scieee Science in your language
[en] (orig)

Uptake and intracellular activity of an optically active ofloxacin isomer in human neutrophils and tissue culture cells

Abstract

The penetration of an optically active ofloxacin isomer [(-)-ofloxacin] into human neutrophils and different tissue culture cells (HEp-2, McCoy, MDCK, and Vero) was studied and compared with that of ofloxacin by a fluorometric assay. The cellular-to-extracellular-concentration ratios (C/E) of (-)-ofloxacin were always higher than 6, significantly greater than those of ofloxacin at extracellular concentrations of 5 and 10 mg/liter. The penetration of (-)-ofloxacin and ofloxacin was doubled when neutrophils were stimulated by phorbol myristate acetate but not affected after ingestion of opsonized Staphylococcus aureus. The C/E ratios of (-)-ofloxacin and ofloxacin for different tissue culture epithelial cells and fibroblasts were lower than those of neutrophils but still higher than 2. Both compounds produced a significant reduction in viable intraphagocytic S. aureus during 3 h of exposure to antimicrobial agents. We conclude that (-)-ofloxacin appears to reach higher intracellular concentrations than ofloxacin, remaining active inside the neutrophils.

Read accessible full text

Uptake and intracellular activity of an optically active ofloxacin isomer in human neutrophils and tissue culture cells

Author: Pascual Hernández, Álvaro; García Luque, Isabel; Perea Pérez, Evelio José
Publisher: American Society for Microbiology
Year: 1990
Source: https://idus.us.es/bitstreams/d7245a62-0044-45fe-b1ce-b9010ad62089/download
Vol.
34,
No.
2
ANTIMICROBIAL
AGENTS
AND
CHEMOTHERAPY,
Feb.
1990,
p.
277-280
0066-4804/90/020277-04$02.00/0
Copy igh
C
1990,
Ame ican
Socie y
o
Mic obiology
Up ake
and
In acellula
Ac i i y
o
an
Op ically
Ac i e
O loxacin
Isome
in
Human
Neu ophils
and
Tissue
Cul u e
Cells
ALVARO
PASCUAL,*
ISABEL
GARCIA,
AND
EVELIO
J.
PEREA
Depa men
o
Mic obiology,
School
o
Medicine,
Uni e si y
o
Se ille,
Apdo.
914,
Se ille41080,
Spain
Recei ed
28
June
1989/Accep ed
31
Oc obe
1989
The
pene a ion
o
an
op ically
ac i e
o loxacin
isome
[(-)-o loxacin]
in o
human
neu ophils
and
di e en
issue
cul u e
cells
(HEp-2,
McCoy,
MDCK,
and
Ve o)
was
s udied
and
compa ed
wi h
ha
o
o loxacin
by
a
luo ome ic
assay.
The
cellula - o-ex acellula -concen a ion
a ios
(CIE)
o
(-)-o loxacin
we e
always
highe
han
6,
signi ican ly
g ea e
han
hose
o
o loxacin
a
ex acellula
concen a ions
o
5
and
10
mg/li e .
The
pene a ion
o
(-)-o loxacin
and
o loxacin
was
doubled
when
neu ophils
we e
s imula ed
by
pho bol
my is a e
ace a e
bu
no
a ec ed
a e
inges ion
o
opsonized
S aphylococcus
au eus.
The
CIE
a ios
o
(-)-o loxacin
and
o loxacin
o
di e en
issue
cul u e
epi helial
cells
and
ib oblas s
we e
lowe
han
hose
o
neu ophils
bu
s ill
highe
han
2.
Bo h
compounds
p oduced
a
signi ican
educ ion
in
iable
in aphagocy ic
S.
au eus
du ing
3
h
o
exposu e
o
an imic obial
agen s.
We
conclude
ha
(-)-o loxacin
appea s
o
each
highe
in acellula
concen a ions
han
o loxacin,
emaining
ac i e
inside
he
neu ophils.
O loxacin
(OFLX)
is
a
quinolone
compound
ha
shows
high
ac i i y
agains
a
a ie y
o
g am-posi i e
and
g am-
nega i e
bac e ia
(17).
By
using
high-pe o mance
liquid
ch oma og aphy,
wo
op ically
ac i e
OFLX
isome s
ha e
been
p epa ed:
(+)-OFLX
and
(-)-OFLX
(6).
