Isocratic separation of seven benzimidazole anthelmintics by high-performance liquid chromatography with photodiode array characterization.
Explore the source record for details and available documents.
SEARCH · Search PubMed
Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.
Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Effects of praziquantel (PZQ), levamisole (LEV), mebendazole (MBZ), fenbendazole (FBZ) and albendazole (ABZ) on the lactate dehydrogenase (LDH) activity of Cotylophoron cotylophorum were studied in vitro. Maximum levels of inhibition of LDH catalysing both oxidation and reduction reactions were observed in PZQ- and LEV-treated worms. Similarly, benzimidazoles - MBZ, FBZ and ABZ - have also significantly inhibited the activity of LDH catalysing the oxidation of lactate; whereas the activity of LDH catalysing the reduction of pyruvate was accelerated. This affects the mitochondrial energy generating process which ultimately proves fatal to the parasite. Therefore, the mode of action of benzimidazoles is primarily on the activation of LDH catalysing the conversion of pyruvate to lactate.
The ovicidal activity of the essential oil of Ocimum gratissimum Linn. (Labideae) and its main component eugenol was evaluated against Haemonchus contortus, gastrointestinal parasite of small ruminants. The oil and eugenol were diluted in Tween 20 (0.5%) at five different concentrations. In the egg hatch test, H. contortus eggs were obtained from feces of goats experimentally infected. At 0.50% concentration, the essential oil and eugenol showed a maximum eclodibility inhibition. These results suggest a possible utilization of the essential oil of O. gratissimum as an aid to the control of gastrointestinal helmintosis of small ruminants.
Explore the source record for details and available documents.
A controlled test of the efficacy of triclabendazole against all stages (early immature, late immature and mature) of Fasciola hepatica has been performed in experimentally infected goats. The influence of triclabendazole treatment on the pathophysiology of the disease, in terms of haematological parameters and serum enzyme levels, and in the dynamics of production of specific antibodies to excretory/secretory products (ESP) of F. hepatica were also examined. Goats were orally infected with 200 viable metacercarie and treated at 4, 8 and 16 weeks postinfection (PI) with triclabendazole at the dose rate of 10 mg kg-1 body weight. The drug can be regarded as highly effective against mature (100%) and late immature (99.2%) flukes and effective against early immature flukes (94.9%). A moderate anaemia was found associated with the presence of late immature and mature flukes in bile ducts. Treatment with triclabendazole, by eliminating most of these flukes, largely reduced haematological alterations. Serum levels of the enzymes aspartate aminotransferase, lactate dehydrogenase and gamma-glutathione transferase reflected hepatic damage during goat fasciolosis. Early treatment (at 4 weeks PI) prevents the development of both parenchyma and bile ducts lesions; treatment at 8 weeks PI only prevents bile ducts lesions and treatment at 16 weeks PI has no appreciable effect on the development of the main hepatic lesions. The antibody response to F. hepatica ESP, as measured by enzyme-linked immunosorbent assay, was also affected by treatment with triclabendazole. In all treated animals a peak in antibody levels was observed between weeks 9 and 13, followed by a drop whose magnitude depended on the efficacy of treatment. In those animals in which triclabendazole was highly effective, antibody levels fell back to negative values similar to those recorded preinoculation at 18-21 weeks PI.
Explore the source record for details and available documents.
