Regulation of heme polymerizing activity and the antimalarial action of chloroquine.

Abstract:

:Mice infected with Plasmodium berghei served as donors of erythrocytes with a high level of parasitemia for the study of ferriprotoporphyrin IX (FP) polymerization. Six hours after treatment of these mice with 3 micromol of chloroquine per 25 g of body weight, there were significant losses of heme polymerase I (HPA I). For chloroquine-susceptible (CS) P. berghei, the rate of FP polymerization decreased from 541 +/- 42 (mean +/- standard deviation; n = 12) to 51 +/- 19 (n = 8) nmol of FP polymerized per h per ml of packed erythrocytes (normalized to represent 1,000 parasites per 1,000 erythrocytes). For chloroquine-resistant (CR) P. berghei, the rate decreased from 284 +/- 19 (n = 16) to 124 +/- 11 (n = 6) nmol per h per ml. The chloroquine-induced loss of HPA I was accompanied by the accumulation of unpolymerized FP in CS P. berghei but not in CR P. berghei, which is consistent with the hypothesis that FP mediates the antimalarial action of chloroquine. Quinine treatment partially reversed the effects of chloroquine in CS P. berghei but not in CR P. berghei. Cycloheximide treatment antagonized the effects of chloroquine in both lines of parasites. To explain these findings, we propose that chloroquine, quinine, and cycloheximide perturb a regulatory process for HPA I. Furthermore, we propose that when chloroquine engages its target in the regulatory process, it initiates a chain of events which culminates in increased production, accessibility, or reactivity of a regulator (inactivator) of HPA I.

authors

Fitch CD,Chou AC

doi

10.1128/AAC.41.11.2461

subject

Has Abstract

pub_date

1997-11-01 00:00:00

pages

2461-5

issue

11

eissn

0066-4804

issn

1098-6596

journal_volume

41

pub_type

杂志文章
  • Penetration of oral fluconazole into gynecological tissues.

    abstract::Penetration of fluconazole into female genital tissues was examined. Fluconazole was administered orally at a dose of 150 mg to patients undergoing total abdominal hysterectomy 1 to 151 h prior to surgery. During surgery, blood, uterus, ovary, and oviduct were sampled. Fluconazole concentrations in each tissue were de...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 临床试验,杂志文章

    doi:10.1128/AAC.43.1.148

    authors: Mikamo H,Kawazoe K,Sato Y,Izumi K,Ito T,Ito K,Tamaya T

    更新日期:1999-01-01 00:00:00

  • Safety and bactericidal activity of rifalazil in patients with pulmonary tuberculosis.

    abstract::Rifalazil, also known as KRM-1648 or benzoxazinorifamycin, is a new semisynthetic rifamycin with a long half-life of approximately 60 h. Rifalazil has potent bactericidal activity against Mycobacterium tuberculosis in vitro and in animal models of tuberculosis (TB). Prior studies in healthy volunteers showed that once...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1128/AAC.45.7.1972-1976.2001

    authors: Dietze R,Teixeira L,Rocha LM,Palaci M,Johnson JL,Wells C,Rose L,Eisenach K,Ellner JJ

    更新日期:2001-07-01 00:00:00

  • Telithromycin- and fluoroquinolone-resistant Streptococcus pneumoniae in Taiwan with high prevalence of resistance to macrolides and beta-lactams: SMART program 2001 data.

    abstract::There is a high prevalence of beta-lactam- and macrolide-resistant Streptococcus pneumoniae in Taiwan. To understand the in vitro susceptibilities of recent isolates of S. pneumoniae to fluoroquinolones and telithromycin (which is not available in Taiwan), the MICs of 23 antimicrobial agents for 936 clinical isolates ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,多中心研究

    doi:10.1128/aac.47.7.2145-2151.2003

    authors: Hsueh PR,Teng LJ,Wu TL,Yang D,Huang WK,Shyr JM,Chuang YC,Wan JH,Yan JJ,Lu JJ,Wu JJ,Ko WC,Chang FY,Yang YC,Lau YJ,Liu YC,Lee CM,Leu HS,Liu CY,Luh KT,SMART Program 2001 Data.

