Bioactive cembrane derivatives from the Indian Ocean soft coral, Sinularia kavarattiensis

Marine organisms and 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 and for in vitro anti-inflammatory activity. In the sc...

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Published in:	Marine drugs Vol. 12; no. 7; pp. 4045 - 4068
Main Authors:	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
Format:	Journal Article
Language:	English
Published:	Switzerland MDPI AG 03-07-2014 MDPI
Subjects:	Animals Anthozoa - metabolism Anti-Inflammatory Agents - isolation & purification Antiviral Agents - isolation & purification Chikungunya Chikungunya virus Chikungunya virus - drug effects Diterpenes - chemistry Diterpenes - isolation & purification Diterpenes - pharmacology Dose-Response Relationship, Drug live cell imaging Marine neuroinflammation NMR spectroscopy norcembranoid replicon cell line Sinularia kavarattiensis soft coral Structure-Activity Relationship ISW, Indian Ocean
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Summary:	Marine organisms and 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 and 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) and one new compound, named kavaranolide (7). The structures were elucidated on the basis of NMR and MS spectroscopic data. Compounds 1-3 and 5-7 were evaluated for their replicon-inhibiting potential in the CHIKV model by using a luminescence-based detection technique and live cell imaging. Compounds 1 and 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 and to possess potential anti-inflammatory properties by dose-dependently reducing the release of pro- and anti-inflammatory cytokines.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	1660-3397 1660-3397
DOI:	10.3390/md12074045