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At least 1,135 records · Page 63Linked to original sources
PubMed2005

In vitro susceptibility of clinical isolates of Brucella melitensis to fucidic acid.

Brucella species are facultative intracellular bacteria, and therefore a limited number of antibiotics are effective against these organisms. The side effects of drug combination schemes, and the incidences of relapses and therapeutic failures, have led to investigations of new drugs to treat brucellosis. The purpose of this study was to test the in vitro susceptibility of 50 Brucella melitensis isolates to fucidic acid, which has not previously been used for the treatment of brucellosis. The minimum inhibitory concentrations (MICs) of fucidic acid to 50 B. melitensis isolates that were obtained from blood and bone marrow cultures of patients with brucellosis were studied by the broth microdilution method. The MIC50 and MIC90 values for the 50 B. melitensis strains' susceptibility to fucidic acid were determined to be 0.5 and 2 microg/ml, respectively, and the MIC range was 0.125-2.0 microg/ml. Further experiments are needed to reassess the activity of fucidic acid against intracellular Brucella spp.

Adolescent↗
PubMed1973

Effects of enzyme inhibitors of catecholamine metabolism and of haloperidol on the pancreatic secretion induced by L-DOPA and by dopamine in dogs.

1. Effects of inhibitors of DOPA decarboxylase, dopamine beta-hydroxylase and monoamine oxidase, and haloperiodol on the secretion of pancreatic juice induced by L-DOPA and dopamine were studied in preparations of the isolated blood-perfused canine pancreas.2. The increased secretion induced by the infusion of L-DOPA (100 mug/min) was completely antagonized by Ro 4-4602 (300 mug), a DOPA decarboxylase inhibitor.3. The secretogogue effect of dopamine (1-10 mug) intra-arterially was not affected by Ro 4-4602, but was enhanced by the infusion of fusaric acid (100 mug/min), a dopamine beta-hydroxylase inhibitor.4. The increase in the secretion induced by dopamine (1-10 mug) was enhanced by treatment with nialamide (100 mg/kg), a monoamine oxidase inhibitor, given intravenously.5. Haloperidol (1 mg) intra-arterially attenuated the dopamine-induced pancreatic secretion.6. It is concluded that L-DOPA is converted to dopamine in the acinar cells which causes an increase in the secretion of pancreatic juice, thus the intracellular level of dopamine may be controlled by enzymatic equilibrium.

Animals↗
PubMed1993

Inhibition of oxidized low-density lipoprotein metabolism in macrophage J774 by helvolic acid.

The antibiotic helvolic acid inhibited cholesteryl ester accumulation in macrophage J774 treated with oxidized low-density lipoprotein (LDL) at a concentration of 50-350 microM. The agent reduced oxidized 125I-LDL degradation and [14C]oleate incorporation into cholesteryl ester. In a cell-free assay, ATP-dependent acidification of endosomes and lysosomes was significantly inhibited by 35 microM helvolic acid, suggesting that this activity accounts for the inhibition of oxidized LDL metabolism in the macrophages.

Adenosine Triphosphate↗
PubMed2004

Conspecificity of the cerulenin and helvolic acid producing 'Cephalosporium caerulens', and the hypocrealean fungus Sarocladium oryzae.

Fermentation processes for the biochemical reagents cerulenin and helvolic acid employ 'Cephalosporium caerulens,' an invalidly published designation that has been used for more than 40 years. However, its identity has never been critically examined because strains were unavailable from major culture collections. An authentic strain of C. caerulens', derived from the original strain KF-140, was recently found and compared to Sarocladium oryzae, another Acremonium-like fungus which also produces cerulenin and helvolic acid. Morphological comparisons, rDNA sequence data, and chromatography of secondary metabolites established that 'C. caerulens' and S. oryzae are conspecific. Sequence data from ribosomal DNA genes indicated S. oryzae belongs to the Hypocreales and is allied with members of the Ceratostomataceae, Scopinella species, Emericellopsis species and certain Acremonium-like anamorphs of uncertain familial relationships. At least two of the isolates of S. oryzae produced titres of cerulenin and helvolic acid similar to those of KF-140. This finding demonstrates that manufacture of cerulenin need not be limited to the original strain.

Acremonium↗
PubMed2002

Treatment of acute neonatal bacterial conjunctivitis: a comparison of fucidic acid to chloramphenicol eye drops.

