Structure-dependent cytotoxic effects of eremophilanolide sesquiterpenes

The aim of this research was to determine the cytotoxic action of sixteen structurally-related eremophilane-type sesquiterpenes, isolated from several species of Senecio, against a panel of cancer cell lines. The cytotoxic activities were evaluated by WST-1 test and the IC50 values calculated. The investigated compounds exerted dose-dependent cytotoxic actions against selected cancer cell lines and no-tumoral HS5 cell line. The comparative structure-activity relationships demonstrated the importance of C-1, C-6, and C-8 substituents in the molecule. Our results show that eremophilane-type sesquiterpenes may represent an important source of novel potential antitumor agents due to their pronounced cytotoxic actions towards malignant cells.

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Bibliographic Details
Main Authors: Agulló-Ortuño, María Teresa, Díaz, Carmen E., González-Coloma, Azucena, Reina, Matías
Other Authors: Ministerio de Economía y Competitividad (España)
Format: artículo biblioteca
Published: Sage Publications 2017
Subjects:Eremophilanolides, Cytotoxic activity, Structure-activity relationships,
Online Access:http://hdl.handle.net/10261/185151
http://dx.doi.org/10.13039/501100003329
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Summary:The aim of this research was to determine the cytotoxic action of sixteen structurally-related eremophilane-type sesquiterpenes, isolated from several species of Senecio, against a panel of cancer cell lines. The cytotoxic activities were evaluated by WST-1 test and the IC50 values calculated. The investigated compounds exerted dose-dependent cytotoxic actions against selected cancer cell lines and no-tumoral HS5 cell line. The comparative structure-activity relationships demonstrated the importance of C-1, C-6, and C-8 substituents in the molecule. Our results show that eremophilane-type sesquiterpenes may represent an important source of novel potential antitumor agents due to their pronounced cytotoxic actions towards malignant cells.