The
la e
isome
inhibi ed
he
supe coiling
ac i i y
o
gy ase
om
Mic ococcus
lu eus
7.4
imes
mo e
e ec i ely
han
did
he
(+)-isome
(7).
Mo eo e ,
he
in
i o
ac i i y
o
(-)-OFLX
agains
a
a ie y
o
g am-posi i e
and
g am-nega i e
bac e ia
was
8
o
128
imes
highe
han
ha
o
(+)-OFLX
and
wice
as
high
as
ha
o
acemic
OFLX
(6).
The
in acellula
pene a ion
and
ac i i y
o
an imic obial
agen s
can
be
an
impo an
ac o
in
he
ea men
o
in ec ions
caused
by
in acellula
acul a i e
o
obliga e
pa hogens.
Mos
s udies
on
he
abili y
o
an imic obial
agen s
o
pene a e
in o
cells
ha e
u ilized
phagocy ic
cells,
and
only
a
ew
s udies
ha e
e alua ed
he
pene a ion
in o
o he
ypes
o
cells,
such
as
epi helial
cells
(1,
2).
The e
is,
howe e ,
s ong
e idence
ha
some
en e oin asi e
bac e ia
such
as
en e oin asi e
Esche ichia
coli
su i e
in
epi helial
cells
despi e
high
ex e nal
aminoglycoside
concen a ions
because
o
he
low
in acellula
pene a ion
a e
o
hese
an imic obial
agen s
(8).
We
ha e
p e iously
epo ed
ha
OFLX
pene a es
in o
human
polymo phonuclea
leukocy es
(PMNs)
by
an
ac i e
mechanism
and
emains
ac i e
in acellula ly
agains
S aph-
ylococcus
au eus
(13).
Since
he
an imic obial
ac i i y
o
OFLX
seems
o
be
media ed
mainly
by
(-)-OFLX,
i
would
be
impo an
o
s udy
whe he
his
isome
can
be
concen-
a ed
in o
phagocy es
and
o he
euca yo ic
cells.
The
pu pose
o
his
s udy
is
o
e alua e
he
in acellula
pene a ion
o
his
op ically
ac i e
OFLX
isome ,
(-)-
OFLX,
in o
human
PMNs
and
di e en
issue
cul u e
cells
compa ed
wi h
ha
o
OFLX.
The
in acellula
ac i i y
in
PMNs
o
bo h
compounds
agains
S.
au eus
is
also
assessed.
MATERIALS
AND
METHODS
Isola ion
o
PMNs.
PMNs
we e
eco e ed
om
hepa in-
ized
enous
blood
o
heal hy
dono s
and
we e
pu i ied
by
p e iously
desc ibed
me hods
(16).
PMN
p epa a ions
we e
*
Co esponding
au ho .
97%
pu e.
Final
cell
suspensions
we e
adjus ed
o
5
x
106
PMNs
pe
ml
in
Hanks
balanced
sal
solu ion.
PMNs
we e
95%
iable
by
ypan
blue
exclusion.
Tissue
cul u e
cells.
HEp-2,
McCoy,
MDCK,
and
Ve o
cells
(Flow
Labo a o ies,
I ine,
Uni ed
Kingdom)
we e
g own
in
minimal
essen ial
medium
(Flow)
supplemen ed
wi h
1
mM
HEPES
(N-2-hyd oxye hylpipe azine-N'-2-
e hanesul onic
acid;
Flow)
and
con aining
10%
e al
cal
se um
(Flow)
wi hou
an ibio ics.
Fo
each
expe imen
cells
we e
de ached
om
issue
cul u e
bo les
wi h
ypsin-
EDTA
(Flow)
and
suspended
i
Hanks
balanced
sal
solu-
ion
a
a
concen a ion
o
5
x
106
cells
pe
ml.
An imic obial
agen
up ake
by
cells.
A
p e iously
de-
sc ibed
luo ome ic
assay
o
measu e
quinolone
up ake
by
human
PMNs
was
used
(13).
The
op ically
ac i e
o loxacin
isome
(-)-OFLX
was
kindly
supplied
by
Daiichi
Seiyaku
Co.,
L d.
(Tokyo,
Japan),
and
OFLX
was
supplied
by
Hoesch
(Fede al
Republic
o
Ge many).
In
hese
expe i-
men s
PMNs
o
issue
cul u e
cells
we e
incuba ed
in
Hanks
balanced
sal
solu ion
con aining
di e en
concen a ions
o
he
an imic obial
agen
(2,
5,
and
10
mg/li e ).
