P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.

Abstract:

:Moxifloxacin (MXF) is a fluoroquinolone antibiotic that is effective against respiratory infections. However, the mechanisms of MXF lung diffusion are unknown. Active transport in other tissues has been suggested for several members of the fluoroquinolone family. In this study, transport of MXF was systematically investigated across a Calu-3 lung epithelial cell model. MXF showed polarized transport, with the secretory permeability being twice as high as the absorptive permeability. The secretory permeability was concentration dependent (apparent P(max) = 13.6 x 10(-6) cm x s(-1); apparent K(m) = 147 microM), suggesting saturated transport at concentrations higher than 350 microg/ml. The P-glycoprotein inhibitor PSC-833 inhibited MXF transport in both directions, whereas probenecid, a multidrug resistance-related protein inhibitor, appeared to have no effect in the Calu-3 model. Moreover, rifampin, a known inducer of efflux transport proteins, upregulated the expression of P-glycoprotein in Calu-3 cells and enhanced MXF active transport. In conclusion, this study clearly indicates that MXF is subject to P-glycoprotein-mediated active transport in the Calu-3 model. This P-glycoprotein-dependent secretion may lead to higher MXF epithelial lining fluid concentrations than those in plasma. Furthermore, drug-drug interactions may be expected when MXF is combined with other P-glycoprotein substrates or modulators.

authors

Brillault J,De Castro WV,Harnois T,Kitzis A,Olivier JC,Couet W

doi

10.1128/AAC.01253-08

subject

Has Abstract

pub_date

2009-04-01 00:00:00

pages

1457-62

issue

4

eissn

0066-4804

issn

1098-6596

pii

AAC.01253-08

journal_volume

53

pub_type

杂志文章
  • In Vitro Antiviral Activity and Resistance Profile Characterization of the Hepatitis C Virus NS5A Inhibitor Ledipasvir.

    abstract::Ledipasvir (LDV; GS-5885), a component of Harvoni (a fixed-dose combination of LDV with sofosbuvir [SOF]), is approved to treat chronic hepatitis C virus (HCV) infection. Here, we report key preclinical antiviral properties of LDV, including in vitro potency, in vitro resistance profile, and activity in combination wi...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02524-15

    authors: Cheng G,Tian Y,Doehle B,Peng B,Corsa A,Lee YJ,Gong R,Yu M,Han B,Xu S,Dvory-Sobol H,Perron M,Xu Y,Mo H,Pagratis N,Link JO,Delaney W

    更新日期:2016-01-11 00:00:00

  • Vancomycin-resistant Staphylococcus aureus isolate from a patient in Pennsylvania.

    abstract::A vancomycin-resistant Staphylococcus aureus (VRSA) isolate was obtained from a patient in Pennsylvania in September 2002. Species identification was confirmed by standard biochemical tests and analysis of 16S ribosomal DNA, gyrA, and gyrB sequences; all of the results were consistent with the S. aureus identification...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.48.1.275-280.2004

    authors: Tenover FC,Weigel LM,Appelbaum PC,McDougal LK,Chaitram J,McAllister S,Clark N,Killgore G,O'Hara CM,Jevitt L,Patel JB,Bozdogan B

    更新日期:2004-01-01 00:00:00

  • The mef(A) gene predominates among seven macrolide resistance genes identified in gram-negative strains representing 13 genera, isolated from healthy Portuguese children.

    abstract::Of the 176 randomly selected, commensal, gram-negative bacteria isolated from healthy children with low exposure to antibiotics, 138 (78%) carried one or more of the seven macrolide resistance genes tested in this study. These isolates included 79 (91%) isolates from the oral cavity and 59 (66%) isolates from urine sa...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.48.9.3451-3456.2004

    authors: Ojo KK,Ulep C,Van Kirk N,Luis H,Bernardo M,Leitao J,Roberts MC

    更新日期:2004-09-01 00:00:00

  • Genetic characterization of vanG, a novel vancomycin resistance locus of Enterococcus faecalis.

