Antischistosomal action of thioxo-imidazolidine compounds: An ultrastructural and cytotoxicity study

• Published in: Experimental parasitology Vol. 128; no. 1; pp. 82 - 90
• Main Authors: Neves, Juliana Kelle A.L., de Lima, Maria do Carmo Alves, Pereira, Valéria Rego Alves, de Melo, Cristiane Moutinho Lagos, Peixoto, Christina Alves, Pitta, Ivan da Rocha, Albuquerque, Mônica Camelo Pessoa Azevedo, Galdino, Suely Lins
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Inc 01-05-2011; Elsevier
• Subjects: adults; Animals; Annexin A5 - chemistry; Apoptosis - drug effects; Biological and medical sciences; Biomphalaria; cell death; Cell Survival - drug effects; cytotoxicity; drugs; Enzyme Inhibitors - chemistry; Female; Fluorescein-5-isothiocyanate - chemistry; Fluorescent Dyes - chemistry; Fundamental and applied biological sciences. Psychology; Imidazolidines - pharmacology; Imidazolidines - toxicity; Imidazolidinone derivatives; in vitro; Indicators and Reagents - chemistry; Life cycle. Host-agent relationship. Pathogenesis; Male; markets; Mice; Mice, Inbred BALB C; Microscopy, Electron, Scanning; Necrosis; parasitology; people; Praziquantel; Praziquantel - pharmacology; Praziquantel - toxicity; Propidium - chemistry; Protozoa; Schistosoma mansoni; Schistosoma mansoni - drug effects; Schistosoma mansoni - ultrastructure; Schistosomiasis; Schistosomiasis mansoni - drug therapy; Schistosomiasis mansoni - parasitology; Schistosomicides - pharmacology; Schistosomicides - toxicity; Spleen - cytology; Spleen - drug effects; Spleen - pathology; therapeutics; Schistosomiasis; Schistosoma mansoni; Imidazolidinone derivatives; Praziquantel; in vitro; Trematode disease; Plathelmintha; Parasite; Cytotoxicity; Parasitosis; Helminthiasis; In vitro; Trematoda; Infection; Helmintha; Imidazolidinone derivatives in vitro; Invertebrata
• ISSN: 0014-4894; 1090-2449
• DOI: 10.1016/j.exppara.2011.01.021

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► LPSF/PT-5 and LPSF/PT-11 are new imidazolidine compounds. ► These compounds induced tegument damage in S. mansoni in vitro. ► LPSF/PT-5 and LPSF/PT-11 showed similar behavior than Praziquantel. ► These imidazolidines can be used as anti-Schistosome compound on in vitro assays.
Schistosomiasis is a disease caused by helminthes of the genus Schistosoma, which threatens approximately 207 million people worldwide. Recently, strains of Schistosoma mansoni appear to be developing tolerance and resistance against Praziquantel, the most commonly available drug on the market used in the treatment of disease. This worrisome development justifies studies that seek alternatives for the prevention, treatment and cure of this disease. This study aimed to evaluate the in vitro activity of new imidazolidine compounds 1-benzyl-4-[(4-chloro-phenyl)-hydrazono]-5-thioxo-imidazolidin-2-one (LPSF/PT-5) and 1-(4-chloro-benzyl)-4-[(4-fluoro-phenyl)-hydrazono]-5-thioxo-imidazolidin-2-one (LPSF/PT-11) against adult worms of S. mansoni. LPSF/PT-5 and LPSF/PT-11 imidazolidine derivatives showed relevant schistosomicidal activity in vitro and induced significant ultrastructural alterations in worms and cell death: results similar to praziquantel. Thus, it is possible that these imidazolidine derivatives can be future candidates as schistosomotic drugs, but further studies are needed to elucidate the induced mechanisms behind this response.