Skip to content
Research Article Open access CC BY 3.0

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

Anekécia Lauro da Silva, Sheilla Andrade de Oliveira, Jamerson Ferreira de Oliveira, Edna de Farias Santiago, Antônio Sérgio Alves de Almeida Júnior, Íris Trindade Tenório Jacobi, Christina Alves Peixoto, Vinícius Pinto Costa Rocha, Milena Botelho Pereira Soares, Ivan da Rocha Pitta, Maria do Carmo Alves de Lima

Journal of Pharmaceutical Research International · pp. 1988–2005 · Published 16 Aug 2014

10.9734/BJPR/2014/12511

Abstract

Aims: Verify the potential of the schistosomicidal imidazolidine derivative (5Z)-3-(4-bromo-benzyl)-5-(4-chloro-benzylidene)-4-thioxo-imidazolidin-2-one. Study Design: In this study, we tested the imidazolidinic derivative 3 through in vitro evaluations, cytotoxicity assay and analysis of Scanning Electron Microscopy to verify its therapeutic potential in the treatment of schistosomiasis. Place and Duration of Study: Departamento de Antibióticos, Universidade Federal de Pernambuco (UFPE), Fundação Oswaldo Cruz (FIOCRUZ)/PE and (FIOCRUZ)/BA between January 2013 and march 2014. Methodology: This study was approved by the Ethics Committee on Animal Use Research Center Aggeu Magalhães/Oswaldo Cruz Fundação (CPqAM/FIOCRUZ) authorized by the license No. 21/2011. Male albino Swiss mice were used Mus musculus 25 days old weighing 50 grams. Compound 3 was assayed for its cytotoxicity through cell J774 macrophage lineage. The amount of inhibitory concentration (LC50) was determined by nonlinear regression using the Graph Pad Prism version 5.01. Then the compound was evaluated against adult worms of S. mansoni by performing the activity in vitro at doses 100-20µg/mL and ultrastructural investigation by Scanning Electron Microscopy (SEM) at doses of 100 and 60μg/ml. The PZQ was the positive control of the experiment. Results: The derivative 3 showed LC50 of 29.7±3.9mM. Compound 3 was able to have decreased motility of S. mansoni culminating with a mortality rate of 100% at doses of 60 and 100µg/mL on the fourth day of observation of the experiment. In the SEM, the compound caused various soft tissue changes of S. mansoni parasites such as blistering, destruction of the integument with loss of spines and tubercles, body contraction and windy. Conclusion: The derivative imidazolidine 3 showed a promising schistosomicidal activity in vitro. However, conducting further studies with the completion of work in front of the live schistosomiasis is required.

Schistosomiasis imidazolidines tegument microscopy

References (51)

