4.7 Article

Cajamolides A-N: Cytotoxic and anti-inflammatory sesquiterpene lactones from Calea jamaicensis

Journal

BIOORGANIC CHEMISTRY
Volume 116, Issue -, Pages -

Publisher

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2021.105351

Keywords

Calea jamaicensis; Asteraceae; Sesquiterpene lactones; Chromenes; Cytotoxicity; Anti-inflammatory; MTT; ICAM-1

Funding

  1. European Union (European Social Fund-ESF) [MIS-5000432]
  2. State Scholarships Foundation (IKY)

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In the study of Calea jamaicensis, a plant endemic to Panama, seventeen sesquiterpene lactones and nine chromene derivatives were isolated, with fourteen sesquiterpene lactones and three chromanes described for the first time. These compounds exhibited strong cytotoxic effects on cancer cell lines and potent anti-inflammatory potential in ICAM-1 assay. This research highlights the therapeutic potential of these bioactive compounds in managing inflammatory diseases.
In the search for bioactive compounds from natural sources against cancer and inflammation, Calea jamaicensis (L.) L., a plant endemic to Panama, was investigated. Using multiple chromatographic steps, seventeen sesquiterpene lactones together with nine chromene derivatives were isolated from the non-polar extract of the plant. Among them, fourteen sesquiterpene lactones and three chromanes are described herein for the first time. Structure elucidation was achieved by extensive spectroscopic analysis and comparison with reported data. The isolated sesquiterpene lactones were tested against HeLa, SK-MEL-28 and HePG2 cancerous cell lines for their cytotoxic effects, as well as in the ICAM-1 assay for their anti-inflammatory potential. This study revealed strong cytotoxic agents on the one hand and strong inhibitors on the other. The compounds inhibited the TNF-alpha induced ICAM-1 expression on the endothelial HMEC-1 cells in a dose-dependent manner and with no toxicity observed on this non-cancerous cell line. In addition to the well-known cytotoxic activities of sesquiterpene lactones, further exploration may offer a novel therapeutic approach to cope with inflammatory diseases and the genus Calea may serve as a biobank for the isolation of potential phytopharmaceuticals, which could be utilized as leads in drug discovery and therapy.

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