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Aspidin PB, a phloroglucinol derivative, induces apoptosis in human hepatocarcinoma HepG2 cells by modulating PI3K/Akt/GSK3β pathway.

Abstract
Aspidin PB, a phloroglucinol derivative isolated from Dryopteris fragrans (L.) Schott, has been previously reported to exert high biological activities. In the present study, we analyzed the apoptotic mechanisms of aspidin PB on human hepatoma cell line, HepG2. Initially, aspidin PB was shown to inhibit the growth of HepG2 cells in a time and dose-dependent manner. After treatment with aspidin PB for 72 h, 48 h and 24 h using MTT assay, the IC(50) values were 10.59 μM, 20.86 μM and 46.59 μM, respectively. Aspidin PB was capable to induce apoptosis, as measured by mitochondrial membrane potential (ΔΨm), acridine orange (AO) staining and propidium iodide (PI)/annexin V-FITC double staining. To further explore the signaling pathway of aspidin PB-mediated apoptosis, we examined PI3K/Akt related proteins. Western blot analysis revealed that aspidin PB inhibited PI3K expression, phosphorylation of Ser473 Akt and Ser9 GSK3β followed by up-regulation of nonsteroidal anti-inflammatory drugs activated gene-1 (NAG-1) expression. Similarly, the effects of aspidin PB on PI3K, Akt, GSK3β, NAG-1 expression were abolished by treatment with the PI3K inhibitor, wortmannin. Taken together, our data suggested that the PI3K/Akt/GSK3β signal pathway may represent one of the major mechanisms of the effects of aspidin PB on human hepatocarcinoma cells.
AuthorsYao Sun, Chang Gao, Meng Luo, Wei Wang, Chengbo Gu, Yuangang Zu, Ji Li, Thomas Efferth, Yujie Fu
JournalChemico-biological interactions (Chem Biol Interact) Vol. 201 Issue 1-3 Pg. 1-8 (Jan 25 2013) ISSN: 1872-7786 [Electronic] Ireland
PMID23178381 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2012 Elsevier Ireland Ltd. All rights reserved.
Chemical References
  • Androstadienes
  • Phosphoinositide-3 Kinase Inhibitors
  • Protein Kinase Inhibitors
  • Phloroglucinol
  • GSK3B protein, human
  • Glycogen Synthase Kinase 3 beta
  • Proto-Oncogene Proteins c-akt
  • Glycogen Synthase Kinase 3
  • Wortmannin
Topics
  • Androstadienes (pharmacology)
  • Apoptosis (drug effects)
  • Carcinoma, Hepatocellular (metabolism)
  • Cell Proliferation (drug effects)
  • Flow Cytometry
  • Glycogen Synthase Kinase 3 (metabolism)
  • Glycogen Synthase Kinase 3 beta
  • Hep G2 Cells
  • Humans
  • Liver Neoplasms (drug therapy, metabolism, pathology)
  • Membrane Potential, Mitochondrial (drug effects)
  • Microscopy, Confocal
  • Phloroglucinol (analogs & derivatives, pharmacology)
  • Phosphatidylinositol 3-Kinases (metabolism)
  • Phosphoinositide-3 Kinase Inhibitors
  • Protein Kinase Inhibitors (pharmacology)
  • Proto-Oncogene Proteins c-akt (metabolism)
  • Signal Transduction (drug effects)
  • Wortmannin

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