Pharmacological evaluation of several major ingredients of Chinese herbal medicines in human hepatoma Hep3B cells

C. C. Chou, S. L. Pan, C. M. Teng, J. H. Guh

Research output: Contribution to journalArticle

70 Citations (Scopus)

Abstract

Long-dan-tan (Chinese name) is one of the most common herbal medicines used by Chinese people with chronic liver disease. Accumulated anecdotal evidence suggests that Long-dan-tan may show a beneficial effect in patients with hepatocellular carcinoma. Long-dan-tan is made from five plants: Gentiana root, Scutellaria root, Gardenia fruit, Alisma rhizome, and Bupleurum root. In this study, we have examined the cytotoxic effects of the five major ingredients isolated from the above plants, i.e. gentiopicroside, baicalein, geniposide, alisol B acetate and saikosaponin-d, respectively, on human hepatoma Hep3B cells. Annexin V immunofluorescence detection, DNA fragmentation assays and FACScan analysis of propidium iodide-staining cells showed that gentiopicroside, baicalein, and geniposide had little effect, whereas alisol B acetate and saikosaponin-d profoundly induced apoptosis in Hep3B cells. Alisol B acetate, but not saikosaponin-d, induced G2/M arrest of the cell cycle as well as a significant increase in caspase-3 activity. Interestingly, baicalein by itself induced an increase in H2O2 generation and the subsequent NF-κB activation; furthermore, it effectively inhibited the transforming growth factor-β1 (TGF-β1)-induced caspase-3 activation and cell apoptosis. We suggest that alisol B acetate and saikosaponin-d induced cell apoptosis through the caspase-3-dependent and -independent pathways, respectively. Instead of inducing apoptosis, baicalein inhibits TGF-β1-induced apoptosis via increase in cellular H2O2 formation and NF-κB activation in human hepatoma Hep3B cells.

Original languageEnglish
Pages (from-to)403-412
Number of pages10
JournalEuropean Journal of Pharmaceutical Sciences
Volume19
Issue number5
DOIs
Publication statusPublished - Aug 2003
Externally publishedYes

Fingerprint

Herbal Medicine
Hepatocellular Carcinoma
geniposide
Pharmacology
Apoptosis
Acetates
Caspase 3
Transforming Growth Factors
Alisma
Scutellaria
Gentiana
Gardenia
Bupleurum
G2 Phase Cell Cycle Checkpoints
Rhizome
Plant Roots
Propidium
Annexin A5
DNA Fragmentation
Names

Keywords

  • Alisol-B-monoacetate
  • Apoptosis
  • Baicalein
  • Hep3B
  • Saikosaponin-d

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Pharmacological evaluation of several major ingredients of Chinese herbal medicines in human hepatoma Hep3B cells. / Chou, C. C.; Pan, S. L.; Teng, C. M.; Guh, J. H.

In: European Journal of Pharmaceutical Sciences, Vol. 19, No. 5, 08.2003, p. 403-412.

Research output: Contribution to journalArticle

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abstract = "Long-dan-tan (Chinese name) is one of the most common herbal medicines used by Chinese people with chronic liver disease. Accumulated anecdotal evidence suggests that Long-dan-tan may show a beneficial effect in patients with hepatocellular carcinoma. Long-dan-tan is made from five plants: Gentiana root, Scutellaria root, Gardenia fruit, Alisma rhizome, and Bupleurum root. In this study, we have examined the cytotoxic effects of the five major ingredients isolated from the above plants, i.e. gentiopicroside, baicalein, geniposide, alisol B acetate and saikosaponin-d, respectively, on human hepatoma Hep3B cells. Annexin V immunofluorescence detection, DNA fragmentation assays and FACScan analysis of propidium iodide-staining cells showed that gentiopicroside, baicalein, and geniposide had little effect, whereas alisol B acetate and saikosaponin-d profoundly induced apoptosis in Hep3B cells. Alisol B acetate, but not saikosaponin-d, induced G2/M arrest of the cell cycle as well as a significant increase in caspase-3 activity. Interestingly, baicalein by itself induced an increase in H2O2 generation and the subsequent NF-κB activation; furthermore, it effectively inhibited the transforming growth factor-β1 (TGF-β1)-induced caspase-3 activation and cell apoptosis. We suggest that alisol B acetate and saikosaponin-d induced cell apoptosis through the caspase-3-dependent and -independent pathways, respectively. Instead of inducing apoptosis, baicalein inhibits TGF-β1-induced apoptosis via increase in cellular H2O2 formation and NF-κB activation in human hepatoma Hep3B cells.",
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