RESUMO
PURPOSE: This study investigated the anthelmintic efficacy of therapeutic baths with the essential oil of Piper marginatum Jacq against the monogeneans Anacanthorus spathulatus Kritsky, Thatcher & Kayton, 1979, Notozothecium janauachensis Belmont-Jégu, Domingues & Laterça 2004, Mymarothecium boegeri Cohen & Kohn, 2005 and Linguadactyloides brinkmanni Thatcher & Krytsky, 1983 in Colossoma macropomum Cuvier, 1818, and its hematological and histopathological effects on this fish. METHODS: Short six therapeutic baths with 100 mg/L of the essential oil of P. marginatum and two control groups (water from the cultivation tank and water from the cultivation tank + 70% alcohol) were used for 20 min every two days. RESULTS: The therapeutic baths with 100 mg/L of the essential oil of P. marginatum had efficacy of 42.8% against monogeneans of C. macropomum gills. Toxicity was low for C. macropomum, because there were few physiological and histopathological changes that did not compromise the functioning of the gills of this fish. CONCLUSION: Short therapeutic baths with 100 mg/L of the essential oil of P. marginatum had low efficacy for controlling monogeneans in C. macropomum and thus cannot be recommended.
Assuntos
Caraciformes , Doenças dos Peixes , Brânquias , Óleos Voláteis , Piper , Infecções por Trematódeos , Animais , Óleos Voláteis/farmacologia , Doenças dos Peixes/parasitologia , Doenças dos Peixes/tratamento farmacológico , Caraciformes/parasitologia , Brânquias/parasitologia , Infecções por Trematódeos/veterinária , Infecções por Trematódeos/parasitologia , Infecções por Trematódeos/tratamento farmacológico , Piper/química , Anti-Helmínticos/farmacologia , Trematódeos/efeitos dos fármacosRESUMO
Parasite infections in fish require constant surveillance and strategies for efficient treatments which guarantee the fish health, their sale value and the non-propagation of pathogens in new environments. Fish treatments based on nanotechnology become of increasing interest since nanoparticles have been shown as efficient materials for optimizing administration of bioactives. In this study a chitosan derivative, alginate and praziquantel conjugated nanobioparticle of effective action for oral treatment of digenetic trematodes in highly infected Corydoras schwartzi was evaluated in terms of histological and hematological safety. The inherent absence of alterations in intestinal tissue and the reversible blood cells counting during a period up to 35 days showed the safety of the drug delivery nanobioparticles, which thus represent a promising strategy for effective applications in pathogens treatments by oral administration.
Assuntos
Peixes-Gato/parasitologia , Doenças dos Peixes/tratamento farmacológico , Nanopartículas , Praziquantel/administração & dosagem , Infecções por Trematódeos/veterinária , Administração Oral , Alginatos , Animais , Quitosana , Portadores de Fármacos , Doenças dos Peixes/parasitologia , Intestinos/efeitos dos fármacos , Intestinos/patologia , Trematódeos/efeitos dos fármacos , Infecções por Trematódeos/tratamento farmacológicoRESUMO
The Excretory/Secretory (ES) proteins of parasites are involved in invasion and colonization of their hosts. In addition, since ES proteins circulate in the extracellular space, they can be more accessible to drugs than other proteins, which makes ES proteins optimal targets for the development of new and better pharmacological strategies. Monogeneans are a group of parasitic Platyhelminthes that includes some pathogenic species problematic for finfish aquaculture. In the present study, 8297 putative ES proteins from four monogenean species which genomic resources are publicly available were identified and functionally annotated by bioinformatic tools. Additionally, for comparative purposes, ES proteins in other parasitic and free-living platyhelminths were identified. Based on data from the monogenean Gyrodactylus salaris, 15 ES proteins are considered potential drug targets. One of them showed homology to 10 cathepsins with known 3D structure. A docking molecular analysis uncovered that the anthelmintic emodepside shows good affinity to these cathepsins suggesting that emodepside can be experimentally tested as a monogenean's cathepsin inhibitor.
