Digitonin is a natural product of the glycoside family and is a detergent. Digitonin has antitumor activity, binds to cholesterol molecules to increase the permeability of cell membranes, and is active in the cleavage of cell membranes in a wide range of cells.

METHODS: Rat adrenal pheochromocytoma cells PC-12 were treated with Digitonin (10 μg/mL) for 10 min to increase cell permeability.
RESULTS: After permeabilization with Digitonin, PC12 cells could be stimulated to release norepinephrine by micromolar concentrations of free Ca2+. [1]
METHODS: Human glioblastoma cells U87 were treated with Digitonin (1-5 μg/mL) for 20 min, and cell viability was measured by MTT after overnight cell incubation.
RESULTS: 1 μg/mL Digitonin treatment resulted in a slight increase in cell viability, 3 μg/mL Digitonin reduced the growth-promoting effect, and the cell viability was similar to that of the control, and 5 μg/mL Digitonin inhibited the cell viability, which indicated a significant toxicity to the cells. [2]
METHODS: Immortalized human T-lymphocytes Jurkat were treated with Digitonin (1-4 μg/mL) for 20 min and cell viability was measured by Resazurin assay.
RESULTS: Digitonin treatment resulted in a significant decrease in metabolic activity and this inhibition was concentration-dependent. [2]

METHODS: To determine whether Digitonin enhances the efficacy of CBDCA in vivo, Digitonin (0.2 mL 400 μM) was hepatic arterially infused into LH rats bearing hepatocellular carcinoma tumors, followed by injection of CBDCA 10 min later.
RESULTS: Digitonin pretreatment increased the tumor uptake of CBDCA and enhanced the cytotoxic effect of CBDCA. [3]