    abstract::Enterococcus faecalis strain WCH9 displays a moderate level of resistance to vancomycin (MIC = 16 microgram/ml) and full susceptibility to teicoplanin but is negative by PCR analysis using primers specific for all known enterococcal vancomycin resistance genotypes (vanA, vanB, vanC, vanD, and vanE). We have isolated a...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.44.11.3224-3228.2000

    authors: McKessar SJ,Berry AM,Bell JM,Turnidge JD,Paton JC

    更新日期:2000-11-01 00:00:00

  • Early discontinuation of ethambutol in pulmonary tuberculosis treatment based on results of the GenoType MTBDRplus assay: A prospective, multicenter, non-inferiority randomized trial in South Korea.

    abstract::No studies have investigated whether discontinuation of ethambutol (EMB) based on the susceptibility to isoniazid and rifampin as determined by the GenoType MTBDRplus assay would be appropriate. We aimed to determine the feasibility of discontinuing EMB before the end of intensive phase treatment based on the result o...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00980-19

    authors: Jo KW,Kim M,Kim YJ,Lee HK,Kim HK,Jeon D,Lyu J,Park HK,Mok J,Kim JS,Heo EY,Choi SB,Yim JJ,Shim TS

    更新日期:2019-09-16 00:00:00

  • Amino acid residues essential for function of the MexF efflux pump protein of Pseudomonas aeruginosa.

    abstract::At least four broad-spectrum efflux pumps (Mex) are involved in elevated intrinsic antibiotic resistance as well as in acquired multidrug resistance in Pseudomonas aeruginosa. Substrate specificity of the Mex pumps has been shown to be determined by the cytoplasmic membrane component (MexB, MexD, MexF, and MexY) of th...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.46.7.2169-2173.2002

    authors: Aires JR,Pechère JC,Van Delden C,Köhler T

    更新日期:2002-07-01 00:00:00

  • Class 1 integron-borne gene cassettes in multidrug-resistant Yersinia enterocolitica strains of different phenotypic and genetic types.

    abstract::Seventy nine strains of Yersinia enterocolitica resistant to one or more antimicrobials were analyzed for integrons. Only class 1 sul1 integrons containing aadA1a (28 strains), aadA1a-dfr1-sat1 (2 strains), and dfr1-aadA1a (1 strain) gene cassettes were found. The first two types were found in clinical isolates belong...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.1.421-425.2003

    authors: Soto SM,Lobato MJ,Mendoza MC

    更新日期:2003-01-01 00:00:00

  • Efficacy of sparfloxacin and autoradiographic diffusion pattern of [14C]Sparfloxacin in experimental Staphylococcus aureus joint prosthesis infection.

    abstract::Using a new rabbit model of methicillin-susceptible Staphylococcus aureus knee prosthesis infection, we compared the efficacies of sparfloxacin (50 mg/kg of body weight subcutaneously, twice a day) and pefloxacin (50 mg/kg subcutaneously, twice a day). A partial knee replacement was performed with a silicone implant f...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.40.9.2111

    authors: Crémieux AC,Mghir AS,Bleton R,Manteau M,Belmatoug N,Massias L,Garry L,Sales N,Mazière B,Carbon C

    更新日期:1996-09-01 00:00:00

  • Efficacy of high doses of levofloxacin in experimental foreign-body infection by methicillin-susceptible Staphylococcus aureus.

    abstract::Antimicrobial efficacy in orthopedic device infections is diminished because of bacterial biofilms which express tolerance to antibiotics. Recently, the use of high doses of levofloxacin with rifampin has been recommended for staphylococcal infections. In the present study, we evaluated the efficacy of levofloxacin at...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00523-06

    authors: Murillo O,Doménech A,Garcia A,Tubau F,Cabellos C,Gudiol F,Ariza J

    更新日期:2006-12-01 00:00:00

  • Overproduction of a penicillin-binding protein is not the only mechanism of penicillin resistance in Enterococcus faecium.

    abstract::In 1989 and 1990, a large number of ampicillin-resistant strains of Enterococcus faecium were isolated from infected patients treated at intensive care units in Berlin, Germany. Twenty-five clinical isolates, including five different biotypes as classified by acid production from various sugars and a wide range of sus...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.36.4.783

    authors: Klare I,Rodloff AC,Wagner J,Witte W,Hakenbeck R

    更新日期:1992-04-01 00:00:00

  • Enzymatic assay for measurement of zidovudine triphosphate in peripheral blood mononuclear cells.

