A penta-substituted pyridine alkaloid from the rhizome of Jatropha elliptica (Pohl) Muell. Arg. is active against Schistosoma mansoni and Biomphalaria glabrata.
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.
Grupo Estudo de Compostos Naturais Bioativos, Centro Universitário Cesmac, 57051-160, Maceió, AL, Brazil.
Aldenir Feitosa
AF
dos Santos
Saskya Araújo
SA
Fonseca
Fernanda Andrade
FA
César
Mônica Camelo Pessoa
MC
de Azevedo Albuquerque
José Valfrido
JV
Santana
Antônio Euzébio Goulart
AE
Santana
D000470:Alkaloids / Q000302:isolation & purification / Q000494:pharmacology; D000818:Animals; D001700:Biomphalaria / Q000187:drug effects*; D001938:Brazil; D031286:Jatropha / Q000737:chemistry*; D008975:Molluscacides / Q000302:isolation & purification / Q000494:pharmacology*; D010936:Plant Extracts / Q000494:pharmacology*; D011725:Pyridines / Q000302:isolation & purification / Q000494:pharmacology; D027343:Rhizome / Q000737:chemistry; D012550:Schistosoma mansoni / Q000187:drug effects*; D012556:Schistosomicides / Q000302:isolation & purification / Q000494:pharmacology*
D000470:Alkaloids; D008975:Molluscacides; D010936:Plant Extracts; D011725:Pyridines; D012556:Schistosomicides; C023666:pyridine