bluuebunny/crossref_metadata_2025_split huggingface dataset:
Dendrimers, a New Class of Candidate Topical Microbicides with Activity against Herpes Simplex Virus Infection
Authors: Bourne N. , Stanberry L. R. , Kern E. R. , Holan G. , Matthews B. , Bernstein D. I. 
Published: July 2002

ABSTRACT
Dendrimers are large highly branched macromolecules synthesized from a polyfunctional core. They have shown a variety of biological properties, including, in some instances, antiviral activity. In this study, five dendrimers were evaluated for in vitro activity against herpes simplex virus (HSV) types 1 and 2 by cytopathic effect (CPE) inhibition and plaque reduction (PR) assay in human foreskin fibroblast cells. All of the compounds were active against both virus types in the CPE inhibition assay, in which drug was added to the cells prior to the addition of virus. Antiviral activity was reduced or lost in the PR assays, in which the cells were incubated with the virus before the drug was added. The prophylactic efficacy suggested that the dendrimers might have potential as topical microbicides, products intended to be applied to the vaginal or rectal mucosa to protect against sexually transmitted infections. Three dendrimers were evaluated for this application against genital HSV infection in mice. Two of the compounds, BRI-2999 and BRI-6741, significantly reduced infection rates when 15 μl of a 100-mg/ml solution was administered immediately prior to intravaginal challenge, and the most effective compound, BRI-2999, provided significant protection even when applied 30 min before challenge. This is the first report of microbicidal activity by dendrimers in vivo.
In Vitro Susceptibilities of 400 Spanish Isolates of
Neisseria gonorrhoeae
to Gemifloxacin and 11 Other Antimicrobial Agents
Authors: Berrón S. , Vázquez J. A. , Giménez M. J. , de la Fuente L. , Aguilar L. 
Published: July 2002

ABSTRACT

The in vitro activity of gemifloxacin versus those of 11 other antimicrobial agents against 400 strains of
Neisseria gonorrhoeae
was determined by microdilution with supplemented GC agar. A total of 37.5% of the strains were β-lactamase positive. A total of 70 and 6.4% of the β-lactamase-negative strains exhibited intermediate and high-level penicillin resistance, respectively. Ceftriaxone and gemifloxacin were the most active drugs (MICs at which 90% of isolates are inhibited, 0.01 versus 0.007 μg/ml, respectively), with 100% of strains inhibited by 0.12 μg/ml.
Comparison of Once-Daily versus Twice-Daily Administration of Cefdinir against Typical Bacterial Respiratory Tract Pathogens
Authors: Ross Gigi H. , Hovde Laurie Baeker , Ibrahim Khalid H. , Ibrahim Yasir H. , Rotschafer John C. 
Published: July 2002

ABSTRACT

In an in vitro pharmacodynamic model, a twice-daily cefdinir dosing regimen was more effective than a once-daily regimen against common bacterial respiratory pathogens in producing 3-log
10
killing and preventing the occurrence of regrowth at 24 h. Twice-daily administration is likely the more appropriate cefdinir dosing strategy for the treatment of community-acquired pneumonia.
Pharmacokinetic-Pharmacodynamic Modeling of Electroencephalogram Effect of Imipenem in Rats with Acute Renal Failure
Authors: Dupuis Antoine , Limosin Anne , Paquereau Joël , Mimoz Olivier , Couet William , Bouquet Serge 
Published: July 2002

ABSTRACT
The epileptogenic activity of imipenem was investigated in rats with experimental renal failure induced by uranyl nitrate injection by using electroencephalogram (EEG) recording and a pharmacokinetic-pharmacodynamic model including an effect compartment. Results previously obtained with healthy rats were used to estimate the dose of imipenem required to induce an observable but nonlethal EEG effect on the assumption that only the pharmacokinetic parameters of the model would be affected by renal failure. Good agreement was observed between the predicted and observed effects.
Influence of Prior Exposure to Zidovudine on Stavudine Phosphorylation In Vivo and Ex Vivo
Authors: Hoggard P. G. , Sales S. D. , Phiboonbanakit D. , Lloyd J. , Maher B. A. , Khoo S. H. , Wilkins E. , Carey P. , Hart C. A. , Back D. J. 
Published: July 2002