A e
di e en
incuba ion
imes
(1.5,
20,
and
30
min)
a
37°C,
cells
we e
sepa a ed
om
ex acellula
solu ion
by
cen i uga ion
h ough
a
wa e -impe meable
silicone-oil
ba ie
in
a
mic o-
cen i uge
ube
(9).
The
en i e
cell
pelle ,
ob ained
by
cu ing
o
he
po ion
o
he
mic o uge
ube
con aining
he
pelle ,
was
placed
in
2
ml
o
0.1
M
glycine-HCl
bu e
(pH
3.0)
and
agi a ed
igo ously
in
a
o ex
shake .
Incuba ion
o
2
h
a
oom
empe a u e
was
su icien
o
elease
ully
in acellula
an imic obial
agen .
The
samples
we e
cen i uged
o
5
min
a
5,600
x
g,
and
he
amoun
o
an imic obial
agen
was
de e mined
by
luo escence
emission
o
he
supe na an s
wi h
a
Kon on
SFM
25
luo escence
spec opho ome e
(Kon on,
Swi ze land).
The
luo escence
exci a ion
and
emission
maxima
o
OFLX
and
(-)-OFLX
in
0.1
M
glycine-
HCl
(pH
3.0)
we e
292
and
496
nm,
espec i ely.
Con ols
wi hou
an imic obial
agen s
we e
always
used
o
de e mine
he
backg ound
luo escence.
The
in acellula
wa e
space
was
measu ed
by
using
i ia ed
wa e
and
he
ex acellula
ma ke
[14C]polye hy-
lene
glycol
(1.4
mCi/g;
New
England
Nuclea
Co p.,
Bos on,
Mass.).
The
cells
we e
incuba ed
wi h
hese
adiolabeled
277
on Augus 2, 2017 by USE/BCTA.GEN UNIVERSITARIAh p://aac.asm.o g/Downloaded om
ANTIMICROB.
AGENTS
CHEMOTHER.
compounds
o
2
min
a
37°C,
and
hen
cells
we e
sepa a ed
om
ex acellula
luid
by
eloci y
g adien
cen i uga ion
as
desc ibed
abo e
and
coun ed
in
a
liquid
scin illa ion
coun e .
The
o al
wa e
con en
o
he
cell
pelle
was
co ec ed
o
apped
ex acellula
wa e ,
i.e.,
polye hylene
glycol
space,
o
ob ain
he
in acellula
wa e
space.
F om
he
alues
ob ained
om
his
p ocedu e,
cell-associa ed
an imic obial
agen
concen a ions
we e
calcula ed
and
exp essed
as
a
a io
o
he
cellula
concen a ion
o
ex acellula
concen a-
ion
(CIE)
(9).
In
a
se ies
o
expe imen s,
OFLX
and
(-)-OFLX
(ex a-
cellula
concen a ion,
5
mg/li e )
up ake
by
human
PMNs
was
measu ed
a e
s imula ion
o
he
cells
wi h
200
nM
ei he
pho bol
my is a e
ace a e
(PMA;
Sigma
Chemical
Co.,
S .
Louis,
Mo.)
o
S.
au eus
ATCC
25923
opsonized
in
5%
pooled
human
se um
(15
min,
37°C)
a
a
10/1
a io
o
bac e ia
o
PMNs.
PMA
o
opsonized
bac e ia
we e
added
o
he
PMN
suspensions
a
he
same
ime
as
he
an imic obial
agen s,
and
he
up ake
was
measu ed
as
desc ibed
abo e.
Since
he
measu emen
o
OFLX
and
(-)-OFLX
is
indi ec
and
dependen
upon
luo escence,
con ols
we e
always
pe o med
o
e alua e
he
e ec
o
s imuli
on
he
luo es-
cence
o
he
an imic obial
agen s
in
cell- ee
sys ems.
In acelula
ac i i y
o
an imic obial
agen s.
To
e alua e
he
in acellula
ac i i y
o
an imic obial
agen s,
a
p e iously
desc ibed
me hod
was
used
(15).
B ie ly,
0.1
ml
o
opsonized
bac e ial
suspension
(5
x
107
CFU/ml)
and
0.1
ml
o
PMNs
(5
x
106
PMNs
pe
ml)
we e
combined
in
a
se ies
o
polyp opylene
bio ials
(Beckman
Ins umen s,
Inc.,
Fulle -
on,
Cali .)
and
incuba ed
in
a
shake
(250
pm)
o
60
min
a
370C.