    abstract::In this report, we describe a new method to measure intracellular zidovudine triphosphate (ZDV-TP) levels in peripheral blood mononuclear cells (PBMCs) from patients treated with ZDV by utilizing inhibition of human immunodeficiency virus type 1 reverse transcriptase activity by ZDV-TP. Intracellular levels of ZDV-TP ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.38.1.115

    authors: Robbins BL,Rodman J,McDonald C,Srinivas RV,Flynn PM,Fridland A

    更新日期:1994-01-01 00:00:00

  • Susceptibility of Clostridium ramosum to antimicrobial agents.

    abstract::The susceptibility of 49 strains of Clostridium ramosum to 10 antibiotics was determined by agar dilution and disk diffusion tests. Results showed that, among the anaerobes, C. ramosum is second only to Bacteroides fragilis in its resistance to antimicrobial agents. All strains were susceptible to penicillin, carbenic...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.5.6.589

    authors: Tally FP,Armfield AY,Dowell VR Jr,Kwok YY,Sutter VL,Finegold SM

    更新日期:1974-06-01 00:00:00

  • Moxalactam (LY127935), a new semisynthetic 1-oxa-beta-lactam antibiotic with remarkable antimicrobial activity: in vitro comparison with cefamandole and tobramycin.

    abstract::Moxalactam (LY127935) exhibited greater in vitro activity than cefamandole and tobramycin against clinical isolates of Enterobacteriaceae, Aeromonas hydrophila, and Pseudomonas maltophilia. The activities of the three drugs against other microorganisms were as follows: for staphylococci, cefamandole = tobramycin great...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.17.4.750

    authors: Jones RN,Fuchs PC,Sommers HM,Gavan TL,Barry AL,Gerlach EH

    更新日期:1980-04-01 00:00:00

  • Comparative activities of the oxa-beta-lactam LY127935, cefotaxime, cefoperazone, cefamandole, and ticarcillin against multiply resistant gram-negative bacilli.

    abstract::A total of 91 multiply resistant bacterial strains, including Klebsiella pneumoniae (32 strains), Pseudomonas aeruginosa (16 strains), and Serratia marcescens (43 strains), were collected during hospital epidemics of nosocomial infection from 1975 to 1979. These strains were resistant to gentamicin, tobramycin, cephal...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.17.2.273

    authors: Hall WH,Opfer BJ,Gerding DN

    更新日期:1980-02-01 00:00:00

  • Functional linkage between genes that regulate osmotic stress responses and multidrug resistance transporters: challenges and opportunities for antibiotic discovery.

    abstract::All cells need to protect themselves against the osmotic challenges of their environment by maintaining low permeability to ions across their cell membranes. This is a basic principle of cellular function, which is reflected in the interactions among ion transport and drug efflux genes that have arisen during cellular...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,评审

    doi:10.1128/AAC.02095-13

    authors: Cohen BE

    更新日期:2014-01-01 00:00:00

  • Effect of bleomycin on deoxyribonucleic acid synthesis in toluene-treated Escherichia coli cells.

    abstract::The antibiotic bleomycin stimulates deoxyribonucleic acid (DNA) synthesis in toluene-treated Escherichia coli cells. The increase in synthesis is linear with bleomycin concentration. Bleomycin-stimulated DNA synthesis is independent of replication and dependent on DNA polymerase I. Replication is spared as the DNA pol...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.9.2.239

    authors: Ross SL,Moses RE

    更新日期:1976-02-01 00:00:00

  • Toward the development of a virus-cell-based assay for the discovery of novel compounds against human immunodeficiency virus type 1.

    abstract::The emergence of human immunodeficiency virus type 1 (HIV-1) strains resistant to highly active antiretroviral therapy necessitates continued drug discovery for the treatment of HIV-1 infection. Most current drug discovery strategies focus upon a single aspect of HIV-1 replication. A virus-cell-based assay, which can ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.2.501-508.2003

    authors: Adelson ME,Pacchia AL,Kaul M,Rando RF,Ron Y,Peltz SW,Dougherty JP

    更新日期:2003-02-01 00:00:00

  • In vitro activity of fluorescent dyes against asexual blood stages of Plasmodium falciparum.

