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Parasitology Today (Personal Ed.) Sep 2000
Topics: Anthelmintics; Drug Resistance; Praziquantel; Schistosomiasis
PubMed: 10951592
DOI: 10.1016/s0169-4758(00)01749-x -
Zhongguo Xue Xi Chong Bing Fang Zhi Za... Mar 2021Praziquantel not only has broad-spectrum anti-trematode and anti-tapeworm effects, but also has pharmacological effects such as regulating inflammatory response and...
Praziquantel not only has broad-spectrum anti-trematode and anti-tapeworm effects, but also has pharmacological effects such as regulating inflammatory response and anti-fibrosis. Hereby, the anti-fibrosis effect of praziquantel and its mechanism were reviewed in order to provide theoretical basis for the treatment of liver fibrosis.
Topics: Humans; Liver Cirrhosis; Praziquantel
PubMed: 34791857
DOI: 10.16250/j.32.1374.2020232 -
International Journal For Parasitology Jul 2023Ion channels have proved to be productive targets for anthelmintic chemotherapy. One example is the recent discovery of a parasitic flatworm ion channel targeted by...
Ion channels have proved to be productive targets for anthelmintic chemotherapy. One example is the recent discovery of a parasitic flatworm ion channel targeted by praziquantel (PZQ), the main clinical therapy used for treatment of schistosomiasis. The ion channel activated by PZQ - a transient receptor potential ion channel of the melastatin subfamily, named TRPM - is a Ca-permeable ion channel expressed in all parasitic flatworms that are PZQ-sensitive. However, little is currently known about the electrophysiological properties of this target that mediates the deleterious action of PZQ on many trematodes and cestodes. Here, we provide a detailed biophysical characterization of the properties of Schistosoma mansoni TRPM channel (Sm.TRPM) in response to PZQ. Single channel electrophysiological analysis demonstrated that Sm.TRPM when activated by PZQ is a non-selective, large conductance, voltage-insensitive cation channel that displays distinct properties from human TRPM paralogs. Sm.TRPM is Ca-permeable but does not require Ca for channel gating in response to PZQ. TRPM from Schistosoma japonicum (Sj.TRPM) and Schistosoma haematobium (Sh.TRPM) displayed similar characteristics. Profiling Sm.TRPM responsiveness to PZQ has established a biophysical signature for this channel that will aid future investigation of endogenous TRPM activity, as well as analyses of endogenous and exogenous regulators of this novel, druggable antiparasitic target.
Topics: Animals; Humans; Praziquantel; Transient Receptor Potential Channels; TRPM Cation Channels; Anthelmintics; Schistosoma mansoni; Schistosomiasis mansoni
PubMed: 36610556
DOI: 10.1016/j.ijpara.2022.11.005 -
Bioorganic & Medicinal Chemistry Letters Feb 2012A praziquantel analog 10-hydroxy praziquantel and eight praziquantel/peroxide conjugates were synthesized. The biological activity of these compounds was evaluated...
A praziquantel analog 10-hydroxy praziquantel and eight praziquantel/peroxide conjugates were synthesized. The biological activity of these compounds was evaluated against juvenile and adult stages of Schistosoma japonicum. Unlike praziquantel, 10-hydroxy praziquantel exhibits activity against both juvenile and adult Schistosoma japonicumin. All hybrid compounds displayed modest to significant worm killing activity. The present study has important significance for the development of hybrid antischistosomal drugs.
Topics: Animals; Humans; Mice; Molecular Structure; Praziquantel; Schistosoma japonicum; Schistosomiasis japonica; Schistosomicides
PubMed: 22264473
DOI: 10.1016/j.bmcl.2011.12.133 -
Frontiers in Public Health 2022Schistosomiasis is a widely distributed parasitic disease and one of the most important neglected tropical diseases globally, for which Praziquantel® (PZQ) is the only...
Schistosomiasis is a widely distributed parasitic disease and one of the most important neglected tropical diseases globally, for which Praziquantel® (PZQ) is the only available treatment. In this context, tests with new PZQ formulations become relevant for disease control. This study evaluated the effects of PZQ treatment in the prepatent phase of schistosomiasis using two formulations: nanoencapsulated (PZQ-NANO) and active pharmaceutical ingredient (PZQ-API). Five experimental groups were established, for which the following serological parameters were evaluated: ALT, AST, ALP, and TP. Animals treated with PZQ-API at 15 and 30 days post-infection showed decreased eggs per gram of feces (EPG) compared to untreated infected animals. The same animals showed reductions of 63.6 and 65.1%, respectively, at 60 days post-infection. Animals treated with PZQ-NANO experienced no significant changes in EPG at any time of observation. Animals treated with either PZQ-API or PZQ-NANO had higher ALT and AST levels in the patent period (60 and 90 days post-infection). Treatment with PZQ, either API or NANO, at 15 days post-infection reduced AST, ALT, and TP levels. It is concluded that prepatent treatment with PZQ-API can reduce the parasite load of infected animals and that treatment at 15 days post-infection can prevent increased serum levels of ALT, AST, and TP.