ABSTRACT

Intracellular phosphorylation of stavudine (d4T) and zidovudine (ZDV) was investigated in peripheral blood mononuclear cells (PBMCs) isolated from ZDV-naive and ZDV-experienced human immunodeficiency virus (HIV)-positive patients. An in vivo study measured the amount of d4T triphosphate (d4TTP), while an ex vivo study assessed the capacity of cells to phosphorylate added d4T. Endogenous dTTP was also measured. d4TTP and dTTP were determined in vivo using a reverse transcriptase chain termination assay. In ex vivo studies, d4T (1 μM) was incubated in resting and phytohemagglutinin-stimulated (10 μg ml
−1
; 72 h) PBMCs for 24 h. After washing and methanol extraction, radiolabeled anabolites were detected by high-performance liquid chromatography. d4TTP reached its highest level 2 to 4 h after dosing (0.21 ± 0.14 pmol/10
6
cells;
n
= 27 [mean ± standard deviation]). Comparison of ZDV-naive and ZDV-experienced individuals showed no significant difference in levels of d4TTP (ZDV naive, 0.23 ± 0.17 pmol/10
6
cells [
n
= 7] versus ZDV experienced, 0.20 ± 0.14 pmol/10
6
cells [
n
= 20];
P
= 0.473) or the d4TTP/dTTP ratio (0.14 ± 0.12 [
n
= 7] and 0.10 ± 0.08 [
n
= 20], respectively;
p
= 0.391). Ex vivo data demonstrated no significant difference in the formation of d4TTP or total d4T phosphates in naive and experienced patients (0.086 ± 0.055 pmol/10
6
cells in ZDV-naive patients [
n
= 17] versus 0.081 ± 0.038 pmol/10
6
cells in ZDV-experienced patients [
n
= 22];
P
= 0.767). The ability of HIV-infected patients to phosphorylate d4T in vivo and ex vivo was unchanged with increasing exposure to ZDV.
Efficacy of an Evernimicin (SCH27899) In Vitro and in an Animal Model of Lyme Disease
Authors: Pavia Charles S. , Wormser Gary P. , Nowakowski John , Cacciapuoti Anthony 
Published: July 2002

ABSTRACT

The MICs of evernimicin at which 90% of
Borrelia burgdorferi
patient isolates were inhibited ranged from 0.1 to 0.5 μg/ml. Evernimicin was as effective as ceftriaxone against
B. burgdorferi
in a murine model of experimental Lyme disease. As assessed by culturing the urinary bladders of infected C3H mice, no live
Borrelia
isolates were recoverable following antibiotic treatment.
New Mutation in ParE in a Pneumococcal In Vitro Mutant Resistant to Fluoroquinolones
Authors: Janoir Claire , Varon Emmanuelle , Kitzis Marie-Dominique , Gutmann Laurent 
Published: July 2002

ABSTRACT

For an in vitro mutant of
Streptococcus pneumoniae
selected on moxifloxacin four- to eightfold-increased MICs of new fluoroquinolones, only a twofold-increased MIC of ciprofloxacin, and a twofold-decreased MIC of novobiocin were observed. This phenotype was conferred by two mutations: Ser81Phe in GyrA and a novel undescribed His103Tyr mutation in ParE, outside the quinolone resistance-determining region, in the putative ATP-binding site of topoisomerase IV.
In Vitro Uptake of SCH 27899 (Evernimicin) by Rat Alveolar Macrophages
Authors: Zbaida Shmuel , Brieland Joan , Krieter Philip , Loebenberg David , Krishna Gopal , Horne Debra , Lu Xiaowen , Yuan Yuan , Hare Roberta , Cayen Mitchell N. , Patrick James E. 
Published: July 2002

ABSTRACT

The in vitro uptake of [
14
C]evernimicin ([
14
C]SCH 27899) by primary cultures of rat alveolar macrophages and hepatocytes was determined. Both cell populations exhibited linear rates of uptake. However, the initial rate of drug uptake by alveolar macrophages was about threefold higher than that by hepatocytes. These findings demonstrate that [
14
C]evernimicin is taken up by rat alveolar macrophages, supporting the likelihood that the drug is able to reach sites of infection.
Molecular Analysis of Tn
1546
-Like Elements in Vancomycin-Resistant Enterococci Isolated from Patients in Europe Shows Geographic Transposon Type Clustering
Authors: Schouten Marinus A. , Willems Rob J. L. , Kraak Wilma A. G. , Top Janetta , Hoogkamp-Korstanje Jacomina A. A. , Voss Andreas 
Published: July 2002

