Fan Limei, Ye Xiansheng, Fang Qian, Li Xiaoxuan, Wang Haiping, Sun Binlian, Shu Xiji, Hou Xiaoying, Liu Yuchen
Cancer Institute, School of Medicine, Jianghan University, Wuhan 430056, China.
Hubei Key Laboratory of Cognitive and Affective Disorders, Wuhan Institute of Biomedical Sciences, School of Medicine, Jianghan University, Wuhan 430056, China.
Molecules. 2024 Nov 30;29(23):5678. doi: 10.3390/molecules29235678.
, a plant in the family, is a traditional Chinese medicinal herb known for its unique therapeutic properties, including reported anti-tumor and antioxidant effects. Recent studies suggest that the main constitute of , coumarins, may have potential anti-tumor activity. Recent research suggests that coumarins, the active compounds in , may hold potential anti-tumor activity. However, the pharmacodynamic constituents remain unidentified. This study aims to isolate and characterize the bioactive compounds of and to assess its anti-tumor effects. Initially, seven compounds, including coumarins, a ketone, and a furanolide, were isolated and identified from by semi-preparative high-performance liquid chromatography (HPLC) and nuclear magnetic resonance (NMR) analysis. The anti-tumor effects of these compounds were evaluated across four different cancer cell lines. Among them, the compound cyclobrachycoumarin showed a significant inhibitory effect on colorectal cancer (CRC) cell proliferation and was selected for further investigation. Cyclobrachycoumarin was found to induce CRC cell apoptosis and cell cycle arrest in a dose-dependent manner. This treatment also led to increased levels of ROS and cleaved PARP, along with decreased expressions of survivin, cyclin D1, and CDK1. In vivo studies further demonstrated that cyclobrachycoumarin effectively reduced tumor growth in HT-29 xenograft models by promoting apoptosis and cell cycle arrest, with a favorable tolerability profile. In summary, this study suggests that cyclobrachycoumarin may be a promising candidate for safe and effective CRC therapy.
[植物名称]是[植物所属科名]科的一种植物，是一种传统的中草药，以其独特的治疗特性而闻名，包括据报道具有抗肿瘤和抗氧化作用。最近的研究表明，[植物名称]的主要成分香豆素可能具有潜在的抗肿瘤活性。最近的研究表明，[植物名称]中的活性化合物香豆素可能具有潜在的抗肿瘤活性。然而，药效成分仍未确定。本研究旨在分离和鉴定[植物名称]的生物活性化合物，并评估其抗肿瘤作用。最初，通过半制备高效液相色谱（HPLC）和核磁共振（NMR）分析从[植物名称]中分离并鉴定了七种化合物，包括香豆素、一种酮和一种呋喃内酯。在四种不同的癌细胞系中评估了这些化合物的抗肿瘤作用。其中，化合物环短叶香豆素对结直肠癌（CRC）细胞增殖显示出显著的抑制作用，并被选作进一步研究。发现环短叶香豆素以剂量依赖的方式诱导CRC细胞凋亡和细胞周期停滞。这种处理还导致活性氧（ROS）水平升高和聚（ADP-核糖）聚合酶（PARP）裂解，同时survivin、细胞周期蛋白D1和细胞周期蛋白依赖性激酶1（CDK1）的表达降低。体内研究进一步证明，环短叶香豆素通过促进凋亡和细胞周期停滞有效地减少了HT-29异种移植模型中的肿瘤生长，具有良好的耐受性。总之，本研究表明环短叶香豆素可能是安全有效的CRC治疗的有希望的候选药物。
