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用氧化锌纳米颗粒封装大型藻类中的间苯三酚以对抗A549肺癌细胞

Encapsulation of Phloroglucinol from Macroalgae with Zinc Oxide Nanoparticles against A549 Lung Cancer Cells.

作者信息

Muthu Sakthivel, Lakshmikanthan Mythileeswari, Edward-Sam Edwin, Subramanian Mutheeswaran, Govindan Lakshmanan, Patcha Afrina Begum Mithen, Krishnan Kathiravan, Duraisamy Nallusamy, Jeyaperumal Selvakumari, Aziz Al Thabiani

机构信息

Center for Global Health Research, Saveetha Medical College and Hospital, Saveetha Institute of Medical and Technical Sciences (SIMATS), Thandalam, Chennai 602105, Tamil Nadu, India.

Department of Biotechnology, University of Madras, Guindy Campus, Chennai 600025, Tamil Nadu, India.

出版信息

Pharmaceutics. 2024 Oct 5;16(10):1300. doi: 10.3390/pharmaceutics16101300.

Abstract

BACKGROUND/OBJECTIVES: Phloroglucinol (PHL), a phenolic compound extracted from the brown alga , exhibits potent antioxidant and anticancer properties. This study aims to extract, purify, and characterize PHL, and further develop functionalized zinc oxide nanoparticles (ZnO NPs) loaded with PHL to enhance its therapeutic potential.

METHODS

PHL was extracted using acetone and purified through Sephadex LH-20 column chromatography, yielding a highly enriched fraction (F-3). The purified compound was characterized by FTIR, HPLC, NMR, and LC-MS. ZnO NPs were synthesized, PEGylated, and conjugated with PHL, forming ZnO-PEG-PHL NPs. Their characterization included DLS, zeta potential, XRD, SEM-EDAX, and encapsulation efficiency studies. Antioxidant assays (DPPH, FRAP, ABTS, RPA) were performed and in vitro cytotoxicity on A549 lung cancer cells were determined to evaluate the therapeutic efficacy of PHL.

RESULTS

The purified PHL fraction showed a high phenolic content (45.65 PHL mg/g), which was was confirmed by spectral analysis. The ZnO-PEG-PHL NPs increased in size from 32.36 nm to 46.68 nm, with their zeta potential shifting from -37.87 mV to -26.82 mV. The antioxidant activity was superior for the ZnO-PEG-PHL NPs in all assays, while the in vitro cytotoxicity tests showed an IC of 40 µg/mL compared to 60 µg/mL for the ZnO NPs and 70 µg/mL for PHL. Apoptotic studies revealed significant cell cycle arrest and apoptosis induction.

CONCLUSIONS

The synthesized ZnO-PEG-PHL NPs demonstrated enhanced antioxidant and anticancer properties, making them promising candidates for cancer therapy and antioxidant applications.

摘要

背景/目的:间苯三酚(PHL)是一种从褐藻中提取的酚类化合物,具有强大的抗氧化和抗癌特性。本研究旨在提取、纯化和表征PHL,并进一步开发负载PHL的功能化氧化锌纳米颗粒(ZnO NPs)以增强其治疗潜力。

方法

使用丙酮提取PHL,并通过葡聚糖凝胶LH - 20柱色谱法进行纯化,得到高度富集的馏分(F - 3)。通过傅里叶变换红外光谱(FTIR)、高效液相色谱(HPLC)、核磁共振(NMR)和液相色谱 - 质谱联用(LC - MS)对纯化后的化合物进行表征。合成ZnO NPs,进行聚乙二醇化,并与PHL共轭,形成ZnO - PEG - PHL NPs。其表征包括动态光散射(DLS)、zeta电位、X射线衍射(XRD)、扫描电子显微镜 - 能谱分析(SEM - EDAX)和包封率研究。进行抗氧化测定(DPPH、FRAP、ABTS、RPA),并测定对A549肺癌细胞的体外细胞毒性,以评估PHL的治疗效果。

结果

纯化的PHL馏分显示出高酚含量(45.65 PHL mg/g),光谱分析证实了这一点。ZnO - PEG - PHL NPs的尺寸从32.36 nm增加到46.68 nm,其zeta电位从 -37.87 mV变为 -26.82 mV。在所有测定中,ZnO - PEG - PHL NPs的抗氧化活性均更优,而体外细胞毒性试验显示其半数抑制浓度(IC)为40 μg/mL,相比之下,ZnO NPs为60 μg/mL,PHL为70 μg/mL。凋亡研究显示有明显的细胞周期停滞和凋亡诱导。

结论

合成的ZnO - PEG - PHL NPs表现出增强的抗氧化和抗癌特性,使其成为癌症治疗和抗氧化应用的有前景的候选物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/07b4/11510838/b306769ecd34/pharmaceutics-16-01300-g001.jpg

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