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Abstract Title:

Leishmanicidal Effects of Piperlongumine (Piplartine) and Its Putative Metabolites.

Abstract Source:

Planta Med. 2018 May 15. Epub 2018 May 15. PMID: 29763945

Abstract Author(s):

Fernanda de Lima Moreira, Thalita Bachelli Riul, Marcela de Lima Moreira, Alan Cesar Pilon, Marcelo Dias-Baruffi, Márcio S S Araújo, Norberto Peporine Lopes, Anderson R M de Oliveira

Article Affiliation:

Fernanda de Lima Moreira

Abstract:

Piperlongumine is an amide alkaloid found in Piperaceae species that shows a broad spectrum of biological properties, including antitumor and antiparasitic activities. Herein, the leishmanicidal effect of piperlongumine and its derivatives produced by a biomimetic model using metalloporphyrins was investigated. The results showed that ICvalues of piperlongumine in promastigote forms ofandwere 7.9 and 3.3 µM, respectively. The ICvalue of piperlongumine in the intracellular amastigote form ofwas 0.4 µM, with a selectivity index of 25. The piperlongumine biomimetic derivatives, Ma and Mb, also showed leishmanicidal effects. We also carried out anmetabolic degradation study showing that Ma is the most stable piperlongumine derivative in rat liver microsome incubations. The results presented here indicate that piperlongumine is a potential leishmanicidal candidate and support the biomimetic approach for development of new antileishmanial derivatives.

Study Type : In Vitro Study
Additional Links
Pharmacological Actions : Leishmanicidal : CK(38) : AC(24)

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