Assuntos
Antiplatelmínticos/química , Biologia Computacional , Desenvolvimento de Medicamentos , Proteínas de Helminto/genética , Trematódeos/efeitos dos fármacos , AnimaisRESUMO
Monogeneans are parasitic flatworms that may be a threat for finfish aquaculture. In this study, the anthelmintic activity of two terpenes, geraniol and ß-citronellol, was tested in vitro against ancyrocephalin and diplectanid monogeneans. Experiments were performed in both water and a culture medium. We observed that monogeneans in culture medium may be more tolerant to treatments compared with bioassays performed only in water. Concentrations of 300 mg/L of both compounds were required to kill 100% of monogeneans at 1 h postexposure. The toxicity of ß-citronellol to fish was not evaluated. However, geraniol at 300 mg/L and 150 mg/L killed juvenile Nile Tilapia Oreochromis niloticus and White Snook Centropomus viridis, respectively, after a few minutes. Therefore, the present work suggests that other alternatives should be studied for use against monogeneans in aquaculture.
Assuntos
Monoterpenos Acíclicos , Ciclídeos , Perciformes , Trematódeos/efeitos dos fármacos , Monoterpenos Acíclicos/efeitos adversos , Monoterpenos Acíclicos/farmacologia , Animais , Anti-Helmínticos/efeitos adversos , Anti-Helmínticos/farmacologia , Especificidade da EspécieRESUMO
PURPOSE: The aim of this study was to evaluate the in vitro and in vivo efficacy of propolis against Ligictaluridus floridanus on Ictalurus punctatus gills. METHODS: This study used an ethanol extract of propolis at a concentration of 300 mg mL-1, with a total polyphenol concentration of 2.77 mg mL-1 as determined by chromatography. In vitro trial used propolis concentrations at 5, 30 as well as 60 mg L-1 and a 70% ethanol control group to treat naturally infected catfish. The in vivo experiment was 16 weeks in duration, consisting of seventy-two fish infected by cohabitation and subjected to one-hour baths every 72 h during the trial. RESULTS: In vitro studies showed that parasites exposed to 60 mg L-1 of propolis displayed a significant reduction (p < 0.05) in their survival time. In vivo studies confirmed the reduction of intensity and abundance of Ligictaluridus floridanus on the gills of channel catfish. CONCLUSION: This study has provided the first challenge of propolis against L. floridanus on I. punctatus gills and shows that propolis has an anthelmintic effect.
Assuntos
Peixes-Gato/parasitologia , Doenças dos Peixes/parasitologia , Própole/farmacologia , Trematódeos/efeitos dos fármacos , Infecções por Trematódeos/veterinária , Animais , Anti-Helmínticos/farmacologia , Brânquias/parasitologia , Trematódeos/isolamento & purificaçãoRESUMO
This study compared the in vitro anthelmintic activity of Copaifera reticulata oleoresin (200, 400, 600, 800 and 1,000 mg/L) and of nanoemulsions prepared with this oleoresin (50, 100, 150, 200 and 250 mg/L) against monogeneans on the gills of Colossoma macropomum. The major compounds present in the oleoresin of C. reticulata were γ-macrocarpene (14.2%), α-bergamotene (13.6%), ß-selinene (13.4%) and ß-caryophyllene (11.7%). All concentrations of the nanoemulsion and the oleoresin without nanoformulation showed anthelmintic efficacy against monogeneans, and higher concentrations led to more rapid parasite mortality. Structural damages to the tegument of the parasites exposed to C. reticulata oleoresin were observed with scanning electron microscopy. At two hours of exposure, fish showed 100% tolerance to all nanoemulsion concentrations used in the in vitro assays, whereas 100% mortality was shown in the fish exposed to the oleoresin without nanoformulation after one hour. The results of this study suggest that nanoemulsions with oleoresin of C. reticulata have advantages in the control and treatment of monogenean infections in C. macropomum when compared to the oleoresin without nanoformulation. In addition, since nanoemulsions with the C. reticulata oleoresin are safe to control monogeneans, the efficacy of these nanoformulations may be assayed in therapeutic baths to treat C. macropomum infected by monogeneans.
