Pharmacodynamic substances and mechanism of Chelidonii Herba-Corydalis Rhizoma against estrogen receptor-positive breast cancer

ZOU Xiang; SHU Qi; WU Shuang; YU Jiahui; ZHANG Xuerui; SUN Yuheng; QU Zhongyuan

doi:10.6039/j.issn.1001-0408.2023.08.08

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Pharmacodynamic substances and mechanism of Chelidonii Herba-Corydalis Rhizoma against estrogen receptor-positive breast cancer

更新时间：2023-04-25

- Pharmacodynamic substances and mechanism of Chelidonii Herba-Corydalis Rhizoma against estrogen receptor-positive breast cancer
- ZHONGGUO YAOFANG Vol. 34, Issue 8, Pages: 935-940(2023)
- 作者机构：
  
  1.哈尔滨商业大学药物工程技术研究中心，哈尔滨　150076
  2.哈尔滨商业大学药学院，哈尔滨　150076
- 作者简介：
- 基金信息：
- DOI：10.6039/j.issn.1001-0408.2023.08.08
  CLC： R917;R966
- Published：30 April 2023，
  
  Received：03 November 2022，
  
  Revised：23 February 2023，
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邹翔,舒淇,吴双等.白屈菜-元胡药对抗雌激素受体阳性乳腺癌药效物质及作用机制 ^Δ[J].中国药房,2023,34(08):935-940.

ZOU Xiang,SHU Qi,WU Shuang,et al.Pharmacodynamic substances and mechanism of Chelidonii Herba-Corydalis Rhizoma against estrogen receptor-positive breast cancer[J].ZHONGGUO YAOFANG,2023,34(08):935-940.
邹翔,舒淇,吴双等.白屈菜-元胡药对抗雌激素受体阳性乳腺癌药效物质及作用机制 ^Δ[J].中国药房,2023,34(08):935-940. DOI： 10.6039/j.issn.1001-0408.2023.08.08.

ZOU Xiang,SHU Qi,WU Shuang,et al.Pharmacodynamic substances and mechanism of Chelidonii Herba-Corydalis Rhizoma against estrogen receptor-positive breast cancer[J].ZHONGGUO YAOFANG,2023,34(08):935-940. DOI： 10.6039/j.issn.1001-0408.2023.08.08.

摘要

目的

分析白屈菜-元胡药对（CHCR）的主要成分，预测其抗雌激素受体（ER）阳性乳腺癌的药效物质、潜在作用靶点及通路并进行验证。

方法

采用超高效液相色谱-四极杆飞行时间串联质谱（UPLC-Q-TOF-MS/MS）技术对CHCR乙醇提取物的成分进行分析；对所得成分进行网络药理学分析，构建CHCR“活性成分-靶点-通路”网络，并对富集通路进行体外细胞实验验证。

结果

共鉴定出58个化学成分，含生物碱57个、有机酸1个。网络药理学共筛选出活性成分38个，“成分-疾病”交集靶点的蛋白质-蛋白质互作网络中有核心靶点38个；得基因本体条目258个，京都基因与基因组百科全书通路137条，主要包括雌激素信号通路、磷脂酰肌醇3激酶/蛋白激酶B（PI3K/Akt）信号通路等。验证实验结果显示，CHCR作用于MCF-7细胞的半数抑制浓度为693 μg/mL；150、300、600 μg/mL的CHCR可显著降低磷酸化PI3K、磷酸化Akt、ERα蛋白和ESR1 mRNA的表达水平（

＜0.01）。

结论

CHCR抗ER阳性乳腺癌的作用可能与调控ER、PI3K/Akt通路有关，具有多成分、多靶点的作用特点。

Abstract

OBJECTIVE

To analyze the main components of Chelidonii Herba-Corydalis Rhizoma （CHCR）， and to predict pharmacodynamic substances against estrogen receptor （ER） -positive breast cancer and their potential targets and signaling pathways， followed by verifying experiments.

METHODS

The ethanol extract of CHCR was analyzed by ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry （UPLC-Q-TOF-MS/MS）. The network pharmacology analysis was performed for the screened components. The network diagram of CHCR “active components-target-pathway” was constructed， and the enrichment pathway

in vitro

was validated.

RESULTS

A total of 58 chemical components were identified， including 57 alkaloids and 1 organic acid. A total of 38 active ingredients were screened from the network pharmacology， and 38 core targets were found in the protein-protein interaction network of “component-disease” intersection targets； 258 gene ontology entries and 137 Kyoto encyclopedia of genes and genomics pathways were obtained， mainly including estrogen signal pathway， phosphatidylinositol-3-kinase/protein kinase B （PI3K/Akt） signal pathway， etc. The results of validation test showed that the median inhibitory concentration of CHCR to MCF-7 cells was 693 μg/mL； 150， 300， 600 μg/mL CHCR could significantly reduce the expressions of phosphorylated PI3K， phosphorylated Akt， ERα protein and ESR1 mRNA （

＜0.01）.

CONCLUSIONS

The anti-ER-positive breast cancer effect of CHCR may be related to the regulation of ER and PI3K/Akt pathways， which has the characteristics of multi-component and multi-target effects.

关键词

白屈菜元胡雌激素受体阳性乳腺癌超高效液相色谱-四极杆飞行时间串联质谱网络药理学实验验证

Keywords

Corydalis yanhusuoestrogen receptor-positive breast cancerUPLC-Q-TOF-MS/MSnetwork pharmacologyexperimental verification

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