ABSTRACT

Resistance mechanism relatedness was studied in 18 clinical, European
vanA
vancomycin-resistant enterococci. Molecular analysis revealed 10 Tn
1546
-like elements, suggesting two evolutionary lineages. Lineage I dominated the European mainland, and lineage II dominated the United Kingdom and Israel. Geographic clustering reflected different types of meat consumption between countries, since each lineage is associated with colonization of different animals.
Bactericidal Activities of BMS-284756, a Novel Des-F(6)-Quinolone, against
Staphylococcus aureus
Strains with Topoisomerase Mutations
Authors: Lawrence Laura E. , Frosco MaryBeth , Ryan Brenda , Chaniewski Susan , Yang Hyekyung , Hooper David C. , Barrett John F. 
Published: July 2002

ABSTRACT

The antistaphylococcal activities of BMS-284756 (T-3811ME), levofloxacin, moxifloxacin, and ciprofloxacin were compared against wild-type and
grlA
and
grlA/gyrA
mutant strains of
Staphylococcus aureus
. BMS-284756 was the most active quinolone tested, with MICs and minimal bactericidal concentrations against
S. aureus
wild-type strain MT5,
grlA
mutant MT5224c4, and
grlA/gyrA
mutant EN8 of 0.03 and 0.06, 0.125 and 0.125, and 4 and 4 μg/ml, respectively. In the time-kill studies, BMS-284756 and levofloxacin exhibited rapid killing against all strains. Ciprofloxacin, however, was not bactericidal for the double mutant, EN8. BMS-284756 and levofloxacin were bactericidal (3 log
10
decrease in CFU/ml) against the MT5 and MT5224c4 strains at two and four times the MIC within 2 to 4 h. Against EN8, BMS-284756 was bactericidal within 4 h at two and four times the MIC, and levofloxacin achieved similar results within 4 to 6 h. Both the wild-type strain MT5 and
grlA
mutant MT5224c4 should be considered susceptible to both BMS-284756 and levofloxacin, and both quinolones are predicted to have clinical efficacy. The in vivo efficacy of BMS-284756, levofloxacin, and moxifloxacin against
S. aureus
strain ISP794 and its single mutant 2C6(1)-1 directly reflected the in vitro activity: increased MICs correlated with decreased in vivo efficacy. The 50% protective doses of BMS-284756 against wild-type and mutant strains were 2.2 and 1.6 mg/kg of body weight/day, respectively, compared to the levofloxacin values of 16 and 71 mg/kg/day and moxifloxacin values of 4.7 and 61.6 mg/kg/day. BMS-284756 was more potent than levofloxacin and equipotent with moxifloxacin against ISP794 both in vitro and in vivo, while BMS-284756 was more potent than levofloxacin and moxifloxacin against 2C6(1)-1.
In Vitro Antianaerobic Activity of Ertapenem (MK-0826) Compared to Seven Other Compounds
Authors: Hoellman Dianne B. , Kelly Linda M. , Credito Kim , Anthony Lauren , Ednie Lois M. , Jacobs Michael R. , Appelbaum Peter C. 
Published: July 2002

ABSTRACT

Ertapenem, imipenem, meropenem, ceftriaxone, piperacillin, piperacillin-tazobactam, clindamycin, and metronidazole were agar dilution MIC tested against 431 anaerobes. Imipenem, meropenem, and ertapenem were the most active β-lactams (MICs at which 50% of the strains are inhibited [MIC
50
s], 0.125 to 0.25 μg/ml; MIC
90
s, 1.0 to 2.0 μg/ml). Time-kill studies revealed that ertapenem at two times the MIC was bactericidal for 9 of 10 strains after 48 h. The kinetics for other β-lactams were similar to those of ertapenem.
Pharmacodynamic Interaction of Doxycycline and Artemisinin in
Plasmodium falciparum
Authors: Sponer Ulrike , Prajakwong Somsak , Wiedermann Gerhard , Kollaritsch Herwig , Wernsdorfer Gunther , Wernsdorfer Walther H. 
Published: July 2002

