Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 198, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112362
Keywords
Elephantopus scaber; Germacrane-type sesquiterpene lactones; Apoptosis; Anti-hepatocarcinoma effect
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Funding
- National Natural Science Foundation of China [81903511]
- Career Development Support Plan for Young and Middle-aged Teachers in Shenyang Pharmaceutical University [ZQN2018006]
- Project of Innovation Team of Liaoning of P.R. China [LT2015027]
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Chromatographic purification of Elephantopus scaber led to 16 new germacrane-type sesquiterpene lactones (1-16), named elephantopinolide A-P, along with a known analogue (17). Their structures were confirmed by comprehensive spectroscopic analyses, single-crystal X-ray diffraction, and comparison between the experimental and calculated ECD spectra. Their hepatocellular inhibition activities against Hep3B and HepG2 cells were screened by MTT assay, and the structure-activity relationships were examined. The results revealed that 10 (IC50 value of 2.83 mu M and 1.98 mu M) is more potent than sorafenib. The underlying mechanism study demonstrated that 10 could markedly induce apoptosis accompanied by increased ROS production and decreased mitochondrial membrane potential, resulting in the autophagy and G2/M phase cell arrest in Hep3B and HepG2 cells. Furthermore, signal pathways including MAPKs and AKT may play important roles in 10-induced hepatocellular carcinoma cells death. (C) 2020 Elsevier Masson SAS. All rights reserved.
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