Therapeutic potential of hydantoin and thiohydantoin compounds against Schistosoma mansoni: An integrated in vitro, DNA, ultrastructural, and ADMET in silico approach.
Mol Biochem Parasitol
; 260: 111646, 2024 Jun 29.
Article
in En
| MEDLINE
| ID: mdl-38950658
ABSTRACT
The study aimed to conduct in vitro biological assessments of hydantoin and thiohydantoin compounds against mature Schistosoma mansoni worms, evaluate their cytotoxic effects and predict their pharmacokinetic parameters using computational methods. The compounds showed low in vitro cytotoxicity and were not considered hemolytic. Antiparasitic activity against adult S. mansoni worms was tested with all compounds at concentrations ranging from 200 to 6.25⯵M. Compounds SC01, SC02, and SC03 exhibited low activity. Compounds SC04, SC05, SC06 and SC07 caused 100â¯% mortality within 24â¯h of incubation at a concentration of 100 and 200⯵M. Thiohydantoin SC04 exhibited the highest activity, resulting in 100â¯% mortality after 24â¯h of incubation at a concentration of 50⯵M and IC50 of 28⯵M. In the ultrastructural analysis (SEM), the compound SC04 (200⯵M) induced integumentary changes, formation of integumentary blisters, and destruction of tubercles and spicules. Therefore, the SC04 compound shows promise as an antiparasitic against S. mansoni.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Language:
En
Journal:
Mol Biochem Parasitol
Year:
2024
Document type:
Article