    更新日期:2003-07-01 00:00:00

  • Phenotypic tolerance: antibiotic enrichment of noninherited resistance in bacterial populations.

    abstract::When growing bacteria are exposed to bactericidal concentrations of antibiotics, the sensitivity of the bacteria to the antibiotic commonly decreases with time, and substantial fractions of the bacteria survive. Using Escherichia coli CAB1 and antibiotics of five different classes (ampicillin, ciprofloxacin, rifampin,...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.49.4.1483-1494.2005

    authors: Wiuff C,Zappala RM,Regoes RR,Garner KN,Baquero F,Levin BR

    更新日期:2005-04-01 00:00:00

  • Outer membrane permeability barrier in Escherichia coli mutants that are defective in the late acyltransferases of lipid A biosynthesis.

    abstract::The tight packing of six fatty acids in the lipid A constituent of lipopolysaccharide (LPS) has been proposed to contribute to the unusually low permeability of the outer membrane of gram-negative enteric bacteria to hydrophobic antibiotics. Here it is shown that the Escherichia coli msbB mutant, which elaborates defe...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.43.6.1459

    authors: Vaara M,Nurminen M

    更新日期:1999-06-01 00:00:00

  • Comparative efficacy of trovafloxacin in experimental endocarditis caused by ciprofloxacin-sensitive, methicillin-resistant Staphylococcus aureus.

    abstract::The new fluoroquinolone trovafloxacin was tested against a ciprofloxacin-sensitive, methicillin-resistant Staphylococcus aureus strain in the rabbit model of endocarditis. Trovafloxacin was more effective than vancomycin (CFU/g of vegetation, 2.65 +/- 1.87 versus 4.54 +/- 2.80 [mean +/- standard deviation]; P < 0.05) ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.42.12.3325

    authors: Kim YS,Liu Q,Chow LL,Chambers HF,Täuber MG

    更新日期:1998-12-01 00:00:00

  • Pharmacokinetics-pharmacodynamics of a respiratory syncytial virus fusion inhibitor in the cotton rat model.

    abstract::Human respiratory syncytial virus (RSV) is a major cause of lower respiratory tract infections in infants, young children, elderly persons, and severely immunocompromised patients. Effective postinfection treatments are not widely available, and currently there is no approved vaccine. TMC353121 is a potent RSV fusion ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00643-10

    authors: Rouan MC,Gevers T,Roymans D,de Zwart L,Nauwelaers D,De Meulder M,van Remoortere P,Vanstockem M,Koul A,Simmen K,Andries K

    更新日期:2010-11-01 00:00:00

  • Efficacy of LFF571 in a hamster model of Clostridium difficile infection.

    abstract::LFF571 is a novel semisynthetic thiopeptide antibiotic with potent activity against a variety of Gram-positive pathogens, including Clostridium difficile. In vivo efficacy of LFF571 was compared to vancomycin in a hamster model of C. difficile infection (CDI). Infection was induced in Golden Syrian hamsters using a to...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.06355-11

    authors: Trzasko A,Leeds JA,Praestgaard J,Lamarche MJ,McKenney D

    更新日期:2012-08-01 00:00:00

  • Susceptibility of Haemophilus influenzae type b to ampicillin-sulbactam.

    abstract::Seventy-five strains of Haemophilus influenzae type b, including 45 beta-lactamase-positive strains, were tested by MIC and time kill studies for susceptibility to ampicillin-sulbactam at various ratios. beta-Lactamase-negative strains were inhibited by lower concentrations of ampicillin-sulbactam than beta-lactamase-...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.33.9.1620

    authors: Azimi PH,Dunphy MG

    更新日期:1989-09-01 00:00:00

  • Liposomal amphotericin B inhibits in vitro T-lymphocyte response to antigen.

    abstract::The effects of free amphotericin B (as Fungizone) and amphotericin B (AMB) incorporated into liposomes on the proliferation of lymphocytes were determined. Freshly obtained guinea pig and rat antigen-specific lymphocytes were compared with rat T-lymphocyte cell lines cultured for a long period of time. Incorporation o...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.35.5.879

    authors: Boggs JM,Chang NH,Goundalkar A

    更新日期:1991-05-01 00:00:00

  • Alterations of penicillin-binding proteins 1A, 2X, and 2B in Streptococcus pneumoniae isolates for which amoxicillin MICs are higher than penicillin MICs.

