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Cassane-type diterpenes from Caesalpinia minax induce apoptosis in pituitary adenoma: structure-activity relationship, ER stress and Wnt/β-catenin pathways. | LitMetric

AI Article Synopsis

  • Plant-based natural products, especially cassane-type diterpenes from the genus Caesalpinia, are valuable sources for new cancer treatments.
  • A study found that among 16 isolated compounds, caesalpin G (CAG) exhibited the strongest anticancer effects on pituitary adenoma cells.
  • The research identified key structural features essential for anticancer activity and indicated that CAG triggers cell death through mechanisms involving protein stress responses and the Wnt/β-catenin signaling pathway.

Article Abstract

Plant-derived natural products have been the highly significant sources of novel antitumor agents. The cassane-type diterpenes of genus Caesalpinia have been reported to bear antiproliferative activities toward different types of cancer cells. In this study, we evaluated the antineoplasmic activities of 16 natural origin cassane-type diterpenes isolated from the CHCl extract of the seeds of C. minax in pituitary adenomas cells and identified caesalpin G (CAG) showed the strongest cytotoxicity. Moreover, we further investigated the structure-activity relationship and molecular mechanism of these derivatives systematically. The results confirmed the unsaturated lactone-type ring, hydroxyl at C-7, and alkenyl at C-11 or C-14 functionality as critical for anticancer activity in this family of natural products. In addition, the mechanism experiments also demonstrated unfolded protein response and ER stress and Wnt/β-catenin pathway were involved in the CAG-induced apoptosis.

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Source
http://dx.doi.org/10.1080/10286020.2016.1217520DOI Listing

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