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PubMed2003

Evaluation of the effect on arthropod populations by using deltamethrin to control Phloeotribus scarabaeoides Bern. (Coleoptera: Scolytidae) in olive orchards.

Field tests were made for the control of an olive insect pest, the olive bark beetle, Phloeotribus scarabaeoides (Col: Scolytidae), using the pyrethroid insecticide deltamethrin (D) and this insecticide combined with ethylene (D+E), an attractant of the olive bark beetle. The tests were run in olive orchards in the provinces of Granada and Jaén (Andalusia, southern Spain), treating several olive rows so as to create a barrier effect to control the pest attack. The main objective was to evaluate the arthropod fauna affected by these treatments. The different taxa captured have been separated in three different trophic groups: parasitoids, predators and phytophagous. A knock-down effect was found during the first dates in all the functional groups in all cases. The results showed the following trend in arthropod abundance: D+E>D>C. This trend was significant (p<0.05) for predators and phytophagous insects in both zones. The parasitoids of Prays oleae (Lep.: Plutellidae), a major olive pest, were most affected by the treatments, together with several groups of predators such as ants, cantharids, coccinellids and mirids. Data from the captures show the need to determine the optimum time for insecticide application in order to minimise its effect on beneficial insect populations.

Agriculture↗
PubMed1988

[In vitro bactericidal effects of ofloxacin on S. aureus].

Two Staphylococcus aureus (S. aureus) strains with differing susceptibility to penicillin G as expressed by the minimum inhibitory concentration were exposed in vitro over a period of 8 h to the continuously changing concentrations of ofloxacin achieved in human serum and cantharides blister fluid (CBF) after the single oral application of 600 mg. In both strains bacterial density was rapidly, but not totally reduced: a reduction by 99 percent took no longer than about 1 and 1.5 h resp. facing the serum level profile and about 1.5 h facing the tissue level profile. The maximum reduction of staphylococcal density in percent (kn) amounted to 0.0007 and 0.0034 and to 0.0038 and 0.0047 resp. Thus not only the serum level profiles but also the skin tissue level profiles obtainable in man proved highly effective in vitro against S. aureus irrespective of the bacterial suspectibility against penicillin G. Therefore oral ofloxacin should prove useful in staphylococcal diseases especially in so far as cutaneous tissue is involved.

Humans↗
PubMed1999

2-Carboxymethylendothal analogues as affinity probes for stabilized protein phosphatase 2A.

Endothal (1diacid) and [3H]cantharidic acid ([3H]CA) bind with high affinity to the catalytic subunit of protein phosphatase 2A (PP2A). PP2A in liver cytosol was greatly stabilized with 30% glycerol as a preliminary step in the potential use of endothal-type derivatives for affinity chromatography. We report here the first introduction of a functionalizable group into endothal which allows retention of binding site affinity (assayed as [3H]CA binding in mouse liver cytosol). 2-Carboxymethylendothal anhydride (7) was prepared in two steps and 97% overall yield from cis-aconitic anhydride and furan. The potency of 7 was retained on conversion to two 2-carboxymethyl esters but not to two 2-(n-alkylcarboxamidomethyl) analogues.

Affinity Labels↗
PubMedDate not supplied

A fast and sensitive technique to study the kinetics and the concentration dependencies of DNA fragmentation during drug-induced apoptosis.

Apoptotic cell death with its characteristic coordinated cellular breakdown can be triggered by cytotoxic drugs. One prominent feature that differentiates apoptotic from necrotic cell death is the caspase-mediated activation of an endonuclease that internucleosomally cleaves DNA resulting in the so-called apoptotic DNA ladder. Here we report a new rapid, sensitive and inexpensive column separation technique to study drug-induced DNA fragmentation from 10(6) or less cells. This technique, which is based on a modified plasmid spin column kit, avoids the use of hazardous chemicals. With this procedure and subsequent densitometric analysis it was possible to study the concentration dependencies and the kinetics of drug-induced DNA fragmentation. The applicability of this technique is shown for okadaic acid- and cantharidic-acid-treated pituitary GH(3) cells as well as highly okadaic-acid-resistant sublines. These studies allowed us to compare as well as to differentiate the effects and potencies of these structurally different but functionally quite similar inhibitors of ser/thr phosphatases 1 and 2A.