A e
incuba ion,
ex acellula
bac e ia
we e
emo ed
by
di e en ial
cen i uga ion.
Cells
we e
hen
suspended
in
0.2
ml
o
RPMI
medium
(GIBCO,
Uni ed
Kingdom).
A
his
ime
(designa ed
ime
ze o)
he
di e en
an imic obial
agen s
we e
added,
and
he
ials
we e
incuba ed
in
a
shake
(250
pm)
a
370C.
Vials
we e
emo ed
a
ime
ze o
(con ol)
and
a e
3
h
o
incuba ion
(con ol
and
samples
wi h
an imic o-
bial
agen s).
Cells
we e
lysed
in
dis illed
wa e ,
and
samples
we e
dilu ed
and
pou
pla ed
in
aga .
Colonies
we e
coun ed
a e
24
h
o
incuba ion
a
370C.
The
da a
we e
exp essed
as
pe cen ages
o
su i ing
s aphylococci
compa ed
wi h
con-
ols
(wi hou
an imic obial
agen s)
a
ime
ze o.
In
addi ion
10-
9-
8-
7-
0
~
6-
4
lx
5
w
'-%
4-
3-
2-
I-
2
5
10
Ex ocellula
concen a ion
(mg/I)
FIG.
1.
OFLX
(C1)
and
(-)-OFLX
(O)
up ake
by
human
PMNs
a
di e en
ex acellula
concen a ions
(n
=
6).
Incuba ions
we e
done
o
20
min.
Fo
he
da a
om
concen a ions
o
5
and
10
mg/li e ,
P
<
0.05.
10
8'
w
5
J4
3
2
I
5
10
20
TIME
(min)
FIG.
2.
OFLX
(0)
and
(-)-OFLX
(A)
up ake
by
human
PMNs
a
di e en
imes
(n
=
4).
The
ex acellula
concen a ion
was
5
mg/li e .
o
de e mining
bac e ial
su i al,
mo phologic
s udies
we e
also
ou inely
pe o med
a
ime
ze o
and
a e
3
h
o
incuba ion
o
e alua e
he
disposi ion
o
bac e ia
(cell
asso-
cia ed
o
ex acellula ).
Samples
o
50
,ul
we e
emo ed
om
bio ials
and
deposi ed
on
glass
slides.
A e
s aining
wi h
W igh
s ain,
samples
we e
examined
by
ligh
mic oscopy.
All
assays
we e
pe o med
in
duplica e
wi h
PMNs
om
i e
di e en
dono s.
S a is ical
analysis
o
da a.
Da a
we e
exp essed
as
he
means
s anda d
de ia ions.
Di e ences
among
g oups
we e
compa ed
by
analysis
o
a iance
wi h
he
Bon e oni
me hod
(18),
used
o
assess
s a is ical
signi icance
a
P
s
0.05.
RESULTS
Up ake
o
an imic obial
agen s
by
PMNS.
Figu e
1
shows
he
CIE
a ios
o
OFLX
and
(-)-OFLX
incuba ed
wi h
human
PMNs
a
di e en
ex acellula
concen a ions.
Bo h
OFLX
and
(-)-OFLX
showed
high
CIE
a ios,
being
signi -
ican ly
highe
o
he
la e
a
ex acellula
concen a ions
o
S
and
10
mg/li e .
The
pene a ion
o
cell
associa ion
o
OFLX
occu ed
sligh ly
mo e
apidly
han
did
ha
o
(-)-OFLX
(Fig.
2).
The
s imula ion
o
PMNs
by
a
memb ane
ac i a o
(PMA)
enhanced
he
in acellula
pene a ion
o
OFLX
and
(-)-
OFLX
2.4
and
1.5
imes,
espec i ely
(Table
1).
The
incu-
ba ion
o
PMNs
wi h
opsonized
S.
au eus
ATCC
25923,
howe e ,
did
no
modi y
he
up ake
o
ei he
compound.
TABLE
1.
E ec
o
he
incuba ion
o
human
PMNs
wi h
ei he
opsonized
S.
au eus
ATCC
25923
o
PMA
on
he
up ake
o
OFLX
and
(-)-OFLX
by
hese
cells
(n
=
4)1
CIE
a io
S imulus
OFLX
(-)-OFLX
None
(con ol)
6.0
±
1.3
8.3
±
1.7
Opsonized
S.
au eus
5.2
±
1.1
7.0
±
1.6
PMA
(200
nM)
14.4
±
2.3"
13.0
±
2.3"
a
Incuba ions
we e
done
o
20
min.
