Jump to main content
Jump to site search
Access to RSC content Close the message box

Continue to access RSC content when you are not at your institution. Follow our step-by-step guide.


Issue 21, 2016
Previous Article Next Article

In vitro antileishmanial activity of aza-scorpiand macrocycles. Inhibition of the antioxidant enzyme iron superoxide dismutase

Author affiliations

Abstract

The in vitro leishmanicidal activity of a series of nine aza-scorpiand-like macrocycles, recently synthesized, was tested on Leishmania infantum, Leishmania braziliensis and Leishmania donovani parasites, using promastigotes and intracellular amastigotes forms. The cytotoxicity of the tested compounds on J774.2 macrophage cells was also measured. Four of the tested compounds (1, 2, 8 and 9) showed selectivity indexes higher than those of the reference drug Glucantime for the three Leishmania species. Moreover, the data on infection rates and on amastigotes showed that compounds 1, 2, 8 and 9 are the most active against the three Leishmania species. The changes in the excretion product profile of parasites treated with the four compounds (1, 2, 8 and 9) were also consistent with substantial cytoplasmic alterations. On the other hand, the most active compounds were potent inhibitors of Fe-SOD in the three parasite species considered, whereas their impact on human CuZn-SOD was low. The high activity, low toxicity, stability, low cost of the starting materials and straightforward synthesis make these compounds appropriate molecules for the development of affordable anti-leishmanicidal agents.

Graphical abstract: In vitro antileishmanial activity of aza-scorpiand macrocycles. Inhibition of the antioxidant enzyme iron superoxide dismutase

Back to tab navigation

Supplementary files

Article information


Submitted
13 Oct 2015
Accepted
28 Jan 2016
First published
04 Feb 2016

RSC Adv., 2016,6, 17446-17455
Article type
Paper
Author version available

In vitro antileishmanial activity of aza-scorpiand macrocycles. Inhibition of the antioxidant enzyme iron superoxide dismutase

C. Marín, M. Inclán, I. Ramírez-Macías, M. T. Albelda, R. Cañas, M. xmlns="http://www.rsc.org/schema/rscart38"> <. P. Clares, J. González-García, M. J. Rosales, K. Urbanova, E. García-España and M. Sánchez-Moreno, RSC Adv., 2016, 6, 17446
DOI: 10.1039/C5RA21262F

Social activity

Search articles by author

Spotlight

Advertisements