ABSTRACT

Parallel in vitro tests, assessing the inhibition of schizont maturation, were conducted with 31 fresh isolates of
Plasmodium falciparum
from Thailand, using artemisinin, doxycycline, and combinations of both. The activities of artemisinin and doxycycline are obviously not correlated. Both compounds showed consistent synergism at 50% effective concentration (EC
50
), EC
90
, and EC
99
levels.
Multicenter Study on Spreading of the
tet
(M) Gene in Tetracycline-Resistant
Streptococcus
Group G and C Isolates in Argentina
Authors: Jeric P. E. , Lopardo H. , Vidal P. , Arduino S. , Fernandez A. , Orman B. E. , Sordelli D. O. , Centrón D. 
Published: July 2002

ABSTRACT

A prospective multicenter study on invasive infections caused by beta-hemolytic streptococci was performed over 6 months and involved 42 centers from 16 cities in Argentina. Among 33 isolates recovered, 9 group G
Streptococcus
isolates (39.1%) and 2 group C
Streptococcus
isolates (20%) exhibited resistance to tetracycline and harbored the
tet
(M) gene. Genealogical analysis revealed that tetracycline resistance has a polyclonal origin in Argentina.
Stability of New Carbapenem DA-1131 to Renal Dipeptidase (Dehydropeptidase I)
Authors: Park Sung Wook , We Jeoung Soon , Kim Gye Won , Choi Seong Hak , Park Haeng Soon 
Published: July 2002

ABSTRACT

The stability of DA-1131 to renal dipeptidase (RDPase) (EC 3.4.13.19) was compared with that of imipenem and meropenem by
V
max
/

K
m

ratios as an index of the enzyme's preference for substrates. Our results showed a decreasing order of imipenem (6.24), meropenem (2.41), and DA-1131 (1.39). The biochemical evaluation of DA-1131 as the least preferred substrate of RDPase suggests its potential use as a novel β-lactam antibiotic which may be usable without coadministration of RDPase inhibitors once its clinical suitability is proven.
Optimal Dose of Amoxicillin in Treatment of Otitis Media Caused by a Penicillin-Resistant Pneumococcus Strain in the Gerbil Model
Authors: Parra Araceli , Ponte Carmen , Cenjor Carlos , García-Calvo Gloria , Giménez María José , Aguilar Lorenzo , Soriano Francisco 
Published: July 2002

ABSTRACT
Amoxicillin at doses of 0.2 to 5 mg/kg of body weight was administered for the treatment of pneumococcal otitis media in a gerbil model. Doses greater than or equal to 2.5 mg/kg, which resulted in concentrations in middle ear fluid of ≥1.4 μg/ml and concentrations in serum higher than the MIC (1 μg/ml) for ≥14% of the dosing interval, were both clinically and bacteriologically effective.
In Vitro Activities of the Des-Fluoro(6) Quinolone BMS-284756 against Aerobic and Anaerobic Pathogens Isolated from Skin and Soft Tissue Animal and Human Bite Wound Infections
Authors: Goldstein Ellie J. C. , Citron Diane M. , Merriam C. Vreni , Warren Yumi A. , Tyrrell Kerin L. , Fernandez Helen 
Published: July 2002

ABSTRACT

BMS-284756, a new des-fluoro(6) quinolone, was very active against 240 aerobic and 180 anaerobic isolates from bite victims. It inhibited 403 of 420 (96%) isolates, including those of
Moraxella
spp., CDC group EF-4, and
Eikenella corrodens
at ≤2 μg/ml and those of all
Pasteurella
spp. and
Bergeyella zoohelcum
at ≤0.015 μg/ml.
Fusobacterium russii
and 6 of 11
Fusobacterium nucleatum
isolates of animal bite origin were resistant, but isolates of human bite origin were susceptible, which suggests that they were of a different subspecies.
Activity of BMS-284756, a Novel Des-Fluoro(6) Quinolone, against
Staphylococcus aureus
, Including Contributions of Mutations to Quinolone Resistance
Authors: Low D. E. , Muller M. , Duncan C. L. , Willey B. M. , de Azavedo J. C. , McGeer A. , Kreiswirth B. N. , Pong-Porter S. , Bast D. J. 
Published: July 2002

