中国药理学通报2026，Vol.42Issue(2)：264-272,9.DOI:10.12360/CPB202506002
羟基红花黄色素A抑制食管鳞癌耐药细胞KYSE150/5-FU生长的作用及机制
The anti-growth effects of hydroxysafflor yellow A on esophageal squamous cell carcinoma-resistant KYSE150/5-FU cells and its mechanisms
摘要
Abstract
Aim To determine the effect of hy-droxysafflower yellow A(HSYA)on tumor cell growth,migration and invasion,and elucidate the un-derlying molecular mechanisms in esophageal squa-mous cell carcinoma-resistant KYSE150/5-FU cells.Methods CCK-8 and colony formation assay were used to the effects of HSYA on KYSE150/5-FU cell growth.Transwell migration and invasion assay were employed to detect the effect of HSYA on the tumor cell migration and invasion.RT-qPCR was performed to detect the mRNA expression of drug-resistance gene including ID1 and ABCB1.Western blotting was uti-lized to detect the protein levels of PAK1(p21-acti-vated kinase 1),ERK1/2(extracellular signal-regulated kinase 1/2)and p-ERK1/2(T202/Y204).Nude mouse transplant tumor model was established to validate the effect of HSYA on KYSE150/5-FU cells in vivo.Results HSYA suppressed the growth of KYSE150/5-FU cells in a dose-and time-dependent manner.HSYA also remarkably reduced the number of colonies in KYSE150/5-FU cells.In addition,HSYA significantly inhibited the migration and inva-sion of KYSE150/5-FU cells.More importantly,the in vivo experimental results demonstrated that HSYA ex-erted a substantial inhibitory effect on the growth of KYSE150/5-FU cell in nude mice.Compared with KYSE150 cells,the mRNA levels of drug resistance genes ID1 and ABCB1,as well as the protein levels of PAK1 and p-ERK1/2(T202/Y204),were obviously upregulated in KYSE150/5-FU cells;while the levels of ID1,ABCB1,PAK1 and p-ERK1/2(T202/Y204)were greatly downregulated by HSYA in a concentra-tion dependent manner in KYSE150/5-FU cells.The animal experiments shown that HSYA inhibited the growth of KYSE150/5-FU cells in nude mice and down-regulated the expression of ID1,ABCB1,PAK1 and p-ERK1/2(T202/Y204)in tumor tissues.Molecular docking experiments revealed that HSYA bound to the active site of PAK1 protein to exert its inhibitory ef-fect.Conclusion HSYA suppresses the growth,mi-gration and invasion via downregulating PAK1/ERK signaling pathway in KYSE150/5-FU cells.关键词
羟基红花黄色素A/食管鳞癌/PAK1/ERK/肿瘤生长/5-FU/耐药Key words
hydroxysafflor yellow A/esophageal squamous cell carcinoma/PAK1/ERK/tumor growth/5-FU/drug resistance分类
医药卫生引用本文复制引用
段佳雪,王新瑗,陈亮..羟基红花黄色素A抑制食管鳞癌耐药细胞KYSE150/5-FU生长的作用及机制[J].中国药理学通报,2026,42(2):264-272,9.基金项目
国家自然科学基金青年项目(No 82103514) （No 82103514）
河南省重点研发与推广专项(科技攻关)(No 242102311055) （科技攻关）
河南省高等学校重点科研项目(No 25A310011) （No 25A310011）