    abstract::Many successful antimicrobial drugs originate from synthetic dyes. This paper reports the in vitro activity of 14 fluorescent dyes against Plasmodium falciparum. Five of these dyes (Hoechst 33342, MitoRed, DiOC(6), SYTO 9, and rhodamine B) show activity at a low nanomolar concentration against two P. falciparum strain...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00709-12

    authors: Joanny F,Held J,Mordmüller B

    更新日期:2012-11-01 00:00:00

  • Retrograde Trafficking Inhibitor of Shiga Toxins Reduces Morbidity and Mortality of Mice Infected with Enterohemorrhagic Escherichia coli.

    abstract::The most deadly outbreak of Escherichia coli O104:H4 occurred in Europe in 2011. Here, we evaluated the effects of the retrograde trafficking inhibitor Retro-2(cycl) in a murine model of E. coli O104:H4 infection. Systemic treatment with Retro-2(cycl) significantly reduced body weight loss and improved clinical scores...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00455-15

    authors: Secher T,Shima A,Hinsinger K,Cintrat JC,Johannes L,Barbier J,Gillet D,Oswald E

    更新日期:2015-08-01 00:00:00

  • In vitro antiviral activity and single-dose pharmacokinetics in humans of a novel, orally bioavailable inhibitor of human rhinovirus 3C protease.

    abstract::(E)-(S)-4-((S)-2-{3-[(5-methyl-isoxazole-3-carbonyl)-amino]-2-oxo-2H-pyridin-1-yl}-pent-4-ynoylamino)-5-((S)-2-oxo-pyrrolidin-3-yl)-pent-2-enoic acid ethyl ester (Compound 1) is a novel, irreversible inhibitor of human rhinovirus (HRV) 3C protease {inactivation rate constant (Kobs/[I]) of 223,000 M-1s-1}. In cell-base...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 临床试验,杂志文章

    doi:10.1128/AAC.49.6.2267-2275.2005

    authors: Patick AK,Brothers MA,Maldonado F,Binford S,Maldonado O,Fuhrman S,Petersen A,Smith GJ 3rd,Zalman LS,Burns-Naas LA,Tran JQ

    更新日期:2005-06-01 00:00:00

  • CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.

    abstract::Two neuraminidase (NA) inhibitors, zanamivir (Relenza) and oseltamivir phosphate (Tamiflu), have been licensed for the treatment of and prophylaxis against influenza. In this paper, the new potent NA inhibitor R-125489 is reported for the first time. R-125489 inhibited the NA activities of various type A and B influen...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00333-08

    authors: Yamashita M,Tomozawa T,Kakuta M,Tokumitsu A,Nasu H,Kubo S

    更新日期:2009-01-01 00:00:00

  • Resistance caused by decreased penetration of beta-lactam antibiotics into Enterobacter cloacae.

    abstract::Strains of Enterobacter cloacae were selected on the basis of resistance to aztreonam, ceftazidime, moxalactam, or imipenem. All strains produced the same E2 beta-lactamase, with an isoelectric point greater than 9.5 and with high hydrolytic activity in the presence of cephaloridine. Resistance to beta-lactams could n...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.27.4.555

    authors: Bush K,Tanaka SK,Bonner DP,Sykes RB

    更新日期:1985-04-01 00:00:00

  • Azlocillin and mezlocillin: new ureido penicillins.

    abstract::The activity of azlocillin and mezlocillin, new semisynthetic ureido penicillins, was investigated and compared with that of other known beta-lactam antibiotics. At a concentration of 25 mug/ml, azlocillin inhibited 74% of Enterobacter, 97% of Proteus mirabilis, 64% of Citrobacter, 91% of Pseudomonas aeruginosa, and 8...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.13.6.930

    authors: Fu KP,Neu HC

    更新日期:1978-06-01 00:00:00

  • Role of extracellular iron in the action of the quinone antibiotic streptonigrin: mechanisms of killing and resistance of Neisseria gonorrhoeae.

