放射性示踪剂标记的胸腺氢醌没食子酸酯封端金纳米粒子作为治疗放射性药物用于靶向抗肿瘤和生物成像

IF 6.1 1区 医学 Q1 PHARMACOLOGY & PHARMACY
Munaza Batool, Batool Fatima, Dilshad Hussain, Rubaida Mahmood, Muhammad Imran, Saeed Akhter, Muhammad Saqib Khan, Saadat Majeed, Muhammad Najam-ul-Haq
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引用次数: 0

摘要

胸腺醌(Tq)和没食子酸(GA)具有抗肿瘤特性。GA通过干扰多种凋亡信号通路、产生更多活性氧(ROS)、关注细胞周期以及抑制癌基因和基质金属蛋白酶(MMPs)的表达来抑制癌细胞增殖。在这项研究中,胸腺醌(还原成胸腺氢醌后)和没食子酸酯化形成胸腺氢醌没食子酸酯(原药)。胸腺氢醌没食子酸酯(THQG)具有更强的抗肿瘤功效和靶向递送潜力。化学和光谱分析证实了酯的合成。金纳米粒子(AuNPs)因其物理化学和光学特性、生物相容性和低毒性而被用作纳米载体。作为一种高效的药物运输工具,金纳米粒子(AuNPs)可以保护共轭药物不被酶消化。原药作为金金属原子的还原剂,在还原后被载入其上。纳米药物用锝和碘进行放射性标记,利用伽马相机和单光子发射计算机断层扫描(SPECT)监测药物在动物体内的生物分布。I 是一种抗肿瘤物质,有助于提高药物的效率。色谱结果显示放射性标记的百分比很有希望。药物释放显示在 pH 值⁓5.8 时可持续释放。3-[4,5-二甲基噻唑-2-基]-2,5-二苯基溴化四氮唑(MTT)细胞毒性试验显示了药物对 CAL 27 和 MCF 7 细胞株的效力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Radiotracer labelled thymohydroquinyl gallate capped gold nanoparticles as theranostic radiopharmaceutical for targeted antineoplastic and bioimaging
Thymoquinone (Tq) and gallic acid (GA) are known for counter-tumorigenic characteristics. GA inhibits cancer cell proliferation by interfering with many apoptotic signaling pathways, producing more reactive oxygen species (ROS), focusing on the cell cycle, and suppressing the expression of oncogenes and matrix metalloproteinases (MMPs). In this study, thymoquinone (after reducing to thymohydroquinone) and gallic acid are esterified to form thymohydroquinyl gallate (a prodrug). Thymohydroquinyl gallate (THQG) possesses enhanced antineoplastic efficacy and targeted delivery potential. The chemical and spectroscopic analysis confirms ester synthesis. Gold nanoparticles (AuNPs) are employed as nanocarriers due to their physicochemical and optical characteristics, biocompatibility, and low toxicity. As an efficient drug transporter, gold nanoparticles (AuNPs) shield conjugated drugs from enzymatic digestion. The prodrug acts as a reducing agent for Au metal atoms and is loaded onto it after reduction. The nano drug is radiolabeled with Tc and I to monitor the drug biodistribution in animals using a gamma camera and single-photon emission computerized tomography (SPECT). I is an antineoplastic that helps enhance the drug's efficiency. Chromatographic results reveal promising radiolabeling percentages. drug release shows sustained release at pH⁓5.8. 3−[4,5−dimethylthiazol−2−yl]−2,5 diphenyl tetrazolium bromide (MTT) cytotoxicity assay reveals drug potency on CAL 27 and MCF 7 cell lines.
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来源期刊
Journal of Pharmaceutical Analysis
Journal of Pharmaceutical Analysis Chemistry-Electrochemistry
CiteScore
16.20
自引率
2.30%
发文量
674
审稿时长
22 weeks
期刊介绍: The Journal of Pharmaceutical Analysis (JPA), established in 2011, serves as the official publication of Xi'an Jiaotong University. JPA is a monthly, peer-reviewed, open-access journal dedicated to disseminating noteworthy original research articles, review papers, short communications, news, research highlights, and editorials in the realm of Pharmacy Analysis. Encompassing a wide spectrum of topics, including Pharmaceutical Analysis, Analytical Techniques and Methods, Pharmacology, Metabolism, Drug Delivery, Cellular Imaging & Analysis, Natural Products, and Biosensing, JPA provides a comprehensive platform for scholarly discourse and innovation in the field.
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