Computation,
Год журнала:
2022,
Номер
10(4), С. 51 - 51
Опубликована: Март 25, 2022
Some
clinical
studies
have
indicated
activity
of
ivermectin,
a
macrocyclic
lactone,
against
COVID-19,
but
biological
mechanism
initially
proposed
for
this
anti-viral
effect
is
not
applicable
at
physiological
concentrations.
This
in
silico
investigation
explores
potential
modes
action
ivermectin
and
14
related
compounds,
by
which
the
infectivity
morbidity
SARS-CoV-2
virus
may
be
limited.
Binding
affinity
computations
were
performed
these
agents
on
several
docking
sites
each
models
(1)
spike
glycoprotein
virus,
(2)
CD147
receptor,
has
been
identified
as
secondary
attachment
point
(3)
alpha-7
nicotinic
acetylcholine
receptor
(α7nAChr),
an
viral
penetration
neuronal
tissue
well
activation
site
cholinergic
anti-inflammatory
pathway
controlled
vagus
nerve.
affinities
calculated
multiple
binding
compound.
Our
results
indicate
high
even
higher
some
other
compounds
evaluated,
all
three
molecular
targets.
These
suggest
mechanisms
limit
stimulate
α7nAChr-mediated
that
could
cytokine
production
immune
cells.
Pharmaceuticals,
Год журнала:
2020,
Номер
13(8), С. 196 - 196
Опубликована: Авг. 17, 2020
Avermectins
are
a
group
of
drugs
that
occurs
naturally
as
product
fermenting
Streptomyces
avermitilis,
an
actinomycetes,
isolated
from
the
soil.
Eight
different
structures,
including
ivermectin,
abamectin,
doramectin,
eprinomectin,
moxidectin,
and
selamectin,
were
divided
into
four
major
components
(A1a,
A2a,
B1a
B2a)
minor
(A1b,
A2b,
B1b,
B2b).
generally
used
pesticide
for
treatment
pests
parasitic
worms
result
their
anthelmintic
insecticidal
properties.
Additionally,
they
possess
anticancer,
anti-diabetic,
antiviral,
antifungal,
several
metabolic
disorders.
Avermectin
works
by
preventing
transmission
electrical
impulse
in
muscle
nerves
invertebrates,
amplifying
glutamate
effects
on
invertebrates-specific
gated
chloride
channel.
has
unwanted
or
reactions,
especially
when
administered
indiscriminately,
which
include
respiratory
failure,
hypotension,
coma.
The
current
review
examines
mechanism
actions,
biosynthesis,
safety,
pharmacokinetics,
biological
toxicity
activities
avermectins.
The Science of The Total Environment,
Год журнала:
2021,
Номер
814, С. 152691 - 152691
Опубликована: Дек. 30, 2021
During
the
COVID-19
pandemic,
high
consumption
of
antivirals,
antibiotics,
antiparasitics,
antiprotozoals,
and
glucocorticoids
used
in
treatment
this
virus
has
been
reported.
Conventional
systems
fail
to
efficiently
remove
these
contaminants
from
water,
becoming
an
emerging
concern
environmental
field.
Therefore,
objective
present
work
is
address
current
state
literature
on
presence
removal
processes
drugs
water
bodies.
It
was
found
that
concentration
most
increased
during
pandemic
Before
Azithromycin
concentrations
surface
waters
were
reported
be
order
4.3
ng
L
Pharmacological Reports,
Год журнала:
2021,
Номер
73(3), С. 736 - 749
Опубликована: Янв. 3, 2021
COVID-19
cases
are
on
surge;
however,
there
is
no
efficient
treatment
or
vaccine
that
can
be
used
for
its
management.
Numerous
clinical
trials
being
reviewed
use
of
different
drugs,
biologics,
and
vaccines
in
COVID-19.
A
much
empirical
approach
will
to
repurpose
existing
drugs
which
pharmacokinetic
safety
data
available,
because
this
facilitate
the
process
drug
development.
The
article
discusses
evidence
available
Ivermectin,
an
anti-parasitic
with
antiviral
properties,
rational
review
was
carried
out
utilizing
their
clinically
significant
attributes.
more
thorough
understanding
met
by
virtual
embodiment
structure
realizable
viral
targets
using
artificial
intelligence
(AI)-based
molecular
dynamics
(MD)-simulation-based
study.
Certain
studies
have
highlighted
significance
ivermectin
COVID-19;
it
requires
evidences
from
Randomised
Controlled
Trials
(RCTs)
dose-
response
support
use.
In
silico-based
analysis
ivermectin's
interaction
specificity
AI
classical
mechanics
simulation-based
methods
indicates
positive
protein
targets,
leading
SARS-CoV
2
N-protein
NTD
(nucleocapsid
N-terminal
domain).
Toxins,
Год журнала:
2021,
Номер
13(5), С. 347 - 347
Опубликована: Май 12, 2021
Macrolides
are
a
diverse
class
of
hydrophobic
compounds
characterized
by
macrocyclic
lactone
ring
and
distinguished
variable
side
chains/groups.
Some
the
most
well
macrolides
toxins
produced
marine
bacteria,
sea
sponges,
other
species.
Many
macrolide
act
as
biomimetic
molecules
to
natural
actin-binding
proteins,
affecting
actin
polymerization,
while
on
different
cytoskeletal
components.
The
disruption
processes
affects
cell
motility
cytokinesis,
can
result
in
cellular
death.
While
many
toxic
nature,
others
have
been
shown
display
therapeutic
properties.
