The present in vitro study was designed to test and compare anthelmintic activity, hepatotoxicity, and biotransformation of four selected aminoacetonitrile derivatives (AADs): monepantel (MOP, anthelmintic approved for the treatment), AAD-970, AAD-1154, and AAD-1336. Micro-agar larval development test, MTT test of cytotoxicity, and biotransformation study coupled with Ultra high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) technique were used for this purpose. Larvae of two Haemonchus contortus strains (drug susceptible and multi-drug resistant) and primary cultures of rat and ovine hepatocytes served as model systems. All AADs (including MOP) exhibited significant larvicidal effect in H. contortus susceptible as well as multi-resistant strains, much higher than those of reference anthelmintics thiabendazole and flubendazole. AAD-1154 provides the best results for most tested parameters among all AADs in this study. The cytotoxicity test showed that all AADs can be considered as nontoxic for hepatocytes. In the biotransformation study, Phase I and Phase II metabolites of AADs were identified and schemes of possible metabolic pathways in ovine hepatocytes were proposed. Biotransformation of MOP was much more extensive than biotransformation of other AADs. Based on obtained results, AAD-1154 and AAD-1336 can be considered as promising candidates for further in vivo testing.
- MeSH
- aminoacetonitrily analogy a deriváty analýza farmakokinetika toxicita MeSH
- anthelmintika analýza farmakokinetika toxicita MeSH
- biotransformace MeSH
- Haemonchus účinky léků MeSH
- hepatocyty metabolismus MeSH
- krysa rodu rattus MeSH
- kultivované buňky MeSH
- larva MeSH
- mebendazol analogy a deriváty analýza farmakokinetika MeSH
- ovce MeSH
- potkani Wistar MeSH
- tandemová hmotnostní spektrometrie MeSH
- thiabendazol analýza farmakokinetika MeSH
- vysokoúčinná kapalinová chromatografie MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- srovnávací studie MeSH
- MeSH
- amébiáza farmakoterapie MeSH
- antibakteriální látky farmakologie klasifikace MeSH
- antinematodní látky MeSH
- antiparazitární látky * farmakokinetika farmakologie klasifikace MeSH
- Apicomplexa MeSH
- cestodózy farmakoterapie MeSH
- cysticerkóza farmakoterapie MeSH
- dítě MeSH
- dospělí MeSH
- echinokokóza farmakoterapie MeSH
- giardiáza farmakoterapie MeSH
- helmintóza farmakoterapie klasifikace MeSH
- ivermektin farmakologie MeSH
- lidé MeSH
- nitrofurany klasifikace terapeutické užití MeSH
- nitroimidazoly klasifikace terapeutické užití MeSH
- oxychinolin analogy a deriváty MeSH
- parazitární nemoci * farmakoterapie patofyziologie MeSH
- protozoální infekce farmakoterapie MeSH
- pyrimethamin MeSH
- směrnice pro lékařskou praxi jako téma MeSH
- sulfadiazin MeSH
- svrab farmakoterapie MeSH
- thiabendazol farmakologie MeSH
- thiazoly MeSH
- Toxoplasma MeSH
- toxoplazmóza farmakoterapie klasifikace MeSH
- trichinelóza farmakoterapie MeSH
- trichomoniáza farmakoterapie MeSH
- Check Tag
- dítě MeSH
- dospělí MeSH
- lidé MeSH
- Publikační typ
- přehledy MeSH
In this contribution we present an innovative way to easy, fast, and highly sensitive analyses by CE with ESI-MS detection. The new method is designed to be applied to ESI-compatible electrolytes (e.g. ammonium acetate) and offers advanced tuning of selectivity conditions within a wide range of analyte mobilities. We use a full capillary ITP format to provide powerful on-line analyte stacking at the ITP boundary all the way to detection and introduce the model of extended ITP where a controlled concentration of the leading ion is added to the terminating zone. Such systems preserve all properties of an ITP system and the velocity of the stacking ITP boundary can be tuned by the composition of both the leading and terminating zone. In this way, the system properties can be controlled flexibly and the mobility window of stacked analytes can be tailored to actual needs. The presented theory and the newly defined concept of zone-related boundary mobility allow easy assessment of system selectivity using simple diagrams. We demonstrate the model and its potential on the example of simple acidic cationic systems composed of only two substances (ammonium and acetate) including the example of thiabendazole analysis with a detection limit of 10(-10) M (20 ng/L) and its determination in orange juice by direct sampling after filtration, selective stacking by a tuned extended ITP system, and ESI-MS detection.
