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In vitro antileishmanial activity of trans-stilbene and terphenyl compounds.
- Source :
-
Experimental parasitology [Exp Parasitol] 2016 Jul; Vol. 166, pp. 1-9. Date of Electronic Publication: 2016 Mar 04. - Publication Year :
- 2016
-
Abstract
- Leishmaniasis are globally widespread parasitic diseases which often leads to death if left untreated. Currently available drugs present different drawbacks, so there is an urgent need to develop new, safe and cost-effective drugs against leishmaniasis. In this study we tested a small library of trans-stilbene and terphenyl derivatives against promastigote, amastigotes and intramacrophage amastigote forms of Leishmania infantum. Two compounds of the series, the trans-stilbene 3 and the terphenyl 11, presented the best activity and safety profiles. Terphenyl 11 showed a leshmanicidal activity higher than pentostam and the ability to induce apoptosis selectively in Leishmania infantum while saving macrophages and primary epithelial cells. Our data indicate that terphenyl compounds, as well as stilbenes, are endowed with leishmanicidal activity, showing potential for further studies in the context of leishmanial therapy.<br /> (Copyright © 2016 Elsevier Inc. All rights reserved.)
- Subjects :
- Animals
Antiprotozoal Agents chemistry
Apoptosis
Cell Cycle drug effects
Cercopithecus
Epithelial Cells drug effects
Flow Cytometry
Humans
Inhibitory Concentration 50
Leishmania infantum cytology
Leishmania infantum growth & development
Macrophages drug effects
Macrophages parasitology
Microscopy, Fluorescence
Stilbenes chemistry
Structure-Activity Relationship
Terphenyl Compounds chemistry
U937 Cells
Antiprotozoal Agents pharmacology
Leishmania infantum drug effects
Stilbenes pharmacology
Terphenyl Compounds pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1090-2449
- Volume :
- 166
- Database :
- MEDLINE
- Journal :
- Experimental parasitology
- Publication Type :
- Academic Journal
- Accession number :
- 26953250
- Full Text :
- https://doi.org/10.1016/j.exppara.2016.03.007