scholarly journals Benzimidazoles Pharmacodynamics in Equine Strongyles

2016 ◽  
Vol 73 (2) ◽  
pp. 360
Author(s):  
Laura Catana ◽  
Csongor Olah ◽  
Raul Catana ◽  
Mihai Cernea
Keyword(s):  
Larval Development ◽  
Treatment Protocol ◽  
Average Intensity ◽  
Egg Hatch ◽  
Maximum Value ◽  
Limited Effectiveness ◽  
Faecal Egg Count ◽  
Comparative Risk

Our research aimed to assess the effectiveness of four benzimidazoles: albendazole, fenbendazole, mebendazole and thiabendazole against equine strongyles. The tests were performed between March 2015 and May 2016, on samples collected from 20 horses and 8 donkeys living in Harghita County. In vivo, Faecal Egg Count Reduction Test (FECRT) was used to evaluate fenbendazole pharmacodynamics. In vitro, Egg hatch assay (EHA) and Larval development assay (LDA) were used to evaluate the effectiveness of albendazole, fenbendazole, mebendazole and thiabendazole. The predominance of small strongyle species was observed, mostly Cyathostomum type A. In the horse group, before treatment, the average intensity was 1595.5 EPG, the maximum value being 4000, and extensivity 55%. Tested again at 14 days after treatment, all samples were negative. In the donkey group, before treatment, the total number was 6550 EPG, intensity of 935.7 and extensivity of 87.5%. 14 days after treatment, the average intensity was 150 and the extensivity 50%. In the horse group, EHA proved the efficacy of fenbendazole (0.0192%), albendazole (0.3740%) and thiabendazole (11.62%) and a major risk of inducing adaptive phenomena for mebendazole (Y parameter 1009.92). In the donkey group, all benzimidazoles had limited effectiveness: thiabendazole (73.93%), mebendazole (87.51%), fenbendazole (94.05%), albendazole (111.67%). All benzimidazoles inhibited larval development. For all tested benzimidazoles, the resistance induction predictive comparative risk analysis highlighted the benefit of their use, provided that the treatment protocol allows sufficient contact time.

Anthelmintic evaluation of Cucurbita pepo againstgastrointestinal nematodes of sheep

2017 ◽  
Author(s):  
Ambalathaduvar Meenakshisundaram ◽  
Tirunelveli Jayagopal Harikrishnan ◽  
Thavasi Anna
Keyword(s):  
Larval Development ◽  
Anthelmintic Activity ◽  
Gastrointestinal Nematodes ◽  
Migration Inhibition ◽  
Egg Hatch ◽  
Larval Migration ◽  
Faecal Egg Count ◽  
Ethanolic Extracts

The study was aimed at to investigate the anthelmintic efficacy of aqueous and ethanolic extracts of Cucurbita pepo against gastrointestinal nematodes of sheep by scientifically validated in vitro and in vivo tests. In vitro anthelmintic activity was determined by egg hatch assay, larval migration inhibition assay and larval development assay against eggs and larvae of mixed gastrointestinal nematodes of sheep. The extracts which were found to be effective in in vitro assays were further evaluated by in vivo faecal egg count reduction test against mixed species of sheep gastrointestinal nematodes with 3 different doses (125, 250 and 500 mg kg-1). Haematological and serum parameters were estimated before and after treatment to determine the impact of plant extracts on health of the animal. Aqueous extract of C. pepo demonstrated significant inhibition of egg hatch at 40 and 80 mg/ml. The ED50 value of egg hatch inhibition was 3.51mg/ml. In larval migration inhibition assay, both aqueous and ethanolic extracts of C. pepo demonstrated inhibition of larval migration and the LM50 was 1.75 and 0.32 mg/ml respectively. However, in larval development assay, both aqueous and ethanolic extracts showed only marginal inhibition of larval development at all concentrations tested. In faecal egg count reduction test (FECRT), aqueous extracts of C. pepo at 500 mg/kg caused significant reduction in eggs per gram (96.61 per cent) the reduction being higher than the result obtained with albendazole, the positive control (93.25 per cent). There was a significant difference in EPG reduction between sheep treated with albendazole and C. pepo. Haematological and serum parameters were not affected in both the treated and untreated sheep indicating that the extracts did not cause toxic effects. Based on the results obtained in this study, the aqueous extract of C. pepo possesses anthelmintic activity and could offer an alternative source for the control of gastrointestinal nematodes of sheep.

