neoglycyrol and Lung-Neoplasms

Molecular targeted therapy for non-small cell lung cancer (NSCLC) has demonstrated promising outcomes. T-lymphokine-activated killer cell-originated protein kinase (TOPK) is found overexpressed in many cancer types such as NSCLC, and is considered to be an effective target for lung cancer treatment. In the present study, we found that glycyrol (GC), a representative coumarin compound isolated from licorice, was highly effective against several human NSCLC cell lines in vitro, and significantly suppressed tumor growth in vivo. Mechanistically, we demonstrated that GC can strongly bind to the TOPK protein and inhibited its kinase activity, leading to the activation of apoptotic signaling pathways. The findings of the present study suggest that GC is a novel promising TOPK inhibitor and this compound deserves to be further investigated for its potential anti-NSCLC activity.

Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Line; Fibroblasts; Flavonoids; Humans; Lung Neoplasms; Male; Mice, Inbred BALB C; Mice, Nude; Mitogen-Activated Protein Kinase Kinases; Protein Kinase Inhibitors; RNA, Small Interfering; Wound Healing