Formosanin-C, an immunomodulator with antitumor activity.

Paris formosana Hayata (Liliaceae) grown in the mountain areas of Taiwan, has been used as a folk remedy for snake bite, and as an anti-inflammatory or anti-neoplastic agent. The effects of formosanin-C, a diosgenin saponin isolated from Paris formosana, on immune responses and transplantable murine tumor were studied. In culture systems, formosanin-C (0.03-0.16 microM) displayed significant enhancement of the blastogenic response of human peripheral blood cells to phytohemagglutinin. Formosanin-C also significantly increased the 3H-thymidine incorporation of ConA-stimulated lymphocytes at concentrations of 0.1 and 0.01 microM. The responsiveness of the granulocyte/macrophage colony-forming cells (GM-CFC) to mouse fibroblast cells L929 conditioned medium was altered in the presence of 0.01 and 0.001 microM of formosanin-C. In addition, formosanin-C given intraperitoneally activated natural killer cell activity at doses of 1-2.5 mg/kg. An intraperitoneal injection of 2.5 mg/kg of formosanin-C markedly induced interferon production, the peak blood level of which was observed 24 h after formosanin-C injection. Growth of subcutaneously transplanted MH134 mouse hepatoma was retarded by intraperitoneal treatment with 1-2.5 mg/kg of formosanin-C. The activity of 5-fluorouracil against MH-134 mouse hepatoma was potentiated by intraperitoneal treatment with formosanin-C. These results suggest that formosanin-C might display antitumor activity in association with modification of the immune system.