Two flavones from Artemisia giraldii and their antimicrobial activity

'Antiphospholipid' (aPL) antibodies are a heterogenous group of autoantibodies that are now considered to be directed mainly to plasma proteins or protein-phospholipid complexes. Standardisation of assays for anticardiolipin (aCL) antibodies and lupus anticoagulants (LA) have been fraught with difficulty despite numerous attempts to perform this by International Standardisation Workshops and Committees.     

Sulfur-containing compounds from Scorodocarpus borneensis and their antimicrobial activity

This paper reports two cases of neotropical echinococcosis caused by Echinococcus oligarthrus and E. vogeli, neither of which has been reported from Suriname. Case 1, a six-year-old boy, presented a 15 x 25 mm retro-ocular cystic tumor (observed by ultrasound, computed tomography scan, and magnetic resonance imaging) causing exophthalmia, chemosis, palpebral ptosis, and blindness of the left eye. Of two tentative diagnoses, Echinococcus cyst or dermoid tumor, the former was shown to be correct at surgery when a clear liquid and detached protoscoleces were aspirated. Rostellar hooks of the protoscolex were characteristic of E. oligarthrus. Case 2, a 41-year-old man, had polycystic masses excised from the liver and abdomen. A presurgery diagnosis of E. vogeli infection was made due to calcifications seen in the lesions, positive serology, residence of the patient in the tropical forest, and later by the size and shape of rostellar hooks. The presence of these two parasites in one of the former Guianas is not surprising; both species are endemic in tropical forest in Central and South America wherever people have not exterminated wild canids, especially the bush dog, (Speothos venaticus), and felids (wild cats of several species), along with pacas, agoutis, and other rodents that serve as intermediate host of these two cestodes. Eighty-six cases of polycystic echinococcosis are known in people from 11 countries from Nicaragua to Argentina: 32 due to E. vogeli, three to E. oligarthrus, and 51 for which determination of the species was not possible because the hooks of the protoscolex were not found or described. Research to elucidate aspects of transmission of E. vogeli and E. oligarthrus is of practical importance for defining measures for preventing the severe and frequently fatal illnesses caused by these two cestodes.     

Bacterial pathogens and their antimicrobial susceptibility in Kumasi, Ghana

Between January, 1994 and June, 1996 a survey of bacterial isolates from clinical specimens and their antimicrobial susceptibility was performed at the Komfo Anokye Teaching Hospital, Microbiology Department, Kumasi, Ghana. A total of 11,380 bacterial isolates were cultured from eight different specimens. The sites of origin were wounds 32.2%, urine 28.1%, ear, nose and throat 3.6%, sputum 2.5% and aspirates 2.5%. Gram-negative bacteria accounted for 7955 (69.9%) isolates, the main species were Escherichia coli 47.1%, Pseudomonas spp. 16.8%, Proteus spp 14.6%, Klebsiella spp 10.2%, Neisseria gonorrhoeae 4.2%, Gram-positive bacteria contributed 3425 ((30.1%) of isolates, with Staphylococcus aureus 54.6% being the most predominant followed by Coagulase negative Staphylococcus 18.1%, Streptococcus pneumoniae 13.7% and Beta-haemolytic streptococci 4.1%. Escherichia coli showed 88% and 82% resistance to ampicillin and cotrimoxazole respectively with 78% being susceptible to gentamicin. Cefuroxime resistance in Gram-negative bacilli was 5%. As much as 30.6% and 21.7% of Streptococcus pneumoniae isolates were resistant to Penicillin and chloramphenicol respectively. Ten per cent of Staphylococcus aureus strains were susceptible to penicillin and 18% were resistant to flucloxacillin.     

