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Antiamoebic effects of sesquiterpene lactones isolated from the zoanthid Palythoa aff. clavata

2021; Elsevier BV; Volume: 108; Linguagem: Inglês

10.1016/j.bioorg.2021.104682

1090-2120

Rubén L. Rodríguez-Expósito, Nathália Nocchi, María Reyes‐Batlle, Inés Sifaoui, Blanca Suárez‐Gómez, Ana R. Dı́az-Marrero, Marı́a L. Souto, José E. Piñero, José J. Fernández, Jacob Lorenzo‐Morales,

Plant Toxicity and Pharmacological Properties

Opportunistic parasitic protozoa of genus Acanthamoeba are responsible to cause severe infections in humans such as Acanthamoeba Keratitis or Amoebic Granulomatous Encephalitis. Current treatments are usually toxic and inefficient and there is a need to access new therapeutic agents. The antiamoebic effects of nephthediol (1) and fourteen germacranolide and eudesmanolide sesquiterpene lactones (2-5, 7-12) isolated from the indigenous zoanthid Palythoa aff. clavata collected at the coast of Lanzarote, Canary Islands were studied against Acanthamoeba castellanii Neff, and the clinical strains A. polyphaga and A. griffini. 4-epi-arbusculin A (11) presented the lowest IC50 value (26,47 ± 1,69 µM) against A. castellanii Neff and low cytotoxicity against murine macrophages, followed by isobadgerin (2), which also showed to be active against A. castellanii Neff cysts. The studies on the mode of action of compounds 2 and 11 revealed these sesquiterpene lactones induce mechanisms of PDC on A. castellanii Neff.