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.
journal_name
Exp Parasitoljournal_title
Experimental parasitologyauthors
Castelli G,Bruno F,Vitale F,Roberti M,Colomba C,Giacomini E,Guidotti L,Cascio A,Tolomeo Mdoi
10.1016/j.exppara.2016.03.007subject
Has Abstractpub_date
2016-07-01 00:00:00pages
1-9eissn
0014-4894issn
1090-2449pii
S0014-4894(16)30033-9journal_volume
166pub_type
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