Activity-guided isolation of antileishmanial compounds from Piper hispidum

Candy Ruiz, Mohamed Haddad, Joaquina Alban, Genevive Bourdy, Ricardo Reategui, Denis Castillo, Michel Sauvain, Eric Deharo, Yannick Estevez, Jorge Arevalo, Rosario Rojas

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16 Scopus citations

Abstract

The bioassay-guided purification of the ethanolic extract from the leaves of Piper hispidum led to the isolation of one new amide, N-2-(3′,4′, 5′-trimethoxyphenyl)ethyl-2-hydroxybenzamide (1) as well as two known chalcones 2′-hydroxy-3′,4′,6′-trimethoxychalcone (2); 2′,4′-dihydroxy-6′-methoxychalcone (cardamonin, 3) and one known flavanone, 5,7-dihydroxyflavanone (Pinocembrin, 4). Their structures were elucidated on the basis of spectroscopic data, including homo- and heteronuclear correlation NMR experiments (COSY, HSQC and HMBC) and comparison with data reported in the literature. The isolated compounds were tested against Leishmania amazonensis axenic amastigotes. The results showed that the known chalcone 2 exhibited the most potent antileishmanial activity with an IC 50 of 0.8 μM (amphotericin B: IC50 = 0.2 μM) but was shown to exhibit mild cytotoxicity.
Original languageAmerican English
Pages (from-to)363-366
Number of pages4
JournalPhytochemistry Letters
Volume4
Issue number3
DOIs
StatePublished - 1 Sep 2011

Keywords

  • Amide
  • Chalcone
  • Flavanone
  • Leishmaniasis
  • Piper

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    Ruiz, C., Haddad, M., Alban, J., Bourdy, G., Reategui, R., Castillo, D., Sauvain, M., Deharo, E., Estevez, Y., Arevalo, J., & Rojas, R. (2011). Activity-guided isolation of antileishmanial compounds from Piper hispidum. Phytochemistry Letters, 4(3), 363-366. https://doi.org/10.1016/j.phytol.2011.08.001