ABSTRACT

The in vitro activity of BMS-284756 against 602
Staphylococcus aureus
isolates, including 152 that were both methicillin and ciprofloxacin resistant (MIC ≥4 μg/ml), was determined. For ciprofloxacin-susceptible and nonsusceptible isolates, the MICs at which 50% of organisms were inhibited were 0.015 and 2 μg/ml and the MICs at which 90% of organisms were inhibited were 0.03 and 4 μg/ml, respectively.
Determining Linezolid’s Baseline In Vitro Activity in Canada Using Gram-Positive Clinical Isolates Collected prior to Its National Release
Authors: Karlowsky James A. , Kelly Laurie J. , Critchley Ian A. , Jones Mark E. , Thornsberry Clyde , Sahm Daniel F. 
Published: July 2002

ABSTRACT

All of the isolates of
Staphylococcus aureus
(
n
= 317),
Enterococcus
species (
n
= 315),
Streptococcus pneumoniae
(
n
= 282), and
Staphylococcus epidermidis
(
n
= 176) collected at 16 Canadian microbiology laboratories from October 2000 to April 2001 were susceptible to linezolid. Future studies will determine how linezolid clinical use in Canada affects its in vitro activity.
Observation of Soft Contact Lens Disinfection with Fluorescent Metabolic Stains
Authors: Gavin J. , Button N. F. , Watson-Craik I. A. , Logan N. A. 
Published: July 2002

ABSTRACT

A rapid fluorescent staining method using a tetrazolium dye and propidium iodide for the in-use assessment of disinfection of
Pseudomonas aeruginosa
biofilms on soft contact lenses showed that 11 to 13% of cells on lenses remained actively respiring and recoverable by culture methods after 30 min of exposure to 3% hydrogen peroxide.
Immunomagnetic Purification of
Colletotrichum lindemuthianum
Appressoria
Authors: Hutchison Katie A. , Perfect Sarah E. , O'Connell Richard J. , Green Jonathan R. 
Published: July 2002

ABSTRACT

We developed a method to purify appressoria of the bean anthracnose fungus
Colletotrichum lindemuthianum
for biochemical analysis of the cell surface and to compare appressoria with other fungal structures. We used immunomagnetic separation after incubation of infected bean leaf homogenates with a monoclonal antibody that binds strongly to the appressoria. Preparations with a purity of >90% could be obtained. Examination of the purified appressoria by transmission electron microscopy showed that most had lost their cytoplasm. However, the plasma membrane was retained, suggesting that there is some form of attachment of this membrane to the cell wall. The purified appressoria can be used for studies of their cell surface, and we have shown that there are clear differences in the glycoprotein constituents of cell walls of appressoria compared with mycelium.
New Method for Evaluation of Virucidal Activity of Antiseptics and Disinfectants
Authors: Papageorgiou Georgios T. , Mocé-Llivina Laura , Jofre Juan 
Published: July 2002

ABSTRACT
Counting culturable viruses adsorbed to cellulose nitrate filters (the VIRADEN method) is proposed as a simple procedure for the evaluation of the virucidal activity of antiseptics and disinfectants. The virucidal activities of two different doses of iodine, chlorine, glutaraldehyde, and chlorhexidine digluconate on poliovirus 1 were tested with a standardized procedure and with the VIRADEN method. The two procedures assayed provided similar results.
Cultivation of Bacteria Producing Polyamino Acids with Liquid Manure as Carbon and Nitrogen Source
Authors: Pötter Markus , Oppermann-Sanio Fred Bernd , Steinbüchel Alexander 
Published: July 2002

ABSTRACT

Poly(γ-
d
-glutamic acid) (PGA)-producing strains of
Bacillus
species were investigated to determine their ability to contribute to reducing the amount of ammonium nitrogen in liquid manures and their ability to convert some of the ammonium into this polyamino acid as a transient depot for nitrogen. Organisms that do these things should help solve the serious environmental problems which are caused by the use of large amounts of liquid manure resulting from intensified agriculture; these problems are mainly due to the high content of ammonium nitrogen.
Bacillus licheniformis
ATCC 9945 and
Bacillus subtilis
were able to grow in liquid manure and to produce PGA in the presence of sodium gluconate. On artificial liquid manure these two strains were able to produce 0.85 and 0.79 g of PGA per liter, respectively. Under conditions that are found in intensified farming situations the ammonia content was reduced within 48 h from 1.3 to 0.75 g/liter. One mutant of
B. subtilis
1551 impaired in the catabolism of PGA was obtained after nitrosoguanidine mutagenesis. This mutant produced PGA at a final concentration of 4.8 g/liter, whereas the wild type produced only 3.7 g/liter.
Biological Activities and Structural Properties of the Atypical Bacteriocins Mesenterocin 52B and Leucocin B-TA33a
Authors: Corbier C. , Krier F. , Mulliert G. , Vitoux B. , Revol-Junelles A.-M. 
Published: July 2002

