Is there reduced susceptibility to praziquantel in <i>Schistosoma japonicum</i>? Evidence from China

Wang, Wei; Dai, Jianrong; Zhang, Dongliang; Shen, Xue-Hui; Liang, You-Sheng

doi:10.1017/s0031182010001204

Cited by 43 publications

(28 citation statements)

References 36 publications

(47 reference statements)

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“…However, it has been demonstrated that by sustained drug pressure on S. mansoni strain under laboratorial conditions, resistance to praziquantel could develop (Fallon and Doenhoff 1994), and it has been found in some schistosome-endemic areas of Africa and North America that there were schistosome strains having tolerance or resistance to praziquantel (Fallon et al 1995;Stelma et al 1995;Ismail et al 1996;Melman et Whether resistance to praziquantel can develop and spread in the endemic foci of schistosomiasis has aroused widespread concern (Cioli and Pica-Mattoccia 2003;Wang et al 2010). Therefore, as a response to the emergence of resistance to praziquantel, it is a pressing need to screening, research and development of novel antischistosomal drugs (Cioli 1998(Cioli , 2000Cioli et al 2008).…”

Section: Discussionmentioning

confidence: 99%

“…Unfortunately, with the long term, repeated praziquantel treatment may cause the worry about the praziquantel resistance or reduced susceptibility (Cioli and Pica-Mattoccia 2003;Wang et al 2010). It was worth noting that the praziquantel-resistant isolate of Schistososma mansoni had been established successfully in the laboratory since the 1990s (Fallon and Doenhoff 1994).…”

Section: Introductionmentioning

confidence: 99%

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Effect of the in vivo activity of dihydroartemisinin against Schistosoma mansoni infection in mice

Liu

Wang

et al. 2011

Parasitol Res

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Dihydroartemisinin, formerly known as an antimalarial drug, is the main metabolite of the mother compound artemisinins, as well as of artemether and artesunate. It has been shown that the drug exhibits antischistosomal efficacy against Schistosoma japonicum.The purpose of the current study was to assess the in vivo effect of dihydroartemisinin against Schistosoma mansoni infection in mice. Drugs at a single oral dose of 300 mg/kg were given to mice to assess the efficacy against different developmental stages of the parasite; juvenile and adult S. mansoni were treated with single doses of dihydroarteminisin with different regimens (at 200, 300, 400 or 600 mg/kg) in the stage of drug sensitivity, and the dose-response relationship was assessed; and the effect of multiple doses (at 200, 300 or 400 mg/kg) on juvenile and adult S. mansoni was also observed. The results showed that a single oral dose (300 mg/kg) of dihydroartemisinin reduced total worm burdens by 13.8-82.1% and female worm burdens by 13-82.8%, and the greatest reductions were seen when treatment was given on day 21 post-infection, with total and female worm burden reductions of 82.1% and 82.8%. Administration of a single oral dose of dihydroartemisinin on day 21 post-infection with different drug dosage (at 200, 300, 400 or 600 mg/kg) reduced total worm burdens by 70.3-87.3% and female worm burdens by 73.5-92.4%, depending on dosage. Similar treatments given on day 49 post-infection reduced total worm burdens by 48.7-68.73% and female worm burdens by 63.25-94.6%. There was obvious dose-response relationship of dihydroartemisinin against the schistosomula and adult worms of S. mansoni observed. Administration with dihydroartemisinin at oral doses of 200, 300 and 400 mg/kg, given once on each of days 20-22 post-infection of three successive days, reduced total worm burdens by 88.5-90.1% and female worm burdens by 89.2-92.1%, depending on dosage. Similar treatments given once on each of days 48-50 post-infection reduced total worm burdens by 60-70.3% and female worm burdens by 77.5-94.9%. It is concluded that dihydroartemisinin exhibits in vivo activity against various developmental stages of S. mansoni, particularly the 21-day schistosomula, and there is obvious dose-response relationship of dihydroartemisinin against the schistosomula and adult worms of S. mansoni observed.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Effect of the in vivo activity of dihydroartemisinin against Schistosoma mansoni infection in mice

