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

IF 4.9 3区 医学 Q1 PHARMACOLOGY & PHARMACY Pharmaceutics Pub Date : 2024-10-05 DOI:10.3390/pharmaceutics16101300
Sakthivel Muthu, Mythileeswari Lakshmikanthan, Edwin Edward-Sam, Mutheeswaran Subramanian, Lakshmanan Govindan, Afrina Begum Mithen Patcha, Kathiravan Krishnan, Nallusamy Duraisamy, Selvakumari Jeyaperumal, Al Thabiani Aziz
{"title":"Encapsulation of Phloroglucinol from <i>Rosenvingea intricata</i> Macroalgae with Zinc Oxide Nanoparticles against A549 Lung Cancer Cells.","authors":"Sakthivel Muthu, Mythileeswari Lakshmikanthan, Edwin Edward-Sam, Mutheeswaran Subramanian, Lakshmanan Govindan, Afrina Begum Mithen Patcha, Kathiravan Krishnan, Nallusamy Duraisamy, Selvakumari Jeyaperumal, Al Thabiani Aziz","doi":"10.3390/pharmaceutics16101300","DOIUrl":null,"url":null,"abstract":"<p><strong>Background/objectives: </strong>Phloroglucinol (PHL), a phenolic compound extracted from the brown alga <i>Rosenvingea intricata</i>, 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.</p><p><strong>Methods: </strong>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.</p><p><strong>Results: </strong>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<sub>50</sub> 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.</p><p><strong>Conclusions: </strong>The synthesized ZnO-PEG-PHL NPs demonstrated enhanced antioxidant and anticancer properties, making them promising candidates for cancer therapy and antioxidant applications.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"16 10","pages":""},"PeriodicalIF":4.9000,"publicationDate":"2024-10-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11510838/pdf/","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceutics","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.3390/pharmaceutics16101300","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0

Abstract

Background/objectives: Phloroglucinol (PHL), a phenolic compound extracted from the brown alga Rosenvingea intricata, 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 IC50 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.

查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
用氧化锌纳米颗粒包封 Rosenvingea intricata 大型藻类中的 Phloroglucinol,对抗 A549 肺癌细胞。
背景/目的:PHL 是一种从褐藻 Rosenvingea intricata 中提取的酚类化合物,具有很强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粒子(ZnO NPs),以提高其治疗潜力:用丙酮提取 PHL,并通过 Sephadex LH-20 柱层析纯化,得到高富集馏分(F-3)。纯化后的化合物通过傅立叶变换红外光谱、高效液相色谱、核磁共振和液相色谱-质谱进行了表征。合成 ZnO NPs、PEG 化并与 PHL 共轭,形成 ZnO-PEG-PHL NPs。其表征包括 DLS、zeta 电位、XRD、SEM-EDAX 和封装效率研究。为了评估 PHL 的疗效,还进行了抗氧化试验(DPPH、FRAP、ABTS、RPA)和 A549 肺癌细胞的体外细胞毒性测定:纯化的 PHL 部分显示出较高的酚含量(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 增大到 46.68 nm,zeta 电位从 -37.87 mV 变为 -26.82 mV。在所有试验中,ZnO-PEG-PHL NPs 的抗氧化活性均优于 ZnO-PEG-PHL,而体外细胞毒性试验显示,ZnO NPs 的 IC50 为 40 µg/mL,而 ZnO NPs 为 60 µg/mL,PHL 为 70 µg/mL。细胞凋亡研究显示细胞周期明显停滞并诱导细胞凋亡:结论:合成的 ZnO-PEG-PHL NPs 具有更强的抗氧化和抗癌特性,有望用于癌症治疗和抗氧化应用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 去求助
来源期刊
Pharmaceutics
Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.90
自引率
11.10%
发文量
2379
审稿时长
16.41 days
期刊介绍: Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications,  and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.
期刊最新文献
Modular Nanotransporters Deliver Anti-Keap1 Monobody into Mouse Hepatocytes, Thereby Inhibiting Production of Reactive Oxygen Species. Nanomaterial-Enhanced Microneedles: Emerging Therapies for Diabetes and Obesity. Effectiveness of Lyoprotectants in Protein Stabilization During Lyophilization. Recent Advances in the Drugs and Glucose-Responsive Drug Delivery Systems for the Treatment of Diabetes: A Systematic Review. A Novel Hydrogel Sponge for Three-Dimensional Cell Culture.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1