Topics: Animals; Disease Models, Animal; Mice; Praziquantel; Schistosoma mansoni; Schistosomiasis; Schistosomiasis mansoni
PubMed: 35692307
DOI: 10.3389/fpubh.2022.848633 -
Salud Publica de Mexico 1982
Topics: Abdomen; Africa; Asia; Cestode Infections; Drug Evaluation; Humans; Isoquinolines; Latin America; Pain; Praziquantel; Trematode Infections
PubMed: 7185175
DOI: No ID Found -
Chemistry (Weinheim An Der Bergstrasse,... Feb 2013The antischistosomal effect of two [(η(6)-praziquantel)Cr(CO)(3)] derivatives was investigated. The compounds (see figure: Cr purple, N blue, O red) were prepared...
The antischistosomal effect of two [(η(6)-praziquantel)Cr(CO)(3)] derivatives was investigated. The compounds (see figure: Cr purple, N blue, O red) were prepared in a one-step procedure from commercially available praziquantel. Both derivatives show a high in vitro activity against Schistosoma mansoni, a parasitic trematode, and only a minor cytotoxic effect on selected mammalian cell lines.
Topics: Animals; Chromium; Coordination Complexes; Molecular Structure; Praziquantel; Schistosoma mansoni; Schistosomicides; Stereoisomerism
PubMed: 23296750
DOI: 10.1002/chem.201204291 -
Parasitology Research Dec 2023Dicrocoelium dendriticum affects the livers of ruminants and causes several deleterious effects on animal health status. The aim of this study was to investigate the...
Dicrocoelium dendriticum affects the livers of ruminants and causes several deleterious effects on animal health status. The aim of this study was to investigate the role of permeability-glycoprotein (P-gp) in absorption of praziquantel (PZQ) into D. dendriticum flukes by co-incubation with verapamil (VPL), an inhibitor of P-gp, under in vitro conditions. Mature flukes of D. dendriticum were collected from naturally infected sheep livers. The flukes were incubated with different concentrations of PZQ and VPL (50 and 100 μg/ml) in culture media and after several times of exposure (2, 6, 12, and 24 h), the concentration of PZQ absorbed in the parasites was measured by high-performance liquid chromatography. At 2-h post-incubation, the highest concentration of PZQ was noted as 0.92 µg/ml in the flukes treated with 100 μg/ml of each PZQ and VPL. After 24-h of exposure, VPL at all tested concentrations resulted in significant increase in absorption of PZQ into the parasite. Co-incubation of lancet flukes with VPL and PZQ roughly doubled the absorption of PZQ into them. Results of tegumental structures analysis by light microscopy confirmed higher efficacy of combination of VPL and PZQ. In conclusion, co-administration of VPL, especially at the concentration of 100 μg/ml, was able to increase PZQ uptake in Dicrocoelium flukes at all time points of the study.
Topics: Sheep; Animals; Praziquantel; Dicrocoelium; Parasites; Verapamil; Permeability
PubMed: 38057607
DOI: 10.1007/s00436-023-08039-3 -
Trends in Parasitology Jan 2022Schistosomiasis is a debilitating helminthiasis which commonly establishes as a chronic infection in people from endemic areas. As a potent modulator of the host immune... (Review)
Review
Schistosomiasis is a debilitating helminthiasis which commonly establishes as a chronic infection in people from endemic areas. As a potent modulator of the host immune response, the Schistosoma parasite and its associated products can directly interfere with its host's ability to mount adequate immune responses to unrelated antigens. As a result, increased attention is gathering on studies assessing the influence of helminths, particularly the causal agent of schistosomiasis, on host responsiveness to vaccines. However, to date, no consensus has been drawn regarding the influence of schistosomiasis on host vaccine responses. Here, we review available evidence on the influence of transgenerational and direct Schistosoma parasite exposure on host immune responses to unrelated vaccines. In addition, we evaluate the potential of praziquantel (PZQ) treatment in restoring schistosomiasis-impacted vaccine responses.
Topics: Animals; Anthelmintics; Humans; Immunity; Praziquantel; Schistosoma; Schistosomiasis; Vaccines
PubMed: 34389214
DOI: 10.1016/j.pt.2021.07.009 -
Fish Physiology and Biochemistry Feb 2016Regulatory approval is being sought to use praziquantel (PZQ) to treat flukes infecting yellowtail kingfish (YTK), but accurate safety data were not available. We...
Regulatory approval is being sought to use praziquantel (PZQ) to treat flukes infecting yellowtail kingfish (YTK), but accurate safety data were not available. We investigated the effect of increased doses or prolonged exposure of orally administered PZQ on YTK by assessing changes in haematological and biochemical characteristics, and mortality. Fish were intubated daily for 3 days with 0, 100, 300 and 500 mg PZQ kg(-1) BW day(-1) or once daily for 9 days at 0 and 100 mg PZQ kg(-1) BW day(-1). Blood was taken 24 h after the cessation of treatment. There was no significant difference between any of the haematological or biochemical indices in YTK treated with PZQ and controls, indicating that PZQ is safe for use at 100 mg PZQ kg(-1) BW day(-1) in YTK and that exposure to high doses or prolonged duration does not have negative effects on the YTK haematological or biochemical parameters we measured.
Topics: Animals; Anthelmintics; Drug Administration Schedule; Fish Diseases; Helminthiasis, Animal; Hematologic Tests; Perciformes; Praziquantel
PubMed: 26314575
DOI: 10.1007/s10695-015-0121-2