Study of the Activity of 3-benzyl-5-(4-chloro-arylazo)-4-thioxo-imidazolidin-2-one against Schistosomiasis Mansoni in Mice

Abstract

<jats:p>Previous studies conducted with the imidazolidinic derivative 3-benzyl-5-(4-chloro-arylazo)-4-thioxo-imidazolidin-2-one (LPSF-PT05) show outstanding activity against adult<jats:italic>Schistosoma mansoni</jats:italic>worms<jats:italic>in vitro</jats:italic>. In the first phase of this study,<jats:italic>S. mansoni</jats:italic>-infected mice were treated, orally, with 100 mg/Kg of the LPSF-PT05 in three formulations: Tween 80 and saline solution, oil/water (70 : 30) emulsion, and solid dispersion with polyethylene glycol (PEG). In the second phase, three other doses of the LPSF-PT05 in PEG were tested: 3, 10, 30 mg/kg. These treatment regimens significantly reduced the number of recovered worms due to increases in the solubility of the compound in this formulation; the greatest reduction (70.5%) was observed at the dose of 100 mg/kg. There was no changes in the pattern of mature egg compared to immature eggs; however there was a significant increase in the number of dead eggs. Histopathological analysis of liver tissue showed changes in morphological aspects of the hepatic parenchyma with decrease exudative-productive hepatic granuloma stages, although we found no significant differences in IFN-<jats:italic>γ</jats:italic>, IL-4, IL-10, or NO production in response to the specific antigen SEA. The results show the derivative LPSF-PT05 to be a potential candidate in the etiological treatment of schistosomiasis with a possible dampening effect of the granulomatous process.</jats:p>

Revisiting the SAR of the Antischistosomal Aryl Hydantoin (Ro 13-3978)

“…Investigation of heterocycle variants showed that the hydantoin core of 1 is required for high antischistosomal activity. In this respect, recent investigations of a series of structurally distinct 4-thiohydantoins reveal that they have activity against S. mansoni in vitro; the best of these effected a 71% worm burden reduction (WBR) in S. mansoni -infected mice when it was administered as five daily 100 mg/kg oral doses …”

Tegumental Changes in Adult Schistosoma mansoni Induced by a New Imidazolidinic Derivative

“…Among the various antischistosomal compounds already tested, the imidazolidinic derivatives are well known for their activity in several works that are studying their in vitro and in vivo efficacy, showing promising results when compared to praziquantel, a control drug available in the market for the treatment of schistosomiasis [34,32,35,53].…”

African Flora as Potential Sources of Medicinal Plants : Towards the Chemotherapy of Major Parasitic and Other Infectious Diseases : A Review

“…Active flavanones and flavonoids were reported from Baccharis retusa(Asteraceae) and Kalanchoe pinnata (Crassulaceae) (Wink, 2012). Warifteine, a Bisbenzylisoquinoline alkaloid, isolated from Cissampelos sympodialis is also an attractive candidate as it induces changes in the parasite morphology and notwithstanding the fact that the plant is commonly being used in Brazilian folk medicine against various diseases (da Silva et al, 2012). Allicin (diallyl thiosulphinate), extracted from garlic, has been tested for its anti-leishmanial activity.…”