Bioactive cembrane derivatives from the Indian Ocean soft coral, Sinularia kavarattiensis
Autor(es): Lillsunde Katja-Emilia, Festa Carmen, Adel Harshada, De Marino Simona, Lombardi Valter, Tilvi Supriya, Nawrot Dorota A, Zampella Angela, D'Souza Lisette, D'Auria Maria Valeria, Tammela Päivi
Resumo: Marine organisms - their metabolites represent a unique source of potential pharmaceutical substances. In this study, we examined marine-derived substances for their bioactive properties in a cell-based Chikungunya virus (CHIKV) replicon model - for in vitro anti-inflammatory activity. In the screening of a marine sample library, crude extracts from the Indian soft coral, Sinularia kavarattiensis, showed promising activity against the CHIKV replicon. Bioassay-guided chemical fractionation of S. kavarattiensis resulted in the isolation of six known norcembranoids (1-6) - one new compound, named kavaranolide (7). The structures were elucidated on the basis of NMR - MS spectroscopic data. Compounds 1-3 - 5-7 were evaluated for their replicon-inhibiting potential in the CHIKV model by using a luminescence-based detection technique - live cell imaging. Compounds 1 - 2 showed moderate inhibition of the CHIKV replicon, but imaging studies also revealed cytotoxic properties. Moreover, the effects of the isolated compounds on primary microglial cells, an experimental model for neuroinflammation, were evaluated. Compound 2 was shown to modulate the immune response in microglial cells - to possess potential anti-inflammatory properties by dose-dependently reducing the release of pro- - anti-inflammatory cytokines.
Imprenta: Marine Drugs, v. 12, n. 7, p. 4045-4068, 2014
Identificador do objeto digital: 10.3390/md12074045
Descritores: Chikungunya virus - Biosynthesis ; Chikungunya virus - Cell ; Chikungunya virus - Immune response ; Chikungunya virus - Cytokines ; Chikungunya virus - Immune response ; Chikungunya Virus - Virus ; Chikungunya virus - Immunology
Data de publicação: 2014