Design, synthesis and in vitro biological evaluation of novel Oleuropein derivatives as potential anti-leishmanial agents

Leishmaniasis is a complex disease caused by multiple subspecies of Leishmania intracellular protozoan parasites. It is the second most deadly vector-transmitted disease, affecting almost 12 million people, predominantly of low socioeconomic status. Although it is considered as a neglected tropical disease, there is a global distribution and several factors have contributed to its expansion during the last years. The lack of safe and effective treatment renders imperative the development of new drugs, which will have a significant health impact along with economical ramifications. Our group has previously reported the promising anti-leishmanial activity of Oleuropein, one of the most important polyphenols of olive tree [1]. Clear epidemiological and biochemical evidence indicates that Oleuropein is endowed with leishmanicidal effects against Leishmania spp. minimising the parasite burden in infected BALB/c mice. Within this context, in the current work, 12 novel Oleuropein analogues were designed and synthesised via a convenient and facile procedure. Τhe compounds were further evaluated in vitro for their potential anti-leishmanial activity using the resazurin cell viability assay, against both developmental stages of a viscerotropic and a dermotropic Leishmania strain. The obtained data produce scientific evidence of the promising anti- leishmanial properties of analogues, emerging from the initial structure of Oleuropein.

Funding ERDF,"RESEARCH-CREATE- INNOVATE", OliveFeed (project code Τ2ΕΔΚ-03891)

Publikationsverlauf

Artikel online veröffentlicht:
16. November 2023

• References

• 1 Kyriazis I.. et al. Parasites Vectors 9: 441 2016;