Evaluation of Oxasqualenoids from the Red Alga Laurencia viridis against Acanthamoeba

被引:28
作者
Lorenzo-Morales, Jacob [1 ]
Diaz-Marrero, Ana R. [2 ]
Cen-Pacheco, Francisco [2 ,3 ]
Sifaoui, Ines [1 ]
Reyes-Batlle, Maria [1 ]
Souto, Maria L. [2 ,4 ]
Hernandez Daranas, Antonio [2 ,5 ]
Pinero, Jose E. [1 ]
Fernandez, Jose J. [2 ,4 ]
机构
[1] Univ La Laguna, Inst Univ Enfermedades Trop & Salud Publ Islas Ca, Avda Astrofis F Sanchez S-N, E-38206 Tenerife, Spain
[2] Univ La Laguna, Ctr Invest Biomed Canarias CIBICAN, IUBO AG, Avda Astrofis F Sanchez 2, E-38206 Tenerife, Spain
[3] Univ Veracruzana, Fac Bioanal, Campus Veracruz, Xalapa 91700, Veracruz, Mexico
[4] Univ La Laguna, Dept Quim Organ, Avda Astrofis F Sanchez 2, E-38206 Tenerife, Spain
[5] CSIC, IPNA, Ave Astrofis Francisco Sanchez 2, E-38206 Tenerife, Spain
来源
MARINE DRUGS | 2019年 / 17卷 / 07期
关键词
oxasqualenoid; marine natural product; Acanthamoeba; triterpene; Laurencia; dehydrothyrsiferol; FREE-LIVING AMEBAS; NATURAL-PRODUCTS; AGENTS;
D O I
10.3390/md17070420
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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 mu M, respectively. The hydroxylated congeners thyrsiferol (2) and 22-hydroxydehydrothyrsiferol (4), active in the same value range at IC50 13.97 and 17.00 mu M, are not toxic against murine macrophages; thus, they are solid candidates for the development of new amoebicidal therapies.
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页数:15
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