Leachianone A as a potential anti-cancer drug by induction of apoptosis in human hepatoma HepG2 cells.

Abstract

The Chinese herbal medicine Radix Sophorae is widely applied as an anti-carcinogenic/ anti-metastatic agent against liver cancer. In this study, Leachianone A, isolated from Radix Sophorae, possessed a profound cytotoxic activity against human hepatoma cell line HepG2 in vitro, with an IC(50) value of 3.4microg/ml post-48-h treatment. Its action mechanism via induction of apoptosis involved both extrinsic and intrinsic pathways. Its anti-tumor effect was further demonstrated in vivo by 17-54% reduction of tumor size in HepG2-bearing nude mice, in which no toxicity to the heart and liver tissues was observed. In conclusion, this is the first report describing the isolation of Leachianone A from Radix Sophorae and the molecular mechanism of its anti-proliferative effect on HepG2 cells.

• Authors: Crystal Sao-Fong Cheung, Karen Ka-Wing Chung, Julian Chun-Kin Lui, Ching-Po Lau, Po-Ming Hon, Judy Yuet-Wa Chan, Kwok-Pui Fung, Shannon Wing-Ngor Au
• Journal: Cancer letters (Cancer Lett) Vol. 253 Issue 2 Pg. 224-35 (Aug 18 2007) ISSN: 0304-3835 [Print] Ireland
• PMID: 17379399 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Chromones
• Proto-Oncogene Proteins c-bcl-2
• leachianone A

Topics

• Animals
• Antineoplastic Agents (pharmacology, therapeutic use)
• Apoptosis
• Carcinoma, Hepatocellular (drug therapy, metabolism)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Chromones (pharmacology, therapeutic use)
• DNA Fragmentation
• Humans
• Liver Neoplasms (drug therapy, metabolism)
• Membrane Potential, Mitochondrial (drug effects)
• Mice
• Mice, Nude
• Proto-Oncogene Proteins c-bcl-2 (metabolism)
• Xenograft Model Antitumor Assays