Animals↗
PubMed1996

Tyrosine-272 is involved in the inhibition of protein phosphatase-1 by multiple toxins.

Protein phosphatase-1 (PP1) is regulated by interaction with different subunits, which include several inhibitory proteins. It is also potently inhibited by several toxins of diverse origins. Recent work has identified a region near the C-terminus of PP1 (residues 274-277) whose modification was shown to moderate okadaic acid binding [Zhang et al. (1994) J. Biol. Chem. 269, 16997-17000]. In this study, the role of this region in toxin binding was explored by site-directed mutagenesis. A residue (Tyr-272) was identified whose mutation had dramatic effects on the spectrum of inhibitor sensitivity of PP1. The IC50's of a number of mutants of Tyr-272 toward okadaic acid, tautomycin, calyculin A, microcystin-LR, nodularin, inhibitor-2, and cantharidic acid were determined and compared to that of the wild-type enzyme. The sensitivity of PP1 toward tautomycin and calyculin A was markedly decreased, by as much as 3 orders of magnitude, with lesser effects on okadaic acid and nodularin, and with microcystin-LR and inhibitor-2 being the least affected. These studies show that Tyr-272 is of specific importance for the binding of these inhibitors and provide strong evidence for the postulate that these toxins all bind to a common inhibitor site on PP1. In addition, our studies show that Tyr-272 is not required for catalytic activity.

Amino Acid Sequence↗
PubMed2000

Hamster pancreatic beta cell lines with altered sensitivity towards apoptotic signalling by phosphatase inhibitors.

Specific inhibitors of serine/threonine phosphatases like okadaic acid can induce apoptotic cell death in the pancreatic beta cell line HIT. Cultivation in stepwise increased concentrations of okadaic acid enabled the isolation of HIT100R cells which proliferate at 100 nM okadaic acid (8 - 10 times the initially lethal concentration). These two cell lines were used to characterize the events triggered by okadaic acid that led to apoptosis. Biochemical markers, e.g. cytochrome c release from mitochondria and increase of caspase-3-like activity, revealed that induction of apoptosis by 100 nM okadaic acid in parental HIT cells started with the release of cytochrome c. In HIT100R cells 500 nM okadaic acid were necessary to induce alterations comparable to those observed with 100 nM okadaic acid in non-resistant HIT cells. In contrast to okadaic acid, the potency of the structurally different phosphatase inhibitor cantharidic acid to induce cytochrome c release, increase of caspase-3-like activity and DNA fragmentation was comparable in HIT and HIT100R cells. Thus, no cross-resistance between these phosphatase inhibitors seemed to exist. Phosphatase activity in extracts from HIT and HIT100R cells did not differ in its total amount or in its sensitivity for okadaic acid. Since higher concentrations of okadaic acid were needed to induce apoptosis in HIT100R cells, a compromised intracellular accumulation of the toxin appeared likely. Functional and structural analysis revealed that this was achieved by the development of the multidrug resistance phenotype in HIT100R cells. The underlying mechanism appeared to be the enhanced expression of the pgp1 but not the pgp2 gene.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed1980

The influence of protein binding upon tissue fluid levels of six beta-lactam antibiotics.

The effect of protein binding upon the penetration of six-beta-lactam (three penicillins and three cephalosporins) antibiotics into tissue fluid was studied in humans. A cantharides blister technique was used. It was found that there was a linear relationship between the percentage of protein binding and the penetration into the blister fluid of the antibiotic as measured by the area under the curve of the protein-free fraction. This finding is further evidence that protein binding may have important influence upon the likely efficacy of an antimicrobial agent.