A comparison of persistent efficacy of doramectin injectable (D) and ivermectin injectable (I) was investigated under field conditions with treated permanent principal (PP) and interval-grazed principal (IGP) calves. The experiment was initiated on October 13, 1992 (day 0). Cattle used were crossbred beef heifers of 185 kg average weight and 8 to 10 months old. By random allotment, 66 calves were divided into two groups of 15 PP-D and PP-I calves for each treatment and two groups of 15 IGP-D and IGP-I calves for each treatment. Three extra or replacement calves were allotted for each group. Permanent principal calves in three replicates of five cattle per treatment grazed continuously on nematode-contaminated replicate pastures from day 0 to day 70. At 2-week intervals, i.e., days 0 to 14, 14 to 28, 28 to 42, 42 to 56 and 56 to 70, one IGP-D and one IGP-I calf was grazed with each of the respective PP-D and PP-I calf replicates and necropsied 21 days after removal from pasture. All respective PP calves and IGP calves were treated with doramectin at 200 micrograms kg-1 or ivermectin at 200 micrograms kg-1 by s.c. injection on day 0. After the day 0-14 interval, all IGP-D calves had zero egg counts. From the day 14-28 interval through the next three grazing intervals, the arithmetic mean egg counts of IGP-D calves were 18, 90, 281 and 31; those of IGP-I calves were 30, 226, 74 and 185. This suggested a persistence effect of approximately 2 to 4 weeks. In PP-D calves, egg counts reached a mean maximum at day 56 of only five eggs per gram, while counts of PP-I calves reached a peak of 40 on day 42. From the day 14-28 interval and through all subsequent intervals, arithmetic mean total worm counts from IGP-I calves were 58 to 73% greater than those in IGP-D tracers. A maximal total worm count of 4159 was observed in IGP-D calves of the day 42-56 interval; total worm counts in IGP-I calves from the day 14-28 interval through the day 42-56 interval were: 5420, 6739 and 9979, respectively. Haemonchus and Cooperia were higher in prevalence than Ostertagia in both treatments. Results of PP-D egg counts and total worm burdens in IGP-I calves indicated a high level of doramectin persistent activity for approximately 4 to 5 weeks and an advantage over persistence activity of ivermectin.
The objective of this study was to investigate the influence of different types of chemoprophylaxis in first season grazing calves on their resistance against a natural reinfection with Ostertagia ostertagi and Cooperia oncophora in the second grazing season. Thirty helminth-naive crossbred calves were randomly divided in three groups of 10 animals. The animals of group B received an ivermectin sustained release bolus on day 0. The calves of group D were treated on days 0 and 56 with a subcutaneous injection of doramectin (0.2 mg kg(-1) BW). Group C was the untreated control group ('immune' controls). Although exposure to gastrointestinal nematodes in the first grazing season was only limited, the chemoprophylactic treatments in groups B and D resulted in three distinctly different infection levels (group C > group D > group B). At the start of the second grazing season, six helminth-naive steers (group N, 'susceptible' controls) were turned out together with the second season animals. After 3 weeks of grazing, the 'susceptible' controls were slaughtered, together with four animals from each other group. Parasitological and immunological parameters indicated that resistance to reinfection with Ostertagia was reduced in the chemoprophylactic treated animals, and was negatively related to the degree of suppression of host-parasite contact in the first grazing season (group C > group D > group B > group N). None of the groups had developed a complete resistance against Cooperia yet. A negative relationship was observed between reduction of first grazing season exposure, and weight gains early in the second grazing season. The remaining animals stayed on pasture until the beginning of November. At the end of the second grazing season, levels of acquired resistance against Ostertagia infection were similar in all groups, and all animals had become immune against Cooperia. No effect of first year chemoprophylaxis on total weight gains could be demonstrated. Because of discrepancy between pasture larval counts and tracer worm counts, it was not possible to draw firm conclusions on the effect of chemoprophylaxis on pasture infestation levels in the second year.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
A series of gem-difluoro-avermectin derivatives was synthesized from the corresponding ketones at positions 4", 4', 13, and 23 using diethylaminosulfur trifluoride (DAST). These fluorinated avermectins exhibit potent antiparasitic activity in a new Haemonchus contortus larval assay and are equipotent to ivermectin. In addition, 23-gem-difluoro-ivermectin displays useful anticonvulsant activity in mouse models.
Following our discovery of the strong binding of thiadiazole 1 to the AF-2 neuropeptide receptor of gastrointestinal nematodes (e.g., Ascaris suum), we prepared two series of analogs. Only the series containing the thiadiazole ring had potencies comparable to that of compound 1. Analog 50 exhibited an apparent potency in the AF-2 binding assay 300 times that of compound 1.