Antiparasitary Potential Of Natural And Semi-Synthetic Labdane Diterpenes

  1. Aline Nazaré Silva Parra
  2. Ana Carolina Ferreira Soares Rocha
  3. Julian Carlos da Silva Pavan
  4. Analuz da Silva Machado
  5. Vinícius José Miranda Rodrigues
  6. Daiane Albino dos Santos
  7. Lizandra Guidi Magalhães
  8. Sérgio de Albuquerque
  9. Vladimir Constantino Gomes Heleno
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Abstract

In this paper is described the obtention of fourteen derivatives from four natural labdane diterpenes isolated from Copaifera oleoresin, named ent-copalic acid (1), ¬ent-3beta-acetoxy copalic acid (2), ent-3beta-hydroxy copalic acid (3) and ent-agathic acid (4). All eighteen compounds were assayed against promastigote form of Leishmania amazonensis and trypomastigote forms of Trypanosoma cruzi, revealing two promising compounds related to leishmanicidal activity (IC50 = 5.94 micromolar and 5.31 micromolar) and three promising compounds with trypanocidal activity, two of them (IC50 = 13.31micromolar and IC50 = 15.05micromolar) displaying similar activity as the reference drug (IC50 = 13.12micromolar) and one of them even more potent with IC50 = 0.425micromolar.

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  1. Version published to 10.20944/preprints202407.1954.v1