Department of cardiovascular medicine, Qingdao Hospital of Traditional Chinese Medicine, Qingdao, Shandong, China.
Cardiovascular disease department, Shandong University of Traditional Chinese Medicine, Jinan, Shandong, Chinas.
Bioengineered. 2022 Apr;13(4):10998-11011. doi: 10.1080/21655979.2022.2066926.
This study aimed to investigate the effects of luteolin on colorectal cancer (CRC) and explore its underlying mechanism. HCT-116 and HT-29 cells were treated with luteolin, cisplatin, or selumetinib. The cell survival, cell proliferation, apoptosis and cell cycle distribution, and DNA damage were detected using Cell Counting Kit-8, colony formation, flow cytometry, and immunofluorescence staining analysis, respectively. Western blotting was used to detect the expression of apoptosis-related, cycle-related, DNA-damage-related, and mitogen-activated protein kinase (MAPK) pathway-related proteins. Luteolin showed inhibitory effects on cellular growth by reducing cell survival and proliferation, inducing apoptosis and DNA damage, and arresting the cell cycle in a concentration-dependent manner in HCT-116 and HT-29 cells. Meanwhile, luteolin increased the expression of pro-apoptotic proteins, p-CHK1 (central to the induction of cell cycle arrest), and DNA excision repair protein and decreased anti-apoptotic proteins, G2-M phase-related proteins, and DNA repair proteins. The combination of cisplatin and luteolin significantly decreased cell survival and increased the apoptosis rate of HCT-116 and HT-29 cells compared with cisplatin alone. Bioinformatic analysis using the Comparative Toxicogenomics Database and STITCH and MalaCards databases showed that the MAPK pathway is involved in the pharmacology of luteolin. Furthermore, western blotting demonstrated that luteolin plays an inhibitory role by suppressing the MAPK signaling pathway in CRC, which is enhanced when combined with selumetinib. Luteolin can also prevent tumourigenesis in CRC in vivo. In conclusion, luteolin suppressed cell proliferation, blocked the cell cycle, and induced DNA damage and apoptosis progression in CRC cells by mediating the MAPK pathway.
本研究旨在探讨木犀草素对结直肠癌(CRC)的影响,并探讨其潜在机制。用木犀草素、顺铂或 selumetinib 处理 HCT-116 和 HT-29 细胞。使用细胞计数试剂盒-8、集落形成、流式细胞术和免疫荧光染色分析分别检测细胞存活、细胞增殖、细胞凋亡和细胞周期分布以及 DNA 损伤。Western blot 用于检测凋亡相关、周期相关、DNA 损伤相关和丝裂原活化蛋白激酶(MAPK)途径相关蛋白的表达。木犀草素通过降低细胞存活率和增殖、诱导细胞凋亡和 DNA 损伤以及浓度依赖性地使细胞周期停滞,对 HCT-116 和 HT-29 细胞的细胞生长表现出抑制作用。同时,木犀草素增加了促凋亡蛋白、p-CHK1(细胞周期阻滞诱导的核心)和 DNA 切除修复蛋白的表达,降低了抗凋亡蛋白、G2-M 期相关蛋白和 DNA 修复蛋白的表达。与单独使用顺铂相比,顺铂和木犀草素联合使用显著降低了 HCT-116 和 HT-29 细胞的存活率并增加了细胞凋亡率。使用比较毒理学基因组数据库(Comparative Toxicogenomics Database)、STITCH 和 MalaCards 数据库进行的生物信息学分析表明,MAPK 途径参与了木犀草素的药理学作用。此外,Western blot 表明,木犀草素通过抑制 MAPK 信号通路在 CRC 中发挥抑制作用,与 selumetinib 联合使用时作用增强。木犀草素还可以预防 CRC 体内的肿瘤发生。总之,木犀草素通过介导 MAPK 通路抑制 CRC 细胞的增殖、阻断细胞周期并诱导 DNA 损伤和凋亡进展。