scholarly journals Comparative anthelmintic efficacy of Arundo donax, Areca catechu, and Ferula assa-foetida against Haemonchus contortus

2021 ◽  
Vol 30 (2) ◽  
Author(s):  
Syed Nadeem Badar ◽  
Zafar Iqbal ◽  
Muhammad Sohail Sajid ◽  
Hafiz Muhammad Rizwan ◽  
Muhammad Shareef ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Haemonchus Contortus ◽  
Anthelmintic Activity ◽  
Parasitic Nematodes ◽  
Egg Hatch ◽  
Faecal Egg Count ◽  
Areca Catechu ◽  
Better Than

Abstract In the present study, anthelmintic activities of Arundo (A.) donax L., Areca (Ar.) catechu L., and Ferula (F.) assa-foetida L. were determined. Leaves of A. donax L., latex of F. assa-foetida L. and seeds of Ar. catechu L. in different solvent fractions were subjected to in vitro (egg hatch assay; EHA, and adult motility assay; AMA) and in vivo (faecal egg count reduction test; FECRT) tests of anthelmintic activity using Haemonchus contortus model. In the AMA, crude aqueous methanol extracts (CAME) and ethyl acetate fractions of F. assa-foetida at 10 hr post-treatment showed maximum mortality of H. contortus at 12.5-50 mg mL-1. In the EHA, CAME of F. assa-foetida was identified as a potent ovicide based on its low LC50 (16.9 µg mL-1), followed in order by Ar. catechu and A. donax. Results from the FECRT also showed the extract of F. assa-foetida L. to be more effective than those of Ar. catechu L. and A. donax L., against the gastrointestinal parasitic nematodes. Chloroform and ethyl acetate fractions showed better anthelmintic activities against the adult worms in vitro, while CAME of these plants were better than their crude powders in vivo. It is recommended to document and investigate indigenous knowledge of possible medicinal plants to plan scientific trials that may justify their endorsement.

scholarly journals Does the in vitro egg hatch test predict the failure of benzimidazole treatment in Haemonchus contortus?

Parasite ◽  
2021 ◽  
Vol 28 ◽  
pp. 62
Author(s):  
Michal Babják ◽  
Alžbeta Königová ◽  
Michaela Urda Dolinská ◽  
Tomas Kupčinskas ◽  
Jaroslav Vadlejch ◽  
...  
Keyword(s):  
Haemonchus Contortus ◽  
Gastrointestinal Parasites ◽  
Resistant Isolate ◽  
Egg Hatch ◽  
Larval Stages ◽  
Tubulin Isotype ◽  
Faecal Egg Count ◽  
Egg Hatch Test

Considerable research has been directed towards optimising in vitro tests that can diagnose resistance in pre-parasitic stages of parasites. The objective of this study was to compare the in vivo faecal egg count reduction test (FECRT), the in vitro egg hatch test (EHT), and the molecular determination of the frequency of a codon 200 allele of β-tubulin isotype 1 associated with benzimidazole resistance in larval stages of Haemonchus contortus obtained from infected goats. Animals were infected with composite infective doses representing 10, 20, 30, 40, 60, and 80% resistant alleles. Faecal samples for the EHT were collected on 28, 33, and 35 days post-infection. The results of the in vivo FECRT indicated that albendazole treatment reduced infections consisting of composite doses of 10, 20, 30, 40, 60, and 80% larvae of the resistant isolate by 91.3, 78.0, 63.3, 48.4, 36.5, and 41.4%, respectively. The drug concentration at which 50% of the eggs were prevented from developing hatching larvae (ED50) in the in vitro EHT varied from 0.09 ± 0.01 to 15.63 ± 12.10 μg/mL thiabendazole. The results of the in vitro EHT indicated that the test could estimate in vivo resistance well. The EHT could thus accurately estimate the in vivo efficacy of the drug and percentage of the resistance allele in the population using hatching parameters in delineation doses. This finding was also supported by comparing the FECRT data to the hatching percentages in the EHT on 30 goat farms in Slovakia with natural mixed infections of gastrointestinal parasites.

