Biotransformation of anthelmintics and the activity of drug-metabolizing enzymes in the tapeworm Moniezia expansa

Parasitology ◽  
2014 ◽  
Vol 142 (5) ◽  
pp. 648-659 ◽  
Author(s):  
LUKÁŠ PRCHAL ◽  
HANA BÁRTÍKOVÁ ◽  
ANETA BEČANOVÁ ◽  
ROBERT JIRÁSKO ◽  
IVAN VOKŘÁL ◽  
...  
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
High Performance ◽  
Ex Vivo ◽  
Ultra Violet ◽  
Drug Metabolizing Enzymes ◽  
Glutathione S Transferase ◽  
Metabolizing Enzymes ◽  
Moniezia Expansa

SUMMARYThe sheep tapeworm Moniezia expansa is very common parasite, which affects ruminants such as sheep, goats as well as other species. The benzimidazole anthelmintics albendazole (ABZ), flubendazole (FLU) and mebendazole (MBZ) are often used to treat the infection. The drug-metabolizing enzymes of helminths may alter the potency of anthelmintic treatment. The aim of our study was to assess the activity of the main drug-metabolizing enzymes and evaluate the metabolism of selected anthelmintics (ABZ, MBZ and FLU) in M. expansa. Activities of biotransformation enzymes were determined in subcellular fractions. Metabolites of the anthelmintics were detected and identified using high performance liquid chromatography/ultra-violet/VIS/fluorescence or ultra-high performance liquid chromatography/mass spectrometry. Reduction of MBZ, FLU and oxidation of ABZ were proved as well as activities of various metabolizing enzymes. Despite the fact that the conjugation enzymes glutathione S-transferase, UDP-glucuronosyl transferase and UDP-glucosyl transferase were active in vitro, no conjugated metabolites of anthelmintics were identified either ex vivo or in vitro. The obtained results indicate that sheep tapeworm is able to deactivate the administered anthelmintics, and thus protects itself against their action.

The activity of drug-metabolizing enzymes and the biotransformation of selected anthelmintics in the model tapeworm Hymenolepis diminuta

Parasitology ◽  
2012 ◽  
Vol 139 (6) ◽  
pp. 809-818 ◽  
Author(s):  
HANA BÁRTÍKOVÁ ◽  
IVAN VOKŘÁL ◽  
LENKA SKÁLOVÁ ◽  
VLADIMÍR KUBÍČEK ◽  
JANA FIRBASOVÁ ◽  
...  
Keyword(s):  
Drug Metabolism ◽  
Ex Vivo ◽  
Mass Spectrometric ◽  
Hymenolepis Diminuta ◽  
Drug Metabolizing Enzymes ◽  
Glutathione S Transferase ◽  
Methyl Derivative ◽  
Metabolizing Enzymes ◽  
Oxidative Metabolites

SUMMARYThe drug-metabolizing enzymes of some helminths can deactivate anthelmintics and therefore partially protect helminths against these drugs' toxic effect. The aim of our study was to assess the activity of the main drug-metabolizing enzymes and evaluate the metabolism of selected anthelmintics (albendazole, flubendazole, mebendazole) in the rat tapeworm Hymenolepis diminuta, a species often used as a model tapeworm. In vitro and ex vivo experiments were performed. Metabolites of the anthelmintics were detected and identified by HPLC with spectrofluorometric or mass–spectrometric detection. The enzymes of H. diminuta are able to reduce the carbonyl group of flubendazole, mebendazole and several other xenobiotics. Although the activity of a number of oxidation enzymes was determined, no oxidative metabolites of albendazole were detected. Regarding conjugation enzymes, a high activity of glutathione S-transferase was observed. A methyl derivative of reduced flubendazole was the only conjugation metabolite identified in ex vivo incubations of H. diminuta with anthelmintics. The results revealed that H. diminuta metabolized flubendazole and mebendazole, but not albendazole. The biotransformation pathways found in H. diminuta differ from those described in Moniezia expanza and suggest the interspecies differences in drug metabolism not only among classes of helminths, but even among tapeworms.

