1-O-Acetylbritannilactone has anticancer activity, it suppresses angiogenesis and lung cancer cell growth possibly via regulating the VEGFR-Src-FAK signaling, it also can combine with gemcitabine elicits a potent apoptosis of lung cancer cell. 1-O-Acetylbritannilactone may serve as a novel therapeutic intervention for various cardiovascular diseases, including chronic ischemia, by regulating VEGF signaling and modulating angiogenesis; it is a potent inhibitor of LPS-stimulated VSMC inflammatory responses through blockade of NF-kappaB activity and inhibition of inflammatory gene COX-2 expression. 1-O-Acetylbritannilactone may act as potent natural skin-lightening agents, it exhibits anti-melanogenic activity by suppression of tyrosinase expression via ERK and Akt signaling.