Royleanones in the roots of Salvia officinalis L. of domestic provenance and their antimicrobial activity

The reported investigation of the constituents of the petroleum ether extract of the root of Salvia officinalis L. confirmed the presence of the following diterpene quinones: 12.hydroxy-8, 12-abietadiene-11, 14-dione (royleanone), 7 alpha, 12-dihydroxy-8.12-abistadiene-11-14-dione (horminone) and 7 alpha-acetoxy-12-hydroxy-8, 12-abietadiene-11,14-dione (7-O-acetylhorminone). The compounds were identified on the basic of the interpretation of results of spectral analysis. Isolated royleanones show antimicrobial activity against gram-positive bacteria (Staphylococcus aureus). A study of abietate diterpenoids in the root of Salvia officinalis L. of Slovak provenance has been performed for the first time.     

Chemistry and antimicrobial activity of caryoynencins analogs

Caryoynencins (1) are antibiotics isolated from liquid cultures of a plant pathogen, Pseudomonas caryophylli, and are unstable C18 carboxylic acids with a conjugated dienetetrayne structure. Enyne analogs of caryoynencins were synthesized from monosilylated 1,3-butadiyne 2 (n = 2), 1,3,5-hexatriyne 2 (n = 3), and 1,3,5,7-octatetrayne 2 (n = 4) by alkynyl metal addition to 2,4-hexadienal (3) followed by allylic rearrangement and deprotection. Tetraynol 5 (n = 4) thus obtained was resolved by enzyme reactions. The conjugated dienetetrayne compounds are mixtures of 3E,5E- and 3E,5Z-isomers, which equilibrate by room light. 13C-NMR chemical shifts of polyynes obey simple rules, which can be used for signal assignments. Antimicrobial activities of conjugated enynes and related compounds were examined. The tetrayne analog 6 (n = 4) possesses potent antibacterial and antifungal activities, while triyne and diyne analogs 6 (n = 3 and 2) are less active. Chirality does not affect the activities. An isomeric enyne compound, 2,4-tetradecadiene-7,9,11,13-tetrayn-6-ol (8), showed potent activity against Tricophyton.     

Preparation, characterization and in vitro antimicrobial activity of ampicillin-loaded polyethylcyanoacrylate nanoparticles

In this paper, the experimental conditions for preparing ampicillin-loaded polyethylcyanoacrylate (PECA) nanoparticles are described. The effects of drug concentration and surfactant type in the polymerization medium on the particle size distribution and loading capacity were studied. The results of these studies show that only the type of surfactant has an impact on the nanoparticle dimensions. The release rate of ampicillin from PECA nanoparticles at pH 7.4 (extracellular value pH) performed either with and without esterases, show that the drug release is considerably increased in the presence of these exzymes. The results of drug release study at pH 1.1 (simulated gastric juice) are very interesting. This study has evidenced that the 70% of ampicillin is released quickly, while the remaining fraction is firmly incorporated in nanoparticles. The released ampicillin is quickly degraded in acid medium while the entrapped fraction is protected from acid degradation and afterwards, when nanoparticles reach the small intestine, can be readily released in the presence of esterases. This result could be exploited for the oral administration of the ampicillin-PECA system. Finally, studies of antimicrobial activity of prepared systems evidenced that ampicillin-loaded PECA nanoparticles exhibit an activity equal or higher than the free drug.     

Synthesis, characterization and antimicrobial activity of zinc and cerium co-doped a-zirconium phosphate

A series of zinc ions or/and cerium ions co-doped α-zirconium phosphate (Zn-Ce@ZrPs) were prepared. The novel Zn-Ce@ZrPs were characterized and the antibacterial activity on Gram-negative Escherichia coli and Gram-positive Staphylococcus aureus were tested. The results showed that zinc ions (Zn2+) or/and cerium ions (Ce3+) were combined with ZrP, and the Ce3+ was adsorbed on the surface of ZrP through hydrogen bonds, while Zn2+ intercalated into the interlayer of ZrP. Zn-Ce@ZrPs showed excellent synergistic antibacterial activity. When Zn2+/Ce3+ atomic ratio was 0.6, the Zn-Ce@ZrP3 showed the highest synergistic antibacterial efficiency, suggesting great potential application as antibacterial agents in microbial control.     

