Department of Neurosurgery, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, People's Republic of China.
Department of Neurosurgery, Xiangya Hospital, Central South University, Changsha, 410008, People's Republic of China.
Drug Des Devel Ther. 2021 Mar 30;15:1369-1383. doi: 10.2147/DDDT.S296862. eCollection 2021.
Chlorogenic acid (CGA) is a type of polyphenolic substance that is widely extracted from many traditional Chinese medicines (eg, Thunb, Oliver) and exhibits a wide range of anti-tumor effects. However, the potential molecular mechanisms of CGA in glioma U373 cells remain unclear.
Network pharmacology analysis was used to explore the potential therapeutic targets of CGA in glioma. Human glioma U373 cells were treated with different concentrations of CGA for 24 h. CCK-8 assays were used to detect the inhibitory rate of cell growth. Annexin V-FITC/PI staining and Hoechst 33342 staining were used to detect apoptosis. PI staining was used to investigate cell-cycle progression. Wound healing assays and transwell assays were used to detect the cell migration and invasion, respectively. Western blotting and immunohistochemistry were used to measure protein levels in vitro and in vivo.
The proliferation of U373 cells was significantly inhibited by CGA in a dose- and time-dependent manner. CGA significantly arrested the cell cycle of U373 cells in the G2/M phase and induced apoptosis. Moreover, CGA significantly suppressed the migration and invasion of U373 cells. Additionally, we found that CGA inhibited the growth of U373 cells in vivo. Furthermore, network pharmacology analysis suggested that the anti-tumor effects of CGA on U373 cells were associated with the down-regulation of the SRC/MAPKs signaling pathway.
The present study indicated that CGA had anti-glioma effects on U373 cells by down-regulating SRC/MAPKs signal pathway.
绿原酸（CGA）是一种广泛存在于多种传统中药（如，Thunb，Oliver）中的多酚类物质，具有广泛的抗肿瘤作用。然而，CGA 对神经胶质瘤 U373 细胞的潜在分子机制尚不清楚。
采用网络药理学分析方法探讨 CGA 治疗神经胶质瘤的潜在作用靶点。用不同浓度的 CGA 处理人神经胶质瘤 U373 细胞 24 h，CCK-8 法检测细胞生长抑制率，Annexin V-FITC/PI 染色和 Hoechst 33342 染色检测细胞凋亡，PI 染色检测细胞周期进程，划痕愈合实验和 Transwell 实验分别检测细胞迁移和侵袭能力，Western blot 和免疫组化检测细胞体外和体内蛋白水平。
CGA 呈剂量和时间依赖性抑制 U373 细胞增殖，显著阻滞 U373 细胞周期于 G2/M 期并诱导细胞凋亡，显著抑制 U373 细胞迁移和侵袭，体内实验亦表明 CGA 抑制 U373 细胞生长。网络药理学分析提示 CGA 对 U373 细胞的抗肿瘤作用可能与下调 SRC/MAPKs 信号通路有关。
本研究表明 CGA 通过下调 SRC/MAPKs 信号通路对 U373 细胞具有抗神经胶质瘤作用。
