99mTc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as an auspicious tumour targeting
Abstract Sulfonamide derivatives are a significant class of medicinal compounds. Gold nanoparticles (AuNPs) offer precise cancer treatment through targeted delivery, boasting high drug-loading capacity and low toxicity. This study aimed to develop and evaluate 99mTc-labeled benzenesulfonamide deriva...
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Nature Portfolio
2025-02-01
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| Online Access: | https://doi.org/10.1038/s41598-025-88862-z |
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| author | Adli A. Selim Tamer M. Sakr Basma M. Essa Galal H. Sayed Kurls E. Anwer |
| author_facet | Adli A. Selim Tamer M. Sakr Basma M. Essa Galal H. Sayed Kurls E. Anwer |
| author_sort | Adli A. Selim |
| collection | DOAJ |
| description | Abstract Sulfonamide derivatives are a significant class of medicinal compounds. Gold nanoparticles (AuNPs) offer precise cancer treatment through targeted delivery, boasting high drug-loading capacity and low toxicity. This study aimed to develop and evaluate 99mTc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as a tumor-targeting agent. A novel benzenesulfonamide derivative bearing a pyridine moiety was synthesized. Compound 3 (4-((3-cyano-4-(2,4-dichlorophenyl)-6-phenylpyridin-2-yl)amino)-N-(diaminomethylene)benzenesulfonamide) exhibited remarkable anti-cancer activity against MCF-7 cells. The chemical reduction method was employed to create compound 3-citrate-AuNPs. A comprehensive examination of the synthesized nano-platform was conducted, including zeta potential, size analysis, radiochemical yield, and in-vivo biodistribution in tumor-bearing mice. The nano-platform was successfully produced with good stability, optimal particle size (9 nm diameter for AuNPs), and high radiochemical purity for [99mTc]Tc-compound 3 (88.31 ± 2.14%). In-vivo investigations revealed that intravenously administered [99mTc]Tc-compound 3-citrate-AuNPs accumulated in tumors with a high target-to-non-target ratio. The findings validate the efficacy of the novel [99mTc]Tc-compound 3-citrate-AuNPs platform as a tumor-targeting agent. |
| format | Article |
| id | doaj-art-ceda1cdee44a462780d2bd3cf4ebd2f4 |
| institution | Kabale University |
| issn | 2045-2322 |
| language | English |
| publishDate | 2025-02-01 |
| publisher | Nature Portfolio |
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| series | Scientific Reports |
| spelling | doaj-art-ceda1cdee44a462780d2bd3cf4ebd2f42025-02-09T12:30:38ZengNature PortfolioScientific Reports2045-23222025-02-0115111010.1038/s41598-025-88862-z99mTc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as an auspicious tumour targetingAdli A. Selim0Tamer M. Sakr1Basma M. Essa2Galal H. Sayed3Kurls E. Anwer4Labelled Compounds Department, Egyptian Atomic Energy Authority (EAEA)Radioactive Isotopes and Generators Department, Egyptian Atomic Energy Authority (EAEA)Radioactive Isotopes and Generators Department, Egyptian Atomic Energy Authority (EAEA)Heterocyclic Synthesis Lab., Chemistry Department, Faculty of Science, Ain Shams UniversityHeterocyclic Synthesis Lab., Chemistry Department, Faculty of Science, Ain Shams UniversityAbstract Sulfonamide derivatives are a significant class of medicinal compounds. Gold nanoparticles (AuNPs) offer precise cancer treatment through targeted delivery, boasting high drug-loading capacity and low toxicity. This study aimed to develop and evaluate 99mTc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as a tumor-targeting agent. A novel benzenesulfonamide derivative bearing a pyridine moiety was synthesized. Compound 3 (4-((3-cyano-4-(2,4-dichlorophenyl)-6-phenylpyridin-2-yl)amino)-N-(diaminomethylene)benzenesulfonamide) exhibited remarkable anti-cancer activity against MCF-7 cells. The chemical reduction method was employed to create compound 3-citrate-AuNPs. A comprehensive examination of the synthesized nano-platform was conducted, including zeta potential, size analysis, radiochemical yield, and in-vivo biodistribution in tumor-bearing mice. The nano-platform was successfully produced with good stability, optimal particle size (9 nm diameter for AuNPs), and high radiochemical purity for [99mTc]Tc-compound 3 (88.31 ± 2.14%). In-vivo investigations revealed that intravenously administered [99mTc]Tc-compound 3-citrate-AuNPs accumulated in tumors with a high target-to-non-target ratio. The findings validate the efficacy of the novel [99mTc]Tc-compound 3-citrate-AuNPs platform as a tumor-targeting agent.https://doi.org/10.1038/s41598-025-88862-zBenzenesulfonamidePyridine moietyCitrate-AuNPsTumour targeting99mTc-radiolabeling |
| spellingShingle | Adli A. Selim Tamer M. Sakr Basma M. Essa Galal H. Sayed Kurls E. Anwer 99mTc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as an auspicious tumour targeting Scientific Reports Benzenesulfonamide Pyridine moiety Citrate-AuNPs Tumour targeting 99mTc-radiolabeling |
| title | 99mTc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as an auspicious tumour targeting |
| title_full | 99mTc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as an auspicious tumour targeting |
| title_fullStr | 99mTc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as an auspicious tumour targeting |
| title_full_unstemmed | 99mTc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as an auspicious tumour targeting |
| title_short | 99mTc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as an auspicious tumour targeting |
| title_sort | 99mtc labeled benzenesulfonamide derivative entrapped gold citrate nanoparticles as an auspicious tumour targeting |
| topic | Benzenesulfonamide Pyridine moiety Citrate-AuNPs Tumour targeting 99mTc-radiolabeling |
| url | https://doi.org/10.1038/s41598-025-88862-z |
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