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PubMed2004

An in vitro larval motility assay to determine anthelmintic sensitivity for human hookworm and Strongyloides species.

With the implementation of programs to control lymphatic filariasis and soil-transmitted helminths using broad spectrum anthelmintics, including albendazole and ivermectin, there is a need to develop an in vitro assay for detection of drug resistance. This report describes an in vitro assay for measuring the effects of ivermectin and benzimidazoles on the motility of larvae of the hookworm species Ancylostoma ceylanicum, A. caninum, and Necator americanus, and Strongyloides species including Strongyloides stercoralis, and S. ratti. A dose-response relationship was demonstrated with each of the parasite species, with distinct differences observed between the various species. In pilot field testing of the assay with N. americanus larvae recovered from human fecal samples, a dose-response relationship was observed with ivermectin. While the assay has demonstrated the ability to determine drug responsiveness, its usefulness in resistance detection will require correlation with the clinical outcome among individuals infected with parasite strains showing different drug sensitivities.

Ancylostomatoidea↗
PubMed1991

[The threat of wide dissemination of anthelmintic resistance by veld ram performance testing units].

A veld ram performance testing unit consists of an association of stud or commercial ram breeders, who compare the performance of selected rams under field conditions on common pastures. The best performers are subsequently auctioned at public sales. To date, at least 10 Merino veld ram clubs have been established in various centres in South Africa. A strain of Haemonchus contortus, which was isolated from the pastures of one of these performance testing units, was found to be resistant to ivermectin, oxfendazole and rafoxanide. Closantel, levamisole and disophenol were more than 99% effective. The wide dispersal of the rams after testing, constitutes a potential danger for dissemination of helminths with resistant genes. Precautionary methods should include careful routine monitoring of drug susceptibility on the communal pastures, on the farms of individual members and thorough deworming of rams before they leave the testing unit. The prevention and control of resistance in such testing units are discussed, but it is emphasised that this is difficult, particularly if the worm strains on the communal grazing have become resistant to some of the anthelmintic groups.

Animals↗
PubMed1991

Study of the acetylcholinesterase activity of Ascaridia galli: kinetic properties and the effect of anthelmintics.

Acetylcholinesterase (EC 3.1.1.7) activity was demonstrated in whole worm homogenates of adult Ascaridia galli with acetylthiocholine as substrate. The pH optimum was not measurable because of an autohydrolysis of the substrate. The Michaelis constant (Km) was 4 mM with saturation by excess substrate. Optimum enzyme activity was noted at a protein concentration of 200 mg/ml assay medium and at a temperature of 37 degrees C. Arrhenius plot of temperature dependence of the enzyme activity showed an energy of activation (delta Ea) of 28.962 K joule/mole above, and 25.448 K joule/mole below, the transition temperature (37 degrees C). Complete inhibition by eserine (physostigmine), a specific and classical acetylcholinesterase inhibitor, established the identity of the enzyme. A marginally higher enzyme activity was observed in females than in males as well as in homogenates from worms of mixed sexes. The enzyme was markedly activated by divalent metal cations such as Fe2+, Mg2+, Cd2+, Cu2+, Zn2+ and Ca2+, while Co2+ and Mn2+ inhibited the activity. Piperazine adipate at a concentration of 10(-3) M caused 45.5% and albendazole, a benzimidazole anthelmintic, 37.5% inhibition in the enzyme activity, while levamisole and mebendazole proved to be practically ineffective, causing an inhibition of 12 and 9%, respectively.

Acetylcholinesterase↗
PubMedDate not supplied

[The effect of the anthelmintics biltricide and chloxyl on the level of cellular and humoral immunity in patients with chronic opisthorchiasis].

The effect of two anthelmintics--biltricide and chloxyl--on the immune status has been compared in patients with chronic opisthorchiasis. It has been established that in using chloxyl there is a more marked and persistent imbalance of immunoregulatory T-lymphocyte subpopulations (T mu-helpers-inducers and T gamma-suppressors-effectors).

Anthelmintics↗
PubMed1990

[Covalently bound residues: the case of anthelmintics].

In target species, most anthelmintics produce unextractable residues, which include covalently bound adducts, and a radioactive fraction, possibly incorporated into intermediary metabolism. Both are responsible for the very long half-life of total residues in tissues. Due to the analytical difficulties encountered in distinguishing between these two fractions and to the controversy about the toxicological significance of bound residues, discrepancies exist in the determination of withdrawal periods for a given drug. Withdrawal time varies from one country to another, depending upon the regulations of the different national agencies.

Animals↗
PubMed1990

Effect of anthelmintics and phenothiazines on adenosine 5'-triphosphatases of filarial parasite Setaria cervi.

