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

Marine Drugs

Katja-Emilia Lillsunde³  Carmen Festa⁴  Harshada Adel¹  Simona De Marino⁴  Valter Lombardi²  Supriya Tilvi¹  Dorota A. Nawrot³  Angela Zampella⁴  Lisette D’Souza¹  Maria Valeria D𠆚uria⁴ 

[1] CSIR-National Institute of Oceanography, Dona Paula, Goa 403004, India; E-Mails:;EuroEspes Biotechnology, Department of Cellular Immunology, Bergondo 15165, A Coruña, Spain; E-Mail:;Centre for Drug Research, Division of Pharmaceutical Biosciences, Faculty of Pharmacy, P.O. Box 56, University of Helsinki, Helsinki FI-00014, Finland; E-Mails:;Department of Pharmacy, University of Naples Federico II (USNF), Naples I-80131, Italy; E-Mails:

关键词: Sinularia kavarattiensis;    soft coral;    norcembranoid;    NMR spectroscopy;    Chikungunya;    replicon cell line;    live cell imaging;    neuroinflammation;   

DOI  :  10.3390/md12074045

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.