The potent antioxidative sesquiterpene, cacalol, was isolated from Cacalia delphiniifolia Sleb et Zucc, and identified by an analysis of the MS and NMR spectral data. Cacalol showed potent antioxidative activity in a rat brain homogenate model (IC 50 of 40 nM). Cacalol also proved to be a potent neuroprotective substance which could protect neuronal hybridoma N18-RE-105 cells from L-glutamate toxicity.