S. cervi showed particulate bound Ca2+ ATPase and Na+,K(+)-ATPase activities while Mg2+ ATPase was detected in traces. ATPase of S. cervi was also differentiated from the nonspecific p-nitrophenyl phosphatase activity. Female parasite and microfilariae exhibited higher Ca2+ ATPase and Na+,K(+)-ATPase activities than the male adults and the enzyme Na+,K(+)-ATPase was mainly concentrated in the gastrointestinal tract of the filarial parasite. Na+,K(+)-ATPase of the filariid was ouabain-sensitive while Ca2(+)-ATPase activity was regulated by concentration of Ca2+ ions and inhibited by EGTA. Phenothiazines, viz. trifluoperazine, promethazine and chlorpromazine caused significant inhibition of Ca2+ ATPase and Na+,K(+)-ATPase. Diethylcarbamazine was a potent inhibitor of these ATPases. Mebendazole, levamisole and centperazine also caused significant inhibition of the ATPases indicating this enzyme system as a common target for the action of anthelmintic drugs.

Adenosine Triphosphatases↗
PubMedDate not supplied

Matrix solid phase dispersion isolation and liquid chromatographic determination of five benzimidazole anthelmintics in fortified beef liver.

A multiresidue method for isolation and liquid chromatographic determination of 5 benzimidazole anthelmintics (thiabendazole, oxfendazole, mebendazole, albendazole, and fenbendazole) in beef liver tissue is presented. Blank or benzimidazole-fortified liver samples (0.5 g) were blended with octadecylsilyl derivatized silica packing material (C18, 18% load, endcapped, 2 g). A column made from the C18/liver matrix was first washed with hexane (8 mL), following which the benzimidazoles were eluted with acetonitrile. The acetonitrile extract was then passed through an activated alumina column. The eluate contained benzimidazole analytes that were free from interfering compounds as determined by UV detection (photodiode array, 290 nm). Correlation coefficients of standard curves for individual benzimidazoles isolated from fortified samples, using internal standardization, were linear (0.996 +/- 0.002 to 0.999 +/- 0.001) with average relative percentage recoveries from 62.0 +/- 6.7 to 86.8 +/- 8.6% for the concentration range (100-3200 ng/g) examined. The interassay variability was 7.0 +/- 4.1 to 12.9 +/- 10.2% with an intra-assay variability from 2.2 to 4.0%.

Animals↗
PubMed1990

In vitro assessment of the activity of anthelmintic compounds on adults of Onchocerca volvulus.

The viability of adult Onchocerca volvulus and the effect of 12 known anthelmintic compounds on the parasites have been evaluated in an in vitro culture system. Three different parameters, a colorimetric assay, using NADH-dependent reduction of a tetrazolium salt to dark blue formazan by living adult worms, motility indices of male worms and lactate excretion of female worms were used to determine worm viability. The experiments showed that over a short term period of six days the viability of the worms did not decline significantly. The use of males isolated by dissection of whole nodules for the evaluation of drug effects in vitro is preferable to collagenase isolated worms. Mel W, milbemycin a and d, ivermectin, levamisole, CGP 6140 and, to a lesser extent, suramin immobilized male worms or significantly reduced the motility indices at a concentration of 10 microM. The tetrazolium reduction by male worms was not affected by levamisole, whereas the other active compounds demonstrated significant inhibitory effects. Diethylcarbamazine, mebendazole, flubendazole, metrifonate and CGP 20376 had no significant effect on male viability. Comparable activity was seen with the intact female worms isolated by collagenase digestion. Mel W, the milbemycins and ivermectin significantly inhibited tetrazolium reduction, whereas suramin and the other compounds had only slight or no inhibitory effects on female O. volvulus. Although one still has to aim at an improvement of the culture conditions, the in vitro test system using adult O. volvulus provides a basis for further research on potential antifilarial compounds.

Animals↗
PubMedDate not supplied

Molecular electrostatic potential-anthelmintic activity relationships of 5H-mebendazole and some related heterocyclic carbamates.

5H-Mebendazole and some related heterocyclic methyl carbamates were synthesized and their anthelmintic activity against Caenorhabditis elegans was determined. In order to study the influence of the heteroaromatic region with regard to the carbamate moiety on biological activity, the molecular electrostatic potentials (MEP) of all structures were calculated and a structure-activity relationship (SAR) was established. The electrostatic pattern of activity includes two minima of the carbamate moiety, a third heterocyclic minimum, and a pi-electronic region.

Animals↗
PubMed1989

Piperazine derivatives of benzimidazole as potential anthelmintics. Part 1: Synthesis and activity of methyl-5-(4-substituted piperazin-1-yl)benzimidazole-2-carbamates.

A series of 5-(4-substituted piperazin-1-yl)-2-nitroanilines (4) and 5-(4-substituted piperazin-1-yl)benzimidazole-2-carbamates (6) has been synthesized starting from 5-chloro-2-nitroaniline (3) and N-monosubstituted piperazines. Catalytic reduction of 4 with Pd/C followed by treatment with 1,3-dicarbomethoxy-S-methylisothiourea yielded the corresponding methyl-5-(4-substituted piperazin-1-yl)benzimidazole-2-carbamates (6) which were for anthelmintic activity against experimental infections of Trichinella spiralis.

Animals↗
PubMed1989

[Derivatives of thioallophanic acid with anthelmintic activity].