PURPOSE: To compare the clinical and bacteriological effects of fucidic acid (Fucithalmic: 1.0%) and chloramphenicol (Minims(R): 0.5%) eye drops in neonates with a clinical diagnosis of acute conjunctivitis of suspected bacterial origin. METHODS: A TOTAL OF 456 N: ewborns with gestational age > 32 weeks with acute conjunctivitis of suspected bacterial origin acquired within the first 28 days of life were included in the study. They were randomly assigned to a 7-day treatment with eye drops using either fucidic acid (1.0%) (Fucithalmic) applied twice per day, or chloramphenicol (0.5%) (Minims Chloramphenicol) applied six times per day. The subjects were followed up with two visits (on days 1 and 8) and by telephone 2 weeks after the end of treatment. RESULTS: Eighty-nine per cent of the neonates treated with Fucithalmic were cured, compared to 87.9% of those treated with Minims Chloramphenicol (n.s). The drug was used as instructed in 90.7% of patients treated with Fucithalmic and in 78.0% of those treated with Minims Chloramphenicol (P < 0.001). CONCLUSION: Treating neonatal conjunctivitis with fucidic acid is easier than with chloramphenicol and is equally effective.

Acute Disease↗
PubMed1999

Bacteremia after dental treatment in mentally handicapped people.

Bacteremia may occur after disruption of the oral mucous membrane, particularly after dental treatment. 18 mentally handicapped patients who underwent dental treatment with general anesthesia were included in our study. None of the patients had general illnesses or received antibiotic protection. From each patient several blood samples were drawn aseptically during dental treatment and cultured. The majority of aerobic bacteria recovered belonged to Streptococcus sp and Gemella sp., anaerobic bacteria mainly belonged to Porphyromonas gingivalis and Peptostreptococcus sp. Resistance of the isolated bacteria to penicillin as well as to oxacillin, erythromycin and Co-trimoxazole was substantial. The highest resistance rate could be shown against fucidic acid.

Adolescent↗
PubMed1982

Staphylococcal infections among newborn babies in two towns in north Norway.

1137 newborn infants in the towns of Harstad and Tromsø were examined for Staphylococcus aureus. The children were followed for two months after birth, and 10% showed signs of infection. The first symptom occurred on the average on the ninth day of life, while the average stay in the maternity ward was six days. 85% of those being regarded on clinical grounds as infected with S aureus showed growth of this bacterium on cultivation of the specimens taken. Over 80% of the strains were resistant to penicillin G/V and approximately 11% resistant to fucidic acid. Resistance to other antibiotics was not found to present any problem. A survey of staphylococcal infections among the newborn should include both the stay in the maternity ward and the first week at home.

Female↗
PubMed2004

Aspergillus fumigatus CY018, an endophytic fungus in Cynodon dactylon as a versatile producer of new and bioactive metabolites.

Aspergillus fumigatus CY018 was recognized as an endophytic fungus for the first time in the leaf of Cynodon dactylon. By bioassay-guided fractionation, the EtOAc extract of a solid-matrix steady culture of this fungus afforded two new metabolites, named asperfumoid (1) and asperfumin (2), together with six known bioactive compounds including monomethylsulochrin, fumigaclavine C, fumitremorgin C, physcion, helvolic acid and 5alpha,8alpha-epidioxy-ergosta-6,22-diene-3beta-ol as well as other four known compounds ergosta-4,22-diene-3beta-ol, ergosterol, cyclo(Ala-Leu) and cyclo(Ala-Ile). Through detailed spectroscopic analyses including HRESI-MS, homo- and hetero-nuclear correlation NMR experiments (HMQC, COSY, NOESY and HMBC), the structures of asperfumoid and asperfumin were established to be spiro-(3-hydroxyl-2,6-dimethoxyl-2,5-diene-4-cyclohexone-(1,3')-5'-methoxyl-7'-methyl-(1'H, 2'H, 4'H)-quinoline-2',4'-dione) and 5-hydroxyl-2-(6-hydroxyl-2-methoxyl-4-methylbenzoyl)-3,6-dimethoxyl-benzoic methyl ester, respectively. All of the 12 isolates were subjected to in vitro bioactive assays against three human pathogenic fungi Candida albicans, Tricophyton rubrum and Aspergillus niger. As a result, asperfumoid, fumigaclavine C, fumitremorgin C, physcion and helvolic acid were shown to inhibit C. albicans with MICs of 75.0, 31.5, 62.5, 125.0 and 31.5 microg/mL, respectively.

Antifungal Agents↗
PubMed2002

Detection and quantification of phytotoxic metabolites of Sarocladium oryzae in sheath rot-infected grains of rice.

