Isochamaejasmine, a natural product isolated and purified from the roots of Stellera chamaejasme Linn., has inhibition of NF-kappaB activation reversed the anti-apoptotic effect, shows antiplasmodial activity, with an IC(50) of 7.3+/-3.8 mM, but the selectivity was rather limited, and induces apoptosis in leukemia cells by inhibiting the activity of Bcl-2 family proteins, providing evidence for further studying the underlying anti-cancer mechanism of S.