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A penta-substituted pyridine alkaloid from the rhizome of Jatropha elliptica (Pohl) Muell. Arg. is active against Schistosoma mansoni and Biomphalaria glabrata
Authors:Aldenir Feitosa dos Santos  Saskya Araújo Fonseca  Fernanda Andrade César  Mônica Camelo Pessoa de Azevedo Albuquerque  José Valfrido Santana  Antônio Euzébio Goulart Santana
Affiliation:1. Grupo Estudo de Compostos Naturais Bioativos, Centro Universitário Cesmac, 57051-160, Maceió, AL, Brazil
2. Grupo de Pesquisa em Química, Universidade Estadual de Alagoas, 57312-270, Arapiraca, AL, Brazil
3. Laboratório de Imunologia e Esquistossomose Experimental, Laboratório de ImunopatologiaKeizoAsami, Universidade Federal de Pernambuco, 50670-901, Recife, PE, Brazil
4. Laboratório de Pesquisa em Recursos Naturais, Instituto de Química e Biotecnologia, Universidade Federal de Alagoas, 57092-970, Maceió, AL, Brazil
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.
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