Effects of glycyrrhetic acid on human chronic myelogenous leukemia cells

INTRODUCTION: Chronic myelogenous leukemia (CML) is a type of blood cancer which is initially treated with imatinib (first Abl kinase inhibitor). However, some patients with CML are able to develop imatinib resistance. Several new generation drugs have been developed, but do not overcome this problem. Glycyrrhetic Acid (GA) is a plant-derived pentacyclic triterpenoid that exhibits multiple pharmacological properties for the treatment of cancers. The current study aims to investigate the effects of GA on K562 cell line (Bcr-Abl positive leukemia).
METHODS: MTT cell proliferation assay was employed to evaluate the cytotoxic effect of GA compared with imatinib (positive control) against leukemia and normal blood cells. For detection of cell death, apoptotic/necrotic/healthy assay was performed against K562 cell line. To investigate kinase inhibitory activity of GA, the Abl1 kinase profiling assay and molecular docking study were performed.
RESULTS: GA showed Abl kinase inhibitory activity with IC50 value of 29.2 μM and induced apoptosis in K562 cell line after 6 h of treatment.
DISCUSSION AND CONCLUSION: The current findings indicate that this class of plant extract could be a potential candidate for treatment of CML.