Munaza Batool, Batool Fatima, Dilshad Hussain, Rubaida Mahmood, Muhammad Imran, Saeed Akhter, Muhammad Saqib Khan, Saadat Majeed, Muhammad Najam-ul-Haq
{"title":"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","authors":"Munaza Batool, Batool Fatima, Dilshad Hussain, Rubaida Mahmood, Muhammad Imran, Saeed Akhter, Muhammad Saqib Khan, Saadat Majeed, Muhammad Najam-ul-Haq","doi":"10.1016/j.jpha.2024.100965","DOIUrl":null,"url":null,"abstract":"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.","PeriodicalId":16737,"journal":{"name":"Journal of Pharmaceutical Analysis","volume":"26 1","pages":""},"PeriodicalIF":6.1000,"publicationDate":"2024-03-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Radiotracer labelled thymohydroquinyl gallate capped gold nanoparticles as theranostic radiopharmaceutical for targeted antineoplastic and bioimaging\",\"authors\":\"Munaza Batool, Batool Fatima, Dilshad Hussain, Rubaida Mahmood, Muhammad Imran, Saeed Akhter, Muhammad Saqib Khan, Saadat Majeed, Muhammad Najam-ul-Haq\",\"doi\":\"10.1016/j.jpha.2024.100965\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"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. 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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.
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.