AIMS: The present study describes the detection and quantification of the Sarocladium oryzae metabolites, helvolic acid and cerulenin in extracts of rice grains collected from plants infected with sheath rot. It also describes the phytotoxicity of these metabolites on rice seedlings. METHODS AND RESULTS: Helvolic acid and cerulenin in sheath rot-infected rice grains were detected using thin layer chromatography (TLC) and nuclear magnetic resonance (NMR) analyses. On the TLC plates helvolic acid and cerulenin moved as brownish yellow spots and showed R(F) values of 0.61 and 0.49, respectively. A standard assay curve was developed on the basis of selective toxicity of helvolic acid towards Calvibacter michiganensis ATCC 2140 and cerulenin towards Candida albicans 1150. The amounts of helvolic acid and cerulenin on the basis of standard assay curve were 2.2 and 1.75 microg g(-1) of infected seeds. Treatment of IR 36 rice seedlings with metabolites induced chlorosis and reduced shoot length by 20%, root length by 30% and root number by 7% relative to control. CONCLUSIONS: Helvolic acid and cerulenin were detected in infected rice grains and these metabolites induced chlorosis and reduced the seed viability and seedling health of rice. SIGNIFICANCE AND IMPACT OF THE STUDY: Antimicrobial and phytotoxic metabolites, helvolic acid and cerulenin are present in infected grains and reduce the seed viability and seedling health. These metabolites may increase the pathogenic potential and survival of S. oryzae in rice seed by competing with other seed-borne fungi.

Cerulenin↗
PubMed1996

Topical lomefloxacin twice daily compared with fucidic acid in acute bacterial conjunctivitis.

Forty-five patients with presumed acute bacterial conjunctivitis were treated in an investigator-masked randomized multicenter study with either lomefloxacin 0.3% or fucidic acid 1% eye drops twice daily. Clinical signs and symptoms were rated by slit-lamp examination and conjunctival swab cultures were performed to evaluate clinical and microbiological efficacy. A total of 57 ocular isolates were tested for susceptibility to nine antibiotics. A significant decrease in clinical symptomatology was achieved by both treatments with a gradual improvement over the treatment period of 7-9 days. Bacteriological recovery was frequently achieved already at the first control visit (day 3-5), but the recovery rate was statistically significant (p = 0.014) only in the lomefloxacin group. The relatively high in vitro resistance rate (46%) to fucidic acid was not reflected by lower clinical efficacy. Two unrelated adverse events (one in each treatment group) and minimal local intolerance problems were observed in both treatment groups. A significantly higher incidence of burning sensation was observed with fucidic acid than with lomefloxacin (p < 0.01). All four treatment failures in the study occurred in the fucidic acid group. Lomefloxacin 0.3% ophthalmic solution demonstrated a high efficacy and good tolerance in the management of acute bacterial conjunctivitis.

Acute Disease↗
PubMed1981

[Process of sodium fusidate inactivation as affected by oxygen and humidity].

The effect of oxygen and moisture on stability of sodium fusidate was studied. It was shown that inactivation of the antibiotic in the atmosphere of oxygen was due to its oxidation in the preparations with low humidity levels. In the preparations with high humidity levels, the main cause of the antibiotic inactivation was hydrolysis with respect to C-16-O-acetyl group. When sodium fusidate was air stored, the salts of 24, 25-dioxy-and 24, 25-dioxy-11-monoketofusidic acids were identified among the products of its inactivation. The salts of 24,25-dioxy-11-monoketofusidic acid were also prepared by oxidation of fusidic acid with potassium permanganate in a weak alkaline medium. The possibility of using sodium sulfite and metabisulfite as stabilizers for th antibiotic storage was shown.

Drug Stability↗
PubMed2004

Detection of Aspergillus fumigatus mycotoxins: immunogen synthesis and immunoassay development.

Immunological detection of secreted low molecular weight toxins represents a potentially novel means of diagnosing infection by the fungus Aspergillus fumigatus. Two such metabolites, gliotoxin and helvolic acid, were selected and conjugated to thyroglobulin for antisera generation in rabbits. Gliotoxin was initially activated using N-[p-maleimidophenyl] isocyanate (PMPI) and subsequently conjugated to S-acetyl thioglycolic acid N-hydroxysuccinimide-activated thyroglobulin, whereas helvolic acid was activated with N-(3-Dimethylaminopropyl)-N'-ethylcarbodiimide (EDC) in the presence of thyroglobulin prior to immunisation. To facilitate subsequent antisera evaluation, both toxins were similarly conjugated to bovine serum albumin (BSA). Matrix-Assisted Laser Desorption Ionisation-Time Of Flight (MALDI-TOF) mass spectrometry and SDS-PAGE analysis confirmed covalent attachment of toxins to BSA in the ratios of 15 and 2.4 mol per mol BSA for gliotoxin and helvolic acid, respectively. Resultant high titer antisera were capable of detecting both BSA-conjugated toxins (inhibitory concentration (IC)(50): 4-5 microg/ml). Free toxins were also detectable by competitive immunoassay, whereby 10 microg/ml free gliotoxin (30 microM) and helvolic acid (17 microM), respectively, inhibited antibody binding to cognate toxin-BSA previously immobilised on microwells. This work confirms that sensitive and specific antisera can be raised against fungal toxins and may have an application in diagnosing fungal infection.

Animals↗