Assuntos
Antiplatelmínticos/farmacologia , Fabaceae/química , Doenças dos Peixes/tratamento farmacológico , Extratos Vegetais/farmacologia , Trematódeos/efeitos dos fármacos , Infecções por Trematódeos/veterinária , Animais , Compostos Bicíclicos com Pontes/farmacologia , Relação Dose-Resposta a Droga , Emulsões/química , Doenças dos Peixes/parasitologia , Nanoestruturas/química , Sesquiterpenos Policíclicos/farmacologia , Sesquiterpenos de Eudesmano/farmacologia , Tetra-Hidronaftalenos/farmacologia , Infecções por Trematódeos/tratamento farmacológico , Infecções por Trematódeos/parasitologiaRESUMO
Trematode infections such as schistosomiasis and fascioliasis cause significant morbidity in an estimated 250 million people worldwide and the associated agricultural losses are estimated at more than US$ 6 billion per year. Current chemotherapy is limited. Triosephosphate isomerase (TIM), an enzyme of the glycolytic pathway, has emerged as a useful drug target in many parasites, including Fasciola hepatica TIM (FhTIM). We identified 21 novel compounds that selectively inhibit this enzyme. Using microscale thermophoresis we explored the interaction between target and compounds and identified a potent interaction between the sulfonyl-1,2,4-thiadiazole (compound 187) and FhTIM, which showed an IC50 of 5 µM and a Kd of 66 nM. In only 4 hours, this compound killed the juvenile form of F. hepatica with an IC50 of 3 µM, better than the reference drug triclabendazole (TCZ). Interestingly, we discovered in vitro inhibition of FhTIM by TCZ, with an IC50 of 7 µM suggesting a previously uncharacterized role of FhTIM in the mechanism of action of this drug. Compound 187 was also active against various developmental stages of Schistosoma mansoni. The low toxicity in vitro in different cell types and lack of acute toxicity in mice was demonstrated for this compound, as was demonstrated the efficacy of 187 in vivo in F. hepatica infected mice. Finally, we obtained the first crystal structure of FhTIM at 1.9 Å resolution which allows us using docking to suggest a mechanism of interaction between compound 187 and TIM. In conclusion, we describe a promising drug candidate to control neglected trematode infections in human and animal health.
Assuntos
Anti-Helmínticos/química , Anti-Helmínticos/farmacologia , Trematódeos/efeitos dos fármacos , Trematódeos/enzimologia , Infecções por Trematódeos/tratamento farmacológico , Triose-Fosfato Isomerase/antagonistas & inibidores , Animais , Anti-Helmínticos/uso terapêutico , Cristalografia por Raios X , Descoberta de Drogas , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/uso terapêutico , Fasciola hepatica/efeitos dos fármacos , Fasciola hepatica/enzimologia , Fasciolíase/tratamento farmacológico , Fasciolíase/parasitologia , Feminino , Masculino , Mesocricetus , Camundongos , Camundongos Endogâmicos BALB C , Modelos Moleculares , Schistosoma mansoni/efeitos dos fármacos , Schistosoma mansoni/enzimologia , Esquistossomose mansoni/tratamento farmacológico , Esquistossomose mansoni/parasitologia , Infecções por Trematódeos/parasitologia , Triose-Fosfato Isomerase/metabolismoRESUMO
Abstract This study investigated the effects of diets supplemented with levamisole on monogeneans on the gills of Colossoma macropomum. Fish were fed with diets containing levamisole at concentrations of 0, 300, 600, 900 and 1200 mg kg-1 for 24, 96 and 240 h and the infection by Anacanthorus spatulatus, Notozothecium janauachensis and Mymarothecium boegeri were evaluated. None of the levamisole concentrations caused either mortality or behavioral alterations in fishes during 240 h of feeding. After 24 h of feeding with 1200 mg kg-1 of levamisole, the abundance of N. janauachensis decreased in comparison with treatments of 0, 300, 600 and 900 mg kg-1, as did the abundance of M. boegeri after 240 h of feeding with 1200 mg kg-1 of levamisole. The efficacy of 900 mg kg-1 of levamisole was only 55.7% after 96 h of feeding, but it was 84.6% after 240 h of feeding with 1200 mg kg-1. Our results show that 1200 mg kg-1 of levamisole for 10 days has good anthelmintic efficacy against monogeneans of C. macropomum. Since monogeneans elicit some of the worst problems in C. macropomum, this study has provided evidence of an effective control method that may be used in fish farms.
