Leachianone A as a potential anti-cancer drug by induction of apoptosis in human hepatoma HepG2 cells.
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.
Cheung
Crystal Sao-Fong
CS
Department of Biochemistry, The Chinese University of Hong Kong, Shatin, Hong Kong, China.
Chung
Karen Ka-Wing
KK
Lui
Julian Chun-Kin
JC
Lau
Ching-Po
CP
Hon
Po-Ming
PM
Chan
Judy Yuet-Wa
JY
Fung
Kwok-Pui
KP
Au
Shannon Wing-Ngor
SW
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D017209:Apoptosis; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy* / Q000378:metabolism; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002867:Chromones / Q000494:pharmacology / Q000627:therapeutic use*; D053938:DNA Fragmentation; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects; D051379:Mice; D008819:Mice, Nude; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000378:metabolism; D023041:Xenograft Model Antitumor Assays
D000970:Antineoplastic Agents; D002867:Chromones; D019253:Proto-Oncogene Proteins c-bcl-2; C523322:leachianone A