Zou Xiang, Sui Yang, Tang Xi-Yu, Zhang Ru, Shu Qi, Gong Tian, Wu Shuang, Sun Zhi-Wei, Li Wen-Lan, Qu Zhong-Yuan
Engineering Research Center of Natural Anticancer Drugs, Ministry of Education, Harbin University of Commerce Harbin 150076, China.
Pharmaceutical Engineering Technology Research Center, College of Pharmacy, Harbin University of Commerce Harbin 150076, China.
Zhongguo Zhong Yao Za Zhi. 2022 Jul;47(13):3597-3608. doi: 10.19540/j.cnki.cjcmm.20220110.402.
This study aimed to decipher the pharmacodynamic material basis and mechanism of herbal pair Bupleurum scorzonerifolium-Paeonia lactiflora(BS-PL) against liver cancer based on UPLC-Q-TOF-MS and network pharmacology. MTT assay and human hepatocellular carcinoma HepG2 cells were used to screen the effective part of BS-PL, the active components of which were further analyzed and identified by UPLC-Q-TOF-MS. Next, we applied Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP) to screen the active ingredients with OB≥30%. Then TCMSP and SwissTargetPrediction were used to collect and predict component targets, followed by the search of liver cancer-related targets with GeneCards and DisGeNET. The intersection targets were obtained using Venny 2.1.0. Protein-protein interaction(PPI) network was constructed using STRING to uncover the core targets, which were subjected to Gene Ontology(GO) and Kyoto Encyclopedia of Genes and Genomes(KEGG) enrichment analysis based on DAVID. Finally, the effects of active ingredients on the expression of main proteins enriched in the key pathways of HepG2 cells were verified by Western blot. The results indicated that compared with 30%, 50%, and 70% ethanol extracts of BS-PL, the n-butanol extraction part(CSYZ) from 95% ethanol extract of BS-PL exhibited the best anti-tumor effect. UPLC-Q-TOF-MS revealed 31 ingredients, 14 of which showed OB≥30%. A total of 220 intersection targets were obtained, from which 35 were selected as the key targets under the condition of two times the median of degree. Among the 215 items with P<0.05 obtained through GO enrichment analysis, 154 were classified into biological processes, 22 into cell components and 39 into molecular functions. KEGG enrichment analysis revealed 95 significantly affected signaling pathways, and the ones(sorted in a descending order by P value) closely related to the anti-liver cancer effect of herbal pair were PI3 K-AKT signaling pathway, TNF signaling pathway, MAPK signaling pathway, HIF-1 signaling pathway, and ErbB signaling pathway. Finally, the PI3 K/AKT signaling pathway involving the largest number of targets was extrapolated, and it was found that this pathway contained 15 core targets and 8 active components. Experimental verification showed that the effective components of BS-PL significantly inhibited the expression of p-PI3 K and p-AKT, consistent with the prediction results of network pharmacology. In conclusion, the main pharmacodynamic substances of BS-PL against liver cancer are 14 components like saikosaponin a, saikosaponin d, and paeoniflorin, which exert the anti-liver cancer effect by regulating PI3 K/AKT pathway.
本研究旨在基于超高效液相色谱-四极杆飞行时间质谱(UPLC-Q-TOF-MS)和网络药理学,解析药对柴胡-白芍(BS-PL)抗肝癌的药效物质基础及作用机制。采用MTT法和人肝癌HepG2细胞筛选BS-PL的有效部位,通过UPLC-Q-TOF-MS进一步分析鉴定其活性成分。接着,应用中药系统药理学数据库与分析平台(TCMSP)筛选口服生物利用度(OB)≥30%的活性成分。然后利用TCMSP和瑞士药物靶点预测工具(SwissTargetPrediction)收集并预测成分靶点,再通过基因卡片(GeneCards)和疾病基因数据库(DisGeNET)检索肝癌相关靶点。使用Venny 2.1.0获取交集靶点。利用STRING构建蛋白质-蛋白质相互作用(PPI)网络以揭示核心靶点,并基于DAVID对其进行基因本体论(GO)和京都基因与基因组百科全书(KEGG)富集分析。最后,通过蛋白质免疫印迹法(Western blot)验证活性成分对HepG2细胞关键通路中富集的主要蛋白表达的影响。结果表明,与BS-PL的30%、50%和70%乙醇提取物相比,BS-PL的95%乙醇提取物的正丁醇萃取部位(CSYZ)表现出最佳的抗肿瘤效果。UPLC-Q-TOF-MS鉴定出31种成分,其中14种的OB≥30%。共获得220个交集靶点,从中选取度中位数两倍条件下的35个作为关键靶点。通过GO富集分析得到的215个P<0.05的条目,其中154个归类于生物学过程,22个归类于细胞组分,39个归类于分子功能。KEGG富集分析显示95条显著受影响的信号通路,与药对抗肝癌作用密切相关的通路(按P值降序排列)为PI3K-AKT信号通路、肿瘤坏死因子(TNF)信号通路、丝裂原活化蛋白激酶(MAPK)信号通路、缺氧诱导因子-1(HIF-1)信号通路和表皮生长因子受体(ErbB)信号通路。最后,推断出涉及靶点数量最多的PI3K/AKT信号通路,发现该通路包含15个核心靶点和8种活性成分。实验验证表明,BS-PL的有效成分显著抑制p-PI3K和p-AKT的表达,与网络药理学预测结果一致。综上所述,BS-PL抗肝癌的主要药效物质为柴胡皂苷a、柴胡皂苷d、芍药苷等14种成分,其通过调节PI3K/AKT通路发挥抗肝癌作用。