The
ex acellula
concen a ion
o
OFLX
o
(-)-OFLX
was
5
mg/li e .
b
p
<
0.05
compa ed
wi h
he
con ol.
278
PASCUAL
ET
AL.
on Augus 2, 2017 by USE/BCTA.GEN UNIVERSITARIAh p://aac.asm.o g/Downloaded om
OFLOXACIN
ISOMER
UPTAKE
BY
HUMAN
NEUTROPHILS
TABLE
2.
OFLX
and
(-)-OFLX
up ake
by
human
PMNs
and
di e en
issue
cul u e
cells
(n
=4)
An imic o-
CIE
a io
bial
agen
PMN
HEp-2
McCoy
MDCK
Ve o
OFLX
5.8
±
1.2
2.1
±
0.2 3.9
±
1.1
2.1
±
0.9
3.4
±
1.2
(-)-OFLX
8.2
1.7b
2.8
±
0.6
4.7
±
1.3
1.9
±
0.9
2.4
±
0.6
a
Incuba ions
we e
done
o
20
min.
The
ex acellula
concen a ion
o
OFLX
o
(-)-OFLX
was
5
mg/li e .
b
p
<
0.05
compa ed
wi h
alue
o
OFLX.
Up ake
o
an imic obial
agen s
by
issue
cul u e
cells.
The
CIE
a ios
o
OFLX
and
(-)-OFLX
incuba ed
wi h
h ee
issue
cul u e
epi helial
cells
om
di e en
o igins
(HEp-2,
McCoy,
and
MDCK)
and
one
issue
cul u e
ib oblas
cell
line
(Ve o)
o
20
min
a
37°C
a e
shown
in
Table
2.
The
CIE
a ios
o
OFLX
and
(-)-OFLX
we e
2
o
3
imes
lowe
han
hose
obse ed
wi h
PMNs,
and
he e
we e
no
signi ican
di e ences
be ween
he
wo
compounds.
In acellula
ac i i ies
o
an imic obial
agen s.
The
in ac-
ellula
ac i i ies
o
di e en
concen a ions
o
OFLX
and
(-)-OFLX
agains
S.
au eus
ATCC
25923
we e
e alua ed
in
a
3-h
assay
(Table
3).
A
all
o
he
concen a ions
e alua ed,
(-)-OFLX
p oduced
a
signi ican
educ ion
o
he
su i al
o
S.
au eus
in
PMNs,
simila
o
ha
p oduced
by
OFLX.
DISCUSSION
(-)-OFLX
is
an
op ically
ac i e
OFLX
isome
ha
shows
highe
in
i o
ac i i y
han
(+)-OFLX
and
he
acemic
compound
OFLX
agains
di e en
mic oo ganisms
(6,
7).
The
pu pose
o
his
s udy
was
o
e alua e
whe he
his
inc eased
ac i i y
was
accompanied
by
a
highe
in acellula
pene a ion
and
ac i i y
han
hose
o
OFLX.
The
(-)-
OFLX
up ake
by
human
PMNs
was
signi ican ly
highe
han
ha
o
OFLX
a
ex acellula
concen a ions
o
5
and
10
mg/li e .
This
di e ence
was
no
obse ed
a
a
lowe
con-
cen a ion
(2
mg/li e ).
Ne e heless,
bo h
compounds
eached
high
in acellula
concen a ions
in
hese
phago-
cy es,
as
has
been
desc ibed
o
o he
quinolones
wi h
di e en
me hodology
(3,
10).
The
pene a ion
o
(-)-OFLX
and
OFLX
was
no
a ec ed
when
PMNs
we e
incuba ed
wi h
opsonized
S.
au eus.
This
has
been
desc ibed
o
o he
an imic obial
agen s
such
as
e y h omycin,
i ampin,
and
gen amicin
(5).
Howe e ,
he
TABLE
3.
