A penta-substituted pyridine alkaloid from the rhizome of Jatropha elliptica (Pohl) Muell. Arg. is active against Schistosoma mansoni and Biomphalaria glabrata

Aldenir Feitosa Dos Santos,Antônio Euzébio Goulart Santana,Saskya Araújo Fonseca,Mônica Camelo Pessoa De Azevedo Albuquerque,José Valfrido Santana,Fernanda Andrade César

doi:10.1007/s00436-013-3743-2

Abstract

Jatropha elliptica is a shrub distributed throughout the north and west of Brazil and reputedly possesses a wide range of therapeutical properties. The roots of this plant possess molluscicidal activity and contain terpenoids, coumarin, lignoid, steroids and alkaloid. In the present study, we assessed the schistosomicidal, miracicidal and cercaricidal activities (against Schistosoma mansoni) and molluscicidal activities (against adults and egg masses of Biomphalaria glabrata) of the alkaloid diethyl 4-phenyl-2,6-dimethyl-3,5-pyridinedicarboxylate, isolated from the ethanol extract of the rhizome of J. elliptica, have been determined. The alkaloid was 100 % lethal to adult schistosomes within 4 days at a concentration of 50 μg/mL. Alterations were observed in the schistosome tegument occasioned by treatment with the alkaloid, such as formation of vesicles and vacuolisation. The extent of tegumental damage of the worm was proportional to the time of incubation and to the concentration of compound. The alkaloid also exhibited a potent cercaricidal activity (LC100 = 2 μg/mL); it was totally ineffective against miracicidal forms of the parasite. Moreover, the alkaloid presented strong activity against adult snails (LC90 = 36.43 μg/mL) but was inactive against their egg masses. It is observed then the potential of this compound for the development of new therapies for the treatment of schistosomiasis.

Highlights

Schistosomiasis is the second most prevalent tropical disease affecting more than 200 million people worldwide (WHO 2005; Rollemberg et al 2011)
We report the evaluation of schistosomicidal, miracidicidal or cercaricidal activities against Schistosoma mansoni and/or molluscicidal activity
An ethanolic extract of the rhizome of J. elliptica, which had previously been shown to exhibit molluscicidal activity against B. glabrata, has been subjected to fractionation guided by activity against cercariae of S. mansoni (Table 1)

Summary

Introduction

Schistosomiasis is the second most prevalent tropical disease affecting more than 200 million people worldwide (WHO 2005; Rollemberg et al 2011). Praziquantel is currently the drug of choice for the treatment of schistosomiasis. This drug does not prevent reinfections, is inactive against juvenile schistosomes and has a limited effect as well on already developed liver and spleen lesions. There is a considerable concern about the development of praziquantel resistance of some strains. These reports emphasise the need of developing new schistosomicidal drugs for the treatment of this neglected tropical disease (Magalhães et al 2009, 2010; Miranda et al 2012)

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Discussion

Conclusion