Planta Med 2003; 69(8): 705-709
DOI: 10.1055/s-2003-42797
Original Paper
© Georg Thieme Verlag Stuttgart · New York

Cytotoxicity and Anti-Hepatitis B Virus Activities of Saikosaponins from Bupleurum Species

Lien-Chai Chiang1 , Lean Teik Ng2 , Li-Teh Liu3 , Den-en Shieh2 , Chun-Ching Lin4
  • 1Graduate Institute of Medicine, Kaohsiung Medical University, Kaohsiung, Taiwan, R.O.C
  • 2Department of Food Science and Technology, Tajen Institute of Technology, Ping-Tung, Taiwan, R.O.C
  • 3Department of Microbiology, College of Medicine, Kaohsiung Medical University, Kaohsiung, Taiwan, R.O.C
  • 4Graduate Institute of Pharmaceutical Sciences, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan, R.O.C.
Further Information

Publication History

Received: December 20, 2002

Accepted: May 1, 2003

Publication Date:
06 October 2003 (online)


Saikosaponins, the main active constituents of Bupleurum spp., have been shown to possess immunomodulatory, hepatoprotective, anti-tumor and anti-viral activities. In this study, saikosaponins a, c and d were evaluated for cytotoxicity and anti-hepatitis B virus (HBV) activities. Results showed that, with the exception of saikosaponins a and d, HBV-transfected human hepatoma cells (2.2.15 cells) cultured with saikosaponin c showed a significantly lower level of HBeAg in culture medium. Saikosaponin c also possessed activity in inhibiting HBV DNA replication; this inhibitory effect was not due to the cytotoxicity of saikosaponin c or its effect on 2.2.15 cell proliferation. Although saikosaponin d exhibited cytotoxicity on 2.2.15 cells, it failed to inhibit HBV multiplication. The cytotoxicity of saikosaponin d against HepG2 human hepatocellular carcinoma cells was due to the induction of apoptosis through the activation of caspases 3 and 7, which subsequently resulted in poly-ADP-ribose-polymerase (PARP) cleavage. DNA fragmentation was clearly noted at more than 6 h after HepG2 cells exposure to saikosaponin d. The present study concludes that saikosaponin c exhibits anti-HBV activity and saikosaponin d possesses potent cytotoxicity against human hepatocellular carcinoma cells.


Professor Chun-Ching Lin

Graduate Institute of Pharmaceutical Sciences

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Kaohsiung Medical University

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