Gallium maltolate is a promising chemotherapeutic agent for the treatment of hepatocellular carcinoma.

Abstract

BACKGROUND:

Hepatocellular carcinoma (HCC) is a particularly lethal cancer with few treatment options. Since gallium is known to accumulate specifically in HCC tumors but not in non-tumor liver, we investigated two gallium compounds, gallium nitrate (GaN) and gallium maltolate (GaM), as potential new agents for treating HCC.

MATERIALS AND METHODS:

The anti-proliferative and apoptotic activities of GaN and GaM were assessed in vitro using four HCC cell lines. HCC gene expression data was analyzed to provide a mechanistic rationale for using gallium in the treatment of HCC.

RESULTS:

Both compounds showed dose-dependent antiproliferative activity in all four HCC cell lines after 6-day drug exposure (IC50 values range from 60-250 microM for gallium nitrate and 25-35 microM for gallium maltolate). Gallium maltolate at 30 microM additionally induced apoptosis after 6 days. HCC gene expression data showed significantly elevated expression of the M2 subunit of ribonucleotide reductase, which is a target for the antiproliferative activity of gallium.

CONCLUSION:

These data support clinical testing of gallium maltolate, an orally active compound, in the treatment of HCC.

• Authors: Mei-Sze Chua, Lawrence R Bernstein, Rui Li, Samuel K S So
• Journal: Anticancer research (Anticancer Res) 2006 May-Jun Vol. 26 Issue 3A Pg. 1739-43 ISSN: 0250-7005 [Print] Greece
• PMID: 16827101 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Organometallic Compounds
• Pyrones
• Receptors, Transferrin
• gallium maltolate
• Gallium
• ribonucleotide reductase M2
• Ribonucleoside Diphosphate Reductase
• gallium nitrate

Topics

• Apoptosis (drug effects)
• Carcinoma, Hepatocellular (drug therapy, genetics, metabolism, pathology)
• Cell Growth Processes (drug effects)
• Cell Line, Tumor
• Dose-Response Relationship, Drug
• Gallium (pharmacology)
• Gene Expression (drug effects)
• Humans
• Liver Neoplasms (drug therapy, genetics, metabolism, pathology)
• Organometallic Compounds (pharmacology)
• Pyrones (pharmacology)
• Receptors, Transferrin (biosynthesis, genetics)
• Ribonucleoside Diphosphate Reductase (biosynthesis, genetics)