OBJECTIVE  To discovery sensitive cell lines of tripterygium glycosides tablet against different subtypes of hematological tumors, and to find out the material base for the effect on proliferative inhibition against sensitive cell lines.

  METHODS  The CCK-8 assay was used to assess the effect of tripterygium glycosides tablet and its extract on cell proliferation in vitro; Then, the in vivo subcutaneous xenograft models by injecting sensitive cells were constructed to test the inhibitory activity of tripterygium glycosides tablet; Furthermore, the extract of tripterygium glycosides was systemically chemical investigated by chromatographic separation techniques, mass spectrometry, and nuclear magnetic resonance, and anti-human acute monocytic leukemia (AMOL) activity was tested for each compound; In the end, preparative HPLC was used for the specific removal of triptolide (TP) from the extract of tripterygium glycosides. The anti-AMOL activity was measured and analyzed after removing TP from the formulations of T. wilfordii.

  RESULTS  The results of cell experiments indicated that tripterygium glycosides exhibited potent anti-AMOL activity; Next, in vivo tumor xenograft models showed tripterygium glycosides significantly inhibited the growth of subcutaneous tumor xenografts of AMOL cells; Furthermore, chemical constituents of tripterygium glycosides extract were isolated systemically, the activity were evaluated at the cellular level. It was found that TP showed the strongest anti-AMOL activity. Finally, it was found that the IC₅₀ values of the tripterygium glycosides tablet and its extract against AMOL cells increased 8 and 13 fold, respectively, after removing TP.

  CONCLUSION  Tripterygium glycosides tablet shows significant inhibitory activity against acute monocytic leukemia cells, and its diterpenoid, triptolide, is the most active ingredient.