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.

Castelli, G., Bruno, F., Vitale, F., Roberti, M., Colomba, C., Giacomini, E., et al. (2016). In vitro antileishmanial activity of trans-stilbene and terphenyl compounds. EXPERIMENTAL PARASITOLOGY, 166, 1-9 [10.1016/j.exppara.2016.03.007].

In vitro antileishmanial activity of trans-stilbene and terphenyl compounds

VITALE, Fabrizio;COLOMBA, Claudia;CASCIO, ANTONIO;
2016-01-01

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.
2016
Castelli, G., Bruno, F., Vitale, F., Roberti, M., Colomba, C., Giacomini, E., et al. (2016). In vitro antileishmanial activity of trans-stilbene and terphenyl compounds. EXPERIMENTAL PARASITOLOGY, 166, 1-9 [10.1016/j.exppara.2016.03.007].
File in questo prodotto:
File Dimensione Formato  
In vitro antileishmanial activity of trans-stilbene and terphenyl.pdf

accesso aperto

Dimensione 1.83 MB
Formato Adobe PDF
1.83 MB Adobe PDF Visualizza/Apri

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/243757
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 13
  • ???jsp.display-item.citation.isi??? 12
social impact