    abstract::The quinone antibiotic streptonigrin is believed to kill bacteria by promoting formation of oxygen radicals. This antibiotic has also been used to select resistant bacterial mutants, some of which vary in iron utilization. We examined the effects of streptonigrin on Neisseria gonorrhoeae and several types of gonococca...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.31.10.1507

    authors: Cohen MS,Chai Y,Britigan BE,McKenna W,Adams J,Svendsen T,Bean K,Hassett DJ,Sparling PF

    更新日期:1987-10-01 00:00:00

  • 4,4'-isopropylidine-bis(2-isopropyl)phenol, a new inhibitor for cell wall formation of Bacillus subtilis.

    abstract::4,4'-Isopropylidine-bis[2-isopropyl]phenol was found to possess antimicrobial activity against gram-positive bacteria and some fungi, whereas it had no effect on gram-negative organisms. The drug has a potent inhibitory action on the synthesis of cell wall mucopeptides of Bacillus subtilis by inhibiting the enzyme d-g...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.9.4.580

    authors: Shimi IR,Shoukry S,Zaki Z

    更新日期:1976-04-01 00:00:00

  • In vivo acquisition of ceftriaxone resistance in Salmonella enterica serotype anatum.

    abstract::The emergence of resistance to antimicrobial agents within the salmonellas is a worldwide and severe problem. A case of treatment failure due to the emergence of resistance to ceftriaxone in Salmonella enterica serotype Anatum was studied. S. enterica serotype Anatum and Escherichia coli, both of which are susceptible...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.2.563-567.2003

    authors: Su LH,Chiu CH,Chu C,Wang MH,Chia JH,Wu TL

    更新日期:2003-02-01 00:00:00

  • Targeting antibacterial agents by using drug-carrying filamentous bacteriophages.

    abstract::Bacteriophages have been used for more than a century for (unconventional) therapy of bacterial infections, for half a century as tools in genetic research, for 2 decades as tools for discovery of specific target-binding proteins, and for nearly a decade as tools for vaccination or as gene delivery vehicles. Here we p...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00169-06

    authors: Yacoby I,Shamis M,Bar H,Shabat D,Benhar I

    更新日期:2006-06-01 00:00:00

  • In vitro comparison of ampicillin-chloramphenicol and ampicillin-cefotaxime against 284 Haemophilus isolates.

    abstract::Since November 1982 at the Sainte-Justine Hospital in Montreal, ampicillin and cefotaxime were used in association as initial treatment (greater than or equal to 48 h) for childhood bacterial meningitis. In this report is described the in vitro interaction of the new regimen in comparison with that of the previous amp...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.29.4.594

    authors: Lapointe JR,Lavallée C,Michaud A,Chicoine L,Joncas JH

    更新日期:1986-04-01 00:00:00

  • In vitro antimicrobial activity of ceftizoxime against glucose-nonfermentative gram-negative rods.

    abstract::Ceftizoxime, a new cephalosporin, was active against Pseudomonas cepacia, Flavobacterium meningosepticum, Alcaligenes faecalis, and Acinetobacter calcoaceticus and was more potent against Pseudomonas aeruginosa and Pseudomonas putida than was carbenicillin. ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.20.1.136

    authors: Yabuuchi E,Ito T,Tanimura E,Yamamoto N,Ohyama A

    更新日期:1981-07-01 00:00:00

  • Correlation of In Vitro Susceptibility Based on MICs and Squalene Epoxidase Mutations with Clinical Response to Terbinafine in Patients with Tinea Corporis/Cruris.

    abstract::Recalcitrant dermatophytoses are on the rise in India. High MICs of terbinafine (TRB) and squalene epoxidase (SQLE) gene mutations conferring resistance in Trichophyton spp. have been recently documented. However, studies correlating laboratory data with clinical response to TRB in tinea corporis/cruris are lacking. F...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 临床试验,杂志文章

    doi:10.1128/AAC.01038-18

    authors: Khurana A,Masih A,Chowdhary A,Sardana K,Borker S,Gupta A,Gautam RK,Sharma PK,Jain D

    更新日期:2018-11-26 00:00:00