Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 1 de 1
Filter
Add more filters










Database
Language
Publication year range
1.
Biomed Pharmacother ; 111: 367-377, 2019 Mar.
Article in English | MEDLINE | ID: mdl-30594049

ABSTRACT

Trichomoniasis is a parasitic infection caused by Trichomonas vaginalis and it is considered to be the most common non-viral sexually transmitted infection in the world. Since the 1960s, nitroimidazoles such as metronidazole are the drugs of choice for the treatment of trichomoniasis, but many adverse effects and allergic reactions may result from their use. Reports of metronidazole-resistant infections also highlight the importance for the search of new anti-T. vaginalis agents. Considering this, herein we report the anti-T. vaginalis evaluation of 21 synthetic monocarbonyl analogues of curcumin, which itself has been reported to possess antiparasitic potential. From the in vitro analysis of the synthetic molecules, untreated trophozoites, and metronidazole at 100 µM, it was observed that three curcumin analogues (3a, 3e, and 5e) exhibited anti-T. vaginalis activity comparable to metronidazole (no significant statistical difference). Optimal antiparasitic concentrations were determined to be 80 µM and 90 µM for propanone derivatives 3a and 3e, respectively, and 200 µM for cyclohexanone derivative 5e. Kinetic growth curves showed that, after 24 h, the trophozoites were completely inhibited. At the tested concentrations, natural curcumin did not significantly inhibit the growth of trophozoites, therefore demonstrating that the designed synthetic molecules not only have better chemical stability, but also higher anti-T. vaginalis potential. Cytotoxicity analysis, performed on VERO cells, demonstrated low, moderate and high cytotoxic effects for analogues 3e, 5e and 3a, respectively. This study suggests that these analogues possess chemical features of interest to be further explored as alternatives for the treatment of trichomoniasis.


Subject(s)
Antiparasitic Agents/chemistry , Antiparasitic Agents/pharmacology , Curcumin/analogs & derivatives , Curcumin/pharmacology , Trichomonas vaginalis/drug effects , Animals , Cell Survival/drug effects , Cell Survival/physiology , Chlorocebus aethiops , Dose-Response Relationship, Drug , Microbial Sensitivity Tests/methods , Trichomonas vaginalis/physiology , Vero Cells
SELECTION OF CITATIONS
SEARCH DETAIL
...