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Open AccessArticle

Bioactive Cembrane Derivatives from the Indian Ocean Soft Coral, Sinularia kavarattiensis

1
Centre for Drug Research, Division of Pharmaceutical Biosciences, Faculty of Pharmacy, P.O. Box 56, University of Helsinki, Helsinki FI-00014, Finland
2
Department of Pharmacy, University of Naples Federico II (USNF), Naples I-80131, Italy
3
CSIR-National Institute of Oceanography, Dona Paula, Goa 403004, India
4
EuroEspes Biotechnology, Department of Cellular Immunology, Bergondo 15165, A Coruña, Spain
*
Author to whom correspondence should be addressed.
Mar. Drugs 2014, 12(7), 4045-4068; https://doi.org/10.3390/md12074045
Received: 1 April 2014 / Revised: 5 June 2014 / Accepted: 17 June 2014 / Published: 3 July 2014
(This article belongs to the Collection Bioactive Compounds from Marine Invertebrates)
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 (16) and one new compound, named kavaranolide (7). The structures were elucidated on the basis of NMR and MS spectroscopic data. Compounds 13 and 57 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. View Full-Text
Keywords: Sinularia kavarattiensis; soft coral; norcembranoid; NMR spectroscopy; Chikungunya; replicon cell line; live cell imaging; neuroinflammation Sinularia kavarattiensis; soft coral; norcembranoid; NMR spectroscopy; Chikungunya; replicon cell line; live cell imaging; neuroinflammation
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Lillsunde, K.-E.; Festa, C.; Adel, H.; De Marino, S.; Lombardi, V.; Tilvi, S.; Nawrot, D.A.; Zampella, A.; D'Souza, L.; D'Auria, M.V.; Tammela, P. Bioactive Cembrane Derivatives from the Indian Ocean Soft Coral, Sinularia kavarattiensis . Mar. Drugs 2014, 12, 4045-4068.

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