Indeed,
some
known
antibiotic
compounds,
including
erythromycin,
macrolides.
In
addition
properties,
antiviral,
antiparasitic,
antifungal,
immunosuppressive
actions.
Here,
we
review
each
functional
for
their
common
structures,
mechanisms
action,
pharmacology,
human
targets.
BMJ evidence-based medicine,
Год журнала:
2021,
Номер
27(3), С. 156 - 158
Опубликована: Апрель 22, 2021
Background:
Avascular
necrosis
(AN)
is
a
disabling
disease
affecting
predominantly
young
men.
It
steadily
progresses
to
secondary
osteoarthritis.
The
rate
of
disability
high,
because
hip
joint
most
commonly
affected
by
AN;
moreover,
the
bilateral
involvement
also
high.
key
event
in
pathogenesis
AN
circulation
disorder
which
results
ischemia
and,
furthermore,
death
bone
tissue.
Nowadays
data
about
lipid
metabolism
patients
with
AN.
Besides,
there
contradictory
role
homocysteine
risk
cardiovascular
events.
Based
on
these,
it
topical
investigate
and
endothelial
function
Objectives:
aim
present
study
was
different
stages
order
find
factors
for
incidence
progression
this
disease.
Methods:
We
recruited
41
femoral
head
or
condyles
aged
51
(35-64)
years,
56,1%
(n=23)
were
male.
inclusion
criteria
diagnosis
confirmed
X-Ray,
CT
MRI.
exclusion
were:
traumatic
AN,
Legg-Calve-Pertes
disease,
connective
tissue
systemic
diseases.
Also
we
divided
into
subgroups
early
(39%
(n=16))
late
(61,0%
(n=25))
Patients
control
group
(n=32)
comparable
age
gender.
proceeded
using
non-parametric
descriptive
statistics.
evaluated
following
parameters:
homocysteine,
total
cholesterol,
high-density
lipoprotein
low-density
very
cholesterol
ratio,
apolipoprotein
A1,
B.
Results:
In
observed
higher
level
(12,119
(7,771-14,38)
vs.
7,911
(6,612-10,54)
mcmol/l,
p=0,05).
are
consistent
that
homocyseine
associated
events
(1).
There
literature
elevated
lower
levels
vitamin
B12
folic
acid.
Thus,
interpretation
homocystene
significance
more
reliable
association
acid
levels.
Also,
HDLP-C
than
pate
(1,55
(1,31-1,57)
1,23
(1,04-1,36)
mmol/l,
р=0,04).
can
be
interpreted
as
protective
factor
against
contralateral
patients.
obtained
existing
lowers
[1]Steven
G.
Chrysant
&
George
S.
(2018)
current
status
disease:
mini
review,
Expert
Review
Cardiovascular
Therapy,
16:8,
559-565,
DOI:
10.1080/14779072.2018.1497974.
[2]Narayanan,
A.,
Khanchandani,
P.,
Borkar,
R.M.
et
al.
Necrosis
Femoral
Head:
A
Metabolomic,
Biophysical,
Biochemical,
Electron
Microscopic
Histopathological
Characterization.
Sci
Rep
7,
10721
(2017).
https://doi.org/10.1038/.
Future Virology,
Год журнала:
2021,
Номер
16(4), С. 277 - 291
Опубликована: Март 25, 2021
Aim:
COVID-19
is
currently
the
biggest
threat
to
mankind.
Recently,
ivermectin
(a
US
FDA-approved
antiparasitic
drug)
has
been
explored
as
an
anti-SARS-CoV-2
agent.
Herein,
we
have
studied
possible
mechanism
of
action
using
in
silico
approaches.
Materials
&
methods:
Interaction
against
key
proteins
involved
SARS-CoV-2
pathogenesis
were
investigated
through
molecular
docking
and
dynamic
simulation.
Results:
Ivermectin
was
found
a
blocker
viral
replicase,
protease
human
TMPRSS2,
which
could
be
biophysical
basis
behind
its
antiviral
efficiency.
The
ADMET
profile
on
par
with
used
anticorona
drugs
such
hydroxychloroquine
remdesivir.
Conclusion:
Our
study
enlightens
candidature
effective
drug
for
treating
COVID-19.
Current Research in Pharmacology and Drug Discovery,
Год журнала:
2022,
Номер
3, С. 100086 - 100086
Опубликована: Янв. 1, 2022
Since
its
inception
in
late
December
2020
China,
novel
coronavirus
has
affected
the
global
socio-economic
aspect.
Currently,
world
is
seeking
safe
and
effective
treatment
measures
against
COVID-19
to
eradicate
it.
Many
established
drug
molecules
are
tested
SARS-CoV-2
as
a
part
of
repurposing
where
some
proved
for
symptomatic
relief
while
ineffective.
Drug
practical
strategy
rapidly
developing
antiviral
agents.
drugs
presently
being
repurposed
utilizing
basic
understanding
disease
pathogenesis
pharmacodynamics,
well
computational
methods.
In
present
situation,
could
be
viewed
new
option
COVID-19.
Several
biologics
engineered
under
different
stages
clinical
development.
A
few
products
approved
by
USFDA
emergency
use
covid
management.
Due
continuous
mutation,
many
vaccines
not
much
efficacious
render
individual
immune
opportunistic
infection
mutants.
Hence,
there
strong
need
cogent
therapeutic
agent
this
review,
consolidated
summary
developments
depicted
along
with
an
overview
management
post
complications.
