Yue-Yu Gu1, Li-Ping Liu1, Jian Qin1, Meng Zhang1, Yuling Chen2, Dongmei Wang3, Zhi Li1, Jing-Zhong Tang4, Sui-Lin Mo5. 1. The First Affiliated Hospital, Sun Yat-sen University, Guangzhou 510080, China. 2. Faculty of Pharmacy, The University of Sydney, NSW 2006, Australia; Kiang Wu Hospital, Macau, China. 3. School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. 4. The First Affiliated Hospital, Sun Yat-sen University, Guangzhou 510080, China. Electronic address: babytangzai@21cn.com. 5. The First Affiliated Hospital, Sun Yat-sen University, Guangzhou 510080, China. Electronic address: mosuilin@mail.sysu.edu.cn.
Abstract
OBJECTIVE: To investigate the effect of baicalein on side population in human multiple myeloma cell line RPMI 8226 and the underlying molecular mechanisms in vitro and in silico. METHODS: MTT assay was applied to detect the anti-proliferation effect of baicalein. The detection of side population cells is based on the Hoechst 33342 exclusion assay technique and flow cytometric analysis. Western blotting assay was used to explore the expression of ABCG2 protein. Homology modeling and molecular docking were performed with Discovery Studio 2.1. RESULTS: Baicalein decreased both cell viability with IC50=168.5 μM and the proportion of SP cells in a dose-dependent manner. Correspondingly, it significantly decreased the expression level of ABCG2 protein. Baicalein also shared similar binding sites and modes with fumitremorgin C to the protein. CONCLUSIONS: Baicalein possessed novel anticancer properties, such as anti-proliferation and drug efflux inhibition in side population cells, which suggested its potential feature of targeting cancer stem cells of multiple myeloma.
OBJECTIVE: To investigate the effect of baicalein on side population in humanmultiple myeloma cell line RPMI 8226 and the underlying molecular mechanisms in vitro and in silico. METHODS:MTT assay was applied to detect the anti-proliferation effect of baicalein. The detection of side population cells is based on the Hoechst 33342 exclusion assay technique and flow cytometric analysis. Western blotting assay was used to explore the expression of ABCG2 protein. Homology modeling and molecular docking were performed with Discovery Studio 2.1. RESULTS:Baicalein decreased both cell viability with IC50=168.5 μM and the proportion of SP cells in a dose-dependent manner. Correspondingly, it significantly decreased the expression level of ABCG2 protein. Baicalein also shared similar binding sites and modes with fumitremorgin C to the protein. CONCLUSIONS:Baicalein possessed novel anticancer properties, such as anti-proliferation and drug efflux inhibition in side population cells, which suggested its potential feature of targeting cancer stem cells of multiple myeloma.