黄芩素通过抑制多发性骨髓瘤细胞系 RPMI 8226 中的 ABCG2 降低侧群比例。
Baicalein decreases side population proportion via inhibition of ABCG2 in multiple myeloma cell line RPMI 8226 in vitro.
机构信息
The First Affiliated Hospital, Sun Yat-sen University, Guangzhou 510080, China.
Faculty of Pharmacy, The University of Sydney, NSW 2006, Australia; Kiang Wu Hospital, Macau, China.
出版信息
Fitoterapia. 2014 Apr;94:21-8. doi: 10.1016/j.fitote.2014.01.019. Epub 2014 Jan 25.
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.
目的
探讨黄芩素对人多发性骨髓瘤细胞系 RPMI 8226 中的侧群细胞的影响及其体外和体内的潜在分子机制。
方法
采用 MTT 法检测黄芩素的抗增殖作用。侧群细胞的检测基于 Hoechst 33342 排除试验技术和流式细胞术分析。Western blot 法检测 ABCG2 蛋白的表达。采用 Discovery Studio 2.1 进行同源建模和分子对接。
结果
黄芩素呈剂量依赖性降低细胞活力（IC50=168.5 μM）和侧群细胞的比例。相应地，它显著降低了 ABCG2 蛋白的表达水平。黄芩素与 Fumitremorgin C 也与该蛋白具有相似的结合位点和模式。
结论
黄芩素有新的抗癌特性，如抗增殖和抑制侧群细胞中的药物外排，提示其具有针对多发性骨髓瘤癌干细胞的潜在特性。
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