دورية أكاديمية
أعرض في EDS

Multi-functionalization of reduced graphene oxide nanosheets for tumor theragnosis: Synthesis, characterization, enzyme assay, in-silico study, radiolabeling and in vivo targeting evaluation.

التفاصيل البيبلوغرافية
العنوان: Multi-functionalization of reduced graphene oxide nanosheets for tumor theragnosis: Synthesis, characterization, enzyme assay, in-silico study, radiolabeling and in vivo targeting evaluation.
المؤلفون: Sakr TM; Radioisotopes Production Facility, Second Egyptian Research Reactor Complex, Egyptian Atomic Energy Authority, Cairo, 13759, Egypt.; Radioactive Isotopes and Generator Department, Hot Labs Center, Egyptian Atomic Energy Authority, Cairo, 13759, Egypt., Elsabagh MF; Radioisotopes Production Facility, Second Egyptian Research Reactor Complex, Egyptian Atomic Energy Authority, Cairo, 13759, Egypt. mohamed.elsabagh@eaea.sci.eg.; Labeled Compounds Department, Hot Labs Center, Egyptian Atomic Energy Authority, Cairo, 13759, Egypt. mohamed.elsabagh@eaea.sci.eg., Fayez H; Labeled Compounds Department, Hot Labs Center, Egyptian Atomic Energy Authority, Cairo, 13759, Egypt., Sarhan MO; Labeled Compounds Department, Hot Labs Center, Egyptian Atomic Energy Authority, Cairo, 13759, Egypt., Syam YM; Department of Therapeutic Chemistry/ National Research Centre, Cairo, Egypt., Anwar MM; Department of Therapeutic Chemistry/ National Research Centre, Cairo, Egypt., Motaleb MA; Labeled Compounds Department, Hot Labs Center, Egyptian Atomic Energy Authority, Cairo, 13759, Egypt., Zaghary WA; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Cairo, Egypt.
المصدر: Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences [Daru] 2024 Jun; Vol. 32 (1), pp. 77-95. Date of Electronic Publication: 2023 Dec 11.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Springer International Publishing Country of Publication: Switzerland NLM ID: 101125969 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 2008-2231 (Electronic) Linking ISSN: 15608115 NLM ISO Abbreviation: Daru Subsets: MEDLINE
أسماء مطبوعة: Publication: 2018- : Cham : Springer International Publishing
Original Publication: Tehran, Iran : The Faculty
مواضيع طبية MeSH: Graphite*/chemistry, Humans ; Animals ; Cell Line, Tumor ; Mice ; Female ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/chemistry ; Molecular Docking Simulation ; Poly (ADP-Ribose) Polymerase-1/antagonists & inhibitors ; Poly (ADP-Ribose) Polymerase-1/metabolism ; Nanostructures/chemistry ; Poly(ADP-ribose) Polymerase Inhibitors/pharmacology ; Poly(ADP-ribose) Polymerase Inhibitors/chemistry ; Breast Neoplasms/drug therapy ; Breast Neoplasms/pathology ; Tissue Distribution
مستخلص: Background: In this study, a combination of nanotechnology, organic synthesis and radiochemistry were utilized in order to design an efficient nano-system conjugated with a suitable radionuclide and an antitumor agent for possible application as tumor theragnostic agent.
Method: Four novel compounds (3 and 4a-c) bearing tetrahydroquinazoline-7-sulfonohydrazide or 1,2,3,4-tetrahydroquinazoline-7-sulfonamide scaffold were designed. Then, docking study predicted that the compounds can be considered as potential inhibitors for PARP-1. Following that; the four compounds were synthesized and properly characterized using 1 HNMR, 13 CNMR, IR and Mass spectroscopy. The cytotoxic effect of the four compounds was evaluated against breast cancer cell line (MDA-MB-436), where compound 3 showed the most promising cytotoxic effect. The inhibitory effect of the four compounds was evaluated in vitro against PARP-1.
Result: Carboxylated graphene oxide nanosheets (NGO-COOH) were synthesized by a modified Hummer's method and has size of range 40 nm. The NGO-COOH nanosheets were proven to be safe and biocompatible when tested in vitro against normal human lung fibroblast cells (MRC-5). The prepared NGO-COOH nanosheets were conjugated with compound 3 then radiolabeled with 99m Tc to yield 99m Tc-NGO-COOH-3 with a radiochemical yield of 98.5.0 ± 0.5%. 99m Tc-NGO-COOH-3 was injected intravenously in solid tumor bearing mice to study the degree of localization of the nano-system at tumor tissue. The results of the study revealed, excellent localization and retention of the designed nano-system at tumor tissues with targeting ratio of 9.0.
Conclusion: Stirred a new candidate tumor theragnostic agent that is safe, selective and stable.
(© 2023. The Author(s).)
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فهرسة مساهمة: Keywords: Active targeting; In-silico study; Nano synthesis; Nanographene sheets; PRAP-1 inhibitor; Radiolabeling; Technetium-99m; Tumor imaging; Tumor theragnosis
المشرفين على المادة: 7782-42-5 (Graphite)
0 (graphene oxide)
0 (Antineoplastic Agents)
EC 2.4.2.30 (Poly (ADP-Ribose) Polymerase-1)
0 (Poly(ADP-ribose) Polymerase Inhibitors)
EC 2.4.2.30 (PARP1 protein, human)
تواريخ الأحداث: Date Created: 20231210 Date Completed: 20240510 Latest Revision: 20240513
رمز التحديث: 20240513
مُعرف محوري في PubMed: PMC11087444
DOI: 10.1007/s40199-023-00487-7
PMID: 38072913
قاعدة البيانات: MEDLINE
الوصف
تدمد:2008-2231
DOI:10.1007/s40199-023-00487-7