Relationships between nocturnal activity, parental ratings of daytime activity and measues from the Children's Sleep Behaviour Scale.

Monitored the nocturnal activity levels of 20 boys and 20 girls (mean age 10.46 yrs) from 12:00 AM to 6:00 AM over 2 consecutive nights in their homes. Frequency of sleep-related behaviors based on retrospective parental ratings was assessed by the Children's Sleep Behavior Scale (CSBS). Children who were rated high on sleep behaviors with an observable motor component were also more active during the night, thereby validating the motor subscale of the CSBS. Nocturnal activity was associated with another CSBS-derived sleep score that included items with positive affective content, such as laughing and smiling while asleep. Children who showed bedtime resistance behaviors and complained of difficulty going to sleep were not more active during the night. Gender, age, and parental perception of daytime activity levels were not related to objective measures of nocturnal activity. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Miocamycin. A review of its antimicrobial activity, pharmacokinetic properties and therapeutic potential

Miocamycin is an orally administered 16-membered macrolide antimicrobial drug. It has a spectrum of in vitro activity similar to that of erythromycin, inhibiting a range of Gram-positive and Gram-negative organisms, atypical microbes and some anaerobes. Importantly, miocamycin demonstrates greater in vitro potency than erythromycin against several pathogens including Legionella pneumophila, Mycoplasma hominis, and Ureaplasma urealyticum. Equally noteworthy is its activity against erythromycin-resistant staphylococcal and streptococcal species expressing inducible-type resistance. Miocamycin possesses poor overall activity against Haemophilus influenzae and is inactive against Enterobacteriaceae. Penetration of miocamycin into body tissues and fluids is both rapid and extensive. The 3 major metabolites of miocamycin possess antimicrobial activity and may contribute to the therapeutic efficacy of the drug. Clinical data indicate that miocamycin is useful in the treatment of upper and lower respiratory tract infections in both adult and paediatric patients. Miocamycin is also effective in the treatment of urogenital tract infections caused by Chlamydia trachomatis or U. urealyticum. Several studies suggest that miocamycin is at least as effective as erythromycin in these indications; however, comparisons with newer macrolide agents have yet to be performed. In other studies, miocamycin proved to be a useful agent in the treatment of periodontal infections and as anti-infective prophylaxis in dental surgery. Miocamycin appears to have a tolerability profile qualitatively similar to that of other macrolides, with gastrointestinal and skin disorders being the most commonly reported adverse events. Current data suggest that the potential for drug interactions with miocamycin is low, with the possible exceptions of carbamazepine and cyclosporin. Thus, although further confirmation and elaboration of various aspects of its efficacy and tolerability profile is needed, at this stage miocamycin offers a useful alternative oral therapy to erythromycin for the treatment of uncomplicated community-acquired respiratory tract infections and nongonococcal urethritis.     

Synthesis, characterization, cytotoxicity, DNA cleavage and antimicrobial activity of homodinuclear lanthanide complexes of phenylthioacetic acid

Lanthanide complexes of Eu(III), Gd(III), Nd(III), Sm(III), and Tb(III) with phenylthioacetic acid were synthesized and characterized by elemental analysis, mass, infrared radiation (IR), electronic sp...     

Structure-activity relationships of protoberberines having antimicrobial activity

13-Alkyl derivatives (2-6 and 8-12) of berberine (1) and palmatine (7) were subjected to in vitro antibacterial activity tests against Bacillus subtilis and Salmonella enteritidis. Antibacterial activity increased as the length of the C-13 aliphatic side chain increased. The effects of the oxygen-substituents on aromatic rings A, C, and D of protoberberinium salts 13-20 on the antimicrobial activity against Staphylococcus aureus, B. subtilis, S. enteritidis, Escherichia coli, and Candida albicans are also discussed. The change in lipophilicity of the protoberberinium salts caused by modification of the substituents appears to influence the antibacterial activity. 13-Hexylberberine (6) and 13-hexylpalmatine (12) exhibited the greatest antibacterial activity.     