    abstract::Penicillin-binding proteins (PBPs) of 15 selected penicillin- and amoxicillin-resistant Streptococcus pneumoniae isolates (MICs of 2 to 8 and 8 to 16 microg/ml, respectively) were studied. In addition to typical changes in PBPs 1A and 2X, these strains had 10 unique changes in PBP 2B, including a (618)A-G substitution...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.48.10.4020-4022.2004

    authors: Kosowska K,Jacobs MR,Bajaksouzian S,Koeth L,Appelbaum PC

    更新日期:2004-10-01 00:00:00

  • Antimicrobial Treatment Provides a Competitive Advantage to Mycobacterium abscessus in a Dual-Species Biofilm with Pseudomonas aeruginosa.

    abstract::The physiological factors that contribute to Mycobacterium abscessus lung infections remain unclear. We determined whether antibiotic treatment targeting a major cystic fibrosis pathogen (i.e., Pseudomonas aeruginosa) could provide the ideal conditions for the establishment of M. abscessus infection. Our data showed t...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01547-19

    authors: Rodríguez-Sevilla G,Crabbé A,García-Coca M,Aguilera-Correa JJ,Esteban J,Pérez-Jorge C

    更新日期:2019-10-22 00:00:00

  • Mechanism-of-Action Classification of Antibiotics by Global Transcriptome Profiling.

    abstract::Antimicrobial resistance (AMR) is an ever-growing public health problem worldwide. The low rate of antibiotic discovery coupled with the rapid spread of drug-resistant bacterial pathogens is causing a global health crisis. To facilitate the drug discovery processes, we present a large-scale study of reference antibiot...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01207-19

    authors: O'Rourke A,Beyhan S,Choi Y,Morales P,Chan AP,Espinoza JL,Dupont CL,Meyer KJ,Spoering A,Lewis K,Nierman WC,Nelson KE

    更新日期:2020-02-21 00:00:00

  • Moxalactam in the therapy of serious infections.

    abstract::Sixty-seven patients were treated with moxalactam in a noncomparative trial of hospitalized patients; 32 had endometritis or chorioamnionitis, 12 had skin and soft tissue infections, 5 had osteomyelitis, 5 had pneumonia, 5 had urinary tract infections, 4 had arthritis, 2 had sepsis from an unknown source, 1 had endoca...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.21.4.650

    authors: Marier RL,Faro S,Sanders CV,Williams W,Derks F,Janney A,Aldridge K

    更新日期:1982-04-01 00:00:00

  • Clarithromycin Resistance Mechanisms of Epidemic β-Lactamase-Nonproducing Ampicillin-Resistant Haemophilus influenzae Strains in Japan.

    abstract::The aim of this study was to clarify the clarithromycin resistance mechanisms of β-lactamase-nonproducing ampicillin-resistant Haemophilus influenzae strains. In all clarithromycin-resistant strains, the transcript level of acrB was significantly elevated, and these strains had a frameshift mutation in acrR Introducti...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00163-16

    authors: Seyama S,Wajima T,Nakaminami H,Noguchi N

    更新日期:2016-04-22 00:00:00

  • Therapy of genital herpes with topically applied interferon.

    abstract::Ninety-four patients with recurrences of genital herpes were randomized in a double-blind trial to receive topical therapy for 5 days with either alpha-2a interferon at 30 X 10(6) IU/ml or 10 X 10(6) IU/ml or placebo six times daily. No differences were noted between either interferon dose and placebo with respect to ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1128/aac.31.7.1137

    authors: Eron LJ,Toy C,Salsitz B,Scheer RR,Wood DL,Nadler PI

    更新日期:1987-07-01 00:00:00

  • Combination antimicrobial susceptibility testing of multidrug-resistant Stenotrophomonas maltophilia from cystic fibrosis patients.