A reaction of potassium thiocyanate with methyl and ethyl ester of chloroformic acid (I-II) resulted in methoxy- and ethoxycarbonyl isothiocyanates which through an addition reaction with various primary and secondary amines, diamines and hydrazines yielded the perinently substituted esters of thioallophanic acid (III-XXI). The obtained agents were tested for anthelmintic and anticoccidial effects.

Animals↗
PubMed1989

South African field strains of Haemonchus contortus resistant to the levamisole/morantel group of anthelmintics.

A strain of Haemonchus contortus from the Pietermaritzburg district of Natal was found to be resistant to levamisole (geometric mean efficacy 76.5%), morantel (41.9%), the benzimidazoles (oxfendazole: 33.7%) and rafoxanide (82.0%), but apparently fully susceptible to closantel and disophenol. In the case of ivermectin, a mean of 5.2% of the H. contortus was not removed at a dosage of 200 micrograms kg-1 live mass. A second strain of H. contortus, from Amsterdam in the south-eastern Transvaal, showed reduced susceptibility to levamisole (80.8%) and morantel (46.2%), the only 2 drugs tested. This is apparently the first report of resistance to the levamisole/morantel group of anthelmintics in sheep in South Africa.

Animals↗
PubMed1989

Controlled test of anthelmintic activity of a macrocyclic lactone (compound F28249-alpha) in lambs.

A controlled blind test was performed in 1984 to evaluate the anthelmintic activity of experimental formulations of compound F28249-alpha against gastrointestinal parasites in lambs in Kentucky. Twenty-five lambs were allotted to 5 groups of 5 lambs/group. The drug was administered SC to 2 groups (A, 0.2 mg/kg of body weight; B, 0.3 mg/kg) and orally to 2 groups (C, 0.2 mg/kg; D, 0.3 mg/kg). Group E received a placebo subcutaneously. Lambs were euthanatized 7 days after treatment for necropsy and identification and enumeration of worm parasites in the gastrointestinal tract. Group-E lambs harbored 7 genera (including 10 species) of nematodes and 1 genus of tapeworms. Worm collection data for group-A lambs indicated 97% to 100% of the mature Haemonchus, Ostertagia, Trichostrongylus, and Trichuris, and immature Haemonchus were removed; and 23% to 73% of the mature Cooperia, Nematodirus, and Strongyloides, and immature Nematodirus were removed. In group-B lambs, 94% to 100% of the mature Haemonchus, Nematodirus, Ostertagia, Trichostrongylus, and Trichuris, and immature Haemonchus were removed as were 70% to 84% of mature Strongyloides and immature Nematodirus, respectively, and 0% for mature Cooperia. The percentage of all nematodes removed in group C and D was 100%, except for Cooperia (95%) in group C and immature Nematodirus (93% and 95%), respectively. Toxicosis was not apparent. Small fibrotic or blood streaked lesions were observed at necropsy in muscle at the injection site of 2 lambs in group B and 1 lamb in group E.

Administration, Oral↗
PubMedDate not supplied

Multiresidue method for isolation and liquid chromatographic determination of seven benzimidazole anthelmintics in milk.

A multiresidue method for the isolation and liquid chromatographic determination of 7 benzimidazole anthelmintics (thiabendazole, oxfendazole, para-hydroxyfenbendazole, fenbendazole sulfone, mebendazole, albendazole, and fenbendazole) in milk is presented. Blank or benzimidazole-spiked milk samples (0.5 mL) were blended with octadecylsilyl (C-18, 18% load, end-capped) derivatized silica packing material. A column made from the C-18/milk matrix was first washed with hexane (8 mL), and then the benzimidazoles were eluted with methylene chloride-ethyl acetate (1 + 2, v/v; 8 mL). The eluate contained benzimidazole analytes which were free from interfering compounds as determined by UV detection (photodiode array, 290 nm). Correlation coefficients of standard curves for individual benzimidazoles isolated from spiked samples were linear (0.989 +/- 0.003 to 0.998 +/- 0.001) with recoveries ranging from 70 +/- 9% to 107 +/- 2% for the concentration range (62.5-2000 ng/mL) examined. The inter-assay variabilities ranged from 4 +/- 1% to 9 +/- 7% with intra-assay variabilities of 3-6%.

Animals↗
PubMed1988

In vitro response of Haemonchus contortus larvae harvested during different times of the patent period to anthelmintics.

Three commercially available ruminant anthelmintics and an investigational drug were evaluated for effects on the motor function/motility of third stage (ensheathed) Haemonchus contortus. Helminth ova were collected at one, five, nine and 13 weeks during the patent period, cultured to the third larval stage and assayed for sensitivity to four different drugs. All four drugs (100 and 10 micrograms ml-1) significantly affected the motility of third stage H contortus larvae cultured from eggs passed at each of the times examined. However, the investigational drug (p-toluoyl chloride phenylhydrazone, 10 micrograms ml-1) had a significantly greater effect on the motility of larvae harvested at 13 weeks than those cultured at nine weeks (32 per cent difference). No other significant differences in the motility response during the patent period were observed.

Albendazole↗