Antiendotoxin activity of cationic peptide antimicrobial agents

The endotoxin from gram-negative bacteria consists of a molecule lipopolysaccharide (LPS) which can be shed by bacteria during antimicrobial therapy. A resulting syndrome, endotoxic shock, is a leading cause of death in the developed world. Thus, there is great interest in the development of antimicrobial agents which can reverse rather than promote sepsis, especially given the recent disappointing clinical performance of antiendotoxin therapies. We describe here two small cationic peptides, MBI-27 and MBI-28, which have both antiendotoxic and antibacterial activities in vitro and in vivo in animal models. We had previously demonstrated that these peptides bind to LPS with an affinity equivalent to that of polymyxin B. Consistent with this, the peptides blocked the ability of LPS and intact cells to induce the endotoxic shock mediator, tumor necrosis factor (TNF), upon incubation with the RAW 264.7 murine macrophage cell line. MBI-28 was equivalent to polymyxin B in its ability to block LPS induction of TNF by this cell line, even when added 60 min after the TNF stimulus. Furthermore, MBI-28 offered significant protection in a galactosamine-sensitized mouse model of lethal endotoxic shock. This protection correlated with the ability of MBI-28 to reduce LPS-induced circulating TNF by nearly 90% in this mouse model. Both MBI-27 and MBI-28 demonstrated antibacterial activity against gram-negative bacteria in vitro and in vivo against Pseudomonas aeruginosa infections in neutropenic mice.     

Synthesis and antimicrobial activity of a dihydroampicillin and a dihydrocephalexin

A dihydroampicillin (3) and a dihydrocephalexin (4) have been synthesized by condensing alpha-(cyclohexa-1, 3-dienyl)glycyl chloride with 6-aminopenicillanic acid (1) and 7-deacetoxycephalosporanic acid (2) respectively. The two antibiotics obtained show enhanced antimicrobial activity towards certain bacterial strains compared with ampicillin and cephalexin.     

Organotin complexes with pyrrole-2-carboxaldehyde monoacylhydrazones. Synthesis, spectroscopic properties, antimicrobial activity, and genotoxicity

The Council on Quality and Leadership in Supports for People With Disabilities (The Council), formerly known as The Accreditation Council, altered its definition of quality from "compliance with organizational process" to "responsiveness to people." Council representatives conducted focus group and individual meetings with people who have disabilities to identify priority outcomes they expect from services and supports. The 1993 Outcome Based Performance Measures was used in 447 interviews as part of 54 accreditation reviews. Staff analysis and factor analysis of the outcome interviews using a principle components extraction and varimax rotation resulted in 24 variables loading onto seven major factors (Identity, Autonomy, Affiliation, Attainment, Rights, Health, and Safeguards), which form the basis of The Council 1997 Personal Outcome Measures.     

Fluconazole. An update of its antimicrobial activity, pharmacokinetic properties, and therapeutic use in vaginal candidiasis

Fluconazole is a bis-triazole antifungal drug which has a pharmacokinetic profile characterised by its high water solubility, low affinity for plasma proteins, and metabolic stability. After a single 150 mg oral dose, therapeutic concentrations in vaginal secretions are rapidly achieved and are sustained for a duration sufficient to produce high clinical and mycological responses in nonimmunocompromised patients with vaginal candidiasis (candidosis). At this dosage, clinical and mycological responses have compared favourably with responses achieved after multiple dose regimens of other oral and intravaginal antifungal agents. Clinical efficacy rates have ranged between 92 and 99% at short term evaluation (5 days post-treatment). At 80 to 100 days post-treatment clinical efficacy rates of 91% have been reported. In addition, limited data indicate that fluconazole is more effective than placebo as prophylactic treatment of frequently recurring vaginal candidiasis. Single oral doses of fluconazole 150 mg are well tolerated. Most frequently observed adverse events are gastrointestinal symptoms, which are generally mild and transient in nature. Thus, fluconazole is a valuable alternative to established systemic and intravaginal azole antifungal drugs which are used to treat vaginal candidiasis. Moreover, in view of its favourable patient acceptability and compliance profile compared with alternative treatments, single-dose oral fluconazole should be considered as a first-line therapeutic choice for the treatment of women with vaginal candidiasis.     