scholarly journals In vitro Anthelmintic Activity of Two Aloe-derived Active Principles against Sheep Gastrointestinal Nematodes

2017 ◽  
Vol 12 (12) ◽  
pp. 1934578X1701201
Author(s):  
Gianluca Fichi ◽  
Matteo Mattellini ◽  
Elisa Meloni ◽  
Guido Flamini ◽  
Stefania Perrucci
Keyword(s):  
Larval Development ◽  
Larval Mortality ◽  
Plant Secondary Metabolites ◽  
Anthelmintic Activity ◽  
Gastrointestinal Nematodes ◽  
Egg Hatch ◽  
Reference Drug ◽  
Faecal Samples ◽  
Aloe Emodin

The in vitro anthelmintic activity on sheep gastrointestinal strongyle (GIS) eggs and larvae of 0.5% aloin and 0.1% aloe-emodin was investigated. From fresh faecal samples collected by ewes naturally infected by Haemonchus, Trichostrongylus and Teladorsagia nematodes, GIS eggs were isolated and cultivated in Petri dishes (100 eggs/dish). For the in vitro evaluation of the anthelmintic activity of tested compounds, the Egg hatch test (EHT), the Larval development test (LDT) and the Larval mortality/paralysis test (LMT) were used. In each assay, the activity of tested compounds was compared to untreated and treated (0.1% thiabendazole, TBZ) controls. Six repetitions were made through the experiment. Obtained data were statistically elaborated using the X2 test. In EHT, 0.5% aloin gave highly significantly different (P<0.01) results from the untreated controls. In LDT, both 0.1% aloe-emodin and 0.5% aloin almost completely prevented the larval development from L1 to L3, showing no significant differences (P<0.01) when compared to TBZ. In LMT, larval mortality observed in 0.5% aloin treated plates was significantly higher (P<0.01) than that observed in TBZ treated controls. These results show the in vitro anthelmintic properties on sheep GIS of the examined plant secondary metabolites. In LDT and/or LMT, the activity of 0.5% aloin and 0.1% aloe-emodin was comparable to or higher than that of the reference drug.

In vitro cytotoxicity and in vivo zebrafish toxicity evaluation of Ru(ii)/2-mercaptopyrimidine complexes

2019 ◽  
Vol 48 (18) ◽  
pp. 6026-6039 ◽  
Author(s):  
Vivianne S. Velozo-Sá ◽  
Luciano R. Pereira ◽  
Aliny P. Lima ◽  
Francyelli Mello-Andrade ◽  
Manuela R. M. Rezende ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Larval Development ◽  
In Vitro Cytotoxicity ◽  
Toxic Effects ◽  
Toxicity Evaluation ◽  
Embryonic And Larval Development

Ru(ii)/2-mercaptopyrimidine complexes active against cancer cells did not present toxic effects during embryonic and larval development of zebrafish.

Tolerability and preliminary efficacy of BXQ-350 for refractory solid tumors and high-grade gliomas: First-in-human, first-in-class phase I trial.

