Issue 29, 2016

Usnic acid is a novel Pim-1 inhibitor with the abilities of inhibiting growth and inducing apoptosis in human myeloid leukemia cells

Abstract

Usnic acid (UA) is a secondary metabolite of lichens with a unique dibenzofuran scaffold. The growth inhibitory and apoptotic effects of UA as well as the potential mechanisms of action were determined in human acute myeloid leukemia HL-60 cells and chronic myeloid leukemia K562 cells. UA inhibits growth and induces apoptosis in both cell lines with HL-60 cells more responsive. The apoptotic effects are associated with a decrease in the levels of the anti-apoptotic protein Mcl-1. UA inhibits mitogen-activated protein kinase-interacting kinase 1/eukaryotic translation-initiation factor 4E (Mnk1/eIF4E) and the proviral integration site of moloney murine leukemia virus-1/eIF4E-binding protein 1 (Pim-1/4E-BP1) signallings in both cell lines. A kinase inhibition assay reveals that UA is a potent Pim-1 inhibitor with limited activity to inhibit Mnk1. Considering the important role of Pim-1 in myeloid leukemia, UA represents a lead compound for developing effective therapeutics for myeloid leukemia treatment.

Graphical abstract: Usnic acid is a novel Pim-1 inhibitor with the abilities of inhibiting growth and inducing apoptosis in human myeloid leukemia cells

Supplementary files

Article information

Article type
Paper
Submitted
14 Jan 2016
Accepted
19 Feb 2016
First published
22 Feb 2016

RSC Adv., 2016,6, 24091-24096

Usnic acid is a novel Pim-1 inhibitor with the abilities of inhibiting growth and inducing apoptosis in human myeloid leukemia cells

Y. Fan, M. Huang, Y. Cao, P. Gong, W. Liu, S. Jin, J. Wen, Y. Jing, D. Liu and L. Zhao, RSC Adv., 2016, 6, 24091 DOI: 10.1039/C6RA01159D

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