VI-16, a newly synthesized flavonoid, induces apoptosis through the mitochondrial pathway in human hepatoma cells.

Abstract

VI-16, a newly synthesized flavonoid, has a hydroxy substitution at C5 position, a methoxyl substitution at C5 position, and a piperazine substitution at C7 position. Here, we firstly investigated the potential antitumor effect of VI-16 in HepG2 human hepatocarcinoma cells. The MTT assay showed that VI-16 inhibited HepG2 cell growth in a concentration- and time-dependent manner. To further investigate whether apoptosis induction contributed to the antitumor effects of VI-16, DAPI staining and Annexin-V/PI double staining were performed in our tests. The data showed that VI-16 could induce apoptotic cell death in HepG2 cells. Moreover, mechanistic studies revealed that VI-16-induced apoptosis was a caspase-dependent process by decreasing the expression of pro-caspase-3. The changes in the expression of caspase-8, capsase-9, Bax and bcl-2 after VI-16 treatment suggested that the mitochondrial pathway was involved in the apoptosis induced by VI-16. Furthermore, VI-16 could significantly increase the loss of mitochondrial membrane potential and the expression of p53. Taken together, these results demonstrated that apoptosis induced by VI-16 might be one of the mechanisms by which VI-16 acts as a preventive antitumor drug against human hepatoma.

• Authors: Na Lu, Libin Wei, Dandan Gong, Yuan Gao, Qinsheng Dai, Zhiyu Li, Qinglong Guo
• Journal: Oncology reports (Oncol Rep) Vol. 27 Issue 3 Pg. 873-9 (Mar 2012) ISSN: 1791-2431 [Electronic] Greece
• PMID: 22179765 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Caspase Inhibitors
• Flavonoids
• Proto-Oncogene Proteins c-bcl-2
• VI-16 flavonoid
• bcl-2-Associated X Protein
• Caspase 3
• Caspase 8
• Caspase 9

Topics

• Antineoplastic Agents (pharmacology)
• Apoptosis (drug effects, genetics)
• Carcinoma, Hepatocellular (drug therapy, genetics, pathology)
• Caspase 3 (genetics)
• Caspase 8 (genetics)
• Caspase 9 (genetics)
• Caspase Inhibitors
• Cell Line, Tumor
• Flavonoids (pharmacology)
• Gene Expression Regulation, Neoplastic (drug effects)
• Genes, p53
• Hep G2 Cells
• Humans
• Liver Neoplasms (drug therapy, genetics, pathology)
• Membrane Potential, Mitochondrial (drug effects)
• Mitochondria (drug effects, genetics)
• Proto-Oncogene Proteins c-bcl-2 (genetics)
• Signal Transduction (drug effects)
• bcl-2-Associated X Protein (genetics)