Antimicrobial properties of 8-hydroxyserrulat-14-en-19-oic acid for treatment of implant-associated infections.

Abstract:

:Treatment options are limited for implant-associated infections (IAI) that are mainly caused by biofilm-forming staphylococci. We report here on the activity of the serrulatane compound 8-hydroxyserrulat-14-en-19-oic acid (EN4), a diterpene isolated from the Australian plant Eremophila neglecta. EN4 elicited antimicrobial activity toward various Gram-positive bacteria but not to Gram-negative bacteria. It showed a similar bactericidal effect against logarithmic-phase, stationary-phase, and adherent Staphylococcus epidermidis, as well as against methicillin-susceptible and methicillin-resistant S. aureus with MICs of 25 to 50 μg/ml and MBCs of 50 to 100 μg/ml. The bactericidal activity of EN4 was similar against S. epidermidis and its Δica mutant, which is unable to produce polysaccharide intercellular adhesin-mediated biofilm. In time-kill studies, EN4 exhibited a rapid and concentration-dependent killing of staphylococci, reducing bacterial counts by >3 log(10) CFU/ml within 5 min at concentrations of >50 μg/ml. Investigation of the mode of action of EN4 revealed membranolytic properties and a general inhibition of macromolecular biosynthesis, suggesting a multitarget activity. In vitro-tested cytotoxicity on eukaryotic cells was time and concentration dependent in the range of the MBCs. EN4 was then tested in a mouse tissue cage model, where it showed neither bactericidal nor cytotoxic effects, indicating an inhibition of its activity. Inhibition assays revealed that this was caused by interactions with albumin. Overall, these findings suggest that, upon structural changes, EN4 might be a promising pharmacophore for the development of new antimicrobials to treat IAI.

authors

Nowakowska J,Griesser HJ,Textor M,Landmann R,Khanna N

doi

10.1128/AAC.01735-12

subject

Has Abstract

pub_date

2013-01-01 00:00:00

pages

333-42

issue

1

eissn

0066-4804

issn

1098-6596

pii

AAC.01735-12

journal_volume

57

pub_type

杂志文章
  • Isolation of trimethoprim-resistant, sulfonamide-susceptible Enterobacteriaceae from urinary tract infections.

    abstract::The isolation of trimethoprim-resistant, sulfonamide-susceptible Enterobacteriaceae causing urinary tract infections is reported. The appearance of these strains followed the introduction of trimethoprim alone for use as treatment. Trimethoprim resistance was attributable to plasmids or transposons less frequently in ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.23.4.617

    authors: Towner KJ,Smith MA,Cowlishaw WA

    更新日期:1983-04-01 00:00:00

  • Treatment of experimental Haemophilus influenzae type b meningitis with 1-oxa-beta-lactam (LY127935).

    abstract::1-Oxa-beta-lactam (LY127935) (Shionogi 6059-S) is a new type beta-lactam antibiotic having a broad spectrum of antibacterial activity. It is highly active against ampicillin-resistant strains of Haemophilus influenzae exhibiting minimal inhibitory concentrations as low as 0.06 microgram/ml. This compound also has the ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.17.2.258

    authors: Cordera CS,Pekarek RS

    更新日期:1980-02-01 00:00:00

  • Pharmacokinetics of (-)-beta-D-2-aminopurine dioxolane and (-)-beta-D-2-amino-6-chloropurine dioxolane and their antiviral metabolite (-)-beta-D-dioxolane guanine in rhesus monkeys.

    abstract::(-)-beta-D-2-Aminopurine dioxolane (APD) and (-)-beta-D-2-amino-6-chloropurine dioxolane (ACPD) are recently synthesized dioxolanylpurine nucleoside derivatives being developed as potential prodrugs for the antiviral nucleoside analog (-)-beta-D-dioxolane guanine (DXG). In vitro, APD and ACPD are converted to DXG by x...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.40.10.2332

    authors: Chen H,Boudinot FD,Chu CK,Mcclure HM,Schinazi RF

    更新日期:1996-10-01 00:00:00

  • Transduction of methicillin resistance in Staphylococcus aureus: recipient effectiveness and beta-lactamase production.

    abstract::The effectiveness of Staphylococcus aureus strain 8325-4 as a recipient for the transduction of methicillin resistance requires the presence of a penicillinase plasmid but was found to be independent of the lysogenic state of the recipient. Effectiveness is conferred by the plasmid in either the autonomous or integrat...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.18.3.424

    authors: Stewart GC,Rosenblum ED

    更新日期:1980-09-01 00:00:00

  • Effect of mannitol infusions into the internal carotid artery on entry of two antibiotics into the cerebrospinal fluid and brains of normal rabbits.

