Antiparasitary Potential Of Natural And Semi-Synthetic Labdane Diterpenes

Aline Nazaré Silva Parra; Ana Carolina Ferreira Soares Rocha; Julian Carlos da Silva Pavan; Analuz da Silva Machado; Vinícius José Miranda Rodrigues; Daiane Albino dos Santos; Lizandra Guidi Magalhães; Sérgio de Albuquerque; Vladimir Constantino Gomes Heleno

doi:10.20944/preprints202407.1954.v1

Preprint Article Version 1 This version is not peer-reviewed

Version 1 : Received: 24 July 2024 / Approved: 24 July 2024 / Online: 24 July 2024 (17:45:24 CEST)

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.

Leishmaniasis; Chagas disease; Copalic acid; Structural Modification; Trypanocidal and Leishmanicidal activities

Chemistry and Materials Science, Applied Chemistry

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Antiparasitary Potential Of Natural And Semi-Synthetic Labdane Diterpenes

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