{"title":"用于缺氧成像的 64Cu 基复合物的合成、表征和密度泛函理论","authors":"","doi":"10.1016/j.jksus.2024.103398","DOIUrl":null,"url":null,"abstract":"<div><p>An important contributing factor to the growth of aggressive and treatment-resistant tumors is tumor hypoxia. In this investigation, we created a unique tracer, <sup>64</sup>Cu-biacetyl-bis(4-methyl-3-semicarbazone) Complex (<sup>64</sup>Cu-[APSC]<sub>2</sub>), for hypoxia imaging. Numerous spectral and electrochemical analyses were used to characterize the synthesized ligand and its metal complex. The coordination of the metal in the metal complex was also supported by DFT (B3LYP model) calculations. The radiochemical yields and purities of <sup>64</sup>Cu-[APSC]<sub>2</sub> were found to be quantitative, as determined by TLC and HPLC analyses.</p><p>Stability studies in human plasma demonstrated that <sup>64</sup>Cu-[APSC]<sub>2</sub> remained steady for at least four hours while being incubated at 37 °C. MDA-MB-231 cell-line xenografts were placed in nude mice for biodistribution research. The results revealed significant accumulation of the tracer in tumors after 2 h post-injection, which correlated with the redox potential and reactive oxygen species. These findings suggest that <sup>64</sup>Cu-[APSC]<sub>2</sub> shows promising evidence as a theranostic radiopharmaceutical for hypoxic tumors.</p></div>","PeriodicalId":16205,"journal":{"name":"Journal of King Saud University - Science","volume":null,"pages":null},"PeriodicalIF":3.7000,"publicationDate":"2024-08-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1018364724003100/pdfft?md5=02f2c46b8e2f400879403e987ce9d4b1&pid=1-s2.0-S1018364724003100-main.pdf","citationCount":"0","resultStr":"{\"title\":\"Synthesis, characterization and density functional theory of 64Cu based complex for hypoxia imaging\",\"authors\":\"\",\"doi\":\"10.1016/j.jksus.2024.103398\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>An important contributing factor to the growth of aggressive and treatment-resistant tumors is tumor hypoxia. In this investigation, we created a unique tracer, <sup>64</sup>Cu-biacetyl-bis(4-methyl-3-semicarbazone) Complex (<sup>64</sup>Cu-[APSC]<sub>2</sub>), for hypoxia imaging. Numerous spectral and electrochemical analyses were used to characterize the synthesized ligand and its metal complex. The coordination of the metal in the metal complex was also supported by DFT (B3LYP model) calculations. The radiochemical yields and purities of <sup>64</sup>Cu-[APSC]<sub>2</sub> were found to be quantitative, as determined by TLC and HPLC analyses.</p><p>Stability studies in human plasma demonstrated that <sup>64</sup>Cu-[APSC]<sub>2</sub> remained steady for at least four hours while being incubated at 37 °C. MDA-MB-231 cell-line xenografts were placed in nude mice for biodistribution research. The results revealed significant accumulation of the tracer in tumors after 2 h post-injection, which correlated with the redox potential and reactive oxygen species. These findings suggest that <sup>64</sup>Cu-[APSC]<sub>2</sub> shows promising evidence as a theranostic radiopharmaceutical for hypoxic tumors.</p></div>\",\"PeriodicalId\":16205,\"journal\":{\"name\":\"Journal of King Saud University - Science\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":3.7000,\"publicationDate\":\"2024-08-17\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.sciencedirect.com/science/article/pii/S1018364724003100/pdfft?md5=02f2c46b8e2f400879403e987ce9d4b1&pid=1-s2.0-S1018364724003100-main.pdf\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of King Saud University - Science\",\"FirstCategoryId\":\"103\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S1018364724003100\",\"RegionNum\":3,\"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":"Journal of King Saud University - Science","FirstCategoryId":"103","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1018364724003100","RegionNum":3,"RegionCategory":"综合性期刊","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"MULTIDISCIPLINARY SCIENCES","Score":null,"Total":0}
Synthesis, characterization and density functional theory of 64Cu based complex for hypoxia imaging
An important contributing factor to the growth of aggressive and treatment-resistant tumors is tumor hypoxia. In this investigation, we created a unique tracer, 64Cu-biacetyl-bis(4-methyl-3-semicarbazone) Complex (64Cu-[APSC]2), for hypoxia imaging. Numerous spectral and electrochemical analyses were used to characterize the synthesized ligand and its metal complex. The coordination of the metal in the metal complex was also supported by DFT (B3LYP model) calculations. The radiochemical yields and purities of 64Cu-[APSC]2 were found to be quantitative, as determined by TLC and HPLC analyses.
Stability studies in human plasma demonstrated that 64Cu-[APSC]2 remained steady for at least four hours while being incubated at 37 °C. MDA-MB-231 cell-line xenografts were placed in nude mice for biodistribution research. The results revealed significant accumulation of the tracer in tumors after 2 h post-injection, which correlated with the redox potential and reactive oxygen species. These findings suggest that 64Cu-[APSC]2 shows promising evidence as a theranostic radiopharmaceutical for hypoxic tumors.
期刊介绍:
Journal of King Saud University – Science is an official refereed publication of King Saud University and the publishing services is provided by Elsevier. It publishes peer-reviewed research articles in the fields of physics, astronomy, mathematics, statistics, chemistry, biochemistry, earth sciences, life and environmental sciences on the basis of scientific originality and interdisciplinary interest. It is devoted primarily to research papers but short communications, reviews and book reviews are also included. The editorial board and associated editors, composed of prominent scientists from around the world, are representative of the disciplines covered by the journal.