    abstract::The rapid infusion of hyperosmolar solutions into the internal carotid artery transiently disrupts the integrity of the blood-brain barrier, permitting entry of substances normally excluded from the nervous system. This study examined the effect of such an infusion on the penetration of vancomycin and tobramycin into ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.24.3.339

    authors: Perkins BA,Strausbaugh LJ

    更新日期:1983-09-01 00:00:00

  • Comparative activity of ciprofloxacin, ofloxacin, sparfloxacin, temafloxacin, CI-960, CI-990, and WIN 57273 against anaerobic bacteria.

    abstract::The in vitro activities of seven fluoroquinolones against 290 anaerobes were determined by agar dilution. CI-960 and WIN 57273 inhibited greater than 95% of the strains at less than or equal to 2 micrograms/ml. CI-990 required less than or equal to 16 micrograms/ml. Clustering around 2 to 4 micrograms/ml was noted for...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.36.5.1158

    authors: Goldstein EJ,Citron DM

    更新日期:1992-05-01 00:00:00

  • Novel OXA-10-derived extended-spectrum beta-lactamases selected in vivo or in vitro.

    abstract::A clinical isolate of Pseudomonas aeruginosa, PAe191, was found to be highly resistant to all anti-Pseudomonas beta-lactam antibiotics (except imipenem) and resistant also to aminoglycosides. It produced a beta-lactamase (with an apparent pI of 7.6) which was not inhibited by clavulanic acid. Cloning and characterizat...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.42.12.3113

    authors: Mugnier P,Casin I,Bouthors AT,Collatz E

    更新日期:1998-12-01 00:00:00

  • E1210, a new broad-spectrum antifungal, suppresses Candida albicans hyphal growth through inhibition of glycosylphosphatidylinositol biosynthesis.

    abstract::Continued research toward the development of new antifungals that act via inhibition of glycosylphosphatidylinositol (GPI) biosynthesis led to the design of E1210. In this study, we assessed the selectivity of the inhibitory activity of E1210 against Candida albicans GWT1 (Orf19.6884) protein, Aspergillus fumigatus GW...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00731-11

    authors: Watanabe NA,Miyazaki M,Horii T,Sagane K,Tsukahara K,Hata K

    更新日期:2012-02-01 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

  • Attenuation of colistin bactericidal activity by high inoculum of Pseudomonas aeruginosa characterized by a new mechanism-based population pharmacodynamic model.

    abstract::Colistin is increasingly being utilized against Gram-negative pathogens, including Pseudomonas aeruginosa, resistant to all other antibiotics. Since limited data exist regarding killing by colistin at different initial inocula (CFUo), we evaluated killing of Pseudomonas aeruginosa by colistin at several CFUo and devel...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00881-09

    authors: Bulitta JB,Yang JC,Yohonn L,Ly NS,Brown SV,D'Hondt RE,Jusko WJ,Forrest A,Tsuji BT

    更新日期:2010-05-01 00:00:00

  • Identification of chromosomal antibiotic resistance genes in Streptococcus anginosus ("S. milleri").

    abstract::Determinants encoding resistance to antibiotics, except penicillin, of 5 of 21 Streptococcus anginosus clinical isolates that we examined transferred by conjugation into Enterococcus faecalis and into 1 to 5 streptococcal recipients at frequencies of 10(-6) to 10(-8) transconjugants per donor. No R plasmids were detec...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.34.9.1685

    authors: Clermont D,Horaud T

    更新日期:1990-09-01 00:00:00

  • Intracellular efavirenz levels in peripheral blood mononuclear cells from human immunodeficiency virus-infected individuals.

    abstract::We describe a novel method for isolating plasma-free peripheral blood mononuclear cells retaining intracellular efavirenz. Quantification of efavirenz in 13 human immunodeficiency virus-infected patients by liquid chromatography-tandem mass spectrometry showed a higher correlation of intracellular levels with unbound ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01613-06

    authors: Tanaka R,Hanabusa H,Kinai E,Hasegawa N,Negishi M,Kato S

    更新日期:2008-02-01 00:00:00

  • Efficacy of alcohol-based hand rinses under frequent-use conditions.

    abstract::Fifty volunteers randomly assigned to one of five hand washing agents (10 subjects per agent)--a nonantiseptic liquid soap (control), an antiseptic hand rinse containing 60% isopropyl alcohol (IPA) with emollients (Alc A), an antiseptic hand rinse containing 70% IPA and 0.5% chlorhexidine gluconate with emollients (Al...

