Bioactivity-guided isolation of anti-proliferative compounds from Curcuma zedoaria against triple negative breast cancer cells†

IF 2.6 3区 化学 Q2 CHEMISTRY, ANALYTICAL Analytical Methods Pub Date : 2025-03-17 DOI:10.1039/D5AY00050E
Hongming Tang, Hongjian Kang, Weijia Zhou, Tao Hou, Zhixin Guo, Yanfang Liu, Xingya Xue and Jixia Wang
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Abstract

Triple-negative breast cancer (TNBC) presents limited clinically effective treatment options. Curcuma zedoaria (C. zedoaria), a traditional medicine, has been used in China to treat various cancers including TNBC, although its active components remain unclear. Herein, we applied multidimensional liquid chromatography combined with bioactivity assay to discover anti-proliferative compounds against TNBC cells from C. zedoaria. Initially, 26 fractions were generated through first-dimensional reverse-phase liquid chromatography and profiled using SUM159 cells for its anti-proliferative activity. Two active fractions were identified and separated. Following the third-dimensional separation, we successfully isolated two compounds, diarylheptanoid a and diarylheptanoid b, and found that both compounds displayed moderate potency in inhibiting SUM159 proliferation with IC50 values of 19.82 ± 3.08 μM and 28.16 ± 1.97 μM, respectively. Transcriptome analysis revealed that the differentially expressed genes induced by diarylheptanoid a were mainly concentrated with the actin function and involved in motor protein pathways. This study suggests that diarylheptanoids may contribute to the anti-TNBC effects of C. zedoaria and provide potential scaffolds for anti-TNBC drug development.

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莪术抗三阴性乳腺癌细胞增殖化合物的生物活性引导分离。
三阴性乳腺癌(TNBC)提供有限的临床有效治疗方案。莪术(Curcuma zedoaria)是一种传统药物,在中国已被用于治疗包括TNBC在内的各种癌症,尽管其有效成分尚不清楚。本研究采用多维液相色谱法结合生物活性测定,发现莪术中抗TNBC细胞增殖的化合物。首先,通过一维反相液相色谱生成26个组分,并使用SUM159细胞对其抗增殖活性进行分析。鉴定并分离了两种活性组分。通过三维分离,我们成功分离到二芳基庚类化合物a和二芳基庚类化合物b,发现这两个化合物对SUM159的增殖均有中等抑制作用,IC50值分别为19.82±3.08 μM和28.16±1.97 μM。转录组分析显示,二芳基庚烷a诱导的差异表达基因主要集中在肌动蛋白功能,参与运动蛋白通路。本研究提示,二芳基庚烷类化合物可能参与了zedoaria抗tnbc的作用,并为抗tnbc药物的开发提供了潜在的支架。
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来源期刊
Analytical Methods
Analytical Methods CHEMISTRY, ANALYTICAL-FOOD SCIENCE & TECHNOLOGY
CiteScore
5.10
自引率
3.20%
发文量
569
审稿时长
1.8 months
期刊介绍: Early applied demonstrations of new analytical methods with clear societal impact
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