High-performance liquid chromatography/fluorescence detection of S -methylglutathione formed by glutathione- S -transferase T1 in vitro

2001 ◽  
Vol 74 (12) ◽  
pp. 760-767 ◽  
Author(s):  
Michael Müller ◽  
Michael Voss ◽  
Christian Heise ◽  
Thomas Schulz ◽  
Jürgen Bünger ◽  
...  
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
Fluorescence Detection ◽  
High Performance ◽  
Glutathione S Transferase

scholarly journals Phytochemical variability during vegetation of Chamerion angustifolium (L.) Holub genotypes derived from in vitro cultures

2021 ◽  
Author(s):  
Mariola Dreger ◽  
Katarzyna Seidler-Łożykowska ◽  
Milena Szalata ◽  
Artur Adamczak ◽  
Karolina Wielgus
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
High Performance ◽  
Array Detector ◽  
Reproduction Rate ◽  
Full Spectrum ◽  
Breeding Programs ◽  
Chamerion Angustifolium ◽  
Oenothein B

AbstractThe purpose of the study was to evaluate Chamerion angustifolium (L.) Holub genotypes for preliminary selection and further breeding programs aimed at obtaining a suitable industrial form for the pharmaceutical applications. Clonally propagated plants representing 10 genotypes of Ch. angustifolium were regenerated under in vitro conditions, hardened and planted in the field. Studies included an evaluation of shoot proliferation, phytochemical assessment of in vitro and ex vitro plants as well as investigations of intraspecies variability regarding four phenological stages: vegetative, beginning of blooming, full blooming, and green fruit phases. Quantitative and qualitative analyses of bioactive compounds were performed using high-performance liquid chromatography coupled with diode array detector and tandem mass spectrometer (HPLC–DAD–MS/MS) and high-performance liquid chromatography (HPLC) methods. The efficiency of shoot multiplication varied between genotypes from 8.12 to 21.48 shoots per explant. A high reproduction rate (> 20 shoots per explant) was recorded for four lines (PL_45, PL_44, PL_58, DE_2). Plants grown in vitro synthesized oenothein B (11.2–22.3 mg g−1 DW) and caffeic acid derivatives. Plants harvested from field contained the full spectrum of polyphenols characteristic for this species, and oenothein B and quercetin 3-O-glucuronide were the most abundant. The maximal content of oenothein B was determined in the vegetative phase of fireweed, while some flavonoids were found in the highest amount in full blooming phase. The results of analysis of variance indicated significant differences among genotypes in oenothein B, 3-O-caffeoylquinic acid and flavonoids accumulation in four phenological phases. PL_44 plants were characterized by high content of oenothein B and quercetin 3-O-glucuronide as well as a relatively high level of other flavonoids. Based on our phytochemical and micropropagation studies, PL_44 genotype was the best candidate for early selection and further breeding programs.

In vitro evaluation of the effect of nicotine, cotinine, and caffeine on oral microorganisms

2008 ◽  
Vol 54 (6) ◽  
pp. 501-508 ◽  
Author(s):  
Karina Cogo ◽  
Michelle Franz Montan ◽  
Cristiane de Cássia Bergamaschi ◽  
Eduardo D. Andrade ◽  
Pedro Luiz Rosalen ◽  
...  
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
High Performance ◽  
Culture Media ◽  
Bacterial Species ◽  
In Vitro Study ◽  
Bacterial Strains ◽  
Planktonic Cells ◽  
Susceptibility Tests

The aim of this in vitro study was to evaluate the effects of nicotine, cotinine, and caffeine on the viability of some oral bacterial species. It also evaluated the ability of these bacteria to metabolize those substances. Single-species biofilms of Streptococcus gordonii , Porphyromonas gingivalis , or Fusobacterium nucleatum and dual-species biofilms of S. gordonii – F. nucleatum and F. nucleatum – P. gingivalis were grown on hydroxyapatite discs. Seven species were studied as planktonic cells, including Streptococcus oralis , Streptococcus mitis , Propionibacterium acnes , Actinomyces naeslundii , and the species mentioned above. The viability of planktonic cells and biofilms was analyzed by susceptibility tests and time-kill assays, respectively, against different concentrations of nicotine, cotinine, and caffeine. High-performance liquid chromatography was performed to quantify nicotine, cotinine, and caffeine concentrations in the culture media after the assays. Susceptibility tests and viability assays showed that nicotine, cotinine, and caffeine cannot reduce or stimulate bacterial growth. High-performance liquid chromatography results showed that nicotine, cotinine, and caffeine concentrations were not altered after bacteria exposure. These findings indicate that nicotine, cotinine, and caffeine, in the concentrations used, cannot affect significantly the growth of these oral bacterial strains. Moreover, these species do not seem to metabolize these substances.

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