    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.30.4.542

    authors: Larson EL,Eke PI,Laughon BE

    更新日期:1986-10-01 00:00:00

  • In vitro and in vivo pharmacokinetics-pharmacodynamics of GV143253A, a novel trinem.

    abstract::The aim of the present study was to characterize the pharmacokinetic-pharmacodynamic relationship of GV143253A, a novel trinem anti-methicillin-resistant Staphylococcus aureus (MRSA) agent active against gram-positive cocci, including multidrug-resistant clinical isolates. An in vitro pharmacodynamic study with methic...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.2.770-776.2003

    authors: Ferrari L,Iavarone L,Braggio S,Di Modugno E

    更新日期:2003-02-01 00:00:00

  • Suppression of murine endotoxin response by E5531, a novel synthetic lipid A antagonist.

    abstract::As a consequence of blood-borne bacterial sepsis, endotoxin or lipopolysaccharide (LPS) from the cell walls of gram-negative bacteria can trigger an acute inflammatory response, leading to a series of pathological events and often resulting in death. To block this inflammatory response to endotoxin, a novel lipid A an...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.42.11.2824

    authors: Kobayashi S,Kawata T,Kimura A,Miyamoto K,Katayama K,Yamatsu I,Rossignol DP,Christ WJ,Kishi Y

    更新日期:1998-11-01 00:00:00

  • Resistance to linezolid in a porcine Clostridium perfringens strain carrying a mutation in the rplD gene encoding the ribosomal protein L4.

    abstract::Coresistance to human reserve antibiotics can be selected by antibiotics used in veterinary medicine. A Clostridium perfringens strain isolated from pig manure was resistant to the reserve drug linezolid and, simultaneously, resistant against florfenicol and erythromycin. We detected a new mutation in a highly conserv...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01208-09

    authors: Hölzel CS,Harms KS,Schwaiger K,Bauer J

    更新日期:2010-03-01 00:00:00

  • Microcin E492 is an unmodified peptide related in structure to colicin V.

    abstract::The pore-forming microcin E492 was purified by solid-phase extraction and reversed-phase high-pressure liquid chromatography. Its molecular mass was 7,886 Da. The entire 84-amino-acid sequence was determined. There is no postranslational modification in the secreted microcin, and the sequence has homologies with the s...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.46.1.229-230.2002

    authors: Pons AM,Zorn N,Vignon D,Delalande F,Van Dorsselaer A,Cottenceau G

    更新日期:2002-01-01 00:00:00

  • Comparison of amphotericin B and N-D-ornithyl amphotericin B methyl ester in experimental cryptococcal meningitis and Candida albicans endocarditis with pyelonephritis.

    abstract::Amphotericin B and N-D-ornithyl amphotericin B methyl ester were compared for therapeutic efficacies against experimentally induced cryptococcal meningitis and Candida albicans endocarditis with pyelonephritis in rabbits. Antifungal activity of the two polyenes in vitro was similar for the yeasts used in these experim...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.28.6.751

    authors: Perfect JR,Durack DT

    更新日期:1985-12-01 00:00:00

  • Crystal Structures of Penicillin-Binding Protein D2 from Listeria monocytogenes and Structural Basis for Antibiotic Specificity.

    abstract::β-Lactam antibiotics that inhibit penicillin-binding proteins (PBPs) have been widely used in the treatment of bacterial infections. However, the molecular basis underlying the different inhibitory potencies of β-lactams against specific PBPs is not fully understood. Here, we present the crystal structures of penicill...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00796-18

    authors: Jeong JH,Cha HJ,Kim YG

    更新日期:2018-08-27 00:00:00

  • Antimicrobial therapy of experimental group B streptococcal infection in mice.

    abstract::Group B beta-hemolytic streptococci (GB-BHS) frequently cause severe infection in newborns. Previous in vitro studies showed accelerated killing of GB-BHS by ampicillin plus gentamicin as compared with ampicillin alone. To extend the in vitro observations, mice were infected experimentally with GB-BHS and treated with...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.11.5.817

    authors: Deveikis A,Schauf V,Mizen M,Riff L

    更新日期:1977-05-01 00:00:00

  • In vitro synergism observed with azithromycin, clarithromycin, minocycline, or tigecycline in association with antifungal agents against Pythium insidiosum.

    abstract::We describe here the in vitro activities of azithromycin, clarithromycin, minocycline, or tigecycline alone and in combination with amphotericin B, itraconazole, terbinafine, voriconazole, anidulafungin, caspofungin, or micafungin against 30 isolates of the oomycete Pythium insidiosum. The assays were based on the CLS...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02349-14

    authors: Jesus FP,Ferreiro L,Loreto ÉS,Pilotto MB,Ludwig A,Bizzi K,Tondolo JS,Zanette RA,Alves SH,Santurio JM

    更新日期:2014-09-01 00:00:00

  • In vitro activity of temocillin (BRL 17421), a novel beta-lactam antibiotic.

