Tenacissoside C

In vitro and in vivo antitumor activities of tenacissoside C from Marsdenia tenacissima.[Pubmed:24338554]

Planta Med. 2014 Jan;80(1):29-38.

Tenacissoside C, a natural bioactive compound of C21 steroidal saponins, was isolated and purified from air-dried stems of Marsdenia tenacissima. In the present study, the MTT assay showed that Tenacissoside C exhibited obvious cytotoxicity in K562 cells with IC50 values of 31.4, 22.2, and 15.1 microM for 24, 48, and 72 h, respectively. Flow cytometry analysis indicated that the antiproliferative activity induced by Tenacissoside C might be executed via G0/G1 cell cycle arrest and proapoptosis in K562 cells. Western blotting analysis elucidated that: A) Tenacissoside C induced K562 cell cycle (G0/G1) arrest via downregulating cycline D1 protein expression; and B) Tenacissoside C induced K562 cell apoptosis via the mitochondrial pathway by downregulating Bcl-2 and Bcl-xL protein expression, upregulating Bax and Bak protein expression, and activating caspase-9 and caspase-3. In vivo, significant tumor growth inhibition activity of Tenacissoside C was observed in K562 cell-bearing nude mice, accompanied by a significant antiangiogenic effect in vivo against K562 cells (a marked decrease in MVD) and associated with enhanced apoptotic cell death (TUNEL staining assay in vivo), both in dose-dependent manners. The treatment with Tenacissoside C did not significantly affect body mass and macroscopic examination of the organs in this mouse tumor model.

[Effects of Marsdenia tenacissima extract on proliferation and apoptosis of hematologic neoplasm cell line cells].[Pubmed:22650025]

Sichuan Da Xue Xue Bao Yi Xue Ban. 2012 Mar;43(2):174-9.

OBJECTIVE: To investigate the effects of the extract from Marsdensia tenacissima on proliferation and apoptosis of human hematologic neoplasm cell line cells. METHODS: Raji, NB4 and K562 cells were treated in vitro with different concentrations of the extract from Marsdensia tenacissima, including different ethanol elution components and C21 steroidal saponin monomer compounds, for different periods. Tumor cell proliferation was measured by MTT colorimetric assay and its apoptosis was determined by the flow cytometry (FCM). RESULTS: Firstly, with higher concentrations, 100 microg/mL and 200 microg/mL, 70% ethanol eluate from Marsdensia tenacissima inhibited the proliferation of Raji, NB4 and K562 cells significantly, in a dose and time dependent manner, compared with 30% and 50% ethanol elution components from Marsdensia tenacissima (P < 0.05). Secondly, four C21 steroidal saponin monomer compounds, tenacissosides B,C,I and marsdenoside K, also inhibited the proliferation of Raji, NB4 and K562 cells in vitro significantly, in a dose and time dependent manner, compared with that of control group (P < 0.05). Among them, Tenacissoside C showed the strongest inhibition effects on proliferation of these cells under all experimental conditions compared with the other three C21 steroidal saponin monomer compounds (P < 0.05). Furthermor, the IC50 of tenacissosides C on proliferation of Raji, NB4 and K562 cells were 64.1 micromol/L, 70.4 micromol/L and 105.8 micromol/L, respectively. Finally, after Raji, NB4 and K562 cells were treated with 98.4 micromol/L Tenacissoside C for 24 h and 48 h, the early apoptosis rates and late apoptosis rates of these tumor cells increased markedly, compared with the control group (P < 0.05). CONCLUSION: The extract from Marsdensia tenacissima, including different ethanol elution components and C21 steroidal saponin monomer compounds, may inhibit the proliferation of some human hematologic neoplasm cell line cells and induce these tumor cells apoptosis in vitro, especially Tenacissoside C, one of the C21 steroidal saponin monomer compounds, showed the strongest effects on proliferation of these tumor cells when compared with other ones, with the strongest inhibition activities on human Burkitt's lymphoma cell line Raji cells.