尽管已经确认芦丁具有强大的抗癌特性，但其作为治疗药物的潜在应用受限于其水溶性。为了克服这一缺点，采用了纳米颗粒技术方法。由于其已被证明具有低毒性且易于功能化，金纳米颗粒（AuNP）成为本研究中首选的纳米体系。合成了新型芦丁封装的金纳米颗粒（AuNPL），并在体外研究了其对人宫颈腺癌HeLa细胞的抗癌效果。AuNPL通过还原氯金酸钠通过在合成过程中添加芦丁完成合成，并对其进行了物理化学特性的表征。通过MTT细胞存活测定，测试了AuNPL对HeLa、人恶性黑色素瘤A375和正常人角质细胞HaCaT的细胞毒性，并确定了其IC50值。通过流式细胞术表明AuNPL能够诱导HeLa细胞的细胞周期阻滞和凋亡。通过DPPH·和ABTS·+清除实验评估了AuNPL的抗氧化活性。通过流式细胞术，通过测量生理和H2O2诱导的细胞内活性氧（ROS）水平来检测AuNPL对HaCaT细胞的细胞保护性。此外，通过单细胞碱性彗星试验，调查了AuNPL对HaCaT细胞的遗传毒性。合成的球形AuNPL在4℃下稳定保存6个月。 观察到AuNPL对HeLa和A375癌细胞比对HaCaT正常角质细胞的细胞毒性更具有选择性。AuNPL通过使细胞在细胞周期的亚G1阶段积累，从而激活caspase-3、-8和-9，诱导细胞凋亡性细胞死亡，发挥其对HeLa细胞的细胞毒性作用。通过DPPH·和ABTS·+清除实验，证实了AuNPL的抗氧化潜力。AuNPL的IC50浓度通过显著降低HaCaT细胞内的生理性ROS水平，对HaCaT细胞表现出细胞保护作用。此外，与芦丁相比，AuNPL对H2O2诱导的细胞内ROS的消除更为成功，对HaCaT细胞具有更强的细胞保护作用。此外，AuNPL的非毒性浓度不会引起HaCaT细胞的明显DNA损伤，表明纳米颗粒的遗传毒性较低。 合成的AuNPL显示出对HeLa细胞的选择性细胞毒性作用，同时对HaCaT细胞具有非毒性和细胞保护作用。观察到的结果鼓励进一步研究AuNPL作为一种有前景的新型抗癌药物。 版权所有 © 2023. Elsevier GmbH出版。

Although luteolin has been confirmed as potent anticancer agent, its potential application as therapeutic is limited by its water solubility. To overcome this shortcoming nanoparticle technology approach was applied. Owing to their proven low toxicity and the possibility to be easily functionalized gold nanoparticles (AuNP) were the nanosystem of choice used in this study. Novel luteolin capped gold nanoparticles (AuNPL) were synthesized and their anticancer effect towards human cervical adenocarcinoma HeLa cells was investigated in vitro.AuNPL were synthesized by reducing chloroauric acid by trisodium citrate with subsequent addition of luteoline during synthesis and their physicochemical characterization was done. AuNPL cytotoxicity against HeLa, human malignant melanoma A375, and normal human keratinocytes HaCaT cells was tested by MTT cell survival assay, and their IC50 values were determined. The capability of AuNPL to induce cell cycle arrest and apoptosis in HeLa cells were demonstrated by flow cytometry. The antioxidant activity of AuNPL was assessed by DPPH· and ABTS·+ scavenging assays. Cytoprotective properties of AuNPL towards HaCaT cells were examined by measuring the physiological and H2O2 induced intracellular reactive oxygen species (ROS) levels using flow cytometry. Also, genotoxicity of AuNPL in HaCaT cells was investigated by the single cell alkaline comet assay.Spherical AuNPL, stable in aqueous solution up to six months at 4 °C were obtained in the synthesis. The selectivity in the cytotoxic action of AuNPL on HeLa and A375 cancer cells compared with their cytotoxicity on normal keratinocytes HaCaT was observed. AuNPL exerted their cytotoxic activity against HeLa cells through accumulation of the cells in the subG1 phase of the cell cycle, inducing the apoptotic cell death mediated by the activation of caspase-3 - 8, and - 9. AuNPL antioxidative potential was confirmed by DPPH· and ABTS·+ scavenging assays. IC50 concentration of AuNPL exerted cytoprotective effect against HaCaT cells by the significant reduction of the physiological intracellular ROS level. Additionally, AuNPL were shown as more cytoprotective towards HaCaT cells then luteolin due to the more successful elimination of H2O2 induced intracellular ROS. Moreover, nontoxic concentrations of AuNPL did not cause considerable DNA damage of HaCaT cells, indicating low genotoxicity of the nanoparticles.Synthesized AuNPL showed selective cytotoxic activity against HeLa cells, while being nontoxic and cytoprotective against HaCaT cells. The observed findings encourage further investigation of AuNPL as a promising novel anticancer agent.Copyright © 2023. Published by Elsevier GmbH.