1. Kamebakaurin (Kamebakaurine) has the ability to protect the liver from APAP-induced hepatotoxicity, presumably by both inhibiting the inflammatory response and oxidative stress. 2. Kamebakaurin inhibits the expression of hypoxia-inducible factor-1α and its target genes to confer antitumor activity. 3. Kamebakaurin has anti-cancer and anti-inflammatory activities through direct inhibition of DNA-binding activity of nuclear factor-kappa B (NF-κB) p50.4. Kamebakaurin has anti-neuroinflammatory activity via inhibition of c-Jun NH -terminal kinase and p38 mitogen-activated protein kinase pathway in activated microglial cells.