaluate
drugs
that
are
already
registered
treatment
other
This
paper
describes
anti-leishmanial
activities
10
FDA-approved
protein
kinase
inhibitors
available
human
cancers.
vitro
in
vivo
models
Leishmania
infection
were
used
potency
selected
inhibitors.
Sunitinib,
sorafenib
lapatinib
identified
as
active
against
donovani
amastigotes
cultured
murine
macrophages
with
IC50
values
1.1,
3.7
2.5
μM,
respectively,
level
similar
miltefosine
(IC50
=
1.0
μM),
not
toxic
mammalian
cells.
addition,
some
L.
BALB/c
mouse
model
infection;
dosing
on
days
7–11
50
mg/kg
oral
dose
sunitinib,
or
reduced
liver
amastigote
burdens
by
41%,
36%
30%,
compared
untreated
control
mice.
Although
less
efficacious,
was
also
intracellular
cutaneous
disease-causing
species
amazonensis,
major
mexicana.
study
demonstrates
activity
clinically
provides
further
evidence
potential
repurposing.
Molecules,
Journal Year:
2016,
Volume and Issue:
21(5), P. 529 - 529
Published: April 28, 2016
Nerolidol
(3,7,11-trimethyl-1,6,10-dodecatrien-3-ol)
is
a
naturally
occurring
sesquiterpene
alcohol
that
present
in
various
plants
with
floral
odor.
It
synthesized
as
an
intermediate
the
production
of
(3E)-4,8-dimethy-1,3,7-nonatriene
(DMNT),
herbivore-induced
volatile
protects
from
herbivore
damage.
Chemically,
nerolidol
exists
two
geometric
isomers,
trans
and
cis
form.
The
usage
widespread
across
different
industries.
has
been
widely
used
cosmetics
(e.g.,
shampoos
perfumes)
non-cosmetic
products
detergents
cleansers).
In
fact,
U.S.
Food
Drug
Administration
(FDA)
also
permitted
use
food
flavoring
agent.
fact
common
ingredient
many
attracted
researchers
to
explore
more
medicinal
properties
may
exert
beneficial
effect
on
human
health.
Therefore,
aim
this
review
compile
consolidate
data
pharmacological
biological
activities
displayed
by
nerolidol.
Furthermore,
includes
pharmacokinetic
toxicological
studies
summary,
demonstrated
highlight
prospects
promising
chemical
or
drug
candidate
field
agriculture
medicine.
Molecules,
Journal Year:
2017,
Volume and Issue:
22(8), P. 1210 - 1210
Published: July 25, 2017
Medicinal
chemists
continue
to
be
fascinated
by
chalcone
derivatives
because
of
their
simple
chemistry,
ease
hydrogen
atom
manipulation,
straightforward
synthesis,
and
a
variety
promising
biological
activities.
However,
chalcones
have
still
not
garnered
deserved
attention,
especially
considering
high
potential
as
chemical
sources
for
designing
developing
new
effective
drugs.
In
this
review,
we
summarize
current
methodological
developments
towards
the
design
synthesis
state-of-the-art
medicinal
chemistry
strategies
(bioisosterism,
molecular
hybridization,
pro-drug
design).
We
also
highlight
applicability
computer-assisted
drug
approaches
address
how
may
contribute
optimizing
research
outputs
lead
more
successful
cost-effective
discovery
endeavors.
Lastly,
present
examples
use
suggest
possible
solutions
existing
limitations.
BioMed Research International,
Journal Year:
2015,
Volume and Issue:
2015, P. 1 - 11
Published: Jan. 1, 2015
Leishmaniasis
is
a
neglected
infectious
disease
caused
by
several
different
species
of
protozoan
parasites
the
genus
Leishmania
.
Current
strategies
to
control
this
are
mainly
based
on
chemotherapy.
Despite
being
available
for
last
70
years,
leishmanial
chemotherapy
has
lack
efficiency,
since
its
route
administration
difficult
and
it
can
cause
serious
side
effects,
which
results
in
emergence
resistant
cases.
The
medical-scientific
community
facing
difficulties
overcome
these
problems
with
new
suitable
efficient
drugs,
as
well
identification
drug
targets.
availability
complete
genome
sequence
given
scientific
possibility
large-scale
analysis,
may
lead
better
understanding
parasite
biology
consequent
novel
In
review
we
focus
how
high-throughput
analysis
helping
us
other
groups
identify
targets
chemotherapeutic
interventions.
We
further
discuss
recent
data
produced
our
group
regarding
use
techniques
helped
assess
potential
identified
Journal of Ethnopharmacology,
Journal Year:
2014,
Volume and Issue:
160, P. 32 - 40
Published: Nov. 25, 2014
Syzygium
cumini
(L.)
Skeels
(Myrtaceae),
commonly
known
as
"jambolão"
in
Brazil
is
widely
used
folk
medicine
against
leishmaniasis,
inflammation,
chronic
diarrhea,
and
ulcers.
