Antitumor Effects of Purified Protosappanin B Extracted From Lignum Sappan

Integr Cancer Ther. 2016 Mar;15(1):87-95. doi: 10.1177/1534735415588929. Epub 2015 Jun 2.


Hypothesis: To assess the antitumor effects of protosappanin B extracted from Lignum Sappan.

Study design: Lignum Sappan was sequentially extracted by boiling water and ethyl acetate. The resulting extract was separated by column chromatography, to yield protosappanin B. The compound was then identified by thin-layer chromatography, high-performance liquid chromatography, elemental analysis, and spectrometry (infrared and ultraviolet). The effects on tumor cell viability and growth of purified protosappanin B were evaluated in vitro by trypan blue exclusion and MTT assays, respectively. And the effects of protosappanin B were assessed in vivo, on H22 mouse liver cancer cell invasion and the survival of tumor-bearing mice.

Results: Protosappanin B (2 mg/mL) reduced the viability of human bladder cancer T24 cells and mouse bladder cancer BTT cells in a time-dependent manner (P < .05) and significantly inhibited the growth of the human colon cancer cell lines HCT-116 and SW-480. IC50 values of 21.32, 26.73, and 76.53 µg/mL were obtained for SW-480, HCT-116, and BTT cells, respectively, after 48 hours of treatment with protosappanin B. In addition, pretreatment of H22 cells with protosappanin B (final concentration = 6.25 mg/mL) resulted in complete inhibition of tumor formation in KM mice. Furthermore, protosappanin B (200 and 300 mg/kg) significantly increased the survival of BTT tumor-bearing T739 mice, at a rate comparable to that of 1 mg/kg mitomycin.

Conclusion: Protosappanin B extracted from Lignum Sappan exerts marked antitumor effects both in vitro and in vivo.

Keywords: Lignum Sappan; antitumor effects; protosappanin B.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Drugs, Chinese Herbal / pharmacology*
  • Female
  • HCT116 Cells
  • Humans
  • Mice
  • Oxocins / pharmacology*
  • Plant Extracts / pharmacology*


  • Antineoplastic Agents
  • Drugs, Chinese Herbal
  • Oxocins
  • Plant Extracts
  • protosappanin B