Comparative two-dimensional HepG2 and L02/ cell membrane chromatography/ C18/ time-of-flight mass spectrometry for screening selective anti-hepatoma components from Scutellariae Radix
Comparative two-dimensional HepG2 and L02/ cell membrane chromatography/ C18/ time-of-flight mass spectrometry for screening selective anti-hepatoma components from Scutellariae Radix
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DOI：
10.1016/j.jpba.2018.10.028
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发表时间：
2019-02-05
影响因子：
3.4
通讯作者：
Yuan, Yongfang
中科院分区：
文献类型：
--
作者：
Gu, Yanqiu;Chen, Xiaofei;Yuan, Yongfang
从中药中筛选有效成分是发现新药或活性结构的有效途径。细胞膜色谱法（CMC）因其高灵敏度和高效性而迅速发展，在病理细胞或组织的活性成分筛选中得到了广泛的应用。然而，单纯利用病理细胞很难明确病理组织与正常组织之间的选择性。本研究建立了一种新型的比较二维（2D）细胞膜色谱系统。简单地说，我们同时加载肝癌HepG2 CMC柱和正常肝脏L02 CMC柱，通过比较黄芩在两种细胞上的保留行为，筛选黄芩中潜在的选择性抗肿瘤成分。黄芩中13种成分在HepG2/ CMC和L02/ CMC两种色谱柱上均有保留。其中，筛选出oroxylin A、wogonin和chrysin三种成分对HepG2细胞有较强的亲和力，在进一步的细胞增殖实验中，HepG2细胞这三种化合物的ICso分别为9.66 μ M、66.77 μ M和36.26 μ M，而L02细胞中，chrysin的ic50为59.10 μ M，其他两种成分的ic50均在200 μ M以上。总体而言，这三种化合物对肝癌细胞的毒性强于对正常细胞的毒性。可以推测oroxylin A、wogonin、chrysin作为选择性抗肝癌活性成分具有开发潜力，有待进一步研究验证。(C) 2018 Elsevier B.V.版权所有
Screening active components from Chinese traditional medicine is an effective approach to discover new drugs or active structures. Cell membrane chromatography (CMC), developed rapidly because of its high sensitivity and effectiveness, has achieved a wide application in screening active components on pathological cells or tissues. However, it is hard to clarify the selectivity between pathological and normal tissues through simply using pathological cells. In this study, a novel comparative two-dimensional (2D) cell membrane chromatography system was established. Briefly, hepatic carcinoma HepG2 CMC columns and normal hepatic L02 CMC columns were simultaneously loaded to screen potential selective antitumor components from Scutellariae Radix by comparing the retention behaviors on two kinds of cells. Totally 13 components in Scutellariae Radix retained on both HepG2/ CMC and L02/ CMC columns. Among them, three components, oroxylin A, wogonin and chrysin, were screened out to perform stronger affinity on HepG2 columns, and in further cell proliferation assay, ICso of these three compounds of HepG2 cells were 9.66 mu M, 66.77 mu M and 36.26 mu M respectively, while of L02 cells, IC(50 )of chrysin was 59.10 mu M and over 200 mu M of the other two components. On the whole, the toxity of these three compounds to hepatoma cells was stronger than to normal cells. It can be supposed that oroxylin A, wogonin, and chrysin own the potential to be developed as selective anti-hepatoma active components, which expects further research to validate. (C) 2018 Elsevier B.V. All rights reserved.