Spandana K J, Rodrigues Wilson Joel, Ghate Sudeep D, Rao R Shyama Prasad, Chandrashekar K R, Bhagya N
Yenepoya Research Centre, Yenepoya (Deemed to be University), Mangalore, 575018, Karnataka, India.
JSS Academy of Higher Education and Research, (Deemed to be University), Shivarathreeshwara Nagara, Mysuru, 570015, Karnataka, India.
Appl Biochem Biotechnol. 2025 May;197(5):2887-2909. doi: 10.1007/s12010-024-05173-1. Epub 2025 Jan 11.
Gymnostachyum febrifugum, a less-known ethnomedicinal plant from the Western Ghats of India, is used to treat various diseases and serves as an antioxidant and antibacterial herb. The present study aims to profile the cytotoxic phytochemicals in G. febrifugum roots using GC-MS/MS, in vitro confirmation of cytotoxic potential against breast cancer and an in silico study to understand the mechanism of action. Phytochemical profiling using GC-MS/MS showed the presence of eight cytotoxic molecules with lupeol in high abundance. A potent cytotoxic effect of G. febrifugum roots against breast cancer was also observed with antiproliferation, antimigration, inhibition in colony formation and death of breast cancer cells. Further, the cytotoxic potential of the plant was confirmed with the apoptosis of cells as observed in the flow cytometry. In silico network pharmacology, GO and KEGG analysis suggested the modulation of proteins of MAPK, PI3K-AKT and apoptosis pathways by lupeol to induce cytotoxicity in breast cancer. Further, dynamic simulation revealed MAPK and AKT as the major targets for lupeol. Our studies comprehensively elucidated the role of lupeol, a major phytochemical in G. febrifugum to induce cytotoxicity against breast cancer by targeting major cancer signaling pathways, providing a promising strategy and scientific basis to explore lupeol in targeted cancer therapy.
发热裸柱草是一种来自印度西高止山脉的鲜为人知的民族药用植物,可用于治疗多种疾病,是一种抗氧化和抗菌草药。本研究旨在利用气相色谱 - 质谱 / 质谱联用技术分析发热裸柱草根中的细胞毒性植物化学物质,体外确认其对乳腺癌的细胞毒性潜力,并通过计算机模拟研究了解其作用机制。利用气相色谱 - 质谱 / 质谱联用技术进行的植物化学分析表明,存在八种细胞毒性分子,其中羽扇豆醇含量很高。还观察到发热裸柱草根对乳腺癌具有显著的细胞毒性作用,表现为抗增殖、抗迁移、抑制集落形成以及乳腺癌细胞死亡。此外,通过流式细胞术观察到细胞凋亡,证实了该植物的细胞毒性潜力。在计算机模拟网络药理学、基因本体论(GO)和京都基因与基因组百科全书(KEGG)分析中表明,羽扇豆醇可调节丝裂原活化蛋白激酶(MAPK)、磷脂酰肌醇 -3- 激酶 - 蛋白激酶 B(PI3K-AKT)和凋亡途径的蛋白质,从而在乳腺癌中诱导细胞毒性。此外,动态模拟显示 MAPK 和 AKT 是羽扇豆醇的主要靶点。我们的研究全面阐明了发热裸柱草中的主要植物化学物质羽扇豆醇通过靶向主要癌症信号通路诱导对乳腺癌细胞毒性的作用,为在靶向癌症治疗中探索羽扇豆醇提供了有前景的策略和科学依据。