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中药北板蓝根(菘蓝)的抗微管活性导致葡萄糖异硫氰酸盐的形成。

Anti-microtubule activity of the traditional Chinese medicine herb Northern Ban Lan (Isatis tinctoria) leads to glucobrassicin.

机构信息

Molecular Cell Biology, Botanical Institute, Karlsruhe Institute of Technology, Fritz-Haber-Weg 4, Karlsruhe, 76131, Germany.

Department of Chemistry, University of Zürich, Winterthurerstr.190, CH-8057, Zürich, Switzerland.

出版信息

J Integr Plant Biol. 2021 Dec;63(12):2058-2074. doi: 10.1111/jipb.13177. Epub 2021 Nov 10.

Abstract

Traditional Chinese medicine (TCM) belongs to the most elaborate and extensive systems of plant-based healing. The herb Northern Ban Lan (Isatis tinctoria) is famous for its antiviral and anti-inflammatory activity. Although numerous components isolated from I. tinctoria have been characterized so far, their modes of action have remained unclear. Here, we show that extracts from I. tinctoria exert anti-microtubular activity. Using time-lapse microscopy in living tobacco BY-2 (Nicotiana tabacum L. cv Bright Yellow 2) cells expressing green fluorescent protein-tubulin, we use activity-guided fractionation to screen out the biologically active compounds of I. tinctoria. Among 54 fractions obtained from either leaves or roots of I. tinctoria by methanol (MeOH/H O 8:2), or ethyl acetate extraction, one specific methanolic root fraction was selected, because it efficiently and rapidly eliminated microtubules. By combination of further purification with ultra-high-performance liquid chromatography and high-resolution tandem mass spectrometry most of the bioactivity could be assigned to the glucosinolate compound glucobrassicin. Glucobrassicin can also affect microtubules and induce apoptosis in HeLa cells. In the light of these findings, the antiviral activity of Northern Ban Lan is discussed in the context of microtubules being hijacked by many viral pathogens for cell-to-cell spread.

摘要

传统中药(TCM)属于最精细和广泛的植物性治疗体系。草药菘蓝(Isatis tinctoria)以其抗病毒和抗炎活性而闻名。尽管迄今为止已经从 I. tinctoria 中分离出了许多成分,但它们的作用方式仍不清楚。在这里,我们表明 I. tinctoria 提取物具有抗微管活性。使用在表达绿色荧光蛋白-微管的活体烟草 BY-2(Nicotiana tabacum L. cv Bright Yellow 2)细胞中的延时显微镜,我们使用基于活性的分级分离来筛选 I. tinctoria 的生物活性化合物。在通过甲醇(MeOH/H2O 8:2)或乙酸乙酯从 I. tinctoria 的叶或根中获得的 54 个馏分中,有一种特定的甲醇根馏分被选中,因为它能有效地快速消除微管。通过与超高效液相色谱和高分辨率串联质谱的进一步组合纯化,大部分生物活性可归因于硫代葡萄糖苷化合物葡萄糖异硫氰酸盐。葡萄糖异硫氰酸盐还可以影响微管并诱导 HeLa 细胞凋亡。鉴于这些发现,讨论了菘蓝的抗病毒活性与微管被许多病毒病原体劫持用于细胞间传播的关系。

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