Autor(es)Gupta Deepak Kumar, Kaur Parveen, Leong See Ting, Tan Lik Tong, Prinsep Michèle R, Chu Justin Jang Hann

ResumoTropical filamentous marine cyanobacteria have emerged as a viable source of novel bioactive natural products for drug discovery - development. In the present study, aplysiatoxin (1), debromoaplysiatoxin (2) - anhydrodebromoaplysiatoxin (3), as well as two new analogues, 3-methoxyaplysiatoxin (4) - 3-methoxydebromoaplysiatoxin (5), are reported for the first time from the marine cyanobacterium Trichodesmium erythraeum. The identification of the bloom-forming cyanobacterial strain was confirmed based on phylogenetic analysis of its 16S rRNA sequences. Structural determination of the new analogues was achieved by extensive NMR spectroscopic analysis - comparison with NMR spectral data of known compounds. In addition, the antiviral activities of these marine toxins were assessed using Chikungunya virus (CHIKV)-infected cells. Post-treatment experiments using the debrominated analogues, namely compounds 2, 3 - 5, displayed dose-dependent inhibition of CHIKV when tested at concentrations ranging from 0.1 µM to 10.0 µM. Furthermore, debromoaplysiatoxin (2) - 3-methoxydebromoaplysiatoxin (5) exhibited significant anti-CHIKV activities with EC50 values of 1.3 ?M - 2.7 ?M, respectively, - selectivity indices of 10.9 - 9.2, respectively.

Palavras-ChaveMarine cyanobacterium; Trichodesmium erythraeum; Aplysiatoxin; Antiviral; Chikungunya virus

ImprentaMarine Drugs, v. 12, n. 1, p. 115-127, 2014

DescritoresChikungunya virus - Biosynthesis ; Chikungunya virus - Cell ; Chikungunya virus - RNA ; Chikungunya Virus - Virus

Data de Publicação:2014