Panaxatriol is a triterpene sapogenin originally found in species of Panax (ginseng) that exhibits anti-inflammatory, hepatoprotective, anti-arrhythmic, and antioxidative activities. Panaxatriol increases expression of heme oxygenase 1 (HO-1) and activation of Nrf2 signaling in neurons in a PI3K/Akt-dependent manner. Panaxatriol also decreases acetaminophen-induced increases in ALT and TNF-α, preventing liver injury in vivo. Additionally, panaxatriol inhibits Ca2+ channels, decreasing channel open time and open state probability in vitro and displaying anti-arrhythmic potential. Panaxatriol is a tyrosine hydroxylase inducer. It shows neuroprotective and cardioprotective effects in vivo. Panaxatriol enhances antioxidant activity and inhibits mitochondria-mediated apoptosis. Pretreatment with ginseng total saponin, especially panaxatriol, ameliorates I/R-induced myocardial damage and this protection is caused by reducing oxidative stress. Panaxatriol can relieve myelosuppression induced by radiation injury. The abilities of regulating the expression of hemopoietic growth factor GM-CSF and promoting the maturation of bone marrow cells may be responsible for some of these beneficial effects.