Biopharmaceutics and Biologic Drugs

Schistosomiasis is a neglected tropical disease that infects over 200 million people worldwide and it is caused by schistosomes (parasitic trematodes). Its treatment relies only on Praziquantel, a drug which shows toxic side eff ects, lack of eff ectiveness against young worms and it may be less useful in the future due to the drug-resistance of schistosomes. Th us, alternative drugs for the treatment are required. Th e crude ethanolic stem extract from Vellozia variabillis (Velloziaceae) has shown in vitro schistosomicidal activity against adult worms of Schistosoma mansoni. Further, the fl avoliganan hydnocarpin D (Figure 1) was isolated from stem extract by chromatographic fractionation plus preparative HPLC; identifi ed by ¹H- NMR, ¹³C-NMR, mass spectrometry methods and evaluated in vitro against S. mansoni. Adult worms of S. mansoni LE strain was recovered from the mesenteric veins of the infected mice and cultured in 24-well plates at 37°C in RPMI1640 media. Hydnocarpin D was dissolved in 10% DMSO and diluted into the medium to give 12.5, 25, 50, 100 and 200 μM. Adult worms were kept for 72 hours and the viability was monitored every 24 hours. As negative control was used adult worms treated with 10% DMSO. Th e biological assay has shown that Hydnocarpin D caused the death of the S. mansoni adult worms (100% at 200 and 100 μM, and 75% at 50 μM aft er 48 hours; 100% at 25 μM aft er 72 hours) and reduced the motor activity signifi cantly of 100% of the adult worms (25, 50, 100, 200 μM aft er 24 hours and at 12,5μM aft er 72 hours). It was also registered a partial tegument alteration at 50, 100 and 200μM. Hydnocarpin D showed good results and can be a good choice to futures studies for the seeking of alternative drugs to schistosomiasis treatment.