2020 ◽  
Vol 38 (15_suppl) ◽  
pp. 3505-3505
Author(s):  
Olivier Rixe ◽  
John Charles Morris ◽  
Robert Wesolowski ◽  
Emrullah Yilmaz ◽  
Richard Curry ◽  
...  
Keyword(s):  
Solid Tumors ◽  
Dose Level ◽  
Human Study ◽  
Treatment Protocol ◽  
High Grade Glioma ◽  
Maximum Tolerated Dose ◽  
High Grade ◽  
Serious Adverse Events

3505 Background: BXQ-350 is a first-in-class agent comprised of Saposin C (SapC) and dioleoyl phosphatidylserine (DOPS). SapC, a multifunctional lysosomal-activator glycoprotein that preferentially interacts with tumor cell phospholipids, has demonstrated anti-tumor effects in both in vitro and in vivo preclinical models. The tolerability and preliminary efficacy of BXQ-350 in the first-in-human study are summarized here. Methods: Eighty-six refractory solid tumor (ST) or high-grade glioma (HGG) patients age ≥18 (36F:50M, age 24-81) were enrolled in a 3-part first-in-human trial (NCT02859857) from 2016-2019 and received at least one dose of BXQ-350. Doses were administered via intravenous infusion during 28-day cycles until disease progression occurred. The previously reported part 1 dose escalation portion of the study (9 HGG, 9 ST patients) established the highest planned dose of 2.4mg/kg as safe but did not identify a maximum tolerated dose. The part 2 expansion cohort treated 37 patients (18 HGG and 19 ST) and an additional part 3 cohort treated 31 ST gastrointestinal (GI) patients, both at the 2.4 mg/kg dose level. Preliminary antitumor activity was evaluated (RECISTv1.1 or RANO). Results: There were no BXQ-350-related serious adverse events, dose limiting toxicities or withdrawals with the exception of 1 allergic type reaction. Three patients (Glioblastoma, Ependymoma, Appendiceal) demonstrated a partial response per RECIST/RANO. Two HGG patients with progressive radiologic enhancement were seen to have treatment effect at surgery, and hence considered to have stable disease. Seven patients (2 HGG, 3 GI, 2 other ST) remain on study and have received treatment for 9+ to 41+ months, with 5 patients treated for > 1 year. A continuing treatment protocol is planned in order to allow these patients to remain on BXQ-350 treatment. Conclusions: BXQ-350 was well tolerated with no significant dose-limiting toxicities at the highest planed dose level. Preliminary results indicate this novel agent demonstrated possible anti-tumor activity in refractory solid tumors and HGG. Clinical trial information: NCT03967093) .

Metabolism of nitrogen fixed by nodules of alfalfa (Medicago sativa L.): II. Asparagine synthesis

1988 ◽  
Vol 66 (12) ◽  
pp. 1349-1354 ◽  
Author(s):  
T.-C. Ta ◽  
F. D. H. Macdowall ◽  
M. A. Faris ◽  
K. W. Joy
Keyword(s):  
Asparagine Synthetase ◽  
Nodule Development ◽  
Nitrogen Transport ◽  
In Vitro Activity ◽  
Sulfhydryl Reagents ◽  
In Vivo Experiments ◽  
Maximum Value ◽  
Medicago Sativa L

Asparagine is a major nitrogen transport compound in many legumes including alfalfa. In vivo experiments with nodulated alfalfa roots exposed to labeled 15N2 and 14CO2 revealed that asparagine is synthesized at a rate of 150 nmol∙gFW nodule−1∙min−1. Nodule segments incorporate [U-14C, 15N]aspartate into asparagine, and the 14C/15N (amino) ratio of asparagine is very similar to that of aspartate. The results show that asparagine is synthesized mainly by the amidation of aspartate utilizing the amide group of glutamine; however, there is evidence that ammonia can also contribute directly to asparagine synthesis. The in vitro activity of asparagine synthetase in nodule extracts was detected at a maximum rate of 44 nmol∙gFW−1∙min−1 through the inclusion of sulfhydryl reagents, EGTA, and glycerol in the extract buffer. The enzyme requires aspartate, glutamine (or ammonia), and ATP as substrates. Activity increases during nodule development, reaching a maximum value 17 days after inoculation. The measured rates for asparagine synthesis and enzyme activity are much higher than previously reported.