ABSTRACT
The antibacterial spectra and modes of action of synthetic peptides corresponding to mesenterocin 52B and leucocin B-TA33a greatly differ despite their high sequence homology. Circular dichroism experiments establish the capacity of each of these two peptides to partly fold into an amphiphilic helix that might be crucial for their adsorption at lipophilic-hydrophilic interfaces.
Fiber-Optic Fluorometer for Microscale Mapping of Photosynthetic Pigments in Microbial Communities
Authors: Thar Roland , Kühl Michael , Holst Gerhard 
Published: July 2002

ABSTRACT
Microscale fluorescence measurements were performed in photosynthetic biofilms at a spatial resolution of 100 to 200 μm with a new fiber-optic fluorometer which allowed four different excitation and emission wavelengths and was configured for measuring phycobiliproteins, chlorophylls, and bacteriochlorophylls. We present details of the measuring system and describe examples of applications in different microbial communities.
Persistence of a
Salmonella enterica
Serovar Typhimurium DT12 Clone in a Piggery and in Agricultural Soil Amended with
Salmonella
-Contaminated Slurry
Authors: Baloda Suraj B. , Christensen Lise , Trajcevska Silvija 
Published: July 2002

ABSTRACT

Prevalence of
Salmonella enterica
on a Danish pig farm presenting recurrent infections was investigated. A comparison of the pulsed-field gel electrophoresis patterns of fecal isolates from piggeries, waste slurry, and agricultural soil amended with
Salmonella
-contaminated animal waste (slurry) and subclinical isolates from the same farm (collected in 1996 and later) showed identical patterns, indicating long-term persistence of the
Salmonella enterica
serovar Typhimurium DT12 clone in the herd environment. Furthermore, when
Salmonella
-contaminated slurry was disposed of on the agricultural soil (a common waste disposal practice), the pathogen was isolated up to 14 days after the spread, indicating potentially high risks of transmission of the pathogen in the environment, animals, and humans.
Streptomyces
Serine Protease (DHP-A) as a New Biocatalyst Capable of Forming Chiral Intermediates of 1,4-Dihydropyridine Calcium Antagonists
Authors: Arisawa Akira , Matsufuji Motoko , Nakashima Takashi , Dobashi Kazuyuki , Isshiki Kunio , Yoshioka Takeo , Yamada Shigeru , Momose Haruo , Taguchi Seiichi 
Published: July 2002

ABSTRACT

Streptomyces viridosporus
A-914 was screened as a producer of an enzyme to effectively form chiral intermediates of 1,4-dihydropyridine calcium antagonists. The supernatant liquid of the growing culture of this strain exhibited high activity for enantioselective hydrolysis of prochiral 1,4-dihydropyridine diesters to the corresponding (4
R
) half esters. The responsible enzyme (termed DHP-A) was purified to apparent homogeneity and characterized. Cloning and sequence analysis of the gene for DHP-A (
dhpA
) revealed that the enzyme was a serine protease that is highly similar in both structural and enzymatic feature to SAM-P45, which is known as a target enzyme of
Streptomyces
subtilisin inhibitor (SSI), from
Streptomyces albogriseolus
. In a batch reaction test, DHP-A produced a higher yield of a chiral intermediate of 1,4-dihydropyridine than the commercially available protease P6. Homologous or heterologous expression of
dhpA
resulted in overproduction of the enzyme in culture supernatants, with 2.4- to 4.2-fold higher specific activities than in the parent
S. viridosporus
A-914. This indicates that DHP-A is suitable for use in reactions forming chiral intermediates of calcium antagonists and suggests the feasibility of developing DHP-A as a new commercial enzyme for use in the chiral drug industry.