- MeSH
- acetáty chemie MeSH
- elektroforéza kapilární metody MeSH
- elektrolyty chemie MeSH
- hmotnostní spektrometrie s elektrosprejovou ionizací metody MeSH
- izotachoforéza metody MeSH
- kationty analýza chemie MeSH
- limita detekce MeSH
- nápoje analýza MeSH
- pomerančovník čínský chemie MeSH
- rezidua pesticidů analýza chemie MeSH
- thiabendazol analýza chemie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
A rapid strip test for semiquantitative or quantitative screening of thiabendazole in some fruit foods (fruits, fruit juices, baby foods) was developed, which is based on la¬teral flow immunoassay (LFIA). Test parameters such as membranes and buffers types, the amount and type of antibodies for labeling with gold nanoparticles, and dilution of gold-labeled antibodies and samples were optimized. The strip contains all the necessary reagents dried on membranes. The test can be accomplished within 10 min. The visual limit of detection was 2 ng ml1. For quantitative assessment a standard curve of LFIA was produced with detection limit of 0.1±0.02 ng ml1, the IC50 value of 2.2 ng ml1, and the linear working range of 0.420 ng ml1. In the test, spiked samples were analyzed. Samples of fruit juices or fruit homogenate filtrates were diluted with buffer and analysed directly without any purification. The coefficients of interassay variation were below 16 %, with recoveries ranging from 91 to 112 %. The proposed LFIA test enables a sensitive, rapid, and facile on-site screening of thiabendazole.
There is increased interest in the investigation and implementation of rapid screening methods for detection of pesticide residues. This study reports development of an immunostrip test for thiabendazole detection based on indirect competitive principle using carbon particles as a label. Nitrocellulose membrane strip was coated with a thiabendazole-protein conjugate in the defined test zone. In flow of an antibody-carbon complex and thiabendazole along the strip, the intensity of black colour formed in the test line reflected the thiabendazole concentration and semi-quantitative estimation could be carried out visually. The optimized test was accomplished within 10 min and the visual detection limit was achieved 0.25 ng mL(-1) of standard sample. Moreover, immunostrip was evaluated quantitatively using scanning densitometry. Based on standard curve, the detection limit of the proposed test was as low as 0.08+/-0.03 ng mL(-1) with an IC(50) value of 0.60+/-0.08 ng mL(-1) and a linear working range of 0.11-4.13 ng mL(-1). Results of testing precision, stability, and specificity demonstrated that the assay provided a reliable performance. This immunostrip was applied to analysis of spiked fruit juices in range of 0.05-5 mg L(-1). Matrix interferences were avoided by simple dilution of samples. Both visual and instrumental evaluations indicated a good agreement with results obtained by ELISA. Recoveries from juices were from 81.9 to 123.6% and relative standard deviations ranged from 9.9 to 19.3%. The developed strip offers potential as a useful rapid and simple method for screening of thiabendazole in fruit juices at levels far below the maximum residue limits.
- MeSH
- biosenzitivní techniky přístrojové vybavení normy statistika a číselné údaje MeSH
- ELISA MeSH
- imunoanalýza přístrojové vybavení normy statistika a číselné údaje MeSH
- koloidy MeSH
- kontaminace potravin analýza MeSH
- lidé MeSH
- maximální přípustná koncentrace MeSH
- nápoje analýza MeSH
- ovoce chemie MeSH
- protilátky MeSH
- rezidua pesticidů analýza imunologie MeSH
- thiabendazol analýza imunologie MeSH
- uhlík MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- hodnotící studie MeSH
- práce podpořená grantem MeSH
- srovnávací studie MeSH
Autorka popisuje případ u nás zatím vzácně se vyskytující kožní choroby způsobené larvami nematodů, nejčastěji Ankylostoma brasiliense. Onemocnění bylo importováno z Brazílie a úspěšně zhojeno po perorální léčbě albendazolem.
A case of rare skin disease in Czech Republic caused by nematode larva is presented. The disease is most frequently caused by Ankylostoma brasiliensis and was imported from Brazil. It was successfully treated by peroral therapy with albendazol.
- Klíčová slova
- Mectizan,
- MeSH
- albendazol aplikace a dávkování terapeutické užití MeSH
- antihistaminika terapeutické užití MeSH
- ivermektin aplikace a dávkování terapeutické užití MeSH
- larva migrans diagnóza terapie MeSH
- lidé MeSH
- parazitární onemocnění kůže diagnóza etiologie terapie MeSH
- thiabendazol aplikace a dávkování terapeutické užití MeSH
- tropické lékařství MeSH
- Check Tag
- lidé MeSH
- MeSH
- finanční podpora výzkumu jako téma MeSH
- hepatocyty enzymologie účinky léků MeSH
- lidé MeSH
- mebendazol farmakologie MeSH
- omeprazol farmakologie MeSH
- protinádorové látky MeSH
- protivředové látky MeSH
- systém (enzymů) cytochromů P-450 enzymologie krevní zásobení MeSH
- thiabendazol farmakologie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- srovnávací studie MeSH