Liu

Wang

et al. 2011

Parasitol Res

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“…Emergence of resistance of S. japonicum to PZQ1 has also received attention (101)(102)(103)(104)(105). However, despite large-scale and repeated use, the current efficacy of PZQ1 remains unchanged and it is highly effective at a curative dosage (a single dose of 40 mg/kg) in the main areas of China where schistosomiasis is endemic (106)(107)(108). Seto et al (106) conducted a cross-sectional survey, in which the efficacy of PZQ1 was evaluated in 33 villages in Sichuan Province, where the prevalence of infection was found to be 5.7%.…”

Section: Pzq Resistance In the Fieldmentioning

confidence: 99%

Praziquantel for Schistosomiasis: Single-Drug Metabolism Revisited, Mode of Action, and Resistance

Vale

Gouveia

Rinaldi

et al. 2017

Antimicrob Agents Chemother

264

218

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Schistosomiasis, a major neglected tropical disease, affects more than 250 million people worldwide. Treatment of schistosomiasis has relied on the anthelmintic drug praziquantel (PZQ) for more than a generation. PZQ is the drug of choice for the treatment of schistosomiasis; it is effective against all major forms of schistosomiasis, although it is less active against juvenile than mature parasites. A pyrazino-isoquinoline derivative, PZQ is not considered to be toxic and generally causes few or transient, mild side effects. Increasingly, mass drug administration targeting populations in sub-Saharan Africa where schistosomiasis is endemic has led to the appearance of reduced efficacy of PZQ, which portends the selection of drugresistant forms of these pathogens. The synthesis of improved derivatives of PZQ is attracting attention, e.g., in the (i) synthesis of drug analogues, (ii) rational design of pharmacophores, and (iii) discovery of new compounds from large-scale screening programs. This article reviews reports from the 1970s to the present on the metabolism and mechanism of action of PZQ and its derivatives against schistosomes.

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“…However, PZQ does not prevent re-infections, it is inactive against juvenile schistosomes, has limited effect on parasite liver forms (Utzinger et al, 2003). Moreover, the reliance on one single antischistosomal drug has culminated in the development of resistant schistosome strains at an alarming rate (Wang et al, 2010;Engels et al, 2002;Ismail et al, 1999), thus the above mentioned observation motivated us to investigate Tagetes erecta L. aiming at the design of novel and inexpensive drugs against Schistosomiasis.…”

Section: Introductionmentioning

confidence: 99%

In vitro schistosomicidal effects of the essential oil of Tagetes erecta

Tonuci¹,

Melo²,

Dias³

et al. 2012

Rev. bras. farmacogn.

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Abstract:The in vitro schistosomicidal effects of the essential oil obtained from Tagetes erecta L. Asteraceae, leaves (TE-EO) collected in Brazil against Schistosoma mansoni worms are reported in this paper. The oil caused a significant decrease in the motor activity at 50 μg/mL as minimal concentration after 24 h. This oil also caused death of all the parasites and the separation of coupled pairs into individual male and female at 100 μg/mL after 24 h. The viability of adult worm groups treated with the TE-EO at 100 μg/mL was similar to that of groups treated with praziquantel (positive control). In addition, the oil promoted the inhibition of eggs development at all the tested concentrations. These data indicate that the TE-EO could be considered as a promising source for the development of new schistosomicidal agents.

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Is there reduced susceptibility to praziquantel in Schistosoma japonicum? Evidence from China

Cited by 43 publications

References 36 publications

Effect of the in vivo activity of dihydroartemisinin against Schistosoma mansoni infection in mice

Effect of the in vivo activity of dihydroartemisinin against Schistosoma mansoni infection in mice

Praziquantel for Schistosomiasis: Single-Drug Metabolism Revisited, Mode of Action, and Resistance

In vitro schistosomicidal effects of the essential oil of Tagetes erecta

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