1. Cassane-type diterpenes from Caesalpinia minax induce apoptosis in pituitary adenoma: structure–activity relationship, ER stress and Wnt/β-catenin pathways.
- Author
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Li, Zong-Yang, Li, Qing-Zhong, Ma, Guo-Xu, Chen, Lei, Zhang, Ce, Chen, Bao-dong, Yang, Jun-Shan, and Li, Wei-Ping
- Subjects
ANIMAL experimentation ,ANTINEOPLASTIC agents ,APOPTOSIS ,BIOLOGICAL assay ,CELL culture ,CELL lines ,CELL physiology ,CELLULAR signal transduction ,CYTOSKELETAL proteins ,ENDOPLASMIC reticulum ,FLAVONOIDS ,FLOW cytometry ,LACTATE dehydrogenase ,MICE ,MOLECULAR structure ,PITUITARY tumors ,PROBABILITY theory ,PROTEOLYTIC enzymes ,RESEARCH funding ,STAINS & staining (Microscopy) ,STATISTICS ,PHYSIOLOGICAL stress ,T-test (Statistics) ,TERPENES ,TOXICITY testing ,WESTERN immunoblotting ,PLANT extracts ,DATA analysis ,WNT proteins ,DESCRIPTIVE statistics ,TEMOZOLOMIDE ,ONE-way analysis of variance - Abstract
Plant-derived natural products have been the highly significant sources of novel antitumor agents. The cassane-type diterpenes of genusCaesalpiniahave 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 CHCl3extract of the seeds ofC. minaxin 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. [ABSTRACT FROM PUBLISHER]
- Published
- 2017
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