E ec
o
OFLX
and
(-)-OFLX
on
he
su i al
o
S.
au eus
ATCC
25923
wi hin
human
PMNs
(n
=
5)
An imic obial
agen
and
%
Su i al
o
concn
(mg/li e )
S.
au eus
a
3
h
No
agen
45.5
±
5.2
OFLX
0.5
20.9
±
3.
la
2
17.6
±
3.0O
5
15.0
±
2.7a
10
5.8
±
1.4a
(-)-OFLX
0.5
17.8
±
3.2a
2
15.5
±
3.
la
5
12.2
±
2.6a
10
9.1
±
2.1la
a
P
<
0.05
compa ed
wi h
he
con ol.
pene a ion
o
o he
an imic obial
agen s,
such
as
clindamy-
cin,
has
been
shown
o
inc ease
a e
phagocy osis
o
S.
au eus
(5).
The
s imula ion
o
PMN
memb anes
by
PMA,
howe e ,
doubled
he
up ake
o
bo h
compounds
by
human
PMNs,
poin ing
ou
ha
he
pene a ion
o
(-)-OFLX
in o
PMNs
could
be
media ed
by
an
ac i e
mechanism,
as
has
been
demons a ed
o
o loxacin
(13),
since
PMA
ac i a es
he
NADPH
oxidase
sys em
ia
p o ein
kinase
C
(11).
To
s udy
he
pene a ion
o
hese
an imic obial
agen s
in o
o he
euca yo ic
cells,
we
used
a
issue
cul u e
cell
model.
The
pene a ion
o
bo h
compounds
in o
issue
cul u e
epi helial
cells
and
ib oblas s
was
signi ican ly
lowe
han
ha
ob-
se ed
in
PMNs
bu
s ill
eached
in acellula
concen a ions
ha
we e
a
leas
double
he
ex acellula
concen a ions.
The
use
o
his
model
o e s
an
in e es ing
insigh
in o
he
pene a ion
o
an ibac e ial
subs ances
in o
cells
and
may
ha e
ele ance
o
human
in ec ions
p oduced
by
mic oo -
ganisms
ha .
a e
able
o
su i e
and
e en
mul iply
wi hin
epi helial
cells.
Con as s
be ween
phagocy e
an imic obial
agen
up ake
and
in acellula
ac i i y
ha e
been
desc ibed
o
a
ew
an imic obial
agen s
(5,
15).
In
ou
s udy,
(-)-OFLX
showed
a
good
in acellula
pene a ion
in o
and
ac i i y
in
PMNs
agains
S.
au eus.
The
in acellula
an imic obial
ac i i y
o
his
isome
was
simila
o
ha
obse ed
o
he
acemic
compound
and
simila
o
hose
desc ibed
o
o he
quino-
lones
agains
di e en
bac e ia
(4,12,
14).
In
summa y,
(-)-OFLX,
an
op ically
ac i e
OFLX
iso-
me ,
pene a ed
in o
human
PMN,
eaching
concen a ions
highe
han
- hose
eached
by
OFLX
and
emaining
ac i e
in acellula ly.
This
compound
also
showed
a
high
pene a-
ion
in o
issue
cul u e
epi helial
cells
and
ib oblas s.
The
high
an imic obial
ac i i y
o
his
compound,
highe
e en
han
ha
o
he
acemic
compound
OFLX,
added
o
he
p ope ies
obse ed
in
his
s udy,
could
jus i y
addi ional
s udies
o
e alua e
he
possible
clinical
ele ance o
hese
indings.
ACKNOWLEDGMENTS
We
hank
M.
C.
Guzman
o
echnical
assis ance
and
C.
Acos a
o
yping
he
manusc ip .
LITERATURE
CITED
1.
B own,
K.
N.,
and
A.
Pe ci al.
1978.
Pene a ion
o
an imic o-
bials
in o
issue
cul u e
cells
and
leukocy es.
Scand.
J.
In ec .
Dis.
14(Suppl.):251-260.
2.
Chadwick,
P.
R.,
and
A. R.
Meile sh.
1987.
The
use
o
a
issue
cul u e
model
o
assess
he
pene a ion
o
an ibio ics
in o
epi helial
cells.
J.
An imic ob.
Chemo he .
19:211-220.
3.
Easmon,
C.
S.
F.,
and
J.
P.
C ane.
1985.
Up ake
o
cip o loxacin
by
mac ophages.
J.
Clin.
Pa hol.
38:442-444.
4.
Easmon,
C.
S.
F.,
J.
P.
C ane,
and
A.
Blowe s.
1986.
E ec
o
cip o loxacin
on
in acellula
o ganisms:
in- i o
and
in- i o
s udies.
J.
An imic ob.
Chemo he .
18(Suppl.
D):43-48.
5.
Hand,
W.