Adult↗
PubMed1984

The pharmacokinetics and tissue penetration of norfloxacin.

The pharmacokinetics and cantharides-induced blister fluid levels of norfloxacin were studied after a single 400 mg oral dose. The mean maximum serum level was 1.45 mg/l and occurred 1.5 h after administration. The serum half-life of norfloxacin was found to be 3.5 h. After 24 h 27% of the administered dose was recovered in the urine as microbiologically active compound. High urine levels were found. Rapid blister fluid penetration occurred, the maximum level (occurring between 2-3 h) was about 1 mg/l. Thereafter the blister fluid level exceeded the serum level, both declining in parallel.

Adult↗
PubMed1984

The pharmacokinetics of orally absorbed cefuroxime compared with amoxycillin/clavulanic acid.

The pharmacokinetics of a new orally absorbed pro-drug of cefuroxime were compared with those of co-administered amoxycillin and clavulanic acid in six healthy male volunteers. Doses of 600 mg of acetoxyethyl cefuroxime and 500 mg amoxycillin plus 250 mg clavulanic acid were each administered for ten doses 8 hourly. Tissue penetration after the first dose of the antibiotic was estimated by a cantharides blister method. The faecal flora of the volunteers was studied throughout the study. The pharmacokinetics of cefuroxime and amoxycillin were very similar, peak levels of about 6.4 mg/l being found between 2 and 2.5 h after administration. The peak serum level of clavulanic acid was 4.3 mg/l at 1.25 h after administration. The serum half-lives were about 1.1 h for all three agents. No drug accumulation occurred over the four days of the study. The 0-8 h urinary recovery of cefuroxime was 30%. All three agents penetrated the blister fluid rapidly, the main peak levels being 64% of the peak serum level for cefuroxime, 72% for amoxycillin and 55% for clavulanic acid. The incidence of side effects was similar for each regimen. Three volunteers having diarrhoea after cefuroxime showed significant alterations in their bowel flora.

Adult↗
PubMed1989

Cefixime, in-vitro activity, pharmacokinetics and tissue penetration.

The in-vitro activity of cefixime was studied with clinical isolates and compared with that of other agents. Cefixime exhibited good activity against the Enterobacteriaceae, Haemophilus influenzae, and Neisseria gonorrhoeae, including beta-lactamase producing strains. Activity was also high against Streptococcus pneumoniae and group A and group B beta-haemolytic streptococci. Staphylococcus aureus, faecal streptococci, anaerobic bacteria and Pseudomonas aeruginosa were not susceptible. Activity against susceptible isolates was comparable to cefotaxime and was normally superior to cefuroxime, cephalexin and amoxycillin. The pharmacokinetics of cefixime were studied in six healthy male volunteers, each receiving a 400 mg oral dose following an overnight fast. Tissue penetration of the antibiotic was estimated with a cantharides-induced blister method. The mean serum elimination half-life was 3.8 h, the mean peak concentration was 3.7 mg/l. Penetration into tissue fluid was rather slow [Tmax 6.7 h) but percentage penetration was high (132.6%). Urinary excretion was low with a 24 h recovery rate of less than 20%, though the concentrations achieved in urine exceeded the MICs of most common urinary tract pathogens for up to 24 h post-dose.

Adult↗
PubMed1990

The pharmacokinetics and inflammatory fluid penetration of orally administered azithromycin.

The pharmacokinetics of azithromycin were determined during a 24 h period following oral administration of a single 500-mg dose to each of six male volunteers. Concentrations in serum, urine and cantharides-induced inflammatory fluid were determined by microbiological assay. The mean peak serum concentration of 0.45 mg/l was obtained at a mean time of 2.6 h post-administration. The elimination half-life from serum was seen to increase with time post-dose; the mean elimination half-life at 16 h post-dose was 9.6 h. Inflammatory fluid was penetrated rapidly, with the mean peak concentration of 0.13 mg/l achieved at a mean time of 3.25 h post-dose. After this peak, levels initially decreased, but after 8 h from drug administration until the end of the trial period, inflammatory fluid concentrations remained relatively constant. The mean inflammatory fluid penetration up to the end of the study period was 74%. The mean urinary recovery of azithromycin, during the initial 24 h post-dose, was 6%.

