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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
- Source :
- Journal of Asian natural products research. 19(5)
- Publication Year :
- 2016
-
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 CHCl3 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.
- Subjects :
- 0301 basic medicine
Pharmaceutical Science
Antineoplastic Agents
Apoptosis
Analytical Chemistry
03 medical and health sciences
Structure-Activity Relationship
0302 clinical medicine
Drug Discovery
Structure–activity relationship
Humans
Pituitary Neoplasms
Caesalpinia
Cytotoxicity
beta Catenin
Pharmacology
biology
Molecular Structure
Organic Chemistry
Wnt signaling pathway
General Medicine
biology.organism_classification
Wnt Proteins
030104 developmental biology
Complementary and alternative medicine
Biochemistry
030220 oncology & carcinogenesis
Catenin
Cancer cell
Seeds
Unfolded protein response
Molecular Medicine
Diterpenes
Drug Screening Assays, Antitumor
Drugs, Chinese Herbal
Subjects
Details
- ISSN :
- 14772213
- Volume :
- 19
- Issue :
- 5
- Database :
- OpenAIRE
- Journal :
- Journal of Asian natural products research
- Accession number :
- edsair.doi.dedup.....7ecb27c7a24622e3a622a47ca210ac35