Wang Binya, Huang Keying, Xiao Jiale, Tao Yangyang, Luo Jingjing, Wu Yonghui, Zhou Sainan, He Yingchun, He Lan
Hunan University of Chinese Medicine, Changsha, 410208, China.
The First Hospital of Hunan University of Chinese Medicine, Changsha, 410007, China.
Med Oncol. 2025 May 1;42(6):189. doi: 10.1007/s12032-025-02749-7.
Nasopharyngeal carcinoma (NPC) is a malignant neoplasm that is highly prevalent in East Asia and presents significant therapeutic challenges due to limited treatment options and severe adverse effects. Ursolic acid (UA) is a pentacyclic triterpenoid with anticancer activity in various tumors; however, its mechanism of action in NPC remains unclear. This study integrated network pharmacology with experimental validation to elucidate the molecular mechanism underlying the effect of UA against NPC. Screening of a network pharmacology database identified 39 targets common to UA and NPC, among which P53, STAT3, Bcl-2, IL1B, and CASP3 showed high node degrees in the protein-protein interaction network. Gene Ontology analysis revealed that these targets were primarily enriched in stress response and apoptosis regulation, whereas Kyoto Encyclopedia of Genes and Genomes analysis indicated significant enrichment in the P53 signaling and apoptosis pathways. UA dose-dependently inhibited the proliferation of the NPC cell lines S18 and S26 (p < 0.01), and induced apoptosis, as demonstrated by Annexin V-FITC/PI double fluorescence staining and confirmed by Hoechst 33,342 staining showing nuclear condensation. UA also caused mitochondrial membrane depolarization, as indicated by JC-1 staining. Western blot analysis showed significant upregulation of P53 and the pro-apoptotic protein BAX (p < 0.01), and downregulation of the anti-apoptotic protein Bcl-2 (p < 0.01) following UA treatment. This study is the first to show that UA induces apoptosis in NPC cells by activating the P53 signaling pathway using network pharmacology and experimental validation.
鼻咽癌(NPC)是一种在东亚地区高度流行的恶性肿瘤,由于治疗选择有限和严重的不良反应,带来了重大的治疗挑战。熊果酸(UA)是一种五环三萜类化合物,在多种肿瘤中具有抗癌活性;然而,其在鼻咽癌中的作用机制仍不清楚。本研究将网络药理学与实验验证相结合,以阐明UA抗鼻咽癌作用的分子机制。通过对网络药理学数据库的筛选,确定了UA和NPC共有的39个靶点,其中P53、STAT3、Bcl-2、IL1B和CASP3在蛋白质-蛋白质相互作用网络中显示出较高的节点度。基因本体分析表明,这些靶点主要富集于应激反应和细胞凋亡调控,而京都基因与基因组百科全书分析表明在P53信号通路和细胞凋亡途径中显著富集。UA剂量依赖性地抑制NPC细胞系S18和S26的增殖(p < 0.01),并诱导细胞凋亡,Annexin V-FITC/PI双荧光染色证明了这一点,Hoechst 33,342染色显示核浓缩进一步证实了这一点。JC-1染色表明UA还导致线粒体膜去极化。蛋白质免疫印迹分析显示,UA处理后P53和促凋亡蛋白BAX显著上调(p < 0.01),抗凋亡蛋白Bcl-2下调(p < 0.01)。本研究首次表明,UA通过网络药理学和实验验证激活P53信号通路诱导NPC细胞凋亡。