Department of Respiratory and Critical Care Medicine, Renmin Hospital of Wuhan University, Zhangzhidong Road No.99, Wuhan, Hubei 430060,China.
Division of Pulmonary and Critical Care Medicine, The First Affiliated Hospital of Wenzhou Medical University, Key Laboratory of Heart and Lung, Wenzhou, Zhejiang 325000,China.
Comb Chem High Throughput Screen. 2022;25(1):29-37. doi: 10.2174/1386207323666201204135941.
Lung cancer is the most commonly occurring cancer, which contributes to the majority of death caused by cancer, where non-small-cell lung cancer (NSCLC) accounts for approximately 85% of lung cancer. To treat NSCLC, STAT3 has been identified as a target with therapeutic potential. The neobavaisoflavone (NBIF) is one of the flavonoids of traditional Chinese medicine Psoralea corylifolial.
Human NSCLC cell lines, PC-9, H460, and A549, were applied to determine NBIF's anti-proliferative effects through cell viability and colony formation detection. The effect of NBIF on cell apoptosis was determined through flow cytometry-based assay. Western blotting was used in this study to confirm the levels of P-STAT3, Bcl-2, and Bax, which are apoptotic proteins.
It was observed that NBIF could decrease the cell viability and its migration and induce apoptosis in human NSCLC cell lines dose-dependently. Levels of P-STAT3, as well as the downstream signals of the STAT3 pathway, were downregulated, suggesting that the tumorsuppression effects of NBIF might be related to the inhibition of STAT3 signaling. Furthermore, NBIF could contribute to the upregulation of BAX and downregulation of BCL2.
NBIF might perform the anti-NSCLC efficacy as a result of the inhibition of the STAT3 pathway. Besides, our work suggests that NBIF could provide therapeutic alternatives for NSCLC.
肺癌是最常见的癌症，也是导致大多数癌症死亡的主要原因，其中非小细胞肺癌（NSCLC）约占肺癌的 85%。为了治疗 NSCLC，STAT3 已被确定为具有治疗潜力的靶点。新补骨脂异黄酮（NBIF）是传统中药补骨脂的一种黄酮类化合物。
应用人非小细胞肺癌细胞系 PC-9、H460 和 A549 来确定 NBIF 通过细胞活力和集落形成检测的抗增殖作用。通过基于流式细胞术的测定来确定 NBIF 对细胞凋亡的影响。本研究采用 Western blot 法来确认凋亡蛋白 P-STAT3、Bcl-2 和 Bax 的水平。
观察到 NBIF 可以降低人非小细胞肺癌细胞系的细胞活力、迁移并呈剂量依赖性诱导细胞凋亡。STAT3 通路的下游信号 P-STAT3 水平下调，表明 NBIF 的肿瘤抑制作用可能与抑制 STAT3 信号有关。此外，NBIF 可以促进 BAX 的上调和 BCL2 的下调。
NBIF 可能通过抑制 STAT3 通路发挥抗 NSCLC 作用。此外，我们的工作表明 NBIF 可为 NSCLC 提供治疗选择。