  1. 1 An Improved Perfusion Technique for Recovering Adult Schistosomes from Laboratory Animals [DOI]
  2. 2 Parasites and poverty: The case of schistosomiasis [DOI]
  3. 3 In vitro and in vivo experimental models for drug screening and development for Chagas disease [DOI]
  4. 4 The sedimentation-concentration method in Schistostomiasis mansoni.
  5. 5 Schistosomiasis elimination: lessons from the past guide the future [DOI]
  6. 6 Schistosoma mansoni: In vitro schistosomicidal activity of piplartine [DOI]
  7. 7 Morphological effects and tegumental alterations induced by mefloquine on schistosomula and adult flukes ofSchistosoma mansoni [DOI]
  8. 8 The role of tegumental aquaporin from the human parasitic worm, Schistosoma monsoni , in osmoregulation and drug uptake [DOI]
  9. 9 Light and electron microscopic studies on the effect of praziquantel onSchistosoma mansoni, Dicrocoelium dendriticum, andFasciola hepatica (trematoda) in vitro [DOI]
  10. 10 In vivo and in vitro experiments on the effects of praziquantel on Schistosoma mansoni. A light and electron microscopic study.
  11. 11 Ultrastructure of the Tegument of Adult Schistosoma mansoni [DOI]
  12. 12 Medicinal chemistry: An introduction [DOI]
  13. 13 Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones [DOI]
  14. 14 Imidazolidines as new anti-Trypanosoma cruzi agents: Biological evaluation and structure–activity relationships [DOI]
  15. 15 Analogues of Fenarimol Are Potent Inhibitors of Trypanosoma cruzi and Are Efficacious in a Murine Model of Chagas Disease [DOI]
  16. 16 Evaluation of the Anti-Schistosoma mansoni Activity of Thiosemicarbazones and Thiazoles [DOI]
  17. 17 Synthesis and Biological Activity of Novel Acridinylidene and Benzylidene thiazolidinediones [DOI]
  18. 18 Ultrastructural alterations in adult Schistosoma mansoni caused by artemether [DOI]
  19. 19 Ultrastructural analysis of miltefosine-induced surface membrane damage in adult Schistosoma mansoni BH strain worms [DOI]
  20. 20 Neuropeptides in Helminths: Occurrence and Distribution [DOI]
  21. 21 Transmission electron microscopic observation on ultrastructural alterations in Schistosoma japonicum caused by mefloquine [DOI]
  22. 22 Potential central nervous system antitumor agents. Hydantoin derivatives [DOI]
  23. 23 (Z)- and (E)-5-Arylmethylenehydantoins: spectroscopic properties and configuration assignment [DOI]
  24. 24 Praziquantel binds Schistosoma mansoni adult worm actin [DOI]
  25. 25 Molecular Identification of a Schistosoma mansoni Tegumental Protein with Similarity to Cytoplasmic Dynein Light Chains [DOI]
  26. 26 Temporal differences in praziquantel- and oxamniquine-induced tegumental damage to adult Schistosoma mansoni: implications for drug-antibody synergy [DOI]
  27. 27 Effects of garlic on albino mice experimentally infected with Schistosoma mansoni: a parasitological and ultrastructural study.
  28. 28 The effect of free and polyethylene glycol–liposome-entrapped albendazole on larval mobility and number in Toxocara canis infected mice [DOI]
  29. 29 Glutamate-mediated signaling in Schistosoma mansoni: A novel glutamate receptor is expressed in neurons and the female reproductive tract [DOI]
  30. 30 Adult worm tegumental damage and egg-granulomas in praziquantel-resistant and -susceptible Schistosoma mansoni treated in vivo [DOI]
  31. 31 Biological and immunological activity of new imidazolidines against adult worms of Schistosoma mansoni [DOI]
  32. 32 Evidence for the presence of glutamatergic receptors in adult Schistosoma mansoni [DOI]
  33. 33 Synthesis and structural study of arylidene thiazolidine and benzothiazine compounds [DOI]
  34. 34 Antischistosomal action of thioxo-imidazolidine compounds: An ultrastructural and cytotoxicity study [DOI]
  35. 35 Scanning electron microscopy of the human low-density lipoprotein interaction with the tegument of Schistosoma mansoni [DOI]
  36. 36 The discovery of Schistosomiasis mansoni in Brazil [DOI]
  37. 37 New imidazolidinic bioisosters: potential candidates for antischistosomal drugs [DOI]
  38. 38 Effect of single-dose oral artemether and tribendimidine on the tegument of adult Clonorchis sinensis in rats [DOI]
  39. 39 The Integument of Schistosoma Mansoni [DOI]
  40. 40 The amount of acetylcholinesterase on the parasite surface reflects the differential sensitivity of schistosome species to metrifonate [DOI]
  41. 41 Schistosoma mansoni: Surface membrane stability in vitro and in vivo [DOI]
  42. 42 The effects of 3-methylclonazepam on Schistosoma mansoni musculature are not mediated by benzodiazepine receptors [DOI]
  43. 43 A resposta do Schistosoma mansoni mantido in vitro frente a derivados imidazolidinonicos
  44. 44 Study of the Activity of 3-benzyl-5-(4-chloro-arylazo)-4-thioxo-imidazolidin-2-one against Schistosomiasis Mansoni in Mice [DOI]
  45. 45 Transmission and scanning electron microscopical studies in the tegument of male Schistosoma mansoni after oxamniquine treatment [DOI]
  46. 46 Schistosoma mansoni: Ultrastructure of adults from mice treated with oxamniquine [DOI]
  47. 47 Tegumental alterations in juvenile Schistosoma haematobium harboured in hamsters following artemether treatment [DOI]
  48. 48 Experimental use of black-seed oil against Schistosoma mansoni in albino mice: II. Surface topography of adult worms.
  49. 49 Crystallographic and spectroscopic studies of 5-arylidene-2-amino-imidazol-4-ones [DOI]
  50. 50 Comparative Effects of Hycanthone in Schistosoma Mansoni and Schistosoma Japonicum [DOI]
  51. 51 Tegumental changes in 21-day-old Schistosoma mansoni harboured in mice treated with artemether [DOI]

Cited by 14

Therapeutic potential of hydantoin and thiohydantoin compounds against Schistosoma mansoni: An integrated in vitro, DNA, ultrastructural, and ADMET in silico approach

Antônio Sérgio de Almeida Júnior, Mayse Manuele Freitas Viana Leal, Diego Santa Clara Marques · Molecular and Biochemical Parasitology · 2024

In vivo study of schistosomicidal action of 1-benzyl-4-[(4-fluoro-phenyl)-hydrazono]-5-thioxo-imidazolidin-2-one

Anekécia Lauro da Silva, Jamerson Ferreira de Oliveira, Willams Leal Silva · Biomedicine & Pharmacotherapy · 2016

Synthesis, in vitro schistosomicidal activity and ultrastructural alterations caused by thiosemicarbazones and thiazolidinones against juvenile and adult Schistosoma mansoni worms (Sambon, 1907)

Rubens Emanoel Tavares da Rocha, Antônio Sérgio Alves de Almeida Júnior, Nairomberg Cavalcanti Portela Júnior · Molecular and Biochemical Parasitology · 2022

Assessment of tegumental damage to Schistosoma mansoni and S. haematobium after in vitro exposure to ferrocenyl, ruthenocenyl and benzyl derivatives of oxamniquine using scanning electron microscopy

Valentin Buchter, Jeannine Hess, Gilles Gasser · Parasites & Vectors · 2018

Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents

Thiago José Matos-Rocha, Maria do Carmo Alves de Lima, Anekécia Lauro da Silva · Revista do Instituto de Medicina Tropical de São Paulo · 2017

Doxycycline hyclate: A schistosomicidal agent in vitro with immunomodulatory potential on granulomatous inflammation in vivo

Miriam Viviane Dias, Aline Pereira Castro, Camila Cabral Campos · International Immunopharmacology · 2019

Showing 6 of 14 known citations — external sources report more than can currently be individually listed.

Related research

Article metrics

Real usage data collected on this platform.

6

Page views

0

PDF downloads

0

Outbound clicks

14

Citations

Views over time

Views by country

Approximate, from request IP at view time — not citizenship or institution. Countries with fewer than 5 views are grouped as "Other".

Traffic sources

Referring site, by host.

Views and downloads exclude known bots/crawlers. Citations combines this platform's own DOI-resolved index with each external source's own reported total — see Cited by above for individually listed citing works. Last refreshed 0 seconds ago.