LAUSR

Licochalcone A (LCA), isolated from the root of Glycyrrhiza inflata, are known to have medicinal effect such as anti‐oxidant, anti‐bacterial, anti‐viral, and anti‐cancer. Though, as a pharmacological mechanism regulator, anti‐cancer studies on LCA were not investigated in human breast cancer. We investigated the anti‐proliferative and apoptotic effect of LCA in human breast cancer cells MCF‐7 and MDA‐MB‐231 through MTS assay, PI staining, Annexin‐V/7‐AAD assay, mitochondrial membrane potential assay, multi‐caspase assay, RT‐PCR, Western blot analysis, and anchorage‐independent cell transformation assay. Our results showed the little difference between two cells, as MCF‐7 cell is both estrogen/progesterone receptor positive, there were only effect on Sp1 protein level, but not in mRNA level. Adversely, estrogen/progesterone/human epidermal growth factor receptor 2 triple negative, MDA‐MB‐231 showed decreased Sp1 mRNA, and protein levels. To confirm the participation of Sp1 in breast cancer cell viability, siRNA techniques were introduced. Both cells showed dysfunction of mitochondrial membrane potential and mitochondrial ROS production, which reflects it passed intracellular mitochondrial apoptosis pathway. Additionally, LCA showed the anti‐proliferative and apoptotic effect in breast cancer cells through regulating Sp1 and apoptosis‐related proteins in a dose‐ and a time‐dependent manner. Consequently, LCA might be a potential anti‐breast cancer drug substitute. J. Cell. Biochem. 118: 4652–4663, 2017. © 2017 Wiley Periodicals, Inc.