Department of Botany, Bangalore University, Jnanabharathi, Bengaluru, 560056, India.
Sci Rep. 2024 Nov 17;14(1):28374. doi: 10.1038/s41598-024-79996-7.
Polyphenols are natural biomolecules known for circumventing several diseases including cancer with little adverse effects. This study aimed to investigate the polyphenol enriched fractions from the leaf extract of Asystasia gangetica for their composition, biological activities such as antioxidant activity, haemolytic effects, and in vitro cytotoxicity against cancer cell lines. LC-MS/MS analysis of the enriched fractions identified a total of 35 distinct polyphenols with caffeic acid, luteolin, apigenin, and protocatechuic acid at higher concentrations. Fractions AG-3 and AG-4 exhibited the highest total antioxidant activity with higher concentration of phenolics and flavonoids. The AG-4 fraction had the highest levels of DPPH radical scavenging (IC = 32.74 µg mL) and ABTS radical scavenging (IC = 29.45 µg mL) activity, in addition to a modest iron chelating activity and reducing power. The fractions exhibited the least haemolytic activity. The cytotoxic potential of enriched fractions against the HCT-116, HeLa, PC-3, and HDF cell lines was further examined. While the extract showed no inhibitory effect on normal HDF cells, the cytotoxic activity of fractions on cell lines varied, with HCT-116 cells having the strongest anticancer activity with an IC of 43.82 µg mL. Additionally, fractions induced apoptotic activity in HCT-116 cells, resulting in cell cycle arrest at the GM phase and an increase in sub-G0/G1 cells, with an IC of 13.54 µg mL after 48 h of incubation. The in silico molecular docking of the active compounds against the TNIK receptor protein and ADMET (Absorption-Distribution-Metabolism-Excretion-Toxicity) characteristics are described. Overall, the study highlights the enhanced biological and antiproliferative activities of polyphenols in Asystasia gangetica leaf extract, which could be further utilized as a potential cancer treatment strategy.
多酚是一类天然生物分子，具有多种生物活性，包括抗癌作用，且副作用较小。本研究旨在从虾钳菜（Asystasia gangetica）叶提取物中分离、鉴定多酚富集部位，并对其组成、抗氧化、溶血和体外细胞毒性进行分析。LC-MS/MS 分析共鉴定出 35 种不同的多酚，其中咖啡酸、木樨草素、芹菜素和原儿茶酸含量较高。AG-3 和 AG-4 两个部位具有较高的总抗氧化活性，其酚类和类黄酮含量也较高。AG-4 部位对 DPPH 自由基（IC = 32.74 µg mL）和 ABTS 自由基（IC = 29.45 µg mL）的清除能力最强，同时还具有适度的铁螯合和还原能力。各部位的溶血活性最低。进一步研究了多酚富集部位对 HCT-116、HeLa、PC-3 和 HDF 细胞系的细胞毒性。提取物对正常 HDF 细胞无抑制作用，而各部位对细胞系的细胞毒性不同，其中 HCT-116 细胞的抑制作用最强，IC 为 43.82 µg mL。此外，各部位能诱导 HCT-116 细胞凋亡，导致细胞周期阻滞在 G0/G1 期，Sub-G0/G1 期细胞增加，48 h 时 IC 为 13.54 µg mL。文中还描述了活性化合物与 TNIK 受体蛋白的分子对接以及 ADMET（吸收-分布-代谢-排泄-毒性）特征。总之，本研究强调了虾钳菜叶提取物中多酚的增强的生物和抗增殖活性，可进一步作为癌症治疗策略的潜在应用。
