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通过靶向PI3K/AKT介导的细胞周期进程发挥抗肝癌作用。 （注：原文句末“and.”表述有误，可能影响准确理解，推测完整内容可能是“and apoptosis”之类，即“通过靶向PI3K/AKT介导的细胞周期进程和凋亡发挥抗肝癌作用” ）

exerts an anti-hepatoma effect by targeting PI3K/AKT-mediated cell cycle progression and .

作者信息

Zhang Yan, Lv Pin, Ma Junmei, Chen Ning, Guo Huishan, Chen Yan, Gan Xiaoruo, Wang Rong, Liu Xuqiang, Fan Sufang, Cong Bin, Kang Wenyi

机构信息

Hebei Key Laboratory of Forensic Medicine, College of Forensic Medicine, Hebei Medical University, Shijiazhuang 050017, China.

Hebei Food Safety Key Laboratory, Hebei Food Inspection and Research Institute, Shijiazhuang 050091, China.

出版信息

Acta Pharm Sin B. 2022 Feb;12(2):890-906. doi: 10.1016/j.apsb.2021.07.010. Epub 2021 Jul 18.

DOI:10.1016/j.apsb.2021.07.010
PMID:35256953
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8897033/
Abstract

is extensively used as a traditional medicine to prevention and treatment of liver cancer. However, its comprehensive chemical fingerprint is uncertain, and the mechanisms, especially the potential therapeutic target for anti-hepatocellular carcinoma (HCC) are still unclear. Using UPLC‒Q-TOF/MS, 139 chemical components were identified in dropping pills (ACDPs). Based on these chemical components, network pharmacology demonstrated that the targets of active components were significantly enriched in the pathways in cancer, which were closely related with cell proliferation regulation. Next, HCC data was downloaded from Gene Expression Omnibus database (GEO). The Cancer Genome Atlas (TCGA) and DisGeNET were analyzed by bioinformatics, and 79 biomarkers were obtained. Furtherly, nine targets of ACDP active components were revealed, and they were significantly enriched in PI3K/AKT and cell cycle signaling pathways. The affinity between these targets and their corresponding active ingredients was predicted by molecular docking. Finally, and experiments showed that ACDPs could reduce the activity of PI3K/AKT signaling pathway and downregulate the expression of cell cycle-related proteins, contributing to the decreased growth of liver cancer. Altogether, PI3K/AKT-cell cycle appears as the significant central node in anti-liver cancer of .

摘要

它被广泛用作预防和治疗肝癌的传统药物。然而，其全面的化学指纹图谱尚不确定，其作用机制，尤其是抗肝细胞癌（HCC）的潜在治疗靶点仍不清楚。使用超高效液相色谱-四极杆飞行时间质谱联用仪（UPLC-Q-TOF/MS），在滴丸（ACDPs）中鉴定出139种化学成分。基于这些化学成分，网络药理学表明活性成分的靶点在癌症相关通路中显著富集，这些通路与细胞增殖调控密切相关。接下来，从基因表达综合数据库（GEO）下载肝癌数据。通过生物信息学分析癌症基因组图谱（TCGA）和疾病基因网络（DisGeNET），获得了79个生物标志物。进一步揭示了ACDP活性成分的9个靶点，它们在PI3K/AKT和细胞周期信号通路中显著富集。通过分子对接预测了这些靶点与其相应活性成分之间的亲和力。最后，实验表明ACDPs可以降低PI3K/AKT信号通路的活性，下调细胞周期相关蛋白的表达，从而导致肝癌生长减缓。总之，PI3K/AKT-细胞周期似乎是ACDPs抗肝癌的重要中心节点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/996b/8897033/d85adbd79ae6/gr8.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/996b/8897033/d85adbd79ae6/gr8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/996b/8897033/af47a631dab2/ga1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/996b/8897033/6c43ded6e765/gr1.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/996b/8897033/55f9f04c656f/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/996b/8897033/7ffc61920c12/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/996b/8897033/a5a4fdb25047/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/996b/8897033/eef0014d2af1/gr6.jpg
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