    abstract::Stenotrophomonas maltophilia is increasingly being isolated from the respiratory tract of individuals with cystic fibrosis, and, because of its multidrug-resistant nature, the selection of suitable treatment regimens can be problematical. Etest methodology was used to facilitate MIC and antimicrobial combination testi...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00072-12

    authors: Milne KE,Gould IM

    更新日期:2012-08-01 00:00:00

  • Microbiological aetiology, epidemiology, and clinical profile of prosthetic joint infections: are current antibiotic prophylaxis guidelines effective?

    abstract::Prosthetic joint infections remain a major complication of arthroplasty. At present, local and international guidelines recommend cefazolin as a surgical antibiotic prophylaxis at the time of arthroplasty. This retrospective cohort study conducted across 10 hospitals over a 3-year period (January 2006 to December 2008...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,多中心研究

    doi:10.1128/AAC.06246-11

    authors: Peel TN,Cheng AC,Buising KL,Choong PF

    更新日期:2012-05-01 00:00:00

  • Quantitative correlation between susceptibility and OprJ production in NfxB mutants of Pseudomonas aeruginosa.

    abstract::Various Pseudomonas aeruginosa PAO1 NfxB mutants were isolated on agar plates containing cefpirome and ofloxacin. They were classified into type A and type B, based on the degrees of changes in their susceptibilities. Type A mutants were four to eight times more resistant to ofloxacin, erythromycin, and new zwitterion...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.40.4.909

    authors: Masuda N,Gotoh N,Ohya S,Nishino T

    更新日期:1996-04-01 00:00:00

  • Bioluminescence for assessing drug potency against nonreplicating Mycobacterium tuberculosis.

    abstract::Targeting dormant Mycobacterium tuberculosis represents a challenge to antituberculosis drug discovery programs. We previously reported and validated the use of the streptomycin (STR)-dependent M. tuberculosis 18b strain as a tool for assessing drug potency against nonreplicating bacteria both in vitro and in vivo. In...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00528-15

    authors: Vocat A,Hartkoorn RC,Lechartier B,Zhang M,Dhar N,Cole ST,Sala C

    更新日期:2015-07-01 00:00:00

  • Comparative in vitro antimicrobial activity of carumonam, a new monocyclic beta-lactam.

    abstract::The antimicrobial activity of carumonam (formerly RO-17-2301), a monocyclic beta-lactam antibiotic, was compared with those of aztreonam, cefotaxime, cefoperazone, ceftazidime, piperacillin, and gentamicin against 455 bacterial isolates. Carumonam did not possess activity against gram-positive cocci and was generally ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.29.2.346

    authors: Smith BR,LeFrock JL,McCloskey RV,Donato JB,Weber SJ,Joseph WS

    更新日期:1986-02-01 00:00:00

  • Antibacterial action of structurally diverse cationic peptides on gram-positive bacteria.

    abstract::Antimicrobial cationic peptides are ubiquitous in nature and are thought to be a component of the first line of defense against infectious agents. It is widely believed that the killing mechanism of these peptides on bacteria involves an interaction with the cytoplasmic membrane. Cationic peptides from different struc...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.44.8.2086-2092.2000

    authors: Friedrich CL,Moyles D,Beveridge TJ,Hancock RE

    更新日期:2000-08-01 00:00:00

  • Interpretive criteria for cefamandole and cephalothin disk diffusion susceptibility tests.

    abstract::A multi-center study of 1,838 clinical isolates established the accuracy of diffusion susceptibility tests with 30-mug cephalothin disks and 30-mug cefamandole disks. The same interpretive zone standards can be applied to tests with either disk but the two drugs cannot be tested interchangeably. ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.15.1.140

    authors: Barry AL,Schoenknecht FD,Shadomy S,Sherris JC,Thornsberry C,Washington JA,Kammer RB

    更新日期:1979-01-01 00:00:00

  • Effect of oral administration of emtricitabine on woodchuck hepatitis virus replication in chronically infected woodchucks.

    abstract::Emtricitabine [(-)FTC] [(-)-beta-2', 3'-dideoxy-5-fluoro-3'-thiacytidine] has been shown to be an effective inhibitor of hepatitis B virus (HBV) in cell culture, with a potency and selectivity that are essentially identical to those of lamivudine. The antiviral activity of oral administration of (-)FTC against WHV rep...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.44.6.1757-1760.2000

    authors: Korba BE,Schinazi RF,Cote P,Tennant BC,Gerin JL

    更新日期:2000-06-01 00:00:00

  • A propensity score analysis shows that empirical treatment with linezolid does not increase the thirty-day mortality rate in patients with Gram-negative bacteremia.

