Antischistosomal activity of a calcium channel antagonist on schistosomula and adult Schistosoma mansoni worms
Current schistosomiasis control strategies are largely based on chemotherapeutic agents and a limited number of drugs are available today. Praziquantel (PZQ) is the only drug currently used in schistosomiasis control programs. Unfortunately, this drug shows poor efficacy in patients during the earli...
| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
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Fundação Oswaldo Cruz (FIOCRUZ)
2013-08-01
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| Series: | Memorias do Instituto Oswaldo Cruz |
| Subjects: | |
| Online Access: | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762013000500600&lng=en&tlng=en |
| _version_ | 1827833058130132992 |
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| author | Vanessa Silva-Moraes Flávia Fernanda Bubula Couto Marah Mileib Vasconcelos Neusa Araújo Paulo Marcos Zech Coelho Naftale Katz Rafaella Fortini Queiroz Grenfell |
| author_facet | Vanessa Silva-Moraes Flávia Fernanda Bubula Couto Marah Mileib Vasconcelos Neusa Araújo Paulo Marcos Zech Coelho Naftale Katz Rafaella Fortini Queiroz Grenfell |
| author_sort | Vanessa Silva-Moraes |
| collection | DOAJ |
| description | Current schistosomiasis control strategies are largely based on chemotherapeutic agents and a limited number of drugs are available today. Praziquantel (PZQ) is the only drug currently used in schistosomiasis control programs. Unfortunately, this drug shows poor efficacy in patients during the earliest infection phases. The effects of PZQ appear to operate on the voltage-operated Ca2+channels, which are located on the external Schistosoma mansoni membrane. Because some Ca2+channels have dihydropyridine drug class (a class that includes nifedipine) sensitivity, an in vitro analysis using a calcium channel antagonist (clinically used for cardiovascular hypertension) was performed to determine the antischistosomal effects of nifedipine on schistosomula and adult worm cultures. Nifedipine demonstrated antischistosomal activity against schistosomula and significantly reduced viability at all of the concentrations used alone or in combination with PZQ. In contrast, PZQ did not show significant efficacy when used alone. Adult worms were also affected by nifedipine after a 24 h incubation and exhibited impaired motility, several lesions on the tegument and intense contractility. These data support the idea of Ca2+channels subunits as drug targets and favour alternative therapeutic schemes when drug resistance has been reported. In this paper, strong arguments encouraging drug research are presented, with a focus on exploring schistosomal Ca2+channels. |
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| format | Article |
| id | doaj.art-0cdce419e77c4023a7bd6c5ffa79fabe |
| institution | Directory Open Access Journal |
| issn | 1678-8060 |
| language | English |
| last_indexed | 2024-03-12T05:24:24Z |
| publishDate | 2013-08-01 |
| publisher | Fundação Oswaldo Cruz (FIOCRUZ) |
| record_format | Article |
| series | Memorias do Instituto Oswaldo Cruz |
| spelling | doaj.art-0cdce419e77c4023a7bd6c5ffa79fabe2023-09-03T07:25:04ZengFundação Oswaldo Cruz (FIOCRUZ)Memorias do Instituto Oswaldo Cruz1678-80602013-08-01108560060410.1590/0074-0276108052013011S0074-02762013000500600Antischistosomal activity of a calcium channel antagonist on schistosomula and adult Schistosoma mansoni wormsVanessa Silva-MoraesFlávia Fernanda Bubula CoutoMarah Mileib VasconcelosNeusa AraújoPaulo Marcos Zech CoelhoNaftale KatzRafaella Fortini Queiroz GrenfellCurrent schistosomiasis control strategies are largely based on chemotherapeutic agents and a limited number of drugs are available today. Praziquantel (PZQ) is the only drug currently used in schistosomiasis control programs. Unfortunately, this drug shows poor efficacy in patients during the earliest infection phases. The effects of PZQ appear to operate on the voltage-operated Ca2+channels, which are located on the external Schistosoma mansoni membrane. Because some Ca2+channels have dihydropyridine drug class (a class that includes nifedipine) sensitivity, an in vitro analysis using a calcium channel antagonist (clinically used for cardiovascular hypertension) was performed to determine the antischistosomal effects of nifedipine on schistosomula and adult worm cultures. Nifedipine demonstrated antischistosomal activity against schistosomula and significantly reduced viability at all of the concentrations used alone or in combination with PZQ. In contrast, PZQ did not show significant efficacy when used alone. Adult worms were also affected by nifedipine after a 24 h incubation and exhibited impaired motility, several lesions on the tegument and intense contractility. These data support the idea of Ca2+channels subunits as drug targets and favour alternative therapeutic schemes when drug resistance has been reported. In this paper, strong arguments encouraging drug research are presented, with a focus on exploring schistosomal Ca2+channels.http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762013000500600&lng=en&tlng=enSchistosoma mansoniantischistosomal drugscalcium channels antagonistsL-type calcium channelsnifedipine |
| spellingShingle | Vanessa Silva-Moraes Flávia Fernanda Bubula Couto Marah Mileib Vasconcelos Neusa Araújo Paulo Marcos Zech Coelho Naftale Katz Rafaella Fortini Queiroz Grenfell Antischistosomal activity of a calcium channel antagonist on schistosomula and adult Schistosoma mansoni worms Memorias do Instituto Oswaldo Cruz Schistosoma mansoni antischistosomal drugs calcium channels antagonists L-type calcium channels nifedipine |
| title | Antischistosomal activity of a calcium channel antagonist on schistosomula and adult Schistosoma mansoni worms |
| title_full | Antischistosomal activity of a calcium channel antagonist on schistosomula and adult Schistosoma mansoni worms |
| title_fullStr | Antischistosomal activity of a calcium channel antagonist on schistosomula and adult Schistosoma mansoni worms |
| title_full_unstemmed | Antischistosomal activity of a calcium channel antagonist on schistosomula and adult Schistosoma mansoni worms |
| title_short | Antischistosomal activity of a calcium channel antagonist on schistosomula and adult Schistosoma mansoni worms |
| title_sort | antischistosomal activity of a calcium channel antagonist on schistosomula and adult schistosoma mansoni worms |
| topic | Schistosoma mansoni antischistosomal drugs calcium channels antagonists L-type calcium channels nifedipine |
| url | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762013000500600&lng=en&tlng=en |
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