Abstract
Acanthamoeba 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 Acanthamoeba keratitis, an ocular sight-threatening disease, and granulomatous amoebic encephalitis, a chronic, very fatal brain pathology. In this study, the amoebicidal activity of sixteen Laurencia oxasqualenoid metabolites and semisynthetic derivatives were tested against Acanthamoeba castellanii Neff. The results obtained point out that iubol (3) and dehydrothyrsiferol (1) possess potent activities, with IC50 values of 5.30 and 12.83 µM, respectively. The hydroxylated congeners thyrsiferol (2) and 22-hydroxydehydrothyrsiferol (4), active in the same value range at IC50 13.97 and 17.00 µM, are not toxic against murine macrophages; thus, they are solid candidates for the development of new amoebicidal therapies.
Highlights
Acanthamoeba spp. [1] are opportunistic free-living amoebae (FLA) that are ubiquitous in nature and widely distributed in different environments such as seawater, soil, lakes, contact lenses, air-conditioning units, as well as hospitals [2,3]
Acanthamoeba keratitis (AK) and granulomatous amoebic encephalitis (GAE) are the main infections caused by Acanthamoeba spp
Drugs 2019, 17, 420 and secrete collagenolytic factors, dissolving the stromal matrix, which results in an inflammatory response that leads to corneal cell death and keratitis [8,9]
Summary
Acanthamoeba spp. (family Acanthamoebidae, order Centramoebidae) [1] are opportunistic free-living amoebae (FLA) that are ubiquitous in nature and widely distributed in different environments such as seawater, soil, lakes, contact lenses, air-conditioning units, as well as hospitals [2,3]. Acanthamoeba keratitis (AK) and granulomatous amoebic encephalitis (GAE) are the main infections caused by Acanthamoeba spp. Mar. Drugs 2019, 17, 420 and secrete collagenolytic factors, dissolving the stromal matrix, which results in an inflammatory response that leads to corneal cell death and keratitis [8,9]. In the case of suspected infection or coinfection, antibiotics like neomycin or chloramphenicol should be added to the regimen, to prevent bacterial infection and to eliminate the food source for the parasite [2]. Mar. Drugs 2019, 17, 420 neomycin or chloramphenicol should be added to the regimen, to prevent bacterial infection and to eliminate the food source for the parasite [2]. Semisynthetic substances (12–16) obtained from the main metabolite dehydrothyrsiferol (1)
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