Panduratin A inhibits topoisomerase 1 activity in acute myeloid leukaemia cells

Information from the abstract

Panduratin A (Pan-A) is a bioactive prenylated chalcone found in the rhizomes of Boesenbergia rotunda (fingerroot). It has various pharmacological properties, including anticancer, anti-inflammatory, antibacterial and antiviral activity. In this study, Pan-A decreased mitosis, reduced the S phase of the cell cycle and induced apoptosis in acute myeloid leukaemia cells, in part, by inhibiting topoisomerase 1 (Top1) and thus preventing DNA relaxation and replication. This inhibition led to the stimulation of AKT and the degradation of forkhead box O3 (FOXO3). Pan-A markedly increased nuclear factor kappa B (NF-κB) activity as early as 15 min after treatment and showed an estimated half-maximal effective concentration of 0.543 µM in the cell line with the strongest NF-κB activity. The cell line with constitutively active NF-κB was the most sensitive to Pan-A. Gene expression analysis demonstrated that distinct expression patterns correlated with the phenotypic response of each cell line. In summary, our findings indicate that Pan-A’s antileukaemic activity and effects on key signalling pathways are at least partially mediated by inhibiting Top1.

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Related topics: Bioactive natural compounds · Ginger and Zingiberaceae research · NF-κB Signaling Pathways