Administration, Oral↗
PubMed1994

The comparative pharmacokinetics and tissue penetration of single-dose ciprofloxacin 400 mg i.v. and 750 mg po.

The pharmacokinetics of ciprofloxacin following single doses of 400 mg i.v. and 750 mg po were compared in six healthy volunteers. Concentrations of ciprofloxacin were measured in plasma, cantharides induced blister fluid and urine, by microbiological assay and high performance liquid chromatography (HPLC). Mean peak plasma concentration was 6.7 +/- 1.4 mg/L after i.v. and 3.9 +/- 1.7 mg/L after oral administration with mean elimination half-lives of 4.2 and 4.0 h respectively. Mean area under the concentration versus time curve (AUC) was greater following oral administration (19.2 +/- 1.1 mg/L.h versus 14.2 +/- 1.1 mg/L.h). Blister fluid peak concentrations following i.v. and oral administration were 2.6 +/- 1.3 mg/L and 2.28 +/- 1.2 mg/L respectively. The elimination half-life from blister fluid was 4.1 +/- 1.1 h and the AUC 13.8 +/- 1.1 mg/L.h following i.v. administration compared with 4.6 +/- 1.5 h and 20.3 +/- 1.3 mg/L.h for the oral dose. A mean of 50.8% of i.v. administered drug and 39.6% or orally administered drug was excreted in urine in 24 h as measured by HPLC. The corresponding values by microbiological assay were greater, suggesting excretion of active metabolites. Both i.v. and oral doses produced levels in blister fluid concentration above the MICs for most Enterobacteriaceae, Pseudomonas aeruginosa, Haemophilus influenzae and Neisseria spp. at 12 h post dose. The pharmacokinetic data from inflammatory fluid indicate that ciprofloxacin 400 mg i.v. is more equivalent to 750 mg po than the plasma pharmacokinetic data suggest.

Administration, Oral↗
PubMedDate not supplied

Childhood bullous pemphigoid: report of a case with life-threatening course during homeopathy treatment.

Bullous pemphigoid (BP) is an autoimmune blistering disorder that may very rarely occur in childhood. We describe a 9-month-old child who developed bullous pemphigoid while she was being treated for presumptive atopic eczema with a homeopathic regimen comprising sulfur, mercury, cantharides, and Rhus (Toxicodendron). She had generalized bullae and a progressive worsening of her general condition with asthenia, dehydration, malnutrition. While the role of homeopathy in triggering the disease remains unclear, our observation attests to the potential life-threatening course of childhood BP in instances where appropriate treatment is withheld.

Dermatitis, Atopic↗
PubMed1981

The effect of probenecid on the pharmacokinetics and distribution of cefoxitin in healthy volunteers.

1 Cefoxitin was given by acute intravenous injection to six healthy volunteers, in a crossover study to investigate the effects of concurrent probenecid administration. 2 Serum antibiotic concentrations were determined by microbiological assay. Cefoxitin concentrations were simultaneously determined in the fluid of blisters produced by topical cantharides. All antibiotic was accounted for in the urine. 3 Cefoxitin was administered by intravenous infusion, subsequent to a loading dose, to produce steady state levels in the region of 10 microgram/ml, in one volunteer. The procedure was later repeated after prior administration of probenecid in the same subject. 4 Pharmacokinetic analyses indicated significant changes only in the parameters associated with renal excretion of drugs. Clearance was reduced by half. 5 The absolute and relative amounts of antibiotic in the central and peripheral compartments were calculated for both modes of administration. In the acute study probenecid produced a small change in distribution away from the peripheral or tissue compartment, towards the central compartment. 6 There was no elevation of initial serum concentrations and sustained levels of antibiotic could be accounted for principally by retarded excretion produced by probenecid, with little contribution by alteration in the disposition of antibiotic. 7 The sustained serum levels of cefoxitin that resulted from its decreased excretion were also reflected in blister fluid. It was concluded that the sustained cefoxitin levels produced by probenecid resulted in similar raised levels in the peripheral or "tissue' compartment, since the redistribution away from the peripheral compartment did not contribute materially to other changes in disposition of drug.

