This study was undertaken to isolate and characterize saponins from seeds of Camellia sinensis. Four triterpene saponins S1, S2, S3, and S4 were isolated by chromatography on silica (60–120 mesh), followed by purification on Sep-Pak C-18 columns. The chemical structures (S1–S4) were elucidated on the basis of 1-D and 2-D NMR. All the saponins show broad-spectrum antifungal activity against Candida albicans, Issatchenkia orientalis, Aspergillus flavus, A. niger, A. ochraceous, A. parasiticus, A. sydowii, and Trichophyton rubrum. The most susceptible test fungus was T. rubrum inhibited at a minimum inhibitory concentration of 31.25 lg/ml by all the four saponins. Cytotoxicity of these saponins was evaluated by methyl thiazole tetrazolium and sulfo-rhodamine B assays. The saponins when tested against five human cancer cells lines, viz., OVCAR-5 (ovarian carcinoma cells), MCF-7 (human breast adenocarcinoma cells), PC-3 (human prostate cancer cells), Colo-205 (colorectal adenocarcinoma cells), and HL-60 (human promyelocytic leukemia cells) showed high cytotoxicity activity (99 %) by S1 and S2 on PC-3 cells at concentration of 100 lg/ml. Similarly, when these saponins were tested against human PBMCs by lymphocytes proliferation assay, none showed significant activity. S3 (IC50 = 1.72 mg/ml) showed high metal-chelating activity at a concentration of 20 mg/ml.