Selaginellin derivatives from Selaginella tamariscina and evaluation for anti-breast cancer activity

A phytochemical investigation of Selaginella tamariscina led to the isolation of 17 selaginellin derivatives. Their inhibitory activities against breast cancer cells were screened, and preliminary structure-activity relationships were also established. Among them, dimeric selaginellin 17 showed potential activity against MDA-MB-231 cells with an IC value of 3.2 ± 0.1 μM, corresponding to 4-fold higher potency than the reference compound 5-FU (IC 14.8 ± 0.2 μM). Mechanistic studies indicated that 17 could cause G2/M phase arrest in MDA-MB-231 cells and induce apoptosis accompanied by increased ROS levels.