    abstract::The minimal inhibitory concentration of temocillin (BRL 17421) against 476 clinical isolates was determined by an agar dilution method. Temocillin was active against most of the Enterobacteriaceae, Haemophilus, and Neisseria strains tested. The compound showed low activity or was inactive against Bacteroides, Campylob...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.22.4.535

    authors: Van Landuyt HW,Pyckavet M,Lambert A,Boelaert J

    更新日期:1982-10-01 00:00:00

  • Antibiotic resistance and serotypes of 100 Streptococcus pneumoniae strains isolated in a children's hospital in Barcelona, Spain.

    abstract::A total of 100 Streptococcus pneumoniae strains with various penicillin G susceptibilities, isolated in Barcelona, Spain, from different pediatric sources during 1983 and the first 4 months of 1984, were tested for susceptibility to tetracycline, chloramphenicol, erythromycin, clindamycin, vancomycin, and rifampin. Th...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.28.2.357

    authors: Latorre C,Juncosa T,Sanfeliu I

    更新日期:1985-08-01 00:00:00

  • Purification of a streptococcal bacteriocin (viridin B) and its separation from alpha-hemolysin.

    abstract::Viridin B, a bacteriocin produced by Streptococcus mitis, copurified with the alpha-hemolysin after ammonium sulfate precipitation and gel filtration on Sephadex G-200. The bacteriocin and hemolysin were separated in some instances by ion-exchange chromatography on diethylaminoethyl-Sephadex A-50, but the two substanc...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.15.3.436

    authors: Apelgren LD,Dajani AS

    更新日期:1979-03-01 00:00:00

  • Comparative study of anti-pseudomonas activity of azlocillin, mezlocillin, and ticarcillin.

    abstract::The anti-pseudomonas activities of azlocillin and mezlocillin were compared with that of ticarcillin. We measured the minimal inhibitory and minimal bactericidal concentrations of the three drugs against 20 different strains of Pseudomonas aeruginosa and found significantly lower values for azlocillin than for the oth...

    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.15.3.396

    authors: Coppens L,Klastersky J

    更新日期:1979-03-01 00:00:00

  • Factors influencing susceptibility of Nocardia species to trimethoprim-sulfamethoxazole.

    abstract::Demonstration of synergism between trimethoprim and sulfamethoxazole against 10 Nocardia isolates was found to be critically dependent upon the isolate, the duration of incubation, and the trimethoprim-sulfamethoxazole ratio. Inoculum effect was not significant. The trimethoprim-sulfamethoxazole ratio in the commercia...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.13.4.624

    authors: Bennett JE,Jennings AE

    更新日期:1978-04-01 00:00:00

  • Pharmacodynamics of metronidazole determined by a time-kill assay for Trichomonas vaginalis.

    abstract::The pharmacodynamic effects of metronidazole on Trichomonas vaginalis have been poorly characterized. The present in vitro study was performed to characterize the relationship between killing of trichomonads and metronidazole exposure (metronidazole concentration and time of exposure). Five laboratory strains and five...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.39.8.1848

    authors: Nix DE,Tyrrell R,Müller M

    更新日期:1995-08-01 00:00:00

  • Impact of lopinavir-ritonavir or nevirapine on bedaquiline exposures and potential implications for patients with tuberculosis-HIV coinfection.

    abstract::Concomitant treatment of tuberculosis (TB) and HIV is recommended and improves outcomes. Bedaquiline is a novel drug for the treatment of multidrug-resistant (MDR) TB; combined use with antiretroviral drugs, nevirapine, or ritonavir-boosted lopinavir (LPV/r) is anticipated, but no clinical data from coinfected patient...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 临床试验,杂志文章

    doi:10.1128/AAC.03246-14

    authors: Svensson EM,Dooley KE,Karlsson MO

    更新日期:2014-11-01 00:00:00

  • Gentamicin pharmacokinetics, nephrotoxicity, and prediction of mortality in febrile neutropenic patients.

    abstract::The pharmacokinetics of gentamicin in 34 febrile neutropenic patients (40 courses) were compared with those in 40 nonneutropenic patients receiving the drug. No pharmacokinetic differences were seen in half-life, volume of distribution (liter per kilogram; total and ideal body weight), or clearance (milliliter per min...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.33.11.1890

    authors: Bianco TM,Dwyer PN,Bertino JS Jr

    更新日期:1989-11-01 00:00:00

  • In vitro evaluation of CP-62,993, erythromycin, clindamycin, and tetracycline against Chlamydia trachomatis.

    abstract::The antimicrobial activity of CP-62,993 against four Chlamydia trachomatis isolates was compared with those of erythromycin, clindamycin, and tetracycline. The MIC of CP-62,993 was 0.26 to 1.02 micrograms/ml for 100% inclusion inhibition and 0.031 to 0.063 microgram/ml for 50% inclusion inhibition. With pharmacokineti...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.31.5.811

    authors: Walsh M,Kappus EW,Quinn TC

    更新日期:1987-05-01 00:00:00