To investigate a new kind of tumor tracer ^99mTc-YIGSR developed from a five amino structure （YIGSR） of the Laminin -chain, which can bind to the laminin receptors of tumor specifically, and radiolabeled with MAG3. ...To investigate a new kind of tumor tracer ^99mTc-YIGSR developed from a five amino structure （YIGSR） of the Laminin -chain, which can bind to the laminin receptors of tumor specifically, and radiolabeled with MAG3. （1） Preparation of the ^99mTc-YIGSR probe： with S-Acetly-NH3- MAG3as the chelator and with proper reductants YIGSR was labeled with ^99mTc;（2） Cell culture and viability measurement： EAC was maintained in RPMI 1640 supplemented with calf serum; the trypan blue exclusion was applied to calculate the cell viability; （3） Study of the cell dynamic： The EAC＇s uptake of ^99mTc-YIGSR and ^99mTc-MIBI was observed at 37℃ and 22 ℃, respectively. （1） The labeling efficiencies of ^99mTc-YIGSR and^99mTc-MIBI were （62±3） % and （96±2） %, respectively; （2） The cell viability was declined with time of incubation; （3） At 37 ℃, the EAC＇S uptake of ^99mTc YIGSR and^99mTc-MIBI reached the peak of （43. 16±2.4） % and （24.4±1.8） % at 60 min, respectively; and at 22 ℃, the highest uptake was （26.5±2. 1） % and （9.47±1.9） % at 60 min, respectively. The in vitro study suggests that ^99mTc-YIGSR is superior to ^99mTc-MIBI in cell uptake and has potential value in tumor imaging.展开更多
One novel complex of （）99mTc-salicylidene-tyrosine Schiff base was designed and synthesized, and its biodistribution was investigated. The theoretical simulation revealed that the cis- and trans-（isomers） might co...One novel complex of （）99mTc-salicylidene-tyrosine Schiff base was designed and synthesized, and its biodistribution was investigated. The theoretical simulation revealed that the cis- and trans-（isomers） might co-exist in aqueous solution. A yield higher than 90% under the optimal condition of synthesis was obtained. Good water-solubility was demonstrated. Very little uptakes in muscle, brain, heart and S-180 sarcoma, as well as very rapid blood clearance were revealed in mice. Good accumulation in bone was shown. At 1 h postinjection the bone uptake was 10.9%ID/g. At 3 and 5 h postinjection, bone-to-muscle ratios were 19.0 and 9.3, and bone-to-blood ratios were 31.6 and 28.9, respectively. The result indicates a bone imaging potency of the complex.展开更多
The validity of ^99mTc-YIGSR, a novel receptor radio-tracer, in imaging the Ehrlich ascites tumor was evaluated. YIGSR, a pentapeptide of laminin, was labeled with ^99mTc by using a bifunctional chelator S-Acetly-NH3-...The validity of ^99mTc-YIGSR, a novel receptor radio-tracer, in imaging the Ehrlich ascites tumor was evaluated. YIGSR, a pentapeptide of laminin, was labeled with ^99mTc by using a bifunctional chelator S-Acetly-NH3-MAG3. The MIBI was labeled with ^99mTc by following the kit instruction. The mice of tumor group were intravenously injected 1-2 mCi of ^99mTc-YIGSR or ^99mTc-MIBI via caudal vein, immobilized and imaged under a Gamma camera. The same procedure was performed in mice of blockade group, in which the unlabeled YIGSR was previously injected to block the receptor-recognition sites, and inflammation group serving as control. The reverse-phase Sep-Pak C18 chromatogram was found to have an essentially complete conjugation between YIGSR and S-Acetly-NH3-MAG3. The conjugated YIGSR could be radio-labeled successfully with ^99mTC at room temperature and neutral pH, with a radio-labeling yield of 62%. Without the chelator S-Acetly-NH3-MAG3, the YIGSR was labeled with ^99mTc at an efficiency of 4%. The imagological study revealed obvious tumor accumulation of ^99mTc-YIGSR 15 min after the injection, and the uptake peaked after 3 h with a tumor-to-muscle ratio （T/M） of 11.36. The radio-tracer was slowly cleared up and resulted in a T/M of 3.01 at the 8th h after the injection. As for blocked group, the tumor uptake of radiotracer was significantly lower, with the highest T/M being 4.61 after 3 h and 0.89 after 8 h. The T/M was 3.72 at the 3rd h and 1.29 at the 8th h after the ^99mTc-YIGSR injection in the inflammatory group. The T/M was significantly higher in tumor group than in inflammatory group or control group （P〈0.001）. In the ^99mTc-MIBI group, the T/M was 1.40 at the 3rd h and 0.55 at the 8th h after the injection, which showed a significant difference as compared with ^99mTc-YIGSR （P〈0.001）. It is concluded that YIGSR can be successfully radiolabelled by using S-Acetly-NH3-MAG3. ^99mTc-YIGSR has many advantages in tumor imaging, such as quick and clear visualization, high sensitivity and specificity, and satisfactory target/non-target ratio （N/NT）. It promises to be tumor radio-tracer.展开更多
