Chemotherapie gegen Schistosomiasis

Thétiot-Laurent, Sophie; Boissier, Jérôme; Robert, Anne; Meunier, Bernard

doi:10.1002/ange.201208390

Cited by 5 publications

(1 citation statement)

References 231 publications

(274 reference statements)

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“…It affected more than 250 million people, mainly in sub-Saharan Africa (Siqueira et al, 2017). Previous study estimated that 4,400 to 200,000 people die from Schistosoma each year (Thétiot-Laurent et al, 2013). Adult worm of the parasite are not the main cause of the injuries in the mammalian host body, but the massive egg production by the female worms, is the major stimulant of chronic disease (Gryseels et al, 2006).…”

Section: Introductionmentioning

confidence: 99%

Effect of Crocus sativus aqueous extract (saffron) on Schistosoma mansoni worms in experimentally infected mice

Shaaban¹,

Ibrahim²,

Mohamed³

2019

Egypt. J. of Aquatic Biolo. and Fish.

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Saffron Granuloma Antioxidants Worm SEMThe present study is designed to evaluate the therapeutic effect of Crocus sativus(saffron) aqueous extract (CSE) alone or in combination with praziquantel on Schistosoma mansoni infected mice. Parasitological, immunological, pathological and immunohistochemical parameters and surface topography of worms were determined. Treatment of S. mansoni infected mice with saffron or PZQ revealed a significant reduction in worm burden, hepatic and intestinal ova count with a decline in granuloma diameter. There was an increase in total IgG and IL-10 blood levels after treatment with PZQ and/or CSE. Superoxide dismutase (SOD) and catalase levels were improved in infected mice treated with CSE in comparison with infected mice. Male worm surface ultrastructure examination showed a swelling, rupture of numerous tubercles with marked decrease in spines and severe peeling of tegumental dorsal surfaces after treatment with saffron. In conclusion, administration of aqueous extract of Crocus sativus is effective treatment for S. mansoni infection.

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Section: Introductionmentioning

confidence: 99%

Effect of Crocus sativus aqueous extract (saffron) on Schistosoma mansoni worms in experimentally infected mice

Shaaban¹,

Ibrahim²,

Mohamed³

2019

Egypt. J. of Aquatic Biolo. and Fish.

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Biarylalkyl Carboxylic Acid Derivatives as Novel Antischistosomal Agents

et al. 2016

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Parasitic platyhelminths are responsible for serious infectious diseases, such as schistosomiasis, which affect humans as well as animals across vast regions of the world. The drug arsenal available for the treatment of these diseases is limited; for example, praziquantel is the only drug currently used to treat ≥240 million people each year infected with Schistosoma spp., and there is justified concern about the emergence of drug resistance. In this study, we screened biarylalkyl carboxylic acid derivatives for their antischistosomal activity against S. mansoni. These compounds showed significant influence on egg production, pairing stability, and vitality. Tegumental lesions or gut dilatation was also observed. Substitution of the terminal phenyl residue in the biaryl scaffold with a 3-hydroxy moiety and derivatization of the terminal carboxylic acid scaffold with carboxamides yielded compounds that displayed significant antischistosomal activity at concentrations as low as 10 μm with satisfying cytotoxicity values. The present study provides detailed insight into the structure-activity relationships of biarylalkyl carboxylic acid derivatives and thereby paves the way for a new drug-hit moiety for fighting schistosomiasis.

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Development of Biarylalkyl Carboxylic Acid Amides with Improved Anti‐schistosomal Activity

et al. 2019

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The parasitic disease schistosomiasis is the cause of more than 200 000 human deaths per year. Although the disease is treatable, there is one major shortcoming: praziquantel has been the only drug used to combat these parasites since 1977. The risk of the emergence of resistant schistosomes is known to be increasing, as a reduced sensitivity of these parasites toward praziquantel has been observed. We developed a new class of substances, which are derived from inhibitors of human aldose reductase, and which showed promising activity against Schistosoma mansoni couples in vitro. Further optimisation of the compounds led to an increase in anti‐schistosomal activity with observed phenotypes such as reduced egg production, vitality, and motility as well as tegumental damage and gut dilatation. Here, we performed structure–activity relationship studies on the carboxylic acid moiety of biarylalkyl carboxylic acids. Out of 82 carboxylic acid amides, we identified 10 compounds that are active against S. mansoni at 25 μm. The best five compounds showed an anti‐schistosomal activity up to 10 μm and induced severe phenotypes. Cytotoxicity tests in human cell lines showed that two derivatives had no cytotoxicity at 50 or 100 μm. These compounds are promising candidates for further optimisation toward the new anti‐schistosomal agents.

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Chemotherapie gegen Schistosomiasis

Cited by 5 publications

References 231 publications

Effect of Crocus sativus aqueous extract (saffron) on Schistosoma mansoni worms in experimentally infected mice

Effect of Crocus sativus aqueous extract (saffron) on Schistosoma mansoni worms in experimentally infected mice

Biarylalkyl Carboxylic Acid Derivatives as Novel Antischistosomal Agents

Development of Biarylalkyl Carboxylic Acid Amides with Improved Anti‐schistosomal Activity

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