Preferential inhibition of hepatocellular carcinoma by the flavonoid Baicalein through blocking MEK-ERK signaling

  • Authors:
    • Rong-Rui Liang
    • Shu Zhang
    • Jun-An Qi
    • Zhi-Dong Wang
    • Jun Li
    • Pei-Jun Liu
    • Chen Huang
    • Xiao-Feng Le
    • Jun Yang
    • Zong-Fang Li
  • View Affiliations

  • Published online on: June 6, 2012     https://doi.org/10.3892/ijo.2012.1510
  • Pages: 969-978
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Abstract

Baicalein is a purified flavonoid extracted from the roots of Scutellaria baicalensis or Scutellaria radix. Although previous studies have suggested that Baicalein possesses an in vitro anti-hepatocellular carcinoma activity, its in vivo effects and mechanisms of action are still not completely understood. In this study, Baicalein at concentrations of 40-120 µM exhibited significant cytotoxicity to three hepatocellular carcinoma (HCC) cell lines but marginal cytotoxicity to a normal liver cell line in vitro. Compared to a standard chemotherapy drug, 5-fluorouracil (5-FU), Baicalein had greater effect on HCC cells but less toxicity on normal liver cells. Treatment with Baicalein dramatically reduced mitochondrial transmembrane potential, and activated caspase-9 and caspase-3. Blockade of Baicalein-induced apoptosis with a pan-caspase inhibitor partially attenuated Baicalein-induced growth inhibition in HCC. Baicalein treatment significantly inhibited tumor growth of HCC xenografts in mice. Induction of apoptosis was demonstrated in Baicalein-treated xenograft tumors by the terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay. Furthermore, Baicalein treatment dramatically decreased the levels of phosphorylation of MEK1, ERK1/2 and Bad in vitro and in vivo. Overexpression of human MEK1 partially blocked Baicalein-induced growth inhibition. Consequently, these findings suggest that Baicalein preferentially inhibits HCC tumor growth through inhibition of MEK-ERK signaling and by inducing intrinsic apoptosis.
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September 2012
Volume 41 Issue 3

Print ISSN: 1019-6439
Online ISSN:1791-2423

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Spandidos Publications style
Liang R, Zhang S, Qi J, Wang Z, Li J, Liu P, Huang C, Le X, Yang J, Li Z, Li Z, et al: Preferential inhibition of hepatocellular carcinoma by the flavonoid Baicalein through blocking MEK-ERK signaling. Int J Oncol 41: 969-978, 2012.
APA
Liang, R., Zhang, S., Qi, J., Wang, Z., Li, J., Liu, P. ... Li, Z. (2012). Preferential inhibition of hepatocellular carcinoma by the flavonoid Baicalein through blocking MEK-ERK signaling. International Journal of Oncology, 41, 969-978. https://doi.org/10.3892/ijo.2012.1510
MLA
Liang, R., Zhang, S., Qi, J., Wang, Z., Li, J., Liu, P., Huang, C., Le, X., Yang, J., Li, Z."Preferential inhibition of hepatocellular carcinoma by the flavonoid Baicalein through blocking MEK-ERK signaling". International Journal of Oncology 41.3 (2012): 969-978.
Chicago
Liang, R., Zhang, S., Qi, J., Wang, Z., Li, J., Liu, P., Huang, C., Le, X., Yang, J., Li, Z."Preferential inhibition of hepatocellular carcinoma by the flavonoid Baicalein through blocking MEK-ERK signaling". International Journal of Oncology 41, no. 3 (2012): 969-978. https://doi.org/10.3892/ijo.2012.1510