Adult↗
PubMed2005

Osseous lesion of the calcaneus following the use of shock wave therapy in a horse.

An 8-year-old Dutch warmblood gelding was presented with a mechanical lameness (2/10) because of the presence of a soft tissue injury on the top of the right tuber calcanei. Plain radiographs of the tarsus demonstrated the presence of soft tissue swelling caudal to the right tuber calcanei, without osseous involvement, and ultrasonography revealed excessive scar tissue within and around the superficial digital flexor tendon. Extra-corporeal shock wave therapy was applied on the right hock to decrease the amount of scar tissue. One month after the therapy the lameness was greater (3/10) and a marginal increase in the size of the swelling was found. Periosteal new bone formation associated with an ill-defined radiolucent area and two bony fragments were detected radiographically at the caudo-proximal aspect of the right tuber calcanei. A blister containing oil of croton, camphor, pine and thyme, turpentine and cantharides was applied on the right calcaneus. Twenty days after blister application, the size of the swelling had been reduced by 50% and the degree of lameness had also been decreased (1/10). On clinical re-evaluation 6 months after treatment, the degree of lameness was stable (1/10) and flexion test of the limb was negative.

Animals↗
PubMed1989

Skin blister fluid levels of ketoconazole during repetitive administration in healthy man.

Ketoconazole administered orally is used in the treatment of superficial and deep mycoses. To evaluate its active concentrations in skin tissue, serum, suction blister fluid (SBF), and cantharides blister fluid (CBF) levels of total and non-protein bound ketoconazole were determined. In general, only the free drug is considered to be the active one. Six healthy subjects received 200 mg once daily for 5 days. Total ketoconazole concentrations were determined by HPLC. The unbound fractions of ketoconazole in SBF (2.3%) and CBF (1.2%) were calculated from plasma protein binding (99.0%). Before the ultimate dose, levels of unbound ketoconazole in SBF and CBF were 0.64 +/- 0.16 and 0.70 +/- 0.25 ng/ml and were thus in accordance with free ketoconazole serum levels (0.52 +/- 0.24 ng/ml; p greater than 0.05). Furthermore, following the ultimate dose, the areas under the blister fluid level-time curves of unbound ketoconazole did not differ from the respective areas under the serum level time curves, thus distribution equilibrium between serum and skin blister fluid was obtained. Peak concentrations of free ketoconazole were (SBF) 8.6 +/- 2.9 ng/ml and (CBF) 8.9 +/- 2.3 ng/ml. Free concentrations in SBF and CBF were far below the MIC values for dermatophytes and Candida ssp. reported in the literature, leaving the concentration-effect relationship of ketoconazole still open for discussion.

Adult↗
PubMed1980

Pharmacokinetics of Ro 13-9904, a broad-spectrum cephalosporin.

The pharmacokinetics of the new cephalosporin Ro-13-9904 were studied in six healthy male volunteers receiving a 500-mg dose as a bolus intravenously. Tissue penetration of the antibiotic was estimated by using a cantharides blister method. The data obtained fitted a two-compartment open model. The mean elimination half-life was about 8 h, which is considerably longer than that of other beta-lactam compounds. The distribution volume was 4.3 liters in the central compartment. Levels of Ro 13-9904 in blister fluid exceeded those in serum after 6.5 h. Approximately 60% of the antibiotic was excreted in the urine.

Adult↗