Synthesis and properties of praziquantel, a novel broad spectrum anthelmintic with excellent activity against Schistosomes and Cestodes

Seubert, J.; Pohlke, R.; Loebich, F.

doi:10.1007/bf01945954

Cited by 123 publications

(42 citation statements)

References 2 publications

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“…Praziquantel (2-cyclohexylcarbonyl-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinolin-4-one) was synthesized in the 1970s (59). While undergoing initial veterinary screening it showed efficacy against cestodes (33,62).…”

Section: Antischistosomal Properties Of Praziquantelmentioning

confidence: 99%

Combination Chemotherapy of Schistosomiasis in Laboratory Studies and Clinical Trials

Utzinger

Keiser

Shuhua

et al. 2003

Antimicrob Agents Chemother

188

124

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Section: Antischistosomal Properties Of Praziquantelmentioning

confidence: 99%

Combination Chemotherapy of Schistosomiasis in Laboratory Studies and Clinical Trials

Utzinger

Keiser

Shuhua

et al. 2003

Antimicrob Agents Chemother

188

124

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“…Schistosomiasis mostly affects the liver and intestine with granuloma formation; necrosis and fibrosis are more common in hepatic tissues [16]. Praziquantel (PZQ), a drug used for treatment of schistosomiasis, was developed by Seubert et al [52]. Praziquantel and Oxamniquine have been extensively used in the treatment of schistosomiasis with good efficiency and low toxicity [32].…”

Section: Introductionmentioning

confidence: 99%

Schistosoma mansoni: Antiparasitic effects of orally administeredNigella sativaoil and/orChroococcus turgidusextract

Ali

Eldahab

Mansour

et al. 2016

Acta Biologica Hungarica

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Schistosoma mansoni is one of the parasites causing schistosomiasis, a disease which threatens millions of people all over the world. Traditional chemical drugs are not fully effective against schistosomaisis due to the evolving drug resistant worm strains, so exploring new remedies derived from natural products is a good way to fight schistosomiasis. In the present investigation two natural products, Nigella sativa oil and Chroococcus turgidus extract were used separately or in a combination to explore their effect on S. mansoni. The infected mice treated with Chroococcus turgidus extract or/and sativa seed oil showed a significant decrease in the total worm burden. The total number of deposited eggs by females of S. mansoni was significantly decreased in the liver of mice treated with Chroococcus turgidus extract or/and sativa seed oil. However, in the intestine, the number of eggs was significantly reduced in mice treated with algal extract and those treated with both algal extract and oil. Fecundity of female S. mansoni showed a significant decrease from mice treated with algal extract or/and sativa seed oil. According to SEM investigations the tegmental surface, oral and ventral suckers of worms also showed considerable changes; as the tubercles lost their spines, some are swollen and torn out. The suckers become edematous and enlarged while the tegmental surface is damaged due to the treatment with Chroococcus turgidus extract or/and sativa seed oil. In conclusion, the Nigella sativa oil and Chroococcus turgidus extract are promising natural compounds that can be used in fighting schistosomiasis.

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“…The drug of choice for treating all schistosome species is Praziquantel (PZQ).It was developed in the late 1970s (Seubert et al, 1977) and has become the only available drug used in control programs (Doenhoff et al, 2008).However, this drug is not effective in the treatment of immature forms or preventing re-infection (Magnussen, 2003). Furthermore, the extensive usage of PZQ, in non-infected and non-diagnosed individuals for prevention, lead to emergence of resistant strains of Schistosoma mansoni (Melman et The resistance of PZQ has already been documented in Egypt and Senegal, in conjunction with new findings about its metabolism and genotoxic properties.…”

Section: Introduction:-mentioning

confidence: 99%

Antiparasitic and physiological evaluation of Curcuma longa extract and/or PZQ on Schistosoma mansoni infected mice.

Aboueldahab¹,

Elhussieny.²

2016

IJAR

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Praziquantel (PZQ) is the drug of choice against schistosomiasis. However, PZQ was found not fully effective. A new trend from natural plant sources was used to compete schistosomiasis. In the present study, the antischistosomal activities of Curcumin extract and /or PZQ were evaluated. Parasitological and histopathological examination of liver has been explored. Moreover, Surface topography of the recovered worms was inspected by SEM. On the other hand, the total protein and DNA fragmentation percentage were estimated in infected and infected treated mice as compared to control group. Treatment of infected CD1 mice with curcumin extract alone didn't show any detectable changes in the parasitological or histological parameters. The infected mice treated with PZQ only, showed a significant decrease in the total worm burden, egg load (52%), with increase in degenerated eggs (58%) in the oogram pattern.However, treating infected CD1 mice with combined therapy (curcumin extract + PZQ) showed extremely significant reduction in female and male worm count (93% & 84%) respectively. Liver tissue egg load decreased by 88%, intestinal egg load decreased by 97%. Combined therapy decreased granuloma count and diameter with significant increase in degenerated egg in the oogram count. Moreover, the studied biomarkers, related to liver function and DNA damage were significantly improved in infected mice treated with curcumin combined with PZQ as compared to either drug alone. . In conclusion, curcumin extract in combination with PZQ has a synergetic effect and could be more promising in controlling schistosomiasis.Copy Right, IJAR, 2016,. All rights reserved.

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Synthesis and properties of praziquantel, a novel broad spectrum anthelmintic with excellent activity against Schistosomes and Cestodes

Abstract: Synthesis and properties of 2-cyclohexylcarbonyl-1,3,4,6,7,11b-hexahydro-2H-pyrazino [2,1-a] isoquinolin-4-one, a novel anthelmintic with excellent activity against all species of Schistosomes pathogenic to man and a wide range of cestodes, will be reported.

Cited by 123 publications

References 2 publications

Combination Chemotherapy of Schistosomiasis in Laboratory Studies and Clinical Trials

Combination Chemotherapy of Schistosomiasis in Laboratory Studies and Clinical Trials

Schistosoma mansoni: Antiparasitic effects of orally administeredNigella sativaoil and/orChroococcus turgidusextract

Antiparasitic and physiological evaluation of Curcuma longa extract and/or PZQ on Schistosoma mansoni infected mice.

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