Two methods of preparation of the organometallic precursor[188Re(CO)3(H2O)3]+ in aqueous were present in this paper.One method uses gaseous carbon monoxide and amine borane(BH3·NH3) as the reducing agent.In other...Two methods of preparation of the organometallic precursor[188Re(CO)3(H2O)3]+ in aqueous were present in this paper.One method uses gaseous carbon monoxide and amine borane(BH3·NH3) as the reducing agent.In other method,CO(g) is replaced by K2[H3BCO2]that releases carbon monoxide during hydrolysis.Both procedures were prepared as radiolabled kits,affording the desired precursor in yields 85% after 20 min at 75 °C.The routine kit-preparation of the precursor[188Re(CO)3(H2O)3]+ in combination with tailor-made ligand systems enables the organometallic labeling of biomolecules with unprecedented high specific activities.展开更多
Click chemistry was used to study on radiolabeling of 1,2,3-triazole analogs with fac-[188 Re(CO) 3 (H 2 O) 3]+ . CuSO 4 /L-sodium ascorbate was chosen as the catalyst system, three terminal alkynes were conjugated wi...Click chemistry was used to study on radiolabeling of 1,2,3-triazole analogs with fac-[188 Re(CO) 3 (H 2 O) 3]+ . CuSO 4 /L-sodium ascorbate was chosen as the catalyst system, three terminal alkynes were conjugated with two different azides respectively, and then the new prepared fac-[188 Re(CO) 3 (H 2 O) 3]+ was coordinated to the six triazoles. The results showed that the radiochemical yields (RCY) of the conjugation of fac-[188 Re(CO) 3]+ with six triazoles were over 90%, and the triazoles showed high stability in phosphate-buffered saline and new-born calf serum. The preliminary biological evaluation results showed that the new 188 Re-labeling method via click chemistry could have general application in labeling bioactive molecules in high radiochemical yield and high specific activity for further SPECT research.展开更多
Carbon monoxide(CO)gas therapy,a novel anti-tumor technique based on the cytotoxicity from the CO released in situ,has become one of the hot topics in cancer treatment.Since the technique is oxygenindependent,it displ...Carbon monoxide(CO)gas therapy,a novel anti-tumor technique based on the cytotoxicity from the CO released in situ,has become one of the hot topics in cancer treatment.Since the technique is oxygenindependent,it displays promising therapeutic effect for hypoxic tumor where traditional photodynamic therapy shows limited efficacy and insufficient penetration depth.To fully address these limitations of PDT,we propose a synergetic sonodynamic-CO gas releasing strategy for the therapy of hypoxic tumor.In this work,two rhenium(Ⅰ)tricarbonyl complexes with different substituted ligands are investigated for US-triggered ROS generation and CO release.Our results indicated that the electron-donating NMe2-substituted complex(Re-NMe2)exhibits stronger luminescence intensity and generates more singlet oxygen(1O2)than the electron-withdrawing NO2-substituted complex(Re-NO2).In addition,Re-NMe2displays release of CO triggered by US,thus showing high sono-cytotoxicity to tumor cells in-vitro and in-vivo.The strong ROS-generating capability combined with rapid CO-releasing feature from Re-NMe2has made it a powerful tool for the efficient treatment of hypoxic tumor.展开更多
文摘Two methods of preparation of the organometallic precursor[188Re(CO)3(H2O)3]+ in aqueous were present in this paper.One method uses gaseous carbon monoxide and amine borane(BH3·NH3) as the reducing agent.In other method,CO(g) is replaced by K2[H3BCO2]that releases carbon monoxide during hydrolysis.Both procedures were prepared as radiolabled kits,affording the desired precursor in yields 85% after 20 min at 75 °C.The routine kit-preparation of the precursor[188Re(CO)3(H2O)3]+ in combination with tailor-made ligand systems enables the organometallic labeling of biomolecules with unprecedented high specific activities.
基金Supported by National Natural Science Foundation of China(No.10875163)Natural Science Foundation of Guangdong Province(Nos.2009B030108036 and S2012010010685)
文摘Click chemistry was used to study on radiolabeling of 1,2,3-triazole analogs with fac-[188 Re(CO) 3 (H 2 O) 3]+ . CuSO 4 /L-sodium ascorbate was chosen as the catalyst system, three terminal alkynes were conjugated with two different azides respectively, and then the new prepared fac-[188 Re(CO) 3 (H 2 O) 3]+ was coordinated to the six triazoles. The results showed that the radiochemical yields (RCY) of the conjugation of fac-[188 Re(CO) 3]+ with six triazoles were over 90%, and the triazoles showed high stability in phosphate-buffered saline and new-born calf serum. The preliminary biological evaluation results showed that the new 188 Re-labeling method via click chemistry could have general application in labeling bioactive molecules in high radiochemical yield and high specific activity for further SPECT research.
基金the financial support of the National Natural Science Foundation of China(NSFC,No.22077085)the Science and Technology Foundation of Shenzhen(Nos.JCYJ20210324095200002,JCYJ20190808153209537)。
文摘Carbon monoxide(CO)gas therapy,a novel anti-tumor technique based on the cytotoxicity from the CO released in situ,has become one of the hot topics in cancer treatment.Since the technique is oxygenindependent,it displays promising therapeutic effect for hypoxic tumor where traditional photodynamic therapy shows limited efficacy and insufficient penetration depth.To fully address these limitations of PDT,we propose a synergetic sonodynamic-CO gas releasing strategy for the therapy of hypoxic tumor.In this work,two rhenium(Ⅰ)tricarbonyl complexes with different substituted ligands are investigated for US-triggered ROS generation and CO release.Our results indicated that the electron-donating NMe2-substituted complex(Re-NMe2)exhibits stronger luminescence intensity and generates more singlet oxygen(1O2)than the electron-withdrawing NO2-substituted complex(Re-NO2).In addition,Re-NMe2displays release of CO triggered by US,thus showing high sono-cytotoxicity to tumor cells in-vitro and in-vivo.The strong ROS-generating capability combined with rapid CO-releasing feature from Re-NMe2has made it a powerful tool for the efficient treatment of hypoxic tumor.
