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1.
Data Brief ; 19: 1393-1397, 2018 Aug.
Article in English | MEDLINE | ID: mdl-30225292

ABSTRACT

In this study, the molluscicidal and antiparasitic activities of divaricatic acid was evaluated, targeting the mollusc Biomphalaria glabrata and cercariae of the helminth Schistosoma mansoni. Divaricatic acid showed high toxicity against both adult snails (5.5 µg/mL) and embryos (20 µg/mL after 6 h of exposure). Similar activity was observed in S. mansoni cercariae after only a short exposure time. The divaricatic acid proved to be a promising substance for the control of the snail B. glabrata, an intermediate host of schistosomiasis, as well as the cercariae of the pathogen.

2.
Acta Trop ; 178: 97-102, 2018 Feb.
Article in English | MEDLINE | ID: mdl-29097241

ABSTRACT

In this study, the molluscicidal and antiparasitic activities of divaricatic acid was evaluated, targeting the mollusc Biomphalaria glabrata and cercariae of the helminth Schistosoma mansoni. In addition, the environmental toxicity of divaricatic acid was assessed by bioassay using the microcrustacean Artemia salina. Divaricatic acid showed high toxicity against both adult snails (5µg/mL) and embryos (20µg/mL after 6h of exposure). Similar activity was observed in Schistosoma mansoni cercariae after only a short exposure time (10µg/mL after 30min of exposure). The divaricatic acid did not show toxicity in the acute test using Artemia salina at concentrations equal to or below 200µg/mL. The divaricatic acid proved to be a promising substance for the elimination of the snail Biomphalaria glabrata, an intermediate host of schistosomiasis, as well as the cercariae of the pathogen, while being non-toxic to the Artemia salina at the same concentrations. This is the first experimental observation of the molluscicidal and cercaricide activity of divaricatic acid.


Subject(s)
Antiparasitic Agents/pharmacology , Biomphalaria/drug effects , Depsides/pharmacology , Molluscacides/pharmacology , Schistosoma mansoni/drug effects , Animals , Artemia , Cercaria/drug effects
3.
J. venom. anim. toxins incl. trop. dis ; J. venom. anim. toxins incl. trop. dis;17(3): 277-286, 2011. graf, tab
Article in English | LILACS | ID: lil-597226

ABSTRACT

Schistosomiasis is a major public health problem with 207 million people infected and more than 779 million at risk. The drug of choice for treating schistosomiasis is praziquantel (PZQ); however, it is inefficient against immature forms of schistosomes. The aim of this study was to test new imidazolidine derivatives LPSF/PT09 and LPSF/PT10 against adult Schistosoma mansoni worms. IC50, cytotoxicity, immune response and cell viability assays were also available for these imidazolidines. Different concentrations of imidazolidine, from 32 to 320 »M, promoted motor abnormalities in breeding and unpaired worms, and death in 24 hours at higher concentrations. Although LPSF/PT09 and LPSF/PT10 did not affect IFN-³ and IL-10 production, they induced nitric oxide production and showed a similar behavior to praziquantel on cell death test. Thus, these new imidazolidine derivatives should undergo further study to develop schistosomiasis drugs.


Subject(s)
Animals , Female , Rats , Imidazolidines/immunology , Schistosoma mansoni/immunology , Public Health
4.
J. Venom. Anim. Toxins incl. Trop. Dis. ; 17(3): 277-286, 2011. graf, tab
Article in English | VETINDEX | ID: vti-4595

ABSTRACT

Schistosomiasis is a major public health problem with 207 million people infected and more than 779 million at risk. The drug of choice for treating schistosomiasis is praziquantel (PZQ); however, it is inefficient against immature forms of schistosomes. The aim of this study was to test new imidazolidine derivatives LPSF/PT09 and LPSF/PT10 against adult Schistosoma mansoni worms. IC50, cytotoxicity, immune response and cell viability assays were also available for these imidazolidines. Different concentrations of imidazolidine, from 32 to 320 »M, promoted motor abnormalities in breeding and unpaired worms, and death in 24 hours at higher concentrations. Although LPSF/PT09 and LPSF/PT10 did not affect IFN-³ and IL-10 production, they induced nitric oxide production and showed a similar behavior to praziquantel on cell death test. Thus, these new imidazolidine derivatives should undergo further study to develop schistosomiasis drugs.(AU)


Subject(s)
Schistosomiasis/pathology , Public Health , Allergy and Immunology/classification , Imidazolidines/pharmacology
5.
Pharmazie ; 60(1): 13-7, 2005 Jan.
Article in English | MEDLINE | ID: mdl-15700773

ABSTRACT

Synthesis and physico-chemical properties of 3-benzyl-5-(4-fluoro-benzylidene)-1-methyl-2-thioxo-imidazolidin-4-ones, 5-benzylidene-3-(4-nitro-benzyl)-2-thioxo-imidazolidin-4-ones and 4-acridin-9-ylmethylene-1-benzyl-5-thioxo-imidazolidin-2-ones compounds are described. These thioxo-imidazolidine derivatives were prepared by alkylation and condensation with 4-fluoro-benzaldehyde or nucleophilic Michael addition with cyanoacrylates. The schistosomicidal activity of 3-benzyl-5-(4-fluoro-benzylidene)-1-methyl-2-thioxo-imidazolidin-4-one compounds was evaluated.


Subject(s)
Imidazolidines/chemical synthesis , Imidazolidines/pharmacology , Schistosomicides/chemical synthesis , Schistosomicides/pharmacology , Animals , Crystallography, X-Ray , Female , Indicators and Reagents , Magnetic Resonance Spectroscopy , Male , Mice , Schistosoma mansoni/drug effects , Schistosomicides/toxicity
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