Effects of SQ109 on Trichomonas vaginalis.
Chemotherapy
Hydrogenosome
SQ109
Trichomoniasis
Journal
Experimental parasitology
ISSN: 1090-2449
Titre abrégé: Exp Parasitol
Pays: United States
ID NLM: 0370713
Informations de publication
Date de publication:
Jul 2023
Jul 2023
Historique:
received:
09
02
2023
revised:
23
04
2023
accepted:
14
05
2023
medline:
6
6
2023
pubmed:
18
5
2023
entrez:
17
5
2023
Statut:
ppublish
Résumé
Trichomonas vaginalis is a protozoan that causes human trichomoniasis, a sexually transmitted infection (STI) that affects approximately 278 million people worldwide. The current treatment for human trichomoniasis is based on 1-(2-hydroxyethyl)-2-methyl-5-nitroimidazole, known as Metronidazole (MTZ). Although effective in eliminating parasitic infection, MTZ is related to serious adverse effects and is not recommended during pregnancy. In addition, some strains are resistant to 5'-nitroimidazoles, prompting the development of alternative drugs for trichomoniasis. Here we show that SQ109 [N-adamantan-2-yl-N'-((E)-3,7-dimethyl-octa- 2,6-dienyl)-ethane-1,2-diamine], a drug under development (antitubercular drug candidate that completed Phase IIb/III) for the treatment of tuberculosis, and previously tested in Trypanosoma cruzi and Leishmania. SQ109 inhibited T.vaginalis growth with an IC50 of 3.15 μM. We used scanning and transmission electron microscopy to visualize the ultrastructural alterations induced by SQ109. The microscopy analysis showed morphological changes on the protozoan surface, where the cells became rounded with increasing surface projections. In addition, the hydrogenosomes increased their size and area occupied in the cell. Furthermore, the volume and a significant association of glycogen particles with the organelle were seen to be altered. A bioinformatics search was done about the compound to find its possible targets and mechanisms of action. Our observations identify SQ109 as a promising compound against T. vaginalis in vitro, suggesting its potential utility as an alternative chemotherapy for trichomoniasis.
Identifiants
pubmed: 37196704
pii: S0014-4894(23)00090-5
doi: 10.1016/j.exppara.2023.108549
pii:
doi:
Substances chimiques
Antiprotozoal Agents
0
Metronidazole
140QMO216E
N-geranyl-N'-(2-adamantyl)ethane-1,2-diamine
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
108549Informations de copyright
Copyright © 2023 Elsevier Inc. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest On behalf of all authors, the corresponding author states that there is no conflict of interest.