Adli A Selim, Tamer M Sakr, Basma M Essa, Galal H Sayed, Kurls E Anwer
{"title":"99mtc标记的苯磺酰胺衍生物包裹的柠檬酸金纳米颗粒作为吉祥的肿瘤靶向。","authors":"Adli A Selim, Tamer M Sakr, Basma M Essa, Galal H Sayed, Kurls E Anwer","doi":"10.1038/s41598-025-88862-z","DOIUrl":null,"url":null,"abstract":"<p><p>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 [<sup>99m</sup>Tc]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 [<sup>99m</sup>Tc]Tc-compound 3-citrate-AuNPs platform as a tumor-targeting agent.</p>","PeriodicalId":21811,"journal":{"name":"Scientific Reports","volume":"15 1","pages":"4687"},"PeriodicalIF":3.9000,"publicationDate":"2025-02-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11806107/pdf/","citationCount":"0","resultStr":"{\"title\":\"<sup>99m</sup>Tc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as an auspicious tumour targeting.\",\"authors\":\"Adli A Selim, Tamer M Sakr, Basma M Essa, Galal H Sayed, Kurls E Anwer\",\"doi\":\"10.1038/s41598-025-88862-z\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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 [<sup>99m</sup>Tc]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 [<sup>99m</sup>Tc]Tc-compound 3-citrate-AuNPs platform as a tumor-targeting agent.</p>\",\"PeriodicalId\":21811,\"journal\":{\"name\":\"Scientific Reports\",\"volume\":\"15 1\",\"pages\":\"4687\"},\"PeriodicalIF\":3.9000,\"publicationDate\":\"2025-02-08\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11806107/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Scientific Reports\",\"FirstCategoryId\":\"103\",\"ListUrlMain\":\"https://doi.org/10.1038/s41598-025-88862-z\",\"RegionNum\":2,\"RegionCategory\":\"综合性期刊\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"MULTIDISCIPLINARY SCIENCES\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Scientific Reports","FirstCategoryId":"103","ListUrlMain":"https://doi.org/10.1038/s41598-025-88862-z","RegionNum":2,"RegionCategory":"综合性期刊","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"MULTIDISCIPLINARY SCIENCES","Score":null,"Total":0}
99mTc-labeled benzenesulfonamide derivative-entrapped gold citrate nanoparticles as an auspicious tumour targeting.
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.
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