Objective: To explore the method of 99 Tc m direct labeling of angiostatin (AS) and investigate the stability and bioactivity of the 99 Tc m labeled AS in vitro . Methods: AS was extracted, validated, and then labeled...Objective: To explore the method of 99 Tc m direct labeling of angiostatin (AS) and investigate the stability and bioactivity of the 99 Tc m labeled AS in vitro . Methods: AS was extracted, validated, and then labeled with 99 Tc m after having been reduced by 2 ME or SnCl 2. The best labeling condition was screened by cross design. The labeling efficiency was measured by TLC and column chromatography. The stability of 99 Tc m AS was observed and compared when BSA, saline and different molar ratios of Cys∶AS were separately added. The bioactivity of 99 Tc m AS was observed in human umbilical vein endothelial cell (CEV304). Results: The labeling efficiency can reach (97±1 5)% for the 2 ME reducing approach. Its best experimental condition was as follows: AS 100 μg,PB(0 5 mol/L, pH 7 3)1 ml, 2 ME 100 μg, MDP (dissolved in 1 ml saline) 10 μl, and 99 Tc mO 4 - 185 MBq. The labeling efficiency using SnCl 2 reducing method can reach (90±3 0)%. The best experimental procedure was as follows: AS 100 μg,boric acid buffer(0 1 mol/L, pH 9 0)1 ml, 2%SnCl 2 (dissolved in 1 mol/L hydrochloric acid) 20 μl, was added into MDP, which was diluted with 1 ml deoxygenized water, and then 20 μl, 99 Tc mO 4 - 185 MBq was added. The product of 99 Tc m labeled AS was stable in vitro and had the same bioactivity as AS. Conclusion: 99 Tc m direct labeling of AS is simple and efficient. And the bioactivity of 99 Tc m AS has no significant change compared with AS.展开更多
The aim of the present work was to develop radiolabelling fatty acids based on 99Tcm carbonyl chemistry for heart imaging. Undecanoic acids functionalised with iminodiacetatic acid and cysteine were radiolabelled with...The aim of the present work was to develop radiolabelling fatty acids based on 99Tcm carbonyl chemistry for heart imaging. Undecanoic acids functionalised with iminodiacetatic acid and cysteine were radiolabelled with [99Tcm (CO)3(H2O)3]+ intermediates, and their radiolabelling conditions were carefully studied. Biodistribution of 99Tcm (CO)3-CYST FAC11 and 99Tcm (CO)3-IDA FAC11 were observed in normal mice. The results showed that two 99Tcm-labelled compounds had similar profile in terms of high initial radioactivity uptake and rapid washout of radio- tracers in the heart. 99Tcm (CO)3-IDA FAC11 was mainly excreted via hepatobiliary system in contrast to 99Tcm (CO)3-CYST FAC11, which was excreted from urinary system. It may be in part attributed to the more lipophilicity of 99Tcm (CO)3-IDA FAC11 than 99Tcm (CO)3-CYST FAC11.展开更多
文摘Objective: To explore the method of 99 Tc m direct labeling of angiostatin (AS) and investigate the stability and bioactivity of the 99 Tc m labeled AS in vitro . Methods: AS was extracted, validated, and then labeled with 99 Tc m after having been reduced by 2 ME or SnCl 2. The best labeling condition was screened by cross design. The labeling efficiency was measured by TLC and column chromatography. The stability of 99 Tc m AS was observed and compared when BSA, saline and different molar ratios of Cys∶AS were separately added. The bioactivity of 99 Tc m AS was observed in human umbilical vein endothelial cell (CEV304). Results: The labeling efficiency can reach (97±1 5)% for the 2 ME reducing approach. Its best experimental condition was as follows: AS 100 μg,PB(0 5 mol/L, pH 7 3)1 ml, 2 ME 100 μg, MDP (dissolved in 1 ml saline) 10 μl, and 99 Tc mO 4 - 185 MBq. The labeling efficiency using SnCl 2 reducing method can reach (90±3 0)%. The best experimental procedure was as follows: AS 100 μg,boric acid buffer(0 1 mol/L, pH 9 0)1 ml, 2%SnCl 2 (dissolved in 1 mol/L hydrochloric acid) 20 μl, was added into MDP, which was diluted with 1 ml deoxygenized water, and then 20 μl, 99 Tc mO 4 - 185 MBq was added. The product of 99 Tc m labeled AS was stable in vitro and had the same bioactivity as AS. Conclusion: 99 Tc m direct labeling of AS is simple and efficient. And the bioactivity of 99 Tc m AS has no significant change compared with AS.
基金Supported by the Co-ordinated Research Programme of the International Atomic Energy Agency (Contract No: 12469/R0)
文摘The aim of the present work was to develop radiolabelling fatty acids based on 99Tcm carbonyl chemistry for heart imaging. Undecanoic acids functionalised with iminodiacetatic acid and cysteine were radiolabelled with [99Tcm (CO)3(H2O)3]+ intermediates, and their radiolabelling conditions were carefully studied. Biodistribution of 99Tcm (CO)3-CYST FAC11 and 99Tcm (CO)3-IDA FAC11 were observed in normal mice. The results showed that two 99Tcm-labelled compounds had similar profile in terms of high initial radioactivity uptake and rapid washout of radio- tracers in the heart. 99Tcm (CO)3-IDA FAC11 was mainly excreted via hepatobiliary system in contrast to 99Tcm (CO)3-CYST FAC11, which was excreted from urinary system. It may be in part attributed to the more lipophilicity of 99Tcm (CO)3-IDA FAC11 than 99Tcm (CO)3-CYST FAC11.
