Antiparasitic activity of furanyl N-acylhydrazone derivatives against Trichomonas vaginalis: in vitro and in silico analyses.
Antiparasitic
Lipid peroxidation
Molecular docking
Trichomonacidal
Trichomoniasis
Journal
Parasites & vectors
ISSN: 1756-3305
Titre abrégé: Parasit Vectors
Pays: England
ID NLM: 101462774
Informations de publication
Date de publication:
11 Feb 2020
11 Feb 2020
Historique:
received:
19
08
2019
accepted:
01
02
2020
entrez:
13
2
2020
pubmed:
13
2
2020
medline:
6
6
2020
Statut:
epublish
Résumé
Trichomonas vaginalis is the causative agent of trichomoniasis, which is one of the most common sexually transmitted diseases worldwide. Trichomoniasis has a high incidence and prevalence and is associated with serious complications such as HIV transmission and acquisition, pelvic inflammatory disease and preterm birth. Although trichomoniasis is treated with oral metronidazole (MTZ), the number of strains resistant to this drug is increasing (2.5-9.6%), leading to treatment failure. Therefore, there is an urgent need to find alternative drugs to combat this disease. Herein, we report the in vitro and in silico analysis of 12 furanyl N-acylhydrazone derivatives (PFUR 4, a-k) against Trichomonas vaginalis. Trichomonas vaginalis ATCC 30236 isolate was treated with seven concentrations of these compounds to determine the minimum inhibitory concentration (MIC) and 50% inhibitory concentration (IC The compounds PFUR 4a and 4b, at 6.25 µM, induced complete parasite death after 24 h of exposure with IC Our results showed that PFUR 4a and 4b are promising molecules that can be used for the development of new trichomonacidal agents for T. vaginalis.
Sections du résumé
BACKGROUND
BACKGROUND
Trichomonas vaginalis is the causative agent of trichomoniasis, which is one of the most common sexually transmitted diseases worldwide. Trichomoniasis has a high incidence and prevalence and is associated with serious complications such as HIV transmission and acquisition, pelvic inflammatory disease and preterm birth. Although trichomoniasis is treated with oral metronidazole (MTZ), the number of strains resistant to this drug is increasing (2.5-9.6%), leading to treatment failure. Therefore, there is an urgent need to find alternative drugs to combat this disease.
METHODS
METHODS
Herein, we report the in vitro and in silico analysis of 12 furanyl N-acylhydrazone derivatives (PFUR 4, a-k) against Trichomonas vaginalis. Trichomonas vaginalis ATCC 30236 isolate was treated with seven concentrations of these compounds to determine the minimum inhibitory concentration (MIC) and 50% inhibitory concentration (IC
RESULTS
RESULTS
The compounds PFUR 4a and 4b, at 6.25 µM, induced complete parasite death after 24 h of exposure with IC
CONCLUSIONS
CONCLUSIONS
Our results showed that PFUR 4a and 4b are promising molecules that can be used for the development of new trichomonacidal agents for T. vaginalis.
Identifiants
pubmed: 32046788
doi: 10.1186/s13071-020-3923-8
pii: 10.1186/s13071-020-3923-8
pmc: PMC7014680
doi:
Substances chimiques
Antiprotozoal Agents
0
Hydrazones
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
59Subventions
Organisme : Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
ID : Finance Code 001 - Masters Scholarship - Grant number 1693097
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