BACKGROUND Praziquantel has been cited as the only drug for treating schistosomiasis.
However, concerns over drug resistance have encouraged the search for novel drug
leads. The antimalarial drug primaquine possesses interesting anti-schistosmal
properties.OBJECTIVES This study is the first to document the potential role of primaquine as a
schistosomicide and the ultrastructural changes induced by primaquine on juvenile
or adult male worms of Schistosoma mansoni.METHODS Ultrastructural alterations in the tegumental surface of 21-day-old juvenile and
adult male worms of S. mansoni were demonstrated following
primaquine treatment at different concentrations (2, 5, 10, 15, and 20 µg/mL) and
incubation periods (1, 3, 6, 24, and 48 h) in vitro, using both scanning and
transmission electron microscopy.FINDINGS At low concentrations (2, 5, and 10 µg/mL) both juvenile and adult male worms
were alive after 24 h of incubation, whereas contraction, paralysis, and death of
all worms were observed after 24 h of drug exposure at 20 µg/mL. The tegument of
juvenile and adult male worms treated with primaquine exhibited erosion, peeling,
and sloughing. Furthermore, extensive damage of both tegumental and subtegumental
layers included embedded spines, and shrinkage of muscles with vacuoles. The in
vitro results confirmed that primaquine has dose-dependent effects with 20 µg/mL
as the most effective concentration in a short incubation period.MAIN CONCLUSIONS The schistosomicidal activity of primaquine indicates that this drug possesses
moderate in vitro activity against juvenile and adult male worms, since it caused
high mortality and tegumental alterations. This study confirmed that the
antimalarial drug primaquine possesses anti-schistosomal activity. Further
investigation is needed to elucidate its mechanism of action.