L.,
and
N.
L.
King-Thompson.
1986.
Con as
be-
ween
phagocy e
an ibio ic
up ake
and
subsequen
in acellula
bac e icidal
ac i i y.
An imic ob.
Agen s
Chemo he .
29:135-
140.
6.
Hayakawa,
I.,
S.
A a ashi,
S.
Yokohama,
M.
Imamu a,
K.
Sakano,
and
M.
Fu ukawa.
1986.
Syn hesis
and
an ibac e ial
ac i i ies
o
op ically
ac i e
o loxacin.
An imic ob.
Agen s
Chemo he .
29:163-164.
7.
Imamu a,
M.,
S.
Shibamu a,
I.
Hayakawa,
and
Y.
Osada.
1987.
Inhibi ion
o
DNA
gy ase
by
op ically
ac i e
o loxacin.
An imi-
c ob.
Agen s
Chemo he .
31:325-327.
8.
Kihis om,
E.,
and
L.
Andake .
1985.
Inabili y
o
gen amicin
and
VOL.
34,
1990
279
on Augus 2, 2017 by USE/BCTA.GEN UNIVERSITARIAh p://aac.asm.o g/Downloaded om
ANTIMICROB.
AGENTS
CHEMOTHER.
os omycin
o
elimina e
in acellula
En e obac e iaceae.
J.
An imic ob.
Chemo he .
15:723-728.
9.
Klempne ,
M.
S.,
and
B.
S y .
1981.
Clindamycin
up ake
by
human
neu ophils.
J.
In ec .
Dis.
144:472475.
10.
Koga,
H.
1987.
High-pe o mance
liquid
ch oma og aphy
mea-
su emen
o
an imic obial
concen a ions
in
polymo phonuclea
leukocy es.
An imic ob.
Agen s
Chemo he .
31:1904-1908.
11.
Ma idonneau-Pa ini,
I.,
S.
M.
T ingale,
and
A.
I.
Taube .
1986.
Iden i ica ion
o
dis inc
ac i a ion
pa hways
o
he
human
neu ophil
NADPH-oxidase.
J.
Immunol.
137:2925-2929.
12.
Mila o ic,
D.
1986.
In aphagocy ic
ac i i y
o
cip o loxacin
and
CI
934.
Eu .
J.
Clin.
Mic obiol.
5:659-660.
13.
Pascual,
A.,
I.
Ga cia,
and
E.
J.
Pe ea.
1989.
Fluo ome ic
measu emen
o
o loxacin
up ake
by
human
polymo phonuclea
leukocy es.
An imic ob.
Agen s
Chemo he .
33:653-656.
14.
Pascual,
A.,
L.
Ma inez-Ma inez,
and
E.
J.
Pe ea.
1989.
E ec
o
cip o loxacin
and
o loxacin
on
human
polymo phonuclea
leukocy e
ac i i y
agains
s aphylococci.
Chemo he apy
(Basel)
35:17-22.
15.
Pascual,
A.,
D.
Tsukayama,
J.
Ko a ik,
G.
Gekke ,
and
P.
K.
Pe e son.
1987.
Up ake
and
ac i i y
o
i apen ine
in
human
pe i oneal
mac ophages
and
polymo phonuclea
leukocy es.
Eu .
J.
Clin.
Mic obiol.
6:152-157.
16.
Pe e son,
P.
K.,
J.
Ve hoe ,
D.
Schmeling,
and
P.
G.
Quie.
1977.
Kine ics
o
phagocy osis
and
bac e ial
killing
by
human
poly-
mo phonuclea
leukocy es
and
monocy es.
J.
In ec .
Dis.
136:
502-509.
17.
Salo,
K.,
Y.
Ma suu a,
M.
Ino e,
T.
Une,
Y.
Osada,
H.
Ogawa,
and
S.
Mi suhashi.
1982.
In
i o
and
in
i o
ac i i y
o
DL-8280,
a
new
oxazine
de i a i e.
An imic ob.
Agen s
Che-
mo he .
22:548-553.
18.
Wallens ein,
S.,
C.
L.
Zucne ,
and
J.
L.
Feiss.
1980.
Some
s a is ical
me hods
use ul
in
ci cula ion
esea ch.
Ci c.
Res.
47:1-9.
280
PASCUAL
ET
AL.
on Augus 2, 2017 by USE/BCTA.GEN UNIVERSITARIAh p://aac.asm.o g/Downloaded om