    abstract::The role of linezolid in empirical therapy of suspected bacteremia remains unclear. The aim of this study was to evaluate the influence of empirical use of linezolid or glycopeptides in addition to other antibiotics on the 30-day mortality rates in patients with Gram-negative bacteremia. For this purpose, 1,126 patien...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.03796-14

    authors: Ternavasio-de la Vega HG,Mateos-Díaz AM,Martinez JA,Almela M,Cobos-Trigueros N,Morata L,De-la-Calle C,Sala M,Mensa J,Marcos M,Soriano A

    更新日期:2014-12-01 00:00:00

  • Pharmacokinetics, pharmacodynamics, and tolerability of GS-9851, a nucleotide analog polymerase inhibitor, following multiple ascending doses in patients with chronic hepatitis C infection.

    abstract::We conducted this double-blind, parallel-group, placebo-controlled, randomized, multiple-ascending-dose study to assess the safety, tolerability, pharmacokinetics, and pharmacodynamics of GS-9851 (formerly PSI-7851) in treatment-naïve patients infected with hepatitis C virus (HCV) genotype 1. Thirty-two patients recei...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,随机对照试验

    doi:10.1128/AAC.01263-12

    authors: Lawitz E,Rodriguez-Torres M,Denning JM,Albanis E,Cornpropst M,Berrey MM,Symonds WT

    更新日期:2013-03-01 00:00:00

  • Pharmacokinetics and pharmacodynamics of granulocyte-macrophage colony-stimulating factor and zidovudine in patients with AIDS and severe AIDS-related complex.

    abstract::Granulocytopenia is a complication of human immunodeficiency virus disease, as well as a toxic manifestation of zidovudine therapy. To evaluate pharmacokinetic and pharmacodynamic relationships, 11 AIDS-AIDS-related complex patients who had developed zidovudine-associated granulocytopenia (mean absolute neutrophil cou...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.37.3.512

    authors: Hewitt RG,Morse GD,Lawrence WD,Maliszewski ML,Santora J,Bartos L,Bonnem E,Poiesz B

    更新日期:1993-03-01 00:00:00

  • Penetration of cefotaxime into respiratory secretions.

    abstract::The objective of this study was to quantitate cefotaxime and its active metabolite, desacetyl cefotaxime, in the distal airways and to compare these levels to concentrations in plasma. Respiratory secretions were obtained from the subsegmental level in 17 adult patients undergoing fiber-optic bronchoscopy within 2 h a...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.31.5.815

    authors: Fick RB Jr,Alexander MR,Prince RA,Kasik JE

    更新日期:1987-05-01 00:00:00

  • Comparison of ofloxacin and ceftriaxone for short-course treatment of enteric fever.

    abstract::An open, randomized comparison of ofloxacin (200 mg, every 12 h) given orally for 5 days and ceftriaxone (3 g, once daily) given intravenously for 3 days in the treatment of uncomplicated enteric fever was conducted in Ho Chi Minh City, Vietnam. Salmonella paratyphi type A was isolated from six patients. Salmonella ty...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1128/aac.38.8.1716

    authors: Smith MD,Duong NM,Hoa NT,Wain J,Ha HD,Diep TS,Day NP,Hien TT,White NJ

    更新日期:1994-08-01 00:00:00

  • Surveillance for antimicrobial susceptibility among clinical isolates of Pseudomonas aeruginosa and Acinetobacter baumannii from hospitalized patients in the United States, 1998 to 2001.

    abstract::Pseudomonas aeruginosa and Acinetobacter baumannii are the most prevalent nonfermentative bacterial species isolated from clinical specimens of hospitalized patients. A surveillance study of 65 laboratories in the United States from 1998 to 2001 found >90% of isolates of P. aeruginosa from hospitalized patients to be ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.5.1681-1688.2003

    authors: Karlowsky JA,Draghi DC,Jones ME,Thornsberry C,Friedland IR,Sahm DF

    更新日期:2003-05-01 00:00:00