Jinan University, Guangzhou, 510632, China.
Jinan University, Guangzhou, 510632, China.
J Ethnopharmacol. 2020 Nov 15;262:113189. doi: 10.1016/j.jep.2020.113189. Epub 2020 Jul 28.
Herba Epimedii (Berberidaceae) has the advantages of "nourishing the kidney and reinforcing the Yang". Many species in this genus have long been used in traditional Chinese medicine (TCM) and have been used as anticancer drugs in traditional Chinese herbal medicine formulations. Icariin, a major flavonoid glycoside extracted from Epimedium brevicornum Maxim, has been widely proven to exert an inhibitory effect on ovarian cancer (OC), and icariin can induce apoptosis and inhibit invasion and migration. However, the underlying mechanism remains unclear, so further research is necessary to verify its traditional use.
This study aimed to explore the regulatory mechanism of icariin in the biological network and signalling pathway of OC through network pharmacology and cytological experiments.
Public databases and R × 3.6.2 software were adopted to predict the potential targets, construct the protein-protein interaction (PPI) network, and perform Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses. After the network pharmacological analysis, cytological experiments, real-time quantitative PCR (qPCR) and Western blot (WB) analyses were used to verify the key signalling pathway.
The targets related to treatment were TNF, MMP9, STAT3, PIK3CA, ERBB2, MTOR, IL2, PTGS2, KDR, and F2. GO and KEGG enrichment analyses indicated that various kinases and the PI3K/AKT signalling pathway were the most enriched molecules and pathways. Icariin inhibited OC SKOV3 cell proliferation, migration and invasion in vitro and promoted apoptosis by inhibiting the PI3K/AKT signalling pathway.
Icariin promotes apoptosis and suppresses SKOV3 cell activities through the PI3K-Akt signalling pathway. This research not only provides a theoretical and experimental basis for more in-depth studies but also offers an efficient method for the rational utilization of a series of icariin flavonoids as anti-tumour drugs.
淫羊藿（小檗科）具有“补肾壮阳”的优点。该属的许多种植物在传统中药（TCM）中已使用多年，并被用于传统中药方剂中的抗癌药物。从淫羊藿中提取的主要黄酮糖苷朝藿定 C 已被广泛证明对卵巢癌（OC）具有抑制作用，朝藿定 C 可诱导细胞凋亡并抑制侵袭和迁移。然而，其潜在机制尚不清楚，因此需要进一步研究来验证其传统用途。
本研究旨在通过网络药理学和细胞学实验，探讨淫羊藿苷在 OC 生物网络和信号通路中的调控机制。
采用公共数据库和 R×3.6.2 软件预测潜在靶点，构建蛋白质-蛋白质相互作用（PPI）网络，并进行基因本体（GO）和京都基因与基因组百科全书（KEGG）富集分析。网络药理学分析后，进行细胞学实验、实时定量 PCR（qPCR）和 Western blot（WB）分析，以验证关键信号通路。
与治疗相关的靶点为 TNF、MMP9、STAT3、PIK3CA、ERBB2、MTOR、IL2、PTGS2、KDR 和 F2。GO 和 KEGG 富集分析表明，各种激酶和 PI3K/AKT 信号通路是最丰富的分子和通路。淫羊藿苷在体外抑制 OC SKOV3 细胞增殖、迁移和侵袭，并通过抑制 PI3K/AKT 信号通路促进细胞凋亡。
淫羊藿苷通过 PI3K-Akt 信号通路促进 SKOV3 细胞凋亡，抑制细胞活性。本研究不仅为更深入的研究提供了理论和实验基础，也为合理利用一系列淫羊藿黄酮类化合物作为抗癌药物提供了有效的方法。