It
one
of
the
most
plants
for
treatment
diabetes
worldwide.
In
previous
studies,
was
shown
to
possess
antihyperlipidemic
anti-allergic
properties,
exhibit
good
performance
an
antimicrobial
agent
bacteria,
fungi,
protozoa
parasites
genus
Leishmania
Trypanosoma.
This
study
aimed
at
evaluating
effects
S.
essential
oil
(ScEO)
its
major
component
α-pinene
on
(Leishmania)
amazonensis,
well
their
cytotoxicity
possible
mechanisms
action.To
evaluate
anti-proliferative
effect
Leishmania,
promastigote
axenic
amastigote
forms
were
assessed
using
tetrazolium
salt
(MTT)
assay.
The
intramacrophagic
amastigotes
exposed
ScEO
determine
survival
index.
To
gain
insight
into
mechanism
action
involved
samples,
we
evaluated
modulation
macrophage
activation
state
by
observing
structural
(phagocytic
lysosomal
activities)
cellular
(nitric
oxide
increase)
changes.
assess
safety
profile
α-pinene,
murine
macrophages
human
red
blood
cells
treated
with
selectivity
index
calculated
each
treatment.α-Pinene
effective
amazonensis
forms,
a
half-maximal
inhibitory
concentration
(IC50)
value
19.7µg/mL.
α-Pinene
more
active
(IC50
values
16.1
15.6µg/mL
intracellular
amastigotes,
respectively)
than
43.9
38.1µg/mL
respectively).
Our
results
showed
that
anti-Leishmania
mediated
immunomodulatory
activity,
evidenced
observed
increases
both
phagocytic
elevated
NO
levels.
exhibited
low
erythrocytes.
50%
(CC50)
MTT
assay
614.1
425.2µg/mL
respectively,
while
corresponding
hemolytic
(HC50)
874.3
233.3µg/mL.Taken
together,
demonstrate
constituent
have
significant
modulated
activation,
acceptable
levels
Further
work
warranted,
involving
in-depth
mechanistic
studies
vivo
investigations.
ChemMedChem,
Journal Year:
2015,
Volume and Issue:
10(10), P. 1606 - 1624
Published: Aug. 20, 2015
Abstract
Infectious
diseases
continue
to
be
one
of
the
major
contributors
human
morbidity.
The
rapid
rate
at
which
pathogenic
microorganisms
have
developed
resistance
against
frontline
antimicrobials
has
compelled
scientists
look
for
new
alternatives.
Given
their
vast
antimicrobial
repertoire,
substantial
research
effort
been
dedicated
toward
development
peptides
(AMPs)
as
alternative
drugs.
However,
inherent
limitations
AMPs
driven
efforts
worldwide
develop
synthetic
mimics
AMPs.
This
review
focuses
on
progress
that
made
small
molecules
emulate
properties
AMPs,
both
in
terms
design
and
biological
activity.
Herein
we
provide
an
extensive
discussion
structural
features
various
designs
examine
exploited.
Furthermore,
raise
a
number
questions
field
yet
solutions
discuss
possible
future
directions
remain
either
unexploited
or
underexploited.
Current Medicinal Chemistry,
Journal Year:
2012,
Volume and Issue:
19(10), P. 1443 - 1474
Published: March 9, 2012
Leishmaniasis
remains
a
public
health
problem
worldwide,
affecting
approximately
12
million
people
in
88
countries;
50
000
die
of
it
each
year.
The
disease
is
caused
by
Leishmania,
obligate
intracellular
vector-borne
parasites.
In
spite
its
huge
impact
on
the
populations
vast
areas,
leishmaniasis
one
most
neglected
diseases.
No
safe
and
effective
vaccine
currently
exists
against
any
form
human
leishmaniasis.
spectrum
efficacy
available
antileishmanial
drugs
are
also
limited.
First
part
this
review
discusses
approaches
used
for
vaccination
that
based
pathogen
includes
virulent
or
attenuated
parasites,
parasites
related
nonpathogenic
species,
whole
killed
parasites'
subunits,
DNA
vaccines,
vaccines
saliva
components
transmitting
phlebotomine
vector.
Second
describes
parasite
detection
quantification
using
microscopy
assays,
cell
cultures,
immunodetection,
DNA-based
methods,
shows
progress
development
application
these
techniques.
third
part,
first-line
alternative
to
treat
characterized,
pre-clinical
research
range
natural
synthetic
compounds
studied
leishmanicidal
activity
described.
suggests
novel
strategies
advances
genetics,
genomics,
advanced
delivery
systems,
high
throughput
screenings
would
lead
improvement
prevention
treatment
disease.
Keywords:
Tropical
disease,
kala-azar,
preventive
medicine,
animal
model,
therapy
visceral,
cutaneous
mucocutaneous
leishmaniasis,
estimation
load,
vector,
antileishmanial,
cultures
