Evaluation of Oxasqualenoids from the Red Alga Laurencia viridis against Acanthamoeba

• Published in: Marine drugs Vol. 17; no. 7; p. 420
• Main Authors: Lorenzo-Morales, Jacob, Díaz-Marrero, Ana R, Cen-Pacheco, Francisco, Sifaoui, Ines, Reyes-Batlle, María, Souto, María L, Hernández Daranas, Antonio, Piñero, José E, Fernández, José J
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 19.07.2019; MDPI
• Subjects: Acanthamoeba; Acanthamoeba castellanii - drug effects; Amebicides - isolation & purification; Amebicides - pharmacology; Animals; Apoptosis; Bacterial infections; Cell Line; Congeners; Cornea; Cysts; Cytotoxicity; dehydrothyrsiferol; Dormancy; Encephalitis; Furans - isolation & purification; Furans - pharmacology; Infections; Inhibitory Concentration 50; Keratitis; Laurencia; Laurencia - chemistry; Macrophages; marine natural product; Metabolites; Mice; oxasqualenoid; Parasites; Pathogens; Pathology; Plant Extracts - isolation & purification; Plant Extracts - pharmacology; Protozoa; Pyrans - isolation & purification; Pyrans - pharmacology; Squalene - analogs & derivatives; Squalene - isolation & purification; Squalene - pharmacology; Toxicity Tests; triterpene; Trophozoites - drug effects; dehydrothyrsiferol; triterpene; oxasqualenoid; marine natural product; Acanthamoeba; Laurencia
• ISSN: 1660-3397; 1660-3397
• DOI: 10.3390/md17070420

genus is a widely distributed and opportunistic parasite with increasing importance worldwide as an emerging pathogen in the past decades. This protozoan has an active trophozoite stage, a cyst stage, and is dormant and very resistant. It can cause keratitis, an ocular sight-threatening disease, and granulomatous amoebic encephalitis, a chronic, very fatal brain pathology. In this study, the amoebicidal activity of sixteen oxasqualenoid metabolites and semisynthetic derivatives were tested against Neff. The results obtained point out that iubol ( ) and dehydrothyrsiferol ( ) possess potent activities, with IC values of 5.30 and 12.83 µM, respectively. The hydroxylated congeners thyrsiferol ( ) and 22-hydroxydehydrothyrsiferol ( ), active in the same value range at IC 13.97 and 17.00 µM, are not toxic against murine macrophages; thus, they are solid candidates for the development of new amoebicidal therapies.