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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
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| 篇名： | 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 |
| TITLE： | Pharmacodynamic substances and mechanism of Chelidonii Herba-Corydalis Rhizoma against estrogen receptor-positive breast cancer |
| 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693μg/mL；150、300、600μg/mL的CHCR可显著降低磷酸化PI3K、磷酸化Akt、ERα蛋白和ESR1mRNA的表达水平（P＜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 （P＜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. |
| 期刊： | 2023年第34卷第08期 |
| 作者： | 邹翔；舒淇；吴双；于佳慧；张雪瑞；孙雨恒；曲中原 |
| AUTHORS： | ZOU Xiang，SHU Qi，WU Shuang，YU Jiahui，ZHANG Xuerui，SUN Yuheng，QU Zhongyuan |
| 关键字： | 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： | Chelidonium majus； Corydalis yanhusuo； estrogen receptor-positive breast cancer； UPLC-Q-TOF-MS/MS； |
| 阅读数： | 126 次 |
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