文摘To investigate a new kind of tumor tracer ^99mTc-YIGSR developed from a five amino structure （YIGSR） of the Laminin -chain, which can bind to the laminin receptors of tumor specifically, and radiolabeled with MAG3. （1） Preparation of the ^99mTc-YIGSR probe： with S-Acetly-NH3- MAG3as the chelator and with proper reductants YIGSR was labeled with ^99mTc;（2） Cell culture and viability measurement： EAC was maintained in RPMI 1640 supplemented with calf serum; the trypan blue exclusion was applied to calculate the cell viability; （3） Study of the cell dynamic： The EAC＇s uptake of ^99mTc-YIGSR and ^99mTc-MIBI was observed at 37℃ and 22 ℃, respectively. （1） The labeling efficiencies of ^99mTc-YIGSR and^99mTc-MIBI were （62±3） % and （96±2） %, respectively; （2） The cell viability was declined with time of incubation; （3） At 37 ℃, the EAC＇S uptake of ^99mTc YIGSR and^99mTc-MIBI reached the peak of （43. 16±2.4） % and （24.4±1.8） % at 60 min, respectively; and at 22 ℃, the highest uptake was （26.5±2. 1） % and （9.47±1.9） % at 60 min, respectively. The in vitro study suggests that ^99mTc-YIGSR is superior to ^99mTc-MIBI in cell uptake and has potential value in tumor imaging.
文摘One novel complex of （）99mTc-salicylidene-tyrosine Schiff base was designed and synthesized, and its biodistribution was investigated. The theoretical simulation revealed that the cis- and trans-（isomers） might co-exist in aqueous solution. A yield higher than 90% under the optimal condition of synthesis was obtained. Good water-solubility was demonstrated. Very little uptakes in muscle, brain, heart and S-180 sarcoma, as well as very rapid blood clearance were revealed in mice. Good accumulation in bone was shown. At 1 h postinjection the bone uptake was 10.9%ID/g. At 3 and 5 h postinjection, bone-to-muscle ratios were 19.0 and 9.3, and bone-to-blood ratios were 31.6 and 28.9, respectively. The result indicates a bone imaging potency of the complex.
基金This project was supported by a grant from the National Natural Sciences Foundation of China (No 30400170)
文摘The validity of ^99mTc-YIGSR, a novel receptor radio-tracer, in imaging the Ehrlich ascites tumor was evaluated. YIGSR, a pentapeptide of laminin, was labeled with ^99mTc by using a bifunctional chelator S-Acetly-NH3-MAG3. The MIBI was labeled with ^99mTc by following the kit instruction. The mice of tumor group were intravenously injected 1-2 mCi of ^99mTc-YIGSR or ^99mTc-MIBI via caudal vein, immobilized and imaged under a Gamma camera. The same procedure was performed in mice of blockade group, in which the unlabeled YIGSR was previously injected to block the receptor-recognition sites, and inflammation group serving as control. The reverse-phase Sep-Pak C18 chromatogram was found to have an essentially complete conjugation between YIGSR and S-Acetly-NH3-MAG3. The conjugated YIGSR could be radio-labeled successfully with ^99mTC at room temperature and neutral pH, with a radio-labeling yield of 62%. Without the chelator S-Acetly-NH3-MAG3, the YIGSR was labeled with ^99mTc at an efficiency of 4%. The imagological study revealed obvious tumor accumulation of ^99mTc-YIGSR 15 min after the injection, and the uptake peaked after 3 h with a tumor-to-muscle ratio （T/M） of 11.36. The radio-tracer was slowly cleared up and resulted in a T/M of 3.01 at the 8th h after the injection. As for blocked group, the tumor uptake of radiotracer was significantly lower, with the highest T/M being 4.61 after 3 h and 0.89 after 8 h. The T/M was 3.72 at the 3rd h and 1.29 at the 8th h after the ^99mTc-YIGSR injection in the inflammatory group. The T/M was significantly higher in tumor group than in inflammatory group or control group （P〈0.001）. In the ^99mTc-MIBI group, the T/M was 1.40 at the 3rd h and 0.55 at the 8th h after the injection, which showed a significant difference as compared with ^99mTc-YIGSR （P〈0.001）. It is concluded that YIGSR can be successfully radiolabelled by using S-Acetly-NH3-MAG3. ^99mTc-YIGSR has many advantages in tumor imaging, such as quick and clear visualization, high sensitivity and specificity, and satisfactory target/non-target ratio （N/NT）. It promises to be tumor radio-tracer.
