Kola acuminate, also known as bizzy nut, is a “cure-all” herbal medicine that has been reported to affect a variety of biological processes. Given the hormonal dependency of some of these biological activities, it is possible that non-steroidal androgen present in the bizzy nut is responsible for the medicinal value attributed to it. Several herbal formulations have been developed to treat and/or manage both hormone-responsive and hormone-refractive prostate cancer. Although these herbal remedies have provided some useful effects, they are usually discontinued because of unwanted side effects. We have identified a potentially powerful bioactive compound in the ether extract of Bizzy nut (Biz-2). Components in this bioactive extract possess the ability to modulate prostate cell function, suggesting that it may be useful in the treatment or prevention of prostate cell malfunction. To this end, two specific aims were developed: Aim 1 - Chemical and biological profiling and characterization of the bioactive compounds in Biz-2 and Aim 2 - Identification and characterization of prostate specific biomarkers for bizzy nut exposure in LNCaP cells. We have resolved the crude extract into five fractions using RP-HPLC and tested each fraction using several bioassays in comparison to the crude extract. The crude extract has a cytotoxic effect on LNCaP cells. Three of the fractions also have cytotoxic effects on the cells; however, one fraction has stimulatory effects relative to the control sample (untreated). The remaining fraction has little effect on the cells under the studied conditions. We are continuing to analyze the fractions using bioassays to confirm our results and we have begun to run chemical analyses in order to identify the compounds present in the crude extract and resulting fractions.