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Abstract

Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalis  †

by
Alexandra Ibáñez-Escribano
1,*,
Jose Antonio Escario
1,
Faustino Mollinedo
2 and
Alicia Gómez-Barrio
1
1
Departamento de Parasitología, Facultad de Farmacia, Universidad Complutense de Madrid, Pza. Ramón y Cajal s/n, 28040 Madrid, Spain
2
Laboratorio de Muerte Celular y Terapia del Cáncer, Centro de Investigaciones Biológicas (CIB-CSIC), c/ Ramiro de Maeztu 9, 28040 Madrid, Spain
*
Author to whom correspondence should be addressed.
Presented at the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain, 8 September 2017.
Proceedings 2017, 1(6), 653; https://doi.org/10.3390/proceedings1060653
Published: 19 October 2017
Edelfosine (ET-18-OCH3) is an alkylphospholipid with an analogous structure to miltefosine. Both molecules are active against kinetoplastids (Leishmania spp., Trypanosoma cruzi and Trypanosoma brucei). However, its trichomonacidal effect has never been studied. For this purpose, edelfosine has been evaluated in vitro for its ability to inhibit proliferation of the common sexually transmitted parasite Trichomonas vaginalis following a standardized fluorimetric procedure. The results show an IC50 = 19.8 µM against metronidazole-sensitive isolates and a remarkable IC50 = 7.6 µM against the metronidazole-resistant IR78. This enhanced effect against the resistant isolate suggests another possible mode of action in comparison with the reference drug. Moreover, T. vaginalis exhibits a different growth rate due to the metabolic modifications according to its resistant trait. These results are in consonance with the trichomonacidal effect observed by other authors using the analog miltefosine against resistant samples, provoking membrane alterations and apoptosis. It is estimated that 2.5–10% of clinical cases of trichomonosis are produced by resistant isolates. The absence of pharmacological alternatives to the unique two 5-nitroimidazole drugs approved by the FDA makes necessary the incorporation of novel trichomonacidal drugs with a different mode of action. Taken together, our results, in consonance with previous reports, suggest the promising use of these alkylphospholipids as an alternative trichomonacidal drug against resistant cases.

Author Contributions

F.M. provided reagents and contributed to the implementation of the research, and to the analysis of the results. J.A.E. and A.G.-B. participated in the evaluation of the biological results and finally A.I.-E. contributed in the development of the parasitic assays, interpretation of data and drafting the manuscript. All the authors participated in the final version. All authors have read and agreed to the published version of the manuscript.

Acknowledgments

This work was partially supported by SAF2015-66690-R and SAF2014-59716-R grants from the Spanish Ministerio de Economia y Competitividad.

Conflicts of Interest

The authors declare no conflict of interest.
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations.

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MDPI and ACS Style

Ibáñez-Escribano, A.; Escario, J.A.; Mollinedo, F.; Gómez-Barrio, A. Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalis . Proceedings 2017, 1, 653. https://doi.org/10.3390/proceedings1060653

AMA Style

Ibáñez-Escribano A, Escario JA, Mollinedo F, Gómez-Barrio A. Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalis . Proceedings. 2017; 1(6):653. https://doi.org/10.3390/proceedings1060653

Chicago/Turabian Style

Ibáñez-Escribano, Alexandra, Jose Antonio Escario, Faustino Mollinedo, and Alicia Gómez-Barrio. 2017. "Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalis " Proceedings 1, no. 6: 653. https://doi.org/10.3390/proceedings1060653

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