TY - JOUR
T1 - In vitro antileishmanial activity of trans-stilbene and terphenyl compounds
AU - Colomba, Claudia
AU - Cascio, Antonio
AU - Giacomini, Elisa
AU - Vitale, Fabrizio
AU - Bruno, Federica
AU - Castelli, Germano
AU - Guidotti, Laura
AU - Roberti, Marinella
AU - Vitale, Fabrizio
PY - 2016
Y1 - 2016
N2 - 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.
AB - 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.
KW - Fluorescence; Stilbenes; Structure-Activity Relationship; Terphenyl Compounds; U937 Cells; Parasitology; Immunology
KW - Leishmaniasis; Programmed cell death; Stilbenes; Terphenyls; Animals; Antiprotozoal Agents; Apoptosis; Cell Cycle; Cercopithecus; Epithelial Cells; Flow Cytometry; Humans; Inhibitory Concentration 50; Leishmania infantum; Macrophages; Microscopy
KW - Fluorescence; Stilbenes; Structure-Activity Relationship; Terphenyl Compounds; U937 Cells; Parasitology; Immunology
KW - Leishmaniasis; Programmed cell death; Stilbenes; Terphenyls; Animals; Antiprotozoal Agents; Apoptosis; Cell Cycle; Cercopithecus; Epithelial Cells; Flow Cytometry; Humans; Inhibitory Concentration 50; Leishmania infantum; Macrophages; Microscopy
UR - http://hdl.handle.net/10447/243757
M3 - Article
VL - 166
SP - 1
EP - 9
JO - Experimental Parasitology
JF - Experimental Parasitology
SN - 0014-4894
ER -