Betulinic acid (BA), a naturally occurring triterpene found in the bark of the white birch tree, has been investigated to induce apoptosis in various cancer cells and animal models. However, there is no report of the chemopreventive effect of BA in cervical cancer cells. Using KB human cervical cancer cells as a model, we currently show that BA decreases cell viability and induces apoptotic cell death. The mechanism of the BA-induced anti-growth response in KB cells is due to the down-regulation of specificity protein 1 (Sp 1) and its downstream targets, myeloid cell leukemia-1(Mcl-1) and survivin. Thus, BA acts as a novel chemopreventive agent through the regulation of Sp1 that is highly expressed in tumors.