scholarly journals Evaluation of Eucalyptus citriodora essential oil on goat gastrointestinal nematodes

2011 ◽  
Vol 20 (3) ◽  
pp. 223-227 ◽  
Author(s):  
Iara Tersia Freitas Macedo ◽  
Claudia Maria Leal Bevilaqua ◽  
Lorena Mayana Beserra de Oliveira ◽  
Ana Lourdes Fernandes Camurça-Vasconcelos ◽  
Luiz da Silva Vieira ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Essential Oil ◽  
Larval Development ◽  
Anthelmintic Activity ◽  
Gastrointestinal Nematodes ◽  
Gastrointestinal Parasites ◽  
Eucalyptus Citriodora ◽  
Egg Hatching

Phytotherapy may be an alternative strategy for controlling gastrointestinal parasites. This study evaluated the anthelmintic efficacy of Eucalyptus citriodora essential oil (EcEO). The in vitro effects of EcEO were determined through testing the inhibition of egg hatching and larval development of Haemonchus contortus. EcEO was subjected to acute toxicity testing on mice, orally and intraperitoneally. The in vivo effects of EcEO were determined by the fecal egg count reduction test (FECRT) in goats infected with gastrointestinal nematodes. The results showed that 5.3 mg.mL-1 EcEO inhibited egg hatching by 98.8% and 10.6 mg.mL-1 EcEO inhibited H. contortus larval development by 99.71%. The lethal doses for 50% of the mice were 4153 and 622.8 mg.kg-1, for acute toxicity orally and intraperitoneally. In the FECRT, the efficacy of EcEO and ivermectin was 66.25 and 79.16% respectively, on goat gastrointestinal nematodes eight days after treatment. EcEO showed in vitro and in vivo anthelmintic activity.

scholarly journals Worm-control practices and prevalence of anthelmintic resistance using in vivo FECRTs on smallholder sheep farms in Lithuania

2016 ◽  
Vol 53 (1) ◽  
pp. 24-30 ◽  
Author(s):  
T. Kupčinskas ◽  
I. Stadalienė ◽  
A. Šalomskas ◽  
P. Trusevičius ◽  
M. Varady ◽  
...  
Keyword(s):  
Anthelmintic Resistance ◽  
Gastrointestinal Nematodes ◽  
Parasitic Nematodes ◽  
Future Studies ◽  
Faecal Samples ◽  
Two Samples ◽  
Faecal Egg Count ◽  
Worm Control

SummaryThis study determined the prevalence of anthelmintic resistance (AR) in parasitic nematodes on smallholder sheep farms in Lithuania from April to November 2014. Faecal samples were collected from two groups of 10-15 sheep treated with fenbendazole (FBZ) or ivermectin (IVM) on 18 sheep farms. Two samples were collected from each group: on day zero (T1) and 10-14 days after treatment. Faecal egg counts (eggs per gramme, EPG) were determined using a modified McMaster technique. Animals with < 140 EPG on day zero were removed from the analysis. The prevalence of AR was estimated using the in vivo faecal egg count reduction test. AR to FBZ was detected on three of 15 farms where FBZ was used (20 %) and was suspected on one farm (6.7 %). AR to IVM was detected on two of 16 farms where IVM was used (12.5 %). The main species of resistant gastrointestinal nematodes (GINs) identified after treatment were Teladorsagia spp. and Trichostrongylus spp. A questionnaire surveying 71 sheep farmers estimated that 71.8 % of sheep farmers used anthelmintics against GINs. IVM was the most frequently (68.6 %) applied anthelmintic, and 62.7 % of the respondents reported treating their animals twice a year. This study confirmed the presence of AR to GIN infections on sheep farms in Lithuania. Future studies should assess the prevalence of AR to GIN infection using in vitro methods.

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