betulafolientriol and Carcinoma--Ehrlich-Tumor

Antitumor and cytotoxic activity of monoglucosides such as 3-0-panaxadiol (1), 12-0-panaxadiol (2) and 20-0-panaxadiol (3) and 3-0-betulafolientriol (4), 12-0-betulafolientriol (5) and 20-0-betulafolientriol (6) was studied. It was found that in concentrations of 10 to 50 micrograms/ml the above monosides induced marked impairment of the selective permeability of the tumor cells and the inhibition of the labeled precursor inclusion into the macromolecule biosynthesis. Administration of the monosides in a single dose of 100 mg/kg 24 hours after the inoculation of the Ehrlich tumor cells resulted in prolongation of the mean life-span of the mice by 144 per cent (1), 153 per cent (2), 144 per cent (3), 125 per cent (4), 133 per cent (5) and 178 per cent (6). A significant reduction of the tumor mass was observed at the early stages of the tumor development and later the tumor progress intensively resumed. The tests for the effect of the monoside-activated macrophages on the growth of the tumor cells showed that production of the growth factors by the macrophages was stable and had a negative action on the efficacy of the chemotherapy with the monoglucosides.

Topics: Animals; Antineoplastic Agents; Antineoplastic Agents, Phytogenic; Carcinoma, Ehrlich Tumor; Cell Membrane Permeability; Drugs, Chinese Herbal; Glycosides; Macrophages; Mice; Molecular Structure; Sapogenins; Triterpenes; Tumor Cells, Cultured

The effect of triterpene glycosides synthesized on the basis of betulafolientriol, ginsenoside Rb1 from gingseng, betulafolientriol and its 3-epimer on the growth of the Ehrlich tumor cell cultures was studied. It was shown that, in relation to the quantitative composition and sites of carbohydrate residue linkage to aglycone as well as configuration of the alpha- or beta-hydroxyl group at C-3, the activity of the triterpenoids of the dammaranic series changed within wide ranges. 3- and 12-0-beta-D-glycosides of 3-epibetulafolientriol proved to be the most active.

Topics: Animals; Antineoplastic Agents; Carcinoma, Ehrlich Tumor; Cell Division; Cells, Cultured; Chemical Phenomena; Chemistry; Culture Media; Glycosides; In Vitro Techniques; Plant Extracts; Trees; Triterpenes