Synthesis and antimicrobial evaluation of indole containing derivatives of 1,3,4-thiadiazole, 1,2,4-triazole and their open-chain counterparts

1. We have studied L-valine transport by the caecal segments of 6- to 8-week-old chickens. Isolated enterocytes from the proximal caecum incubated with 0.1 mM L-valine can accumulate the substrate against a concentration gradient. After 50 min incubation, the intracellular L-valine concentration reached 0.53 mM, a value higher than that observed in enterocytes from the jejunum (0.34 mM; P< 0.01). 2. Enterocytes from the medial and distal caccal regions are unable to transport L-valine uphill (cell concentration: 0.1 mM). 3. Amino acid accumulation by proximal caecal cells was Na+ -dependent and was inhibited by ouabain and 2,4-dinitrophenol. L-methionine inhibits L-valine uptake and a 2.5 mM concentration abolishes the capacity of enterocytes to accumulate the substrate. 4. The high accumulation ratios shown by the proximal caecum for L-valine suggest a role for this intestinal segment in the absorption of neutral amino acids present in the caecal chamber.     

A one-year survey of respiratory and urinary pathogens and their antimicrobial susceptibility

Human cytomegalovirus (CMV) infection is often associated with myelosuppression and acute inflammatory reaction in immunocompromised patients. We have previously documented that CMV exposure of bone marrow (BM) stromal cells reduces the capacity of these cells to support hematopoiesis because of a decreased production of colony-stimulating factors. This study examines the potential role of CMV on constitutive and lipopolysaccharide (LPS)-stimulated production of cytokines involved in inflammatory reaction, interleukin-6 (IL-6) and leukemia inhibitory factor (LIF) by BM stromal cells. The release of IL-6 was already detectable 2 hours post CMV-infection (2.5-fold increase in production) and the cumulative production of IL-6 after 5 days of infection was 23 +/- 1.2 ng/mL (ninefold increase in production). CMV was also able to induce a time-dependent production of LIF that was maximal 8 hours after CMV infection (2.5-fold increase in production). Concomitantly, there was no detectable release of granulocyte colony-stimulating factor (G-CSF) and granulocyte-macrophage CSF (GM-CSF) by CMV-infected stromal cells. The similar IL-6 and LIF production in the presence of polymyxin B ruled out the possibility that this increase could be caused by contamination of the viral stock by endotoxin. In addition, ultraviolet-inactivated virus behaved similarly to live virus and caused the release of IL-6 and LIF. However, heat-inactivated CMV was unable to induce IL-6 and LIF secretion by BM stromal cells. The production of IL-6 and LIF was also evaluated after stimulation by LPS. After 5 days of CMV exposure, the LPS-stimulated production of IL-6 and LIF was significantly lower than uninfected controls. This LPS-induced release of cytokine production was found to be dependent of viral replication. The experiments have shown that CMV is a potent inducer of IL-6 and LIF with differential effect on constitutive and LPS-stimulated cytokine production by stromal cells; we suggest that CMV induction of IL-6 and LIF during the first hours of infection could play a role in CMV-induced inflammatory reaction. Moreover, our results show that human CMV can disturb the balanced cytokine network involved in the regulation of hematopoiesis.     

Synthesis, structure elucidation and antimicrobial activity of some 3-hydroxy-2-naphthoic acid hydrazide derivatives

In this study, some 1,4-disubstituted thiosemicarbazide, 1,2,4-triazole and 1,3,4-thiadiazole type novel compounds derived from 3-hydroxy-2-naphthoic acid hydrazide were synthesized to screen for their antimicrobial activity. The structures of these substances were elucidated using elemental analysis and UV, 1H NMR, and mass spectral methods. All of these compounds were tested in vitro for their antibacterial and antifungal activity.