Resumo Este estudo investigou os efeitos de dietas suplementadas com levamisol na infecção por monogeneas nas brânquias de Colossoma macropomum. Os peixes foram alimentados com dietas contendo 0, 300, 600, 900 e 1200 mg kg-1 de levamisol por 24, 96 e 240 h e os níveis de infecção por Anacanthorus spatulatus, Notozothecium janauachensis e Mymarothecium boegeri, foram avaliados. Nenhuma das concentrações de levamisol causou mortalidade ou alterações comportamentais nos peixes durante 240 h de alimentação. Após 24 h de alimentação com 1.200 mg kg-1 de levamisol, a abundância de N. janauachensis diminuiu quando comparada aos tratamentos com 0, 300, 600 e 900 mg kg-1, bem como a abundância de M. boegeri após 240 h de alimentação com 1200 mg kg-1 de levamisol. A eficácia de 900 mg kg-1 de levamisol foi somente de 55,7% após 96 h de alimentação, mas foi de 84,6% após 240 h de alimentação com 1200 mg kg-1. Os resultados mostram que 1200 mg kg-1 de levamisol durante 10 dias, tem uma boa eficácia antihelmíntica contra monogeneas de C. macropomum. Como monogeneas provocam alguns dos piores problemas em C. macropomum, este estudo forneceu evidências de um método de controle eficaz que pode ser usado em pisciculturas.
Assuntos
Animais , Trematódeos/efeitos dos fármacos , Levamisol/administração & dosagem , Dieta , Doenças dos Peixes/prevenção & controle , Peixes/parasitologia , Ração Animal , Antinematódeos/administração & dosagem , Doenças dos Peixes/parasitologiaRESUMO
This study investigated the effects of diets supplemented with levamisole on monogeneans on the gills of Colossoma macropomum. Fish were fed with diets containing levamisole at concentrations of 0, 300, 600, 900 and 1200 mg kg-1 for 24, 96 and 240 h and the infection by Anacanthorus spatulatus, Notozothecium janauachensis and Mymarothecium boegeri were evaluated. None of the levamisole concentrations caused either mortality or behavioral alterations in fishes during 240 h of feeding. After 24 h of feeding with 1200 mg kg-1 of levamisole, the abundance of N. janauachensis decreased in comparison with treatments of 0, 300, 600 and 900 mg kg-1, as did the abundance of M. boegeri after 240 h of feeding with 1200 mg kg-1 of levamisole. The efficacy of 900 mg kg-1 of levamisole was only 55.7% after 96 h of feeding, but it was 84.6% after 240 h of feeding with 1200 mg kg-1. Our results show that 1200 mg kg-1 of levamisole for 10 days has good anthelmintic efficacy against monogeneans of C. macropomum. Since monogeneans elicit some of the worst problems in C. macropomum, this study has provided evidence of an effective control method that may be used in fish farms.
Assuntos
Ração Animal , Antinematódeos/administração & dosagem , Dieta , Doenças dos Peixes/prevenção & controle , Peixes/parasitologia , Levamisol/administração & dosagem , Trematódeos/efeitos dos fármacos , Animais , Doenças dos Peixes/parasitologiaRESUMO
INTRODUCTION: Herbal therapy is a potentially beneficial alternative for fish aquaculture, since it may be cheaper and more effective than chemotherapy. The aim of this study was to investigate the in vitro efficacy of Ficus insipida latex on monogeneans of Colossoma macropomum gills. MATERIALS AND METHODS: To evaluate the anthelmintic activity, four concentrations of F. insipida latex (250, 500, 750 and 1000 µL/L) and exposure time to cause immobilization on monogeneans were used. In addition, two control groups, being one with water from the breeding tank and the other with breeding water from the tank + 70% ethyl alcohol were used. RESULTS: At the concentration of 250 µL/L of F. insipida latex, the immobilization of the monogeneans occurred after 4 h of exposure, while at the concentration of 500 µL/L, it occurred after 2 h. At the concentrations of 750 and 1000 µL/L of F. insipida latex, the immobilization of the monogeneans occurred after 1 h and 30 min, respectively. After exposure to 250 µL/L of F. insipida latex, 100% of immobilization of monogeneans was observed within 4 h, to 500 and 750 µL/L, 100% immobilization occurred within 4 h and to 1000 µL/L, 100% mortality occurred after 2 h. CONCLUSIONS: Thus, we recommended the use of 1000 µL/L of F. insipida latex for therapeutic baths in of C. macropomum against monogeneans, after previous test of toxicity.